Zhang Chunjuan, Xu Tonghua, Zhang Donglei, He Wei, Wang Siling, Jiang Tongying
Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
He University, Sishui Street 66, Shenyang 110163, China.
Asian J Pharm Sci. 2018 Nov;13(6):527-535. doi: 10.1016/j.ajps.2018.02.010. Epub 2018 Apr 23.
To improve the corneal permeability and water-solubility of disulfiram (DSF), which is an ocular drug for cataract, P188 was selected as a matrix to prepare solid dispersion of DSF (DSF) by hot melt method. The DSF was characterized by DSC, XRD, and IR, and the results suggested that DSF was amorphous in DSF. The DSF was added to borate buffer solution (BBS) contained 20% poloxamer P407 and 1.2% poloxamer P188 to form in-situ gel. and experiments revealed that DSF combined with in-situ gel (DSF/in-situ gel) increased the residence time and the amount of DSF penetrated through the corneal. The pharmacodynamics studies exhibited DSF/in-situ gel delayed the development of selenium-induced cataract at some content. These results investigated that DSF/in-situ gel as a drug delivery system can improve DSF ocular permeability.
为提高用于治疗白内障的眼用药物双硫仑（DSF）的角膜渗透性和水溶性，选择泊洛沙姆188（P188）作为基质，采用热熔法制备双硫仑固体分散体（DSF）。通过差示扫描量热法（DSC）、X射线衍射法（XRD）和红外光谱法（IR）对DSF进行表征，结果表明DSF在DSF中为无定形。将DSF加入含有20%泊洛沙姆P407和1.2%泊洛沙姆P188的硼酸盐缓冲溶液（BBS）中形成原位凝胶。实验表明，DSF与原位凝胶（DSF/原位凝胶）结合可延长DSF在角膜的滞留时间并增加其透过角膜的量。药效学研究表明，在一定含量下，DSF/原位凝胶可延缓硒诱导的白内障的发展。这些结果表明，DSF/原位凝胶作为一种药物递送系统可提高DSF的眼部渗透性。
