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目的 通过对胰岛素聚氰基丙烯酸正丁酯纳米粒(IPN)在油介质(含有 0 .5%吐温 20和 5%维生素E的豆油)中的稳定性及其口服后对链脲霉素引起的糖尿病大鼠降血糖作用的研究,希望得到一种稳定而有效的胰岛素纳米粒口服制剂。方法 依据IPN中的胰岛素含量,IPN的平均粒径和粒子跨度,及其体外释药来评估其稳定性。将IPN分散在含有 0 .5% 吐温 20,pH2 0的水溶液中作为对照。结果 研究表明,不论样品是在(25±2)℃条件下避光放置 1年,还是在体外与 3种消化道酶 37℃酶解 30min,油介质中的IPN都比水介质中IPN稳定性好。依据单剂量po给药后,在 0-144h血糖降低的百分数与时间曲线上面积(AAC)可知,poIPN的油溶液(50u·kg-1 )相对于sc胰岛素(2u·kg-1 )的生物利用度为 22 .4%,明显高于poIPN水溶液的相对生物利用度(15. 5% )。结论 分散在油介质中的IPN具有较好的稳定性和相对较高的生物利用度,因此,含有 0 .5%吐温 20和 5%维生素E的豆油有望成为口服胰岛素聚氰基丙烯酸正丁酯纳米粒的有效而稳定的分散介质。
OBJECTIVE To investigate the stability of insulin polybutylcyanoacrylate nanoparticles (IPN) in oily medium (soybean oil containing 0.5% Tween 20 and 5% vitamin E) and oral administration of streptozotocin Of diabetic rats hypoglycemic effect, hoping to get a stable and effective oral preparation of insulin nanoparticles. Methods The stability of IPNs was evaluated based on their insulin content, IPN mean particle size and particle spans, and their in vitro release. IPN was dispersed as a control in an aqueous solution containing 0 .5% Tween 20, pH 20. Results The results showed that IPN in oil medium was higher than IPN in aqueous medium, regardless of whether the sample was placed in the dark at (25 ± 2) ℃ for 1 year or in vitro with 3 digestive enzymes at 37 ℃ for 30 min it is good. The poIPN oil solution (50u · kg-1) vs. sc-insulin (2u · kg-1) creatures was shown to be proportional to the percentage of time to blood glucose reduction (AAC) at 0-144h after single dose po administration The degree of utilization was 22.4%, which was significantly higher than the relative bioavailability of poIPN solution (15.5%). Conclusion IPN dispersed in oil medium has good stability and relatively high bioavailability. Therefore, soybean oil containing 0.5% Tween 20 and 5% vitamin E is expected to become oral insulin polybutylcyanoacrylate An effective and stable dispersing medium for ester nanoparticles.