盐酸甲唑醇的药代动力学及片剂与胶囊的生物利用度比较  

Pharmacokinetics of methimidol hydrochloride and a comparison of bio availability between its capsules and tablets

作　　者：张正光[1] 熊春生[1] 

机构地区：[1]军事医学科学院微生物流行病研究所,北京100071

出　　处：《中国药理学与毒理学杂志》1990年第4期286-288,共3页Chinese Journal of Pharmacology and Toxicology

摘　　要：犬po盐酸甲唑醇(methimidol hydrochlo-ride)片剂或胶囊后,用分光光度计测定了不同时间的血药浓度,用3P87电子计算机程序计算了药代动力学参数,对两种剂型的生物利用度进行了比较。结果表明该药在犬体内以双指数函数衰减,即符合二室开放模型,胶囊与片剂的末相半衰期分别为6.9 h和6.1 h,片剂的相对生物利用度为胶囊的80.6％。1-(2'-hydroxy)-ethyl-2-methyl-imidazol(methimidol hydrochloride)is a new anti-leptospiral compound.The methimidol in blood samples at different times after a single oral administration of 120mg/kg of the capsule or tablet to dogs was extracted with chloroform through removing protein and alkalization,and determined by a spectrophotometer at a wavelength of 650 nm after reaction with bromothymol blue(BTB).The pharmacokinetic parame-ters of the drug were computed by the Marquadt's method and statistical moment analysis of '3P87 Pharmacokinetic Program' with a IBMPC/XT computer.The concentration of methimidol in blood can be characterized by a biexponential equation.The terminal half-life period of the capsule and tablet is 6.90 and 6.07 h,the area under the curve is 177 and 143μg·h·ml-1 and the mean residence time(MRT)is 5.9 and 6.3 h,respectively.The bioa-vailability of the tablet is only 80.6% of that of the capsule.

关 键 词：盐酸甲唑醇 药代动力学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]