Wang Jiaxing, Tao Yong, Feng Jing, Niu Yidong, Liu Jichao, Huang Yanbin
Key Laboratory of Advanced Materials (MOE), Department of Chemical Engineering, Tsinghua University Beijing 100084 China
Department of Ophthalmology, Beijing Chaoyang Hospital, Capital Medical University Beijing 100020 China
RSC Adv. 2019 Jul 9;9(37):21318-21322. doi: 10.1039/c9ra03070k. eCollection 2019 Jul 5.
Sodium foscarnet is an antiviral drug against cytomegalovirus retinitis, and clinically it is used frequent intravitreal injection which causes various ocular complications. Here we propose to use benzathine foscarnet in a new salt form with much lower aqueous solubility, and as a potential long-acting intravitreally injectable solid form for foscarnet. Benzathine foscarnet (1 : 1) microcrystals were synthesized and evaluated both and . The aqueous solubility of benzathine foscarnet was 14.2 mM, which is in between those of the currently-used sodium foscarnet and our previously-reported calcium foscarnet salt. In a rabbit model, the injected microcrystals last for about 3 weeks in the vitreous, suggesting its solubility and dissolution profile is appropriate for its intended use. However, the injected benzathine foscarnet microcrystals also caused adverse effects .
膦甲酸钠是一种抗巨细胞病毒性视网膜炎的抗病毒药物，临床上常用于玻璃体内频繁注射，这会导致各种眼部并发症。在此，我们提议使用具有低得多的水溶解度的新盐形式的苄星膦甲酸钠，作为膦甲酸钠潜在的长效玻璃体内可注射固体形式。合成了苄星膦甲酸钠（1∶1）微晶并进行了体外和体内评估。苄星膦甲酸钠的水溶解度为14.2 mM，介于目前使用的膦甲酸钠和我们先前报道的膦甲酸钠钙盐之间。在兔模型中，注射的微晶在玻璃体内持续约3周，表明其溶解度和溶解特性适合其预期用途。然而，注射的苄星膦甲酸钠微晶也会引起不良反应。
