Vitreous and Aqueous Concentrations of Brimonidine Following Topical Application of Brimonidine Tartrate 0.1% Ophthalmic Solution in Humans
Vitreous and Aqueous Concentrations of Brimonidine Following Topical Application of Brimonidine Tartrate 0.1% Ophthalmic Solution in Humans
复制标题
DOI：
10.1089/jop.2015.0003
复制
发表时间：
2015-06-01
影响因子：
2.3
通讯作者：
Inatani, Masaru
中科院分区：
文献类型：
--
作者：
Takamura, Yoshihiro;Tomomatsu, Takeshi;Inatani, Masaru
目的：测定0.1%布莫尼定滴眼液在玻璃体和房水中的浓度。方法：前瞻性观察病例系列包括特发性视网膜前膜或黄斑裂孔患者，他们计划行玻璃体切割术。术前每日两次外用0.1%酒石酸溴莫尼定滴眼液，疗程1周。玻璃体切割术前采集玻璃体和房水，用LC/MS/MS法测定药物浓度。结果：纳入患者24例，其中有晶状体眼19例，人工晶状体眼5例。房水和玻璃体中的平均浓度分别为336.0276.2和4.8+/-3.2 nm。玻璃体和水样之间存在显著的相关性(P=0.034，R2=0.22)。其中19只眼(79%)玻璃体内酒石酸溴莫尼定浓度>2 nm。有晶状体眼玻璃体中溴莫尼定平均浓度为4.9+/-3.3 nm，人工晶状体眼为4.1+/-2.4 nm，两者差异无统计学意义(P=0.59)。结论：在给药1周后，大多数局部使用0.1%酒石酸溴莫尼定的患者玻璃体中的分子浓度都在2 nM以上，这是已知激活动物视网膜神经保护性-2受体的原因。药物对玻璃体的渗透似乎与晶状体状态无关。
Purpose: To determine the vitreous and aqueous concentrations of brimonidine after topical application of the ophthalmic solution 0.1%. Methods: The prospective observational case series included patients with an idiopathic epiretinal membrane or macular hole who were scheduled for a pars plana vitrectomy. Brimonidine tartrate ophthalmic solution 0.1% was topically administered twice daily for 1 week preoperatively. Vitreous and aqueous humor was collected before vitrectomy, and then, the brimonidine concentration was measured with liquid chromatography tandem spectrometry (LC/MS/MS). Results: Twenty-four patients (19 phakic eyes and 5 pseudophakic eyes) were enrolled. The mean concentrations in the aqueous humor and vitreous were 336.0276.2 and 4.8 +/- 3.2nM, respectively. A significant relationship was observed between the vitreous and aqueous samples (P=0.034, R-2=0.22). Nineteen (79%) of the 24 eyes showed more than 2nM of brimonidine tartrate concentration in the vitreous. In the phakic eyes, the mean concentration of brimonidine in the vitreous was 4.9 +/- 3.3nM, while the mean concentration in the pseudophakic eyes was 4.1 +/- 2.4nM, demonstrating no significant difference between pseudophakic and phakic eyes (P=0.59). Conclusions: After 1 week of dosing, in most of the patients who topically received brimonidine tartrate 0.1%, the concentration in the vitreous of the molecule was above 2nM, which is known to activate neuroprotective -2 receptors in animal retina. The drug penetration into the vitreous seems to be independent of lens status.