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口服和局部给药后环丙沙星在人房水和玻璃体液中的水平。

Human aqueous and vitreous humour levels of ciprofloxacin following oral and topical administration.

作者信息

Cekiç O, Batman C, Yasar U, Başci N E, Bozkurt A, Kayaalp S O

机构信息

Department of Vitreoretinal Surgery, SSK Eye Hospital Akara, Turkey.

出版信息

Eye (Lond). 1999 Aug;13 ( Pt 4):555-8. doi: 10.1038/eye.1999.137.

Abstract

PURPOSE

To assess aqueous and vitreous humour ciprofloxacin concentrations following oral and topical administration of ciprofloxacin in patients with non-inflamed cornea and an intact crystalline lens, and to compare the concentrations of the drug given by either route.

METHODS

In this prospective study, 34 patients undergoing pars plana vitrectomy for various ocular pathologies were divided into two groups. Eighteen patients received 2 drops of 0.3% ophthalmic solution of ciprofloxacin every 30 min for 3 h and then every 60 min for the next 3 h, and 16 patients received a single oral dose of 1000 mg ciprofloxacin 6 h before surgery. The aqueous and vitreous humour samples were simultaneously harvested after oral or topical administration during pars plana vitrectomy to assess penetration of the drug. These samples were assayed for ciprofloxacin concentrations by a method described previously by us using high-performance liquid chromatography.

RESULTS

The aqueous and vitreous humour levels of ciprofloxacin were 0.59 +/- 0.06 microgram/ml (mean +/- SEM) and 0.64 +/- 0.06 microgram/ml after oral and 0.44 +/- 0.07 microgram/ml and 0.22 +/- 0.04 microgram/ml after topical ciprofloxacin administration, respectively. Aqueous humour levels were not statistically significantly different following oral and topical administration (p = 0.069). However, the vitreous level of the drug after oral administration was significantly higher than that after topical administration (p < 0.001).

CONCLUSION

Ocular bioavailability of ciprofloxacin in aqueous humour following oral and topical administration is found to be similar when the drug was applied as described above. Penetration of ciprofloxacin into vitreous humour is less than that into aqueous humour after topical administration.

摘要

目的

评估在角膜未发炎且晶状体完整的患者中,口服和局部应用环丙沙星后房水和玻璃体液中环丙沙星的浓度,并比较两种给药途径下药物的浓度。

方法

在这项前瞻性研究中,34例因各种眼部疾病接受玻璃体切割术的患者被分为两组。18例患者每30分钟滴入2滴0.3%环丙沙星眼药水,共3小时,随后每60分钟滴入2滴,持续3小时;16例患者在手术前6小时口服1000毫克环丙沙星。在玻璃体切割术中口服或局部给药后,同时采集房水和玻璃体液样本以评估药物的渗透情况。使用我们之前描述的高效液相色谱法测定这些样本中环丙沙星的浓度。

结果

口服环丙沙星后房水和玻璃体液中环丙沙星的水平分别为0.59±0.06微克/毫升(平均值±标准误)和0.64±0.06微克/毫升,局部应用环丙沙星后分别为0.44±0.07微克/毫升和0.22±0.04微克/毫升。口服和局部给药后房水中的药物水平在统计学上无显著差异(p = 0.069)。然而,口服给药后玻璃体内的药物水平显著高于局部给药后(p < 0.001)。

结论

按上述方法应用药物时,口服和局部应用环丙沙星后房水中的眼部生物利用度相似。局部给药后环丙沙星进入玻璃体液的渗透率低于进入房水的渗透率。

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