右旋布洛芬/盐酸改性蒙脱土的制备及体外释放研究

Study on Preparation and in Vitro Release of Acid-montmorillonite Drug Delivery Sustained-release Systems

摘要:

目的：以酸改性蒙脱土为药物载体，制备右旋布洛芬/酸改性蒙脱土复合物，提高右旋布洛芬的载药量，并探索载药复合物在不同释放介质中的释放规律。方法：首先用浓度为5%~20%的盐酸对蒙脱土进行预处理，利用X-射线衍射（XRD）、比表面积测定（BET）、扫面电子显微镜（SEM）等表征方法对蒙脱土进行结构表征，筛选最佳酸处理浓度；然后用溶液插层法将右旋布洛芬负载于酸化后的蒙脱土上，制得右旋布洛芬/酸改性蒙脱土复合物；采用透析法对右旋布洛芬/酸改性蒙脱土复合体系进行体外释放实验。结果：经酸改性后蒙脱土的结构发生改变，当酸浓度为15%时，蒙脱土的比表面积达到最大值246 m2/g。上载右旋布洛芬后，载药量最大可达352.4 mg/g。体外释放实验表明，右旋布洛芬/酸改性蒙脱土的累积释药百分量受pH的影响，当pH为1.2时，其累积释药百分量为18.6%，当pH为6.8时，则为89.3%。结论：盐酸改性蒙脱土有助于提高药物的负载量，右旋布洛芬/酸改性蒙脱土复合物具有良好的缓释作用并有一定的pH响应性，有望制成肠道缓释口服药物制剂。

Abstract:

Objective: In order to improve the drug loading, the acid-montmorillonite as the carrier of S( )-ibuprofen, and prepared S( )-ibuprofen/acid-modified montmorillonite complexes, to explore the drug compounds release law in different pH values. Methods: The montmorillonite was treated by different concentrations of hydrochloric acid (5%~20%), and characterized by powder XRD, BET, SEM and so on. The effects of the pH of release media on in vitro release of the S( )-ibuprofen were assessed by a dialysis method. Results: The acid concentration of 15%, the specific surface area of montmorillonite is maximum 246 m2/g, and the drug-loading has increased to 352.4mg2/g. In vitro release experiments showed that the cumulative release percentage amounts of the composite effect of pH, In the artificial gastric juice (pH 1.2) and in the artificial intestinal juice (pH 6.8) , the in vitro cumulative amount of the composites were respectively, 18.6 % and 89.3 %. Conclusion: Acid-treatement can improve the drug-loading, and the drug compounds has pH response and sustained-release behavior. This composites is expected to be sustained-release and intestinal oral preparation.