首页|期刊导航|中国动物传染病学报|宠物抗真菌药伊曲康唑溶液与分散片药代动力学研究

宠物抗真菌药伊曲康唑溶液与分散片药代动力学研究OA

Pharmacokinetic Evaluation of Pet Antifungal Drug Itraconazole Solution and Dispersible Tablet

中文摘要英文摘要

本研究旨在建立伊曲康唑(itraconazole,ITZ)药代动力学研究方法,研究伊曲康唑制剂的药代动力学参数,为兽医临床用药及药物研发提供参考.选用8只2.6~4.2 kg的健康英国短毛猫公母各半,随机分为2组,分别给单剂量伊曲康唑内服溶液和分散片5 mg/kg、10 mg/kg.运用DAS2.0非房室动力学模型分析算相关药动学参数,结果显示,内服溶液主要药动学参数如下:t1/2(32.45±43.19)h、Tmax(2.75±1.58)h、Cmax(0.752±0.146)μg/mL、AUC0-t(15.01±5.26)μg/mL*h、AUC0-∞(21.94±19.00)μg/mL*h、MRT(49.59±56.91)h、Vz/F(329.13±157.74)L/kg、CLz/F(0.75±0.15)L/h/kg、Frel(218.39%).分散片主要药动学参数如下:t1/2(52.68±44.52)h、Tmax(3.13±1.13)h、Cmax(0.16±0.08)μg/mL、AUC0-t(3.07±1.32)μg/mL*h、AUC0-∞(5.02±3.69)μg/mL*h、MRT(67.13±66.00)、Vz/F(173.91±78.11)L/kg、CLz/F(3.22±2.69)L/h/kg、Frel(45.79%).以上结果显示,口服分散片的给药剂量10 mg/kg血药浓度远低于文献中提及的治疗真菌感染的有效浓度,建议在使用分散片治疗真菌感染时增加给药剂量.

This study aimed to establish a pharmacokinetic research method for itraconazole(ITZ),evaluate the pharmacokinetic parameters of commercially available itraconazole preparations and provide a reference for veterinary clinical medication and drug development.Eight healthy British shorthairs with a weight range of 2.6 to 4.2 kg,half male and half female,were randomly divided into two groups according to experimental requirements.Each cat was administered with single dose of itraconazole oral solution at 5 mg/kg or dispersible tablets at 10 mg/kg.The relevant pharmacokinetic parameters were analyzed and calculated using the DAS2.0 non atrioventricular kinetic model.The main pharmacokinetic parameters of itraconazole oral solution were summarized as follows:t1/2(32.45±43.19)h,Tmax(2.75±1.58)h,Cmax(0.752±0.146)μ g/mL,AU C0-t(15.01±5.26)μg/mL*h,AUC0-∞(21.94±19.00)μg/mL* h,MRT(49.59±56.91)h,Vz/F(329.13±15 7.74)L/kg,CLz/F(0.7 5±0.15)L/h/kg,Fr el(218.3 9%).T he main pharmacokinetic parameters of itraconaz ole dispersible tablets were listed below:t1/2(52.68±44.52)h,Tmax(3.1 3±1.13)h,Cmax(0.16±0.08)μg/mL,AUC0-t(3.07±1.32)μg/m L*h,AUC0-∞(5.02±3.69)μg/mL*h,MRT(67.13±66.00),V z/F(1 73.91±78.11)L/kg,C Lz/F(3.22±2.69)L/h/kg,Fre l(45.79%).In concl usion,the bl ood itraconazole concentration was much lower than the effective range mentioned in the literature for treating fungal infections when the single dosage of oral dispersible tablets was administered at 10 mg/kg.Therefore,it is recommended to increase the dosage when dispersible tablets were used for the treatment of fungal infections.

薛华磊;陶贻炯;黄琳杰;李晓;陈凯;张可煜;王米

中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241中国农业科学院上海兽医研究所,上海 200241

农业科技

伊曲康唑分散片内服溶液药代动力学

Itraconazoledispersible tabletoral solutionpharmacokinetics

《中国动物传染病学报》 2026 (2)

58-62,5

"十四五"国家重点研发计划项目(2023YFD1801304)

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