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作 者 ：党云洁,朱春燕

期 刊 ：中国中药杂志 2009年 34卷 16期 页码：2088.

关键词：斑蝥素；比格犬；药动学；GC-MS；

Keywords:cantharidin, beagle dogs, pharmacokinetics, GC-MS,

摘 要 ：目的：测定斑蝥素单剂量静脉和口服给药后的比格犬体内的药-时曲线，并与斑蝥素静脉单剂量给药相比，计算其体内的药代动力学参数和生物利用度。方法：6只比格犬给药，血样盐酸酸化后，乙酸乙酯萃取，使用GC-MS方法测定血浆中的微量斑蝥素，用WinNonLin程序计算药代动力学参数和生物利用度。结果：比格犬静脉注射斑蝥素（34 μg·kg^-1）的主要药代学参数：AUC (203.5±23.8) h·μg·L^-1，CL (168.8±18.6) mL·h^-1·kg^-1，t_1/2 (0.69±0.03) h；比格犬单剂量口服斑蝥素（102 μg·kg^-1）主要药代学参数是：AUC (160.4±26.9) h·μg·L^-1，CL (649.1±97.7) mL·h^-1·kg^-1，t_1/2 (0.38±0.1) h。与静脉注射相比，生物利用度为26.7%。结论：比格犬口服斑蝥素后，斑蝥素在犬体内的吸收较少，提示要提高斑蝥素的口服生物利用度，提高临床用药有效性。

Abstract:Objective： To study the pharmacokinetics and bioavailability of cantharidin in beagle dogs to evaluate the pharmacokinetic parameters and bioavailability of cantharidin in beagle dogs by determining dose-time curve and by comparing with the pharmacokinetics of cantharidin injection.Method： Six beagle dogs， after protein precipitation by hydrochloric acid，ethyl acetate was applied to extract cantharidin from plasma. The plasma concentration of cantharidin in beagle dogs was determined by GC-MS. The WinNonL in program was used to calculate the pharmacokinetic parameters and bioavailability. Result： The main pharmacokinetic parameters of cantharidin by iv in dogs (34 mL·h^-1·kg^-1) were AUC (203.5±23.8) h·μg·L^-1，CL (168.8±18.6) mL·h^-1·kg^-1， t_1/2 (0.69±0.03) h. The main pharmacokinetic parameters of cantharidin by op (102 μg·kg^-1) were： AUC (160.4±26.9） h·μg·L^-1，CL ( 649.1±97.7） mL·h^-1·kg^-1， t_1/2 (0.38±0.1) h.， F (bioavailability) =26.7% comparing to injection. Conclusion： As compared with cantharidin injection， the absorption of catharidin by op is poor and the bioavailability is also low， indicating that enhancement of the bioavailability will be beneficial to the clinical application.

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