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抗孕唑(DL-111-IT)在恒河猴体内药代动力学 被引量:3

PHARMACOKINETICS OF CONTRAGESTAZOL(DL-111-IT),A NEW NON-STEROID ANTIFERTILITY AGENT IN MONKEYS
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摘要 恒河猴分别iv抗孕唑20%cremophorEL生理盐水液25,12.5及6.3mg·kg-1后,用柱切换HPI(法测定给药后24h内各时间点的血药浓度,根据各猴血药浓度-时间数据拟合曲线,均呈二房室动力学模型.其Y1/2a分别为0.38h,0.20h及0.36h;Y1/2β分别为6.60h,10.2h及10.1h;V(C)分别为5.30,1.26和1.48L·kg-1.分别im抗孕唑茶油液50,25和12.5mg·kg-13种剂量后,同上测定血药浓度,各猴血药浓度一时间数据拟合曲线,均呈-房室动力学模型。其Ka分别为0.98h,1.03h及1.45h;Ke为0.42h,0.37h及0.59h;T1/2Ke为1.66h,1.90h及1.16h;T(peak)为1.52h,1.57h及1.09h。 The pharmacokinetics of contragestazol,an early pregnancy temperating agent 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole,DL-111-IT]was studied in Rhesus monkey.The blood concentration of DL-111-IT was determined by coupled column system HPLCmethed,Using an aqueous vehicle(20% cremophor EL in saline)DL-111-IT was injectedintravenously to monkeys at doses of 25,12.5 and 6.3 mg·kg-1.Blood drug concentration weremeasured.Using a programmable calculator the calculated pharmacokinetic parameters were asfollows: α1.83h-1,4.71h-1 and 3.61 h-1;β0.15h-1,0.08h-1 and 0.09h-1;T1/2β6. 63h,10.2 h and 10.1h;AUC 9.54 ug·h-1·ml-1,3.94 ug·h-1·ml-1 and 3. 75ug·h-1·ml-1.An oil solution of DL-111-IT was injected intramuscularly in monkeys at doses of 50,25 and12.5 mg·kg-1.Its blood concentrations were determined at 0.08,0.25,0.5,0.75,1,1.5,2,4, 8,12 and 24 h after administration.From the time vs concentration curve,the pharmacokineticporameters obtained were as follows:Ka 0.98 h-1,1.03 h-1 and 1.45 h-1;Ke 0.42 h-1,0.37h-1 and 0.60 h-1;T1/2 Ke 1. 66 h,1.90 h and 1.16 h;T(peak)1.52 h,1.57 h and 1.09 h;AUC 4.86ug·h-1·ml-1,5.61 ug·h-1·ml-1 and 1.74 ug·h-1·ml-1.
出处 《药学学报》 CAS CSCD 北大核心 1995年第6期408-411,共4页 Acta Pharmaceutica Sinica
关键词 抗孕唑 药代动力学 高效液相色谱 恒河猴 Contragestazol Pharmacokinetics HPLC
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参考文献2

  • 1骆文莹,现代应用药学,1991年,8卷,1页
  • 2骆文莹,浙江医科大学学报,1991年,20卷,23页

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