Weijtens Olga, Schoemaker Rik C, Romijn Fred P H T M, Cohen Adam F, Lentjes Eef G W M, van Meurs Jan C
The Rotterdam Eye Hospital, Rotterdam, The Netherlands.
Ophthalmology. 2002 Oct;109(10):1887-91. doi: 10.1016/s0161-6420(02)01176-4.
To study the dexamethasone concentration in aqueous humor, vitreous, and serum of patients after repeated topical application of dexamethasone disodium phosphate.
Prospective nonrandomized comparative trial.
Twenty phakic patients scheduled for a first vitrectomy.
All participants received dexamethasone disodium phosphate drops according to an application schedule intended to result in steady-state drug concentrations. Starting on the preoperative day, they received 1 drop of dexamethasone disodium phosphate (0.1%) every 1 hours until the time of vitrectomy (total, 10 or 11 drops). At night, ointment containing dexamethasone (0.3 mg/g) and gentamicin (5 mg/g) was administered once. From 7 AM on, the drop application schedule was resumed. At the start of the vitrectomy, samples were taken from the aqueous humor, vitreous, and blood.
The dexamethasone concentrations in the aqueous humor, vitreous, and serum measured by radioimmunoassay.
The mean dexamethasone concentrations in the aqueous humor, vitreous, and serum were 30.5 ng/ml (range, 7.1-57.7; standard deviation [SD] 15.0), 1.1 ng/ml (range, 0.0-1.6; SD 0.4), and 0.7 ng/ml (range, 0.0-1.2; SD 0.4), respectively.
Compared with previously tested administration routes (peribulbar or subconjunctival injection or oral administration), the penetration of dexamethasone into the vitreous after repeated drop application is negligible. Despite the frequent dosing schedule, the dexamethasone concentration in the aqueous humor is far lower than after a subconjunctival injection with dexamethasone disodium phosphate. Systemic uptake is low.
研究磷酸地塞米松钠反复局部应用后患者房水、玻璃体和血清中的地塞米松浓度。
前瞻性非随机对照试验。
20例计划首次行玻璃体切除术的有晶状体眼患者。
所有参与者按照旨在达到稳态药物浓度的用药方案接受磷酸地塞米松钠滴眼液。从术前一天开始,每1小时滴1滴磷酸地塞米松钠(0.1%),直至玻璃体切除术时(共10或11滴)。夜间,给予一次含地塞米松(0.3mg/g)和庆大霉素(5mg/g)的眼膏。从上午7点开始,恢复滴眼液用药方案。在玻璃体切除术开始时,采集房水、玻璃体和血液样本。
通过放射免疫测定法测量房水、玻璃体和血清中的地塞米松浓度。
房水、玻璃体和血清中的地塞米松平均浓度分别为30.5ng/ml(范围7.1 - 57.7;标准差[SD]15.0)、1.1ng/ml(范围0.0 - 1.6;SD 0.4)和0.7ng/ml(范围0.0 - 1.2;SD 0.4)。
与先前测试的给药途径(球周或结膜下注射或口服给药)相比,反复滴用后地塞米松进入玻璃体的渗透率可忽略不计。尽管给药频率较高,但房水中的地塞米松浓度远低于结膜下注射磷酸地塞米松钠后的浓度。全身吸收较低。