Development of Metadoxine Lipid Microspheres for Alcohol intoxication

Abstract

Objective: The need of the study is to develop Controlled release Metadoxine tableted microsphere in order to extend the action of the drug so that it can release medicament in a controlled manner and maintain its concentration constantly at the alcohol metabolising site for the treatment of alcohol intoxication. Methods: The present study involves the use of Congealable Dispersion phase Encapsulation technique to formulate Metadoxine microspheres. Hydrogenated cottonseed oil (HCSO) and stearic acid were employed as the lipid matrix materials and Tween 60 as the droplet stabilizer. Drug to lipid ratio was taken as 1:2. The prepared microspheres were characterized to assess their behaviour, optimized and compressed into a tablet using various release modifiers such as Eudragit L, PEG 4000, Sodium alginate and Cross-linked Sodium carboxymethyl cellulose. Further the compressed tablets were evaluated to predict the controlled release behaviour. Results: The drug release from Stearic acid-lipid microspheres was rapid with sustained action. Tablets formulated using release modifiers like Eudragit L and PEG 4000 (S6A and S6B) showed release retardation whereas formulations containing Sodium alginate and Cross-linked carboxymethylcellulose (S6C and S6D) produced a controlled release. Release obtained from formulation S6C was observed to be pH-dependent. With the tablet of a Stearic acid microsphere containing cross-linked sodium carboxymethylcellulose (S6D), the controlled release had been achieved due to gradual disintegration from tablet to aggregates and to individual microspheres.