环孢素-泊洛沙姆188固体分散体的体外评价

目的以泊洛沙姆188（F68）为载体制备环孢素（CsA）固体分散体并考察其体外溶出。方法以溶剂一熔融法制备固体分散体，以差示扫描量热法（DSC）和X．射线衍射法鉴定CsA在体系中的存在状态，以FTIR表征药物与载体的相互作用，以摇瓶法测定CsA的溶解度，按《中国药典》溶出度第三法测定CsA从物理混合物和固体分散体中的溶出。结果X-射线衍射图谱显示CsA结晶衍射峰消失，提示药物以无定形或分子状态存在于固体分散体中。FTIR结果表明药物与载体间无相互作用。药物溶解度和溶出度均随着F68比例的增加而增大，固体分散体和物理混合物60min的累积溶出百分率分别为99．32％和75．41％，两者具显著性差异（P〈0．01）。结论F68能提高CsA的溶解度和溶出度，可用来制备CsA的固体剂型。

In vitro evaluation of solid dispersions of ciclosporin with poloxamer 188

AIM To prepare solid dispersions of ciclosporin (CsA) with poloxamer 188 (F68) and examine the dissolution properties of CsA from this system. METHODS Solid dispersions containing CsA and F68 were prepared by solvent-melt method. The differential scanning calorimeter (DSC) and powder X-ray diffractometry (PXRD) were used to identify the state of the drug existence in the system. Solubility of CsA in water from solid dispersions and physical mixtures was determined by shake-flask method. Dissolution of drug was conducted at 37 ℃. RESULTS CsA existed in the system in the form of amorphous or solid solution state from PXRD. Solubility and dissolution of CsA increased with the formation of physical mixtures and solid dispersions. The accumulative release of CsA within 60 min was 99.32 % for solid dispersion and 75.41 % for physical mixture (P < 0.01). CONCLUSION F68 can enhance the solubility and dissolution of CsA. It could be a candidate carrier for a solid dosage form of CsA.