Gastroretentive drug delivery systems.
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) are unstable in the intestinal or colonic environment, or iv) exhibit low solubility at high pH values. This article gives an overview of the parameters affecting gastric emptying in humans as well as on the main concepts used to design pharmaceutical dosage forms with prolonged gastric residence times. In particular, bioadhesive, size-increasing and floating drug delivery systems are presented and their major advantages and shortcomings are discussed. Both single- and multiple-unit dosage forms are reviewed and, if available, results from in vivo trials are reported.
Streubel
Alexander
A
College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany. alexander.streubel@roche.com
Siepmann
Juergen
J
Bodmeier
Roland
R
D000268:Adhesiveness; D000284:Administration, Oral; D000818:Animals; D004304:Dosage Forms; D016503:Drug Delivery Systems; D005746:Gastric Emptying; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D011108:Polymers / Q000737:chemistry
D004304:Dosage Forms; D011108:Polymers