G2.0聚酰胺-胺树状大分子及其水杨醛修饰物体外释药性能的研究

Study on the drug release in virto of G2.0 PAMAM and G2.0 PAMAM-SA

目的考察G2.0聚酰胺-胺树状大分子(PAMAM)及水杨醛修饰物(PAMAM-SA)的释药机制。方法用紫外可见分光光度法检测2种大分子环境敏感性及对氧氟沙星的增溶作用。氧氟沙星含量测定采用HPLC法:ODS-C18色谱柱(150mm×4.6mm,5μm);流动相为乙腈、三乙胺溶液(磷酸调pH 4.0)(14∶86);检测波长294nm;流速1.0mL·min-1;柱温40℃。结果氧氟沙星单独释放80%需要2h,G2.0PAMAM-氧氟沙星复合物释放氧氟沙星80%需要5h,G2.0PAMAM-SA-氧氟沙星复合物释放氧氟沙星80%需要2.5h。结论 2种大分子具有环境敏感性,对氧氟沙星具有增溶、缓释作用,2种复合物形成是大分子的氨基阳离子与氧氟沙星的羧基阴离子之间静电作用的结果。

Objective To investigate the release mechanism of G2.0 PAMAM and G2.0 PAMAM-SA.Methods The UV spectro-photometry was employed to measure the environmental sensitivity of G2.0 PAMAM and G2.0 PAMAM-SA and their effects on the solubility enhancement of ofloxacin （OFL）.The content of OFL was measured by an HPLC method with an ODS-C18 chroma-tographic column（150 mm × 4.6 mm,5μm）which was kept at 40 ℃,with a mobile phase of acetonitrile-triethylamine （14∶86, adjusting pH to 4.0 by phosphoric acid）at a flow rate of 1.0 mL ·min-1 and the detection wavelength was 294 nm.Results It took 2 h for 80% OFL to release alone,5 h to release 80% OFL from G2.0 PAMAM-OFL compound and 2.5 h to release 80%OFL from G2.0 PAMAM-SA-OFL compound.Conclusion G2.0 PAMAM and G2.0 PAMAM-SA are environmentally sensitive, and it is an effective way to enhance the solubility and suspend the release of OFL.The formations of the two compounds may re-sult from the interaction between the amino group of PAMAMs and the carboxyl group of OFL.