灯盏乙素-胡椒碱共无定型复合物的制备及其体外释放度评价

Preparation of scutellarin-piperine co-amorphous complex and its in vitro release

目的制备灯盏乙素-胡椒碱共无定型复合物,以期达到增加药物溶出度的目的。方法采用溶剂法制备灯盏乙素-胡椒碱共无定型复合物,运用差示扫描量热法(DSC)、扫描电镜法(SEM)、X射线粉末衍射法(XRD)和红外光谱(IR)等分析方法对其微观结构进行表征和分析,并对其体外溶出行为进行考察,研究灯盏乙素和胡椒碱的共无定型复合物的形成情况。结果 DSC和XRD结果显示灯盏乙素与胡椒碱均以无定型形式存在,IR谱图提示二者之间有分子间作用。体外溶出结果表明,相较于灯盏乙素和胡椒碱,复合物中二者在水中的累积溶出率均得到较大提高。结论所制备的灯盏乙素-胡椒碱共无定型复合物能显著改善灯盏乙素和胡椒碱的溶出度,所形成的药物-药物共无定型药物系统,为提高难溶性药物的溶出速率和溶解度提供了一定的参考。

Objective To prepare scutellarin-piperine co-amorphous complex, in order to improve their dissolution and solubility. Methods Scutellarin-piperine co-amorphous complex was prepared using solvent evaporation method. The microscopic structure and physicochemical properties of co-amorphous complex were analyzed using differential scanning calorimetry （DSC）, scanning electron microscopy （SEM）, X-ray powder diffraction （XRD）, and infrared vibrational spectra （IR）. And its in vitro release also was investigated. The formation of the co-amorphous complex in scutellarin and piperine was studied. Results DSC and XRD analysis suggested that scutellarin and piperine may be present as amorphous substance. IR results indicated molecular interactions between scutellafin and piperine. The in vitro release determination results of scutellarin-piperine co-amorphous complex showed accumulated dissolution rate of scutellarin and piperine could both be improved. Conclusion The drug-drug co-amorphous system can provide certain reference for insoluble drugs to improve their dissolution and solubility.