A comparison of the fourth-generation fluoroquinolones gatifloxacin 0.3% and moxifloxacin 0.5% in terms of ocular tolerability

PURPOSE: To compare the ocular tolerability of the commercially available ophthalmic solutions of the fourth-generation fluoroquinolones, gatifloxacin 0.3% (Zymar, Allergan, Inc., Irvine, CA) with benzalkonium chloride (BAK) and moxifloxacin 0.5% (Vigamox) without BAK. METHODS: A baseline evaluation was conducted on 30 healthy volunteers for conjunctival hyperemia, conjunctival vascularity, pupil size, and anterior chamber (AC) cell and flare. Pupils were measured under scotopic conditions with a Colvard pupillometer. Conjunctival hyperemia and vascularity, and AC reaction were measured on a Likert-like scale of 0-3. Subjects then received drops in both eyes from masked bottles of gatifloxacin ophthalmic solution 0.3% with BAK (in one eye determined randomly) and moxifloxacin ophthalmic solution 0.5% without BAK (in the contralateral eye) in a double-masked fashion. Subjects graded pain and ocular irritation in each eye on a scale of 1-10 after 5 min with their eyes closed. The examination was then repeated. RESULTS: The average age of this study population was 34.4 years. The groups of eyes receiving moxifloxacin 0.5% demonstrated an increase in mean conjunctival hyperemia (0.21 [range: 0-1] at baseline to 1.52 [range: 0-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.22 [range: 0-1] at baseline to 0.45 [range: 0-2] at 5 min). The group receiving moxifloxacin 0.5% showed an increase in conjunctival vascularity (0.55 [range: 0-1] at baseline to 1.61 [range: 0.5-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.52 [range: 0-1] at baseline to 0.68 [range: 0-2] at 5 min.). Significantly less pain (1.2 vs. 3.2, p = 0.001) and irritation (0.64 vs. 3.42, p = 0.001) occurred with gatifloxacin 0.3% than with moxifloxacin 0.5%. Pupil size was significantly reduced (5.65 mm-5.05 mm) in eyes receiving moxifloxacin 0.5% (p = 0.004) and no significant change occurred in pupil size (5.60 mm-5.65 mm) in eyes that received gatifloxacin 0.3% (p = 0.878). No AC reaction was noted with either medication. CONCLUSIONS: The group of eyes receiving gatifloxacin 0.3% with BAK demonstrated greater ocular tolerability in comparison to the group receiving moxifloxacin 0.5% without BAK. Moxifloxacin-induced pupillary miosis may be due to prostaglandin release in the anterior chamber. A limitation of this study is the relatively young age of the study population.     

A multicenter,randomized, parallel-group,clinical trial comparing the safety and efficacy of loteprednol etabonate 0.5%/tobramycin 0.3% with dexamethasone 0.1%/tobramycin 0.3% in the treatment of Chinese patients with blepharokeratoconjunctivitis

Abstract

Objective:

To compare the efficacy and safety of loteprednol etabonate 0.5%/tobramycin 0.3% (LE/T) and dexamethasone 0.1%/tobramycin 0.3% (DM/T) ophthalmic suspensions in a Chinese population with ocular inflammation associated with blepharokeratoconjunctivitis (BKC).     

Pharmacokinetics of falintolol II. Absorption, distribution and elimination from tissues and organs following ocular administration and intravenous injection of falintolol in albino rabbits

The absorption, distribution and elimination of falintolol maleate was studied in various ocular and extraocular tissues and organs following ocular instillation, intravenous injection of a 0.5% 14C-falintolol ophthalmic solution and repeated ocular instillations of a 1% non-labeled falintolol ophthalmic solution into albino New Zealand rabbits. Falintolol was distributed in all studied tissues and organs after both routes of administration. After ocular instillation, levels of total radioactivity were distinctly higher in ocular tissues than after intravenous injection. Thus, the level was 475 times more important in cornea, 72 times in aqueous humor and 36 times in iris and ciliary body after ocular instillation. On the other hand, levels of total radioactivity in extraocular tissues and organs were 30-50% higher after intravenous injection compared to ocular instillation of the same dose. Peak levels of total radioactivity were generally achieved between 30 min and 1 h after ocular instillation, while 1.5 h after intravenous injection an increase in the declining part of the curve occurred. This increase, characteristic of an enterohepatic reabsorption, was also observed in blood and plasma 1 h after intravenous injection. Urinary elimination was the major means of excretion since 79.6% of total radioactivity was found in urine 6 h after intravenous injection and 74.5% 12 h after ocular instillation. But after ocular instillation, only 5% was excreted as unchanged falintolol. Whatever the route of administration, after single or repeated application, no drug accumulation was evident.     

Safety and tolerability of naproxen ophthalmic solution in comparison to placebo

BACKGROUND: Naproxen is a classic non-steroidal anti-inflammatory drug (NSAID) with established analgesic and anti-inflammatory potency. Its action is related to cyclooxygenase inhibition and consequent decrease in prostaglandin concentration in various fluids and tissues. Since prostaglandin release is involved in several ocular alterations, various NSAID eye drops have come into use in the clinical setting during the last decade. SUBJECTS, MATERIAL AND METHODS: A randomized, double-blind, placebo-controlled, three-way crossover design phase I was performed in 12 healthy volunteers to determine both tolerance and safety of a new NSAID ophthalmic solution containing sodium naproxen (0.1% and 0.2%). Both single dose and repeated dose (TID for 6 days) instillation were performed. Evaluation was entirely based upon tolerance criteria. Subjective and objective signs of ocular irritation and subject comfort preference were evaluated. Also medical examination, hematology, blood chemistry and urine analysis were also assessed to evaluate any possible effect of the test drugs and control. RESULTS: Neither ophthalmic tolerance parameters nor vital signs or laboratory parameters were influenced by treatments. A slight hyperemia of the conjunctiva was the only change observed in the eye during the study, whereas the only symptom mentioned was burning. CONCLUSION: It is concluded that both tolerability and safety of 0.1% and 0.2% naproxen solution are acceptable after single and repeated conjunctival administration.     

A comparison of the fourth-generation fluoroquinolones gatifloxacin 0.3% and moxifloxacin 0.5% in terms of ocular tolerability

SUMMARY

Purpose: To compare the ocular tolerability of the commercially available ophthalmic solutions of the fourth-generation fluoroquinolones, gatifloxacin 0.3% (Zymart, Allergan, Inc., Irvine, CA) with benzalkonium chloride (BAK) and moxifloxacin 0.5% (Vigamoxt) without BAK.

Methods: A baseline evaluation was conducted on 30 healthy volunteers for conjunctival hyperemia, conjunctival vascularity, pupil size, and anterior chamber (AC) cell and flare. Pupils were measured under scotopic conditions with a Colvard pupillometer. Conjunctival hyperemia and vascularity, and AC reaction were measured on a Likert-like scale of 0-3. Subjects then received drops in both eyes from masked bottles of gatifloxacin ophthalmic solution 0.3% with BAK (in one eye determined randomly) and moxifloxacin ophthalmic solution 0.5% without BAK (in the contralateral eye) in a double-masked fashion. Subjects graded pain and ocular irritation in each eye on a scale of 1-10 after 5min with their eyes closed. The examination was then repeated.

Results: The average age of this study population was 34.4years. The groups of eyes receiving moxifloxacin 0.5% demonstrated an increase in mean conjunctival hyperemia (0.21 [range: 0-1] at baseline to 1.52 [range: 0-3] at 5min.)

that was significantly greater (p?=?0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.22 [range: 0-1] at baseline to 0.45 [range: 0-2] at 5min). The group receiving moxifloxacin 0.5% showed an increase in conjunctival vascularity (0.55 [range: 0-1] at baseline to 1.61 [range: 0.5-3] at 5?min.) that was significantly greater (p?=?0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.52 [range: 0-1] at baseline to 0.68 [range: 0-2] at 5?min.). Significantly less pain (1.2 vs. 3.2, p?=?0.001) and irritation (0.64 vs. 3.42, p?=?0.001) occurred with gatifloxacin 0.3% than with moxifloxacin 0.5%. Pupil size was significantly reduced (5.65mm-5.05mm) in eyes receiving moxifloxacin 0.5% (p?=?0.004) and no significant change occurred in pupil size (5.60mm-5.65mm) in eyes that received gatifloxacin 0.3% (p?=?0.878). No AC reaction was noted with either medication.

Conclusions: The group of eyes receiving gatifloxacin 0.3% with BAK demonstrated greater ocular tolerability in comparison to the group receiving moxifloxacin 0.5% without BAK. Moxifloxacin-induced pupillary miosis may be due to prostaglandin release in the anterior chamber. A limitation of this study is the relatively young age of the study population.     

Thermosensitive PEG–PCL–PEG (PECE) hydrogel as an in situ gelling system for ocular drug delivery of diclofenac sodium

Development of efficient ocular drug delivery systems was still a challenging task. The objective of this article was to develop a thermosensitive PEG–PCL–PEG (PECE) hydrogel and investigate its potential application for ocular drug delivery of diclofenac sodium (DIC). PECE block polymers were synthesized by coupling MPEG-PCL co-polymer using IPDI reagent, and then its sol–gel transition as a function with temperature was investigated by a rheometer. The results showed that 30% (w/v) PECE aqueous solution exhibited sol–gel transition at approximately 35?°C. In vitro release profiles showed the entrapped DIC was sustained release from PECE hydrogels up to 7 days and the initial drug loading greatly effect on release behavior of DIC from PECE hydrogels. MTT assay results indicated that no matter PECE or 0.1% (w/v) DIC-loaded PECE hydrogels were nontoxic to HCEC and L929 cells after 24?h culturing. In vivo eye irritation test showed that the instillation of either 30% (w/v) PECE hydrogels or 0.1% (w/v) DIC-loaded PECE hydrogels to rabbit eye did not result in eye irritation within 72?h. In vivo results showed that the AUC_0–48?h of 0.1% (w/v) DIC-loaded PECE hydrogels exhibited 1.6-fold increment as compared with that of commercial 0.1% (w/v) DIC eye drops, suggesting the better ophthalmic bioavailability could be obtained by the instillation of 0.1% (w/v) DIC-loaded PECE hydrogels.     

Moxifloxacin 0.5% ophthalmic solution: in bacterial conjunctivitis

The fourth-generation 8-methoxyfluoroquinolone moxifloxacin is available as an 0.5% ophthalmic solution for use in the treatment of bacterial conjunctivitis. Moxifloxacin had good activity against various Gram-positive and -negative ocular isolates in vitro, and moxifloxacin 0.5% ophthalmic solution achieved good penetration into ocular tissues in healthy volunteers and patients undergoing ocular surgery. The efficacy of moxifloxacin 0.5% ophthalmic solution in the treatment of bacterial conjunctivitis has been shown in three randomized, double-blind, multicentre trials. In a trial in patients aged ≥1 year, the clinical success rate was significantly higher with moxifloxacin 0.5% ophthalmic solution than with placebo. In a trial in patients aged ≥12 years, moxifloxacin 0.5% ophthalmic solution was noninferior to levofloxacin 0.5% ophthalmic solution in terms of the clinical success rate. In a third trial, the clinical cure rate was significantly higher with moxifloxacin 0.5% ophthalmic solution than with trimethoprim 1.0%/polymixin B 10,000?IU/mL ophthalmic solution in paediatric patients aged ≤18 years. Moxifloxacin 0.5% ophthalmic solution was well tolerated in patients with bacterial conjunctivitis. Ocular adverse events (e.g. eye pain, eye irritation) were the most commonly reported treatment-related adverse events, with the majority being of mild severity.     

Topical netilmicin compared with tobramycin in the treatment of external ocular infection.

In a pilot double-blind, randomized, prospective controlled study the effectiveness and safety of 0.3% netilmicin ophthalmic solution were compared with those of 0.3% tobramycin in treating external bacterial ocular infections in 45 eligible patients. The treatment with both study medications resulted in a significant (p < 0.001, Wilcoxon test) reduction in the mean cumulative score of the signs and symptoms. However, no statistically significant differences were observed between the two groups. The clinical improvement rate was almost complete with either antibiotics. There was a statistically positive trend in the netilmicin group with regard to the microbiological improvement that was achieved in (87% of the netilmicin patients) compared with 77% of the tobramycin patients (77%). Antibiotic sensitivity revealed that 84% of the organisms isolated were sensitive to netilmicin whereas only 64% of them were sensitive to tobramycin. Only minor adverse events occurred in patients treated with either netilmicin or tobramycin. In conclusion, this study demonstrates that netilmicin is a promising new antibiotic for treating external ocular infections.     

Ocular hypotensive efficacy and safety of brinzolamide ophthalmic suspension 1% added to travoprost ophthalmic solution 0.004% therapy in patients with open-angle glaucoma or ocular hypertension

OBJECTIVE: The primary objective of this study was to determine if combined travoprost ophthalmic solution 0.004% and brinzolamide ophthalmic suspension 1% therapy is superior in lowering intraocular pressure (IOP) compared to travoprost monotherapy for patients with open angle glaucoma or ocular hypertension. The secondary objective was to measure the percentage of patients achieving IOP levels of 18 mmHg or less. STUDY DESIGN AND METHODS: Single arm, open-label. PARTICIPANTS: eighty-two patients with inadequate IOP control with travoprost monotherapy. INTERVENTION: the addition of brinzolamide ophthalmic suspension 1% twice daily. MAIN OUTCOME MEASURES: The primary endpoint was mean IOP reduction from baseline at 4 and 12 weeks. The percentage of patients who achieved IOP values 相似文献   

Ocular penetration of moxifloxacin 0.5% and gatifloxacin 0.3% ophthalmic solutions into the aqueous humor following topical administration prior to routine cataract surgery

A prospective, double-masked, randomized, parallel-group study (n = 25) was conducted to examine the ocular penetration of moxifloxacin 0.5% ophthalmic solution and gatifloxacin 0.3% solution into the aqueous humor following topical administration prior to routine cataract surgery. One drop of antibiotic was instilled every 10 min for four doses beginning 1 h prior to surgery. Preliminary results showed aqueous humor concentrations for moxifloxacin that were significantly greater (p < 0.01) than those for gatifloxacin.     

Ketorolac 0.45% ophthalmic solution

Ketorolac 0.45% ophthalmic solution is a topical NSAID indicated in the US for the treatment of ocular pain and inflammation following cataract surgery. In animal studies, the ocular relative bioavailability of single-dose topical ketorolac 0.45% ophthalmic solution was 2- to 3-fold higher than that of ketorolac 0.4% ophthalmic solution. In two identically designed, randomized, double-masked, multicentre trials in adult patients undergoing cataract extraction, the proportions of patients with a summed ocular inflammation score of zero for anterior chamber cell count plus anterior chamber flare on day 14 after surgery were significantly greater in those treated with topical ketorolac 0.45% ophthalmic solution than in those treated with vehicle placebo. Compared with placebo, topical ketorolac 0.45% ophthalmic solution significantly increased the proportion of patients who were pain-free on the day after surgery in both trials. Ketorolac 0.45% ophthalmic solution was generally well tolerated in clinical trials with lower overall incidences of treatment-emergent and treatment-related adverse events than placebo, and with no single treatment-related adverse event having a higher incidence than with placebo.     

Ophthalmic bioequivalence of steroid/antibiotic combination formulations

This study compared the relative ocular bioavailability in rabbits of the antibiotic/steroid combination of 0.3 per cent tobramycin and 0.1 per cent fluorometholone acetate to each of the two single-entity products. Two separate studies were conducted, one measuring fluorometholone acetate in cornea and aqueous humour through 240 min and the other measuring tobramycin in the cornea through 120 min. The results for fluorometholone acetate show that the combination product is 15 per cent higher in AUC for the cornea than the single-entity product (0.05 less than p less than 0.1). However, the combination product is only 4.4 per cent higher in AUC when aqueous humour levels are compared (N.S.). The single-entity fluorometholone acetate ointment yielded cornea and aqueous humour levels which were 20 per cent (p less than 0.01) and 6 per cent (N.S.) higher in AUC than the same tissues measured after topical instillation of the suspension. Statistical treatment of the data indicated that the suspension and ointment products, were bioequivalent with respect to fluorometholone acetate in aqueous humour, but not with respect to corneal concentrations. Tobramycin was measured in the cornea following instillation of either the single-entity solution or the combination suspension. Per cent bound (tobramycin to rabbit antibodies determined in vitro from the radioimmunoassay results) was used for statistical analyses of all group means and standard errors. The results indicated that the products were bioinequivalent.     

Ocular diclofenac. A review of its pharmacology and clinical use in cataract surgery, and potential in other inflammatory ocular conditions.

Diclofenac sodium is a potent nonsteroidal anti-inflammatory drug with analgesic activity. When instilled as a topical 0.1% solution in a limited number of patients undergoing cataract surgery, diclofenac limits surgically induced miosis, reduces signs of ocular inflammation, does not cause elevations in intraocular pressure, and reduces the occurrence and severity of cystoid macular oedema. Preliminary findings suggest a niche for topical diclofenac in other ocular inflammatory conditions such as iritis, episcleritis and conjunctivitis, although its efficacy in these areas awaits confirmation. The drug appears well tolerated, apart from a transient burning sensation after instillation in some patients. Ocular diclofenac thus appears well suited as a local anti-inflammatory adjunct to cataract surgery, and may be useful in some other inflammatory ocular conditions.     

Comparative efficacy of olopatadine 0.1% ophthalmic solution versus levocabastine 0.05% ophthalmic suspension using the conjunctival allergen challenge model

OBJECTIVE: To compare the efficacy of olopatadine and levocabastine in reducing ocular allergic itching and vascular hyperemia (redness) induced by conjunctival allergen challenge. RESEARCH DESIGN AND METHODS: The study was a randomized, double-masked, contralateral study using the conjunctival allergen challenge (CAC) model. At Visit 1, subjects with a positive allergen skin test and a history of allergic conjunctivitis were administered increasing concentrations of allergen until at least a moderate grade 2 ocular itching and conjunctival redness response was obtained in both eyes. Allergic signs were graded on standardized 0-4 scales. Subjects who reacted positively were re-challenged at Visit 2 with the pre-determined concentration of allergen. Subjects who again responded with at least a grade 2 bilateral ocular itching and conjunctival redness score at Visit 2 were eligible for drug evaluation. At Visit 3, subjects received olopatadine in one eye and levocabastine in the contralateral eye according to a computer-generated randomization scheme generated prior to commencement of the study. Ocular discomfort was then graded in both eyes. Subjects were bilaterally challenged with the predetermined concentration of allergen 27 min after topical drug administration, such that the first post-challenge assessment was made 30 min post-drug instillation. Allergic signs and symptoms were evaluated at 3 min, 10 min, and 20 min postchallenge and safety and efficacy analyses were performed. RESULTS: Sixty-eight subjects received study drug and were included in the safety and efficacy analyses. Ocular itching scores for olopatadine were significantly lower than levocabastine at 3 min and 10 min post-challenge (p < 0.001). Ocular redness scores for olopatadine were significantly lower than levocabastine at all time points post-challenge (p < 0.0001). Of all subjects, 4.41% reported ocular discomfort in the olopatadine eye and 26.5% in the levocabastine treated eye. CONCLUSION: Olopatadine treated eyes had significantly less itching and redness than levocabastine treated eyes after conjunctival allergen challenge. Olopatadine was also associated with less discomfort upon instillation than levocabastine.     

Azithromycin 1.5% ophthalmic solution: in purulent bacterial or trachomatous conjunctivitis

The second-generation macrolide azithromycin is available as a 1.5% ophthalmic solution for use in the treatment of bacterial or trachomatous conjunctivitis. This article reviews the pharmacological properties of azithromycin 1.5% ophthalmic solution and its clinical efficacy and tolerability in patients with purulent bacterial conjunctivitis or trachomatous conjunctivitis caused by Chlamydia trachomatis. Azithromycin 1.5% ophthalmic solution had good in vitro activity against Haemophilus influenzae and C. trachomatis, and achieved good concentrations in tear samples from healthy volunteers. Azithromycin 1.5% ophthalmic solution for 3 days (1 drop twice daily) was noninferior to tobramycin 0.3% ophthalmic solution for 7 days (1 drop every 2 hours) in paediatric and adult patients with purulent bacterial conjunctivitis, with regard to clinical cure and bacteriological resolution on day 9, in a randomized, investigator-masked, multicentre study. In children with trachomatous inflammation, 3-day treatment with azithromycin 1.5% ophthalmic solution was noninferior to a single dose of azithromycin oral suspension, with regard to clinical cure rate in the worst eye at 60 days, in a randomized, double-masked, multicentre study. Azithromycin 1.5% ophthalmic solution was well tolerated in patients with bacterial or trachomatous conjunctivitis. Most events were of mild to moderate severity.     

Case in which tranilast ophthalmic solution was thought to be effective for the prevention of symblepharon and recurrence after pterygium surgery

We report our experience of a case in which a combination of conjunctival symblepharon detachment, conjunctival granuloma excision, and conjunctival free flap transplantation was performed for the treatment of symblepharon after pterygium surgery, with satisfactory outcomes. The patient was referred to our hospital with pterygium recurrence, symblepharon and granuloma formation after pterygium surgery in the right eye at another hospital. We performed conjunctival symblepharon detachment along with conjunctival autograft transplantation, and started instillation of tranilast ophthalmic solution immediately after the surgery, to inhibit proliferation and adhesion formation. During the 6 months' follow-up of the patient at our hospital, the postoperative course was satisfactory, and no recurrence of symblepharon, pterygium or granuloma was observed. There were no adverse drug reactions associated with the instillation of tranilast ophthalmic solution. Tranilast ophthalmic solution may be effective not only for prevention of pterygium recurrence, but also for inhibition of symblepharon and granuloma formation.     

Comparison of the safety and efficacy of loteprednol 0.5%/tobramycin 0.3% withdexamethasone 0.1%/tobramycin0.3% in the treatment of blepharokeratoconjunctivitis

ABSTRACT

Objective: This study compared the safety and efficacy of loteprednol etabonate 0.5%/tobramycin 0.3% (LE/T; Zylet) with dexamethasone 0.1%/tobramycin 0.3% (DM/T; Tobradex) in the treatment of ocular inflammation associated with blepharokeratoconjunctivitis.

Research design and methods: This was a multicenter, randomized, investigator-masked, parallel-group study. Subjects with clinically diagnosed blepharokeratoconjunctivitis in at least one eye were randomized to LE/T (n?=?138) or DM/T (n?=?138) administered four times per day, for 14 days. The primary efficacy endpoint was the change from baseline to Day 15 (± 1?day) in the signs and symptoms composite score using a non-inferiority metric to compare LE/T to DM/T. Safety endpoints included visual acuity (VA), biomicroscopy, intraocular pressure (IOP) assessments, and adverse events.

Results: At Day 15, the mean (SD) change from baseline in the signs and symptoms composite score was ?15.2 (7.3) for LE/T-treated subjects and ?15.6 (7.7) for DM/T-treated subjects. The upper bound of the 90% confidence interval for the difference in change from baseline was less than the non-inferiority margin not only at Day 15 but also at Day 7 and Day 3 for both the intent-to-treat and per protocol populations. Subjects treated with DM/T experienced a significant increase in IOP versus those treated with LE/T at Day 7, Day 15, and overall (mean [SD] of 0.6 [2.3] vs, ?0.1 [2.2], p?=?0.03, 1.0 [3.0] vs. ?0.1 [2.4], p?=?0.01, and 2.3 [2.3] vs. 1.6 [1.7], p?=?0.02, respectively).

Conclusions: LE/T satisfied the condition of non-inferiority to DM/T in decreasing the signs and symptoms of ocular inflammation associated with blepharokeratoconjunctivitis. Subjects treated with DM/T experienced more of an increase in IOP.

Limitation: Although the single-masked design of this study could be considered a limitation, care was taken to ensure that the investigator was masked.     

The effect of gatifloxacin 0.3% or moxifloxacin 0.5% on corneal healing,ocular tolerability and toxicity following pterygium surgery

Purpose: To compare the rate of corneal epithelial healing and ocular tolerability following pterygium surgery between gatifloxacin and moxifloxacin.

Methods: In this double masked, prospective, controlled study 40 patients were randomized to receive prophylactic topical gatifloxacin 0.3% or moxifloxacin 0.5% following pterygium surgery. Patients were examined on days 1, 3, 7 and 21 post-operatively or until complete corneal epithelial healing. The primary outcome measure was the area of corneal epithelial defect during the post-operative period. Patients graded post-operative ocular pain, foreign body sensation, tearing, general burning sensation and burning sensation post-antibiotic drops instillation on a scale of 1–5. Conjunctival hyperemia and superficial punctate keratopathy (SPK) were measured on a scale of 0–3.

Results: No significant differences between groups were found in terms of corneal epithelial defect percentage over time (p?=?0.989) and there was no significant difference between groups on each of the post-operative days. No significant differences were noted in terms of post-operative ocular pain, foreign body sensation, tearing, general burning sensation, burning sensation post-antibiotic drops instillation, conjunctival hyperemia and SPK.

Conclusions: Gatifloxacin and moxifloxacin showed equivalent results in terms of corneal epithelial healing and ocular tolerability following pterygium surgery. This study suggests that there was no apparent added epithelial toxicity due to the presence of benzalkonium chloride in the gatifloxacin preparation when compared to moxifloxacin.     

复方妥布霉素滴眼液的质量控制及刺激性研究

目的:建立复方妥布霉素滴眼液的质量控制方法并对其进行刺激性研究。方法:采用高效液相色谱法测定复方妥布霉素滴眼液中主药的含量。给家兔右眼滴用复方妥布霉素滴眼液,每天5次,连续21 d后观察兔眼结膜、角膜、虹膜的刺激反应并评分。结果:妥布霉素和地塞米松分别在10.00～100.00 mg·L^-1（r=0.999 7）和6.25～200.00 mg·L^-1（r=0.999 8）范围内呈良好的线性关系,家兔眼刺激的综合平均分值在0～2范围内。结论:该方法简便快速,结果准确可靠,可用于复方妥布霉素滴眼液的定量分析。该滴眼液对家兔眼无明显刺激。     

Intraocular pressure lowering effect of brinzolamide 1.0% as adjunctive therapy to latanoprost 0.005% in patients with open angle glaucoma or ocular hypertension: an uncontrolled, open-label study

PURPOSE: A prospective study was conducted to evaluate the intraocular pressure (IOP) lowering effect of brinzolamide 1.0% ophthalmic suspension as an adjunctive therapy with latanoprost 0.005% ophthalmic solution in patients with open angle glaucoma or ocular hypertension. PATIENTS AND METHODS: Fourteen patients with open angle glaucoma (OAG) or ocular hypertension (OH) who had been using latanoprost 0.005% for more than 6 months were initiated on adjunctive brinzolamide therapy. The IOP values at 1 month, 2 months, and 3 months were compared with those measured immediately before adding brinzolamide to the regimen (baseline). The incidence of adverse events such as conjunctival hyperemia and corneal epithelial defect were also examined. RESULTS: The baseline IOP was 21.1 +/- 4.8 mmHg (mean +/- standard deviation). After 1 month, 2 months, and 3 months of therapy IOP was 16.9 +/- 4.5 mmHg, 16.6 +/- 4.0 mmHg, and 15.9 +/- 3.1 mmHg, respectively, showing significant reductions in IOP at all the measuring time-points during the study compared with the baseline value (p < 0.01). Conjunctival hyperemia developed in one patient after 1 month and in another after 2 months; however, both were mild, and therapy was continued. Corneal epithelium defect was observed in 3 patients. One of them had mild defect before brinzolamide was added to the regimen. Increase of eye discharge was seen in one patient. No serious side effects were otherwise observed. CONCLUSION: The addition of brinzolamide to a latanoprost 0.005% regimen may further lower intraocular pressure in patients with open angle glaucoma or ocular hypertension.