Microencapsulation of Verapamil Hydrochloride: A Novel Approach for Gastric Retention Using Different Polymers

Patel Manish P,Patel Jayvadan K,Patel Ravi R

doi:10.4172/2161-0444.1000118

Abstract

The aim of the present investigation was to prepare and evaluate gastroretentive floating microspheres of Verapamil hydrochloride that would retain the drug in stomach and continuously release the drug in controlled manner up to a predetermined time. Floating microspheres were prepared by emulsion solvent evaporation technique. In the present investigation three polymers were used in various concentrations; Methocel K4M, Methocel K15M and Methocel K100M. In vitro performance was evaluated by the usual pharmacopoeial and other tests such as particle size analysis, drug entrapment efficiency, flow properties, in vitro floatability studies, in vivo floatability studies in dog, in vitro drug release studies, stability studies etc. Results showed that the mixing ratio of components in the organic phase affected the size, size distribution, yield, drug content, floating time and drug release of microspheres. In most cases good in vitro floating behavior was observed and a broad variety of drug release pattern could be achieved by variation of the drug, polymer and solvent ratio.

Highlights

The high cost involved in the development of a new drug molecule has diverted the pharmaceutical industries to investigate various strategies in the development of new drug delivery systems [1]
Verapamil hydrochloride belongs to the group of calcium channel antagonists, used in the treatment of several cardiovascular disorders, angina pectoris, supraventricular tachycardia and hypertension
The physico-chemical properties of Verapamil and is shorter half-life make its suitable molecule for preparation of floating microspheres

Summary

Introduction

The high cost involved in the development of a new drug molecule has diverted the pharmaceutical industries to investigate various strategies in the development of new drug delivery systems [1]. Prolonged gastric retention improves bioavailability, reduces drug waste and improves solubility for drugs that are less soluble in a high pH environment It has applicable for local drug delivery to the stomach and proximal small intestine [4]. The principle of floating preparation offers a simple and practical approach to achieve increased gastric residence time for the dosage form and sustained drug release. Due to its extensive first pass effect it has much low bioavailability (10-20%) It has shorter half-life (4 h) dosing frequency is high. The objective of the present study is to develop suitable gastroretentive floating microspheres of Verapamil HCL and to study release kinetics of drug with a view to reduce the dose frequency and to achieve a controlled drug release with improved bioavailability

Objectives

Methods

Results