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以HPMC、CP为粘附材料,通过单因素和正交实验设计筛选处方,制备萘哌地尔胶囊、生物粘附胶囊I和生物粘附胶囊Ⅱ.测定比较两种生物粘附性胶囊与大鼠离体胃肠组织的粘附力.以自身对照方式单剂量分别给予家犬三种胶囊200 mg,测定比较三种胶囊在家犬体内的药物动力学与生物利用度.试验结果表明普通胶囊的C0→∞,Cmax和Tmax分别为3494.7±466.47 h.ng.mL-1、 697.48±94.22 ng.mL-1和1.15±0.49 h.缓释胶囊I的C0→∞,Cmax和Tmax分别为4618.46±316.68h.ng.mL-1、468.59±61,25 ng.mL-1和4.0±0.71 h.缓释胶囊Ⅱ的这些参数分别为4746.44±317.22 h.ng.mL-1、512.00±72.29 ng.mL-1和4.0±0.71 h.以萘哌地尔普通胶囊为参比制剂,萘哌地尔粘附胶囊I与Ⅱ的生物利用度分别为133.40±12.72%and137.53±17.49%,两种生物粘附胶囊的药动学参数之间没有明显差异.利用生物粘附技术能明显提高萘哌地尔的生物利用度.“,”To improve the bioavailability of naftopidil, bioadhesive sustained-release capsules and non-bioadhesive capsules were prepared. Bioadhesive polymers such as hydroxypropyl methylcellulose (HPMC) andCarbopol 934 (CP 934) were used in the bioadhesive capsules formulations. Naftopidil capsule and two formulationsof bioadhesive sustained-release capsules (I and II) were respectively given to five healthy male dogs in an openrandomized cross-over test. The naftopidil concentrations in plasma were determined by a newly developed HPLCmethod. The pharmacokinetic parameters and the relative bioavailability were measured. The AUC0→24, Cmax and Tmaxof non-bioadhesive naftopidil capsules were 3494.7±466.47 h@ng@mL-1, 697.48±94.22 ng@mL-1 and 1.15±0.49 h. Thesepharmacokinetic parameters of bioadhesive sustained-release capsules I and II were 4618.46±316.68 h@ng@ mL-1 and4746.44±317.22 h@ng@mL-1, 468.59±61.25 ng@mL-1 and 512.00±72.29 ng@mL-1, both 4.0±0.71 h respectively. Resultsfrom statistical analysis showed that there were significant differences between the two bioadhesive formulations andthe non-bioadhesive one in AUC0→24, Cmax and Tnax @ The relative bioavailability of the two bioadhesive sustained-release capsules were respectively 133.40±12.72% and 137.53±17.49% when compared with non-bioadhesivecapsules. The bioavailability of naftopidil in dogs was improved hy using bioadhesion.