抗孕唑（DL－111－IT）在恒河猴体内药代动力学  

PHARMACOKINETICS OF CONTRAGESTAZOL(DL-111-IT),A NEW NON-STEROID ANTIFERTILITY AGENT IN MONKEYS

作　　者：骆文莹[1] 应赢[1] 李志雄[1] 范春梅[1] 周建华[1] 方小聪 

机构地区：[1]浙江杭州医科大学药学系,福建计生所非人灵长类实验中心

出　　处：《药学学报》1995年第6期408-411,共4页Acta Pharmaceutica Sinica

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.

关 键 词：抗孕唑 药代动力学 高效液相色谱 恒河猴 

分 类 号：R969.1[医药卫生—药理学] R979.21[医药卫生—药学]