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서지반출
Enhanced Bioavailability of Poorly Water-Soluble Clotrimazole by Inclusion with ${eta}$-Cyclodextrin
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  • Enhanced Bioavailability of Poorly Water-Soluble Clotrimazole by Inclusion with ${eta}$-Cyclodextrin
  • Enhanced Bioavailability of Poorly Water-Soluble Clotrimazole by Inclusion with ${eta}$-Cyclodextrin
저자명
Prabagar. Balakrishnan,Yoo. Bong-Kyu,Woo. Jong-Soo,Kim. Jung-Ae,Rhee. Jong-Dal,Piao. Ming Guan,Choi. Han-Gon,Yong. Chul-Soon
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2007년|30권 2호|pp.249-254 (6 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

Clotrimazole, a poorly water-soluble antimycotic agent, is a promising agent for various diseases including cancer and sickle cell anemia. To improve the oral bioavailability of clotrimazole, the inclusion compound of clotrimazole with ${eta}$-cyclodextrin was prepared by spray-drying method and characterized by phase solubility, differential scanning calorimetry and dissolution. Furthermore, the pharmacokinetics after oral administration in rats was then performed compared with clotrimazole powder. The solubility of clotrimazole increased linearly as a function of ${eta}$-cyclodextrin concentration, resulting in A$_L$ type Phase solubility diagram Which revealed a formation of inclusion compound in a molar ratio of 1:2, with the apparent association constant of 230.2 M$^{-1}$. The dissolution rate of clotrimazole in the inclusion compound increased greatly compared to clotrimazole powder in pH 7.4 phosphate buffer solution. The inclusion compound gave significantly higher initial plasma concentrations, Cmax and AUC of clotrimazole than did clotrimazole powder when they were administered as suspension form, indicating that the drug from inclusion compound could be more orally absorbed in rats. Thus, the oral bioavailability of clotrimazole could be improved markedly by inclusion complexation, possibly due to an increased dissolution rate.