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目的研究抗胆碱新药盐酸三环哌酯（ＴＣＰＮ）在小鼠体内的药代动力学及组织分布。方法药代动力学采用放射受体分析法研究，组织中的分布用放射同位素分析法研究。结果小鼠ｓｃＴＣＰＮ后，血液中药物浓度的经时过程符合一级吸收二室模型（Ｔ１／２β为２．２８ｈ，Ｔｍａｘ为０．１２５ｈ，Ｃｍａｘ为３．４４μｇ·Ｌ－１，Ｃｌ为２３．０Ｌ·ｋｇ－１·ｈ－１）。小鼠ｓｃ［３Ｈ］－ＴＣＰＮ后，分布高峰放射性依次为肾＞肝＞脑＞颌下腺＞肠１９９８－０４－０３收稿，１９９８－０７－２６修回＊国家自然科学基金资助课题，Ｎｏ３９１３００９０－２作者简介：葛召恒，男，３２岁，硕士，助理研究员；阮金秀，男，６２岁，研究员，博士生导师，中国毒理学会副理事长，中国药理学会药物代谢专业委员会主任委员＞心＞肌肉，唯有脑组织的放射性以较高的水平维持较长的时间。预先给小鼠ｓｃ不同剂量的ＱＮＢ，可不同程度地降低脑中放射性的分布。结论ＴＣＰＮ从血中的消除较快，但在脑组织分布时间长，这与药物与脑中Ｍ受体的特异性结合有关。
Objective To study the pharmacokinetics and tissue distribution of tricyclic piperazine hydrochloride (TCPN) in mice. Methods Pharmacokinetics was studied by radioimmunoassay and tissue distribution was studied by radioisotope analysis. Results Time course of drug concentration in blood was in accordance with the first-order absorption two-compartment model (T1 / 2β was 2.28h, Tmax was 0.125h, Cmax was 3.44μg · L-1 and Cl was 23 after scTCPN in mice. 0L · kg-1 · h-1). Mouse sc [3H] -TCPN, the distribution of peak radioactivity followed by kidney> liver> brain> submandibular gland> intestinal 1998-04-03 Received, 1998-07-26 repaired * National Natural Science Fund Project, No39130090-2 Male, aged 62, researcher and doctoral tutor, vice chairman of China Toxicology Society, chairman of the Chinese Society of Pharmacological Society of Drug Metabolism Professional Committee> heart> muscle, Only the radioactivity of brain tissue is maintained at a higher level for a longer period of time. Pretreatment of mouse sc with different doses of QNB can reduce the distribution of radioactivity in the brain to varying degrees. Conclusion The removal of TCPN from the blood faster, but in the brain tissue distribution for a long time, which is related to the specific binding of drugs and M receptors in the brain.