载塞克硝唑Poloxamer188■复合聚L-乳酸薄膜的药物释放行为

Drug Release Behavior of Secnidazole Poloxamer188■ Composite Poly L-lactic Acid Film

目的考察聚L-乳酸薄膜中Poloxamer188■复合量和塞克硝唑载量对药物包裹和释放行为的影响。方法二氯甲烷溶解塞克硝唑、Poloxamer188■和聚L-乳酸,形成均相溶液后玻璃板上铺膜。扫描电子显微镜观察薄膜的微观形态,广角X-射线衍射、差示热分析考察材料复合和载药状态。高效液相色谱-紫外分光光度测定从薄膜中释放至介质中的塞克硝唑的浓度,对时间做其累积释放曲线,并对方程回归探讨其释放机理。结果肉眼观察当薄膜中塞克硝唑的载量提高时,薄膜由透明变半透明且开始泛白。扫描电子显微镜下薄膜表面均光滑,无分相结构和晶体析出。差示热分析和X-射线衍射结果说明塞克硝唑-Poloxamer188■-聚L-乳酸在薄膜中复合良好。塞克硝唑和Poloxamer188■在薄膜中载量的升高均有助于药物释放量的增加,但是前者对药物释放量的影响大于后者。塞克硝唑和Poloxamer188■载量同步提高后可以使前者的释放量达到载量的90%以上。塞克硝唑释放曲线可被Peppas方程式较好拟合。结论可以通过Poloxamer188■和药物本身的复合量调节塞克硝唑从聚L-乳酸薄膜中的释放,直至释放较为完全。

Objective To investigate the effect of Poloxamer188■ compound amount and secnidazole loading on drug encapsulation and release behavior in poll-lactic acid film.Methods Dichloromethane dissolves secnidazole,Poloxamer188■ and poly(l-lactic acid),forming homogeneous solution and coating the glass plate.The microstructure of the film was observed by scanning electron microscopy,and the composite and drug loading states were investigated by wide-angle X-ray diffraction and differential thermal analysis.The concentration of secnidazole released from the film to the medium was determined by high performance liquid chromatography-ultraviolet spectrophotometry,the cumulative release curve was made with time,and the release mechanism was discussed by regression equation.Results Observed by naked eye,the film changed from transparent to translucent and began to whiten when the amount of secnidazole in the film increased.The surface of the film is smooth under scanning electron microscope,and there is no phase separation structure and crystal precipitation.The results of differential thermal analysis and X-ray diffraction showed that secnidazol-Poloxamer188■-poly(L-lactic acid)had good composite properties in thin films.The increase of the loading of secnidazole and Poloxamer188■ in the film contributed to the increase of drug release,but the effect of secnidazole on drug release was greater than that of Poloxamer188■.The release amount of secnidazole and Poloxamer188■ reached more than 90%of the load when the load of secnidazole and Poloxamer188■ increased synchronously.Secnidazole release curve can be well fitted by Peppas equation.Conclusion The release of secnidazole from poly(L-lactic acid)films can be regulated by the compound amount of Poloxamer188■ and the drug itself until the release is complete.