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Kurmi et al. World Journal of Pharmacy and Pharmaceutical Sciences

COMPREHENSIVE REVIEW ON GASTRORETENTIVE DRUG

DELIVERY SYSTEM: AN APPROACH TO ENHANCE GASTRIC

RETENTION TIME AND ITS FUTURE POTENTIAL

Dipankar Kurmi* and Shaffi Tangri

Department of Pharmaceutics, School of Pharmaceutical Sciences, Sri Guru Ram Rai

University, Patel Nagar, Dehradun, Uttrakhand. Pin – 248001.

ABSTRACT

The main objective of this review is the prolongation of Gastric

retention to improve Bioavailability. Floating drug delivery system is a

method to deliver the drugs that are active locally with a narrow

absorption window in the upper gastrointestinal tract, unstable in the

lower intestinal environment and posses low solubility with higher pH.

The review highlights the prolongation of the GRT, including floating

drug delivery system (FDDS), also known as hydrodynamically

balanced systems (HBS), swelling and expanding systems, polymeric

bioadhesive systems, modified-shape systems, high-density systems,

and other delayed gastric emptying devices. Based on the mechanism

of buoyancy, two distinctly different technologies, i.e. effervescent and

non-effervescent systems, have been include in the development of

FDDS. The parameters of evaluation and implementation of floating medication delivery

systems are also summarised in this paper.

KEYWORD: FDDS, HBS, GRT.

INTRODUCTION

Oral administration of a medicine is likely the least predictable mode of drug delivery, it is

the most used. Oral drugs, such as tablets and capsules, are very inexpensive to produce,

provide a convenient method of drug administration, and lower the risk of total dose errors

when the patient self-administers the dosage form. Oral drugs are typically given in

immediate-release dose forms. The recurrent frequency of medication delivery and charges in

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 7.632

Volume 10, Issue 9, 658-674 Review Article ISSN 2278 – 4357

*Corresponding Author

Dipankar Kurmi

Department of

Pharmaceutics, School of

Pharmaceutical Sciences, Sri

Guru Ram Rai University,

Patel Nagar, Dehradun,

Uttrakhand. Pin – 248001.

Article Received on

25 June 2021,

Revised on 14 July 2021,

Accepted on 04 Aug. 2021,

DOI: 10.20959/wjpps20219-19765


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plasma drug levels are the principal drawbacks of such quick release formulations were

developed.[1]

Due to various virtues, oral controlled drug delivery systems (CDDS) have been

developed for the past several years. The primary goal of the oral CDDS design is to achieve

more predictable and enhanced drug bioavailability, hence enhancing treatment efficiency.[2]

They aid in the reduction of administration frequency, as single doses at regular intervals are

sufficient, resulting in increased patient compliance. Physiological challenges, such as the

difficulty to constrain and position the CDDS within desirable parts of the gastrointestinal

(GI) tract due to fluctuating stomach emptying and motility, obstruct the development

process.[3]

Gastro retentive systems can stay in the gastric region for several hours, considerably

extending the duration medications spend in the stomach. Prolonged stomach retention

improves bioavailability, lowers drug waste, and increases solubility for medicines that are

less soluble in a high pH environment. It can also be used to deliver drugs to the stomach and

proximal small intestines on a local level.

Gastro retention aids in the provision of innovative drugs with novel treatment possibilities

and significant patient advantages. The discovery of new diseases and the resistance to

existing medications necessitated the development of novel therapeutic compounds. As a

result, a large number of chemical entities have been developed, some of which have

complete absorption throughout the gastrointestinal tract (GIT), some of which have

absorption windows (i.e. absorption sites, particularly in the upper part of the small intestine),

and some of which have poor solubility in intestinal media. A particular delivery method is

necessary for medications in the second and third categories, as well as those that require

local action in the stomach. All of the foregoing parameters can be accomplished, and fDDS

can deliver medications to the absorption window effectively for local action and the

treatment of gastric problems such gastro oesophageal reflux.[4]

FDDS are low-density hydrodynamically controlled systems with enough buoyancy to float

above gastric contents and remain buoyant in the stomach for an extended period of time

without altering the gastric emptying rate. With the release of the medication, the stomach's

residual system is emptied. As a result, the stomach residence period is increased, and the

fluctuations in plasma drug concentrations are better controlled. The notion of buoyant

preparation is a straightforward and effective method for increasing the dosage form's

stomach residence period and ensuring long-term medication release. In some cases,


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extending the stomach retention of a delivery method is desirable for achieving increased

therapeutic efficacy of the medicinal ingredient. Medications with improved absorption at the

proximal part of the gastrointestinal system and drugs with limited solubility that breakdown

in alkaline pH, for example, have been proven to be effective in extending gastric retention.

Furthermore, prolong gastric retention of the therapeutic moiety for sustained drug delivery

to the stomach and proximal small intestine in treating certain ulcerative conditions, and thus

offer numerous advantages including improved bioavailability and therapeutic efficacy with

reduced dosing frequency.[5]

Basic Gastrointestinal Tract Physiology

The stomach is separated into three parts: the fundus, the body, and the antrum (pylorus). The

antrum is the major site for mixing motions and works as a pump for gastric emptying via

thrusting actions, while the proximal part comprised of fundus and body acts as a reservoir

for undigested material. Fasting and fed conditions both result in gastric emptying. The

pattern of mobility in the two states, however, is different. An interdigestive series of

electrical events occurs during the fasting state, cycling through the stomach and intestine

every 2 to 3 hours. The interdigestive myloelectric cycle, also known as the migrating

myloelectric cycle (MMC), is divided into four phases.

a) Phase 1: The stomach emptying rate is slow in this phase because the beginning of MMC

is delayed. This period normally lasts 30 to 60 minutes. During this phase, there is no

contraction. The basal phase is another name for it.

b) Phase 2: Bile secretion and mucus discharge occur during this phase, as well as

intermediate contraction. It lasts 20 to 40 minutes. The pre-burst period is another name for it.

As the phase develops, the intensity and frequency gradually rise.

c) Phase 3: During this phase, you will have regular and severe contractions for a brief

period of time. It normally lasts 10 to 20 minutes. This phase is also known as the

housekeeping wave since it tends to empty the stomach's fasting contents. In the fed stage,

large goals remain in the stomach, but during this phase, they are passed down to the small

intestine.

d) Phase 4: occurs between phases III and I of two consecutive cycles and lasts 0 to 5

minutes. The pattern of contractions shifts from a starved to a fed condition after consuming a

mixed meal. This pattern, also known as the digestive motility pattern, consists of continuous

contractions similar to phase II of the fasting state. Food particles are reduced in size (to less


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than 1 mm) and thrown into suspension toward the pylorus as a result of these contractions.

The beginning of MMC is delayed in the fed state, resulting in a slower stomach emptying

rate.[6]

Figure 1: GIT Motility Patter.

Mechanism of Floating Systems

To increase the retention time, many measures have been undertaken to keep the dose form in

the stomach. Floating dosage forms (gas-generating systems and swelling or expanding

systems), mucoadhesive systems, high-density systems, changed shape systems, gastric-

emptying delaying devices, and co-administration of gastric-emptying delaying medications

are examples of these approaches. The floating dose formulations are the most regularly

utilised among these. Floating drug delivery systems (FDDS) have a lower bulk density than

gastric fluids, therefore they float in the stomach for longer periods of time without altering

the gastric emptying rate. While the system is floating on the contents of the stomach, the

medicine is slowly removed from the system at the desired rate. The residual system is

removed from the stomach once the drugs has been released. As a result, GRT is raised, and

variations in plasma drug concentrations are better controlled.

Figure 2: Mechanism of floating system.


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CLASSIFICATION OF FDDS

A. EFFERVESCENT FDDS

1. Gas generating system

2. Volatile liquid containing system

B. NON – EFFERVESCENT FDDS

1. Colloidal gel barrier system

2. Microporous compartment system

3. Floating microsphere

4. Alginate Floating Beads

C. RAFT FORMING SYSTEM

Classification of Floating Drug Delivery Systems

[A] EFFERVESCENT SYSTEM FLOATING DRUG DELIVERY SYSTEM

These are specific drug delivery systems that include a matrix type and a swellable polymer

like methylcellulose or chitosan, as well as effervescent chemicals like sodium bicarbonate,

tartaric acid, and citric acid. These are designed in such a way that when they come into

contact with stomach juice, co2 is released and entrapped in a swelling hydrocolloid, which

provides buoyancy for the dosage form. The distribution technique is based on a swellable

asymmetric triple layer tablet form.[7,9]

I. Gas Generating System

Low-density FDDS is based on the emission of CO2 following oral delivery when it comes

into contact with stomach contents. The materials are designed so that after entering the

stomach, co2 is librated as a result of an interaction with acidic gastric content, and then

contained in the gel-based hydrocolloid. It causes the dose form to rise in the air and retains

its buoyancy. As a result, the specific gravity of the dose form decreases, resulting in a float

on the chime. The co2 generating components are blended in a single layer or multi-layered

form within the tablet matrix to establish a gas generating mechanism in the hydrocolloid

layer, while the medication in the other layer results in a prolonged release effect.[7,10]

II. Volatile liquid containing systems (osmotically controlled drug system)

This is an osmotically regulated floating system that consists of a device that is made up of a

hollow deformable unit in collapsed state. Internally, the housing would be connected to its

deformable unit and divided into a first and second chamber separated by an impermeable,


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pressure-sensitive movable unit. The first chamber normally contains an active drug, while

the second chamber contains a volatile liquid, such as cyclopentane or ether, which is

vaporised at a physiological temperature to create a gas, allowing the drug reservoir to float.

With the help of a bioerodible plug, the unit is evacuated from the stomach, allowing the

vapour to escape.[7,10]

[B] Non – effervescent FDDS

Non-Effervescent Floating Drug Delivery Systems are made up of polysaccharide-based gel-

forming (or) swellable cellulose hydrocolloids, as well as matrix-forming polymers such as

polycarbonate, polymethacrylate, and polystyrene. The standard formulation approach is

combining the medicine with gel-forming hydrocolloids, which swell in contact with gastric

fluid during oral administration and preserve shape and a bulk density barrier. The air trapped

by the swelled polymer gives the dosage forms buoyancy.[7,10]

I. Colloidal gel barrier system (Hydrodynamic balanced systems)

This technique increases the amount of medication that reaches its absorption site in solution

form by extending stomach retention time. It basically consists of a medication mixed with

gel-forming hydrocolloids to keep it buoyant in the stomach. One or more gel-forming

cellulose type hydrocolloids, such as hydroxypropyl methylcellulose (HPMC),

polysaccharides, and matrix-forming polymers, such as polycarbophil, polystyrene, and

polyacrylate, are included in such a system. The hydrocolloid in the system hydrates when it

comes into touch with GI fluid, forming a colloid gel barrier to its surroundings.[7,10]

II. Microporous compartments systems

This approach uses a drug reservoir that is encapsulated inside a microporous compartment

having pores on the top and bottom walls. The drug reservoir compartment's peripheral wall

is entirely sealed to prevent undissolved drug from coming into contact with the stomach

surface. The delivery system floats over the gastric content in the stomach due to the flotation

chamber, which is made up of entrapped air. Gastric fluid penetrates via the aperture to the

extent that it prevents them from being separated from the drug and transports the dissolved

drug across the intestine for absorption.[10]

III. Floating Microsphere/Micro balloons

Micro balloons, commonly known as hollow microspheres, are a very effective buoyant

mechanism. Inside the microsphere, it is made up of a core hollow region. A unique solvent


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Diffusion method for emulsion is used to create hollow microspheres that are loaded with a

medicine in their outer polymer shelf.[9]

IV. Alginate Beads/Floating beads

Calcium alginate spherical beads of about 2.5 mm in diameter have been developed and can

be fabricated by adding sodium alginate solution to an aqueous solution of calcium chloride,

resulting in calcium alginate precipitation. The beads are then separated, snap-frozen in liquid

nitrogen, and packaged. After being freeze-dried at 400°C for 24 hours, a porous system is

formed. This constructed system would maintain a floating force for more than 12 hours, and

these floating beads have a residence time of more than 5.5 hours.[10]

[C] Raft-forming systems

For the administration of antacids and drugs for gastro infection and disorders, raft-forming

systems are receiving a lot of interest. When a gel-forming solution comes into contact with

gastric fluid, it expands and creates a viscous cohesive gel encased in co2 bubbles,

establishing a raft layer on top of the gastric fluid, allowing the medicine to be released

slowly in the stomach.[10]

Advantages of Floating Drug Delivery System

1. Floating dosage forms, such as tablets or capsules, will continue in the solution for a long

period, if the intestine has an alkaline pH.

2. Drugs that have a local action in the stomach benefit from FDDS. eg: Antacids

3. FDDS dosage forms are beneficial in cases of diarrhoea and vigorous intestinal

movement because they retain the medicine in a floating state in the stomach, allowing

for a greater reaction.

4. When an acidic chemical, such as aspirin, comes into touch with the stomach wall, it

produces irritation, hence FDDS formulations may be effective for the administration of

aspirin and other related medications.

5. For medications that are absorbed through the stomach, the FDDS are beneficial.

Eg: Ferrous salts, antacids.

6. The drug concentration variation over a critical concentration is reduced by FDDS, which

improves the pharmacological effects and therapeutic results.

7. The retention of pharmaceuticals in GRDF at the stomach reduces the amount of drugs

that reach the colon and hence inhibits drug breakdown in the colon.


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8. A floating dose form is a widely used method for medications with limited absorption

sites in the upper small intestine.[11]

Disadvantages of Floating Drug Delivery System

1. For drug delivery to float and perform efficiently, these systems require a high volume of

fluid in the stomach.

2. Not recommended for medications that have a difficulty with solubility or stability in the

GI tract.

3. Nifedipine (calcium channel blocker), which is well absorbed throughout the GIT and

passes first-pass metabolism, may not be the best choice.

4. Drugs that irritate the stomach mucosa are also undesirable and inappropriate.

5. Drugs that are unstable in the stomach's acidic environment are not ideal candidates for

incorporation into systems.

6. A full glass of water should be used to provide the dose form (200- 250 ml).

7. These systems do not provide considerable benefits over traditional drug dose forms that

are absorbed through the gastrointestinal tract.[12]

Drugs that could be used in floating medication delivery systems

In general, molecules that have low colonic absorption but have superior absorption

capabilities at the upper gastrointestinal tract are good candidates for Controlled-GRDF, a

component of the GIT.

Riboflavin and levodopa, for example, have a narrow absorption window in the GI tract.

Calcium supplement, chlordiazepoxide, and cinnarizine, for example, are absorbed

mostly from the stomach and upper GI tract.

H2 receptor antagonists, antacids, and misoprostol are examples of drugs that operate

locally in the stomach.

Ranitidine HCL and metronidazole are examples of drugs that degrade in the gut.

Amoxicillin trihydrate, for example, is a drug that disrupts typical colonic

microorganisms.[13,14]

Factors Affecting Floating Drug Delivery System

1. Density of Dosage Form

Floating is a result of dose from buoyancy, which is affected by density. The dosage form's

density should be less than the contents of the stomach (1.004gm/ml). Floating feature

necessitates a density of less than 1.0 gm/cm3.[15]

As a result, dose forms with a lower density


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than the gastric contents might float to the top of the stomach, whereas high density systems

sink to the bottom.

2. Shape and size of dosage form

Other factors that influence stomach retention include the shape and size of the dose form.

When comparing dosage form units with a diameter of more than 7.5 mm to those with a

diameter of 9.9 mm, it has been found that those with a diameter of more than 7.5 mm boost

GRT. When compared to other shapes, the dosage form with tetrahedron and ring shape

devises with a flexural modulus of 48 and 22.5 kilo pounds per square inch (KSI) is claimed

to have improved GIT retention for 90 to 100 percent retention at 24 hours.[16]

3. Food Intake and its Nature

Food intake, viscosity and volume of food, caloric value, and feeding frequency all have a

significant impact on dosage form gastric retention. The gastric retention time (GRT) of the

dose form is affected by the presence or absence of food in the gastrointestinal tract (GIT).

Feeding indigestible polymers or fatty acid salts might cause changes un the digestive system.

The shift in the stomach's motility pattern to a fed state results in a slower gastric emptying

rate and longer medication release.

4. Caloric content

With a high-protein, high-fat meal, the gastric retention time (GRT) can be enhanced by 4 to

10 hours.[17]

When floating for several days in a row, the time spent floating can climb by

almost 400 minutes. Due to the low frequency of migrating myoelectric complexes, multiple

meals are supplied rather than a single meal (MMC).

5. Effect of gender, posture and age

Females' stomach emptying rates are slower than males'. In terms of the mean stomach

retention time, the effect of posture does not make a significant difference (GRT). Because

elderly people, particularly those over the age of 70, have a much longer GRT, stomach

emptying is retarded. Drug delivery is also affected by diseases such as diabetes and Crohn's

disease.

6. Fed or Unfed State

The gastric motility is characterised by periods of intense motor activity, or migrating

myoelectric complexes (MMC), that occur every 1.5 to 2 hours during fasting conditions. The


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MMC removes undigested material from the stomach, so if the formulation is given at the

same time as the MMC, the unit's GRT should be quite brief. MMC is delayed in the fed

condition, and GRT is significantly longer.[18]

7. Concomitant drug administration

Floating time can be affected by anticholinergics like atropine and propantheline, opiates like

codeine, and prokinetic drugs like metoclopramide and cisapride.[19]

8. Single or multiple unit formulation

When compared to single unit dosage forms, multiple unit formulations are more predictable

due to unit failure, allow co-administration of units with distinct release profiles or containing

incompatible chemicals, and provide a higher margin of safety against dosage form failure.

Application of Floating Drug Delivery

1. Enhanced Bioavailability

In comparison to the administration of non-GRDF CR polymeric formulations, riboflavin

CR-GRDF has a much higher bioavailability. There are various processes that function in

concert to determine the magnitude of drug absorption, including drug absorption and transit

in the gastrointestinal system.

2. Enhanced first-pass Biotransformation

The pre-systemic metabolism of the tested compound may be significantly increased when

the drug is presented to the metabolic enzymes (cyto chrome P450, in particular CYP3A4) in

a sustained manner rather than by a bolus input, similar to the increased efficacy of active

transporters with capacity limited activity.

3. Sustained drug delivery/reduced frequency of dosing

For medications with a short biological half-life, persistent and slow input from CR-GRDF

may cause a pharmacokinetic flip-flop, allowing for lower dose frequency. This characteristic

has been linked to increased patient compliance, which enhances therapy.

4. Targeted therapy for local ailments in the upper GIT

Longer and more consistent drug administration from GRDF to the stomach may be

beneficial for local therapy in the stomach and small intestine. Therapeutic medication

concentrations can be achieved locally with this method of administration, but systemic

amounts are negligible after drug absorption and dispersion.


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5. Reduced Fluctuations of drug concentration

In comparison to immediate release dosage forms, continuous input of the drug after

CRGRDF treatment creates blood drug concentrations within a tighter range. As a

result, pharmacological impact variations are reduced, and concentration-dependent adverse

effects associated with peak concentrations can be avoided. This is especially important for

medications with a limited therapeutic index24.

6. Minimization of fluctuations in drug concentration

It allows for a degree of selectivity in the pharmacological response evoked by medicines that

activate various types of receptors at varying doses.

7. Reduced counter-activity of the body

In many circumstances, when a pharmaceutical response interferes with natural physiologic

processes, the body responds with a rebound activity that reduces drug activity.Slowing the

drug's entry into the body has been proven to reduce counter-activity, resulting in greater

pharmacological efficacy.

8. Extended time over critical (effective ) concentration

The clinical response is not connected with peak concentration for certain medications having

non-concentration dependent pharmacodynamics, such as beta lactam antibiotics, but rather

with the duration of time over a key therapeutic concentration. The sustained route of

administration allows for a longer period of time over a critical concentration, which

increases pharmacological effects and clinical results.

9. Minimized adverse activity at the colon

The amount of medicine that enters the colon is reduced when the drug is retained in the

GRDF at the stomach. As a result, the drug's unwanted effects in the colon may be avoided.

This pharmacodynamic aspect justifies GRDF formulation for beta-lactam antibiotics that are

only absorbed from the small intestine and whose presence in the colon causes

microorganism resistance to develop.

10. Site specific drug delivery

A floating dose form is a viable option, particularly for medicines with few absorption sites in

the upper small intestine. The controlled, gradual distribution of the medicine to the stomach

ensures enough local therapeutic levels while limiting the drug's systemic exposure. The


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drug's adverse effects in the blood circulation are reduced as a result. Furthermore, a site

guided delivery system's longer stomach availability may lower dose frequency.[20,21]

Evaluation of Floating Drug Delivery System

Shape of Tablets

The shape consistency of compressed tablets designed for FDDS is determined by looking at

them under a magnifying lens.

Tablet Dimensions

The thickness and diameter of FDDS tablets are measured using calibrated Vernier callipers,

much like regular tablets, according to official compendia. Three tablets of each formulation

are chosen at random and their thicknesses are measured separately.

Hardness of the Tablet

With the use of a Monsanto type hardness tester, randomly picked twenty tablets from each

batch of formulations should be utilised to determine hardness.

Weight Variation

Twenty pills are chosen at random and carefully weighed, with the average weight of each

tablet computed. The individual weight divergence from the average weight is then

determined.

Thickness of the Tablet

For each batch, the crown to crown thickness of ten tablets is measured with slide callipers.

Measurement of Floating Capacity

Three separate tablets are placed in a 400 mL flask containing 0.1(N) HCL solutions. The

time it takes for each tablet to go from the bottom to the top of the flask (floating lag time)

and the time it takes for tablets to float on the water surface continuously (duration of

floating) are then calculated in minutes. Following that, the sample mean and standard

deviation are determined.

Density of the formulation

The apparent densities of the tablets are estimated in triplicate using their volumes and

masses. Using the mathematical equation for a cylinder, the volume V of the cylindrical


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tablets is estimated from their height h and radius r (both measured using a micrometre

gauge). (V = A x r2 x h).

Drug content in Tablets

Ten tablets are chosen at random from each batch and transferred to a 100 mL volumetric

flask containing 0.1(N) HCL. Stir and let away for 2 hours before transferring 1 ml from the

volumetric flask to the test tube. After that, the samples are filtered, diluted appropriately, and

spectrophotometrically evaluated at a suitable wavelength.[22,23]

In Vitro Dissolution study

Inside the dissolving vessel, the tablet was inserted. 5 ml of sample is extracted at 1 hour, 2

hours, 3 hours, 4 hours, 5 hours, 6 hours, 8 hours, 10 hours, and 12 hours, or at any additional

time intervals as needed. By adjusting the volume of dissolving fluid to 900 ml. After each

sampling, replace the dissolving media with a fresh 5 ml. The investigations were carried out

with "n" tablets, and the mean values were plotted against time. Each sample is examined

using a UV visible spectrophotometer at maximum wavelength against a reagent blank, and

the corresponding concentration is calculated from the calibration curve.[24]

Buoyancy/Floating test

The time between the dosage form's introduction and its buoyancy on the simulated gastric

fluid, as well as the duration the dosage form remains buoyant, are both measured. The

amount of time it takes for a dosage form to emerge on the surface of a medium is known as

floating lag time (FLT) or buoyancy lag time (BLT), and the entire amount of time it takes

for the dosage form to remain buoyant is known as total floating time (TFT).

Swelling Index

The weight gain or water intake of a dose form is used to determine its swelling behaviour.

The growth in tablet diameter and/or thickness over time could be used to quantify the

dimensional changes. Water uptake can be calculated as a percentage weight gain.[25]

INNOVATIVE TECHNOLOGIES FOR FDDS

1. OleotecTM

and SoctecTM

Skyepharma developed the OleotecTM

and SoctecTM

gastro-retentive capsule technologies.

OleotacTM

technology is designed for drugs with large therapeutic dosages, but it is not

suitable for standard dosage forms. This method is used to produce drugs that have an effect


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largely in the proximal section of the gastro intestinal tract. The Oleotec system is a gel in the

shape of a stick pack that produces a continuous coating on the stomach's walls. The

SoctecTM

system is developed for medications that should be given as a controlled release and

absorbed in the proximal section of the colon in order to increase drug bioavailability. Soctec

is a drug-filled elongated capsule. It can be utilised with a variety of medications that have a

small absorption window and are absorbed best in the proximal gut. It can also help to

increase the bioavailability of medications that are destroyed by the GIT's distal pH.

2. According PillTM

Technology

This is a biodegradable polymer-based gastro adhesive formulation with a wide range of

applications. It's a multi-layer, planar construction that's been folded into an accordion shape

to fit into a standard-size capsule. When the capsule reaches the stomach, it dissolves, the

folded pill unfolds, and the effect lasts up to 12 hours in the stomach. The pill releases the

drug in a controlled manner towards the proximal part of the GI tract while in the stomach,

resulting in a prolonged and continuous absorption phase of the drug in the upper part of the

GI tract, resulting in improved efficacy and safety profiling, as well as reduced frequency

dosing. The Accordion pillTM

retention mechanism is not required for medication release. The

Accordion PillTM

is destroyed in the intestinal media after it is discharged from the stomach.

For this system, drugs from BCS Class II and BCS Class IV are preferred.

3. Gastro Retentive Innovative Device (GRID)

The Gastro Retentive Innovative Device (GRID) is a once-daily device for medications that

would ordinarily only be absorbed in the stomach or small intestine. The GRID system is

designed to keep the medicine in the stomach for up to eight hours. Longer stomach retention

promotes medication absorption. The tablet provides a mix of immediate and prolonged

medication release characteristics, and the fact that it is only taken once a day helps patient

compliance. This novel approach consists of a dosage form with numerous specialised

coatings. When the dosage form is swallowed with food, it floats on the gastrointestinal

contents instantly. The coatings on GRID are activated by gastrointestinal fluid, which causes

enlargement of eight to eleven times its original volume. As a result, plasma concentrations

of medicines are maintained in the therapeutic range for a longer period of time, allowing this

dosage form to be administered as a "once-a-day" medication. Using this new dosage form,

specific medication release profiles can be adjusted to create a combination of instant and


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gradual release. Retaining the dosage form near the absorption site may aid in lowering the

dose and hence the side effects.

4. Multiple Polymers Hydrophillic Matrix Technology

A sustained gastro medication delivery device is based on multiple polymer hydrophilic

matrix technology. Cetapin XR is a Sanofi-patented formulation of this system that contains

Metformin XR as a medication to achieve Metformin hydrochloride prolonged release. Non-

ionic and ionic hydrophilic polymers are combined to create the polymers. The medication is

released from the matrix pore by dissolving the drug and allowing it to diffuse through the gel

matrix in a sustained way. With good optimum absorption, minimal discomfort, enhanced

plasma drug levels, and good bioavailability, this method produces consistent and repeatable

outcomes.

5. Acuform Technology

Depomed's Acuform is a patented formulation. It's a polymer-based technique designed to

improve medicine delivery in the gastrointestinal tract. This method allows for precise drug

administration to the proximal (upper) GIT, which is the preferred absorption site for many

oral medications. This method is especially useful for medications that are absorbed in the

upper gastrointestinal tract. It's also useful for medications that aren't water soluble, irritate

the mucosa of the small intestine, or aren't safe in the distal GIT, and it's more successful

when plasma drug levels fluctuate less.

6. Ga3strointestinal permeation Enhancement Technology

Merrion Pharmaceuticals created Gastrointestinal Permeation Enhancement Technology

(GIPET), a revolutionary method that allows medications that can only be injected

parenterally to now be given orally (injectable). To be transformed into oral solid forms, such

as tablets or capsules, and to improve oral drug absorption. Gastrointestinal Permeation

Enhancement Technology employs specially formulated oral absorption enhancers that

activate micelle production during medication transport, resulting in increased absorption

with high repeatability and a low risk profile.[26]

CONCLUSION

New and essential treatment possibilities will emerge as a result of dosage formulations with

a prolonged GRT. They will greatly lengthen the amount of time that medications can be

released, allowing dosing intervals to be extended and patient compliance to rise above that


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of conventional CRDFs. Many "once-a-day" formulations will be replaced with medications

that have a 24-hour release and absorption phase. Moreover, FDDS will substantially

improve the pharmacotherapy of the stomach itself by allowing for local drug release,

resulting in high drug concentrations at the gastric mucosa that last for a long time. Finally,

medications with the "absorption window" will be carried by FDDS.

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