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首页> 外文期刊>International Journal of Pharmacy and Pharmaceutical Sciences >ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NEBIVOLOL BY SOLID DISPERSION TECHNIQUE
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ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NEBIVOLOL BY SOLID DISPERSION TECHNIQUE

机译：固体分散技术提高奈必洛尔的溶解度和溶解度

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Objective: Solubility is greater challenges for formulation which can be explain by different technological approaches during the pharmaceutical product development and to improve water solubility and drug release respectively. Methods: The solid dispersions of nebivolol were prepared in ratio 1:1, 1:3, 1:5 and 1:7 by fusion and solvent evaporation method using PEG 6000 and PVP K30 as carriers to enhance solubility of compound. Results: All the solid dispersions were evaluated for drug content, phase solubility, in vitro dissolution study. Deferential Scanning Calorimetric (DSC) and Fourier Transformer Infra Red (FTIR) showed no chemical interaction between the drug and its carriers. Solubility of PEG 6000 and PVP K30 indicates a linear relationship (A L type of curve) in the investigated polymer concentration range. The Gibb’s free energy showed declined trend with increase in the carrier concentrations. The uniformly of drug content was found in all solid dispersions. The drug release obtained from different drug-carrier concentration level fitted to different kinetic model and it was found that solid dispersions exhibited fickian diffusional characteristics and best fitted to higuchi model. A PVP K30 solid dispersion (1:7 ratio) prepared by solvent evaporation method showed faster dissolution rate (94.38 %) in 30 min among studied solid dispersions.. Conclusion: The overall results showed that process of nebivolol transfer from water to carrier solution is more favorable at higher level of PVP K30. The solid dispersion of drug: PVP K 30 (1:7 ratio) prepared by solvent evaporation method was found to be optimum in term of solubility and dissolution rate. Hence, we can concluded that solubility of nebivolol can be enhanced using this carrier ratio. Keywords: Nebivolol, Solid dispersion, Fusion method, Solvent evaporation method.
机译：目的：溶解度是制剂面临的更大挑战，这可以用药物开发过程中的不同技术方法来解释，并分别改善水溶性和药物释放。方法：采用聚乙二醇6000和PVP K30为载体，通过熔融和溶剂蒸发法，以1：1、1：3、1：5和1：7的比例制备奈必洛尔固体分散体，以提高化合物的溶解度。结果：评估了所有固体分散体的药物含量，相溶解度，体外溶出度研究。差示扫描量热法（DSC）和傅立叶红外光谱仪（FTIR）显示该药物与其载体之间没有化学相互作用。 PEG 6000和PVP K30的溶解度表明在所研究的聚合物浓度范围内呈线性关系（曲线的A L型）。随着载流子浓度的增加，吉布的自由能呈下降趋势。在所有固体分散体中均发现药物含量均匀。从不同的药物载体浓度水平获得的药物释放适合于不同的动力学模型，并且发现固体分散体表现出菲克扩散特性并且最适合于higuchi模型。通过溶剂蒸发法制得的PVP K30固体分散体（比例为1：7）在30分钟内显示出较快的溶解速率（94.38％）。结论：总体结果表明奈必洛尔从水转移到载体溶液的过程是PVP K30级别越高，越有利。发现通过溶剂蒸发法制备的药物：PVP K 30（1：7比率）的固体分散体在溶解度和溶解速率方面是最佳的。因此，我们可以得出结论，使用该载流子比例可以提高奈必洛尔的溶解度。关键词：奈必洛尔，固体分散体，熔融法，溶剂蒸发法。

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