Sharma Trisha, Kamath M Manjunath, Kamath M Gurudutt, Nayak Rajesh R, Bairy K L, Musmade Prashant B
Department of Ophthalmology, Kasturba Medical College, Manipal University, Mangalore, Karnataka, India.
Department of Pharmacology, Kasturba Medical College, Manipal University, Manipal, Karnataka, India.
Br J Ophthalmol. 2015 Sep;99(9):1182-5. doi: 10.1136/bjophthalmol-2014-306502. Epub 2015 Mar 30.
To assess the intraocular penetration of 0.5% moxifloxacin hydrochloride into aqueous humour after oral and topical administration.
A prospective, interventional study of 42 patients scheduled to undergo cataract surgery was carried out. Out of the 42 subjects, 21 were randomly categorised into Group I and received one drop of 0.5% topical moxifloxacin four times, at 15 min intervals starting 75 min before the surgery. Another 21 subjects were categorised into Group II and all subjects in this group were administered a single tablet of 400 mg of moxifloxacin, 12 h before the surgery. Estimation of moxifloxacin in aqueous samples was carried out using high-performance liquid chromatography. Results were analysed using Student unpaired 't' test and analysis of variance. The value of p<0.05 was considered to be significant.
Mean aqueous concentration of moxifloxacin attained in the oral group (n=21) was 0.504±0.30 μg/mL while that in the topical group (n=21) was 2.04±0.72 μg/mL, and this difference in levels was statistically significant (p<0.005). The levels attained by both the groups well exceeded the MIC90 (minimum inhibitory concentration of antibiotic required to inhibit growth of 90% of bacteria strains) levels for most of the organisms causing endophthalmitis. Penetration of moxifloxacin in aqueous in both the groups was not affected by gender, intraocular pressure or comorbidities significantly. However, aqueous levels were found to be higher among the younger subjects within the topical group.
Moxifloxacin has an impressive spectrum of coverage and this pharmacokinetic study reinforces its potential as a prophylactic drug against intraocular infections, given the high aqueous levels post topical administration.
评估口服和局部应用0.5%盐酸莫西沙星后其在房水中的眼内渗透性。
对42例计划行白内障手术的患者进行了一项前瞻性干预性研究。在这42名受试者中,21名被随机分为第一组,在手术前75分钟开始,每隔15分钟接受一滴0.5%的局部用莫西沙星,共4次。另外21名受试者被分为第二组,该组所有受试者在手术前12小时服用一片400毫克的莫西沙星。使用高效液相色谱法对房水样本中的莫西沙星进行测定。结果采用学生非配对“t”检验和方差分析进行分析。p<0.05的值被认为具有统计学意义。
口服组(n = 21)莫西沙星的平均房水浓度为0.504±0.30μg/mL,而局部应用组(n = 21)为2.04±0.72μg/mL,两组浓度差异具有统计学意义(p<0.005)。两组达到的浓度水平均远远超过了大多数引起眼内炎的微生物的MIC90(抑制90%细菌菌株生长所需的抗生素最低抑菌浓度)水平。两组房水中莫西沙星的渗透不受性别、眼压或合并症的显著影响。然而,在局部应用组中,年轻受试者的房水浓度较高。
莫西沙星具有广泛的覆盖范围,这项药代动力学研究强化了其作为预防眼内感染药物的潜力,因为局部应用后房水浓度较高。