瑞格列奈固体分散体的制备及体外溶出

Preparation and in vitro evaluation of repaglinide solid dispersions

目的制备瑞格列奈的固体分散体,提高瑞格列奈的体外溶出度。方法以聚乙二醇6000(polyethylene glycol 6000,PEG6000)作为载体,采用溶剂-熔融法制备不同处方的瑞格列奈固体分散体,进行溶出度考查。采用红外光谱、差示扫描量热(differential scanning calorimetry,DSC)与X-射线衍射(X-ray diffraction,XRD)对瑞格列奈固体分散体进行物相分析。结果与瑞格列奈原料和物理混合物相比,固体分散体可显著提高瑞格列奈的体外溶出度,物相鉴定表明,瑞格列奈大部分以无定形状态分散于PEG6000中,提高了药物的体外溶出度。结论制备瑞格列奈的PEG6000固体分散体能显著提高药物的体外溶出度,可满足速释制剂的要求。

Objective To improve in vitro release of repaglinide, the technology of solid dispersion was used to prepare repaglinide solid dispersion. Methods Repaglinide solid dispersions were prepared by melting-sol- vent method using PEG6000 as carrier. The dissolution characteristics of pure drug and physical mixture and solid dispersions were compared. The existing forms of repaglinide in dispersions were investigated by using fourier-transform infrared（FTIR） spectroscopy, differential scanning calorimetry （DSC） and X-ray diffrac- tion （XRD）. Results The dissolution of repaglinide solid dispersion was significantly higher than that of the pure drug and physical mixture. The DSC and XRD studies indicated that most repaglinide existed as amo- rohous state in solid dispersions. Conclusions The solid dispersions can increase the in vitro dissolution rate, which satisfy the demand for the design of the immediate-release dosage form.