McDermott M L, Tran T D, Cowden J W, Buggé C J
Kresge Eye Institute, Wayne State University School of Medicine, Detroit, MI 48201.
Ophthalmology. 1993 Feb;100(2):197-200. doi: 10.1016/s0161-6420(13)31672-8.
Use of fluoroquinolone agents as single drug treatment for severe bacterial keratitis requires that adequate stromal drug concentrations are achievable that exceed the MIC90 for common corneal pathogens. The purpose of this study, therefore, is to document the human stromal penetration of the fluoroquinolone, ciprofloxacin, in human tissue obtained from patients undergoing penetrating keratoplasty.
Twelve patients, all with intact corneal epithelia, received 0.3% ciprofloxacin (Ciloxan) eyedrops every 15 minutes for the first hour and then every hour for 10 hours before their scheduled keratoplasty. Corneal tissue samples obtained from the excised buttons at the time of surgery were frozen and subsequently analyzed for drug concentration using high-pressure liquid chromatography.
A mean corneal tissue concentration of 5.28 +/- 3.4 micrograms/g tissue (mean +/- standard deviation) of ciprofloxacin was determined. Tissue levels ranged from 1.43 micrograms/g of tissue to 10.58 micrograms/g of tissue.
Ciprofloxacin penetration was variable in patients with an intact epithelium and, in some cases, did not exceed the MIC90 for some gram-positive organisms. The presence of an epithelial defect is expected to potentiate the penetration of ciprofloxacin to most likely exceed the MIC90 for most corneal pathogens.
使用氟喹诺酮类药物作为严重细菌性角膜炎的单一药物治疗，需要达到足够的基质药物浓度，以超过常见角膜病原体的MIC90。因此，本研究的目的是记录氟喹诺酮类药物环丙沙星在接受穿透性角膜移植术患者的人体组织中的基质渗透情况。
12例角膜上皮完整的患者，在预定角膜移植术前，第1小时每15分钟滴注0.3%环丙沙星（西洛仙）眼药水，然后每小时滴注10小时。手术时从切除的角膜片中获取的角膜组织样本冷冻保存，随后使用高压液相色谱法分析药物浓度。
测定环丙沙星的角膜组织平均浓度为5.28±3.4微克/克组织（平均值±标准差）。组织水平范围为1.43微克/克组织至10.58微克/克组织。
环丙沙星在角膜上皮完整的患者中的渗透情况存在差异，在某些情况下，对某些革兰氏阳性菌的浓度未超过MIC90。预计存在上皮缺损会增强环丙沙星的渗透，很可能超过大多数角膜病原体的MIC90。
