口服降钙素肠溶微粒的制备及其降血钙作用的实验研究

Preparation and bioavailability study of calcitonin oral microparticle in rats

目的 :制备降钙素口服肠溶微粒。 方法 :以二酮哌嗪为载体材料 ,采用单凝聚法 ( self-assembly)制备降钙素肠溶微粒 ,对微粒的性状、体外溶出、在大鼠体内降血钙作用及生物利用度进行观察。 结果 :微粒粒径为 1～ 3μm,粒度分布较为均匀 ,含药量为 0 .42 % ,包封率为 91.1% ,药物在人工胃液中 2 h基本无释放 ,在人工肠液中完全释放为 6 h,大鼠口服该微粒后3h就有明显的降血钙作用 ,持续时间达 12 h以上。 结论 :降钙素肠溶微粒具有缓释作用 。

Objective: To prepare the calcitonin oral microparticle. Methods: The oral delivery system of salmon calcitonin was made using diketopiperazine microparticles as carrier by the method of sole solifification. The parameters including the shape of microparticle,dissolving in vitro , the effect of reducing bleed calcium and bioavailability etc . were observed. Results: The diameter of the microparticles was 1 3 μm, and the drug concentration was 0.42%. The rate of encapsulating was 91.1%. The drug did not release within 2 h in artificial gastric fluid and completely released in artificial intestinal fluid within 6 h. The microparticles had obvious effect of reducing bleed calcium 3 h after it was taken, the effect lasted for 12 h. Conclusion: The microparticles of salmon calcitonin release slowly and have better effects of reducing bleed calcium by oral delivery system.