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Effect of solvent on retarding the release of diltiazem HCl from Polyox-based liquisolid tablets

机译:溶剂对盐酸地尔硫卓从Polyox基液化片剂中释放的抑制作用

摘要

ObjectivesududThe aim of this work was to investigate the use of liquisolid technique to sustain the release of a model highly soluble drug, diltiazem HCl, from liquisolid matrices containing Polyox, a recently proposed matrix-forming hydrophilic polymer as an alternative to hypromellose.udMethodsududPolyox-based liquisolid formulations prepared using several non-volatile solvents (i.e. polysorbate 80, polyethylene glycol, polyethylene glycol 200 and polyethylene glycol 600) and then characterised using differential scanning calorimetry and powder X-ray diffraction. The influence of solvent on retarding the release of diltiazem HCl from Polyox-based liquisolid tablets compared to conventional physical mixture tablets was studied.udKey findingsududLiquisolid tablets exhibited greater retarding properties compared to conventional tablets. The use of polysorbate produced a slower release pattern of the drug from diltiazem hydrochloride (DTZ) liquisolid tablets compared to propylene glycol and polyethylene glycol (200 and 600). The release retardation was decreased with the increase in the concentration of the drug within drug:solvent liquid medication used. Solid-state analysis suggested the presence of a fraction of the drug mass in a solubilised state within polysorbate in liquisolid powders.udConclusionududPolyox-based matrix tablets prepared using liquisolid technique in the presence of a carefully selected non-volatile solvent could produce desirable, more sustained release profiles of highly water-soluble drugs compared to conventional physical mixture tablets.
机译:目的 ud ud这项工作的目的是研究使用液体固体技术从含有Polyox的液体固体基质中持续释放模型高度可溶的药物盐酸地尔硫卓,该溶液最近被提议形成基质形成亲水性聚合物,作为羟丙甲纤维素的替代品 udMethods ud ud使用多种非挥发性溶剂(例如,聚山梨酯80,聚乙二醇,聚乙二醇200和聚乙二醇600)制备基于聚氧的液状固体制剂,然后使用差示扫描量热法和粉末X射线衍射进行表征。与常规的物理混合物片剂相比,研究了溶剂对Polyox基液状固体片剂中盐酸地尔硫卓释放的影响。 ud关键发现 ud ud与常规片剂相比,液状固体片剂显示出更大的阻滞性能。与丙二醇和聚乙二醇(200和600)相比,聚山梨酯的使用从盐酸地尔硫卓(DTZ)液体固体片剂中释放的药物释放速度较慢。释放延迟随着所用药物:溶剂型液体药物中药物浓度的增加而降低。固态分析表明,液状固体粉末中的聚山梨酯中存在一部分溶解状态的药物。 ud结论 ud ud在谨慎选择的非挥发性溶剂存在下,使用液固技术制备的聚甲醛基片剂可以与常规的物理混合物片剂相比,可产生所需的,高度持续释放的高水溶性药物释放曲线。

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