Liquisolid-Technology A Promising Tool for Solubility Enhancement of Poorly Water Soluble Drugs

Abstract

Oral ingestion is the most suitable and convenient route of drug delivery due to its ease of administration, high patient compliance, cost effectiveness, least sterility constraints, and flexibility in the design of dosage form. Thus, many of the generic drug companies are inclined more to produce bioequivalent oral drug products. In fact, liquisolid tablets deliver active ingredient(s) in a similar mechanism as soft gelatin capsule preparation which contains liquid because in liquisolid tablets, non-volatile liquid vehicle was used to dissolve the solid drug, and the preparation does not involve drying and evaporation process; therefore, the drug is held in the solution even though it is in a tabletted or encapsulated dosage form. Consequently, drug dissolution properties and oral bioavailability will be improved. In conclusion, this study proved that liquisolid technology is a viable technique for the dissolution enhancement of antiarthritic drugs (leflunomide and diacerein) which are the model hydrophobic drugs with low dissolution properties caused by its poor aqueous solubility. The present study confirms the potentiality of liquisolid systems to improve the dissolution properties of poorly water soluble drugs. Leflunomide and diacerein were selected as a model drugs for designing liquisolid systems. Leflunomide newlineexhibits oral bioavailability of 80% but it was practically insoluble in water (less than newline40mg/L) and diacerein aqueous solubility was 7-10 and#956;g /ml at pH 7.0 at 40 o C. newlineHence, the above two drugs were further developed for fabricating liquisolid newlineformulation. In this study, various liquisolid formulation were prepared using newlineselective non-volatile solvent which is based on the saturation solubility of the newlinesolvent and different formulation variables were studied like the effect of carrier newlinecoating ratio, effect of drug concentration and FM value on dissolution newlinecharacteristics. newline newline