Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers
Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers
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DOI：
10.1136/bjophthalmol-2012-302466
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发表时间：
2013-05-01
影响因子：
4.1
通讯作者：
van Haarlem, Thomas
中科院分区：
文献类型：
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作者：
Kopczynski, Casey;Novack, Gary D.;van Haarlem, Thomas
背景/目的 评估两种 0.5% AR-12286 滴眼液制剂的降眼压功效、眼部和全身安全性以及全身暴露。 方法 这是一项在 18 名正常成年志愿者中进行的双盲、单中心交叉研究。志愿者被随机分配到两种给药顺序之一：配方 A 每天一次，双眼 (OU) 持续 8 天，最少 7 天清洗，然后配方 B，或相反。主要结果指标是眼部耐受性、眼内压 (IOP) 和 AR-12286 及其代谢物的血液水平。结果 全身吸收较低，大多数受试者血浆中没有可测量的药物浓度（
Background/aims To evaluate the ocular hypotensive efficacy, ocular and systemic safety, and systemic exposure of two formulations of 0.5% AR-12286 Ophthalmic Solution.Methods This was a double-masked, single-centre, crossover study in 18 normal adult volunteers. Volunteers were randomised to one of two dosing sequences: Formulation A once daily, both eyes (OU) for 8 days, a 7-day minimum washout, and then Formulation B, or the reverse. The main outcome measures were ocular tolerability, intraocular pressure (IOP) and blood levels of AR-12286 and its metabolites.Results Systemic absorption was low, with a majority of subjects showing no measurable drug concentration in plasma (