A new cephalosporin derivate, cefazolin phthalidyl ester(CFZ-PT) was synthesized to improve oral absorption and bioavailability of parent drug by esterification of sodium cefazolin(CFZ). Partition coefficient studies showed that CFZ-PR is more lipophilic than CFZ. The pharmacokinetic characteristics of CFZ-PT and CFZ preparations were compared following oral administrations of these compounds to rabbits. The analysis of CFZ in plasma was conducted by HPLC method. The ester compound was not detected in plasma following oral administration of CFZ-PT was increased by yielding 3.5-fold bioavailability rather than CFZ. From the results of this experiment, it was concluded that CFZ-PT could be a novel prodrug of CFZ which can improve the oral bioavailability of CFZ.
저자
박용채 [ Park, Yong Chae | 조선대학교 약학대학 (College of Pharmacy, Chosun University) ]
이진환 [ Lee, Jin Hwan | 조선대학교 약학대학 (College of Pharmacy, Chosun University) ]
최준식 [ Choi, Jun Shik | 조선대학교 약학대학 (College of Pharmacy, Chosun University) ]
범진필 [ Burm, Jin Pil | 조선대학교 간호전문대학(College of Nursing, Cholsun University) ]