흰쥐에서 이부프로펜 리신염의 물리화학적 특성 및 약물동태에 관한 평가
Physicochemical Characteristics and Pharmacokintics of Ibuprofen Lysine Salts
  • 정연복
  • 신대환
  • 김태성
  • 박승혁
  • 김시현
  • 외 2명
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초록

Two types of water soluble lysine salts of ibuprofen were prepared and evaluated. Physicochemical properties for ibuprofen-l-lysinate (IBL-l), ibuprofen-dl-lysinate (IBL-dl) and ibuprofen (IB) were studied on melting point, specific ratation, UV spectra and ^1H-NMR spectra. There were not differences between IBL-dl and IBL-l in UV spectra and 1H-NMR spectra. The pharmacokinetic parameters of IB were compared to those of its lysine salts (IBL-l and IBL-dl) after i.v. or oral administration at the dose of 50 mg/kg (calculated as IB). Total body clearance (CL_t) and area under the plasma concentration- time curve (AUC) were not different between IB group and IBL groups after i.v. administration. On the other hand, IBL-l and IBL-dl produced peak plasma concentrations (C_(max)) significantly ealier and higher than IB. Time to reach peak concentration (T_(max)) after IBL administration was lower than that after IB administration. There was no difference in AUC across all different groups (IB, IBL-l and IBL-dl) after oral administration. However, absorption rate constant (k_a) of IBL-l and IBL-dl were significantly increased than that of IB. These results indicated that the administration of IBL-l and IBL-dl may be advantageous if rapid and reliable onset of pain relief is required.

키워드

ibuprofenlysinatepharmacokineticsphysicochemical properties
제목
흰쥐에서 이부프로펜 리신염의 물리화학적 특성 및 약물동태에 관한 평가
제목 (타언어)
Physicochemical Characteristics and Pharmacokintics of Ibuprofen Lysine Salts
저자
정연복신대환김태성박승혁김시현조한준한건
발행일
2011-06
저널명
약 학 회 지
55
3
페이지
260 ~ 266