Olopatadine Research Articles

Efficacy and safety of olopatadine-mometasone combination nasal spray for the treatment of seasonal allergic rhinitis

BackgroundGSP301 nasal spray is a fixed-dose combination of olopatadine hydrochloride (antihistamine) and mometasone furoate (corticosteroid). ObjectiveTo evaluate the efficacy and safety of GSP301 in patients with seasonal allergic rhinitis (SAR). MethodsIn this double-blind study, eligible patients (≥12 years of age) with SAR were randomized 1:1:1:1 to twice-daily GSP301 (665 μg of olopatadine and 25 μg of mometasone), olopatadine (665 μg), mometasone (25 μg), or placebo for 14 days. The primary end point—mean change from baseline in average morning and evening 12-hour reflective Total Nasal Symptom Score (rTNSS)—was analyzed via a mixed-effect model repeated measures (P < .05 was considered to be statistically significant). Additional assessments included average morning and evening 12-hour instantaneous TNSS (iTNSS), ocular symptoms, individual symptoms, onset of action, quality of life, and adverse events (AEs). ResultsA total of 1176 patients were randomized. GSP301 provided statistically significant and clinically meaningful rTNSS improvements vs placebo (least squares mean difference, -1.09; 95% CI, -1.49 to -0.69; P < .001) and vs olopatadine (P = .03) and mometasone (P = .02). Similar significant improvements in iTNSS were also observed with GSP301 (P < .05 for all). Furthermore, GSP301 significantly improved overall ocular symptoms, individual nasal and ocular symptoms, and quality of life vs placebo (P ≤ .001 for all). Onset of action for GSP301 was observed within 15 minutes and was maintained at all subsequent timepoints. Treatment-emergent AEs occurred in 15.6%, 12.6%, 9.6%, and 9.5% of patients in the GSP301, olopatadine, mometasone, and placebo groups, respectively. ConclusionGSP301 is efficacious and well tolerated vs placebo for treating SAR-associated nasal and ocular symptoms, with a rapid onset of action of 15 minutes in adult and adolescent patients 12 years and older. Clinical Trial RegistrationClinicalTrials.gov: NCT02870205.

Olopatadine hydrochloride loaded Kollidon® SR nanoparticles for ocular delivery: Nanosuspension formulation and in vitro–in vivo evaluation

IntroductionAllergic eye diseases includes a spectrum of diseases, with each state being characterized by a complicated immunopathology. In the present study, polymeric Kollidon® SR nanoparticles loaded with olopatadine hydrochloride (OLO) were formulated as a suspension for ocular drug delivery. The formulations were developed to treat ocular allergic disease and characterized by their improved duration of corneal retention. MethodsOLO-loaded Kollidon® SR nanoparticles were prepared using the spray-drying method. The active agent was quantified using ultra-high performance liquid chromatography (U-HPLC). The nanoparticles were characterized according to entrapment efficiency, particle size, zeta potential, morphology, solid-state characterizations, and drug release. The in vitro release studies on OLO-loaded nanoparticles were examined in simulated tear fluid (pH 7.4). In vivo studies were conducted on healthy female/male Anatolian Merino sheep to investigate the retention time of the active agent. Results and DiscussionCharacterization studies showed that OLO was successfully loaded into the nanoparticle system and that the suspension formulation is suitable for ocular administration. Using DDSolver, the in vitro release of the OLO from nanoparticle formulations followed the Korsmeyer-Peppas model. ConclusionsThe proposed spray-drying method can be successfully applied for preparing OLO-loaded nanoparticles without adding crosslinkers. OLO-loaded nanoparticles appear to be a promising extended-release drug delivery system that can be used to treat ocular diseases with a more prolonged drug-residence time on the ocular surface.

Poly (vinyl chloride) matrix membrane sensors for the quantification of olopatadine and oxeladine in pharmaceutical preparations and human plasma

Two novel potentiometric sensors were developed for the quantification of olopatadine hydrochloride and oxeladine citrate in pure forms, pharmaceutical preparations and human plasma. The both sensors were fabricated on incorporating the olopatadine and oxeladine tetraphenylborate ion-pairs as electroactive materials in plasticized poly (vinyl chloride) matrix membranes with o-nitrophenyl octyl ether. They displayed Nernstian and near Nernstian responses over the concentration ranges of 1.0 × 10−5–1.0 × 10−2 mol L−1 oxeladine and olopatadine with cationic slopes of 60 and 50 mV decade−1, respectively. Detection limits were reported to be 4.4 × 10−6 and 5.0 × 10−6 mol L−1 while the response times were 3.0 and 18 s for oxeladine and olopatadine, respectively. The useful ranges of pH were 2.5–8.5 and 3.0–4.5 for oxeladine and olopatadine, respectively. The life extents were long (3 months) for both sensors. The sensors were successfully used for the assay of oxeladine and olopatadine in pharmaceutical dosage forms with a recovery of 100.0% for both drugs. Also the oxeladine sensor was used for the estimation of the drug in human plasma with an average recovery of 99.49%.

Isolation and Characterization Photo Degradation Impurities of Drug Product Olopatadine Hydrochloride by Spectral Techniques

Unknown impurities were detected during Photo degradation of Olopatadine Hydrochloride ophthalmic solution 0.5% (w/v) when analyzed using the High performance liquid chromatographic technique with Photo Diode Array Detection. For further investigation was carried out by isolating these impurities from impurity rich sample of Olopatadine Hydrochloride ophthalmic solution 0.5% (w/v) using preparative isolation technique. The Olopatadine Hydrochloride ophthalmic solution 0.5% (w/v) was subjected to photolytic forced degradation in the presence of Benzalkonium chloride and other excipients like Hypromellose, Mannitol, Hydroxypropyl, Boric acid, Kollidon 30 LP and mixture of solvents (Acetonitrile: Methanol; 1: 1 (v/v) under Ultra violet visible light. This led to the formation of the said impurities in higher concentration. This sample was then subjected to preparative HPLC for isolation of these unknown impurities. The structure of these unknown impurities was further elucidated using a different technique like Infra Ray Spectroscopy, Direct infusion (DI) Mass Spectroscopy, Ultra violet-Visible Spectroscopy, Proton Nuclear Magnetic Resonance Spectroscopy, carbon Nuclear Magnetic Resonance and Distortionless Enhancement by Polarization Transfer (DEPT) Spectroscopy which helped to confirm the structure of the impurities. Structure elucidation of the two impurities revealed that these are E and Z isomers of the Olopatadine hydrochloride Carbaldehyde. Olopatadine Z- isomer is used in the formulation of the Olopatadine Hydrochloride Ophthalmic Solution 0.5% (w/v). The minor amount of E- isomer also remains present in this solution as a potential impurity. However, the amount of E-isomer may increase in the solution form due to racemization. Hence, the respective Carbaldehyde impurities (both E and Z isomers) are forming during Photolytic degradation. This formation is happening through photolytic Norrish type-1 reaction which is elaborated in the paper.

The in-use stability study of multi-use ophthalmic solutions -Focused on Olopatadine, Fluorometholone, Dorzolamide, Timolol-

The in-use stability study of multi-use ophthalmic solutions -Focused on Olopatadine, Fluorometholone, Dorzolamide, Timolol-

Development and in vitro/in vivo evaluation of thermo-sensitive in situ gelling systems for ocular allergy

Ocular allergy is one of the most common disorders of the eye surface. Following diagnosis this condition is typically treated with preparations containing antihistamines. However, anatomy of the eye and its natural protective mechanisms create challenges for ocular drug delivery. Rapid elimination of antihistamine substances due to short residency times following application can lead to insufficient treatment of ocular allergies. With this in mind, the aim of this study was to prepare a controlled ocular delivery system to extend the retention time of olopatadine hydrochloride (OLO) and in doing so to reduce the need for frequent application. We developed extended-release ocular in situ gelling systems for which in vivo retention times were determined in sheep following in vitro characterization and cytotoxicity studies. In vivo results were then compared to commercially available Patanol eye drops. the transparent gels formulated using appropriate amounts of polymers and having longer ocular retention times appear to be a viable alternative to commercially available eye drops.

Development and validation of uplc method for the determination of olopatadine hydrochloride in polymeric nanoparticles

Development and validation of uplc method for the determination of olopatadine hydrochloride in polymeric nanoparticles

Intrinsic Stability Study and Forced Degradation Profiling of Olopatadine hydrochloride by RP-HPLC-DAD-HRMS Method

Intrinsic Stability Study and Forced Degradation Profiling of Olopatadine hydrochloride by RP-HPLC-DAD-HRMS Method

Therapeutic effects of Houttuynia eye drops combined with olopatadine hydrochloride eye drops on vernal keratoconjunctivitis.

Therapeutic effects and safety of houttuynia eye drops combined with olopatadine hydrochloride eye drops on vernal keratoconjunctivitis (VK) were evaluated. A total of 926 patients with VK were collected in the Eye Hospital of Wenzhou Medical University from July 2011 to January 2017. Patients were divided into group A, B and C according to the use of different eye drops. Group A included 276 patients who were treated with houttuynia eye drops; group B included 305 patients who were treated with olopatadine hydrochloride eye drops; group C included 345 patients who were treated with houttuynia eye drops and olopatadine hydrochloride eye drops. Treatment was performed for 14 days. Eye symptoms before and after treatment, and at 1 h, 7 days and 14 days after drug administration were compared among groups to evaluate the therapeutic effect. At 1 h after drug administration, highest excellent rate was observed in group C, followed by group A, and good outcome rate was significantly higher in group C than in the other two groups (P<0.05), and effective rate was also significantly higher in group C than in the other two groups (P<0.05). At 7 days after treatment, excellent rate was significantly higher in group C than in the other two groups (P<0.05), and effective rate was higher in group C than in group B (P<0.05). At 14 days after treatment, excellent rate was significantly higher in group C than in the other two groups (P<0.05), while lowest good outcome rate and ineffective rate were found in group C, and no significant differences were found between group A and B (P>0.05). Houttuynia ophthalmic solution and olopatadine hydrochloride eye drops can both achieve good effect in the treatment of VK, and combined use of them can increase the efficacy and shorten treatment period. So, the combined treatment should be popularized.

Effect of olopatadine-mometasone combination nasal spray on seasonal allergic rhinitis symptoms in an environmental exposure chamber study

BackgroundGSP301 nasal spray is a fixed-dose combination of the antihistamine olopatadine hydrochloride and the corticosteroid mometasone furoate intended for seasonal allergic rhinitis (SAR) treatment. ObjectiveTo evaluate the efficacy and safety of once-daily or twice-daily GSP301 in a ragweed pollen environmental exposure chamber. MethodsIn this randomized, double-blind, double-dummy study, adults (18-65 years old) with SAR were equally randomized to 665 μg of olopatadine and 25 μg of mometasone (twice-daily GSP301), 665 μg of olopatadine and 50 μg of mometasone (once-daily GSP301), a US Food and Drug Administration–approved formulation of 137 μg of azelastine and 50 μg of fluticasone twice-daily (AzeFlu), a US Food and Drug Administration–approved formulation of 665 μg of olopatadine twice-daily, or placebo (twice-daily). During 2 visits (baseline and end of 14-day treatment), participants assessed SAR symptoms at specified time points. The primary end point—mean change from baseline in instantaneous total nasal symptom score (iTNSS) for twice-daily or once-daily GSP301 vs placebo—was analyzed by analysis of covariance. Onset of action, ocular symptoms, and adverse events were assessed. ResultsA total of 180 participants were randomized. Treatment with twice-daily or once-daily GSP301 provided statistically significant improvements in iTNSS vs placebo (twice-daily GSP301: least squares mean difference, −3.60; 95% confidence interval [CI], −4.89 to −2.30; once-daily GSP301: least squares mean difference, −3.05; 95% CI, −4.35 to −1.76; P < .0001 for both). Significant improvements in iTNSS with twice-daily GSP301 occurred by 10 minutes after dosing (−1.26; 95% CI, −2.30 to −0.21; P = .02) and were maintained at all later time points except one (2.5 hours). Treatment-emergent adverse events occurred in 22.2%, 30.6%, 25.0%, 22.2%, and 16.7% of participants in the twice-daily GSP301, once-daily GSP301, AzeFlu, olopatadine, and placebo groups, respectively. ConclusionIn an environmental exposure chamber model, twice-daily and once-daily GSP301 treatments were well tolerated and provided statistically significant and clinically meaningful SAR symptom improvement vs placebo. Trial RegistrationClinicalTrials.gov Identifier: NCT03444506

Pharmacokinetics of intranasal olopatadine in the fixed-dose combination GSP301 versus two monotherapy intranasal olopatadine formulations

GSP301 is a fixed-dose combination of the antihistamine olopatadine hydrochloride and the corticosteroid mometasone furoate developed as a single nasal spray. To assess the relative bioavailability of olopatadine administered as GSP301 versus two olopatadine monotherapy nasal spray formulations. In this single-dose, open-label, crossover study, healthy adults (18-65 years old) were equally randomized to one of six treatment sequences for three 48-hour treatment periods with GSP301 (olopatadine 665 μg-mometasone 50 μg), the olopatadine monotherapy component of GSP301 (OLO-sponsor; 665 μg) and U.S. Food and Drug Administration approved olopatadine (OLO; 665 μg); each treatment was administered as a single dose (two sprays in each nostril). To assess the relative bioavailability of olopatadine in the fixed-dose nasal spray versus two monotherapies, pharmacokinetic (PK) estimates, maximum plasma concentration (Cmax), area under the plasma concentration time curve (AUC) from time 0 to the last time point with measurable concentration (AUC0-t), and AUC from time 0 to time infinity (AUC0-∞) were compared by analysis of variance. Safety and tolerability were also evaluated. A total of 30 healthy adults (mean age, 43.1 years) were randomized. The majority of the subjects were white men. The geometric mean ratios for natural log transformed Cmax, AUC0-t, and AUC0-∞ of olopatadine in GSP301 and OLO-sponsor were 86.63, 86.92, and 92.83, respectively. For GSP301 and OLO, geometric mean ratios for Cmax, AUC0-t, and AUC0-∞ were 84.68, 87.87, and 93.80, respectively. The percentage of subjects who reported treatment-emergent adverse events (AE) for GSP301, OLO-sponsor, and OLO were 13.8, 10.3, and 10.0%, respectively, with mild AEs reported. One subject withdrew from the study due to an AE (minor oropharyngeal pain) during OLO treatment, before receiving GSP301. Olopatadine bioavailability with GSP301 was comparable with OLO-sponsor and OLO. The presence of mometasone in GSP301 did not considerably affect the PK of olopatadine. GSP301 was well tolerated, with only mild AEs reported.

Pharmacokinetics of intranasal mometasone in the fixed-dose combination GSP301 versus two monotherapy intranasal mometasone formulations.

GSP301 is a fixed-dose combination (FDC) of the antihistamine olopatadine hydrochloride and the corticosteroid mometasone furoate developed as a single nasal spray (NS). To assess the relative bioavailability of mometasone administered as GSP301 FDC versus two mometasone monotherapy NS formulations. In this single-dose, open-label, crossover study, healthy adults (age range, 18-65 years) were randomized equally to one of six treatment sequences for three 72-hour treatment periods with GSP301 (olopatadine 665 μg-mometasone 50 μg), the mometasone furoate monotherapy component of GSP301 (MF-sponsor, 50 μg), and U.S. Food and Drug Administration-approved mometasone (MF, 50 μg); all the treatments were administered as two sprays per nostril. To evaluate the relative bioavailability of mometasone, pharmacokinetic (PK) estimates, the maximum plasma concentration (Cmax), the area under the plasma concentration time curve (AUC) from time 0 to the last time point with measurable concentration (AUC0-t), and AUC from time 0 to time infinity (AUC0-∞) were compared by analysis of variance. Safety and tolerability were also assessed. A total of 30 healthy subjects were randomized. Most subjects were white men who were not obese, mean age of ∼43 years. The geometric mean ratios for natural log transformed Cmax, AUC0-t, and AUC0-∞ of mometasone in GSP301 to MF-sponsor were 113.83, 118.36, and 118.50, respectively. For GSP301 and MF, geometric mean ratios for Cmax, AUC0-t, and AUC0-∞ were 141.84, 109.92, and 115.14, respectively. The percentages of subjects who reported treatment-emergent adverse events (TEAE) were 10.0%, 13.3%, and 10.3% for GSP301, MF-sponsor, and MF treatments, respectively. All TEAEs were mild, and none resulted in discontinuation. Mometasone bioavailability with GSP301 was comparable with MF-sponsor and MF monotherapies. A slightly higher Cmax was observed with GSP301 than with MF, but AUC was comparable. The addition of olopatadine to mometasone in GSP301 did not considerably affect the PK of mometasone. GSP301 was well tolerated, with only mild adverse events reported.

A prospective study of efficacy and safety of olopatadine versus azelastine in allergic conjunctivitis at a tertiary care hospital

Background: Allergic conjunctivitis, an ocular surface inflammatory disease with significant social and economic impact affects approximately 25% of the general population. H1 receptor blockers, mast cell stabilizers and drugs that block cytokine and prostaglandin formation form the treatment armamentarium. Olopatadine hydrochloride and Azelastine hydrochloride are dual-acting selective H1 receptor antagonist with mast-cell stabilizing property. This study was undertaken to assess the efficacy and safety of olopatadine hydrochloride 0.1% and Azelastine hydrochloride 0.05% in allergic conjunctivitis amongst Indians.Methods: After obtaining Institutional Ethics Committee approval and written informed consent, 120 patients diagnosed with allergic conjunctivitis fulfilling the inclusion/exclusion criteria were enrolled in the study. Study was done from April 2014 to June 2015 at Minto eye hospital. Study subjects were treated with olopatadine hydrochloride 0.1% and Azelastine hydrochloride 0.05% eye drops BD for 15 days. Ocular symptoms, instead of and signs and adverse events, if any were recorded on the day 8 and day 15 follow up visits.Results: At the end of the study period, the reduction in the ocular itching score from baseline was higher in the olopatadine group compared to the azelastine group (p&lt;0.002). Similarly, the scores of ocular congestion (p&lt;0.008), foreign body sensation (p&lt;0.009), tearing (p&lt;0.001), erythema (p&lt;0.002) and chemosis (p&lt;0.015) also showed larger reduction in the olopatadine treated patients. The common adverse events encountered in both the groups were stinging after instillation, burning, bitter taste and headache.Conclusions: In allergic conjunctivitis, both olopatadine and azelastine were found to be effective in relieving ocular signs and symptoms, but olopatadine was found to be superior in terms of efficacy, safety and tolerability with minimal side effects.

Olopatadine hydrochloride ophthalmic solution for the treatment of allergic conjunctivitis

ABSTRACTIntroduction: Olopatadine hydrochloride is an antihistamine and mast cell stabilizer available as oral, intranasal and ocular preparations. Most of the practical applications of olopatadine therapy focus on the treatment of allergic rhinoconjunctivitis via intranasal and ocular routes.Areas covered: This article was created from a comprehensive literature search with information taken from meta-analyses, systematic reviews, and clinical trials of children and adults. The articles that have been selected, evaluate the use of intranasal and ocular antihistamines and their role in allergic rhinoconjunctivitis.Expert opinion: Olopatadine is significantly more effective than placebos in relieving the symptoms of allergic rhinoconjunctivitis. It can function both as a viable alternative or addition to first line therapies such as intranasal steroids and oral antihistamines.

Pooled analysis of two studies evaluating efficacy and safety of olopatadine hydrochloride 0.77% in patients with allergic conjunctivitis

PurposeTwo individual phase 3 conjunctival allergen challenge (CAC) studies of similar design have assessed the efficacy and safety of olopatadine hydrochloride (HCl) 0.77% for the treatment of allergic conjunctivitis. The purpose of this study is to evaluate the integrated efficacy and safety of olopatadine HCl 0.77% from a larger dataset by pooling data from the two individual CAC studies.MethodsData were pooled from two phase 3, randomized, multicenter, double-masked, active- and vehicle-controlled CAC studies. The primary comparison was on ocular itching scores between olopatadine HCl 0.77% versus vehicle (at onset and 24 hours) and olopatadine HCl 0.77% versus olopatadine 0.2% (at 24 hours). Additional end points included conjunctival redness, total redness, and proportion of itching responders at onset and 24-hour duration of CAC. For both primary and secondary analysis, mixed model repeated measures analysis was used, except for proportion of ocular itching responders. Sensitivity analyses were carried out using a two-sample t-test.ResultsThis analysis included 448 patients. Olopatadine HCl 0.77% was superior to vehicle (P<0.0001) at onset and 24-hour duration of action (difference in means: −1.14 to −1.52) and to olopatadine 0.2% (P=0.0009) at 24-hour duration of action in relieving ocular itch. Additionally, olopatadine HCl 0.77% substantially reduced conjunctival redness and total redness over vehicle and olopatadine 0.2% at onset and 24-hour duration of action. At 24 hours CAC, there were a higher proportion of itching responders with olopatadine HCl 0.77% compared to vehicle or olopatadine 0.2% (difference in proportion of responders: 43.17%, P<0.0001, and 17.25%, P=0.0012, respectively). No safety concerns were identified.ConclusionThis analysis confirms the findings from the individual studies. The rapid onset and prolonged duration of action (for 24 hours) of olopatadine HCl 0.77% supports once-daily dosing in the treatment of allergic conjunctivitis.

Pharmacokinetics and safety of olopatadine hydrochloride 0.77% in healthy subjects with asymptomatic eyes: data from 2 independent clinical studies.

PurposeTo assess the pharmacokinetics and safety of hydrochloride ophthalmic solution 0.77% olopatadine from 2 independent (Phase I and Phase III, respectively) clinical studies in healthy subjects.Materials and methodsThe Phase I, multicenter, randomized (2:1), vehicle-controlled study was conducted in subjects ≥18 years old (N=36) to assess the systemic pharmacokinetics of olopatadine 0.77% following single- and multiple-dose exposures. The Phase III, multicenter, randomized (2:1), vehicle-controlled study was conducted in subjects ≥2 years old (N=499) to evaluate long-term ocular safety of olopatadine 0.77%. Subjects received olopatadine 0.77% or vehicle once daily bilaterally for 7 days in the pharmacokinetic study and 6 weeks in the safety study.ResultsIn the pharmacokinetic study, olopatadine 0.77% was absorbed slowly and reached a peak plasma concentration (Cmax) of 1.65 ng/mL following single-dose and 1.45 ng/mL following multiple-dose exposures in 2 hours (time to reach maximum plasma concentration [Tmax]). After reaching peak concentrations, olopatadine showed a similar mono-exponential decay following single and multiple doses with mean elimination half-life ranging from 2.90 to 3.40 hours. No accumulation in olopatadine exposure (Cmax and area under the plasma concentration–time curve from 0 to 12 hours) was evident after multiple doses when compared to single dose. In the safety study, treatment-emergent adverse events were reported in 26.7% and 31.4% of subjects with olopatadine 0.77% and vehicle, respectively. Blurred vision was the most frequent ocular treatment-emergent adverse event in both treatment groups (olopatadine 0.77% vs vehicle, 4.8% vs 4.1%). No deaths or serious adverse events were reported during the study.ConclusionOlopatadine 0.77% had minimal systemic exposure or accumulation in healthy subjects and was well tolerated in both adult and pediatric subjects.

Reverse engineering and formulation by QBD of olopatadine hydrochloride ophthalmic solution

Reverse engineering of innovator product’s formulation is a cost-effective strategy for accelerating generic product development. The total market share for olopatadine hydrochloride (OLH) ophthalmic solution used as an antihistamine in US is nearly $230 million dollars. By using ‘Differential solubility technique’ and 32 factorial designs for separation of components, nine different batches were prepared. The separated quantities of OLH and excipients i.e. benzalkonium chloride (BKC), sodium chloride (NaCl) and sodium phosphate dibasic (Na2HPO4) were 0.111, 0.01, 0.65 and 0.5 g respectively. Statistical analysis by ANOVA resulted significant model having P values <0.0001 for BKC and 0.0001 for OLH. X-ray diffraction study revealed that separated OLH was found to be polymorphic form A with characteristic 2θ values of 15.44°, 17.55°, 18.20°, 18.971°, 20.58°, 20.68°, 23.89°, 25.30°, 28.25°. The differential scanning calorimetry of OLH gave an endothermic peak at approximately 255 °C. The refractive index of separated BKC was 1.4. Based upon the reverse engineering data generic form of OLH was prepared with pH of 7.1 ± 0.3; osmolarity of 302 ± 1.5 mOsmol/l, assay of 99 ± 2% and viscosity of 0.9715 ± 0.12 pas. The prepared generic formulation of OLH is equivalent and stable with marketed formulation of OLH.

ALLERGIC EYE DISEASES IN CHILDREN. MODERN VIEW ON PATHOGENESIS AND TREATMENT

The prevalence off allergic diseases has been significantly increased among adults and children during last 30-40 years. International study has shown that the frequency of atopy in developed countries, including Russia, is higher than in developing. Often atopic dermatitis, started in infancy, can develop into an “allergic march” — food allergy, followed by the formation of allergic rhinitis, allergic conjunctivitis and other allergic diseases. The problem of prophylaxis and treatment of allergic pathology becomes actual for these reasons. An opinion according some preventive measures has changed in recent. It was noted that in families with many children, where children were often sick with respiratory infections, the incidence of allergic diseases was lower than among rarely sick children. It is explained by the “hygienic theory” — insufficient “training” of the Th1 response in rarely sick children. Allergic diseases, which are based on IgE-mediated inflammation, have a common pathogenetic nature and, consequently, general principles of therapy, in which, as is well known, antihistamines take a significant place. This is cased by the mandatory involvement of histamine in the mechanism of development of the main symptoms of allergic diseases. Current capabilities of local ophthalmologic antiallergic therapy includes medicines with multiple action mechanisms, such as mast cell stabilizers, antihistamines, combined agents, steroids and nonsteroidal anti-inflammatory effects. The latest generation antihistamine drug — olopatadine hydrochloride 0.2% is a new form of the molecule of olopatadine, which is intended to increase the duration of the action. The article considers the main modern directions in prevention and treatment of allergic diseases, including allergic eye diseases, which are a manifestation of the underlying disease and have a common pathogenetic nature to all atopic diseases, based on the IgE-mediated inflammation reaction.

Clinical effectiveness of olopatadine therapy in children with allergic conjunctivitis

Background: Olopatadine hydrochloride is one of the most promising agents with a broad range of pharmacological effects. It has both antihistaminic and mast cell stabilizing properties. It is used in various allergic diseases, and its ophthalmic solution is used in allergic conjunctivitis. Aims and Objectives: To assess the clinical effectiveness of olopatadine therapy in children with allergic conjunctivitis. Materials and Methods: This was a prospective interventional study conducted to assess the clinical efficacy and safety of 0.2% olopatadine hydrochloride ophthalmic solution on 49 pediatric allergic conjunctivitis patients. 1-2 drops of the ophthalmic solution were administered once daily in each eye for 6 weeks. Scoring of redness, itching, watering, and photophobia was estimated at baseline, 2 week and 6 weeks. Adverse effects were noted at each visit if any. Results: The mean scores of redness, itching, watering, and photophobia were reduced after 2 weeks of treatment which was statistically significant (P < 0.001). Conclusion: Olopatadine hydrochloride 0.2% once daily administration was effective in reducing ocular signs and symptoms in allergic conjunctivitis in the pediatric population.

Citric Acid Suppresses the Bitter Taste of Olopatadine Hydrochloride Orally Disintegrating Tablets.

Orally disintegrating tablets (ODTs) are formulated to disintegrate upon contact with saliva, allowing administration without water. Olopatadine hydrochloride, a second-generation antihistamine, is widely used for treating allergic rhinitis. However, it has a bitter taste; therefore, the development of taste-masked olopatadine ODTs is essential. Some studies have suggested that citric acid could suppress the bitterness of drugs. However, these experiments were performed using solutions, and the taste-masking effect of citric acid on ODTs has not been evaluated using human gustatory sensation tests. Thus, this study evaluated citric acid's taste-masking effect on olopatadine ODTs. Six types of olopatadine ODTs containing 0-10% citric acid were prepared and subjected to gustatory sensation tests that were scored using the visual analog scale. The bitterness and overall palatability of olopatadine ODTs during disintegration in the mouth and after spitting out were evaluated in 11 healthy volunteers (age: 22.8±2.2 years). The hardness of the ODTs was >50 N. Disintegration time and dissolution did not differ among the different ODTs. The results of the gustatory sensation tests suggest that citric acid could suppress the bitterness of olopatadine ODTs in a dose-dependent manner. Olopatadine ODTs with a high content of citric acid (5-10%) showed poorer overall palatability than that of those without citric acid despite the bitterness suppression. ODTs containing 2.5% citric acid, yogurt flavoring, and aspartame were the most suitable formulations since they showed low bitterness and good overall palatability. Thus, citric acid is an effective bitterness-masking option for ODTs.