盐酸小檗碱明胶微球的制备及其性能表征

Preparation and characterization of berberine hydrochloride gelatin microspheres

以明胶为载体,采用乳化-化学交联法制备盐酸小檗碱微球。以包封率及载药量为评价指标,通过Box-Behnken效应面法确定盐酸小檗碱明胶微球的最优处方,并通过扫描电子显微镜(SEM)、傅里叶变换红外光谱(FT-IR)、X射线衍射(XRD)、差示扫描热量法及热重分析(DSC&TG)对盐酸小檗碱明胶微球进行表征,同时以体外释放度考察其释药情况。盐酸小檗碱明胶微球的最优处方为明胶质量分数12%,投药量25%,油水比值4.79。所得盐酸小檗碱明胶微球的载药量为(19.97±0.17)%、包封率为(67.71±0.93)%,外观圆整、平均粒径为(131.81±1.58)μm,DSC、XRD和红外光谱分析显示微球中盐酸小檗碱以无定型形式存在。体外释放结果表明,微球中盐酸小檗碱在pH值为2.5和7.4的磷酸盐缓冲溶液中12 h累积释放率约为91%和95%,说明该明胶微球具有一定的缓释作用。

Berberine Hydrochloride microspheres were prepared by emulsification-chemical cross-linking method using gelatin as carrier.With the encapsulation efficiency and drug loading as evaluation indexes,the effects of gelatin concentration,dosage and oil-water ratio were investigated by Box-Behnken design and response surface method.Scanning electron microscopy(SEM),Fourier transform infrared spectroscopy(FT-IR),X-ray diffraction(XRD),differential scanning calorimetry and thermogravimetric analysis(DSC&TG)were used for characterization.At the same time,the drug release property was evaluated with the drug release in vitro.The optimal prescription was determined as follows:the optimum gelatin mass fraction was 12%,the dosage was 25%and the oil-water ratio was 4.79.The drug loading rate and encapsulation rate of microspheres prepared by the optimized prescription was(19.97±0.17)%and(67.71±0.93)%,respectively.The microspheres had a round appearance with an average particle size of(131.81±1.58)μm.The results of DSC,XRD and FT-IR spectroscopy showed that berberine hydrochloride was present in the microspheres in an amorphous form.The cumulative release rates in vitro of 12 h were about 91%and 95%in phosphate buffered solutions at pH 2.5 and 7.4,respectively indicating that the gelatin microspheres had a sustained release effect.