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친수성 기제와 소수성 기제를 이용한Sarpogrelate hydrochloride 서방정의 제조 및 평가

Effect of Hydrophilic and Hydrophobic Polymers on the Sustained-release Sarpogrelate HCl from Matrix Tablets

약학회지 2020년 64권 6호 p.446 ~ 453
채유병, 김성엽, 강진양, 박준범,
소속 상세정보
채유병 ( Chai Yu-Byoung ) - Sahmyook University College of Pharmacy
김성엽 ( Kim Sung-Yeop ) - Sahmyook University College of Pharmacy
강진양 ( Kang Chin-Yang ) - Sahmyook University College of Pharmacy
박준범 ( Park Jun-Bum ) - Sahmyook University College of Pharmacy

Abstract


The purpose of this study was to develop a sustained-release (SR) matrix tablet containing sarpogrelatehydrochloride (SH) and investigate the effect of hydrophilic and/or hydrophobic polymers on SH release. SH was selectedas a water-soluble drug, Hypromellose (HPMC) and Polyethylene oxide (PEO) as hydrophilic matrix-forming agents, andglyceryl behenate (GB; Compritol 888 ATO) as a hydrophobic agent. SR tablets with varying compositions of theaforementioned agents were prepared using wet granulation and tablet compression. Dissolution tests were performed usingthe paddle method per the US Pharmacopeia Apparatus II. Tablets containing only HPMC did not retard the initial releaseof 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 ofhydrophilic PEO and hydrophobic GB exhibited swelling and erosion that resulted in a zero-order, ideal drug-releasepattern for 12 h, with an R2 value of 0.914. Therefore, these results demonstrated that a combination of hydrophilic andhydrophobic polymers can form a matrix system that is more effective for the sustained release of SH compared to thematrix system formed using a single polymer.

키워드

sarpogrelate hydrochloride; sustained-release; hypromellose; polyethylene oxide; glyceryl behenate

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