literature review literature review -...
TRANSCRIPT
_____________________________________________________________Literature Review
15
LITERATURE REVIEW
2.1 Fast Dissolving Tablet of Anti-Emetic Drugs
Gudas GK et al., (2010), prepared FDT of chlorpromazine. The tablets were prepared
with sodium starch glycolate, crospovidone, croscarmellose, L-HPC, pre-gelatinised
starch. The blends were examined for angle of repose, bulk density, tapped density,
compressibility index and Hausner’s ratio. The tablets were evaluated for hardness,
friability, disintegration time, dissolution rate and drug content.1
Kumar DN et al., (2010), prepared fast dissolving tablets of granisetron HCl using
novel coprocessed superdisintegrants consisting of crospovidone and sodium
starchglycolate in the different ratios (1:1, 1:2 & 1:3). The developed
superdisintegrants were evaluated for angle of repose, carr’s index and Hausner’s
ratio in comparison with physical mixture of superdisintegrants. The angle of repose
of the developed excipients was found to be < 250, carr’s index in the range of 10-
15% and Hausner’s ratio in the range of 1.11-1.14. Short-term stability studies on
promising formulation indicated that there were no significant changes in drug
content and in vitro dispersion time (p<0.05).2
Randale SA et al., (2010), masked the intensely bitter taste of metoclopramide and
formulated a rapid disintegrating tablets of the taste masked drug. Taste masking was
done by complexing metoclopramide with Eudragit in different ratio by the extrusion-
precipitation method. Drug-polymer complexes (DPCs) were tested for drug content,
in vitro taste in simulated salivary fluid, taste evaluation in oral cavity. The complex
having drug-polymer ratio of 1 : 2 shows significant taste masking, confirmed by
drug. Prepared tablets were evaluated for various parameters like tensile strength,
wetting time, water absorption ratio, in vitro disintegration time and disintegration in
oral cavity.3
Goel H et al., (2010), developed a disintegrating system that could be used for
preparing fast disintegrating tablets of highly water soluble drug metoclopramide
without compromising on the mechanical strength. For this purpose disintegrating
system consisting of chitosan-alginate (CTN-ALG) complex (1:1): glycine and chitin
was developed. The results revealed that when CTN-ALG and glycine were mixed in
the ratio of 30:70, the granules exhibited a minimum water sorption time and
maximum effective pore radius. The results suggested incorporation of chitin (5-10%
_____________________________________________________________Literature Review
16
w/w) while preparing FDTs of metoclopramide to enhanced the disintegration without
compromising their mechanical strength.4
Shirshand SB et al., (2010), developed fast disintegrating tablets of proclorperazine
maleate with a view to enhance patient compliance by direct compression method. In
this method, crospovidone and croscarmellose sodium in combination were used as
superdisintigrant.5
Dahima R and Sharma R, (2010), masked the intensely bitter taste of
metoclopramide hydrochloride and to formulate orodispersible tablets of taste mask
drug. Drug-resin complex were optimize by considering parameters such as
optimization of resin concentration, optimization of swelling time, optimization of
stirring time, optimization of pH and optimization of temperature on maximum drug
loading. In vitro drug release study of taste masked tablets showed that more than 85%
of the drug release within 10 min. Thus, results conclusively demonstrated successful
masking of taste and rapid disintegration of the formulated tablets in the oral cavity.6
Mahamuni SB et al., (2009), prepared fast dissolving tablets, which can rapidly
disintegrate in the saliva using taste-masked granules of drugs with a bitter taste,
Promethazine HCl. The taste masked granules were prepared using gastro erodible
Eudragit E-100 by extrusion method. Fast dissolving tablets were prepared using
taste-masked granules and a mixture of excipients containing optimized level of
microcrystalline cellulose and starch. The effect of various superdisintegrants
crospovidone, sodium starch glycolate, croscarmellose sodium was also studied. The
prepared tablets were evaluated for taste, crushing strength, disintegration time and
dissolution.7
Singh SK et al., (2009), prepared fast disintegrating combination tablets of
omeprazole and domperidone by using pertinent disintegrant. The tablets were
prepared using mannitol as diluent and sodium saccharin as sweetening agent along
with three different levels of disintegrant. The superdisintegrant used in this study
were Kollidon CL, Ac-di-sol and SSG. The tablets were evaluated for weight
variation, hardness, friability, wetting time, water absorption ratio, disintegration time
and dissolution study. Using the same excipients, the tablets were prepared by direct
compression and were evaluated in the similar way. Drug content was estimated by
using HPLC. Tablet formulation prepared with 4.76% Ac-di-sol i.e. 10 mg showed
_____________________________________________________________Literature Review
17
disintegration time 15 s. Also the hardness, friability, dissolution rate and assay of
prepared tablets were found to be acceptable according to standard limits.8
Shirsand SB et al., (2009), designed fast disintegrating tablets of prochlorperazine
maleate by direct compression method. Mucilage of plantago ovata and crospovidone
were used as superdisintegrants (2-8% w/w) along with microcrystalline cellulose
(20-60% w/w) and directly compressible mannitol to enhance mouth feel. The
prepared batches of tablets were evaluated for hardness, friability, drug content
uniformity, wetting time, water absorption ratio and in vitro dispersion time.
Formulation prepared by using 8% w/w of plantago ovata mucilage and 60% w/w of
microcrystalline cellulose emerged as the overall best formulation.9
Fars KA, (2007), formulated metoclopramide FDT with sufficient mechanical
strength and fast disintegration from bases prepared by both spray and freeze drying
techniques. Different disintegration accelerators were utilized to prepare the proper
FDT using various superdisintegrants (Ac-di-sol, kollidon and sodium starch
glycolate), a volatilizing solvent (ethanol) and an amino acid (glycine).10
2.2 Fast Dissolving Tablet of Other Drugs
Khemariya P et al., (2010), developed mouth dissolving tablet of meloxicam by
sublimation technology. The tablets were prepared by wet granulation procedure. The
tablets were evaluated for friability, wetting and disintegration time. Sublimation of
camphor from tablets resulted in better tablets as compared to the tablets prepared
from granules that were exposing to vacuum.11
Bhardwaj S et al., (2010), developed fast disintirating tablets of accelofenac. Tablets
were prepared by sodium starch glycolate following by direct compression technique.
The tablets were evaluated for hardness, friability, weight variation, disintegration
time, water absorption ratio and wetting time. All the formulation showed
disintegration time in range of 12.2 to 27.5 s along with rapid in vitro dissolution.12
Abed KK et al., (2010), prepared orodispersible tablets of diazepam using different
types of superdisintegrants (Ac-di-sol, sodium starch glycolate and crospovidone and
different types of subliming agents camphor and ammonium bicarbonate at different
concentrations and two methods of tablets preparations (wet granulation and direct
compression methods). The formulations were evaluated for flow properties, wetting
time, hardness, friability, content uniformity, in vivo disintegration time, release
_____________________________________________________________Literature Review
18
profiles and buccal absorption tests. All formulations showed satisfactory mechanical
strength except formulation which contains camphor and formulation which was
prepared by direct compression method. The results revealed that the tablets
containing crospovidone as a superdisintegrant had good dissolution profile with
shortest disintegration time.13
Chandira RM et al., (2010), prepared FDT of etoricoxib using variety of super
disintegrants like primogel, kollidone, Ac-di-sol, L-HPMC, L-HPC. The prepared
tablets were evaluated for weight variation, hardness, friability, in vitro disintegration
time, wetting time and in vitro dissolution study. Formulation contain L-HPC 8%
shows the lowest disintegration time (44 s) and wetting time (52 s).14
El-Massik MA et al., (2010), utilized a maltodextrin to prepare orally disintegrating
tablets of meclizine. Tablets were prepared by both direct compression and wet
granulation techniques. The effect of maltodextrin concentrations on ODT
characteristics-manifested as hardness and disintegration time-was studied. The effect
of conditioning as a post-compression treatment on ODT characteristics was also
assessed. Maltodextrin-pronounced hardening effect was investigated using
differential scanning calorimetry (DSC) and X-ray analysis.15
Keny RV et al., (2010), developed mouth disintegrating tablets of rizatriptan benzoate
to produce the intended benefit. Mouth dissolving tablets of rizatriptan benzoate were
prepared using superdisintigrant crospovidone, carboxymethylcellulose calcium,
indion 414 and indion 234 using direct compression method. The tablets prepared
were evaluated for thickness, uniformity of weight, content uniformity, hardness,
friability, wetting time, in vivo and in vitro disintegration time, mouth feel, in vitro
drug release and assay by high performance liquid chromatography.16
Parikh BN et al., (2010), developed solid oral formulations of telmisartan which can
be prepared using less complicated and expensive processes and fulfill all prerequisites
for pharmaceutical use, i.e. long-lasting stability of the formulation under different
climatic conditions and sufficient solubility of the active substance for sufficient
gastrointestinal absorption in the slightly acidic and neutral pH region. Preferably, the
formulations should have immediate release characteristics and a dissolution showing
no essential pH dependency within the physiological relevant pH interval of the
gastrointestinal tract. Tablets were evaluated for various parameters like, weight
_____________________________________________________________Literature Review
19
variation, content uniformity, in-vitro dissolution studies were performed using United
States Pharmacopeia (USP) apparatus type II.17
Shid SL et al., (2010), prepared orodispersible tablets of flurbiprofen using various
superdisintegrants such as croscarmellose sodium, sodium starch glycolate,
crospovidone and camphor (as subliming agent) in different ratio and subjected for
evaluation. Results revealed that the tablets of all formulations have acceptable
physical parameters.18
Rajalakshmi G et al., (2010), formulated pheniramine maleate a selective H1 receptor
antagonist into orodispersible tablets. The tablets were prepared by direct compression
method using superdisintegrants like croscarmellose sodium, crospovidone, sodium
starch glycolate, low hydroxylpropyl cellulose and pre-gelatinized starch in different
ratios. The blends examined for various pre compression parameters. Tablets were
evaluated by measuring hardness, friability, content uniformity, weight variation and
drug release pattern.19
Kalia A et al., (2009), prepared mouth dissolving tablets of oxcabazepine using two
different technologies, direct compression method and solid dispersion technology.
Tablets produced by direct compression method contain crospovidone as a
superdisintegrant and aspartame as a sweetener. Solid dispersions of oxcarbazepine
with polyvinylpyrrolidone K-30 and polyethylene glycol 6000 in different weight
ratios were prepared with a view to increase its water solubility. Oxcarbazepine solid
dispersions with polyvinylpyrrolidone K-30 in 1:2 ratios of drug: carrier showed
maximum drug release and hence, compressed along with other excipients into mouth
dissolving tablet. The results compared for both the technologies showed that the
oxcarbazepine tablets prepared using solid dispersion technology was found to have
good technological properties and satisfying and reproducible drug dissolution
profiles.20
Rao NG et al., (2009), developed rapidly disintegrating oral tablets by direct
compression using cogrinding and solid dispersion methods by using chlorthalidone
as a model drug. The tablet formulation containing polyvinyl pyrrolidone K-12 solid
dispersion showed maximum drug release than the chlorthalidone polyvinyl
pyrrolidone K-12 co-grinding method. The prepared tablets were evaluated for
hardness, friability, wetting time, disintegration time and in vitro drug release. DSC
_____________________________________________________________Literature Review
20
and FTIR studies revealed that no chemical interaction between the drug and the
carrier. The stability studies were conducted as per the ICH guidelines and the
formulations were found to be stable with insignificant change in the hardness, and
disintegration time.21
Kumar DN et al., (2009), prepared fast dissolving tablets of fexofenadine by
effervescent method with a view to enhance patient compliance. Three super-
disintegrants viz., crospovidone, croscarmellose sodium and sodium starch glycolate
along with sodium bicarbonate and anhydrous citric acid in different ratios were used
and directly compressible mannitol to enhance mouth feel property of tablets. The
prepared batches of tablets were evaluated for hardness, friability, drug content
uniformity and in vitro dispersion time. Among the three promising formulations, the
formulation containing 8% w/w of crospovidone and mixture of 24% w/w sodium
bicarbonate, 18% w/w of anhydrous citric acid emerged as the best based on the in
vitro drug release characteristics compared to conventional commercial tablet
formulation. Short-term stability studies on the formulations indicated that there were
no significant changes in drug content and in vitro dispersion time (P<0.05).22
Swamy PV et al., (2009), designed orodispersible tablets of pheniramine maleate by
effervescent method. Mixture of sodium bicarbonate and tartaric acid were used along
with superdisintegrants pregelatinized starch, sodium starch glycolate, croscarmellose
sodium and crospovidone. The prepared batches of tablets were evaluated for
hardness, friability, drug content uniformity and in vitro dispersion time. Formulation
containing 4% w/w crospovidone and mixture of sodium bicarbonate and tartaric acid
emerged as the overall best formulation.23
Devireddy SR et al., (2009), formulated orally disintegrating tablets of levocetirizine
dihydrochloride with different superdisintegrants (sodium starch glycollate,
croscarmellose sodium, and crospovidone) using mannitol as a diluent. Tulsion-335,
Indion-204 and poly kyron T-134 cation exchange resins were used as taste-masking
agents. The drug and resin complex was prepared by the kneading method. Ten
formulations were prepared with varying combinations of superdisintegrants and ion-
exchange resins by the wet granulation technique, using polyvinylpyrrolidone K-30 as
the binder. The prepared tablets were evaluated for degree of taste masking, weight
variation, hardness, friability, in vitro and in vivo disintegration time, content
uniformity and water absorption ratio.24
_____________________________________________________________Literature Review
21
Okuda Y et al., (2009), designed a new orally disintegrating tablet that has high
tablet hardness and a fast oral disintegration rate using a new preparation method. To
obtain rapid disintegration granules (RGD), a saccharide, such as trehalose, mannitol,
or lactose, was spray-coated with a suspension of corn starch using a fluidized-bed
granulator. As an additional disintegrant, crospovidone, light anhydrous silicic acid,
or hydroxypropyl starch was also included in the suspension. The RDGs obtained
possessed extremely large surface areas, narrow particle size distribution, and
numerous micro-pores. When tabletting these RDGs, it was found that the RDGs
increased tablet hardness by decreasing plastic deformation and increasing the contact
frequency between granules. In all tablets, a linear relationship was observed between
tablet hardness and oral disintegration time.25
Giri TK and Sa B, (2009), described the formulation of rapidly disintegrating,
diazepam tablets. The tablets were prepared by the conventional wet granulation
method using solid dispersion of the drug with PEG-4000 and/or PEG-6000. A 32
factorial design was used to reduce the number of experimental runs and to obtain
several formulations by which tablets disintegrated within 3 min and released 85% of
the drug in less than 30 min. Several tablet formulations prepared with different
amounts of PEGs in solid dispersion met the above two criteria. However, tablets
which were prepared with PEG-4000 alone at the lowest concentration disintegrated
in the shortest time (32.12 s) and released 85% of the drug most rapidly (11.03 min).26
Gupta A et al., (2009), investigated correlation between disintegration and
dissolution for immediate release tablets containing a high solubility drug and to
identify formulations where disintegration test, instead of the dissolution test, may be
used as the acceptance criteria based on International Conference on Harmonization
Q6A guidelines. A statistical design of experiments was used to study the effect of
filler, binder, disintegrating agent and tablet hardness on the disintegration and
dissolution of verapamil hydrochloride tablets. All formulation variables, i.e., filler,
binder and disintegrating agent were found to influence tablet dissolution and
disintegration, with the filler and disintegrating agent exerting the most significant
influence.27
Jacob S et al., (2009), prepared fast dissolving effervescent tablets were prepared by
the modification of nonreactive liquid based wet granulation technique. Citric acid
was coated with plastic materials such as polyethylene glycol (PEG), which provide a
_____________________________________________________________Literature Review
22
physical barrier to the reaction. The inherent hygroscopic nature of PEG could
decrease the affinity for moisture of effervescent mixtures and can provide a
stabilizing effect. Sodium bicarbonate was blended with sugar alcohol like mannitol,
which would give a protective coating. PEG 1000 melts at body temperature and
thereby does not delay the reaction between the acid source and base.28
Singh J and Singh R, (2009), formulated and optimized orodispersible tablets of
meloxicam using a 22 factorial design for enhanced bioavailability. The tablets were
made by non-aqueous wet granulation using crospovidone and mannitol. A 22 factorial
design was used to investigate the amount of crospovidone and taste masking,
soothening hydrophilic agent (mannitol), as independent variables and disintegration
time as dependent response.29
Madan J et al., (2009), prepared fast dissolving tablets of the nutraceutical, freeze-
dried aloe vera gel by dry granulation method. The tablets were evaluated for crushing
strength, disintegration time, wetting time, friability, drug content and drug release. A
32 full factorial design was applied to investigate the combined effect of two
formulation variables - amounts of microcrystalline cellulose and mannitol. The results
of multiple regression analysis revealed that in order to obtain fast dissolving tablets of
the aloe vera gel, an optimum concentration of mannitol and a higher content of
microcrystalline cellulose should be used.30
Late SG et al., (2009), investigated effects of calcium silicate (disintegration-
promoting agent) and various lubricants on an optimized cyclodextrin-based fast
disintegrating tablets formulation. Effects of moisture treatment were also evaluated at
75, 85 and 95% relative humidities. A two factors at three levels (32) full factorial
design were used to optimize concentrations of calcium silicate and lubricant.
Magnesium stearate, being commonly used lubricant, was used to optimize lubricant
concentration in optimization study. Results of multiple linear regression analysis
revealed that concentration of calcium silicate had no effect; however concentration of
lubricant was found to be important for tablet disintegration and hardness.31
Fujii M et al., (2009), investigated the factors affecting disintegration time in the
mouth (DTM) of rapidly disintegrating tablets. The relation between DTM and
stationary time of upper punch displacement (STP) was examined using a tabletting
process analyzer. Results indicated that the bulk density of mixed excipient powder
_____________________________________________________________Literature Review
23
used for tablet preparation affects both DTM and STP. As the value of bulk density
increased, STP became longer and DTM shorter. The results of a combination of
granules and powder with or without drug showed linear relation between apparent
volume and DTM (r2 = 0.7332). For a DTM less than 60 s, a formulation with a bulk
density greater than 0.5 g/mL should be chosen with a compression force of 5 kN. The
hardness of tablets could be greater than 3 kg if at least one high-compressibility
excipient was used in the formulation.32
Madgulkar et al., (2009), developed novel taste masked mouth-dissolving tablets of
tramadol that overcomes principle drawback of such formulation which was
inadequate mechanical strength. In this work, the bitter taste of tramadol HCl was
masked by forming a complex with an ion exchange resin Tulsion335. The novel
combination of a superdisintegrant and a binder that melts near the body temperature
was used to formulate mechanically strong tablets that showed fast disintegration. A 32
full factorial design and statistical models were applied to optimize the effect of two
factors, i.e., superdisintegrant (crospovidone) and a mouth-melting binder (gelucire
39/01). It was observed that the responses, i.e., disintegration time and percent
friability were affected by both the factors. The statistical models were validated and
can be successfully used to prepare optimized taste masked mouth-dissolving tablets
of tramadol HCl with adequate mechanical strength and rapid disintegration.33
Zade PS et al., (2009), prepared bitterless fast dissolving tablet of tizanidine
hydrochloride using Eudragit E 100 as a taste masking agent. Mass extrusion was the
technique used for preparing taste masked granules. The tablets were prepared with
three superdisintegrants e.g. sodium starch glycolate, crosscarmellose sodium and
crospovidone.34
Chaulang G et al., (2009), prepared solid dispersion of furosemide in SSG in ratios of
1:1 and 1:2 by kneading method. The solid dispersion was characterized FTIR, DSC
and XRD to ascertain if there were any physicochemical interactions between drug
and carrier that could affect dissolution. Tablets containing the solid dispersion were
formulated and their dissolution characteristics compared with commercial furosemide
tablets.35
Furtado S et al., (2008), prepared orodispersible tablets of famotidine using camphor
as subliming agent and sodium starch glycollate together with crosscarmellose sodium
_____________________________________________________________Literature Review
24
as superdisintegrants. The formulations were evaluated for weight variation, hardness
and friability, drug content, wetting time, in vitro and in vivo dispersion time, mouth
feel and in vitro dissolution. The results revealed that the tablets containing subliming
agent had a good dissolution profile.36
Mohapatra A et al., (2008), prepared the tablets of metformin using starch RX1500
and microcrystalline cellulose by direct compression. The tablets showed erosion
behavior rather than disintegration. Then lactose was incorporated which created
pores to cause burst release of drug. But these tablets did not give good mouth feel.
Thus, Pearlitol SD 200 (spray dried mannitol) was used to prepare tablets by wet
granulation (10% polyvinylpyrrolidone in Isopropyl alcohol as binder). The optimized
batches of tablets not only exhibited desired mouth feel but also disintegration time, in
vitro dispersion time, water absorption ratio and in vitro drug release. All the batches
contained 15% starch and 4% of croscarmellose sodium.37
Kuno Y et al., (2008), evaluated the effect of lubricants on the characteristics of
orally disintegrating (OD) tablets manufactured using the phase transition of sugar
alcohol. OD tablets were produced by directly compressing a mixture containing
lactose–xylitol granules, disintegrant, glidant and lubricant and subsequent heating.
The effect of the type of lubricant on the tablet characteristics was evaluated using
magnesium stearate, sodium stearyl fumarate (SSF) and talc as lubricants.38
Seong HJ and Kinam P, (2008), investigated complex formation between drugs and
ion-exchange resins and the effects of coating by various aqueous polymeric
dispersions on the complexes were evaluated for developing new sustained-release
fast-disintegrating tablets. Complexes of ion-exchange resin and dextromethorphan, a
model drug, were prepared using different particle sizes of the resins. Based on drug
loading, release profiles and scanning electron microscopy images, the coated
particles were granulated with suitable tablet excipients and then compressed into the
tablets. As the particle size of resins increased, the drug loading and release rate
decreased due to the reduced effective diffusion coefficient and surface area.39
Patel IM and Patel MM, (2008), developed fast dissolving tablets of etoricoxib.
Granules containing etoricxib, crospovidone, aspartame and menthol prepared by wet
granulation technique. Menthol was sublimed from the granules by exposing the
granules to vacuum. The porous granules were then compressed into tablets.
_____________________________________________________________Literature Review
25
Alternatively, the tablets were prepared and later exposed to vacuum. The tablets were
evaluated for percentage friability and disintegration time. A 32 full factorial design
was applied to investigate the combined effect of two formulation variables; amount
of menthol and crospovidone. The result of multiple regression analysis indicated that
for obtaining for fast dissolving tablet optimum amount of menthol and higher
percentage of crospovidone should be used.40
Masareddy RS et al., (2008), studied two different methods direct compression and
sublimation in formulation of mouth dissolving tablets of clozapine. Total four
formulations using various superdisintegrants and subliming agents were prepared. All
prepared formulations were evaluated for physico-chemical parameters. The
formulations exhibited good disintegration properties with total disintegration time in
the range of 25 to 35 s. Comparative evaluation of two methods showed direct
compression method was a better alternative to sublimation method as its formulations
rapidly disintegrate in oral cavity. Kinetic studies indicated that all the formulations
followed first order release with diffusion mechanism.41
Shen YC et al., (2007), designed an orally disintegrating tablet formulation of
olanzapine to dissolve rapidly upon contact with saliva also described a manic patient
who has an esophageal stricture and chronic pharyngitis, two conditions that impede
the swallowing of medications. She was successfully treated for her mania with this
orally disintegrating formulation.42
Mohammad BJ et al., (2007), prepared carbamazepine solid dispersions by the co-
grinding technique using an insoluble but highly hydrophilic crospovidone and
soluble hydroxypropylmethylcellulose (HPMC) as the carriers. The ratios of drug to
carrier were 1:1, 1:5 and 1:10. Comparison of the dissolution of the drug from its
cogrounds with that of the unground drug, its ground form and the corresponding
physical mixtures revealed considerable differences. The percentage of drug dissolved
during the first 30 min (% D30), for the ground and coground drug was 75-95, whereas
the % D30 for ungrounded drug and its physical mixtures ranged from 41-62.43
Malke S et al., (2007), prepared fast dissolving tablets of oxycarbazepine containing
Avicel PH 102 as a diluent and Ac-di-sol as a superdisintegrant by wet granulation
process. All the formulations were evaluated for characteristics such as hardness,
friability, weight variation, wetting ability, disintegration time and dissolution rate.44
_____________________________________________________________Literature Review
26
Pandey PV and Amarnath R, (2007), investigated performance of three
disintegrants, sodium starch glycolate, croscarmellose sodium and crospovidone using
intragranular and extragranular methods, both in the same quantity of 2% w/w.
Chloroquine phosphate was the drug of choice for the present study. Other excipients
used in the formulation of tablets were lactose monodehydrate, polyvinylpyrolidone
K-30 (PVP K-30), aerosil and magnesium stearate.45
Modi A and Tayade P, (2006), investigated enhancement of the dissolution profile of
valdecoxib using solid dispersion with polyvinylpyrrolidine. They also described the
preparation of fast-dissolving tablets of valdecoxib by using a high amount of
superdisintegrants. A phase solubility method was used to evaluate the effect of
various water-soluble polymers on aqueous solubility of valdecoxib.46
Ahmed IS et al., (2006), developed ketoprofen tablets which dissolve rapidly in the
mouth. The solubility and dissolution rate of poorly water-soluble ketoprofen was
improved by preparing a lyophilized tablet of ketoprofen using freeze-drying
technique.47
Cirri M et al., (2006), developed a tablet formulation based on an effective
flurbiprofen-cyclodextrin system, able to allow a rapid and complete dissolution of
this practically insoluble drug. Three different cyclodextrins were evaluated the parent
beta-cyclodextrin (previously found to be the best partner for the drug among the
natural cyclodextrins) and two amorphous, highly soluble beta-cyclodextrin
derivatives, i.e., methyl-beta-cyclodextrin and hydroxyethyl-beta-cyclodextrin.48
Shishu and Bhatti A, (2006), formulated compressed tablets of diazepam using
microcrystalline cellulose as directly compressible filler and sodium starch glycolate
as superdisintegrant. The taste masked microspheres were prepared using amino alkyl
methacrylate copolymer (Eudragit E-100) by solvent evaporation technique. Taste
evaluation of these microspheres was done by both spectrophotometric taste
evaluation technique and panel testing.49
Takagi H et al., (2005), established a pharmaceutical composition useful for rapid
disintegration, which comprises of a sparingly soluble medicament held on a gel-
forming water-soluble polymer as a solid dispersion.50
Francesco C, (2005), studied the feasibility of preparing fast-dissolving
mucoadhesive microparticulate delivery systems containing amorphous piroxicam to
_____________________________________________________________Literature Review
27
improve drug residence time on sublingual mucosa and drug dissolution rate. The two
new mucoadhesive carriers Eudragit L 100 and Eudragit S 100 sodium salts, both
characterized by a fast intrinsic dissolution rate, have selected.51
Rasetti EC and Grange V, (2005), developed new non-steroidal anti-inflammatory
drugs (NSAID) formulations with faster onset of analgesic action like fast dissolving
tablets. An open-label, randomized, single dose, crossover study with a 18 days
washout period was conducted in 16 healthy volunteers to compare the
pharmacokinetic profile of 20 mg piroxicam freeze-dried tablet (Proxalyoc, Cephalon)
with that of 20 mg piroxicam capsule (Feldene, Pfizer).52
Abdelbary G et al., (2005), assessed the in vitro disintegration profile of rapidly
disintegrating tablets (RDT) was very important in the evaluation and the
development of new formulations of this type. So far neither the US Pharmacopoeia
nor the European Pharmacopoeia has defined a specific disintegration test for RDT;
currently, it was only possible to refer to the tests on dispersible or effervescent
tablets for the evaluation of RDT's disintegration capacity. In the present study, they
have evaluated the disintegration profile of RDT manufactured by main
commercialized technologies, using the texture analyzer .53
Yoshio K et al., (2005), studied the properties of rapidly disintegrating (RD) tablets
manufactured by the phase transition method. RD tablets were produced by
compressing powder containing erythritol (melting point: 122°) and xylitol (melting
point: 93-95°) and then heating at about 93° for 15 min. The hardness and oral
disintegration time of the heated tablets increased with an increase of the xylitol
content.54
Kuchekar BS et al., (2004), in the present work, an attempt was made to formulated
and evaluated mouth dissolving tablets of salbutamol sulphate. Formulations were
prepared by factorial design technique. Different disintegrates were used to formulate
fast dissolving tablets.55
Abu-Izza et al., (2004), formulated tablets which dissolve rapidly in the mouth and
provide an excellent mouth feel. The tablets of the invention comprise a compound,
which melts at about 37o or lower, have a low hardness, high stability and generally
comprise few insoluble disintegrants which may cause a gritty or bulky sensation in
_____________________________________________________________Literature Review
28
the mouth. Convenient and economically feasible processes by which the tablets of
the invention may be produced were also provided.56
Mizumoto T et al., (2004), developed a quick disintegrating tablet in buccal cavity,
comprising a mixture of drug, a sugar (A) and an amorphous sugar (B) and after
forming a tablet, it was humidified and dried. The tablet in the present invention was
to provide stability against moisture at preserved, because the amorphous sugar
changed to the crystalline state in a non-reversible reaction after it was humidified and
dried in a manufacturing process.57
Johnson ES and Lacy J, (2004), formulated a composition for oral administration
comprising a carrier and as active ingredient, an opioid (µ-receptor) agonist, such as
fentanyl or a salt thereof, characterized in that the composition was in the form of a
fast-dispersing dosage form designed to release the active ingredient rapidly in the
oral cavity.58
Luber J and Bunick FJ, (2004), studied an immediate release tablet capable of being
chewed or disintegrated in the oral cavity, which comprises a pharmaceutically active
ingredient and a matrix comprising polyethylene oxide having a weight average
molecular weight of from about 500,000 to about 10,000,000. The tablets possesses
exceptionally good mouth feel and stability.59
Hall M et al., (2004), developed a composition comprising a carrier and an active
ingredient, wherein the carrier was fish gelatin and the composition was a fast-
dispersing dosage form designed to release the active ingredient rapidly on contact
with a fluid. In one embodiment, the composition was designed for oral
administration and releases the active ingredient rapidly in the oral cavity on contact
with saliva. The fish gelatin can be obtained from cold water fish sources and was
preferably the non-gelling, non-hydrolyzed form. A process for preparing such a
composition and a method of using fish gelatin in a fast dispersing dosage form were
also provided.60
Lalla JK and Mamania HM, (2004), studied the inclusion complex of rofecoxib, an
NSAID with β-cyclodextrin using ball milling technique has been prepared and
evaluated using differential scanning calorimetry thermograph. The fast dissolving
tablet composition with 25 mg equivalent rofecoxib showed complete release of
_____________________________________________________________Literature Review
29
rofecoxib in 12 min as compared to 20% drug release from the conventional release
marketed tablets during the same period.61
Shirwaikar AA and Ramesh A, (2004), formulated atenolol as fast disintegrating
tablets using three superdisintegrants, croscarmellose sodium (Ac-di-sol),
crospovidone (Polyplasdone XL) and sodium starch glycolate (Explotab). All the
superdisintegrants were used at different concentration levels to assess their efficiency
and critical concentration level.62
Valleri M et al., (2004), investigated the possibility of developing glyburide tablets,
allowing fast, reproducible and complete drug dissolution, by using drug solid
dispersion in polyethylene glycol. The glyburide dissolution profile from the newly
developed tablets was clearly better than those from various commercial tablets at the
same drug dosage.63
Drooge DJ et al., (2004), studied anomalous dissolution behavior of tablets consisting
of sugar glass dispersions was investigated. The poorly aqueous soluble diazepam was
used as a lipophilic model drug. The release of diazepam and sugar carrier was
determined to study the mechanisms governing dissolution behavior.64
Gohel M et al., (2004), developed mouth dissolving tablets of nimesulide. Granules
containing nimesulide, camphor, crospovidone and lactose were prepared by wet
granulation technique. Camphor was sublimed from the dried granules by exposure to
vacuum. The porous granules were then compressed. Alternatively, tablets were first
prepared and later exposed to vacuum. The tablets were evaluated for percentage
friability, wetting time, and disintegration time. In the investigation, a 32 full factorial
design was used to investigate the joint influence of 2 formulation variables: amount
of camphor and crospovidone.65
Schroeder M and Steffens K, (2003), prepared rapidly disintegrating preparations
containing at least one active pharmaceutical ingredient and at least one excipient by a
simple process in which the predominant part of the complete composition of the
ingredients was granulated, the resulting granules and where appropriate, the
remainder of the ingredients were shaped in the presence of liquid virtually without
pressure, and the resulting shaped articles were dried.66
Zakarian N et al., (2003), invented dispersible tablets containing macrolides as active
ingredients either on their own or associated with other active ingredients, in addition
_____________________________________________________________Literature Review
30
to a method for the production thereof. The dispersible tablets were characterized in
that the macrolide was chosen from a group that was made up of pristinamycin,
azithromycin, roxithromycin, clarithromycin and spiramycin.67
Murray OJ et al., (2003), studied fast dispersing solid dosage forms that preferably
dissolve in the oral cavity within sixty, more preferably within thirty, most preferably
within ten seconds. A novel feature of the solid dosage forms according to the
invention resided in the fact that the composition was essentially free or absolutely
free of mammalian gelatin.68
Laruelle C et al., (2003), established pharmaceutical dosage forms with rapid
disintegration in the mouth and to their process of preparation. The pharmaceutical
dosage forms comprised of at least one active principle dispersed in a mixture of
excipients and were characterized in that the mixture of excipients comprised at least
one weakly compressible diluting agent other than trehalose and a copolymer of 1-
vinylpyrrolidin-2-one and of vinyl acetate.69
Murali M et al., (2002), designed nimodipine tablets with fast in vitro release rates
using nimodipine-modified gum karaya co-grinding mixtures. Co-grinding mixtures of
nimodipine and gum karaya were also prepared to highlight the efficiency of modified
gum karaya.70
El-Arini SK and Clas SD, (2002), studied in vitro disintegration behavior of fast
dissolving system, manufactured by the main commercialized technology, using the
texture analyzer instrument.71
Simone S and Peter CS, (2002), prepared two types of tablets containing coated
ibuprofen as a high dosed model drug. The properties of the water dispersible tablet,
such as porosity, hardness, disintegration time and increase in viscosity after
dispersion, were investigated. The selected tablet formulation, containing 26%
galactomannan and 5% crospovidone, disintegrated before the galactomannan started
to swell. These tablets dispersed in water within 40 s and showed a crushing strength
of 95 N.72
Sunanda H and Bi Y, (2002) developed rapidly disintegrating tablets using both
direct compression and wet compression methods. Tablet properties such as porosity,
tensile strength, wetting time and disintegration time were evaluated and the
formulation and disintegration time of the tablets were elucidated. Formulation and
_____________________________________________________________Literature Review
31
preparation conditions were optimized using polynomial regression or artificial neural
network.73
Khankari et al., (2001), formulated a rapidly dissolving robust dosage form. The
invention was directed to a hard tablet that can be stored, packaged and processed in
bulk. The tablet dissolved rapidly in the mouth of the patient with a minimum of grit.
The tablet was created from an active ingredient mixed into a matrix of no direct
compression filler and a relatively high lubricant content.74
Gilis P and De Conde V, (2000), formulated a fast-dissolving tablets for oral
administration comprising of an active ingredient, a therapeutically effective amount
of galanthamine hydrobromide and a pharmaceutically acceptable carrier,
characterized in that the said carrier comprised a spray-dried mixture of lactose
monohydrate and microcrystalline cellulose as diluents, and a disintegrant; and direct
compression process for preparing such fast dissolving tablets was used.75
2.3 Formulations of Promethazine Theoclate
Argemi A et al., (2010), prepared and characterized of transdermal patches of
promethazine. A mixture of ethylene vinyl acetate and Eudragit ( E100) (80:20, w/w)
was used as a polymeric matrix to obtain a thin membrane. Patches synthesized in this
way were loaded with about 1% promethazine. The drug release and diffusion process
through a membrane have been studied chromatographically using a Franz diffusion
cell. Results have shown that a sustained delivery for more than 24 h was obtained.76
Bhanja S et al., (2010), formulated and evaluated of mucoadhesive buccal tablets
containing promethazine to circumvent the first pass effect and to improve its
bioavailability with reduction in dosing frequency and dose related side effects. The
tablets were prepared by direct compression method. Eight formulations were
developed with varying concentrations of polymers like carbopol 934, polyethylene
oxide and hydroxy propyl methyl cellulose. The tablets were tested for weight
variation, hardness, surface pH, drug content uniformity, swelling index and
bioadhesive strength and in-vitro drug dissolution study. The in vitro release kinetics
studies reveal that all formulations fits well with zero order kinetics followed by
korsmeyer-peppas, first order and then higuchi’s model and the mechanism of drug
release was non-fickian diffusion.77
_____________________________________________________________Literature Review
32
Adhikari SN et al., (2010), developed buccal patches for the delivery of
promethazine using sodium alginate with various hydrophilic polymers like carbopol
934 P, sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose in
various proportions and combinations were fabricated by solvent casting technique.
Various physicomechanical parameters like weight variation, thickness, folding
endurance, drug content, moisture content, moisture absorption, and various ex vivo
mucoadhesion parameters like mucoadhesive strength, force of adhesion and bond
strength were evaluated. An in vitro drug release study was designed and it was
carried out using commercial semipermeable membrane. All these fabricated patches
were sustained for 24 h and obeyed first-order release kinetics.78
Patel RS and Poddar SS, (2009), prepared and evaluated of mucoadhesive buccal
patches for the controlled systemic delivery of promethazine theoclate to avoid first
pass hepatic metabolism. The developed patches were evaluated for the
physicochemical, mechanical and drug release characteristics. The patches showed
desired mechanical and physicochemical properties to withstand environment of oral
cavity. The in vitro release study showed that patches could deliver drug to the oral
mucosa for a period of 7 h. The patches exhibited adequate stability when tested
under accelerated conditions.79
Sekhar K et al., (2008), described buccal permeation of promethazine theoclate and
its transbuccal delivery using mucoadhesive buccal patches. Permeation of drug was
calculated in vitro using porcine buccal membrane and in vivo in healthy humans.
Buccal formulations were developed with hydroxyethylcellulose and evaluated for in
vitro release, moisture absorption, mechanical properties and bioadhesion. Optimized
formulation was subjected for bioavailability studies in healthy human volunteers.80
2.4 Formulations of Prochlorperazine Maleate
Obata Y et al., (2010), developed transdermal drug delivery system for
prochlorperazine (PCPZ) and performed an in vitro skin permeation study with
hairless mouse skin. When the concentration of L-menthol in the hydrogel was
0-0.5%, the PCPZ flux was small; on the other hand, the flux was increased
remarkably when the L-menthol concentration was higher than 1%. The optimal
formulation of hydrogel would be contained 20% isopropanol (IPA), 10% N-methyl-
2-pyrrolidone (NMP), 2% L-menthol and 1% PCPZ. The strong inhibitory effects to
_____________________________________________________________Literature Review
33
stereotyped behavior were observed at 4 h after administration of PCPZ hydrogel, and
the efficacy was sustained for at least 8 h after the administration in mice in vivo.
Thus, it was considered that PCPZ was delivered to brain via systemic circulation by
the administration of PCPZ hydrogel.81
Suresh S et al., (2010), designed fast disintegrating tablets of prochlorperazine
maleate with crospovidone (upto 3% w/w) and croscarmellose sodium (upto 5% w/w)
in combination were used as superdisintegrants. The prepared formulations were
evaluated for hardness, friability, drug content uniformity, dispersion time, wetting
time and water absorption ratio. Among the formulations tested, formulation
containing 5% w/w of croscarmellose sodium and 3% w/w of crospovidone as
superdisintegrant emerged as the overall best based on drug release characteristics in
pH 6.8 phosphate buffer compared to commercial conventional tablet formulation.82
Misao N et al., (2009), developed oral disintegrating film
containing prochlorperazine using microcrystalline cellulose, polyethlene glycol and
hydroxypropylmethyl cellulose as the base materials. The uniformity of dosage units
of the preparation was acceptable according to the criteria of JP15 or USP27. The
film showed an excellent stability at least for 8 weeks when stored at 40° and 75% in
humidity. The dissolution test revealed a rapid disintegration property, in which most
of prochlorperazine dissolved within 2 min after insertion into the medium.83
Finn A et al., (2005), developed buccal dosage form of prochlorperazine and also
conducted two clinical studies to characterize the single-dose and multiple-dose
pharmacokinetics of prochlorperazine and its metabolites after buccal administration.
The results of these studies demonstrate that buccal administration of
prochlorperazine produces plasma concentrations more than twice as high as an oral
tablet, with less than half the variability. In addition to the metabolites, N-desmethyl
prochlorperazine and prochlorperazine sulfoxide, 2 new metabolites, prochlorperazine
7-hydroxide and prochlorperazine sulfoxide 4-N-oxide, were identified and
quantitated. Exposure to metabolites after the buccal prochlorperazine formulation
was approximately half that observed after the oral tablet. Buccal administration of
prochlorperazine, twice daily, should enhance the therapeutic role of prochlorperazine
in preventing and treating nausea and vomiting.84
_____________________________________________________________Literature Review
34
Singh S et al., (1999), prepared and evaluated buccal prochlorperazine (Bukatel) for
its efficacy and tolerability with commonly used metoclopramide. Bukatel was well
tolerated and well rated by both patients and investigators with no adverse effects on
buccal mucosa and causing less drowsiness and sedation. Results indicated that
Bukatel was safe and effective for the treatment of nausea and/or vomiting in patients
suffering from vertiginous disorders and could be safely and strongly recommended
as an alternative to less bioavailable and indiscriminately used oral metoclopramide
tablets.85
Nagarsenker MS et al., (1998), prepared coevaporates of prochlorperazine maleate
(PCPM) by using different polymers by solvent evaporation technique. Ethyl
cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose phthalate were
used in preparation of coevaporates. The coevaporates were characterized by X-ray
diffraction studies, IR spectrophotometry and Differential scanning calorimetry.
Dissolution behavior of coevaporates was studied using buffer solution with pH 1.2
and 6.8 by half change method. A two level, two factor factorial design was used to
quantitate effect of polymers on dissolution profile of PCPM. Dissolution of drug in
pH 6.8 buffer improved with increasing content of hydroxypropyl methylcellulose
phthalate in coevaporates.86
_____________________________________________________________Literature Review
35
REFERENCES
1. Gudas GK, Manasa B, Rajesham VV, Kumar SK, Kumari JP. Formulation and
evaluation of fast dissolving tablets of chlorpromazine hydrochloride. J Pharm
Sci Tech 2010; 2(1): 99-102.
2. Kumar DN, Raju SA, Shirsand SB, Para MS. Design of fast dissolving
granisetron tablets using novel coprocessed superdisintegrants. Int J Pharm Sci
Rev Res 2010; 1(1): 58-62.
3. Randale SA, Dabhi CS, Tekade AR, Belgamwar VS, Gattani SG, Surana SJ.
Rapidly disintegrating tablets containing taste masked metoclopramide
hydrochloride prepared by extrusion-precipitation method. Chem Pharm Bull
2010; 58(4): 443-448.
4. Goel H, Kaur G, Tiwary AK, Rana V. Formulation development of stronger and
quick disintegrating tablets: a crucial effect of chitin. Yakugaku Zasshi 2010;
130(5): 729-735.
5. Shirsand SB, Suresh S, Swamy PV, Para MS, Kumar DN. Formulation design of
fast dissolving tablets using disintegrant blends. Indian J Pharm Sci 2010; 72(1):
130-133.
6. Dhima R, Sharma R. Formulation and in vitro evaluation of taste masked
orodispersible tablet of metoclopramide hydrochloride using indion 204. Int J
Chem Tech Res 2010; 2(1): 447-453.
7. Mahamuni SB, Shahi SR, Shinde NV, Agrawal GR. Formulation and evaluation
of fast dissolving tablets of promethazine hydrochloride with masked bitter
taste. Int J Pharm Res Dev 2009; 7: 1-5.
8. Singh SK, Mishra DN, Jassal R, Soni P. Fast disintegrating combination tablets
of omeprazole and domperidone. Asian J Pharm Clin Res 2009; 2(3): 74-82.
9. Shirsand SB, Suresh S, Para MS, Swamy PV, Kumar DN. Plantago ovata
mucilage in the design of fast disintegrating tablets. Indian J Pharm Sci 2009 ;
71(1): 41-45.
10. Fars KA. Evaluation of spray and freeze dried excipients bases containing
disintegration accelerator for the formulation of metoclopramide orally
disintegrating tablets. Saudi Pharm J 2007; 15: 105-109.
_____________________________________________________________Literature Review
36
11. Khemariya P, Gajbhiye KR, Vaidya VD, Jadon RS, Mishra S, Shukla A,
Bhargava M, Singhai SK, Goswami S. Preparation and evaluation of mouth
dissolving tablets of meloxicam. Int J Drug Deliv 2010; 2: 76-80.
12. Bhardwaj S, Jain V, Jat RC, Mangal A, Jain S. Formulation and evaluation of
fast dissolving tablet of aceclofenac. Int J Drug Deliv 2010; 2: 93-97.
13. Abed KK, Hussein AA, Ghareeb MM, Abdulrasool AA. Formulation and
optimization of orodispersible tablets of diazepam. AAPS Pharm Sci Tech 2010;
11(1): 356-361.
14. Chandira RM, Venkataeswarlu BS, Kumudhavalli MV, Debjitbhowmik, Jayakar
B. Formulation and evaluation of mouth dissolving tablets of the etoricoxib. Pak
J Pharm Sci 2010; 23(2): 178-181.
15. El-Massik MA, Abdallah OY, Ebian AE. Maltodextrin: a novel excipient used
in sugar-based orally disintegrating tablets and phase transition process. AAPS
Pharm Sci Tech. 2010; 11: Article 20.
16. Keny RV, Desouza C, Lourenco CF. Formulation and evaluation of rizatriptan
benzoate mouth disintegrating tablets. Indian J Pharm Sci 2010; 72(1): 79-85.
17. Parikh BN, Patel DM, Patel CN, Dave JB, Gothi GD, Patel TD. Formulation
optimization and evaluation of immediate release tablet of telmisartan. J Global
Pharm Tech 2010; 2(2):79-84.
18. Shid SL, Hiremath SP, Borkar SN, Sawant VA, Shende VS, Tote MV, Birari
RB, Changrani SR. Effect of superdisintegrants in rapidly disintegrating
flurbiprofen sodium orodispersible tablets via direct compression and camphor
sublimation. J Global Pharm Tech 2010; 2(1): 107-117.
19. Rajalakshmi G, Damodharan N, Chudhary A, Reddy DM. Formulation and
evaluation of orodispersible tablets of pheniramine maleate. Chem Tech Res
2010; 2(1): 310-318.
20. Kalia A, Khurana S, Bedi N. Formulation and evaluation of mouth dissolving
tablets of oxcarbazepine. Int J Pharm Pharm Sci 2009; 1(1):17-21.
21. Rao NG, Kota RK, Setty CM, Rao P. Formulation and evaluation of fast
dissolving chlorthalidone tablets. Int J Pharm Pharm Sci 2009; 1(1): 80-87.
_____________________________________________________________Literature Review
37
22. Kumar DN, Raju SA, Shirsand SB, Para MS, Rampure MV. Fast dissolving
tablets of fexofenadine by effervescent method. Indian J Pharm Sci 2009; 71(2):
116–119.
23. Swamy PV, Divate SP, Shirsand SB, Rajendra P. Preparation and evaluation of
orodispersible tablets of pheniramine maleate by effervescent method. Indian J
Pharm Sci 2009; 71(2): 151-154.
24. Devireddy SR, Gonugunta CS, Veerareddy PR. Formulation and evaluation of
taste-masked levocetirizine dihydrochloride orally disintegrating tablets. J
Pharm Sci Technol 2009; 63(6): 521-526.
25. Okuda Y, Irisawa Y, Okimoto K, Osawa T, Yamashita S. A new formulation for
orally disintegrating tablets using a suspension spray-coating method. Int J
Pharm 2009; 382(1-2): 80-87.
26. Giri TK, Sa B. Statistical evaluation of influence of polymers concentration on
disintegration time and diazepam release from quick-disintegrating rapid release
tablet. Yakugaku Zasshi 2009; 129(9): 1069-1075.
27. Gupta A, Hunt RL, Shah RB, Sayeed VA, Khan MA. Disintegration of highly
soluble immediate release tablets: a surrogate for dissolution. AAPS Pharm Sci
Tech 2009; 10(2): 495-459.
28. Jacob S, Shirwaikar A, Nair A. Preparation and evaluation of fast-disintegrating
effervescent tablets of glibenclamide. Drug Dev Ind Pharm 2009; 35(3): 321-
328.
29. Singh J, Singh R. Optimization and formulation of orodispersible tablets of
meloxicam. Trop J of Pharm Res 2009; 8(2):153-159.
30. Madan J, Sharma AK, Singh R. Fast dissolving tablets of aloe vera gel. Trop J
of Pharm Res 2009; 8(1): 63-70.
31. Late SG, Ying Y, Banga AK. Effects of disintegration-promoting agent,
lubricants and moisture treatment on optimized fast disintegrating tablets. Int J
Pharm 2009; 365: 4–11.
32. Fujii M, Yamamoto Y, Kenichi W, Tsukamoto M, Shibata Y, Kondoh M,
Watanabe Y. Effect of powder characteristics on oral tablet disintegration. Int J
Pharm 2009; 365: 116-120.
_____________________________________________________________Literature Review
38
33. Madgulkar, Ashwini R, Bhalekar, Mangesh R, Padalkar, Rahul R. Formulation
design and optimization of novel taste masked mouth-dissolving tablets of
tramadol having adequate mechanical strength. AAPS Pharm Sci Tech 2009;
10(2): 574-581.
34. Zade PS, Kawtikwar PS, Sakarkar DM. Formulation, evaluation and
optimization of fast dissolving tablet containing tizanidine hydrochloride. Int J
Pharm Tech Res 2009; 1(1): 34-42.
35. Chaulang G, Patel P, Hardikar S, Kelkar M, Bhosale A, Bhise S. Formulation
and evaluation of solid dispersions of furosemide in sodium starch glycolate.
Trop J Pharm Res 2009; 8: 43-51.
36. Furtado S, Deveswaran R, Bharath S, Basavaraj BV, Abraham S, Madhavan V.
Development and characterization of orodispersible tablets of famotidine
containing a subliming agent. Trop J Pharm Res 2008; 7(4):1185-1189.
37. Mohapatra A, Parikh RK, Gohel MC. Formulation, development and evaluation
of patient friendly dosage forms of metformin, part-I: orally disintegrating
tablets. Asian J Pharm 2008; 2(3): 167-171.
38. Kuno Y, Masazumi K, Hiroaki N, Etsuo Y, Katsuhide T. Effect of the type of
lubricant on the characteristics of orally disintegrating tablets manufactured
using the phase transition of sugar alcohol. Eur J Pharm Biopharm 2008; 69:
986-992.
39. Seong HJ, Kinam P. Development of sustained release fast-disintegrating tablets
using various polymer-coated ion-exchange resin complexes. Int J Pharm 2008;
353: 195–204.
40. Patel IM, Patel MM. Optimization of fast dissolving etoricoxib tablets prepared
by sublimation technique. Indian J Pharm Sci 2008; 70(1):71-76.
41. Masareddy RS, Kadia RV, Manvi FV. Development of mouth dissolving tablets
of clozapine using two different techniques. Indian J Pharm Sci 2008; 70: 526-
528.
42. Shen YC, Lee MY, Chaucer CH, Chen CH. Orally disintegrating olanzapine for
the treatment of a manic patient with esophageal stricture plus chronic
pharyngitis. Progress Neuro Psycho Biol Psych 2007; 31: 541–542.
_____________________________________________________________Literature Review
39
43. Mohammad BJ, Hadi V, Siavoush D, Mohammad R, Siahi S, Azim BJ, Khosro
A, Mohammad G. Enhancing dissolution rate of carbamazepine via cogrinding
with crospovidone and hydroxypropylmethylcellulose. Iran J Pharm Res 2007; 6
(3): 159-165.
44. Malke S, Shidhaye S, Kadam VJ. Formulation and evaluation of oxcarbazepine
fast dissolving tablets. Indian J Pharm Sci 2007; 69(2): 211-214.
45. Pandey PV, Amarnath R. formulation and evaluation of chlorquine phosphate
tablets using some disintegrants. The Indian Pharmacist 2007; 6(66): 75-79.
46. Modi A, Tayade P. Enhancement of dissolution profile by solid dispersion
(kneading) technique. AAPS Pharm Sci Tech 2006; 7(3): 68.
47. Ahmed IS, Nafadi MM, Fatahalla FA. Formulation of fast-dissolving ketoprofen
tablet using freeze-drying in blisters technique. Drug Dev Ind Pharm 2006;
32(4): 437-442.
48. Cirri M, Valleri M, Mura P, Maestrelli F, Ballerina R. Development of fast-
dissolving tablets of flurbiprofen-cyclodextrin complexes. Drug Dev Ind Pharm
2005; 31(7): 697-707.
49. Shishu, Bhatti A. Fast disintegrating tablets of diazepam. Indian Drugs 2006;
43(8): 643-648.
50. Takagi H, Kajiyama A, Yangisawa M. Rapidly disintegrable pharmaceutical
composition.US Patent 6,899,899; 2005.
51. Francesco C. Fast dissolving mucoadhesive microparticulate delivery system
containing piroxicam. Eur J Pharm Sci 2005; 24: 355-361.
52. Rasetti EC, Grange V. Pharmacokinetic profiles of two tablet formulations of
piroxicam. Int J Pharm 2005; 13:129-34.
53. Abdelbary G, Eouani C, PrinderreP, Joachim J, Reyneir J. Determination of the
in vitro disintegration profile of rapidly disintegrating tablets and correlation
with oral disintegration. Int J Pharm 2005; 292(1-2): 29-41.
54. Yoshio K, Masazumi, K, Shuichi A, Hiroaki N. Evaluation of rapidly
disintegrating tablets manufactured by phase transition of sugar alcohols. J
Control Rel 2005; 105(1-2):16-22.
_____________________________________________________________Literature Review
40
55. Kuchekar BS, Mahajan S, Bandhan AC. Mouth dissolve tablets of sumatriptan.
Indian Drugs 2004; 41(10): 592-598.
56. Abu-Izza, Khawla A, Vincent H, Look JL, Parr GD, Schineller M. Fast
dissolving tablet. US Patent 6,733,781; 2004.
57. Mizumoto T, Masuda Y, Kajiyama A, Yanagisawa M, Nyshadham JR.
Technical Field. US Patent 6,803,054; 2004.
58. Johnson ES, Lacy J. Opioid agonist in a fast dispersing dosage form. US
Patent 6,680,071; 2004.
59. Luber J, Bunick FJ. Soft tablet containing high molecular weight polyethylene
oxide. US Patent 6,753,009; 2004.
60. Hall M, Kearney P, Green R. Fast dispersing dosage forms containing fish
gelatin. US Patent 6,709,669; 2004.
61. Lalla JK, Mamania HM. Fast dissolving rofecoxib tablets. Indian J Pharm Sci
2004; 59(4): 23-26.
62. Shirwaikar AA, Ramesh A. Fast disintegrating tablets of atenolol by dry
granulation method. Indian J Pharm Sci 2004; 66(4): 422-426.
63. Valleri M, Mura P, Maestrelli F, Cirri M, Ballerini R. Development and
evaluation of glyburide fast dissolving tablets using solid dispersion technique.
Drug Dev Ind Pharm 2004; 30(5): 525-534.
64. Drooge DJ, Hinrichs WLJ, Frijlink HW. Anomalous dissolution behaviour of
tablets prepared from sugar glass-based solid dispersions. J Control Rel 2004;
97: 441-452.
65. Gohel M, Patel M, Agrawal R, Amin A, Dave R, Bariya N. Formulation
design and optimization of mouth dissolving tablets of nimesulide using vacuum
drying technique. AAPS Pharm Sci Tech. 2004; 5(3): Article 36.
66. Schroeder M, Steffens K. Method for producing quickly decomposable solid
pharmaceutical preparations. US Patent 6,602,520; 2003.
67. Zakarian N, Laruelle C, Gimet R, Toselli D. Dispersible macrolide compounds
and method for production thereof. US Patent 6,605,301; 2003.
_____________________________________________________________Literature Review
41
68. Murray OJ, Green R, Kearney P, Grother LP. Dispersing dosage forms
essentially free of mammalian gelatin. US Patent 6,509,040; 2003.
69. Laruelle C, Gimet R, Toselli D, Zakarian N, Galenic. Formulations fast
disintegrating in the mouth and method for preparing same. US
Patent 6,669,957; 2003.
70. Murali M, Himasnakar K, Kishore K, Janki RB, Seshasayana A, Ramana MK.
Formulation and evaluation of tablet dosage forms of nimodipine-modified gum
karaya co-grinding mixtures. Indian J Pharm Sci 2002; 23: 256-259.
71. El-Arini SK, Clas SD. Evaluation of disintegration testing of different fast
dissolving tablets using the texture analyzer. Pharm Dev Technol 2002; 7(3):
361-371.
72. Simone S, Peter CS. Fast dispersible ibuprofen tablets. Eur J Pharm Sci 2002;
15(3): 295-305.
73. Sunanda H, Bi Y. Preparation, evaluation and optimization of rapidly
disintegrating tablets. Powder Tech 2002; 122: 188-198.
74. Khankari RK, Hontz J, Chastain SJ, Katzner L. Rapidly dissolving robust
dosage form. US Patent 6,221,392; 2001.
75. Gilis P, De Conde V. Fast dissolving galanthamine hydrobromide tablet. US
Patent 6,099,863; 2000.
76. Argemi A, Ellis JL, Saurina J, Tomasko DL. Development of a polymeric patch
impregnated with promethazine as a model of transdermal sustained release
system. J Pharm Sci 2011; 100(3): 992-1000.
77. Bhanja S, Ellaiah P, Martha SK, Sahu1 PK, Tiwari SP. Formulation and in vitro
evaluation of mucoadhesive buccal tablets of promethazine. Int J Pharm Biomed
Res 2010; 1(4): 129-134.
78. Adhikari SN, Nayak BS, Nayak AK, Mohanty B. Formulation and evaluation of
buccal patches for delivery of promethazine. AAPS PharmSciTech 2010; 11(3):
1038-1044.
79. Patel RS, Poddar SS. Development and characterization of mucoadhesive buccal
patches of promethazine theoclate. Curr Drug Deliv 2009; 6(1): 140-144.
_____________________________________________________________Literature Review
42
80. Sekhar KC, Naidu KV, Vishnu YV, Gannu R, Kishan V, Rao YM. Transbuccal
delivery of promethazine from mucoadhesive buccal patches. Drug Deliv 2008;
15(3): 185-191.
81. Obata Y, Otake Y, Takayama K. Feasibility of transdermal delivery of
prochlorperazine. Biol Pharm Bul 2010; 33(8): 1454-1457.
82. Suresh S, Swamy PV, Para MS, Nagendra KD. Formulation design of fast
disintegrating tablets using disintegrant blends. Indian J Pharm Sci. 2010; 72(1):
130-133.
83. Misao N, Katsuhiko M, Tadao T, Hirotaka Y, Naoki I, Tadashi S. In vitro and in
vivo characteristics of prochlorperazine oral disintegrating film. Int J Pharm
2009; 368: 98-102.
84. Finn A, Collins J, Voyksner R, Lindley C. Bioavailability and metabolism of
prochlorperazine administered via the buccal and oral delivery route. J Clin
Pharmacol 2005; 45(12): 1383-1390.
85. Singh S, Sharma DR, Chaudhary A. Evaluation of prochlorperazine buccal
tablets (Bukatel) and metoclopramide oral tablets in the treatment of acute
emesis. J Indian Med Assoc 1999; 97(8): 346-347.
86. Nagarsenker MS, Garad SD. Physical characterization and optimisation of
dissolution parameters of prochlorperazine maleate coevaporates. Int J Pharm
1998; 160(2): 251-255.