利用生物粘附技术提高萘哌地尔的生物利用度

被引:7
作者
丁劲松
蒋学华
袁牧
机构
[1] 湖南医科大学附属第二医院!湖南长沙,华西医科大学药学院!四川成都,贵阳医学院药学系!贵州贵阳
关键词
萘哌地尔; 生物粘附; 药物动力学; 生物利用度;
D O I
10.16438/j.0513-4870.2001.05.014
中图分类号
R965 [实验药理学];
学科分类号
100602 ; 100706 ;
摘要
目的 为提高萘哌地尔生物利用度 ,制备生物粘附性萘哌地尔胶囊。方法 制备萘哌地尔胶囊、生物粘附胶囊I和II;比较两种生物粘附性胶囊与大鼠离体胃肠组织的粘附力 ;用自身对照方式单剂量分别给予家犬 3种胶囊 2 0 0mg ,比较 3种胶囊在家犬体内的药物动力学与生物利用度。结果 与普通胶囊相比 ,生物粘附性萘哌地尔胶囊I和II在家犬体内的血药峰浓度 (Cmax)下降 ,达峰时间 (Tmax)延迟 ,药时曲线下面积 (AUC0→∞)明显增加 ,两者为生物不等效制剂 ,与普通胶囊相比 ,萘哌地尔粘附胶囊I与II的生物利用度分别为 15 0 %± 14%和 15 4%± 2 3% ,两种生物粘附胶囊的药动学参数间无明显差异。结论 利用生物粘附技术能明显提高萘哌地尔的生物利用度
引用
收藏
页码:377 / 380
页数:4
相关论文
共 11 条
[1]  
Smart JD,Kellaway IW.Pharmaceutical factors influencing the rate of gastrointestinal transit in an animal model. International Journal of Pharmaceutics . 1989
[2]  
Ohno H,Sakai T,Tsuchida E,et al.Interaction of human erythrocyte ghost or liposomes with polyethylene glycol detected by fluorescence polarization. Biochemical and Biophysical Research Communications . 1981
[3]  
Mortazavi SA,Smart JD.An investigation of some factors influencing the in vitro assessment of mucoadhesion. International Journal of Pharmaceutics . 1995
[4]  
Himmel HM.Naftopidil, A novel antihypertensive drug. Cardiovascular Drugs . 1994
[5]  
Akiyama Y,Nagahara N,Nara E,et al.Evaluation of oral mucoadhesive microspheres in man on the basis of the pharmacokinetics of furosemide and riboflavin,compounds with limited gastrointestinal absorption sites. Journal of Pharmacy and Pharmacology . 1998
[6]  
Rao RKV,Buri P.A novel in situ method to test polymers and coated microparticles for bioadhesion. International Journal of Pharmaceutics . 1989
[7]  
Ding JS,Jiang XH.Determination of naftopidil in dog plasma by HPLC. J West China Pharm ( in Chinese) . 2000
[8]  
Park K,Robinson JT.Bioadhesive polymer as platform for oral-controlled drug delivery: method to study bioadhesion. International Journal of Pharmaceutics . 1984
[9]  
Thomas JK.Radiation-induced reaction in organized assemblies. Chemical Reviews . 1980
[10]  
Chng HS,Robinson JT.Bioadhesive polymers as platform for oral-controlled drug delivery II: synthesis and evaluation of some swelling water-insoluble bioadhesive polymers. Journal of Pharmacological Sciences . 1985