盐酸纳美芬鼻腔喷雾剂纤毛毒性影响因素的考察与评价  

Evaluation of the influencing factors on the ciliotoxicity of nalmefene hydrochloride nasal sprays

作　　者：杜玍妮[1] 高永良[2] 潘卫三[1] 

机构地区：[1]沈阳药科大学,沈阳110015 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2007年第15期1199-1202,共4页Chinese Journal of New Drugs

摘　　要：目的:考察盐酸纳美芬鼻腔喷雾剂纤毛毒性的影响因素并对其进行评价。方法:应用离体蟾蜍上颚黏膜为实验模型,同时应用光学显微镜观察不同因素对纤毛摆动时间的影响。结果:药物浓度、溶液pH值和羟丙基-β-环糊精(HP-β-CD)在一定范围内或浓度下对纤毛摆动时间无显著性影响,而渗透压和三氯叔丁醇对纤毛摆动时间有显著性影响,并且HP-β-CD和三氯叔丁醇之间存在相互作用,两者合用时,三氯叔丁醇的纤毛毒性明显下降。结论:在一定范围内或浓度下,鼻腔给药的纤毛毒性受药物浓度、溶液pH值和HP-β-CD的影响较小,受渗透压、三氯叔丁醇影响较大,HP-β-CD可以降低三氯叔丁醇的纤毛毒性。Objective： To evaluate the influencing factors on the ciliotoxicity of nalmefene hydroehloride nasal sprays. Methods：Isolated toad palate was employed as in vitro model, and an optical microscope was used to investigate the influencing factors on the lasting time of ciliary movement after ap- plication of nalmefene hydroehloride solutions. Results ： Drug concentration, pH value and HP-β-CD concentration of nalmefene hydroehloride solution had little effect on the lasting time of ciliary movement, while osmotic pressure of the testing solution and presence of ehlorobutanol had obvious influence on the lasting time of ciliary movement. In addition, HP-β-CD interacted with ehlorobutanol when they were applied together, resulting in a significant decrease in the eiliotoxieity of ehlorobutanol. Conclusions ：Within a certain range of concentration, eiliotoxieity was influenced slightly by drug concentration, pH value and HP-β-CD concentration of nalmefene hydroehloride but significantly by osmotic pressure and ehlorobutanol. HP-β-CD could reduce the eiliotoxieity of ehlorobutanol.

关 键 词：蟾蜍上颚离体法 纤毛毒性 盐酸纳美芬 三氯叔丁醇 羟丙基-Β-环糊精 

分 类 号：R965.3[医药卫生—药理学]