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

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...

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Published inJournal 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
LanguageEnglish
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
Online AccessGet full text
ISSN2093-5552
2093-6214
DOI10.1007/s40005-017-0330-z

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Abstract 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.
AbstractList 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 oncea- 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. KCI Citation Count: 2
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.
Author Lee, Hyo-Jung
Shin, Beom-Soo
Jun, Hun
Park, Chun-Woong
Author_xml – sequence: 1
  givenname: Hun
  surname: Jun
  fullname: Jun, Hun
  organization: College of Pharmacy, Chungbuk National University
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  organization: College of Pharmacy, Chungbuk National University
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Keywords Dual release tablet
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In vitro–in vivo correlation
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Snippet 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...
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Title Preparation and in vivo characterization of dual release tablet containing sarpogrelate hydrochloride
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