A Study on Solubility and Dissolution Enhancement of Roxithromycin

Abstract

AIM OF THE STUDY: Roxithromycin is a BCS Class II /IV drug belonging to macrolide antibiotic used in the treatment of a broad variety of infections, of which respiratory tract infections are the primary indication. But Roxithromycin has only 50% oral bioavailability, due to its poor aqueous solubility, which limits its potential for optimal drug delivery and therapeutic effect. Its poor solubility is thus an obstacle in formulation development. So it is more cost effective to chemically re-design a molecule than to move through the whole development process, it is crucial to develop a formulation that overcomes problems of insolubility. The aim of this study to enhance the solubility of Roxithromycin by using its solvates. OBJECTIVE OF THE STUDY: The objectives of this study to enhance the solubility and Dissolution by To Prepare Roxithromycin solvates using Choloroform and Ethanol as olvents To characterise the different forms prepared; To evaluate the Solvated form forms on their solubility and Dissolution To find the suitability of Solvated form in Pharmaceutical Formulation. PLAN OF WORK: The present work carried out to solubility and dissolution enhancement of roxithromycin which is having low bioavailability due to its poor aqueous solubility. So study was carried out to enhance the Solubility and dissolution of Roxithromycin in the following steps Literature survey, Procurement of drug and Chemicals, Preformulation of Roxithromycin, Preparation of Roxithromycin Solvates Characterisation of Roxithromycin Solvates Formulation of Roxithromycin Solvates CONCLUSION According to recent estimates, nearly 40% of new chemical entities are rejected because of poor solubility i.e. biopharmaceutical properties. Poor Solubility of drug may result in inadequate bioavailability and thus in ineffective treatment regimes. Similarly, roxithromycin also has a poor solubility profile and the form available on the market is mostly the stable, crystalline monohydrate with the oral bioavailability 50%.So the Objective of the present study to enhance the solubility and dissolution of Roxithromycin using solvates. Two solvate forms of roxithromycin were prepared by recrystallisation using chloroform and ethanol solvents. It was found that the Solvates showed better solubility and dissolution profile compared to Roxithromycin.Among Solvate Choloroform solvate showed better solubility and Dissolution profile than Ethanol solvate. The tablets of Choloroform solvates were formulated by direct compression method to find the suitability of Solvates in the formulation of Pharmaceutical Dosage form by comparing Freshly Prepared Choloroform Solvates against 3 months old choloroform solvate .The variants of solvates were used to find out the stability of solvates.Based on the evaluation of tablets it was found that During storage the solvates transformed in to more crystalline substance which may affect dissolution profile from the dosage. From the study it was concluded that Solvates can be used to enhance the solubility and dissolution of Poorly soluble drugs