한국임상약학회지 (Korean Journal of Clinical Pharmacy)
- 제8권2호
- /
- Pages.133-138
- /
- 1998
- /
- 1226-6051(pISSN)
- /
- 2508-786X(eISSN)
세프테졸 프탈리미딜 에스텔의 흡수에 관한 연구
Study on the Absorption of Ceftezole Phthalimidyl Ester
- Lee, Jin Hwan (College of Pharmacy, Chosun University) ;
- Choi, Jun Shick (College of Pharmacy, Chosun University) ;
- Kim, Eun Cheol (College of Pharmacy, Chosun University)
- 발행 : 1998.12.01
초록
Phthalimidyl ester of ceftezole (CFZ-PT) was synthesized as a prodrug by esterification of ceftezole (CFZ) with N-bromophthalimide. CFZ-PT was more lipophilic than CFZ when the lipophilicity was assessed by partition coefficients between n-octanol and water at various pH. The pharmacokinetic characteristic of CFZ-PT and CFZ preparations were compared following oral administrations of these compounds to rabbits. CFZ-PT is expected to be metabolized rapidly to CFZ in the body. The metabolism process appears to be hydrolysis of the ester to CFZ, the parent drug of CFZ-PT. In vivo metabolism of CFZ-PT to CFZ was confirmed in rabbit by HPLC analysis. CFZ concentration in the serum samples taken after oral administration of CFZ-PT(equivalent amount of CFZ) were released and higher than those of CFZ. Oral bioavailability of CFZ-PT was 1.9 fold higher than at of CFZ in rabbits because of enhanced lipophilicity and absorption. Finally, it was concluded that CFZ-PT appears useful as a prodrug of CFZ to improve the oral bioavailability of CFZ.
키워드