Preparation and Evaluation of Multi-Particulate System (Pellets) of Prasugrel Hydrochloride

Navjot Kanwar,V.R Sinha,Rakesh Kumar

doi:10.2174/1874844901502010074

Abstract

Multiparticulate systems (pellets) of prasugrel hydrochloride were prepared by extrusion spheronization method using MCC (micro crystalline cellulose). Optimum spheronization time and method of drying were selected as the process parameters for the preparation of final batches. Various pellet properties were evaluated like size & shape analysis, flow properties, bulk & tapped density, friability, moisture content, drug content, in vitro release rate and in vivo pharmacodynamic studies. All pellet batches showed a narrow particle size distribution, good sphericity and excellent flow properties. Drug content and moisture content of different pellet batches were found in specified limits. The release kinetics of drug loaded MCC pellets followed Peppas model with Fickian diffusion of prasugrel from the pellets. In vivo pharmacodynamic studies exhibited improved bleeding time in pellet group when compared with the marketed tablet formulation.

Highlights

Multiparticulate drug delivery systems provide better gastrointestinal distribution and transportation resulting in minimizing the peak plasma fluctuations and side effects related to drug which are major advantages over single unit systems
Prasugrel hydrochloride was a generous gift from MSN Laboratories Limited, Bollaram, India
Water is considered as the choice of granulationg fluid over ethyl alcohol and isopropyl alcohol in preparation of MCC pellets

Summary

Introduction

Multiparticulate drug delivery systems (like pellets, granules, etc.) provide better gastrointestinal distribution and transportation resulting in minimizing the peak plasma fluctuations and side effects related to drug which are major advantages over single unit systems. These delivery systems facilitate co-administration of incompatible drugs (using coated pellets) [1,2,3]. Pellets provide flexibility of delivery system, i.e. either be filled in capsules or compressed into tablets. Pellets reduce the intra- and inter-subject variability in drug concentration by reducing the gastric emptying rate and transit time [9]

Methods

Results

Conclusion