环孢素-PVP固体分散体的体外研究

 目的以聚维酮(PVP)为载体制备环孢素(CyA)固体分散体,并考察其体外溶出。方法以溶剂法制备固体分散体,以X-射线衍射法鉴定CyA在体系中的存在状态,用红外光谱法检查药物与载体间是否具相互作用,以摇瓶法测定CyA在不同浓度十二烷基硫酸钠(SLS)中的溶解度,按《中国药典》2005年版溶出度第三法测定CyA从固体分散体中的溶出。结果X-射线衍射图谱显示CyA结晶衍射峰消失,药物以无定形或分子状态存在于固体分散体中;红外光谱的结果表明,药物与PVP间无分子间作用力。药物从固体分散体中的溶出度比原药粉末显著提高,且随着PVP比例的增加而增大。结论PVP能显著提高CyA的溶出度,可进一步用来制备CyA的固体剂型。

Preparation and in Vitro Study of Solid Dispersions of Cyclosporine A

OBJECTIVE To prepare and characterize the solid dispersions of cyclosporine A(CyA)and PVP with the intention of improving drug dissolution.METHODS Solid dispersions containing CyA and PVP were prepared by solvent method.Powder X-ray diffractometry(PXRD)was used to identify the state of the drug in the system.The Fourier-transformed infrared(FTIR)spectra were recorded to detect the possible molecular interaction between CyA and PVP.The solubility of CyA in aqueous solutions of sodium lauryl sulfate(SLS)was determined by shake-flask method.The dissolution of drug was conducted by apparatus No.3 method in 0.1% SLS at 37 ℃.RESULTS CyA existed in the solid dispersion at amorphous forms or solvates from PXRD.The FTIR revealed no significant interaction between CyA and PVP.The dissolution rate of CyA was increased dramatically after the formation of solid dispersion compared with the pure drug powder.CONCLUSION PVP can enhance the dissolution rate of CyA dramatically.It could be used as a candidate carrier for the development of the solid form of CyA.