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Solubility Enhancement of Nebivolol by Micro Emulsion Technique

机译:微乳技术提高奈必洛尔的溶解度

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Nebivolol is a third-generation beta-a drenoceptor antagonist. It differs from other beta-a drenoceptor an tagonists as it combines highly selective beta (1)-adrenoceptor antagonist properties with nitric oxide-mediated vasodilator actions and beneficial effects on endothelial function. But this very useful drug use is limited due to challenge of poor water solubility (0.0403 mg/ml). Present study deals with enhancement of solubility of Nebivolol by micro emulsion technique. Various oils, surfactants, and co-surfactants were used to check solubility of Nebivolol. Pseudoternary phase diagrams were constructed using various combinations of ingredients i.e. oil: surfactant: co-surfactant. Micro emulsion batches were prepared by phase titration method. Developed micro emulsion was evaluated for various physicochemical, stability parameters, in-vitro and ex-vivo parameters. Results showed stable micro emulsion form of Nebivolol improved solubility.
机译:奈比洛尔是第三代β-α受体受体拮抗剂。它不同于其他β-a肾上腺素受体拮抗剂,因为它结合了高度选择性的β(1)-肾上腺素受体拮抗剂特性和一氧化氮介导的血管舒张作用以及对内皮功能的有益作用。但是由于挑战水溶性差(0.0403 mg / ml),限制了这种非常有用的药物使用。本研究涉及通过微乳液技术提高奈必洛尔的溶解度。各种油,表面活性剂和辅助表面活性剂用于检查奈必洛尔的溶解度。伪三元相图是使用各种成分(即油:表面活性剂:助表面活性剂)的各种组合构建的。通过相滴定法制备微乳液批次。评价了开发的微乳液的各种理化,稳定性参数,体外和离体参数。结果显示稳定的奈比洛尔微乳液形式提高了溶解度。

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