ABSTRACT
Comparative evaluation of bepotastine besilate versus olopatadine and ketorolac combination onupper tarsal conjunctival brush cytology in patients of vernal keratoconjunctivitis. This studywas a prospective, open label, randomized, comparative clinical study. 100 patients of vernalkeratoconjunctivitis between 6 to 20 years of age of either sex willing to give informed consentwere enrolled in the study. In Group 1, 50 patients received Bepotastine besilate (0.15%) eyedrops twice daily for 8 weeks whereas in Group 2, 50 patients received Olopatadine (0.2%) andKetorolac (0.4%) combination eye drops twice daily for 8 weeks. Upper tarsal conjunctival brushcytology for eosinophil count was done in both the drug groups during the baseline and at 8th weekduring the treatment. It was found that after the 2 months of drug therapy, patients in both thegroups showed reduction in the eosinophil count. However, there was no statistically significantdifference between the two treatment groups at the baseline and at 8th week. There was 32%reduction in group A versus 28% reduction in group B in eosinophil count at the end of 8th weekcompared to baseline. Both bepotastine besilate versus olopatadine and Ketorolac combinationwere found to be effective in reducing the eosinophil count in patients of VKC.
ABSTRACT
Objective: To prepare bepotastine besilate film-coated tablets, determine the dissolution rate by HPLC, and evaluate the similarity of dissolution curves for self-made tablets and the original tablets. Methods: Bepotastine besilate tablets were prepared by using microcrystalline cellulose, hydroxypropyl cellulose, mannitol, aspartame and magnesium stearate as the accessories. Bepotas-tine besilate film-coated tablets were prepared by using OpadryⅡpremixed spray-coating liquid. The formulation was screened with the angle of repose, disintegration time, content uniformity and dissolution rate as the indices. The coating material amount was screened with the dissolution rate as the index. Results: The optimal formulation of bepotastine besilate film-coated tablet contained bepotastine besilate 5 mg,mannitol 43 mg,microcrystalline cellulose 21. 5mg,aspartame 0. 5 mg,magnesium stearate 0. 5 mg and hydroxypropyl cellulose 15 mg. The optimal weight of coating material was 5% . The self-made tablets and the original tablets had similar dissolution behavior in 4 media including water, hydrochloric acid(pH 1. 2), acetate buffer solution(pH 4. 5) and phosphate buffer solution(pH 6. 8). Conclusion:The self-made tablets have similar dissolution behavior in vitro with the original tablets, and their quality is similar.
ABSTRACT
OBJECTIVE: To establish a method for isomer analysis of bepotastine besilate eye drops and test the stability of isomer in the preparation. METHODS: The analysis was performed on an ULTRON ES-CD chiral column (6.0 mm×150 mm, 5 μm). The mobile phase was 0.02 mol·L-1 potassium phosphate monobasic-acetonitrile(75∶25) at the flow of 0.8 mL·min-1. The column temperature was maintained at 35℃ and the detection wavelength was set at 225 nm. The injection volume was 10 μL. RESULTS: The limit of detection and limit of quantification of bepotastine besilate R-isomer were 12 and 48 ng, respectively. The linear range of bepotastine besilate R-isomer was 0.01-0.1 mg·mL-1 and the repeatability was good at high, medium and low concentrations. CONCLUSION: The method is simple and accurate, which can be used for isomer separation of bepotastine besilate and testing the stability of isomer in bepotastine besilate eye drops.
ABSTRACT
ObjectiveTo evaluate the efficacy and safety of bepotastine besilate in the treatment of chronic urticaria.MethodsA randomized,double-blind,parallel-controlled clinical study was conducted in 5 centers.Patients were randomly assigned to 2 groups to be treated with bepotastine besilate 20 mg or loratadine 10 mg once a day,respectively,for 4 weeks.Visits were scheduled before and after 1,2 and 4 weeks of treatment.Itching degree,number of wheals and diameter of the largest wheal were recorded for efficacy evaluation.ResultsTotally,240 patients were enrolled and 227 patients completed the study.The response rate was 74.6％ and 77.9％ respectively in bepotastine besilate- and loratadine-treated patients,respectively(P ＞0.05).No significant difference was observed in the incidence of adverse reactions between bepotastine besilate- and loratadine-treated patients(12.8％ vs.17.9％,P ＞ 0.05).The main side effects were mild to moderate drowsiness,dry mouth,dizziness.ConclusionBepotastine besilate is effective and safe for the treatment of chronic urticaria,with an efficacy and safety profile similar to that of loratadine.