Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Pharmacokinetic Evaluation and Gastric Ulcer Symptoms comparison of Ketorolac Tromethamine Sustained-Release Pellets after Oral Administration in Beagle Dogs

비글견을 이용한 케토롤락트로메타민 서방형 펠렛 제제의 위궤양 증상 비교와 약물속도론적 평가

  • Yoon, Yang-No (College of Pharmacy, Sungkyunkwan University,Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Kim, Su-Ji (College of Pharmacy, Chungnam National University,Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Jung, Suk-Hyun (Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Kim, Hyo-Jeong (Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Park, Eun-Seok (College of Pharmacy, Sungkyunkwan University) ;
  • Hwang, Sung-Joo (College of Pharmacy, Chungnam National University) ;
  • Lee, Yong-Won (College of Veterinary Medicine, Chungnam National University) ;
  • Seong, Ha-Soo (Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Shin, Byung-Cheol (Korea Research Institute of Chemical Technology Biomaterial Research Center) ;
  • Cho, Sun-Hang (Korea Research Institute of Chemical Technology Biomaterial Research Center)
  • 윤양노 (성균관대학교 약학대학,한국화학연구원 바이오소재연구센터) ;
  • 김수지 (충남대학교 약학대학,한국화학연구원 바이오소재연구센터) ;
  • 정석현 (한국화학연구원 바이오소재연구센터) ;
  • 김효정 (한국화학연구원 바이오소재연구센터) ;
  • 박은석 (성균관대학교 약학대학) ;
  • 황성주 (충남대학교 약학대학) ;
  • 이영원 (충남대학교 수의과대학) ;
  • 성하수 (한국화학연구원 바이오소재연구센터) ;
  • 신병철 (한국화학연구원 바이오소재연구센터) ;
  • 조선행 (한국화학연구원 바이오소재연구센터)
  • Published : 2009.12.20
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Abstract

Ketrorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug (NSAID) is required repeated administration due to its short blood half-life. To avoid dose-dependent side effects of KT, sustained-release pellets containing KT were prepared by coating with Eudragit$^{(R)}$ RS 100 and Eudragit$^{(R)}$ NE 30D. The in vitro and in vivo drug release behavior of KT from Eudragit$^{(R)}$ RS 100 and NE 30D coated pellet (SR-A), Eudragit$^{(R)}$ RS 100 coated pellet (SR-B) and conventional commercial immediate-release tablet (IR) was investigated. KT from SR-A and SR-B was slowly released over several hours, whereas IR showed rapid initial release in vitro. The pharmacokinetic study in vivo was performed by oral administration in beagle dogs. 5 mg IR was administered 3 times at intervals 5 hr. Five milligrams of IR was administered 3 times at intervals of 5 hr and 15 mg of SR-A and SR-B did once. After administering IR, KT concentration in blood showed high peak- trough fluctuation and stomach ulcer were discovered. On the other hand, SR-A and SR-B sustainedly released KT and reduced the occurrence of stomach ulcer. There sustained-release pellets will be effective system to minimize dosedependent of side effect and improve patient compliance.

Keywords

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