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KMID : 0369820090390060401
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Jorunal of Korean Pharmaceutical Sciences
2009 Volume.39 No. 6 p.401 ~ p.409
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Pharmacokinetic Evaluation and Gastric Ulcer Symptoms comparison of Ketorolac Tromethamine Sustained-Release Pellets after Oral Administration in Beagle Dogs
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Yoon Yang-No
Kim Su-Ji
Jung Suk-Hyun
Kim Hyo-Jeong
Park Eun-Seok
Hwang Sung-Joo
Lee Young-Won
Seong Ha-Soo
Shin Byung-Cheol
Cho Sun-Hang
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Abstract
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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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KEYWORD
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Ketorolac tromethamine, Sustained-release, Pellets, Pharmacokinetics, Gastric endoscop
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