论文部分内容阅读
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 C_→∞, C_max 和 T_max 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C→∞, C_max 和 T_max 分别为4618.46±316.68 h·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% and 137.53±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。
Naftopidil capsules, bioadhesive capsules I and bioadhesive capsules II were prepared by single factor and orthogonal experimental design with HPMC and CP as adherent materials. Determination of adhesion between two bioadhesive capsules and rat in vitro gastrointestinal tissue. The self-control single-dose dogs were given three capsules 200 mg, determination of three kinds of capsules in dogs pharmacokinetics and bioavailability. The results showed that C_ → ∞, C_max and T_max of ordinary capsules were 3494.7 ± 466.47 h · ng · mL -1, 697.48 ± 94.22 ng · mL -1 and 1.15 ± 0.49 h, respectively. The C → ∞, C_max and T_max of sustained release capsules I were 4618.46 ± 316.68 h · ng · mL -1,468.59 ± 61.25 ng · mL -1 and 4.0 ± 0.71 h, respectively.These parameters of sustained release capsules II were 4746.44 ± 317.22 h · ng · mL -1, 512.00 ± 72.29 ng · mL -1, and 4.0 ± 0.71 h. The bioavailability of Naftopidil-containing capsules I and II with nafampiril capsules as reference preparation were 133.40 ± 12.72% and 137.53 ± 17.49%, respectively. The pharmacokinetic parameters of the two bioadhesive capsules There is no significant difference between. The bioadhesion technique can significantly improve the bioavailability of naftopidil.