RESUMO
Background: Vernal keratoconjunctivitis (VKC) is a recurrent, bilateral, external, ocular inflammation primarily affecting young adults living in warm dry climates. The objectives of the research was to compare the two ophthalmic solutions of olopatadine hydrochloride (0.1%) and epinastine hydrochloride (0.05%) on clinical signs of vernal keratoconjuntivitis and to determine side effects of both the drugs.Methods: The study was carried out in 40 patients who attended the out-patient department (OPD) Ophthalmology, Darbhanga Medical College and Hospital, Laheriasarai from July 2007 to December 2008. Forty patients with symptoms of VKC (ocular itching, ropy discharge, papillary hypertrophy, gelatinous thickening and horner-trantas spots were selected and included in our study.Results: Mean score of palpebral hyperemia at 0, 14, 28 and 42 days in olopatadine treated eye were 2.1, 1.4, 0.8 and 0.4 respectively having p value <0.01, and <0.01 and <0.05 respectively, while mean score at same stages in placebo eye were 2.1, 2, 1.9, and 1.5 having value >0.05. Epinastine treated group mean score of palpebral hyperemia were <0.01 and <0.01 respectively in epinastine treated eye whereas in placebo treated eye, mean score were 2.1, 2.0, 1.8 and 1.6 respectively having p value >0.05 in all stages. Statistically insignificant reduction at day 14 while very significant reduction at day 28 and 42 was observed in epinastine treated eye as compared to placebo.Conclusions: The present study had shown that both olopatadine and epinastine were effective in treating clinical signs of VKC as compared to placebo.
RESUMO
Objective To evaluate the efficacy and safety of desloratadine citrate disodium versus epinastine for the treatment of chronic urticaria (CU).Methods A randomized,double-blind,double-dummy controlled clinical trial was conducted.Patients with CU were divided into test group and control group to be treated by oral desloratadine citrate disodium (8.8 mg/d) and epinastine (10 mg/d) respectively once a day for 28 days.All the patients were followed up after starting treatment.Therapeutic effect was evaluated,and adverse reactions were observed.Results One hundred and fifty-seven patients were enrolled in this study,and 142 patients were valid for evaluation of efficacy and safety at the end of study.After treatment for 28 days,there was no significant difference between the test group and control group in response rate (81.16 ％ vs.78.08 ％,P ＞ 0.05) or incidence rate of adverse reactions (13.89 ％ vs.12.16 ％,P＞ 0.05).Conclusion Desloratadine citrate disodium is effective and safe for the treatment of CU.
RESUMO
A simple, specific, accurate and stability-indicating high performance liquid chromatographic method was developed and validated for the determination of Epinastine Hydrochloride in pharmaceutical dosage form. The chromatographic conditions comprised of a reverse-phase, C18 column (150×4.6 mm), 5μm with a mobile phase consisting of a mixture of aqueous phase (3.8g of sodium pantanesulphonate monohydrate and 4.0g of potassium dihydrogen orthophosphate was dissolved in 1L of water and pH of solution was adjusted to 4.5 with o-phosphoric acid) and organic phase (acetonitrile and methanol was mixed in the ratio of 4:1 v/v) in the ratio of 60:40 v/v at a flow rate of 1.0ml/min. Detection was carried out at 220nm. The retention time of Epinastine Hydrochloride was found to be 3.5 min. The calibration curve was found linear between 2-200μg/ml. The percentage recoveries of Epinastine Hydrochloride were found to be in the range of 99.05-100.50%. The method was validated for accuracy, linearity, precision, detection limit, quantitation limit and robustness. The drug was subjected to acidic hydrolysis, basic hydrolysis, neutral hydrolysis, oxidation, photochemical and thermal degradation. All the peaks of degraded product were resolved from the active pharmaceutical ingredient with significantly different retention time. As the method could effectively separate the drug from its degradation product, it can be employed as a stability indicating one.
RESUMO
A simple, specific, accurate and stability-indicating high performance liquid chromatographic method was developed and validated for the determination of Epinastine Hydrochloride in pharmaceutical dosage form. The chromatographic conditions comprised of a reverse-phase, C18 column (150×4.6 mm), 5μm with a mobile phase consisting of a mixture of aqueous phase (3.8g of sodium pantanesulphonate monohydrate and 4.0g of potassium dihydrogen orthophosphate was dissolved in 1L of water and pH of solution was adjusted to 4.5 with o-phosphoric acid) and organic phase (acetonitrile and methanol was mixed in the ratio of 4:1 v/v) in the ratio of 60:40 v/v at a flow rate of 1.0ml/min. Detection was carried out at 220nm. The retention time of Epinastine Hydrochloride was found to be 3.5 min. The calibration curve was found linear between 2-200μg/ml. The percentage recoveries of Epinastine Hydrochloride were found to be in the range of 99.05-100.50%. The method was validated for accuracy, linearity, precision, detection limit, quantitation limit and robustness. The drug was subjected to acidic hydrolysis, basic hydrolysis, neutral hydrolysis, oxidation, photochemical and thermal degradation. All the peaks of degraded product were resolved from the active pharmaceutical ingredient with significantly different retention time. As the method could effectively separate the drug from its degradation product, it can be employed as a stability indicating one.
RESUMO
Objective To observe the effect of several antihistamines,including epinastine,on the release of leukotriene B4(LTB4),interleukin 4(IL-4)and interleukin 5(IL-5)from spleen lymphocytes of allergic mice challenged by ovalbumin(OVA).Methods OVA-sensitized BALB/c mice were used as animal model of allergy.Spleen lymphocytes isolated from these mice were treated with epinastine(0.1,1.0,10 μmol/L),ebastine(10 μmol/L),cetirizine(10 μmol/L),and dexamethasone(1.0 μmol/L),respectively,followed by incubation with OVA.Those cells without pretreatment with antihistamines served as the control.One hour after the challenge,enzyme-linked immunosorbent assay(ELISA)was applied to measure the level of LTB4,IL-4 and IL-5 in the cell culture supernates.Results Following the incubation with OVA,the levels of LTB4,IL-4 and IL-5 increased significantly in culture supernates of control spleen lymphocytes.Epinastine significantly inhibited the release of LTB4,IL-4 and IL-5 in a dose-dependent manner.At the concentration of 10 μmol/L,the inhibitory effect of epinastine was more potent than that of ebastine and cetirizine for IL-5 and LTB4 release(all P＜0.05):for IL-4,the efrect of epinastine was similar to that of ebastine (P＞0.05)but more potent than that of cetirizine(P＜0.05).Conclusion Epinastine has a potent anti-inflammatory effect.
RESUMO
To determine the pharmacokinetics and bioequivalence of epinastine (EPN) hydrochloride, a promising histamine H1 receptor antagonist, in healthy Chinese volunteers under fasting conditions. METHODS: EPN hydrochloride test and reference tablets were administered as a single dose on two treatment days separated by a 1-week washout period. After dosing, serial blood samples were collected for a period of 36 h, and plasma EPN hydrochloride concentrations were determined by a validated reversed-phase HPLC method and pharmacokinetic parameters were calculated with DAS software. RESULTS: Plasma concentration-time profiles were adequately described by a two-compartment open model. The compound was rapidly absorbed and cleared slowly from plasma with a half-life of approximately 10 h. The main pharmacokinetic parameters of EPN hydrochloride test and reference tablets were as follow: tmax were (2.2±0.5) and (2.0±0.4)h, Cmax were (66±16)and (68±13)μg/L, t1/2 were(10.1±1.3) and (10.4±2.4)h, AUC0-36 were (592±88) and (601±94)μg·h·L-1, respectively. The relative bioavailability of test tablets was (99±13)%. CONCLUSION: The results indicate that the two formulations of EPN hydrochloride tablets are bioequivalent in the rate and extent of absorption.
RESUMO
0.05).The relative bioavailability of domestic EPST tablets was(96.70?14.47)%.CONCLUSION: The result of the statistical analysis showed that the two formulations of EPST were bioequivalent.
RESUMO
BACKGROUND: Alesion, which is known as one of the second generation anti-histamine agents, has diverse anti-allergic effects. Some investigators have reported the clinical effects of Alesion as acting like an addictive agents to inhaled steroid in mild to moderate persistent bronchial asthma. METHODS: We evaluated the additive effects of daily administration of 20 mg of Alesion (epinastine HCl) in 30 mild to moderate persistent bronchial asthma patients. We estimated the clinical effects of Alesion with symptom scores, morning PEFR without bronchodilator, sputum eosinophil counts of induced sputum, spirometer parameters and frequency of short acting 2 agonist inhalation. RESULTS: With administration of Alesion for 4 weeks, the score of dyspnea, cough, nocturnal symptoms and limitation of daily activity were significantly improved. The mean value of morning PEFR without bronchodilator was also significantly improved by administration of Alesion. These improvements appeared after 1 week of administration. But, the frequencies of short acting 2 agonist inhalation, FEV1, FVC, peripheral blood eosinophil count, eosinophil percentage of induced sputum were not changed by the Alesion. About 64% of the enrolled patients expressed the clinical effects of Alesion. The patients complained of headache (1 case), drowsiness or sleepiness (3 cases), and weight gain (1 case) as adverse effects of Alesion. CONCLUSIONS: We suggest that Alesion can be effective as an the additive agent in mild to moderate persistent degree of bronchial asthma.