Dissolution and permeation characteristics of artemether tablets formulated with two gums of different surface activity

Emmanuel O Olorunsola,Musiliu O Adedokun,Michael U Adikwu,Partap G Bhatia,Babajide A Tytler

doi:10.4314/tjpr.v16i5.3

Abstract

Purpose: To evaluate the dissolution and permeation characteristics of artemether tablets formulated with cashew and prosopis gums, and compare with tablets prepared with acacia gum.Methods: Artemether tablets containing varying concentrations (1.0 to 4.0 %w/w) of cashew and prosopis gums or 3 %w/w of acacia (control) gum as binders were formulated by wet granulation method. The tablets were evaluated for crushing strength, friability and disintegration time. Dissolution and permeation characteristics of the formulations were studied using USP methods.Results: Tablets formulated with prosopis gum had higher crushing strength, higher friability and higher disintegration time compared to those of cashew gum at corresponding binder concentrations. Tablets formulated with 3 %w/w cashew gum exhibited complete drug release within 1 h, 95 % drug permeation in 188 min (in simulated gastric fluid [SGF]) and 95 % permeation in 224 min (under simulated intestinal fluid [SIF] condition) while those made with 3 %w/w prosopis gum exhibited 70.7 % drug release in 1 h, 95 % permeation in 135 min (in SGF) and 95 % permeation in 170 min (under SIF condition).Conclusion: Cashew gum is effective as a binder over a relatively wide range of concentrations to achieve fast drug release though with minimal permeation enhancement while prosopis gum is characterized by delayed drug release but enhanced permeation of the released drug.Keywords: Cashew gum, Acacia, Prosopis, Artemether, Drug release, Dissolution, Permeation

Highlights

The mechanisms by which surface active agents can influence drug delivery vary widely and include micellar solubilization and permeation enhancement [1]
While there was no significant difference in drug flux from tablets containing 3 %w/w acacia gum (ACG) and 3 %w/w cashew gum (CSG), tablets containing the same concentration of Prosopis gum (PRG) exhibited significantly higher drug flux
Cashew gum is similar to acacia gum in terms of binding, release and permeation-enabling properties

Summary

Introduction

The mechanisms by which surface active agents can influence drug delivery vary widely and include micellar solubilization and permeation enhancement [1]. The release of poorly watersoluble drugs from tablets and capsules may be enhanced by the presence of surfactants in their formulations. Increase in saturation solubility of such drugs by solubilization in surfactant micelles might enhance dissolution and absorption [2]. The effect of surface active agents on drug delivery depends on the nature of the drug especially its water solubility. Artemether is a white crystalline powder with good solubility in organic solvents and poor solubility in water [3]. It is a lipid-soluble artemisinin [4]

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