Abstract

MIXTURE DESIGN EXPERIMENT ON FORMULATION DEVELOPMENT AND OPTIMIZATION OF EMPAGLIFLOZIN INN TABLET A NEW MILESTONE ON IMMEDIATE RELEASE DRUG DELIVERY SYSTEM

Md. Mehdi Hasan*, Saiful Islam, Kanchi Akter lima, Sharmin Akter Bristy, Md. Feroze Mahmud, Nishat Angum, Israt Jahan Mim and Md. Yakub Hossain

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Abstract

Background & Objectives: The oral drug delivery system which includes the solid dosages form such as conventional dosages form and immediate release dosages form. The objective of this study was to formulate orodispersible tablets containing empagliflozin by direct compression method with sufficient hardness and rapid disintegration time and to study the effect of functionality differences of super-disintegrants on the tablet properties. Methods: The basic approach used in development immediate release solid dosages form by using superdisintegrant like sodium starch glycolate (Primogel, Explotab), Polyvinylpyrrolidone (PVP) etc. Impact of various formulation variables in extended release part was assessed usingstatistical interpretation such as analysis of variance. Which provides in instantaneous disintegration of tablet after administration. By using various techniques in can be formulate like wet granulation, direct compression etc. Prepared batches were evaluated for all pre-compression parameters and post-compression parameters. This method was found to be linear in a concentration range of 5-30 μg/ml of the drug (r 2= 0.999). The low value of % RSD in the precision study indicates reproducibility of the method. The low value of LOD and LOQ suggests the sensitivity of the method. Optimization was done by fitting experimental data to the software program (design expert). The design spacefor formulation variables and its influence on drug release was developed. In-vitro release data observed fromthe optimized formulation was fitted into various kinetic equations. Results: The results of forced degradation studies indicated that the drug was less stable in thermal and photolytic condition and degraded in acidic, basic, oxidative conditions. On the basis of formulation evaluation, batch was found to be promising formulation suitable for the immediate release of empagliflozin. Conclusions: Results obtained by validation studies suggested that the developed stability indicating assay method is simple, accurate, specific, sensitive and precise. Thus, this method can be used for routine analysis of empagliflozin formulation and to check the stability testing. The immediate release of empagliflozin tablets was successfully developed by employing granulation technology and formulation optimization facilitated by experimental design.

Keywords: Empagliflozin, Formulation R&D, Tablets, HPLC, Stability indicating assay method.