曼尼地平固体分散体的制备、表征及溶解度增强

Laxmi Raj A, Y. Kumar
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引用次数: 0

摘要

采用溶剂蒸发法,采用Labrafac PG、Kolliwax RH 40、Soluplus、Kolliwax GMS II、Kolliphor EL和SLS等新型载体,以载药比配制曼尼地平固体分散体。对配方进行了物理外观、溶解度和体外溶出度的研究。采用Kolliwax GMS II和SLS对优化后的配方进行了表征,通过溶解度、溶出度等参数对优化后的配方SD13进行了表征。优化处方在90 min内的释药率为99.41±5.38%。对固体分散体进行粉末x射线衍射研究表明,在溶剂蒸发法制备的固体分散体中,曼尼地平以非晶态存在。此外,扫描电镜研究表明结晶曼尼地平转化为无定形。因此,以Kolliwax GMS II为亲水性载体的固体分散体可以成功地用于改善曼尼地平的溶解度和溶出度。
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Formulation, Characterization and Solubility Enhancement of Manidipine Solid Dispersions
The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS.  The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine.  
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