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

• Published in: Journal of pharmaceutical investigation Vol. 48; no. 3; pp. 363 - 372
• Main Authors: Jun, Hun, Lee, Hyo-Jung, Shin, Beom-Soo, Park, Chun-Woong
• Format: Journal Article
• Language: English
• Published: Singapore Springer Singapore 01.05.2018; 한국약제학회
• Subjects: Biomedical and Life Sciences; Biomedicine; Original Article; 약학; Dual release tablet; Pharmacokinetics; Sarpogrelate; In vitro–in vivo correlation
• ISSN: 2093-5552; 2093-6214
• DOI: 10.1007/s40005-017-0330-z

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 C max 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.