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Effect of Hydrophilic and Hydrophobic Polymers on the Sustained-release Sarpogrelate HCl from Matrix Tablets
Yakhak Hoeji 2020;64(6):446-453
Published online December 31, 2020
© 2020 The Pharmaceutical Society of Korea.

Yu-Byoung Chae, Sung-Yeop Kim, Chin-Yang Kang, and Jun-Bom Park#

College of Pharmacy, Sahmyook University
Correspondence to: Jun-Bom Park, Ph.D., Assistant Professor, College of Pharmacy, Sahmyook University, Seoul, 139-742, South Korea
Tel: +82-2-3399-1624, Fax: +82-2-3399-1617
E-mail: junji4@gmail.com
Received October 29, 2020; Revised November 25, 2020; Accepted December 14, 2020.
Abstract
The purpose of this study was to develop a sustained-release (SR) matrix tablet containing sarpogrelate hydrochloride (SH) and investigate the effect of hydrophilic and/or hydrophobic polymers on SH release. SH was selected as a water-soluble drug, Hypromellose (HPMC) and Polyethylene oxide (PEO) as hydrophilic matrix-forming agents, and glyceryl behenate (GB; Compritol 888 ATO) as a hydrophobic agent. SR tablets with varying compositions of the aforementioned agents were prepared using wet granulation and tablet compression. Dissolution tests were performed using the paddle method per the US Pharmacopeia Apparatus II. Tablets containing only HPMC did not retard the initial release of SH easily, whereas those containing only PEO did not maintain the late-stage sustained-release profiles well. Hydrophobic GB polymer alone did not facilitate tailored drug release. However, a formulation comprising a mixture of hydrophilic PEO and hydrophobic GB exhibited swelling and erosion that resulted in a zero-order, ideal drug-release pattern for 12 h, with an R2 value of 0.914. Therefore, these results demonstrated that a combination of hydrophilic and hydrophobic polymers can form a matrix system that is more effective for the sustained release of SH compared to the matrix system formed using a single polymer
Keywords : sarpogrelate hydrochloride, sustained-release, hypromellose, polyethylene oxide, glyceryl behenate


December 2020, 64 (6)
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