A REVIEW ON FLOATING DRUG DELIVERY SYSTEM AS AN APPROACH TO INCREASE THE

GASTRIC RETENTION OF DRUGS

SUBHRADIP ROYCHOWDHURY* & SATARUPA BHATTACHARJEE**

*M.PHARM [PHARMACEUTICAL CHEMISTRY] DEPT. OF PHARM. SC.

BIRLA INSTITUTE OF TECHNOLOGY, MESRA-835215

** B.PHARM 4TH YEAR GURU NANAK INSTITUTE OF PHARMACEUTICAL SCIENCE AND TECHNOLOGY, KOLKATA-114

WHY THE ENHANCEMENT OF GASTRIC RETENTION

Gastric emptying of dosage forms is an extremely variable process and ability to prolong and control emptying time is a valuable asset for dosage forms, which reside in the stomach for a longer period of time than conventional dosage forms.

Several difficulties are faced in designing controlled release systems for better absorption and enhanced bioavailability.

One of such difficulties is the inability to confine the dosage form in the desired area of the gastrointestinal tract.

Drug absorption from the gastrointestinal tract is a complex procedure and is subject to many variables.

It is widely acknowledged that the extent of gastrointestinal tract drug absorption is related to contact time with the small intestinal mucosa.

Thus small intestinal transit time is an important parameter for drugs that are incompletely absorbed.

FLOATING DRUG DELIVERY SYSTEM- WHAT IS IT?

These are Hydrodynamically controlled systems.

Floating Drug Delivery systems are low-density systems that have sufficient buoyancy to float over the gastric contents.

These remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time.

While the system is floating on the gastric contents, the drug is released slowly at the desired rate from the system.

EQUATION GOVERNING THE FLOATING

FACTORS AFFECTING THE FLOATING TIME

CLASSIFICATION

A. SINGLE UNIT FLOATING DOSAGE SYSTEMS

a) Non- Effervescent Systems

b) Effervescent Systems [Gas Generating Systems]

B. MULTIPLE UNIT FLOATING DOSAGE SYSTEMS

a) Non- Effervescent Systems

b) Effervescent Systems [Gas Generating Systems]

c) Raft Forming Systems

d) Hollow Microspheres

EFFERVESCENT SYSTEMS

These are matrix type of systems prepared with the help of swell able polymers such as methyl cellulose, chitosan and various effervescent compounds Eg. Sodium Bicarbonate, Tartaric Acid etc.

They are formulated in such a way that when in contact with the acidic gastric contents, CO2 is liberated and gets entrapped in swollen hydro colloids which provide the buoyancy.

NON EFFERVESCENT SYSTEMS [ALGINATE BEADS]

These are spherical beads of approximately 2.5 mm in diameter can be prepared by dropping a sodium alginate solution in to aqueous solutions of calcium chloride causing precipitation of calcium alginate.

The beads are then separated snap and frozen in liquid nitrogen and freeze dried at -40°C for 24 hours leading to the formation of porous system which can maintain a floating force over 12 hours.

RAFT FORMING SYSTEMS

On contact with the gastric fluid a gel forming solution ( Eg. Sodium Alginate) swells and forms a viscous cohesive gel containing entrapped CO2 bubbles.

This forms a raft layer on top of gastric fluid which releases drug slowly in the stomach .

HOLLOW MICRO SPHERES [HOLLOW BALOONS]

Hollow microspheres are considered advantageous because these possess the unique advantages of multiple unit systems as well as better floating properties because of central hollow space.

The general techniques involved in their preparation include simple solvent evaporation and solvent diffusion and evaporation.

ADVANTAGES

1. These systems are advantageous for drugs absorbed through the stomach. E.g. Ferrous salts, antacids.

2. Acidic substances like aspirin cause irritation on the stomach wall when come in contact with it. Hence Floating Formulations may be useful for the administration of aspirin and other similar drugs.

3. Administration of prolongs release floating dosage forms, tablet or capsules, will result in dissolution of the drug in the gastric fluid. They dissolve in the gastric fluid would be available for absorption in the small intestine after emptying of the stomach contents. It is therefore expected that a drug will be fully absorbed from floating dosage forms if it remains in the solution form even at the alkaline pH of the intestine.

4. These are advantageous for drugs meant for local action in the stomach. e.g. antacids.

5. When there is a vigorous intestinal movement and a short transit time as might occur in certain type of diarrhoea, poor absorption is expected. Under such circumstances it may be advantageous to keep the drug in floating condition.

DISADVANTAGES

1. Floating system is not feasible for those drugs that have solubility or stability problem in G.I. tract.

2. These systems require a high level of fluid in the stomach for drug delivery to float and work efficiently-coat, water.

3. The drugs that are significantly absorbed through out gastrointestinal tract, which undergo significant first pass metabolism, are only desirable candidate.

4. Some drugs present in the floating system causes irritation to gastric mucosa.

APPLICATIONS

1. SUSTAINED DRUG DELIVERY:

These systems can remain in the stomach for long periods and hence can release the drug over a prolonged period of time. The problem of short gastric residence time encountered with an oral CR formulation hence can be overcome with these systems.

Eg. Sustained release floating capsules of Nicardipine Hydrochloride were developed and were evaluated in vivo. The formulation compared with commercially available MICARD capsules using rabbits. Plasma concentration time curves showed a longer duration for administration [16 hours] in the sustained release floating capsules as compared with conventional MICARD capsules [8 hours].

2. SITE SPECIFIC DRUG DELIVERY:

These systems are particularly advantageous for drugs that are specifically absorbed from stomach or the proximal part of the small intestine.

Eg. Furosemide is primarily absorbed from the stomach followed by the duodenum. It has been reported that a monolithic floating dosage form with prolonged gastric residence time was developed and the bioavailability was increased. AUC obtained with the floating tablets was approximately 1.8 times those of conventional furosemide tablets.

3. ABSORPTION ENHANCEMENT:

Drugs that have poor bioavailability because of site specific absorption from the upper part of the gastrointestinal tract are potential candidates to be formulated as floating drug delivery systems, thereby maximizing their absorption.

FUTURE ASPECTS

Identification of a minimal cut-off size above that DFs retained in the human stomach for prolonged period of time. This would permit a more specific control to be achieved in gastro-retentivity.

Design of array of FDDS, each having a narrow GRT for use according to the clinical need e.g. dosage and state of disease.

This may be achieved by compounding polymeric matrices with various bio degradation properties.

Study of the effect of various geometric shape, in a more excessive manner than previous studies, extended dimensions with high rigidity, on gastro-retentivity.

Design of novel polymers according to clinical and pharmaceutical need.

REFERENCES

1. Mayavanshi A.V. , Gajjar SS ; Floating drug delivery systems to increase gastric retention of drugs: A Review; ISSN 0974-3618, Research J. Pharm and Tech 1(4): Oct.-Dec. 2008

2. Dixit N; Floating Drug Delivery System; Journal of Current Pharmaceutical Research 2011;7(1):6-20

3. http://www.pharmatutor.org/articles/floating-drug-delivery-system-as-approach-to-increase-the-gastric-retention-of-drugs cited on 13.08.2013

4. http://www.authorstream.com/Presentation/siva.pharma45-944248-floating-drug-delivery-systems/ cited on 13.08.2013

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