1324608013 bhakti shah
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FORMULATION AND CHARACTERISATION OF ORAL DISPERSIBLE TABLET OF APREPITANT
GUIDED BY:Dr. ZANKHNA SETHASSISTANT PROFESSOR and HEAD OF DEPARTMENTS.K.C.O.P
PRESENTED BY:BHAKTI. M. SHAHM.PHARM SEM IV(PHARMACEUTICS)ENROLLMENT NO. 132460808013S.K.C.O.P
Department of PharmaceuticsSat Kaival College of Pharmacy
1
2
LITERATURE REVIEW
CONTENT
2
1. AIM OF WORK &OBJECTIVE
3.RATIONAL
4. REVEIW OF LITERATURE
5. DRUG PROFILE
2. INTRODUCTION
6. PRE-FPRMUATION STUDY
7. MATERIAL & METHODOLOGY
8.RESULT
9. SUMMARY &CONCLUSION
10.COMPLANCE REPORT
11. REFRENCES
3
AIM & OBJECTIVE OF WORK To formulation and characterization of oral dispersible
tablets of an anti-emetic drug by direct compression. The oral route of drug administration is more common
and convenient where tablets and capsules emerged as popular dosage form but many patients have dysphasia or difficulty in swallowing which is currently affecting 35% general population.
Difficulty in swallowing (Dysphasia) is a common problem of all age groups, especially the elderly and pediatrics because of physiological changes associated with these groups.
4
RATIONALE
Aprepitant is an antiemetic drug which induced nausea and vomiting during the treatment of chemotherapy.
Aprepitant is neurokinin 1 receptor antagonist . Neurokinin 1 receptor available in brain in high concentration on
vomiting center and reflex of its create vomiting. In aprepitant injectable approach are available ,but this approach are
very costly , time consuming, pain full and dose not use for pediatric and geriatric patient.
Oral dispersible method are very easy to prepare ,patient compliance and economic method.
so, compare to injectable method this approach are reliable Hence, the present work is aimed at the formulation and evaluation
of aprepitant oral dispersible tablet
5
What are ODT?Solid dosage form
Rapiddisintegrationon the tongue
A stable, oral dosage formwith the dosing ease of a liquid.
Fast DissolveDosage Form
Oral route ofadministration
6
INTRODUCTION
Oral Dispersible tablet are solid single unit dosage forms that are placed in mouth , allowed to disperse or dissolve in saliva without need of water for frequently release of drug for quick onset of action.
Oral Dispersible tablet disappears rapidly before swallowing.
Disintegrates in 15 sec to 1 min. Also called as fast dissolving tablet, orodispersible tablet,
melt in mouth tablet, repimelts tablet, porous tablet.
[1,2;3}
7
Aprepitant may also be useful in the treatment of cyclic vomiting syndrome & late-stage chemotherapy induced vomiting.
Aprepitant use as a antiemetic, anxiolytic and anti depressant
8
LITERATURE SURVEY
9
LITURATURE REVIEW Sr. no.
Researcher Drug Superdisntegr
antDosage form Journal
1
Deshmukh, A. K. Seth. Tejas K Ghelani, Sharad Kumar,
Hemangi Patel, Sachin Chauhan[1]
Famotidine
Crospovidone,Croscarmelose
sodiumOro dispersible tablet
Indo American Journal Of
Pharmaceutical Research
2Leela Manasa K,
Ramana G and Digpati Roy [2]
Alfuzosin Hydrochloride
Crospovidone,Croscarmelose
sodiumOro dispersible tablet
Journal of Applied
Pharmaceutical Science
3
Milind P Wagh*, Chetan P Yewale, Santosh U Zate, Paresh I Kothawade, Ganesh H Mahale[3]
AceclofenacCrospovidone,Croscarmelose
sodiumOro dispersible tablet
International Journal of
Pharmacy and Pharmaceutical
Sciences
4
*Devendra Revanand Rane, Hemant Narhar Gulve, Vikas Vasant
Patil, Vinod Madhaorao Thakare, Vijay
Raghunath Patil [4]
AlbendazoleCrospovidone,Croscarmelose
sodiumOro dispersible tablet
International Current
Pharmaceutical Journal
10
Researcher Drug Polymers Dosage form Journal
5
B Chandrasekhara Rao, S Vidyadhara ,
RLC Sasidhar and YA Chowdary[14]
Aprepitant
Polyethylene glycol- 4000 Polyethylene glycol- 8000
Solid dispersion
Research Journal of
Pharmaceutical, Biological and
Chemical Sciences
6
P. Durga Bhavani, S. Venkata Ramana Reddy, Laxmidhar
Sahoo, K. Harinadha Baba[15]
AprepitantCarboxy methyl cellulose sodium
Nano suspension
International Journal of Advanced
Pharmaceutics
11
DRUG PROFILE
Structure of Etodolac
Systematic (IUPAC) Name:5-([(2R,3S)-2-((R)-1-[3,5-
bis(trifluoromethyl)phenyl]ethoxy)-3-(4-fluorophenyl)morpholino]methyl)-1H-1,2,4-triazol-
3(2H)-one
Molecular formula C23H21F7N4O3
Molecular weight 534.4gm/mol
Color and appearance Off white crystalline powder
Category Anti –emetic , Neurikinin receptor bloker
BCS class Class –II
Log P 5.22
pka Acidic(9.65)Basic(3.51)
[15]
12
Solubility Insoluble water
Sparingly soluble EthanolSlightly soluble in acetonitrile
Melting point
244-246 °C
Indication Mainly use for the treatment ofAnti emetic
Half life 9 -13 hours
Bioavailability(%) 60 – 65 %
Excretion Urine(5%) and feaces (86%)
Metabolism stomach
UV Absorption 210 nm
13
Mechanism of action Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.
Side effect abdominalpain,changedsenseoftaste,constipation,diarrhea,Dizziness,dry mouth, fatigue,flushing, headache, heartburn, loss of appetite, muscle cramps, upset stomach, vomiting, weakness
14
Mechanism of Aprepitant
15
15
SUMMARY OF PSAR
Sr no.
PSAR Title name
1 US2013/0317016A1 APREPITANT INJECTABLE FORMULATION
2 US8497303B2 METHOD TO ENHANCE AQUEOSUES SOLUBILITY OF POORLY SOLUBLE ACTIVES
3 US 2010/0092564A1 COMPOSITION OF METHOD FOR PREPARING ORALLY DISINTEGRATING TABLTS
4 US 739050B1 ONDASETRON ODT
5 US 2001/0014532A2 COMPRESSED TABLETS FORMULATION
PSAR SUMMARY
16
Looikng of above patent. the patent is available in injectable approach on Aprepiatnt drug. the patent are available other dosage form and field of chemistry. that mean s no patent are available related to my dissertation topic aprepitant are indicated for the nausea and vomiting . there are severable formulation are available of aprepitant like injectable. dosage form oral dosage method are easy to prepare , patent compliance, and economic method . there is no available about oro dispersible tablet of Aprepiatnt that’s why i am selecting this topic
17
Preformulation Study
Formulation of dispersible tablet
Optimization Study
Stability Studies
EXPERIMENTAL WORK
18
Pre-formulation study
Observed value
Standard value(17)
245˚C 244-246˚C
Melting point
19
SR NO. SOLVENT SOLUBILITY
1 Water Insoluble
2 Ethanol Sparingly
3 Aceto nitrile Slightly
4 Di- methyl formide(DMF) Soluble
Solubility of Aprepitant
20
IR spectrogram of Etodolac
Interpretation of FT-IR Spectra
3. FTIR
21Data for Calibration Curve
Calibration Curve of Aprepitant data
Concentration(μg/ml) Abs(nm)±SD
5 0.071±0.016
10 0.194±.0017
15 0.321±0.018
20 0.473±0.018
25 0.614±0.017
30 0.728±0.014
35 0.907±0017
4.Calibration curve
22
0 5 10 15 20 25 30 35 400.000
0.200
0.400
0.600
0.800
1.000
f(x) = 0.026752380952381 x − 0.0427142857142825R² = 0.999542949161075
Aprepitant at 210nm
Ab
so
rba
nc
e
Concentration(μg/ml)
Calibration Curve of Aprepitant
23
Materials &Method
Materials uses
Aprepitant Drug carrier
Polyplasdone XL 10 superdisintegrant
Polyplasodone XL superdintegrant
Polyplasdone INF10 superdisintegratint
Crosscarmelose sod ium superdisintegratint
SSG superdisintegratint
Spray dried lactose filler
Mannitol diluent
Sodium stearyl fumarate lubricant
Straw berry flavour Flavour
Aspatartame Swetner
24
SR NO. EQUIPMENT COMPANIES NAME
1 Electronic weighing balance Metter Toledo PG403-S,Denver Instrument
2 Melting point appratus VMP-1(VEEGO)
3 Hot air oven Hicon,ELE InsrumentPvt.ltd
4 Disintegration appratus Krishna engineering
5 Tablet compression machine Hicon Insrument
6 Dissolution Appratus VDA-6D USPStd.(VEEGO)
7 U.V.Visible Spectrometer
UV-1700(Shimadzu Inc. Japan)
8 Hardness tester Hicon 9 Roche friability Electro Lab
10 Digital bulk density Mitutoyo
11 Vernier calipers Electro lab bulk density tester USP,ETD-1020
25
S1 Aprepitant : SSG ( 1:1)
S2 Aprepitant : SSG (1:3)
S3 Aprepitant : SSG (1:5)
S4 Aprepitant : CROSPOVIDONE (1:1)
S5 Aprepitant : CROSPOVIDONE (1:3)
S6 Aprepitant : CROSPOVIDONE (1:5)
P1 Aprepitant : SSG (1:5)
P2 Aprepitant : CROSPOVIDONE (1:5)
D Pure Drug
Solid dispersion (kneading method)
26
Time (min) Cumulative Drug Release
S1 S2 S3 P1 D5 91.81±1.01 98.04±0.11 87.82±0.13 34.59±0.93 0
10 102.01±0.13 98.04±0.58 91.25±0.95 41.25±0.48 10.57±0.77
20 101.67±0.56 101.0±0.91 95.02±0.78 42.99±0.19 19.78±0.37
30 98.79±0.49 100.32±1.01 94.26±0.79 52.79±0.63 30.11±0.93
45 98.63±0.69 100.32±0.35 95.77±1.17 63.35±0.17 45.59±0.18
60 99.29±1.12 100.32±0.51 91.25±0.95 76.18±0.49 52.68±0.83
IN VITRO DISSOLUTION STUDY OF SOLID DOSAGE FORM
Solid dispersion by kneading method in 6.8 buffer pH solution.
27
Time (min) Cumulative % Drug Release
S4 S5 S6 P2 D
5 97.28±0.27 94.26±0.61 99.55±0.19 24.39±0.79 0
10 101.43±0.89
103.55±1.16
97.34±0.87 39.89±0.19 10.57±0.77
20 99.55±0.61 101.85±1.07
98.85±0.29 41.25±0.48 19.78±0.37
30 98.79±0.94 100.98±0.58
97.33±0.64 49.02±0.87 30.11±0.93
45 97.74±1.06 100.98±0.48
92.62±0.35 55.81±0.58 45.59±0.18
60 98.5±0.73 99.56±0.83 94.12±1.03 64.11±0.49 52.68±0.83
28
0 10 20 30 40 50 60 700
20
40
60
80
100
120
S1S2S3P1D
TIME(min)
%C
DR
Figure no: dissolution profile of solid dispersion S1,S2,S3 in comparision with pure drug and physical mixture(P2) in 6.8 buffer pH.
29
0 10 20 30 40 50 60 700
20
40
60
80
100
120
S4S5S6P2D
Dissolution Profile of solid dispersion
%C
DR
Figure no: dissolution profile of solid dispersion S4,S5,S6 in comparison with pure drug and physical mixture(P2) in 6.8 buffer pH.
30
TRIAL BATCHES
31
INGREDIENTS(mg) A1 A2 A3 A4 A5 A6 A7 A8 A9 A10
Aprepitant 80 80 80 80 80 80 80 80 80 80
Mannitol 68 62 68 62 68 62 68 62 68 62
Spray.dried lactose 44 40 44 40 44 40 44 40 44 40
Polyplasdone XL 20 30 - - - - - - - -
Polyplasdone XL 10 - - 20 30 - - - - - -
Polyplasdone INF 10 - - - - 20 30 - - - -
Cross carmeloss
sodium
- - - - - - 20 30 - -
Sodium starch
glycolate
- - - - - - - - 20 30
Arosil 200 5 5 5 5 5 5 5 5 5 5
Mg.Stearate. 2 2 2 2 2 2 2 2 2 2
Powder Flavoure
(strawberry)
1 1 1 1 1 1 1 1 1 1
Total 220 220 220 220 220 220 220 220 220 220
32
FACTORIAL BATCHES
33
LEVAL
FACT OR
-1 0 +1
POLYPLASDONE
XL10
26mg 30mg 34mg
MANNITOL 50mg 56mg 62mg
32 FACTORIAL DESIGN Independent variables:
Polyplasdone XL10 Mannitol
Dependent variables: Disintegration time(sec) Wetting time(sec)
34
BATCH NO. X1 X2F1 -1 -1
F2 -1 0
F3 -1 +1
F4 0 -1
F5 0 0
F6 0 +1
F7 +1 -1
F8 +1 0
F9 +1 +1
35
INGREDIENT(mg)
F1 F2 F3 F4 F5 F6 F7 F8 F9
Aprepitant 80 80 80 80 80 80 80 80 80
Mannitol 50 56 62 20 56 62 50 56 62
Spray dried lactose
44 40 44 40 44 40 44 40 44
PolyplasdoneXL 10
26 26 26 30 30 30 34 34 34
Aerosil200 5 5 5 5 5 5 5 5 5
Mg.Stearate 2 2 2 2 2 2 2 2 2
Powder flavour (straw berry)
1 1 1 1 1 1 1 1 1
Factorial Design Batches
36
RESULTS AND CONCLUSION
37
Evaluation Parameter for Tablet
Pre-compression parameters
Bulk density
Tapped Density
Carr’s Index
Hausner’s ratio
Angle of repose
Post-compression parameters
Tablet Thickness
Tablet Hardness
Weight variability
Friability
Drug content uniformity
In-Vitro Drug Release Study
38
Post formulation study
Batches Avg. Wt(mg) ±SD
Hardness(kp) ±SD
Thickness(mm ) ±SD
Friability(%w/w)
Drug content%±SD
A1 220.12±0.01 4.91±0.77 3.91±0.05 0.64 98.19±0.01
A2 219.85±.001 4.88±0.79 3.87±0.05 0.69 97.23±0.01
A3 219.82±0.04 4.18±0.96 3.89±0.06 0.79 97.76±0.01
A4 220.05±0.01 4.67±1.08 3.92±0.06 0.94 97.89±0.04
A5 219.78±0.02 4.62±2.97 3.91±0.04 0.89 97.26±0.03
A6A7
219.83±0.01219.95±0.01
4.09±1.104.52±0.85
3.90±0.04 0.97 97.48±0.02
3.63±0.03 0.75 98.02±0.01
A8 220.10±0.01 4.65±0.72 3.85±0.04 0.93 97.65±0.02
A9 219.87±0.02 4.95±0.81 3.73±0.05 0.72 98.15±0.01
A10 219.98±0.01 4.23±0.73 3.78±0.04 0.86
97.59±0.03
##±SD=n=20 ###±SD=n=10
39
Batches Bulk density(gm/cm3)
±SD
Tapped density
(gm/cm3)
±SD
Hausner's ratio
%±SD
Carr’s Index(%)
±SD
Angle of repose
(Ɵ) ±SD
A1 0.51±0.01 0.60±0.01 1.31±0.01 23.71±0.01 23.29±0.01
A2 0.45±0.01 0.52±0.01 1.15±0.01 14.41±0.01 22.47±0.02
A3 0.45±0.03 0.54±0.04 1.18±0.01 15.6±0.02 20.18±0.01
A4 0.49±0.01 0.55±0.01 1.13±0.02 11.76±0.02 21.8±0.03
A5 0.43±0.02 0.51±0.03 1.19±0.01 16.38±0.01 23.89±0.01
A6 0.41±0.01 0.49±0.01 1.18±0.02 15.83±0.01 23.8±0.02
A7 0.42±0.02 0.53±0.01 1.17±0.01 17.23±0.02 22.57±0.02
A8 0.47±0.01 0.57±0.02 1.16±0.02 13.52±0.01 20.42±0.01
A9 0.44±0.01 0.56±0.01 1.21±0.01 18.21±0.01 24.2±0.01
A10 0.46±0.02 0.59±0.03 1.23±0.01 12.29±0.02 21.56±0.03
Preliminary screening batches pre-formulation study
##±SD=n=3
40
Disintegration time(sec) Wetting time(sec)
A1 48.±2 52.±3
A2 43.±1 50±2
A3 37.±3 41±1
A4 36.±4 38±2
A5 38.±5 43±1
A6 40.±2 44±3
A7 61.±3 64±2
A8 63.±1 66±3
A9 56.±2 59±1
A10 58.±1 61±2
41
Bulk densitygm/cm3±SD
Tapped density(gm/cm3) ±SD
Hauser ratio ±SD
Carr's index%±SD
Angle of repose (Ɵ) ±SD
F1 0.20±0.01 0.30±0.01 1.15±0.06 20.7±0.012 26±0.03
F2 0.17±0.01 0.31±0.01 1.19±0.01 22.6±0.016 21±0.01
F3 0.21±0.02 0.35±0.02 1.18±0.03 23±0.020 24.2±0.01
F4 0.19±0.01 0.29±0.01 1.17±0.04 20±0.019 22.3±0.02
F5 0.16±0.02 0.26±0.01 1.15±0.01 18.2±0.016 24.5±0.01
F6 0.22±0.01 0.32±0.02 1.19±0.03 21.5±0.023 23.6±0.01
F7 0.18±0.01 0.34±0.01 1.16±0.02 19.6±0.013 25.1±0.01
F8 0.17±0.02 0.28±0.01 1.17±0.01 20.5±0.015 22±0.01
F9 0.24±0.01 0.33±0.01 1.18±0.01 21±0.014 23±0.02
PRECOMPRESION PARAMETER OF FACTORIAL BATCHES
42
Avg. Wt(mg)±SD
Hardness (kp) ±SD
Thickness(mm) ±SD
Friability(%w/w)
±SD
Drug content
±SDF1 220.20±2.30 4.45±0.71 3.89±0.03 0.398 98.07±0.12
F2 219.80±2.10 4.04±0.79 3.91±0.05 0.430 99.01±0.57
F3 220.50±2.64 3.99±0.84 3.91±0.04 0.532 98.00±0.98
F4 220.40±1.90 3.90±0.75 3.87±0.03 0.521 97.90±0.7
F5 219.80±1.62 4.78±0.21 3.93±0.02 0.562 99.1±.0.22
F6 220.1±1.20 4.33±0.82 3.93±0.03 0.432 99.45±0.14
F7 218.90±1.85 3.52±0.45 3.90±0.02 0.356 99.56±0.28
F8 220.90±1.73 4.30±0.80 3.91±0.01 0.486 98.14±0.91
F9 221.10±1.85 4.31±0.70 3.93±0.02 0.512 99.21±0.45
POST COMPRESION PARAMETER OF FACTORIAL BATCHES
43
Factorial batches Disintegration time(sec)
Wetting time(sec)
F1 35.±2. 36±1
F2 28.±1 30.±1
F3 31.±1. 32±4
F4 34.±2 35±2
F5 27.±1 28.±2
F6 29.±1. 31.±1
F7 32.±2 33.±2.
F8 23.±2. 23±3.
F9 24.±1. 25.±1
44
R square 0.9903
Adjusted R square 0.9741
SOURCE
COEFFICIENT P – value
β0 +27.55 0.0032
β1 -2.40 0.0032
β2 -2.93 0.0018
β12 -1.59 0.0453
β22 +4.69 0.0023
STATITICAL ANALYSIS The response (Y) is measured for each trial. Y = B0 + B1X1 + B2X2 + B12X1X2 + B1
1X12 + B2
2X22
REGRESION OF Y1(DISINTEGRTION TIME)
45
Design-Expert® SoftwareFactor Coding: ActualR1 DT (sec.)
Design points above predicted valueDesign points below predicted value35
23.02
X1 = A: A conc of polyplasdone XL 10X2 = B: B conc. of mannitol
-1
-0.5
0
0.5
1
-1
-0.5
0
0.5
1
22
24
26
28
30
32
34
36
R1
DT
(s
ec
.)
A: A conc of polyplasdone XL 10 (mg)
B: B conc. of mannitol (mg)
Full model equation
Y1= 27.55-2.40X1-2.93X2-1.5X12 +4.69x22
46
R square 0.9743
Adjusted R square 0.9316
SOURCE
Coefficient P value
β0 +28.26000 0.0136
β1 -2.77000 0.0086
β2 -2.52333 0.0112
β12 -0.81000 0.2374
β12 -1.36000 0.1789
β22 +4.87000 0.0082
REGRESION OF Y2 (WETTINGTIME)
47
Design-Expert® SoftwareFactor Coding: ActualR2 WT (sec.)
Design points above predicted valueDesign points below predicted value36.23
23.39
X1 = A: A conc of polyplasdone XL 10X2 = B: B conc. of mannitol
-1
-0.5
0
0.5
1
-1
-0.5
0
0.5
1
22
24
26
28
30
32
34
36
38
R2
WT
(s
ec
.)
A: A conc of polyplasdone XL 10 (mg)
B: B conc. of mannitol (mg)
Full model equationY2= +28.26 -2.77X1-2.93X2 – 0.81X1X2-1.36X1
2+4.87X22
Reduced model equation on the basis of P value Y2= 28.26-2.77X 1-2.52X2 + 4.87X2
2
48
TIME(min) F1 F2 F3 F4 F5 F6 F7 F8 F9
0 0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
0.000± 0.0
5 46.51± 0.65
52.16± 0.25
52.69± 0.65
45.34± 0.41
54.18± 0.99
54.42± 0.56
48.38± 0.75
55.67± 0.55
56.13±0.89
10 60.49± 0.83
62.45± 0.91
63.99± 0.29
65.12± 0.47
65.44± 0.59
65.86± 0.53
66.87± 0.63
67.23±0.45
69.85± 0.31
1574.43± 0.43
74.97± 0.87
76.56± 0.95
77.86± 0.91
78.15± 0.74
79.12± 0.65
79.16± 0.61
80.49± 0.54
82.53±0.78
2082.67± 0.52
83.69± 0.32
85.20± 0.86
85.25± 0.82
86.45± 0.38
86.72± 0.25
86.86± 0.28
89.2 ±
0.55
90.23± 0.67
2589.49± 0.67
91.52± 0.85
93.64± 0.45
94.61± 0.49
95.79± 0.86
96.27± 0.65
97.20± 0.12
98.42±0.64
99.25± 0.3
3090.52 ±
0.8993.21±
0.4296.56±
0.7897.40±
0.2597.98±
0.0298.34±
0.8599.51±
0.4299.99±
0.2599.78±
0.48
In Vitro Drug Release study of Dispersible tablet (F1-F9)In 6.8 buffer pH solution
±SD=n=6
49
0 5 10 15 20 25 30 350
20
40
60
80
100
120
F1F2F3F4F5F6F7F8F9
time(min)
%C
DR
In vitro drug release profile
50
TIME(min) INITIAL AFTER 30 DAYS0 0 05 55.67 55.45
10 67.23 66.7815 80.49 79.86
20 89.2 88.74
25 98.42 98.15
30 99.83 99.76
STABILITY STUDY
0 5 10 15 20 25 30 350
20
40
60
80
100
120
INITIALAFTER 30 DAYS
Time (min)
%C
DR
51
Stability at 40ºc /75%RH
Batch no F8 optimsed Initial After 30 days
Avg.wt 220.0.2 219.98
Hardness 4.30 4.19
Thickness 3.91 3.89
Friaility 0.484 0.462
Disingration time (sec) 20.83(1.23) 21.45(1.86)
Wetting time(sec) 21.56(1.47) 20.63(0.75)
52
SUMMARY AND CONCLUSION
53
Aprepitant is an anti emetic drug which is in used in nausea and vomiting in chemotherapy.
It is a BCS class-II drug so, increases solubility solid dispersion was carried out using kneading method. In 6.8 buffer pH in vitro dissolution was carried out .
For trial batchesA1-A10 were taken respectively. using different superdisintegrant in which after evaluation It was concluded that A4 was optimsed and polyplasdone XL10 is used as superdisintegrant.
For the optimisation of tablet factorial design 32 was carried out. In which independent variable are polyplasdone XL10 and Mannitol . And dependent variable were time and wetting time were carried out. And design was applied.
53
Summary
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the dissolution was carried out for to increases solubility of aprepitant in 6.8 buffer
pH . Stability study was carried out .F8 was optimisable batch stablisable on
evaluation of it.
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CONCLUSION The method of preparation of Oral dispersible tablet of Aprepitant
presented in this research work is simple. All formulation showed good physicochemical properties like % Drug release, hardness, thickness, disintegrating time etc.
The in-vitro release data showed that drug release from the
tablet formulation have been affected by types of superdisintegrant and other exepients
These studies indicated that as the concentration of superdisintegrant increased the tablet was decreased disintegration time and increase wetting time.
It was concluded that batch F8 was found to be excellent among all evaluation parameter..
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57
COMPLAINCE REPORT
SR. NO COMMENT
FULL FILLMENT OF
COMMENT
YES/NO
1
1.Taste masking ----
2.Stability study Yes
3.Experimental design Yes
4.Through research on polyplasdone Yes
5. Statically analysis Yes
58
REFERENCES
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2. Leela Manasa K, “Formulation and Evaluation of Oral disintegrated tablets of Alfuzosin Hydrochloride using super- disintegrants ”, J.A.P.S, 2011 , 161-165.
3. Milind P Wagh,“Formulation And Evaluation of Fast Dispersible Tablets of Aceclofenac Using Different Superdisintegrant.” I.J.P.phrma,sci. 2010,vol 2.
4. Devendra Revanand Rane, “Formulation and evaluation of fast dissolving tablet of albendazole ”, I.C.P.G , 2012, 1(10), 311-316
5. Sudheshnababu Sukhavasi., “Formulation and evaluation of fast dissolving tablets of amlodipine besylate by using Fenugreek seed mucilage and Ocimum basilicum gum Fundamentals and Applications”, I.C.P.F 2012, 1(9), 243-249
6. Dr. M M Gupta, “Formulation And Evaluation Oral Dispersible Tablet of Cinnarizine ”, j.drug.ther. 2013, 3(2), 12-17 .
7. Shailendra Kumar Singh, “Fast Disintegrating Combination Tablets of Omeprazole and Dmperidone” , A.J.pharm.res, Vol.2 2009.
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8. Arshady R, “Microspheres and Microcapsules: A Survey of Manufacturing Techniques 1: Suspension and Cross linking”, Poly. Eng. Sci. 1990, 30(15), 905- 914.
9. Jayadev Patil , “Formulation, Design And Evaluation of Orally Disintegrating Tablets Of Loratadine Using Direct Compression Process ”, int.j.phar.bio.sci 2011.
10. Mahajan Yogesh Y, “Formulation & Evaluation of Orally Disintegrating Tablet of Ondansetron Hydrochloride”, int.J.del.2012
11. Shailesh Sharma, “Formulation of Fast-Dissolving Tablets of Promethazine Theoclate ”, T.j.pharma.res., 2010, 9 (5), 489-497 .
12.K.P.R. Chowdary, “Recent Research on Orodispersible Tablets”, Int.J. Pharm. Res. 2014, 4(1),64-73
13.Dr.R.K.GOYAL..Elementes of Pharmacology. B.S.Shah prakashan Eighteenth edition 2008-2009 . pg no. 484-486.
14.B Chandrasekhara Rao, “Dissolution Enhancement of Poorly Soluble Drug Aprepitant by Hot Melt Extrusion Method Using Hydrophilic Polymer: A Solid Dispersion Technique. ”, Res.J.pharm.bio.sci, 0975-8585.
15. P. Durga Bhavani, “Formulation And Evaluation of Nanosuspension of Aprepitant By Wet Milling Technique” , Int .J.Adv.Pharm, 2013 ,20-29.16.Apripitant associated no. (APRD00100)13thJUN. 2005.www.drugbank.ca/drugs/DB0067317. .Tushar.Hingori. APRIPITANT injectable formulation.USPTO patent US2013/03177016,2013
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18. .David .B.wurn. Method To enhance aquoues solubility of poorly soluble actives. USPTO patant US 8,497,303 B2,2013.19. 18. .David .B.wurn. Method To enhance aquoues solubility of poorly soluble actives. USPTO patant US 8,497,303 B2,201320. Salah.U.ahmed. Ondasetron orally disintegeating tablets.USPTO patant US7,390,503B1200821. Udit badra Compressed tablets formulation.USPTO patant US2001/0014532A2,200122. K.D.Tripathi. 5th edition.Essential of medical Pharmacology. jaypee brother Pg no. 601-60723.Sameer singh “review of solid dispersion” Int jor. Phrm nov.201124.Polyplasdone crospovidone superdisintegrant. ASHLAND .25.Polyplasdone poorly soluble drugs. ASHLAND .26.Efficacy of polyplasdoneINF-10 I direct compressed placebo and acetyl salicylic acid tablet.
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