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Improved oral delivery of valsartan from maltodextrin based proniosome powders

机译:从基于麦芽糊精的前体体粉中改善缬沙坦的口服给药

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Proniosome powders proved to be the potential carriers for efficient oral delivery of lipophilic or amphi-philic drugs. Henceforth, an attempt was made to improve the oral delivery of valsartan by loading into maltodextrin based proniosome powders. The proniosome powders were prepared by varying the ratio of span 60 and cholesterol and evaluated for micromeritic properties and the results indicate acceptable flow properties. The formulation containing equimolar ratio of span 60 and cholesterol showed smaller vesicle size, high surface charge and entrapment efficiency. The formation of nibsomes and surface morphology of optimized proniosome formulation was studied by optical and scanning electron microscopy, respectively. FT-IR, differential scanning calorimetry, and powder X-ray diffraction studies performed to understand the solid state properties of the drug reveal the absence of chemical interaction, drug transformation from crystalline to amorphous and molecular state. The in vitro dissolution study carried out in both simulated gastric and intestinal fluid demonstrate improved dissolution characteristics compared to pure drug. The augment in permeation enhancement from proniosome formulation across rat intestine suggest the potential of proniosome carriers for improved oral delivery of valsartan.
机译:proniosome粉末被证明是有效口服亲脂性或两亲性药物的潜在载体。今后,通过将麦芽糊精为基的前体小体粉末填充,试图改善缬沙坦的口服递送。通过改变跨度60和胆固醇的比例来制备原核小体粉末,并评价其微粒性能,结果表明可接受的流动性能。含有等摩尔比的跨度60和胆固醇的制剂显示出较小的囊泡尺寸,高的表面电荷和包封效率。通过光学和扫描电子显微镜分别研究了脂质体的形成和优化的脂质体配方的表面形态。为了解药物的固态特性而进行的FT-IR,差示扫描量热法和粉末X射线衍射研究表明,不存在化学相互作用,药物从晶体状态转变为非晶态和分子状态。在模拟胃液和肠液中进行的体外溶出度研究表明,与纯药物相比,溶出度特性得到改善。 proniosome制剂在大鼠肠道中的渗透增强作用增强,表明pronoiosome载体具有改善缬沙坦口服递送的潜力。

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