聚谷氨酸-表阿霉素偶合物的稳定性研究

STABILITY OF POLYGLUTAMIC ACID-EPIRUBICIN CONJUGATES

目的 :考察腙键连接的聚谷氨酸 -表阿霉素的稳定性及pH敏感性。方法 :样品置于不同试验条件下 ,于不同时间取样 ,过Sephadex柱分离测定 ,计算偶合率 /解离率。结果 :表阿霉素与聚谷氨酸交联后稳定性提高 ;偶合物在中性条件下稳定性较好 ,4℃避光贮存 4个月偶合率在 88%以上 ;随着pH值降低 ,偶合物解离率升高 ,说明偶合物对酸敏感。结论 :腙键连接的聚谷氨酸 -表阿霉素在中性条件下稳定 。

AIM To study the stability and pH-sensitivity of polyglutamic acid-epirubicin conjugates.METHODS The conjugates were separated from free drug by the Sephadex column after treated under different conditions for different time period.The percent of drug conjugated/released was obtained by determining the drug concentration at 495nm.RESULTS The stability of Epirubicin in solution improved after conjugated to the macromolecular carriers. The conjugates were stable in neutral solution, with 88 percent of drugs conjugated after 3 months storage under darkness at 4℃.The ratio of drug release increased as pH decreased,which indicates that the conjugates are sensitive to pH.CONCLUSION Polyglutamic acid-epirubicin conjugates are stable under neutral condition, while in slight acidic solution the conjugates are likely to release free drugs.