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特比萘芬在猫体内的单剂量药代动力学

Single dose pharmacokinetics of terbinafine in cats.

作者信息

Wang Ang, Ding Huanzhong, Liu Yiming, Gao Yan, Zeng Zhenling

机构信息

Laboratory of Veterinary Pharmacology, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.

出版信息

J Feline Med Surg. 2012 Aug;14(8):540-4. doi: 10.1177/1098612X12442280. Epub 2012 Mar 8.

Abstract

The pharmacokinetics of terbinafine was studied in six healthy fasted cats following a single intravenous and oral administration at a dose of 10 mg/kg and 30 mg/kg, respectively, according to a two-period crossover design. Plasma terbinafine concentrations were determined using a reverse phase liquid chromatographic method. The pharmacokinetic parameters were calculated by non-compartmental analysis with WinNonlin 5.2.1 software. After intravenous administration, the terminal half-life and area under the curve from time 0 to infinity were 10.40 ± 4.56 h, 15.20 ± 3.61 h·µg/ml, respectively. After oral dosing, the mean maximum concentration was 3.22 ± 0.60 µg/ml, reached at 1.33 ± 0.41 h. The terminal half-life, area under the curve from time 0 to infinity and apparent volume of distribution were 8.01 ± 3.46 h, 13.77 ± 4.99 h·µg/ml, 25.63 ± 6.29 l/kg, respectively. The absolute bioavailability of terbinafine hydrochloride tablets after oral administration was 31.00 ± 10.85%. Although bioavailability was low, excellent penetration at the site of infection and low minimum inhibitory concentrations values provided terbinafine with good efficacy against dermatophyte infections.

摘要

根据两周期交叉设计,在6只健康禁食猫中分别以10mg/kg和30mg/kg的剂量单次静脉注射和口服给药后,研究了特比萘芬的药代动力学。采用反相液相色谱法测定血浆特比萘芬浓度。使用WinNonlin 5.2.1软件通过非房室分析计算药代动力学参数。静脉给药后,终末半衰期和0至无穷大的曲线下面积分别为10.40±4.56小时、15.20±3.61小时·微克/毫升。口服给药后,平均最大浓度为3.22±0.60微克/毫升,在1.33±0.41小时达到。终末半衰期、0至无穷大的曲线下面积和表观分布容积分别为8.01±3.46小时、13.77±4.99小时·微克/毫升、25.63±6.29升/千克。口服盐酸特比萘芬片后的绝对生物利用度为31.00±10.85%。尽管生物利用度较低,但特比萘芬在感染部位具有出色的穿透力和较低的最低抑菌浓度值,使其对皮肤癣菌感染具有良好的疗效。

相似文献

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Single dose pharmacokinetics of terbinafine in cats.特比萘芬在猫体内的单剂量药代动力学
J Feline Med Surg. 2012 Aug;14(8):540-4. doi: 10.1177/1098612X12442280. Epub 2012 Mar 8.
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Terbinafine pharmacokinetics after single dose oral administration in the dog.犬单次口服给药后特比萘芬的药代动力学。
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