氯诺昔康固体分散体的热焓变化及溶出度改善特性

目的：制备非甾体抗炎药氯诺昔康的固体分散体以提高难溶性氯诺昔康体外溶出速率。研究载体类型及药物-载体混合比例对固体分散体体外溶出速率的影响，并根据：DSC测定结果考察各种混合物中氯诺蕾康热焓变化的特性。方法：分别以Poloxamer188、PVPK30和Gelucire 44／14为载体，采用溶剂蒸发法制备氯诺昔康固体分散体。采用浆法进行体外溶出度试验。根据DSC实测数据考察热焓变化特征。结果：固体分散体体外溶出速率的先后顺序为PXM，PVP，GLC，物体混合物顺序为PXM，GLC，PVP，随着载体比例的增加，PVP和泊洛沙姆固体分散体溶出速率常数增加。DSC圈谱表明，随着载体比例的增加，氯诺昔康放热峰的起始温度和△H降低，当氯诺昔康的泊洛沙姆比例为1：10时，药物以无定形状态存在于结晶性的泊洛沙姆中，从而使其在体外具有最快的溶出速率。结论：载体类型及药物-载体比例影响氯谱诺昔康固体分散体的体外溶出特性及热焓变化。

Characteristics of Enthalpy Change and Dissolution Improvement of Lornoxicam from Solid Dispersions

AIM: Solid dispersions of water-insoluble lornoxicam were prepared in order to improve their dissolution rate.Dissolution study and differential scan calorimetry(DSC) study were performed to investigate the characteristics of enthalpychange and comparative dissolution improvement. METHOD: Lornoxicam solid dispersions were prepared by classical solventevaporation technique with PVP K-30, Gelucire 44/14 and poloxamer 188 as carriers. The effects of main process variables,including types of carriers and mixing ratios, on the physicochemical characteristics were investigated by dissolution study andDSC study. RESULT:The dissolution rate constants were olbserved to depend on the types of carriers and mixing ratios. Onsettemperature and entbalpy change of lornoxicam from DSC profiles were found to decrease significantly with the increase of mix-ing ratios. Lornoxicam can be converted to an amorphous state in crystalline PXM, which is consistent with the excellent disso-lution improvement of PXM coevaporates in vitro experiment. CONCLUSION: The types of carriers and drug-carrier ratio hadgreat effect on the characteristics of in vitro dissolution and enthalpy change of lornoxicam solid dispersion.