ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Anti-solvent sonocrystallization to enhance the dissolution rate of clopidogrel using Box-Behnken design

Nishita Mangal and Sanjaykumar R. Patel

Department of Chemical Engineering, Sardar Vallabhbhai National Institute of Technology, Surat, India

E-mail: srpatel079@gmail.com

Received: 12 September 2020  Accepted: 15 March 2021

Abstract:

The purpose of this study was to enhance dissolution rate of a poorly water-soluble drug clopidogrel (CLP) by reducing its particle size. For this, CLP microparticles were prepared by ultrasound-assisted antisolvent precipitation. The Box–Behnken (BBD) design with three-factor and three-level has been employed to optimize the process parameters. Independent variables selected were temperature ((X_{1})), sonication amplitude ((X_{2})), and sonication time ((X_{3})). The prepared microparticles were assessed for % drug release (DR). The optimized condition was 27.098 °C, 41.098%, and 60 min. Optimum formulation showed 73.91% DR in 20 min, whereas the pure CLP showed 53.25% DR in 20 min. Prepared CLP microparticles were characterized using X-ray powder diffraction (XRPD), Fourier transformed infrared (FT-IR), and scanning electron microscope (SEM). Further, the effect of stabilizers PVP K-30 and Tween 80 on % DR have been studied. The maximum % DR obtained was 78.76% in 20 min at concentration 0.6% (w/v) of PVP K-30, whereas the maximum % DR of 76.49% in 20 min was obtained at concentration 0.4% (w/v) of Tween 80. Thus, these results suggest that ultrasound-assisted antisolvent precipitation could act as promising technique to improve solubility of poorly soluble drugs.

Keywords: Clopidogrel; Ultrasound; Drug release; PVP K-30; Tween 80

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-021-01605-y

Chemical Papers 75 (8) 3797–3806 (2021)