Preparation and in vivo characterization of dual release tablet containing sarpogrelate hydrochloride

被引：9

作者：

Jun H. ^{[1
]}

Lee H.-J. ^{[1
]}

Shin B.-S. ^{[2
]}

Park C.-W. ^{[1
]}

机构：

[1] College of Pharmacy, Chungbuk National University, 194-31, Osongsangmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju, 28160, Chungcheongbuk-do

[2] College of Pharmacy, Catholic University of Daegu, Gyeongsan, 38430, Gyeongbuk

来源：

Journal of Pharmaceutical Investigation | 2018年 / 48卷 / 3期

基金：

新加坡国家研究基金会;

关键词：

Dual release tablet; In vitro–in vivo correlation; Pharmacokinetics; Sarpogrelate;

D O I：

10.1007/s40005-017-0330-z

中图分类号：

学科分类号：

摘要：

The aim of the present study was to prepare and evaluate the once-a-day dual release tablets of sarpogrelate and to perform in vitro and in vivo characterization. Carboxymethylcellulose calcium and cellulose-derived polymer were used as release modifier in immediate release (IR) and extended release (ER) granules, respectively. Dual release tablets containing 300 mg of sarpogrelate were consisted of IR and ER granules as the drug ratio of 100:200 (DRT-1) and 75:225 (DRT-2). In vitro release profiles of the dual release tablets were provided an initial burst release portion (up to 1.5 h), then followed by a constant extended release portion (for 24 h). The initial release rate of dual release tablets was controlled by ratio of IR and ER. Anplag® (100 mg) three times and dual release tablets (300 mg) once were administrated to beagle dogs, and evaluated the pharmacokinetics. It was indicated that once-a-day DRT-1 showed equivalent Cmax and AUC with conventional drug, and also good correlation between in vitro release faction and in vivo absorption fraction. The present study had a potential of once-a-day sarpogrelate tablet for improved patience compliance, safety and efficacy. © 2017, The Korean Society of Pharmaceutical Sciences and Technology.

引用

页码：363 / 372

页数：9

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