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The effect of beta-cyclodextrin complexation on the bioavailability and hepatotoxicity of clotrimazole

Title
The effect of beta-cyclodextrin complexation on the bioavailability and hepatotoxicity of clotrimazole
Author
최한곤
Issue Date
2007-10
Publisher
GOVI-VERLAG PHARMAZEUTISCHER VERLAG GMBH
Citation
PHARMAZIE, v. 62, No. 10, Page. 756-759
Abstract
Clotrimazole, a poorly water-soluble antimycotic agent, is a promising therapeutic agent for various diseases including cancer and sickle cell anemia. The oral bioavailability and hepatic toxicity of clotrimazole were compared with its P-cyclodextrin inclusion form which was prepared by the spray-drying method. The inclusion complex gave significantly higher initial plasma concentrations, C-max and AUC than did clotrimazole alone, indicating that the drug from the inclusion compound could be more easily absorbed in rats. Furthermore, mice treated with the inclusion compound showed significantly higher GOT/GPT values compared to clotrimazole alone. The inclusion compound also induced hypertrophy of hepatic cells by fat accumulation and disappearance of hepatic sinusoids, indications of pathological changes of liver, suggesting that the inclusion compound could induce more severe tissue damage in the liver than clotrimazole alone. Thus, hepatotoxicity of clotrimazole seems to be correlated with the enhanced oral bioavailability by inclusion complexation. Our results suggest that, in the development of a novel oral product, appearance or enhancement of hepatic toxicity must be considered along with oral bioavailability.
URI
https://www.ingentaconnect.com/content/govi/pharmaz/2007/00000062/00000010/art00009http://repository.hanyang.ac.kr/handle/20.500.11754/107094
ISSN
0031-7144
DOI
10.1691/ph.2007.10.7018
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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