Fomuation Development of an immediate release solid oral Dosage form for an Anti coagulant drug

Abstract

The present experimental work was aimed to formulate and develop a generic product which was an immediate release solid oral dosage form for a BCS class II anticoagulant drug. Two main concerns with respect to the development of this product were i) to solve the issue related to the low solubility of the drug which may directly impact the dissolution profile and ii) to develop a non-infringing formulation. The issue related to the low drug solubility was addressed by micronization of the API and use of a wetting agent in the formulation. On the other hand, for the development of a non-infringing formulation- three different granulation techniques were used along with the use of the hydrophilic binding agent in concentration other than the one claimed in the patent. Dry granulation by Roller Compaction, Wet granulation by FBP and Wet granulation by RMG were the three granulation techniques that were used, out of which Wet granulation by RMG was found to be the most suitable for the present product to be developed. Preliminary activities for the present work were started by a comprehensive review of literature so as to understand the potential challenges in the formulation as well as analytical method development. The next step was the characterization of the RLD product, on the basis of which further development was continued. The excipients used for the formulation of the generic product were same as the ones used in the RLD product. Pre-formulation studies were carried out to check for any potential incompatibilities between the API and the excipients. Subsequently development trials for optimization of the final batch were carried out. Characterization involved the In-process quality control tests, along with dissolution, water content and assay for the analysis of the product. The optimized batches were charged for stability studies as per the requirement standards. After evaluation of the developed tablets; all the arameters were found to be within limits. Thus the developed generic formulation was found fective for further processing of scale-up batches, commercial development and marketing in the near future.