Absorption of Topically Administered Ciprof loxacin. Of loxacin and Gentamicin in the Inflamed Rabbit Eye

Behrens–Baumann, W.

doi:10.1159/000310687

Cited by 21 publications

(6 citation statements)

References 9 publications

(12 reference statements)

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“…Similarly, the ocular surface of older dogs may accommodate a larger volume due to laxity in the eyelids, and the instilled solution may be retained for longer durations due to reductions in tear volume, reflex tearing, and tear turnover rate (49,50). In addition, the present findings do not fully represent the physiology of eyes with ocular surface disease, in which chemosis can reduce the volumetric capacity of the palpebral fissure (51), inflammation can affect tear drainage (52), and ocular absorption (53), and excessive tearing from ocular irritation can further dilute the administered solution (54). In particular, patients with inflamed nasolacrimal duct (dacryocystitis) may actually benefit from instillation of a second drop, as greater nasolacrimal drainage would theoretically be beneficial in such cases.…”

Section: Discussionmentioning

confidence: 71%

Kinetics of Fluorescein in Tear Film After Eye Drop Instillation in Beagle Dogs: Does Size Really Matter?

et al. 2019

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The study aimed to determine the impact of drop size on tear film pharmacokinetics and assess important physiological parameters associated with ocular drug delivery in dogs. Two separate experiments were conducted in eight healthy Beagle dogs: (i) Instillation of one drop (35 µl) or two drops (70 µl) of 1% fluorescein solution in each eye followed by tear collections with capillary tubes from 0 to 180 min; (ii) Instillation of 10 to 100 µl of 0.1% fluorescein in each eye followed by external photography with blue excitation filter (to capture periocular spillage of fluorescein) and tear collections from 1 to 20 min (to capture tear turnover rate; TTR). Fluorescein concentrations were measured in tear samples with a fluorophotometer. The TTR was estimated based upon non-linear mixed-effects analysis of fluorescein decay curves. Tear film pharmacokinetics were not superior with instillation of two drops vs. one drop based on tear film concentrations, residual tear fluorescence, and area under the fluorescein-time curves (P ≥ 0.163). Reflex TTR varied from 20.2 to 30.5%/min and did not differ significantly (P = 0.935) among volumes instilled (10-100 µl). The volumetric capacity of the canine palpebral fissure (31.3 ± 8.9 µl) was positively correlated with the palpebral fissure length (P = 0.023). Excess solution was spilled over the periocular skin in a volume-dependent manner, predominantly in the lower eyelid, medial canthus and lateral canthus. In sum, a single drop is sufficient for topical administration in dogs. Any excess is lost predominantly by spillage over the periocular skin as well as accelerated nasolacrimal drainage.

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Section: Discussionmentioning

confidence: 71%

Kinetics of Fluorescein in Tear Film After Eye Drop Instillation in Beagle Dogs: Does Size Really Matter?

et al. 2019

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“…4 , 16 To date, many preclinical and clinical studies of fluoroquinolones for the treatment of a host of infectious diseases have identified the relevance of C max :MIC and/or the AUC:MIC to treatment efficacy. 10 – 15 , 17 …”

Section: Discussionmentioning

confidence: 99%

“…Bacterial infections can disrupt the epithelium and that disruption can enhance the penetration of topically applied fluoroquinolones. 17 , 18 …”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and aqueous humor penetration of levofloxacin 1.5% and moxifloxacin 0.5% in patients undergoing cataract surgery

Bucci¹,

Nguimfack²,

Fluet³

2016

OPTH

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PurposeThe objective of this study was to compare the pharmacokinetics of levofloxacin 1.5% and moxifloxacin hydrochloride 0.5% ophthalmic solutions in aqueous humor after multiple doses prior to cataract surgery.MethodsNinety-eight eyes underwent cataract surgery and met the requirements of PK analysis. Eligible eyes were randomly assigned in a 1:1 ratio to receive levofloxacin or moxifloxacin prior to cataract surgery and were randomized into one of four sampling time points (ie, 1, 2, 4, and 6 hour post-last dose). Randomization was investigator and laboratory-masked. Three days prior to cataract surgery, each patient instilled one drop of the assigned study medication into the operative eye four times daily. One aqueous humor specimen was collected from the eye at the randomized time point. Aqueous humor specimens were assayed for drug concentration using a validated liquid chromatography and tandem mass spectrometer.ResultsConcentrations of the drug in the aqueous humor, as described by mean Cmax and pooled AUC0–6 values, were greater for levofloxacin than moxifloxacin (Cmax: 1.43, 0.87 μg/ml, respectively, P=0.008; AUC0–6 6.1, 3.8 μg·min/ml, P<0.001 respectively). No treatment-emergent adverse events were reported.ConclusionSignificantly greater drug exposures were attained in aqueous humor following the administration of levofloxacin 1.5% than moxifloxacin 0.5% ophthalmic solution. Achieving considerable higher drug concentration in the aqueous humor with levofloxacin 1.5% may demonstrate a greater potential for bacterial eradication.

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“…However, considering the slow raise in vitreous and aqueous levels observed along with time in lomefloxacin and sparfloxacin groups in the present study, further studies with multiple dosing to evaluate their corresponding increase in aqueous and vitreous levels are required. In the present study, the drug levels were studied in non-inflamed eyes, where as, the effect of inflammation induced breakage of ocular barriers [11,12] needs further studies.…”

Section: Discussionmentioning

confidence: 99%

Intraocular Penetration of Orally and Intravenously Administered Fluoroquinolones in Non-Inflamed Eyes of the Patients Undergoing Vitrectomy Surgery

Ravi¹,

Biswas²,

Velpandian³

et al. 2010

TOPROCJ

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Abstract:Purpose: This study evaluated intraocular penetration of fluoroquinolones (FQs) viz, ofloxacin, pefloxacin, lomefloxacin and sparfloxacin in aqueous, vitreous humors, and plasma after oral/intravenous administration in the subjects undergoing vitrectomy. Methods: Ofloxacin, pefloxacin, lomefloxacin and sparfloxacin were included for oral administration. Only ofloxacin and pefloxacin included for intravenous study. Each group was sub-divided into 3 time points (3, 6 and 12hrs post dose). For each time point, 8 eyes (8 patients) were included and a total of 144 patients were enrolled. Intra-operatively, 80-110 l aqueous, 100-250 l vitreous and 2ml of venous blood samples were collected. Plasma was separated and all samples were stored at -70 o C and subjected for quantification using HPLC and compared with their known MIC 90 of common ocular pathogens. Results: In oral 400mg single dose, among all 4 FQs, ofloxacin showed a maximum concentration at 3 hours in aqueous [0.98(0.12) g/ml] and vitreous [0.78(0.12) g/ml]. Intravenous infusion of 400mg ofloxacin also showed the similar levels in the humors of the eye. Despite low plasma levels, lomefloxacin showed higher aqueous to plasma (a/p) and vitreous to plasma (v/p) ratio. Conclusion: FQs 400mg (as iv and oral) as a single dose could not reach the desired therapeutic concentration (above MIC 90 for all ocular pathogens) in aqueous and vitreous humors. The concentration reached in the humors may not be directly dependent on their plasma levels. Relatively non-polar FQs such as lomefloxacin and sparfloxacin showed better a/p and v/p ratios as compared to their polar analogs such as pefloxacin and ofloxacin.

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Absorption of Topically Administered Ciprof loxacin. Of loxacin and Gentamicin in the Inflamed Rabbit Eye

Cited by 21 publications

References 9 publications

Kinetics of Fluorescein in Tear Film After Eye Drop Instillation in Beagle Dogs: Does Size Really Matter?

Kinetics of Fluorescein in Tear Film After Eye Drop Instillation in Beagle Dogs: Does Size Really Matter?

Pharmacokinetics and aqueous humor penetration of levofloxacin 1.5% and moxifloxacin 0.5% in patients undergoing cataract surgery

Intraocular Penetration of Orally and Intravenously Administered Fluoroquinolones in Non-Inflamed Eyes of the Patients Undergoing Vitrectomy Surgery

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