酮洛芬-聚乙烯吡咯烷酮固体分散物的制备及其体外溶出度的研究

目的提高难溶性药物酮洛芬体外溶出速度。方法以聚乙烯吡咯烷酮(PVPK30)为载体,制备药物与载体不同比例的固体分散物及物理混合物,采用X射线衍射和红外吸收方法,比较二者及药物的结晶形态,并进行体外药物溶出度的测定。结果固体分散物体外溶出速率明显高于物理混合物及酮洛芬原料的体外溶出速度,且随载体比例增加而增大。固体分散物的X射线衍射及红外吸收图谱确定了酮洛芬以无定形态分散在载体中,放置6个月后,固体分散物X射线衍射图谱没有明显变化。结论药物与载体以合适比例制备的固体分散物可以明显提高药物体外溶出速度。

Preparation and dissolution of the solid dispersions of ketoprofen-polyvinylpyrrolidone

Objective To enhance the dissolution rate of ketoprofen(KPF) by adopting the solid dispersion method.Methods Solid dispersions and physical mixtures with different proportion of weight of KPF and polyvinylpyrrolidone(PVP) were prepared by using PVP as a carrier.The physical states of KPF were investigated by X-ray powder diffraction and IR analysis.The dissolution rates of KPF in solid dispersions and in physical mixtures were also compared.Results The dissolution rate of KPF-PVP_(K30) solid dispersions was much faster than that of the physical mixtures,and increased with the increase of the proportion of the carrier.The X-ray power diffraction and IR showed that the drug in the solid dispersion existed in amorphous form,and there were no significant changes for the solid dispersion kept in dry place for six months.Conclusions The dissolution rate of KPF can be improved greately by solid dispersions with proper ratio of drug and carrier.