Enhancement of Simvastatin dissolution by surface solid dispersion: effect of carriers and wetting agents

Ebtessam Ahmed Essa,Mai Dwaikat

doi:10.7324/japs.2015.54.s8

Abstract

Article history: The aim of this work was to improve the aqueous solubility of simvastatin using the surface solid dispersion (SSD) technique. Water soluble (mannitol and lactose) and insoluble (Avecil PH101) carriers were used. The effect of the addition of polymeric wetting agents (namely PEG6000, Pluronic F68, Myrj 52 and PVP K-30) to drug/carrier composite was also investigated. SSD was prepared by solvent evaporation technique. All formulations were studied regarding the dissolution behavior and solid state characterization (DSC, FT-IR and X- ray diffraction). Both water soluble and insoluble carriers improved dissolution behaviour compared to unprocessed drug, with the former showing the best results. Addition of wetting agent to the water insoluble carrier greatly improved drug dissolution, with PVP K-30 showing better dissolution parameters that was comparable to that of marketed product. Physical state characterization using DSC indicated the marked reduction in drug crystallinity. Xray diffraction confirmed drug amorphousness. The results indicated that SSD may serve as a successful strategy for enhancing solubility of poorly water soluble drugs by proper manipulation of the used additives.

Highlights

Oral route of drug administration is the most common and accepted delivery method from the patient’s prospective
Surface solid dispersion technique was a successful tool in enhancing the dissolution rate of simvastatin, a poorly water soluble drug
Both water soluble and insoluble, but hydrophilic, carriers showed a better dissolution behaviour compared to unprocessed drug

Summary

Introduction

Oral route of drug administration is the most common and accepted delivery method from the patient’s prospective. It is a problematic and inefficient route of delivery for many drugs specially poorly water soluble ones. The bioavailability of poorly water soluble drugs is a true challenge that faces the development of the conventional oral solid dosage forms. In consequence of the low water solubility of such drugs, bad dissolution profile and lower absorption and bioavailability are usually accompanying those drugs (Gu et al, 2007). There are techniques that can resolve the bioavailability issue with poorly water-soluble drugs, these techniques involve complicated technology and sophisticated machinery which are not

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