Progress in Controlled Gastroretentive Delivery Systems

Controlled release (CR) dosage forms have been extensively used to improve therapy with several important drugs. However, the development processes are faced with several physiological difficulties such as the inability to restrain and localize the system within the desired region of the gastrointestinal tract and the highly variable nature of the gastric emptying process. This variability may lead to unpredictable bioavailability and times to achieve peak plasma levels. On the other hand, incorporation of the drug in a controlled release gastroretentive dosage forms (CR-GRDF) which can remain in the gastric region for several hours would significantly prolong the gastric residence time of drugs and improve bioavailability, reduce drug waste, and enhance the solubility of drugs that are less soluble in high pH environment. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. Thus, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits to patients. Controlled gastric retention of solid dosage form may be achieved by the mechanisms of floatation, mucoadhesion, sedimentation, expansion or by a modified shaped system. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive dosage forms.

[1]  Yiqiao Hu,et al.  Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers. , 2006, International journal of pharmaceutics.

[2]  M. Patel,et al.  Gastroretentive drug delivery system of ranitidine hydrochloride: Formulation and in vitro evaluation , 2004, AAPS PharmSciTech.

[3]  Saurabh Wadhwa,et al.  Floating microspheres of cimetidine: formulation, characterization and in vitro evaluation. , 2005, Acta pharmaceutica.

[4]  Y. Tanwar,et al.  Formulation and evaluation of famotidine floating tablets. , 2007, Current drug delivery.

[5]  F. N. Christensen,et al.  The effect of density on the gastric emptying of single- and multiple-unit dosage forms , 1986, Pharmaceutical Research.

[6]  A. Moes.  Gastroretentive dosage forms. , 1993, Critical reviews in therapeutic drug carrier systems.

[7]  A. Awasthi,et al.  Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: preparation and in vitro characterization. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[8]  C. Lehr,et al.  Bioadhesion technologies for the delivery of peptide and protein drugs to the gastrointestinal tract. , 1994, Critical reviews in therapeutic drug carrier systems.

[9]  N. K. Jain,et al.  Floating microspheres bearing acetohydroxamic acid for the treatment of Helicobacter pylori , 2003, The Journal of pharmacy and pharmacology.

[10]  Y. Fujibayashi,et al.  Pharmacoscintigraphic evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans. , 2004, Journal of controlled release : official journal of the Controlled Release Society.

[11]  I. El-Gibaly.  Development and in vitro evaluation of novel floating chitosan microcapsules for oral use: comparison with non-floating chitosan microspheres. , 2002, International journal of pharmaceutics.

[12]  J. B. Park,et al.  Preparation of alginate beads for floating drug delivery system: effects of CO(2) gas-forming agents. , 2002, International journal of pharmaceutics.

[13]  A. Hoffman,et al.  Pharmacodynamic aspects of modes of drug administration for optimization of drug therapy. , 1999, Critical reviews in therapeutic drug carrier systems.

[14]  J. Timmermans,et al.  The Bilayer Floating Capsule: A Stomach-Directed Drug Delivery System for Misoprostol , 1992, Pharmaceutical Research.

[15]  P. Yeole,et al.  Studies on formulation and evaluation of ranitidine floating tablets , 2005 .

[16]  C. Rhodes,et al.  Development of a Novel Controlled-Release System for Gastric Retention , 1997, Pharmaceutical Research.

[17]  S. Lakshmi,et al.  A floating-type oral dosage form for piroxicam based on hollow polycarbonate microspheres: in vitro and in vivo evaluation in rabbits. , 2002, Journal of controlled release : official journal of the Controlled Release Society.

[18]  R. Gröning,et al.  Oral Dosage Forms with Controlled Gastrointestinal Transit , 1984 .

[19]  S. Davis,et al.  In vitro evaluation of alginate gel systems as sustained release drug delivery systems , 1986 .

[20]  J H Collett,et al.  Floating dosage forms: an in vivo study demonstrating prolonged gastric retention. , 1998, Journal of controlled release : official journal of the Controlled Release Society.

[21]  Y. Kawashima,et al.  Hollow microspheres for use as a floating controlled drug delivery system in the stomach. , 1992, Journal of pharmaceutical sciences.

[22]  Sara Eyal,et al.  Novel levodopa gastroretentive dosage form: in-vivo evaluation in dogs. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[23]  A. El-Kamel,et al.  Preparation and evaluation of ketoprofen floating oral delivery system. , 2001, International journal of pharmaceutics.

[24]  J. Timmermans,et al.  Factors controlling the buoyancy and gastric retention capabilities of floating matrix capsules: new data for reconsidering the controversy. , 1994, Journal of pharmaceutical sciences.

[25]  P. R. Sheth,et al.  The Hydrodynamically Balanced System (Hbs™): A Novel Drug Delivery System for Oral Use , 1984 .

[26]  P. Vavia,et al.  Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin. , 2006, International journal of pharmaceutics.

[27]  R. Gröning,et al.  Dosage forms with controlled gastrointestinal passage — studies on the absorption of nitrofurantoin , 1989 .

[28]  P. Sher,et al.  Development of hollow/porous calcium pectinate beads for floating-pulsatile drug delivery. , 2007, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[29]  A. Hoffman,et al.  Expandable gastroretentive dosage forms. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[30]  P. Deasy,et al.  In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihydrate , 1992 .

[31]  K. Muthusamy,et al.  Preparation and evaluation of lansoprazole floating micropellets , 2005 .

[32]  A. Hoffman,et al.  Novel Gastroretentive Dosage Forms: Evaluation of Gastroretentivity and Its Effect on Riboflavin Absorption in Dogs , 2002, Pharmaceutical Research.

[33]  J. Siepmann,et al.  Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release. , 2003, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[34]  Juergen Siepmann,et al.  Gastroretentive drug delivery systems , 2006, Expert opinion on drug delivery.

[35]  J. Timmermans,et al.  How well do floating dosage forms float , 1990 .

[36]  Parviz Mojaverian,et al.  Effects of Gender, Posture, and Age on Gastric Residence Time of an Indigestible Solid: Pharmaceutical Considerations , 1988, Pharmaceutical Research.

[37]  Brahma N. Singh,et al.  Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[38]  J. Timmermans,et al.  Intragastric positioning of two concurrently ingested pharmaceutical matrix dosage forms. , 1991, International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology.

[39]  P. Vavia,et al.  Development of sustained release gastroretentive drug delivery system for ofloxacin: in vitro and in vivo evaluation. , 2005, International journal of pharmaceutics.

[40]  A. Hoffman,et al.  Pharmacodynamic aspects of sustained release preparations. , 1998, Advanced drug delivery reviews.

[41]  K. Ladefoged,et al.  Distribution of pellets in the gastrointestinal tract. The influence on transit time exerted by the density or diameter of pellets , 1978, The Journal of pharmacy and pharmacology.

[42]  S. Basak,et al.  Design and in vitro testing of a floatable gastroretentive tablet of metformin hydrochloride. , 2007, Die Pharmazie.

[43]  Ziyaur Rahman,et al.  Design and evaluation of bilayer floating tablets of captopril. , 2006, Acta pharmaceutica.

[44]  E. Doelker,et al.  Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery , 1996 .

[45]  Y. Kawashima,et al.  In vitro and in vivo evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans. , 2004, International journal of pharmaceutics.

[46]  A. Pawar,et al.  Low density multiparticulate system for pulsatile release of meloxicam. , 2006, International journal of pharmaceutics.

[47]  J. Fell,et al.  Development of a gastroretentive dosage form. , 1996 .