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Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

机译:美洛昔康-辣木凝结剂-PVP三元固体分散体的固相表征和溶解特性

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摘要

The effect of ternary solid dispersions of poor water-soluble NSAID meloxicam with moringa coagulant (obtained by salt extraction of moringa seeds) and polyvinylpyrrolidone on the in vitro dissolution properties has been investigated. Binary (meloxicam–moringa and meloxicam–polyvinylpyrrolidone (PVP)) and ternary (meloxicam–moringa–PVP) systems were prepared by physical kneading and ball milling and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry. The in vitro dissolution behavior of meloxicam from the different products was evaluated by means of United States Pharmacopeia type II dissolution apparatus. The results of solid-state studies indicated the presence of strong interactions between meloxicam, moringa, and PVP which were of totally amorphous nature. All ternary combinations were significantly more effective than the corresponding binary systems in improving the dissolution rate of meloxicam. The best performance in this respect was given by the ternary combination employing meloxicam–moringa–PVP ratio of [1:(3:1)] prepared by ball milling, with about six times increase in percent dissolution rate, whereas meloxicam–moringa (1:3) and meloxicam–PVP (1:4) prepared by ball milling improved dissolution of meloxicam by almost 3- and 2.5-folds, respectively. The achieved excellent dissolution enhancement of meloxicam in the ternary systems was attributed to the combined effects of impartation of hydrophilic characteristic by PVP, as well as to the synergistic interaction between moringa and PVP.
机译:研究了水溶性较弱的NSAID美洛昔康与辣木凝结剂(辣木籽的盐提取物)和聚乙烯吡咯烷酮的三元固体分散体对体外溶出性能的影响。通过物理混炼和球磨制备二元(美洛昔康–辣木和美洛昔康–聚乙烯吡咯烷酮(PVP))和三元(美洛昔康–辣木–PVP)系统,并通过傅里叶变换红外光谱,差示扫描量热法和X射线衍射仪进行表征。通过美国药典II型溶出度仪评估了来自不同产品的美洛昔康的体外溶出行为。固态研究的结果表明,美洛昔康,辣木和PVP之间存在强相互作用,这是完全无定形的。所有三元组合在提高美洛昔康的溶出度方面均明显优于相应的二元系统。在这方面,最好的性能是通过球磨制备的美洛昔康-辣木-PVP比为[1:(3:1)]的三元组合,其溶出率提高了约六倍,而美洛昔康-辣木(1 :3)和通过球磨制备的美洛昔康– PVP(1:4)分别将美洛昔康的溶出度提高了近3倍和2.5倍。美洛昔康在三元体系中获得的优异的溶解增强作用归因于PVP赋予亲水特性的综合作用,以及辣木与PVP之间的协同相互作用。

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