Abstract

Aduri Prakash Reddy*, G. Aravind Kumar, K. Srujana, S. Sai Chandana, S. K. Sameena, S. K. Thahera, V. Yashwanth and A. Swapna Madhuri

ABSTRACT

Aim of the study: Erythromycin is a BCS Class II /IV drug belonging to macrolideantibiotic used in the treatment of a broad variety of infections, of which respiratorytract infections are the primary indication. But Erythromycin has only 50% oralbioavailability, due to its poor aqueous solubility, which limits its potential foroptimal drug delivery and therapeutic effect. Its poor solubility is thus an obstaclein formulation development. So it is more cost effective to chemically re-design amolecule than to move through the whole development process, it is crucial todevelop a formulation that overcomes problems of insolubility. The aim of thisstudy to enhance the solubility of Erythromycin by using its solvates. Objective ofthe study: The objectives of this study to enhance the solubility and Dissolution byTo Prepare Erythromycin solvates using Choloroform and Ethanol as solvents Tocharacterise the different forms prepared; To evaluate the Solvated form forms ontheir solubility and Dissolution To find the suitability of Solvated form inPharmaceutical Formulation. Plan of work: The present work carried out tosolubility and dissolution enhancement of Erythromycin which is having lowbioavailability due to its poor aqueous solubility. So study was carried out toenhance the Solubility and dissolution of Erythromycin in the following stepsLiterature survey, Procurement of drug and Chemicals, Preformulation ofErythromycin, Preparation of Erythromycin Solvates Characterisation ofErythromycin Solvates Formulation of Erythromycin Solvates Conclusion:According to recent estimates, nearly 40% of new chemical entities are rejectedbecause of poor solubility i.e. biopharmaceutical properties. Poor Solubility of drugmay result in inadequate bioavailability and thus in ineffective treatment regimes.Similarly, Erythromycin also has a poor solubility profile and the form available onthe market is mostly the stable, crystalline monohydrate with the oral bioavailability50%. So the Objective of the present study to enhance the solubility and dissolutionof Erythromycin using solvates. Two solvate forms of Erythromycin were preparedby recrystallisation using chloroform and ethanol solvents. It was found that theSolvates showed better solubility and dissolution profile compared toErythromycin. Among Solvate Choloroform solvate showed better solubility andDissolution profile than Ethanol solvate. The tablets of Choloroform solvates wereformulated by direct compression method to find the suitability of Solvates in theformulation of Pharmaceutical Dosage form by comparing Freshly PreparedCholoroform Solvates against 3 months old choloroform solvate. The variants ofsolvates were used to find out the stability of solvates. Based on the evaluation oftablets it was found that During storage the solvates transformed in to morecrystalline substance which may affect dissolution profile from the dosage. From the study it was concluded that solvates can be used to enhance the solubility anddissolution of Poorly soluble drugs.