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首页> 外文期刊>RSC Advances >The effect of nanonization on poorly water soluble glibenclamide using a liquid anti-solvent precipitation technique: aqueous solubility, in vitro and in vivo study
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The effect of nanonization on poorly water soluble glibenclamide using a liquid anti-solvent precipitation technique: aqueous solubility, in vitro and in vivo study

机译：使用液体抗溶剂沉淀技术的纳米化对水溶性可溶性Glibenclamide的影响：含水溶解度，体外和体内研究

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摘要

The aim of the present research was to improve the aqueous solubility and oral bioavailability of glibenclamide (GLB), a BCS class-II drug. A GLB nanosuspension (NS) was prepared using a liquid anti-solvent (LAS) precipitation technique and stabilized using HPMC K15M and lactose. Different in-process variables which directly affect the precipitated particle size have been thoroughly studied and optimized. The effect of a cryoprotective agent which could prevent agglomeration during lyophilisation was investigated. The optimal formulations of GD-H0.3d and GD-H0.4f exhibited a size range of 168.6 and 342.2 nm respectively and did not show any interaction when screened for incompatibility using FT-IR and DSC, but exhibited a decrease in crystallinity. The prepared GLB NPs exhibited superior aqueous solubility and dissolution when compared to pure GLB. The oral bioavailability of optimized formulations was found to exhibit 2.59, 1.67, 1.19, 2.50 and 2.40 folds of increment with respect to C-max, K-el (h(-1)), t(1/2), AUC(0-24) h and AUC(0-infinity) for GD-0.3d in contrast to pure GLB.
机译：本研究的目的是改善GCS-II类药物的Glibenclamide（GLB）的水溶性和口服生物利用度。使用液体抗溶剂（LAS）沉淀技术制备GLB纳米溶解（NS），并使用HPMC K15M和乳糖稳定。已经彻底研究和优化了直接影响沉淀粒度的不同的过程变量。研究了能够防止冻干过程中凝聚的冷冻保护剂的效果。 GD-H0.3D和GD-H0.4F的最佳制剂分别显示出168.6和342.2nm的尺寸范围，并且在使用FT-IR和DSC的不相容性筛选时没有显示出任何相互作用，但表现出结晶度降低。与纯GLB相比，制备的GLB NPS表现出优异的水溶性和溶解。发现优化配方的口腔生物利用度表现出2.59,1.67,19,2.50和2.40倍，相对于C-Max，K-E1（H（-1）），T（1/2），AUC（0与纯GLB相比，-24）H和AUC（0-Infinity）对于GD-0.3D。

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