Abstract

GENERATION AND EVALUATION OF NOVEL NON-SWELLING MATRIXING CO-PROCESSED EXCIPIENT WITH GASTRORETENTIVE AND POLYMORPH STABILIZING ACTIVITY

Prashant Kumar Choudhari*, H. K. Jain, P. Sharma and B. Srivastava

ABSTRACT

The purpose of this study was to develop novel non-swelling matrixing co-processed excipient to prolong gastric residence time of a model drug due to its narrow absorption window in the gastrointestinal tract (GIT) and short biological half-life (3-5 hr). The delivery system was based on the sustained release formulation with floating property in order to prolong the gastric residence time as well as sustained the drug release for longer period of time. Novel co-processed excipient was developed by techniques such as physical mixing and rapid mixer granulation utilizing release retarding polymer Eudragit EPO, separately, in combination with different concentration of hydroxyl propyl methyl cellulose 100 cps (Methocel K-100 M, HPMC), ethyl cellulose (Ethocel N50, EC) and hydroxyl propyl cellulose (Klucel EF, HPC). All co-processed excipients were evaluated for their flow properties and particle size distribution. Out of various combinations, six exhibited promising flow properties were found suitable for direct compression and formulated as tablets. Ciprofloxacin (anhydrous form) was selected as a model drug and the formulation was developed using direct compression approach. Various formulations were evaluated for physical parameters like assay, uniformity of weight, hardness, friability, floating lag time, floating duration, swelling index and in vitro drug release profile. In vitro dissolution study confirms that formulation prepared using co-processed excipient showed sustained drug release. The optimised formulation was characterised by DSC, PXRD and FTIR which confirms the absence of polymorphic change (ciprofloxacin anhydrous to hydrous form) of drug during the development. The optimised formulation was kept for stability study for six months as per ICH guidelines and found to be stable. In the present work it was concluded that the floating duration was more in tablet with EC as compared with formulations containing HPMC and HPC. Ciprofloxacin release could be prolonged about 15 hr in the GIT by using blend of co-processed excipient and formulate it as a gastro retentive floating tablet.

Keywords: Co-processed excipient, Ciprofloxacin, Direct compression, Ethyl cellulose, Floating duration, Gastro retentive floating tablet.