Abstract

Smart phase transformation systems@hard capsule (SPTS@hard capsule) based on lyotropic liquid crystalline (LLC) were developed for oral sustained release in this study. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) were used as hydrophilic and hydrophobic model drug, respectively. Two systems were added with different additives, that is, gelucire 39/01, PEG 1000 and Tween 80 to adjust their melting point and release profiles. The phase transformation of these systems could be triggered by water as well as temperature. They could spontaneously transform into cubic phase or hexagonal phase when coming across with water, to achieve the 24 h sustained release profile. In addition, the obtained systems could switch between semisolid state and liquid state when temperature changed within room temperature and body temperature, which facilitated the phase transformation in gastrointestinal tract and during their encapsulation into hard capsules. LLC-based SPTS@hard capsule revealed potential for the industrialization of its oral administration on account of its drugs accommodation with different solubility, controllable release profile and simple preparation process.

 抽象的

本研究开发了基于溶致液晶（LLC）的智能相变系统@硬胶囊（SPTS@硬胶囊）用于口服缓释。盐酸多西环素（DOXY）和美洛昔康（MLX）分别用作亲水性和疏水性模型药物。两个系统添加了不同的添加剂，即gelucire 39/01、PEG 1000和Tween 80，以调整它们的熔点和释放曲线。这些系统的相变可以由水和温度触发。当遇到水时，它们可以自发转变为立方相或六方相，从而实现24小时的缓释曲线。此外，当温度在室温和体温范围内变化时，所获得的系统可以在半固态和液态之间切换，这有利于胃肠道中和封装成硬胶囊的过程中的相变。基于LLC的SPTS@硬胶囊由于其药物具有不同的溶解度、可控的释放曲线和简单的制备工艺，显示出其口服给药的工业化潜力。