The Experts below are selected from a list of 351 Experts worldwide ranked by ideXlab platform
Mitra Jelvehgari - One of the best experts on this subject based on the ideXlab platform.
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fabrication and in vitro evaluation of Ketotifen Fumarate loaded plga nanoparticles as a sustained delivery system
Iranian Journal of Pharmaceutical Research, 2017Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Ketotifen Fumarate is a non-bronchodilator anti-asthmatic drug which inhibits the effects of certain endogenous substances known to be inflammatory mediators, and thereby exerts antiallergic activity. The present study describes the formulation of a sustained release nanoparticle (NP) drug delivery system containing ketoftifen, using poly (D,L lactide-co-glycolide) acid (PLGA). Biodegradable NPs were prepared using 50 : 50 PLGA by a water in-oil-in-water (w/o/w) double emulsion-solvent evaporation procedure and characterized for drug content, DSC (differential scanning calorimetry, XRD (X-ray diffractionl), FTIR (Fourier transform spectroscopy), particle size , surface morphology using scanning electron microscopy, and drug release rate. The effects of different drug-to-polymer ratios on the characteristics of the NPs were investigated. NPs prepared were spherical with a smooth surface. Size of NPs was dependent on the concentration of polymer (10 mg/mL, 754.6 nm). Increasing the external organic phase volume (primary emulsion) resulted in larger particles with higher encapsulation efficiency (55%). The best drug to polymer ratio in the NP was F3 (1:10 ratio) which showed loading efficiency of 55%, and mean particle size of 754.6 nm, respectively. The FTIR, XRPD, and DSC results ruled out any chemical interaction between the drug and PLGA. The NPs prepared with low ratio of drug to polymer (1:5) F1 formulation showed faster dissolution rate than those with high drug to polymer ratio (1:10) F3 formulation. In conclusion, by selecting an appropriate level of the investigated parameters, spherical NPs with encapsulation efficiencies higher than 55% and a prolonged drug release over 24h (73.67-90.05%) were obtained.
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comparison of different nanosuspensions as potential ophthalmic delivery systems for Ketotifen Fumarate
Advanced Pharmaceutical Bulletin, 2016Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Purpose: The objective of this study was to develop, characterize, and comparatively investigate the Ketotifen Fumarate (KF) nanosuspensions (NSS) to enhance the permeability of KF. Methods: In the present work, the NSP and NSE were prepared by double-emulsion solvent evaporation/nanoprecipitation methods with poly (D,Llactide-co-glycolide) and Eudragit RL100 polymers, respectively. The loading efficiency, particle size, and polydispersity index of prepared different NSs were evaluated with scanning electron microscopy (SEM), X-ray diffraction, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and in vitro release and transcorneal permeation . NSs were also compared on the basis of particle size and polydispersity index. Results: Particle size, polydispersity index, and loading efficiency of NSP1 and NSE3 showed the best value (158 nm, 117 nm, 0.21, 0.43 and 43%, 95.23%, respectively). SEM showed spherical globules and DSC results showed the reduction in crystallinity. The NSE3 formulations demonstrated significantly (p<0.05) higher drug release rates than the NSP1 due to increases in the surface area. Comparative studies showed that NSE release and permeability are higher than NSP. Conclusion: It is concluded that both NSP and NSE provide a useful dosage form for the ocular drug delivery which can enhance the permeability of KF.
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design of eudragit rl nanoparticles by nanoemulsion method as carriers for ophthalmic drug delivery of Ketotifen Fumarate
Iranian Journal of Basic Medical Sciences, 2016Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Objective(s): Ketotifen Fumarate (KF) is a selective and noncompetitive histamine antagonist (H1-receptor) that is used topically in the treatment of allergic conditions of rhinitis and conjunctivitis. The aim of this study was to formulate and improve an ophthalmic delivery system of KF.Ocular nanoparticles were prepared with the objective of reducing the frequency of administration and obtaining controlled release to improve the anti-inflammatory drug delivery. Materials and Methods:In the present study, ocular KF loaded Eudragit RL 100 nanoparticles were prepared using O/W solvent diffusion method. The nanoparticles were evaluated for particle size, entrapment efficiency, surface morphology, X-ray diffraction (XRD), Fourier transform spectroscopy (FTIR), and differential scanning calorimetry (DSC). In vitro release and permeation studies were also carried out on nanoparticles. Results: An average size range of 182 to 314.30 nm in diameter was obtained and encapsulation efficiency up to 95.0% was observed for all the formulations. Drug release for all formulations after 24 hr was between 65.51% and 88.82% indicating effective controlled release property of KF. The mechanism of drug release for best formulation was found to be fickian diffusion mechanism. KF nanoparticles containing high polymer concentration (1:15) presented a faster drug release and a higher drug penetration; on the contrary, nanoparticles containing low polymer concentration (1:7.5) were able to give a more sustained release of the drug and thus a slower KF permeation through the cornea. Conclusion: The study revealed that KF NPs were capable of releasing the drug for a prolonged period of time and increasing the ocular bioavailability.
René Lanz - One of the best experts on this subject based on the ideXlab platform.
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efficacy and safety of Ketotifen eye drops in the treatment of seasonal allergic conjunctivitis
British Journal of Ophthalmology, 2003Co-Authors: Michael Kidd, Suzanne Mckenzie, I Steven, Chris Cooper, René LanzAbstract:Background: Ketotifen blocks histamine H1 receptors, stabilises mast cells, and prevents eosinophil accumulation. These multiple, pharmacological mechanisms provided the rationale for assessing the efficacy and safety of Ketotifen 0.025% eye drops in subjects with seasonal allergic conjunctivitis (SAC) in an environmental setting. Methods: This was a double masked, randomised, multicentre trial conducted in Australia. Subjects were randomly assigned to Ketotifen Fumarate 0.025% ophthalmic solution, placebo (as vehicle), or levocabastine hydrochloride 0.05% ophthalmic suspension, twice daily in each eye for a 4 week period. Subjects were assessed at follow up (days 5–8) and termination (days 25–31) visits. The primary efficacy variable was the responder rate, based on the subjects’ assessment of global efficacy at the follow up visit. Results: 519 subjects were randomised to treatment. At the follow up visit, the responder rate, based on subjects’ assessment of global efficacy, was significantly greater in the Ketotifen group (49.5%) than in the placebo group (33.0%) for subjects with a positive diagnostic test for pollen allergy (p = 0.02). The investigators’ assessment of responder rates also showed that Ketotifen was superior to placebo (p = 0.001). Ketotifen produced a significantly better outcome than levocabastine (p<0.05) for relief of signs and symptoms of SAC, at both the follow up and the termination visit. The type and frequency of adverse events were similar across treatment groups. Conclusions: In an environmental setting, Ketotifen Fumarate 0.025% ophthalmic solution was well tolerated and effective in reducing the signs and symptoms of SAC, and in preventing their recurrence. Ketotifen consistently showed the best efficacy in comparison with both placebo and levocabastine. These results indicate that Ketotifen eye drops are a valuable treatment option for this condition.
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onset and duration of action of Ketotifen 0 025 and emedastine 0 05 in seasonal allergic conjunctivitis efficacy after repeated pollen challenges in the vienna challenge chamber
Clinical Drug Investigation, 2003Co-Authors: Friedrich Horak, René Zieglmayer, Alexander Kawina, Michael Moser, Petra Stubner, René LanzAbstract:Objective: To compare the efficacy, onset and duration of action, and the safety of Ketotifen Fumarate 0.025% ophthalmic solution and emedastine diFumarate 0.05% ophthalmic solution in subjects with seasonal allergic conjunctivitis (SAC) induced by allergen exposure, using the Vienna Challenge Chamber model.
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onset and duration of action of Ketotifen 0 025 and emedastine 0 05 in seasonal allergic conjunctivitis efficacy after repeated pollen challenges in the vienna challenge chamber
Clinical Drug Investigation, 2003Co-Authors: Friedrich Horak, René Zieglmayer, Alexander Kawina, Michael Moser, Petra Stubner, René LanzAbstract:Objective: To compare the efficacy, onset and duration of action, and the safety of Ketotifen Fumarate 0.025% ophthalmic solution and emedastine diFumarate 0.05% ophthalmic solution in subjects with seasonal allergic conjunctivitis (SAC) induced by allergen exposure, using the Vienna Challenge Chamber model. Design and setting: This was a double-masked, randomised, comparative, crossover study conducted at an allergy outpatient clinic in Austria. Study participants: Subjects with an allergy to grass pollen were exposed to the allergen in a pollen chamber for 4 hours, followed by a 3-hour break and then a second exposure for 3 hours. Interventions: Study participants were randomised to a treatment sequence (Ketotifen followed by emedastine or emedastine followed by Ketotifen), receiving 1 drop per eye of Ketotifen or emedastine 2 hours after the initial allergen exposure in the pollen chamber. Outcomes: Individual and composite ocular, individual and composite nasal, and total (ocular + nasal) symptom complex scores were determined by repeated exposure to allergen 0–2 hours and 5–8 hours after dosing. Onset of action was defined as the time to the first observation of a 20% reduction from baseline in the composite ocular symptom score. Results: All 37 subjects enrolled completed the study. The median time to onset of action was 15 minutes for Ketotifen and 30 minutes for emedastine. This difference was significant using the generalised linear model (p = 0.048), but not for the log-rank test analysis. In the initial 2 hours post dose, Ketotifen provided significantly greater relief of both composite ocular symptoms (p = 0.026) and total symptom complex (p = 0.014). Both medications were effective in reducing symptoms 5 to 8 hours after dosing. No adverse events were reported for either treatment. Conclusions: In the Vienna Challenge Chamber model, Ketotifen and emedastine both effectively alleviated ocular symptoms of SAC after single-dose administration. Ketotifen had a faster onset of action and provided better symptom relief than emedastine during the first 2 hours after dosing. The rapid onset of action and symptom control make Ketotifen a valuable treatment for SAC.
Xinsong Li - One of the best experts on this subject based on the ideXlab platform.
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in vitro and in vivo evaluation of Ketotifen Fumarate loaded silicone hydrogel contact lenses for ocular drug delivery
Drug Delivery, 2011Co-Authors: Jinku Xu, Xinsong LiAbstract:The purpose of this work was to evaluate the usefulness of silicone hydrogel contact lenses loaded with Ketotifen Fumarate for ocular drug delivery. First, silicone contact lenses were prepared by photopolymerization of bitelechelic methacrylated polydimethylsiloxanes macromonomer, 3-methacryloxypropyltris(trimethylsiloxy)silane, and N,N-dimethylacrylamide using ethylene glycol dimethacrylate as a cross-linker and Darocur 1173 as an initiator followed by surface plasma treatment. Then, the silicone hydrogel matrices of the contact lenses were characterized by equilibrium swelling ratio (ESR), tensile tests, ion permeability, and surface contact angle. Finally, the contact lenses were loaded with Ketotifen Fumarate by pre-soaking in drug solution to evaluate drug loading capacity, in vitro and in vivo release behavior of the silicone contact lenses. The results showed that ESR and ion permeability increase, and the surface contact angle and tensile strength decreased with the increase of DMA component in t...
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in vitro and in vivo evaluation of Ketotifen Fumarate loaded silicone hydrogel contact lenses for ocular drug delivery
Drug Delivery, 2011Co-Authors: Jinku Xu, Xinsong LiAbstract:The purpose of this work was to evaluate the usefulness of silicone hydrogel contact lenses loaded with Ketotifen Fumarate for ocular drug delivery. First, silicone contact lenses were prepared by photopolymerization of bitelechelic methacrylated polydimethylsiloxanes macromonomer, 3-methacryloxypropyltris(trimethylsiloxy)silane, and N,N-dimethylacrylamide using ethylene glycol dimethacrylate as a cross-linker and Darocur 1173 as an initiator followed by surface plasma treatment. Then, the silicone hydrogel matrices of the contact lenses were characterized by equilibrium swelling ratio (ESR), tensile tests, ion permeability, and surface contact angle. Finally, the contact lenses were loaded with Ketotifen Fumarate by pre-soaking in drug solution to evaluate drug loading capacity, in vitro and in vivo release behavior of the silicone contact lenses. The results showed that ESR and ion permeability increase, and the surface contact angle and tensile strength decreased with the increase of DMA component in t...
Saieede Soltani - One of the best experts on this subject based on the ideXlab platform.
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fabrication and in vitro evaluation of Ketotifen Fumarate loaded plga nanoparticles as a sustained delivery system
Iranian Journal of Pharmaceutical Research, 2017Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Ketotifen Fumarate is a non-bronchodilator anti-asthmatic drug which inhibits the effects of certain endogenous substances known to be inflammatory mediators, and thereby exerts antiallergic activity. The present study describes the formulation of a sustained release nanoparticle (NP) drug delivery system containing ketoftifen, using poly (D,L lactide-co-glycolide) acid (PLGA). Biodegradable NPs were prepared using 50 : 50 PLGA by a water in-oil-in-water (w/o/w) double emulsion-solvent evaporation procedure and characterized for drug content, DSC (differential scanning calorimetry, XRD (X-ray diffractionl), FTIR (Fourier transform spectroscopy), particle size , surface morphology using scanning electron microscopy, and drug release rate. The effects of different drug-to-polymer ratios on the characteristics of the NPs were investigated. NPs prepared were spherical with a smooth surface. Size of NPs was dependent on the concentration of polymer (10 mg/mL, 754.6 nm). Increasing the external organic phase volume (primary emulsion) resulted in larger particles with higher encapsulation efficiency (55%). The best drug to polymer ratio in the NP was F3 (1:10 ratio) which showed loading efficiency of 55%, and mean particle size of 754.6 nm, respectively. The FTIR, XRPD, and DSC results ruled out any chemical interaction between the drug and PLGA. The NPs prepared with low ratio of drug to polymer (1:5) F1 formulation showed faster dissolution rate than those with high drug to polymer ratio (1:10) F3 formulation. In conclusion, by selecting an appropriate level of the investigated parameters, spherical NPs with encapsulation efficiencies higher than 55% and a prolonged drug release over 24h (73.67-90.05%) were obtained.
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comparison of different nanosuspensions as potential ophthalmic delivery systems for Ketotifen Fumarate
Advanced Pharmaceutical Bulletin, 2016Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Purpose: The objective of this study was to develop, characterize, and comparatively investigate the Ketotifen Fumarate (KF) nanosuspensions (NSS) to enhance the permeability of KF. Methods: In the present work, the NSP and NSE were prepared by double-emulsion solvent evaporation/nanoprecipitation methods with poly (D,Llactide-co-glycolide) and Eudragit RL100 polymers, respectively. The loading efficiency, particle size, and polydispersity index of prepared different NSs were evaluated with scanning electron microscopy (SEM), X-ray diffraction, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and in vitro release and transcorneal permeation . NSs were also compared on the basis of particle size and polydispersity index. Results: Particle size, polydispersity index, and loading efficiency of NSP1 and NSE3 showed the best value (158 nm, 117 nm, 0.21, 0.43 and 43%, 95.23%, respectively). SEM showed spherical globules and DSC results showed the reduction in crystallinity. The NSE3 formulations demonstrated significantly (p<0.05) higher drug release rates than the NSP1 due to increases in the surface area. Comparative studies showed that NSE release and permeability are higher than NSP. Conclusion: It is concluded that both NSP and NSE provide a useful dosage form for the ocular drug delivery which can enhance the permeability of KF.
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design of eudragit rl nanoparticles by nanoemulsion method as carriers for ophthalmic drug delivery of Ketotifen Fumarate
Iranian Journal of Basic Medical Sciences, 2016Co-Authors: Saieede Soltani, Parvin Zakerimilani, Mohammad Barzegarjalali, Mitra JelvehgariAbstract:Objective(s): Ketotifen Fumarate (KF) is a selective and noncompetitive histamine antagonist (H1-receptor) that is used topically in the treatment of allergic conditions of rhinitis and conjunctivitis. The aim of this study was to formulate and improve an ophthalmic delivery system of KF.Ocular nanoparticles were prepared with the objective of reducing the frequency of administration and obtaining controlled release to improve the anti-inflammatory drug delivery. Materials and Methods:In the present study, ocular KF loaded Eudragit RL 100 nanoparticles were prepared using O/W solvent diffusion method. The nanoparticles were evaluated for particle size, entrapment efficiency, surface morphology, X-ray diffraction (XRD), Fourier transform spectroscopy (FTIR), and differential scanning calorimetry (DSC). In vitro release and permeation studies were also carried out on nanoparticles. Results: An average size range of 182 to 314.30 nm in diameter was obtained and encapsulation efficiency up to 95.0% was observed for all the formulations. Drug release for all formulations after 24 hr was between 65.51% and 88.82% indicating effective controlled release property of KF. The mechanism of drug release for best formulation was found to be fickian diffusion mechanism. KF nanoparticles containing high polymer concentration (1:15) presented a faster drug release and a higher drug penetration; on the contrary, nanoparticles containing low polymer concentration (1:7.5) were able to give a more sustained release of the drug and thus a slower KF permeation through the cornea. Conclusion: The study revealed that KF NPs were capable of releasing the drug for a prolonged period of time and increasing the ocular bioavailability.
Mark B. Abelson - One of the best experts on this subject based on the ideXlab platform.
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bioequivalence of two formulations of Ketotifen Fumarate ophthalmic solution a single center randomized double masked conjunctival allergen challenge investigation in allergic conjunctivitis
Clinical Therapeutics, 2008Co-Authors: Gail Torkildsen, Mark B. Abelson, Paul J GomesAbstract:Abstract Background: Ketotifen Fumarate ophthalmic solution 0.025% (reference formulation), a topical mast cell stabilizer/antihistamine combination, has been found to be effective and well tolerated in the prevention of ocular itching associated with allergic conjunctivitis (AC). A recently developed formulation of Ketotifen Fumarate ophthalmic solution 0.025% (test formulation) contains the same active ingredient in the same concentration as the reference formulation, is intended for twice-daily dosing, and may provide a treatment option in patients with AC. Objective: The aim of this study was to determine the clinical bioequivalence of the test and reference formulations using a conjunctival allergen challenge (CAC) model. Methods: This prospective, randomized, double-masked, active- and placebo-controlled CAC study was conducted in a clinical setting (ORA Clinical Research and Development, North Andover, Massachusetts). Patients aged Results: There were 108 patients enrolled (61 men, 47 women; mean age, 42 years; 91.7% white). The test and reference formulations both yielded clinically significant results compared with placebo in the prevention of ocular itching at CACs performed 8 hours and 15 minutes after instillation. At the 8-hour posttreatment CAC, the mean ocular itching scores for test formulation-treated eyes were 1.158, 1.265, and 1.305 units lower, respectively, than for eyes at 3, 5, and 7 minutes that were administered placebo. At 15-minute posttreatment CAC, the mean ocular itching scores for reference formulation-treated eyes at 3, 5, and 7 minutes were 1.481, 1.622, and 1.565 units lower, respectively, than for eyes that were administered placebo. With regard to the primary and secondary efficacy variables, no statistically significant differences were observed between test and reference formulations at any post-CAC time point. Conclusions: In this population of patients with AC, the test formulation of Ketotifen Fumarate ophthalmic solution 0.025% met criteria for bioequivalence to the reference formulation, as established by the protocol. The test and reference formulations were well tolerated in the population studied.
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efficacy and safety of single and multiple dose Ketotifen Fumarate 0 025 ophthalmic solution in a pediatric population
Pediatric Allergy and Immunology, 2004Co-Authors: Mark B. Abelson, Nancy J Ferzola, Cecilia L Mcwhirter, Henry J CramptonAbstract:Allergic conjunctivitis can seriously disrupt children's daily activities. This study assessed the efficacy (onset and duration of action) and safety of Ketotifen Fumarate 0.025% ophthalmic solution compared with vehicle placebo in pediatric subjects after single and multiple dosing. This was a double-masked, multicenter, fellow-eye, placebo-controlled, conjunctival allergen challenge trial. Eligible subjects (8-16-yr-olds) who produced a qualifying reaction to allergen were randomized to a single dose (one drop) of Ketotifen Fumarate in one eye and vehicle placebo in the fellow eye, followed by an allergen challenge at 15 min and 8 h post-dose. Subjects who had a qualifying reaction to allergen in the placebo-treated eye and a qualifying response to Ketotifen in the active-treated eye following the single dose were re-randomized to a multiple-dose treatment period. They were instructed to instill one drop of Ketotifen Fumarate in one eye and placebo in the other eye twice daily for 4 wk. An allergen challenge was conducted 8 h after the last dose. The primary efficacy assessment was ocular itching, judged by the subject at 3, 7, and 10 min post-allergen challenge after single- and multiple-dose treatments. Other ocular signs and symptoms were assessed at 7, 10, and 15 min post-dose. A total of 133 subjects were randomized to single-dose treatment; 105 were evaluable for efficacy. Of these, 60 were re-randomized to multiple-dose treatment, and 55 were evaluable for efficacy. After single and multiple doses, Ketotifen Fumarate significantly inhibited ocular itching compared with placebo at all post-challenge timepoints (p < 0.001) and also significantly reduced hyperemia, chemosis, and lid swelling (p = 0.031). No drug-related systemic adverse events were reported, and ocular adverse events were comparable to placebo. No subject discontinued prematurely due to an adverse event. These results indicate that Ketotifen Fumarate 0.025% ophthalmic solution is an effective and safe treatment option for children with allergic conjunctivitis.
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efficacy and safety of Ketotifen Fumarate 0 025 in the conjunctival antigen challenge model of ocular allergic conjunctivitis
American Journal of Ophthalmology, 2003Co-Authors: Jack V Greiner, Barry M. Kapik, Naveed B. K. Shams, Thomas K Mundorf, Harvey Dubiner, John Lonsdale, Richard Casey, Leonard M Parver, Mark B. AbelsonAbstract:Abstract Purpose To determine the duration of action of Ketotifen 0.025% eye drops vs placebo taken as single or multiple doses in an allergen challenge model. Design Two randomized, multicenter, double-masked, contralateral placebo-controlled studies, one a single-dose and one a multiple-dose study. Methods Two conjunctival provocation tests (CPTs) were initially conducted to confirm reproducibility of subject responses in both studies. Subjects in study 1 (n = 87) received single doses of Ketotifen in one eye and placebo in the other 15 minutes, 6 hours, and 8 hours before CPT. Subjects in study 2 (n = 85) received Ketotifen or placebo once 8 hours before CPT. Single-dose efficacy results were used to further qualify a subject as a responder. Responders were re-randomized to a 4-week twice daily dosing regimen with a CPT 8 hours after the final dose. In both studies, ocular symptoms were assessed at three time points 3 to 15 minutes after challenge. There were no significant differences in adverse events between groups. Results For both studies, ocular itching and vascular injection were significantly reduced ( P P Conclusions Ketotifen 0.025% eye drops were safe and statistically effective in preventing ocular itching, injection, and other signs and symptoms of allergic conjunctivitis at 15 minutes, 6 hours, and 8 hours after a single dose and at 8 hours after the final dose of a 4-week twice daily regimen.
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efficacy of Ketotifen Fumarate 0 025 ophthalmic solution compared with placebo in the conjunctival allergen challenge model
Archives of Ophthalmology, 2003Co-Authors: Mark B. Abelson, Barry M. Kapik, Matthew Jonathan Chapin, Naveed ShamsAbstract:Background Ketotifen Fumarate blocks histamine 1 (H 1 ) receptors, stabilizes mast cells, and acts as an eosinophil inhibitor (decreases chemotaxis and activation of eosinophils). Objective To assess the efficacy of Ketotifen 0.025% ophthalmic solution in the prevention of symptoms of allergic conjunctivitis, using the conjunctival allergen challenge model. Methods This was a single-center, double-masked, randomized, placebo-controlled, contralateral-eye comparison, allergen challenge trial conducted in the United States. Subjects were randomized to receive Ketotifen 0.025% in one eye and placebo in the other. At visits 1 and 2, allergen challenges were performed to determine the allergen concentration eliciting a qualifying reaction for each subject. At the 3 subsequent visits, subjects received 1 drop of Ketotifen 0.025% ophthalmic solution in one eye and vehicle solution as placebo in the other eye 15 minutes (visit 3), 6 hours (visit 4), and 8 hours (visit 5) before allergen challenge. The primary efficacy measure was the subject's rating of itching at 3, 7, and 10 minutes after challenge. Results Of the 89 subjects randomly assigned to masked trial medication at visit 3, 72 completed the study. At visits 3, 4, and 5, mean itching scores were significantly better for Ketotifen-treated eyes at all postchallenge time points, compared with placebo ( P P Conclusions Ketotifen was safe and statistically effective in reducing ocular itching and hyperemia associated with allergic conjunctivitis. Ketotifen's rapid onset of action (within 15 minutes) and extended duration of action (at least 8 hours) make it a valuable treatment for allergic conjunctivitis.
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Ocular tolerability and safety of Ketotifen Fumarate ophthalmic solution
Advances in Therapy, 2002Co-Authors: Mark B. Abelson, Matthew J. Chapin, Barry M. Kapik, Naveed B. K. ShamsAbstract:Ketotifen Fumarate, formulated for the treatment of allergic conjunctivitis, is a histamine H_1-receptor antagonist, mast cell stabilizer, and eosinophil inhibitor (decreases chemotaxis and activation of eosinophils). In this study, healthy volunteers 3 years of age or older received Ketotifen Fumarate .025% ophthalmic solution (n = 330) or placebo (n = 165) four times daily for 6 weeks. Ketotifen was safe and well tolerated in the adult and pediatric populations, with an incidence of ocular adverse events of 18.2%, compared with 15.2% with placebo. No ocular rebound vasodilation or itching was observed within 48 hours after treatment. Ketotifen has a favorable safety and tolerability profile, which may have a positive impact on compliance, an important aspect of effective symptomatic control of allergic conjunctivitis.
