几种一叶萩碱制剂体内吸收水平的测定与比较  

Bio-assay and comparison of absorption of different securinine preparations

作　　者：陶忠华[1] 谷士杰[1] 

机构地区：[1]中国医学科学院药物研究所

出　　处：《中国药学杂志》1990年第1期16-18,共3页Chinese Pharmaceutical Journal

摘　　要：本文报道了一种简便、灵敏度较高的一叶秋碱（SCRN）制剂体内吸收的生物测定法。此法根据SCRN在血液中的浓度达到一定水平时会引起动物抽搐的特征，测得本批实验用鼠静注SCRN硝酸盐时的半数抽搐量（CD50^IV)为3．98mg/kg，并以此为基准比较了4种SCRN制剂在肌注或口服后进入血液的速度、所能达到的血药水平及其时间效应。试验结果表明：肌注SCRN硝酸盐的CD50为15mg/kg。它能很快被吸收，但3h后血药水平很低。肌注SCRN油剂则与之相反，给药量虽高达26mg/kg，也只能使3h后出现的血药水平峰值为24．6％，但它有长效作用，10h后才降至5．8％。初步临床试验的结果也表明后者的有效率略有高些。此外，还试验和讨论了某些口服制剂的吸收效果。A simple biological assay was used to de-termine the level of absorption of securininewith a relatively high sensitivity. When the con-centration of securinine in blood reached a cri-tical level, convulsion in animals occurred.In rats, 50% convulsion dosage (CD_(50)) of secu-rinine nitrate injected intravenously was 3.98%mg/kg. By using this dosage, the level of ab-sorption of different securinine preparations wasmeasured and compared including the rate ofabsorption after intramuscular injection or oraladministration, the concentrations in blood aswell as time effects. The experiment showedthat the CD_(50) of securinine nitrate injected in-tramuscularly was 15mg/kg and could be ab-sorbed rapidly but reduced to a very low level af-ter 3 hours. On the contrary, the intramuscularinjection of 26mg/kg of securinine oil couldonly make the level to reach a peak of 24.6%after 3 hours with a long-action effect; the le-vel, reduced continueously to 5.8 % after 10hours. The experiment also showed that the effe-ctive rate of the latter slightly better. The eff-ectiveness of some P. O. securinine prepara-tions was also studied.

关 键 词：一叶秋碱 生物测定 半数抽搐量 制剂 中枢神经兴奋剂 

分 类 号：R971.7[医药卫生—药品]