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Preparation and In Vivo Evaluation of Nimodipine Solid Dispersions

机译:尼莫地平固体分散体的制备及体内评价

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ABSTRACT Nimodipine, a poorly soluble drug, was considered to be fit for solid dispersions to improve its solubility and bioavailability. Our study intended to prepare Nimodipine solid dispersions by solvent evaporation method using various novel polymers. Solubility and dissolution studies indicate that Kolliwax RH 40 and SLS is the most suitable polymer. The solubility studies were corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96±5.15% in about 90 minutes. In-vitro release data from several formulations containing XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. From in vivo bioavailability studies, Cmax of the optimized formulation SD15 was 4.34±0.08ng /ml, was significantly higher as compared to pure drug suspension, i.e., 2.78±0.35ng/ml. Tmax of optimized formulation was decreased significantly when compared with pure drug (1.00±0.05hr, 2.00±0.01hr), AUC0-α and AUC0-t for optimized solid dispersion formulation was significantly higher (p
机译:摘要尼莫地平是一种难溶药物,被认为适合用于固体分散体,以改善其溶解度和生物利用度。我们的研究旨在使用各种新型聚合物通过溶剂蒸发法制备尼莫地平固体分散体。溶解度和溶解度研究表明,Kolliwax RH 40和SLS是最合适的聚合物。溶解度研究与溶出数据相对应,发现制剂SD15在约90分钟内具有最高的药物释放,约98.96±5.15%。包含XRD和SEM研究的几种配方的体外释放数据表明,优化配方SD15中没有结晶性。 FTIR研究表明,所制备制剂的所有组分之间都具有良好的药物赋形剂相容性。根据体内生物利用度研究,优化制剂SD15的Cmax为4.34±0.08ng / ml,与纯药物悬浮液相比明显更高,即2.78±0.35ng / ml。与纯药物(1.00±0.05hr,2.00±0.01hr)相比,优化配方的Tmax明显降低,优化固体分散体配方的AUC0-α和AUC0-t显着更高(

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