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首页> 外文期刊>American Journal of Drug Discovery and Development >Modification of Felodipine Properties using Spherically Agglomerated Solid Dispersions
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Modification of Felodipine Properties using Spherically Agglomerated Solid Dispersions

机译：球形团聚固体分散体对非洛地平性质的改性

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摘要

The objective of the present work was to enhance the solubility, dissolution rate and micromeritic properties of Felodipine (FL) a poorly water soluble antihypertensive, using spherical agglomeration by Quasi Emulsion Solvent Diffusion (QESD) method. In this study methanol, water and dichloromethane were used as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like Hydroxypropyl β-cyclodextrin, β-cyclodextrin, Lutrol F68, Lutrol F127 were used in agglomeration process. The pure drug (FL) and its agglomerates with different polymers were characterize for their drug loading as well as by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), FTIR spectroscopic studies and Scanning Electron Microscopy (SEM). The DSC results indicated decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility (53.69±0.53 μg mL-1), dissolution rate (100.09±2.27% in 60 min) and micromeritic properties (bulk density, flow property, compactability) compared with FL. The SEM studies showed that the agglomerate possesses a good spherical shape.
机译：本工作的目的是使用准乳液溶剂扩散法（QESD）进行球形附聚，以提高水溶性较差的非洛地平（FL）的溶解度，溶解速度和微链性能。在这项研究中，分别使用甲醇，水和二氯甲烷作为良溶剂，不良溶剂和桥接液体。团聚过程中使用了亲水性聚合物，如羟丙基β-环糊精，β-环糊精，Lutrol F68，Lutrol F127。纯药物（FL）及其与不同聚合物的附聚物的特征在于其载药量以及差示扫描量热法（DSC），X射线衍射（XRD），FTIR光谱研究和扫描电子显微镜（SEM）。 DSC结果表明与晶体含量无序有关的熔融焓降低。 XRD研究还显示了结晶度的变化，红外光谱表明重结晶的附聚物没有化学变化。与FL相比，具有不同聚合物的球形团聚固体分散体的溶解度（53.69±0.53μgmL-1），溶出速率（60分钟内为100.09±2.27％）和微团聚性质（堆积密度，流动性，可压实性）显着增加。 SEM研究表明，附聚物具有良好的球形。

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