硫氰酸红霉素固体分散体的制备及其体外溶出度测定

目的 采用固体分散技术提高硫氰酸红霉素的体外溶出度.方法 选用聚乙二醇6 000和聚维酮k30为载体材料,分别采用熔融法和溶剂法制备硫氰酸红霉素固体分散体(ET-SD).采用X-射线衍射法、差示扫描量热法对ET-SD进行鉴定,并对ET-SD进行体外溶出度的测定.结果 固体分散体的X-射线衍射及DSC图谱确定了硫氰酸红霉素以无定形态分散在载体中,体外溶出度实验表明其硫氰酸红霉素的溶出较原料药、物理混合物均有明显提高.结论 固体分散技术可以提高硫氰酸红霉素的体外溶出度,这为更有效地利用硫氰酸红霉素等生物利用度低药物提供一种新的制剂手段.

Studies on Preparation and Dissolution of the Solid Dispersions of Erythromycin Thiocyanate

Objective To enhance the dissolution rate of erythromycin thiocyanate(ET)which is a poorly water-soluble drug by solid dispersion.Methods Solid dispersions of erythromycin thiocyanate(ET-SD) were prepared by melting or by solution,with polyethylene glycol(PEG) or polyvinylpyrrolidone(PVP) as a carrier.The physical states of ET were investigated by X-ray powder diffraction analysis and DTA.The dissolution rate of ET from solid dispersions and that from physical mixtures were also compared.Results The X-ray power diffraction and DSC spectrum of the solid dispersion showed that erythromycin thiocyanate existed in amorphous form in the carrier.The dissolution of ET solid dispersions was much faster than that of ET and the physical mixtures.Conclusion The dissolution rate of ET can be enhanced by solid dispersion;this may provide a new pharmaceutical manner for more efficaciously utilizing ET and other medicines which have low bioavailability.