氟康唑在兔体内的药代动力学及组织穿透性
Pharmacokinetics and tissue penetration of fluconazole in rabbits.
作者信息
Walsh T J, Foulds G, Pizzo P A
机构信息
Pediatric Branch, National Cancer Institute, Bethesda, Maryland 20892.
出版信息
Antimicrob Agents Chemother. 1989 Apr;33(4):467-9. doi: 10.1128/AAC.33.4.467.
Abstract
Fluconazole is a new bis-triazole antifungal compound which has in vivo and in vitro activity against Candida spp. and Cryptococcus neoformans and excellent penetration into cerebrospinal fluid. However, little is known about the penetration of fluconazole into tissue sites other than cerebrospinal fluid. We therefore studied by high-pressure liquid chromatography the penetration of fluconazole into nine different tissue sites at times of peak and trough concentrations in plasma in rabbits. Fluconazole penetrated into all tissue sites. Tissue/plasma concentration ratios were greater at time of trough concentrations in plasma than at times of peak concentrations in plasma. The finding that fluconazole penetrated into target organs commonly infected by Candida spp. and C. neoformans further supports the therapeutic potential of fluconazole for disseminated candidiasis or cryptococcosis in immunocompromised hosts.
摘要
氟康唑是一种新型双三唑类抗真菌化合物，具有体内外抗念珠菌属和新型隐球菌的活性，且能很好地穿透进入脑脊液。然而，除脑脊液外，对于氟康唑在其他组织部位的穿透情况了解甚少。因此，我们通过高压液相色谱法研究了兔血浆中氟康唑浓度达峰和谷时在九个不同组织部位的穿透情况。氟康唑可穿透进入所有组织部位。组织/血浆浓度比在血浆谷浓度时高于血浆峰浓度时。氟康唑可穿透进入念珠菌属和新型隐球菌常见感染的靶器官这一发现，进一步支持了氟康唑对免疫功能低下宿主播散性念珠菌病或隐球菌病的治疗潜力。
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