Prednisolone Acetate Suspension Research Articles

Loteprednol etabonate gel 0.5% vs prednisolone acetate suspension 1% for the treatment of inflammation after cataract surgery in children.

To compare loteprednol etabonate (LE) gel 0.5% with prednisolone acetate suspension (PA) 1% for the treatment of inflammation after cataract surgery in children. Eleven sites in the United States. Randomized, double-masked, parallel-group, noninferiority study. Eligible patients were aged 11 years or younger and candidates for routine, uncomplicated cataract surgery. Patients were randomized to a 4-week postsurgical regimen with LE gel 0.5% or PA 1%, twice on the day of surgery, 4 times daily for 2 weeks, twice daily for 1 week, and once daily for 1 week. Assessments included anterior chamber (AC) cells/flare, anterior chamber inflammation (ACI), synechiae, precipitates on the intraocular lens/cornea, visual acuity, and intraocular pressure. The intent-to-treat population comprised 105 patients (LE gel, n = 53; PA 1%, n = 52) including 52 patients aged 3 years or younger. Patients achieved a similar mean ACI grade on postoperative day 14 (primary efficacy endpoint) whether treated with LE gel 0.5% or PA 1% (difference = 0.006, 2-sided 95% CI, -0.281 to 0.292). Similar ACI outcomes additionally were observed in patients aged 3 years or younger. LE gel 0.5% and PA 1% also appeared equally effective in resolving inflammation at all visits (days 7, 14, and 28 postsurgery), based on categorical distributions of ACI, AC cells, and AC flare scores/grades (P ≥ .06). Synechiae and corneal/IOL precipitates occurred infrequently with no significant differences between groups. No safety or tolerability concerns were identified, including no treatment-related IOP increases. LE gel 0.5% was safe and effective in treating pediatric postcataract surgical inflammation, with similar outcomes as PA 1%.

Acute Idiopathic Endotheliitis Early After Corneal Cross-linking With Riboflavin and Ultraviolet-A

To present a case of acute idiopathic endotheliitis occurred early after corneal collagen cross-linking (CXL) for progressive keratoconus, and to discuss possible risk factors, causes, and other similar complications in the literature. A 24-year-old woman with bilateral keratoconus underwent a corneal de-epithelization and subsequently CXL in the right eye, which was performed with the application of 0.1% riboflavin with 20% dextran, and exposure to ultraviolet-A light (370 nm, 2.9-3.1 mW/cm) for 30 minutes. A bandage contact lens was placed until complete re-epithelialization. Postoperatively, the patient received 0.5% topical moxifloxacin (3 times a day) and preservative free artificial tears (6 times a day). Postoperatively, the patient presented with significant hyperemia and photophobia on day 3. On biomicroscopy, ring-shaped endothelial infiltrates and localized corneal edema were observed in the inferior paracentral location of the cornea. Idiopathic endotheliitis was diagnosed, the therapeutic contact lens was removed, and 1% prednisolone acetate suspension was started every hour in addition to hypertonic ophthalmic solution every 3 hours. After this intensive corticosteroid treatment, the infiltrates improved and completely resolved after 1 week. We reported a successfully treated acute idiopathic endotheliitis occurring early after routine CXL. This very rare complication is hypothesized to occur as a result of the phototoxic effect of ultraviolet-A transmission on the corneal endothelium, or as an inflammatory response to surgical trauma or solutions used throughout the procedure.

Comparison of Efficacy and Ocular Surface Toxicity of Topical Preservative-free Methylprednisolone and Preserved Prednisolone in the Treatment of Acute Anterior Uveitis

The aim of this study was to compare the antiinflammatory effect and ocular surface toxicity of topical nonpreserved methylprednisolone sodium succinate 1% and preserved prednisolone acetate suspension 1% for the management of acute anterior uveitis (AAU). In this prospective, randomized, investigator-masked, comparative clinical trial, patients with mild-to-moderate noninfectious AAU were assigned randomly to receive either hourly nonpreserved methylprednisolone 1% (group A) or preserved prednisolone 1% (group B) eye drops followed by a 2-week tapering regimen. Anterior chamber cells and flare were clinically evaluated for the objective comparison of the antiinflammatory effect. The main outcome measure was the percentage of patients with a resolution of inflammation (anterior chamber cells <1+) on day 14. Ocular surface toxicity was assessed by means of the corneal fluorescein staining score, tear breakup time, Schirmer I test, and questionnaire-based grading of ocular discomfort parameters. Seventy-two eyes of 68 patients were studied, of which 38 eyes were enrolled in group A and 34 eyes were enrolled in group B. On day 14, 76.3% of the patients in group A had resolution of inflammation compared with 70.6% of the patients in group B, proving noninferiority (χ = 0.303, P = 0.582). The mean anterior chamber cell grade reduction for patients in group A was similar to that in group B (2.52 vs. 2.86, respectively; P = 0.92). Group A patients showed significantly lower corneal fluorescein staining scores (P < 0.001) and reported milder subjective ocular discomfort (0.55 vs. 1.43, P = 0.01) as compared with group B. Both preparations demonstrated equal antiinflammatory effects for the treatment of AAU. Nonpreserved methylprednisolone eye drops exhibited a significantly lower ocular surface toxicity profile and milder subjective discomfort when compared with that exhibited by preserved prednisolone.

Alopecia following oral acyclovir for the treatment of herpes simplex keratitis

The authors report acyclovir-induced alopecia in a patient treated for herpetic keratouveitis. A 32-years-old female was diagnosed with herpetic keratouveitis. She was placed on prednisolone acetate (1%) suspension four times a day, atropine sulfate (1%) thrice a day, and oral acyclovir 400 mg twice-daily. Three weeks following oral acylovir, keratouveitis improved, but she developed alopecia without any drug eruptions. Oral acyclovir was discontinued. Three months later, alopecia completely resolved. Alopecia may be considered a possible complication following oral acyclovir.

Dose uniformity of loteprednol etabonate ophthalmic gel (0.5%) compared with branded and generic prednisolone acetate ophthalmic suspension (1%)

IntroductionLoteprednol etabonate (LE) ophthalmic gel 0.5% (Lotemax®) is a new polycarbophil-based, nonsettling topical ophthalmic formulation. The formulation is a semisolid gel at rest and a shear thinning fluid when expressed through a dropper tip. The present study was undertaken to determine how the nonsettling character of LE ophthalmic gel affects dose uniformity. Prednisolone acetate ophthalmic suspension 1% (Pred Forte®) and a generic prednisolone acetate suspension 1% were used as comparators.MethodsDrug concentrations of LE ophthalmic gel, Pred Forte, and a generic prednisolone acetate suspension were determined following simulated dosing – consisting of 2 drops, expressed four times daily for 2 weeks, with bottles that were shaken or not shaken immediately prior to expressing the drops. Drug concentrations were determined using a reverse-phase high-performance liquid chromatography (HPLC) method and reported as a percentage of the declared (labeled) concentration. Comparative kinetics of drug particle sedimentation were also determined for each formulation, using dispersion analysis under gravity.ResultsMean drug concentrations in drops of all three formulations were within a few percentage points of the declared concentration when the bottles were shaken for 5 seconds prior to dispensing. Only LE ophthalmic gel showed consistent and on-target concentrations when the bottles were unshaken prior to dispensing, with a mean (standard deviation [SD]) percent declared concentration of 102% (1.92%) over the 2-week dosing regimen. Drug concentrations for the branded and generic prednisolone acetate suspensions following expression from unshaken bottles were highly variable (overall relative SDs of 16.8% and 20.3%, respectively), with mean concentrations for both falling significantly below the declared concentration for drops expressed at the beginning of the 2-week dosing regimen and significantly above the declared concentration for drops expressed near the end of the dosing regimen. Dispersion analysis at 120× g showed no drug particle sedimentation for LE ophthalmic gel over the 24-hour testing period, whereas the prednisolone acetate suspensions settled in less than 6 hours.ConclusionLE ophthalmic gel 0.5% provided consistent dose uniformity at the declared concentration whether or not the bottle was shaken prior to dispensing, whereas Pred Forte® and the generic prednisolone acetate required shaking to provide consistent drug concentrations. LE ophthalmic gel may be beneficial to patients because it eliminates the potential impact on the clinical response of both under- and overdosing.

Evaluation of four drugs for inhibition of paracentesis-induced blood-aqueous humor barrier breakdown in cats

To compare inhibitory effects of topically applied 1% prednisolone acetate suspension, 0.03% flurbiprofen solution, 0.1% dexamethasone suspension, and 0.1% diclofenac solution on paracentesis-induced blood-aqueous barrier breakdown in cats. 9 healthy cats. Paracentesis of the anterior chamber was performed in both eyes of each cat. One eye of each cat was treated with a topically administered anti-inflammatory medication (1% prednisolone [n = 7 cats], 0.03% flurbiprofen [7], 0.1% dexamethasone [9], or 0.1% diclofenac [8]) immediately following paracentesis and at 6, 10, and 24 hours after paracentesis. The contralateral untreated eye served as the control eye. Each cat had a 6-day washout period between experimental drugs. Breakdown of the blood-aqueous barrier was quantified by use of laser flaremetry. Topical administration of 1% prednisolone significantly reduced aqueous humor flare at 4, 8, and 26 hours after paracentesis. Topical administration of 0.1% diclofenac significantly reduced aqueous humor flare at 8 and 26 hours after paracentesis. Topical administration of 0.1% dexamethasone and 0.03% flurbiprofen did not significantly decrease flare at any time point. There were significant differences in intraocular pressures between NSAID-treated eyes and untreated contralateral eyes. Topical administration of 1% prednisolone and 0.1% diclofenac significantly reduced intraocular inflammation in cats with paracentesis-induced uveitis. Topical administration of 1% prednisolone or 0.1% diclofenac may be appropriate choices when treating cats with anterior uveitis. Topical administration of diclofenac and flurbiprofen should be used with caution in cats with a history of ocular hypertension.

Dose uniformity of topical corticosteroid preparations: difluprednate ophthalmic emulsion 0.05% versus branded and generic prednisolone acetate ophthalmic suspension 1%

PurposeTo compare the dose uniformity of difluprednate ophthalmic emulsion 0.05% (Durezol®) with both branded and generic prednisolone acetate ophthalmic suspension 1% under different simulated patient usage conditions.MethodsDrug concentrations of difluprednate emulsion, branded prednisolone acetate suspension (Pred Forte®) and generic prednisolone acetate suspension following three storage conditions (upright, then shaken; upright, not shaken; inverted, not shaken) were analyzed by high performance liquid chromatography assay and results were reported as percent of declared concentration. Two drops were dispensed every four hours four times daily.ResultsRegardless of bottle orientation and shaking, all difluprednate emulsion concentrations at each time point analyzed were within 15% of declared concentration. Both branded and generic prednisolone acetate suspension concentrations varied substantially throughout the study. For the bottle stored upright and not shaken, 46% of the branded concentrations were not within 15% of declared concentration; for the bottle stored upright and shaken prior to use, 60% failed to meet this criterion. None of the branded concentrations from the inverted and not shaken bottle was within 15% of declared concentration. Generic prednisolone concentrations demonstrated the poorest dose uniformity, with 96% of the concentrations from the inverted and not shaken bottle not within 15% of declared concentration; 94% of the concentrations from the upright and shaken bottle and 87% from the upright and not shaken bottle similarly failed to meet this criterion.ConclusionsDose uniformity of Durezol emulsion was predictable in all simulated patient usage conditions, whereas the drop concentrations of Pred Forte and generic prednisolone acetate suspensions were highly variable throughout the study. Drop concentrations are more predictable with Durezol emulsion than with either prednisolone acetate suspension.

Comparative Analysis of Prednisolone Acetate Suspensions

The aim of this study was to determine differences in particle size between three prednisolone acetate suspensions: Pred Forte, EconoPred Plus, and generic prednisolone acetate 1%. This study employed the setting of a laboratory evaluation. Qualitative assessment of sedimentation rate as a function of particle size was the method employed for this study. Samples of the three products were taken from the top of the suspensions at 0 and 6 h and then at 12-h intervals from 12 to 72 h. At 72 h, a sample was pulled from the bottom of each suspension. Particle size in aliquots removed from the top of the suspensions steadily decreased over time. In the Pred Forte sample, results for 72 h (bottom) were consistent with T = 0 h results. In the generic and EconoPred Plus lots, the T = 72 h (bottom) results exceeded the T = 0 h results, suggesting a tendency for these particles to agglomerate more readily. The prednisolone particles in Pred Forte were smaller and more uniform at all time points, allowing them to stay in suspension longer. This may result in greater homogeneity between doses and increased ocular bioavailability.

In vivo Morphological Changes in Rat Lenses Induced by the Administration of Prednisolone after Subliminal X-lrradiation

In order to induce steroid cataracts in rat lenses, prednisolone acetate was administered together with a single subliminal dose of X-irradiation, which was applied unilaterally before steroid application started. The rats were divided into a control group (without prednisolone acetate administration), a group with a topically administered daily dose of 1 mg/kg prednisolone acetate suspension and a group with a systemically applied daily dose of 0.8-1.0 mg/kg prednisolone acetate suspension. Changes in the lens were objectively evaluated with in vivo Scheimpflug slit images during a 30-week period. Although body weight increase was significantly affected in both groups administered prednisolone, animals survived until the end of the observation period. The initial changes in the lens were the dissociation of the Y-suture and a slight increase in scattering light intensity at the posterior embryonic nucleus after both topical and systemic steroid administration.

Dissolution performance related to particle size distribution for cohpiercially available prednisolone acetate suspensions

AbstractDissolution performance for three commercially available parenteral prednisolone acetate suspensions was analyzed using a diffusion based model. Physicochemical properties of the drug and particle size characteristics of the formulation were included in the model as important determinants of dissolution performance.The model describes the dissolution profile for each formulation with a single characteristic value, the dissolution rate constant. For Products I and II with similar particle size characteristics, the model sufficiently describes the dissolution profile for each formulation but does not provide conclusive evidence about reasons for differences in dissolution performance between the two products. For Product III, the model sufficiently describes the dissolution profile and adequately includes the effect of a bimodal distribution of larger drug particles.This approach to the analysis of dissolution data for suspension formulations is suggested as being useful during the formulation proce...

Comparative Corneal Penetration of Prednisolone Sodium Phosphate and Prednisolone Acetate in NZW Rabbits

Comparative corneal penetration studies in the literature with prednisolone sodium phosphate solution and prednisolone acetate suspension administered to rabbit eyes give conflicting results concerning the greater bioavailability of prednisolone acetate. A recent in vitro penetration study shows similar fluxes for both salt forms in terms of prednisolone, quantified by a specific HPLC assay. An in vivo comparison has been conducted in NZW rabbit eyes and shows similar bioavailability for both drugs. Prednisolone sodium phosphate, prednisolone acetate and the primary metabolite prednisolone are quantified by a specific HPLC assay in aqueous humor.

Leaching of antioxidants and vulcanization accelerators from rubber closures into drug preparations

A thin-layer chromatographic method was used to highlight the leaching into drug preparations of several constituents of elastomeric closures. Among the 150 preparations analysed, the twenty-eight local anaesthetics presented in single-dose delivery syringe-cartridges, one Epinephrine injection in prefilled syringes, eight insulin preparations and two Prednisolone acetate suspensions in the form of small volume flasks (less than or equal to 20 ml) were contaminated by one or more of the following: 2-mercaptobenzothiazole (MBT), 2-mercaptobenzothiazole disulphide and 2-mercaptobenzimidazole (MBI). Prednisolone acetate suspensions also contained 2,2'-methylene-bis(4-methyl-6-alpha-methylcyclohexylphenol). No contamination was found in drug preparations presented in large volume flasks (250-1000 ml). 2-(2-Hydroxyethylthio)-benzothiazole was not present, which indicated that the rubbers had not been sterilized with ethylene oxide. Elastomeric parts of drug closures analysed in the same way contained the same compounds as those found in drugs, one case excepted, which confirms the origin of the contamination. The lowest and the highest concentrations were found in syringe-cartridges; they ranged from 8.3 to 13.8 micrograms ml-1 for MBT, from 2.9 to 9.3 micrograms ml-1 for MBTS and from 2.8 to 11.1 micrograms ml-1 for MBI. Variable results were obtained, for a same preparation, depending upon the batches analysed, which indicates that rubber formulations and/or vulcanization conditions differed. The allergenic, toxic, embryotoxic and mutagenic properties of the compounds leached are discussed.

Biological Equivalence of Ophthalmic Prednisolone Acetate Suspensions

We compared both concentrations (0.125 and 1.0%) of two widely used commmerical brands of prednisolone acetate suspensions. We investigated the concentration that each product attained in the cornea and aqueous humor, and each product's anti-inflammatory effectiveness in the cornea. There was no statistically significant difference in the corticosteroid levels measured in cornea or aqueous humor after administration of the two suspensions. Similarly, there was no significant difference in the ability of the two commercial preparations to suppress corneal inflammation.