Dispersible tablets Itraconazole pharmacokinetics and bioequivalence studies.docVIP

 PAGE \* MERGEFORMAT 13 Dispersible tablets Itraconazole pharmacokinetics and bioequivalence studies Author: Ho Kang Zhou, Yang Li-long, Zhu-Wen-bing, ZHANG Bi-kui, ZHU Yun-gui, XU Ping 【Abstract】 Objective: To study the tablet of itraconazole and itraconazole capsules in the normal human pharmacokinetics and bioequivalence. Methods: 18 healthy male volunteers randomized crossover single-dose oral administration of 0.2 g tablet of itraconazole subjects formulations and itraconazole capsule reference formulation, the use of high-performance liquid chromatography determination of itraconazole in plasma drug concentration, using analysis of variance and two one-sided t test to determine their biological equivalence. Results: The two kinds of preparations are in line with an open one-compartment model absorption, itraconazole tablet and capsule itraconazole main pharmacokinetic parameters AUC0 → 72, respectively (2 221.9 ± 762.9), and (2 311.9 ± 844.4) ng / (h * mL), AUC0 → ∞, respectively (2 374.2 ± 790.8), and (2 473.3 ± 878.9) ng / (h * mL), Cmax were (179.8 ± 56.8) and (174.1 ± 64.1) ng / mL, Tmax were (3.6 ± 1.0) and (4.1 ± 1.3) h, t1 / 2, respectively (16.5 ± 4.2) and (17.5 ± 3.1) h. Itraconazole tablet relative bioavailability (97.8 ± 14.0)%. Conclusion: Itraconazole tablet and itraconazole capsules were bioequivalent. Keywords: Itraconazole; pharmacokinetics; bioequivalence Itraconazole for antifungal agents, mainly for Candida vaginitis, tinea versicolor, dermatophytoses, such as the bottom of the foot tinea, ringworm palm, oral candidiasis, fungal keratitis, a fungal disease as well as system fungal diseases. Because itraconazole is a highly lipophilic compound, in patients taking itraconazole bioavailability after volatile [1]. Clinically, the general approach to take delivery immediately after the meal, but the food composition would affect its bioavailability [2  3]. In this paper, two manufacturers of itraconazole tabl