Wang Ang, Ding Huanzhong, Liu Yiming, Gao Yan, Zeng Zhenling
Laboratory of Veterinary Pharmacology, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.
J Feline Med Surg. 2012 Aug;14(8):540-4. doi: 10.1177/1098612X12442280. Epub 2012 Mar 8.
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.
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。