The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).

中文翻译：

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2-羟丙基-β-环糊精包合物在口服胺碘酮中的作用研究

这项研究的目的是通过使用胺碘酮与2-羟丙基-β-环糊精（HP- β -CD）的包合配合物来提高盐酸胺碘酮的溶解度和药物释放。通过共沉淀和冷冻干燥制备包合物。通过相溶解度方法评估了AMD /HP- β -CD包合物的溶解度提高了4-22倍。通过光谱方法，动态光散射（DLS）和zeta电位分析，SEM和DSC对溶液和固态中的包合物进行了研究。AMD /HP- β的配方相对于不溶性AMD药物，-CD包合物作为粉末形式和作为基质片剂均显示出优异的药代动力学性能，从而改善了负载和释放特性。体外动力学研究揭示了一个复杂的释放机制，该过程分为三个步骤：第一个归因于爆发效应，另外两个归因于包合物中存在的不同键。的体内含有KOLLIDON？和脱乙酰壳多糖基质片剂试验也揭示一个多个（至少两个）峰释放图，因为该包合复合物的两种结构的以及在生物介质中吸收（消化道）的不同位点。