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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(34μg.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,t1/2(0.69±0.03)h;比格犬单剂量口服斑蝥素(102μg.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,t1/2(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。
OBJECTIVE: To determine the drug-time curve of Beagle dogs after a single intravenous and corticosteroid administration of cantharidin, and compare their pharmacokinetic parameters and bioavailability with single dose cantharidin intravenous injection. METHODS: Six Beagle dogs were administered blood acidified with hydrochloric acid and extracted with ethyl acetate. Trace levels of cantharidin in plasma were determined by GC-MS. Pharmacokinetic parameters and bioavailability were calculated using the WinNonLin program. RESULTS: The main pharmacokinetic parameters of Beagle dogs were as follows: AUC (203.5 ± 23.8) h.μg.L-1, CL (168.8 ± 18.6) mL.h.lkg -1, t1 / 2 (0.69 ± 0.03) h. The main pharmacokinetic parameters of beagle dogs with single dose of 102μg.kg-1 were AUC (160.4 ± 26.9) h.μg.L- (649.1 ± 97.7) mL.h-1.kg-1, t1 / 2 (0.38 ± 0.1) h. Compared with intravenous injection, bioavailability was 26.7%. Conclusion: Beagle dog cantharidin, cantharidin in dogs less absorption, suggesting that to improve the oral bioavailability of cantharidin and improve the effectiveness of clinical medication.