Van Doorne H, Bosch E H, Lerk C F
Department of Pharmaceutical Technology, State University of Groningen, The Netherlands.
Pharm Weekbl Sci. 1988 Apr 22;10(2):80-5. doi: 10.1007/BF01962683.
Complex formation between beta-cyclodextrin and six antimycotic imidazole derivatives has been studied. The solubility of all drugs was increased in the presence of beta-cyclodextrin. The smallest increase (approx. 5-fold) was observed for miconazol, and the largest increase (approx. 160-fold) was observed for bifonazol. Apparent 1:1-complex constants were measured and found to decrease in the order: bifonazol greater than ketoconazol greater than tioconazol greater than miconazol greater than itraconazol greater than clotrimazol. The complexes appeared to possess a low, if any, antimicrobial activity. Measurement of inhibition zone sizes, with four test organisms was used to study the release of the antimycotic drugs from topical preparations. The antimycotic drugs were more readily released from topical preparations containing beta-cyclodextrin than from the same vehicles without beta-cyclodextrin. The rationale of beta-cyclodextrin addition to antimycotic topical preparations is discussed.
已对β-环糊精与六种抗真菌咪唑衍生物之间的络合物形成进行了研究。在β-环糊精存在的情况下，所有药物的溶解度均有所增加。咪康唑的溶解度增加最小（约5倍），联苯苄唑的溶解度增加最大（约160倍）。测定了表观1:1络合常数，发现其顺序为：联苯苄唑＞酮康唑＞噻康唑＞咪康唑＞伊曲康唑＞克霉唑。这些络合物似乎具有很低的抗菌活性（如果有的话）。用四种测试微生物测量抑菌圈大小，以研究抗真菌药物从局部制剂中的释放情况。与不含β-环糊精的相同载体相比，抗真菌药物从含β-环糊精的局部制剂中更容易释放。讨论了在抗真菌局部制剂中添加β-环糊精的原理。
