Bioavailability Study of a 1200 mg Miconazole Nitrate Vaginal Ovule in Healthy Female Adults

Abstract

This study was undertaken to determine the bioavailabilityof a 1200 mg miconazole nitrate vaginal ovule in 20 healthy premenopausal females following a single application (Day 1, Group 1) and two applications, 48 hours apart (Day 1 and Day 3, Group 2). In Dose Group 1 (n = 10), the mean Cmax of 10.7 ng/ml occurred at 18.4 hours. The average plasma miconazole concentration was calculated to be 5.7 ng/ml during the 4- to 96-hour time interval. In Dose Group 2 (n = 10), mean Cmax values were 10.8 ng/ml and 12.0 ng/ml and occurred at 18.4 hours (Day 1) and 16.0 hours (Day 3), respectively. Comparing AUC0-48 on Days 1 and 3 (338 vs. 408 ng x h/ml) indicated small accumulation of plasma miconazole, while AUC0-48 obtained from Dose Group 2, Day 1 was similar to that of Dose Group 1 (338 vs. 329 ng x h/ml, respectively). Plasma miconazole profiles were best described by a monoexponential equation with zero-order input. Pharmacokinetic simulations performed on the pooled data from two dose groups (n = 20) suggest a steady-state accumulation after five doses administered daily or three doses taken once every other day. Drug exposure was similar to that of the marketed formulation (MONISTAT 7 vaginal cream), applied once daily for 7 days and more than 100-fold less than that reported when given intravenously or orally.

Przegląd Preparatów Najczęściej Stosowanych W Leczeniu Chorób Grzybiczych

“…Aplikowany dożylnie jako lek drugiego rzutu oraz doustnie w grzybicach o łagodnym przebiegu. Mikonazol, podobnie jak ketokonazol lub klotrimazol może być podawany w maściach lub kremach jednocześnie z hydrokortyzonem w łojotokowym zapaleniu skóry lub w trądziku pospolitym [47,48].…”

Vaginal drug administration in the hospital setting

“…19,20 In fact, the reduced rate of absorption of many vaginally administered drugs as compared with absorption achieved with other methods may minimize the potential risk to the baby during pregnancy and breastfeeding. 21 This feature is particularly advantageous in obstetric patients and their babies because they have a higher risk of drug injury and often lack safe pharmacologic therapeutic options.…”