비글견을 이용한 케토롤락트로메타민 서방형 펠렛 제제의 위궤양 증상 비교와 약물속도론적 평가 (Pharmacokinetic Evaluation and Gastric Ulcer Symptoms comparison of Ketorolac Tromethamine Sustained-Release Pellets after Oral Administration in Beagle Dogs)

서지정보

· 발행기관 : 한국약제학회
· 수록지 정보 : Journal of Pharmaceutical Investigation / 39권 / 6호 / 401 ~ 409페이지
· 저자명 : 윤양노, 김수지, 정석현, 김효정, 박은석, 황성주, 이영원, 성하수, 신병철, 조선행

초록

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® RS 100 and Eudragit® NE 30D. The in vitro and in vivo drug release behavior of KT from Eudragit® RS 100 and NE 30D coated pellet (SR-A), Eudragit® 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.

영어초록

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® RS 100 and Eudragit® NE 30D. The in vitro and in vivo drug release behavior of KT from Eudragit® RS 100 and NE 30D coated pellet (SR-A), Eudragit® 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.

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