Merck
  • Home
  • Search Results
  • Effect of different polymers and their combinations on the release of metoclopramide HCl from sustained-release hydrophilic matrix tablets.

Effect of different polymers and their combinations on the release of metoclopramide HCl from sustained-release hydrophilic matrix tablets.

Pharmaceutical development and technology (2012-08-14)
Ayhan Savaşer, Çetin Taş, Ziya Bayrak, Cansel Köse Özkan, Yalçın Özkan
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
羧甲基纤维素钠, average Mw ~90,000
Sigma-Aldrich
羧甲基纤维素 钠盐, low viscosity
Sigma-Aldrich
羧甲基纤维素 钠盐, Medium viscosity
Sigma-Aldrich
羧甲基纤维素 钠盐, High viscosity
Sigma-Aldrich
羧甲基纤维素钠, average Mw ~700,000
Sigma-Aldrich
羧甲纤维素 钠, meets USP testing specifications, Medium viscosity
Sigma-Aldrich
羧甲基纤维素钠, average Mw ~250,000, degree of substitution 0.7
Sigma-Aldrich
羧甲基纤维素钠, average Mw ~250,000, degree of substitution 1.2
Sigma-Aldrich
羧甲基纤维素钠, average Mw ~250,000, degree of substitution 0.9
Sigma-Aldrich
羧甲基纤维素 钠盐, medium viscosity
Sigma-Aldrich
羧甲基纤维素 钠盐, ultra high viscosity, highly purified
Supelco
甲氧氯普胺, VETRANAL®, analytical standard