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Čvrsta disperzija meloksikama: faktorijalno dizajnirani dozirani pripravak za gerijatrijsku populaciju

机译:美洛昔康的固体分散体:针对老年人群的因子设计剂量配方

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摘要

The objective of the present work was to improve the dissolution properties of the poorly water-soluble drug meloxicam by preparing solid dispersions with hydroxyethylcellulose (HEC), mannitol and polyethylene glycol (PEG) 4000 and to develop a dosage form for geriatric population. Differential scanning calorimetry, X–ray diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used to investigate the solid-state physical structure of the prepared solid dispersions. Higher in vitro dissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. PEG 4000 in 1:9 drug to carrier ratio exhibited the highest drug release (100.2%), followed by mannitol (98.2%) and HEC (89.5%) in the same ratio. Meloxicam-PEG 4000 solid dispersion was formulated into suspension and optimization was carried out by 23 factorial design. Formulations containing higher levels of methyl cellulose and higher levels of either sodium citrate or Tween 80 exhibited the highest drug release.
机译:本工作的目的是通过用羟乙基纤维素(HEC),甘露醇和聚乙二醇(PEG)4000制备固体分散体来改善水溶性差的药物美洛昔康的溶解特性,并开发一种用于老年人群的剂型。差示扫描量热法,X射线衍射法,傅立叶变换红外光谱法和扫描电子显微镜法用于研究制备的固体分散体的固态物理结构。与相应的物理混合物和纯药物相比,固体分散体的体外溶出度更高。 PEG 4000以1:9的药物/载体比例显示出最高的药物释放(100.2%),其次是甘露醇(98.2%)和HEC(89.5%),比例相同。将Meloxicam-PEG 4000固体分散体配制为悬浮液,并通过23因子设计进行优化。含有较高含量的甲基纤维素和较高含量的柠檬酸钠或吐温80的制剂显示出最高的药物释放。

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