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THE PHARMA REVIEW (OCTOBER - NOVEMBER 2007)

Gastroretentive Drug Delivery System

R.K. Rishi

Abstract: Oral delivery of drugs is by far the most preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in formulation, etc. From immediate release to site specific delivery, oral dosage forms have really progressed. However, it is a well-accepted fact that it is difficult to predict the real in vivo time of release with solid, oral controlled release dosage forms. Thus, drug absorption in the gastrointestinal (GI) tract may be very short and highly variable in certain circumstances. It is evident from the recent scientific and patent literature that an increased interest in novel dosage forms that are retained in the stomach for a prolonged and predictable period of time exists today in academic and industrial research groups. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in the GI tract is to control the gastric residence time (GRT). Dosage forms with a prolonged GRT, i.e. gastroretentive dosage forms (GRDFs), will provide us with new and important therapeutic options.

Gastric retention will provide advantages such as the delivery of drugs with narrow absorption windows in the small intestinal region. Also, longer residence time in the stomach could be advantageous for local action in the upper part of the small intestine, for example treatment of peptic ulcer disease. Furthermore, improved bioavailability is expected for drugs that are absorbed readily upon release in the GI tract. These drugs can be delivered ideally by slow release from the stomach.

A controlled drug delivery system with prolonged residence time in the stomach is of particular interest for drugs that:

i) Are locally active in the stomach,
ii) Have an absorption window in the stomach or in the upper small intestine,
iii) Drugs with narrow window of absorption,
iv) Are unstable in the intestinal or colonic environment, or
v) Exhibit low solubility at high pH values.

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