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.

Continuous twin screw granulation of controlled release formulations with various HPMC grades

“…HPMC is the most popular hydrophilic matrix former for production of controlled release tablets as it is non-ionic, stable over a broad pH range, enzyme resistant, odourless and tasteless, extensively studied and understood, non-toxic and costeffective [4][5][6][7][8]. Moreover the available variety of HPMC grades with different substitution degrees and viscosities make it a versatile matrix former for controlled release of a wide range of drugs with varying solubilities and doses [8].…”

Application of Multivariate Methods to Evaluate Differential Material Attributes of HPMC from Different Sources

“…Hydroxypropyl methylcellulose (HPMC) is the most commonly used hydrophilic matrix in the pharmaceutical industry owing to its nonionicity, nontoxicity, stability in different pH solutions, and cost-effectiveness. 6 To find out the DMAs of HPMC, many previous studies have examined the chemical, 7 mechanical, 8 and thermal 9 properties of HPMC, as well as the effects of viscosity, particle size, and other properties on drug release. 10 Recent types of research have investigated the relationship between the HPMC properties and the drug dissolution by using various new characterization methods, such as modulated differential scanning calorimetry (DSC) 11 nuclear magnetic resonance, 12 FTIR, 13 and statistical methods.…”

Development of Sustained Release Preparations of Metoclopramide Hydrochloride Based on Fatty Matrix

“…3,4 It shows a good stability in acidic and alkaline medium but has a short half-life of 3-5 hours. 1,5 MH is usually given at a dose of 10-15 mg for four times a day to maintain the effective blood concentration. It has been suggested that a sustained release (SR) preparation of MH designing for twice daily administration might be an advantageous dosage form, especially in long term therapy.…”

“…It has been suggested that a sustained release (SR) preparation of MH designing for twice daily administration might be an advantageous dosage form, especially in long term therapy. [3][4][5][6] Correspondence to: Syed Shabbir Haider Email: haidersyedshabbir@yahoo.com Dhaka Univ. J. Pharm.…”

“…[15][16][17][18][19] So far, sustained release tablets of MH have been prepared using hydroxypropylmethylcellulose, carboxymethylcellulose sodium, chitosan, carbopol 981, crospovidone, croscarmellose sodium, etc. 5,20 Our aim was to use less number of cheap, readily available raw materials and adopt simple techniques that can be utilized easily, even if used for commercial purpose. Preparations based on wax-lipid matrix were supposed to fulfill our requirements and, therefore, selected for investigation in the present study.…”