口服降钙素微粒制备工艺的研究

目的:制备口服降钙素微粒给药系统.方法:选用氨基酸环合脱水、环二聚化的方法合成二酮哌嗪,以二酮哌嗪作为包裹材料采用固化凝聚法制备降钙素微粒,通过正交设计筛选降钙素微粒的制备工艺,并对其物理形态、体外释放进行了研究.结果:微粒的物理性质稳定,在水溶液中的分散性好,平均粒径1～3μm,药物回收率74%,微球主药含量1.36%,体外释放符合零级方程.结论:此微粒系统在低pH条件下稳定,在生理环境中可溶解,可作为在胃液中不稳定药物特别是蛋白质和多肽类药物口服给药载体.

Study on the Preparation of the Micropaticle of Oral Calcitonin

Objective: The preparation of the oral delivery system of salmon calcitonia. Method: The researches mainly focused on the synthesis of diketopiperazine which was formed by cyclodimerization and dehydration of amino acids. The microparticles containing salmon calcitonin were prepared by adding acid to solidify the basic solution of diketopiperazine. The drug which incorporated into diketopiperazine microparticles was physically stable. The parameters of the pharmaceutic preparation were studied. Results: These types of microparticles had the diameter of 1-3 um and the rate of drug recovery was 74%. Drug concentration was contained 1. 36%. The release (in vitro) was ruled by the zero order mechanism. Discussion: Drug delivery systems had been developed base on the formation of diketopiperazine microparticles. Which were stable at low pH and disintegrates at physiological pH, and is particularly useful for oral drug delivery.