Aim: Aim of this study was to design a solid oral delivery system for a weakly basic drug such as dasatinib (DAS), so as to achieve pH-independent dissolution and improved oral bioavailability.Methods: DAS was solubilised using sodium lauryl sulphate as an aqueous micellar system and such a system containing lactose monohydrate as carrier was spray-dried to obtain a solid mass. Subsequently, the DAS-solid was converted into a tablet using conventional tableting methods.Results: The dissolution study revealed pH-independent dissolution over a wide range of pH conditions. An in vivo bioavailability testing on rats revealed an improved Cmax and AUC0-24. Similarly, viability assay showed a better inhibitory effect of spray-dried dasatinib over the DAS.Conclusions: Micellar solubilisation and spray-drying technology can be approached to resolve poor dissolution and bioavailability of drugs belonging to biopharmaceutical classification system II and III. This technology is amenable to scale-up and has commercial potential.

中文翻译：

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胶束包埋的微粒技术：解决水溶性差的药物的溶解和生物利用度问题的新方法。

目的：本研究的目的是设计一种弱碱性药物（如达沙替尼（DAS））的固体口服给药系统，以实现pH依赖性的溶出度和改善的口服生物利用度。将水性胶束体系和含有乳糖一水合物作为载体的体系喷雾干燥以获得固体。随后，使用常规压片方法将DAS固体转化为片剂。结果：溶出度研究表明，在很宽的pH条件下，pH无关的溶出度。对大鼠的体内生物利用度测试显示，Cmax和AUC0-24有所改善。同样，生存力分析显示喷雾干燥的dasatinib优于DAS的抑制作用。可以采用胶束增溶和喷雾干燥技术来解决属于生物药物分类系统II和III的药物的不良溶解和生物利用度。该技术适合扩大规模并具有商业潜力。