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Liquigroud technique: a new concept for enhancing dissolution rate of glibenclamide by combination of liquisolid and co-grinding technologies

机译:液固技术:通过液固和共研技术的结合提高格列本脲溶解速率的新概念

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摘要

>Introduction: The potential of combining liquisolid and co-grinding technologies (liquiground technique) was investigated to improve the dissolution rate of a water-insoluble agent (glibenclamide) with formulation-dependent bioavailability. >Methods: To this end, different formulations of liquisolid tablets with a wide variety of non-volatile solvents contained varied ratios of drug: solvent and dissimilar carriers were prepared, and then their release profiles were evaluated. Furthermore, the effect of size reduction by ball milling on the dissolution behavior of glibenclamide from liquisolid tablets was investigated. Any interaction between the drug and the excipient or crystallinity changes during formulation procedure was also examined using X-ray diffraction (XRD) and differential scanning calorimetry (DSC). >Results: The present study revealed that classic liquisolid technique did not significantly affect the drug dissolution profile as compared to the conventional tablets. Size reduction obtained by co-grinding of liquid medication was more effective than the implementation of liquisolid technique in enhancing the dissolution rate of glibenclamide. The XRD and DSC data displayed no formation of complex or any crystallinity changes in both formulations. >Conclusion: An enhanced dissolution rate of glibenclamide is achievable through the combination of liquisolid and co-grinding technologies.
机译:>简介:研究了液体固体和共研技术(液体地面技术)相结合的潜力,以提高水不溶性药物(格列本脲)的溶出速率,并具有取决于制剂的生物利用度。 >方法:为此,制备了具有多种非挥发性溶剂的液状固体片剂的不同制剂,其中含有不同比例的药物:溶剂和异种载体,然后评估了它们的释放曲线。此外,研究了通过球磨减小尺寸对格列本脲从液状固体片剂中的溶解行为的影响。还使用X射线衍射(XRD)和差示扫描量热法(DSC)检查了制剂过程中药物与赋形剂之间的任何相互作用或结晶度的变化。 >结果:本研究表明,与传统片剂相比,经典液固技术对药物溶出度没有明显影响。与液体固体技术的实施相比,通过液体药物共研磨获得的尺寸减小在提高格列本脲的溶出率方面更为有效。 XRD和DSC数据显示两种配方均未形成络合物或结晶度变化。 >结论:通过液固和共研技术的结合,可以提高格列本脲的溶解速度。

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