APPLICATION AND EVALUATION OF 3-COMPONENT MIXTURE OF DIRECTLY COMPRESSIBLE EXCIPIENTS IN TABLET FORMULATION USING AN OPTIMIZATION TECHNIQUE

APPLICATION AND EVALUATION OF 3-COMPONENT MIXTURE OF DIRECTLY COMPRESSIBLE EXCIPIENTS IN TABLET FORMULATION USING AN OPTIMIZATION TECHNIQUE


Agubata CO 1*, Orjiezoke AC1, Nzekwe IT2, Okoye IE 2

1Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka, Nigeria
2Department of Pharmaceutics and Pharmaceutical Technology, Nnamdi Azikiwe University, Awka, Nigeria

Afr. J Pharm Res Dev; Volume 9(1): 30-39; June/July 2017
ABSTRACT
Different excipients can be mixed to achieve optimal outcomes in direct compression of tablets. The aim of this study is to formulate and evaluate hydrochlorothiazide tablets based on mixtures of directly compressible excipients using the simplex lattice optimization technique. Hydrochlorothiazide tablets were prepared by direct compression technique using a simplex lattice optimization design involving eight different formulations with varied amounts of microcrystalline cellulose (MCC), dextrose and lactose granules. The tablets were evaluated for weight uniformity, crushing strength, friability, disintegration time and dissolution rate. The friability values of the tablets were within the range of 0.2-0.5% while the crushing strengths were within the range of 7-12 KgF. Batches 2 and 8 containing MCC (26.5% w/w and 32.4% w/w, respectively), dextrose (37.5% w/w and 23.4% w/w, respectively) and lactose granules (26.5% w/w and 34.7% w/w, respectively) were selected as the optimized products on the basis of high dissolution (97.7% and 101.8% respectively, at 60 min) and least disintegration time of 13.8 min and 12.7 min, respectively. Equations and response surface plots were derived for the prediction of hydrochlorothiazide release, tablet disintegration time and friability using Design Expert® 10 software. Optimization has proven to be an effective tool in product development and can be used to achieve Quality by Design (QbD). Mixtures of the directly compressible excipients were effectively optimized for the formulation of hydrochlorothiazide tablets.

KEYWORDS: Directly compressible, optimization, excipients, simplex lattice

Email of correspondence: chukwuma.agubata@unn.edu.ng