Fabrication and evaluation of captopril modified-release oral formulation

Abstract

The present research was directed towards fabrication of modified-release captopril oral formulation. A 3² full factorial design was employed for optimization using captopril to Compritol® ATO 888 ratio (X₁) and extragranular fraction of ethyl cellulose (X₂) as independent variables. The percentage drug released in 1 h (Y₁) and the time required to release 80% of the drug (Y₂) were selected as dependent variables. Eutectic blend of camphor and menthol was used as a solvent to facilitate the drug distribution in matrix. The optimized batch containing  50 mg captopril,  160 mg Compritol® ATO 888 and  220 mg ethyl cellulose was formulated by overlapping the contour plots of Y₁ and Y₂. The responses Y₁ and Y₂ of optimized batch were 25% and 520 min, respectively. The kinetics of drug release was best explained by Korsmeyer-Peppas model. The results of artificial neural network were superior in prediction power than the factorial design for both the responses (Y₁ and Y₂).

Keywords::

• Modified-release oral formulation
• captopril
• eutectic mixture
• factorial design
• artificial neural network

Acknowledgments

We are grateful to Indian Council of Medical Research (ICMR) for providing senior research fellowship (SRF) to one of the authors for this project. We are thankful to Zydus Cadila (Ahmedabad, India), Colorcon Asia Pvt. Ltd. (Goa, India) and Cabot Sanmar Pvt. Ltd. (Chennai, India) for kindly providing the gift samples.

Declaration of Interest: The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.