title: Effect of different polymers and their combinations on the release of metoclopramide HCl from sustained-release hydrophilic matrix tablets.
abstract: Metoclopramide HCl (MTC) is commonly used for the management of gastrointestinal disorders. It has a short biological half-life and is usually administered four times daily to maintain effective concentrations throughout the day. The aim of this study is to develop sustained-release hydrophilic matrix tablet formulations of drug to achieve reproducible and predictable release rates, extended duration of activity, decreased toxicity, reduction of required dose, optimized therapy, and improved patient compliance. Hydroxypropylmethyl cellulose (HPMC), carboxymethylcellulose sodium (NaCMC), chitosan and Carbopol 981 were incorporated in the matrix system separately or in combinations as release controlling factor by direct compression technique. Compatibility among the formulation components was assessed by DSC and FTIR analysis. MTC release from matrix was evaluated by using the US Pharmacopeia dissolution apparatus II. All formulations met the criteria of pharmacopeial requirements. Dissolution studies show that polymer type and concentration are important parameters on drug release. Chitosan, carbopol and NaCMC formulations exhibited pH-dependent drug release profile whereas HPMC did not. All the formulations containing 1:1 ratio of HPMC and chitosan exhibited desired drug release showing that all active substance releases progressively in a period of whole dissolution time and therefore it can be regarded as worthy of consideration for the manufacture of sustained-release MTC product.
authors.affiliation: Department of Pharmaceutical Technology, Gülhane Military Medical Academy, Ankara, Turkey. asavaser@gata.edu.tr
authors.forename: Ayhan
authors.initials: A
authors.lastname: Savaşer
authors.forename: Çetin
authors.initials: Ç
authors.lastname: Taş
authors.forename: Ziya
authors.initials: Z
authors.lastname: Bayrak
authors.forename: Cansel Köse
authors.initials: CK
authors.lastname: Özkan
authors.forename: Yalçın
authors.initials: Y
authors.lastname: Özkan
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D005079:Excipients / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008787:Metoclopramide / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D013607:Tablets / Q000737:chemistry*
chemical_list: D000180:Acrylic Resins; C516894:Carbopol 981; D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D013607:Tablets; D048271:Chitosan; D002266:Carboxymethylcellulose Sodium; D008787:Metoclopramide