Preparation and In vitro Evaluation of Enteric Coated Oral Vancomycin Hydrochloride Sustained Release Formulation with Mucoadhesive Properties

Abstract

Clostridium difficile is a species of gram-positive bacteria thought to infect patients with weakened immune response resulting in colitis. Oral vancomycin hydrochloride is given four times a day to treat Clostridium difficile colitis and is commercially available in the form of capsule and solution. Patient’s compliance is the main issue in this treatment due to the multiple dosing frequencies. Accordingly, replacement of such dose regimen with a once daily dosage will enhance patient compliance. In this study, mucoadhesive vancomycin hydrochloride tablets were prepared with the use of chitosan to exert a local effect in the colon. Sustained release property was also imparted by chitosan. Enteric coating with Eudragit® S 100 was applied to prevent the sticking of chitosan tablets in the stomach and small intestine and deliver the tablets intact to the colon. The prepared tablets were evaluated for In vitro drug release for 24 hours and compared with the marketed formulation. The formulation was found to release in a sustained manner in pH 7.4 buffer allowing the colon delivered oral vancomycin hydrochloride to be a promising formulation in the development of a once daily treatment for Clostridium difficile colitis.