Struck H G, Bariszlovich A, Kuhlmann O, Weiss M
Klinik und Poliklinik für Augenheilkunde, Magdeburger Str. 8, 06097 Halle/Saale.
Klin Monbl Augenheilkd. 2001 Feb;218(2):85-8. doi: 10.1055/s-2001-12250.
The mean diclofenac level in the aqueous humor after i.v.-injection should be examined as an example for other systemic applied drugs. The clinical effect is to be evaluated with regard to perioperative anti-inflammatory therapy in patients undergoing cataract surgery.
In this prospective clinical study 59 patients (age 41-86 years) scheduled for phacoemulsification by the tunnel technique, received 75 mg diclofenac-sodium by short time i.v.-infusion (30 min) within an interval between 30 min and 7 h before surgery. Aqueous humor samples and one blood sample were taken at the beginning, and a second blood sample was taken at different time intervals before surgery.
The plasma concentration of diclofenac one minute after infusion was 13,961 +/- 4277 ng/ml. The concentration decreased rapidly during the distribution phase (1305 +/- 324 ng/ml after 40 min) and reached after 336 min 419 +/- 277 ng/ml. A concentration of 83.9 ng/ml diclofenac was found for the last sampling point after 353 min in the elimination phase. The mean diclofenac concentration in the aqueous humor reached after about 60 min the highest level (21.7 +/- 12.7 ng/ml). This level decreases to 4.4 +/- 0.4 ng/ml (120 min) and 3.1 +/- 1.3 ng/ml (300 min), respectively.
The calculated mean residence time of diclofenac molecules in aqueous humor of 123 min matched the mean disposition residence time of diclofenac in the body (119 min).
静脉注射后房水中双氯芬酸的平均水平应作为其他全身应用药物的一个例子进行研究。应就白内障手术患者围手术期抗炎治疗评估其临床效果。
在这项前瞻性临床研究中,59例计划采用隧道技术行超声乳化白内障吸除术的患者(年龄41 - 86岁),在手术前30分钟至7小时的间隔内,通过短时间静脉输注(30分钟)接受75毫克双氯芬酸钠。在开始时采集房水样本和一份血样,在手术前不同时间间隔采集第二份血样。
输注后1分钟双氯芬酸的血浆浓度为13961±4277纳克/毫升。在分布阶段浓度迅速下降(40分钟后为1305±324纳克/毫升),336分钟后达到419±277纳克/毫升。在消除阶段353分钟后的最后一个采样点,双氯芬酸浓度为83.9纳克/毫升。房水中双氯芬酸的平均浓度在约60分钟后达到最高水平(21.7±12.7纳克/毫升)。该水平分别降至4.4±0.4纳克/毫升(120分钟)和3.1±1.3纳克/毫升(300分钟)。
计算得出双氯芬酸分子在房水中的平均驻留时间为123分钟,与双氯芬酸在体内的平均处置驻留时间(119分钟)相符。