壳聚糖基卡托普利的合成及其释药研究

克服水溶性药物的突释现象,可减少给药次数,提高疗效.本研究以卡托普利为模型药物,壳聚糖为载体,采用耦合的方法,设计合成了壳聚糖-卡托普利和壳聚糖-赖氨酰-卡托普利两种新的键连型壳聚糖基载药体系,产物结构经IR、1 H NMR和MS表征;并测试了两种化合物在PBS缓冲溶液(pH=7.4)和HCl-KCl缓冲溶液(pH=1.2)中72h的累积释药率:壳聚糖-卡托普利的累积释药率分别为59.2%和78.4%,壳聚糖-赖氨酰-卡托普利的累积释药率分别为55.2%和76.4%.结果表明,两种键连型载药体系均消除了突释现象,具有很好的缓释效果,这将有望成为水溶性药物的理想载药体系.

Synthesis of Chitosan-based Captopril Derivatives and Its in vitro Release

In order to overcome the burst release of water-soluble drugs, reduce dosing frequency and improve curative effect,two new bond-linking type drug-loaded control-releasing systems: Chitosan-Captopril and Chitosan-Lysyl-Captopril were synthesized from captopril as a model drug and chitosan as carriers. The products were characterized by IR, 1H NMR and MS. The accumulation of drug release rates of Chitosan-Captopril are 59.2% in PBS buffer (pH=7.4) and 78.4% in HCl-KCl buffer (pH=1.2). The accumulation of drug release rates of Chitosan-Lysyl-Captopril are 55.2% in PBS buffer (pH=7.4) and 76.4% in HCl-KCl buffer (pH=1.2). The results show that the two kinds of drug-loaded systems eliminate the phenomenon of burst releasing and have excellent sustained release properties, which are expected to become the ideal control-releasing system of water-soluble drugs.