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静脉注射马波沙星在实验性诱导急性眼内炎兔体内的眼内药代动力学。

Intraocular pharmacokinetics of intravenously administered marbofloxacin in rabbits with experimentally induced acute endophthalmitis.

作者信息

Regnier Alain, Schneider Marc, Concordet Didier, Toutain Pierre-Louis

机构信息

UMR181 Physiopathologie et Toxicologie Expérimentales, INRA, ENVT, Ecole Nationale Vétérinaire,Toulouse Cedex 3, France.

出版信息

Am J Vet Res. 2008 Mar;69(3):410-5. doi: 10.2460/ajvr.69.3.410.

Abstract

OBJECTIVE

To compare penetration of IV administered marbofloxacin in intraocular fluids of healthy and inflamed eyes in rabbits with endotoxin-induced endophthalmitis.

ANIMALS

35 pigmented rabbits.

PROCEDURES

Endophthalmitis was induced in the right eye via intravitreal administration of Escherichia coli endotoxin. The left eye was a control eye. After 24 hours, a single dose of marbofloxacin (4 mg/kg, IV) was administered. Groups of rabbits (n = 5/group) were euthanized 0.5, 1, 2, 4, 6, 10, and 18 hours later, and blood and ocular fluids were collected. Marbofloxacin concentrations were determined via reverse-phase high-performance liquid chromatography, and pharmacokinetic analysis of the data was performed with a mono-compartmental model.

RESULTS

Mean area under the aqueous concentration-time curve was significantly lower in control eyes (1.64 +/- 0.07 microgh/mL) than in inflamed eyes (3.31 +/- 0.11 microgh/mL). Similarly, drug penetration into aqueous humor was 33% and 65% for control eyes and inflamed eyes, respectively. Mean area under the vitreous humor concentration-time curve for control eyes(1.75 +/- 0.05 microgh/mL) was significantly less than for inflamed eyes (2.39 +/- 0.16 microgh/mL). In the vitreous humor, corresponding penetrations were 34% and 47%, respectively.

CONCLUSIONS AND CLINICAL RELEVANCE

Penetration of marbofloxacin into the aqueous and vitreous humor after IV administration was significantly enhanced by intraocular inflammation, suggesting a role for this antimicrobial in the prophylaxis or treatment of bacterial endophthalmitis caused by susceptible pathogens.

摘要

目的

比较静脉注射马波沙星在患有内毒素诱导性眼内炎的兔的健康眼和炎症眼中眼内液的渗透情况。

动物

35只有色兔。

实验步骤

通过玻璃体内注射大肠杆菌内毒素诱导右眼发生眼内炎。左眼为对照眼。24小时后,静脉注射单剂量马波沙星(4毫克/千克)。分别于给药后0.5、1、2、4、6、10和18小时对每组5只兔实施安乐死,并采集血液和眼内液。通过反相高效液相色谱法测定马波沙星浓度,并使用单室模型对数据进行药代动力学分析。

结果

对照眼中房水浓度-时间曲线下的平均面积(1.64±0.07微克·小时/毫升)显著低于炎症眼中的(3.31±0.11微克·小时/毫升)。同样,对照眼和炎症眼中药物进入房水的渗透率分别为33%和65%。对照眼玻璃体内浓度-时间曲线下的平均面积(1.75±0.05微克·小时/毫升)显著小于炎症眼中的(2.39±0.16微克·小时/毫升)。在玻璃体内,相应的渗透率分别为34%和47%。

结论及临床意义

眼内炎症显著增强了静脉注射后马波沙星进入房水和玻璃体内的渗透,表明该抗菌药物在预防或治疗由易感病原体引起的细菌性眼内炎中具有一定作用。

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