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氢溴酸右美沙芬药物树脂缓释混悬剂在家犬体内药物动力学研究
刘天富1，李三鸣[1]，吴顺芹2，赵国斌3
(1.哈尔滨泰华药业股份有限公司，黑龙江 阿城 150302；2.沈阳药科大学药学院，辽宁 沈阳110016；3.吉林省药品检验所，吉林 长春 130062)
摘要：目的 建立测定家犬血浆中氢溴酸右美沙芬的代谢产物去甲右美沙芬含量测定的方法，并研究氢溴酸右美沙芬缓释混悬剂在家犬体内的药物动力学性质。方法 以己酮可可碱为内标,乙腈-0.3%( )磷酸盐缓冲液（60:30=V:V,三乙胺调pH为6.2）为流动相，Kromasil ODS-1 色谱柱（250 mm×4.6 mm,5μm）为固定相，检测波长为278 nm,以HPLC法测定家犬体内去甲右美沙芬。结果 本缓释制剂的AUC0-t为7 988.354 (μg·h)·L-1，ρmax为750.5 g·L-1，tmax为4 h；常释片（参比制剂）的AUC0-t为7 787.5 (μg·h)·L-1，ρmax为1 467.1μg·L-1，tmax为2 h；缓释制剂的相对生物利用度为97.5 %。结论 本缓释制剂具有良好的缓释效果，且与参比制剂生物等效。
关键词：药剂学；缓释混悬剂；药物树脂；药物动力学；氢溴酸右美沙芬；去甲右美沙芬
中图分类号：R 94 文献标识码：A
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Pharmacokinetic study on dextromethorphan hydrobromide drug-resin oral sustained-release suspensions in dogs
LIU Tian-fu1，LI San-ming2，WU Shun-qin2,ZHAO Guo-bin3
(1.Harbin Taihua Pharmaceutical Co.,Ltd,, Acheng 150302, China; 2.Shenyang Pharmaceutical University, Shenyang 110016, China ;3. Jilin Province Institute for Drug Control ,Changchun 130062 China )
Abstract: Objective To establish a HPLC method for determining the metabolism dextrophan of dextromethorphan hydrobromide in plasma and study the pharmacokinetic of the drug in dogs . Methods The internal standard was pentoxifylline .Plasma concentration of dextrophan was determined by HPLC using acetonitrile-0.3%( ) phosphate buffer (60:30=V:V) as the mobile phase, the Kromasil column packed with ODS-1 (250 mm×4.6 mm,5 μm) as a fixed phase and 278 nm as the detector wavelength. Results The obtained pharmacokinetic parameters of the test and reference formulation were as follows : AUC0-t 、ρmax 、tmax for the sustained- release suspensions were 7 988.354 (μg·h)·L-1, 750.5 μg∙L-1, 4 h，respectively; for the reference formulation were 7 787.5 (μg·h)·L-1 , 1467.1μg∙L-1, 2 h，respectively；the relative bioavailability of the test formulation was 97.5%. Conclusion The test formulation is a good sustained- release suspension and it is bioequivalent with the reference formulation..
Key words: pharmaceutics; sustained-release suspensions; drug-resin; pharmacokinetics; dextromethorphan hydrobromide; dextrophan