ISSN:
1573-739X
Keywords:
Administration, topical
;
Complexation
;
Cyclodextrin, beta
;
Drag compounding
;
Imidazoles
;
Solubility
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Complex formation between β-cyclodextrin and six antimycotic imidazole derivatives has been studied. The solubility of all drugs was increased in the presence of β-cyclodextrin. The smallest increase (approx. 5-fold) was observed for miconazol, and the largest increase (approx. 160-fold) was observed for bifonazol. Apparent I:I-complex constants were measured and found to decrease in the order: bifonazol 〉 ketoconazol 〉 tioconazol 〉 miconazol 〉 itraconazol 〉 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 \-cyclodextrin than from the same vehicles without β-cyclodextrin. The rationale of β-cyclodextrin addition to antimycotic topical preparations is discussed.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01962683
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