Bilastine 2.5mg/ml oral solution sugar free

BACKGROUND: Oral H1-antihistamines (OAHs) are among the most frequently used medications for the treatment of allergic rhinitis (AR). OBJECTIVE: To perform a systematic review and network meta-analysis comparing the efficacy and safety of individual OAHs in patients with AR. METHODS: We searched 4 electronic bibliographic databases and 3 clinical trial databases for randomized controlled trials assessing adults with perennial or seasonal AR, and comparing (1) OAH versus placebo or (2) different individual OAHs. We performed a network meta-analysis on the Total Nasal Symptom Score, Total Ocular Symptom Score, Rhinoconjunctivitis Quality-of-Life Questionnaire, development of adverse events, and withdrawals due to adverse events. Certainty of evidence for comparisons involving the most clinically relevant second-generation OAHs was assessed using Grading of Recommendations, Assessment and Evaluation approach to network meta-analysis. RESULTS: We included 74 randomized controlled trials (21 on perennial AR and 53 on seasonal AR). Cetirizine, ebastine, bilastine, and rupatadine were among the individual medications associated with the highest efficacy for improving nasal symptoms. For other efficacy outcomes, the most efficacious interventions varied. A similar frequency of adverse events was observed among different individual second-generation OAHs, with serious adverse events being rare. For most comparisons, the certainty of evidence was rated as "low" or "very low," indicating substantial uncertainty regarding the treatment effects. CONCLUSIONS: Although some OAHs seem to be more efficacious than others, most of the differences between individual second-generation medications are trivial or small. In addition, we did not find any relevant differences in the safety profiles of second-generation OAHs.

Abstract licence: CC BY

Orodispersible tablets (ODT) rapidly dissolve in the oral cavity and can improve patient’s convenience. This pharmacokinetic study assessed the bioequivalence of a novel 20 mg ODT formulation of bilastine compared with bilastine 20 mg tablets in healthy volunteers under fasting conditions. A phase I, single-center, open-label, two-period, two-sequence crossover randomized clinical trial was conducted. The study comprised two periods, in which participants were administered a single oral dose of bilastine 20 mg in the form of ODT as the test product, or conventional tablets as the reference product, and a washout of 7 days between each period. Blood samples were collected for up to 72 h. Bioequivalence was established if the 90% confidence intervals of the Cmax and AUC0–t were within the acceptance range (80−125%). Safety was evaluated at the follow-up visit (days 4−7 after the second dose) and throughout the study. A total of 42 healthy volunteers were randomized, and 41 completed the study. Pharmacokinetic parameters were comparable for both formulations after a single dose of 20 mg. Bilastine ODT and conventional tablets were bioequivalent as the 90% confidence intervals of the test over reference ratios were within the predefined range (80−125%). Both formulations were well tolerated and showed a similar safety profile. Bilastine ODT was bioequivalent to the reference treatment formulated as conventional tablets when administered as a single oral dose of 20 mg under fasting conditions. Both formulations showed a similar tolerability and safety profile, with no serious adverse events or significant analytical alterations reported. Trial Registration: 2019-004071-39. Date of authorization: 10 December 2019.

Abstract licence: CC BY-NC

Introduction: Allergic Rhinitis (AR), affecting 10-25% of the global population, is commonly treated with antihistamines and corticosteroids. H2-blockers, when combined with H1 antihistamines, enhance treatment efficacy and reduce symptoms. There is a need to conduct studies to establish more evidence around this combination and aid in the informed clinical decision-making process. Aim: To compare the efficacy of Bilastine versus Bilastine combined with Famotidine in the management of AR at days 7 and 14 and also to compare serum IgE levels at days 0 and 14 among both groups. Materials and Mehods: This open-label Randomised Controlled Trial (RCT) was conducted in the Pharmacology and Otorhinolaryngology department of Agartala Government Medical College (AGMC) and Govind Ballabh Pant Hospital (GBPH) between 1st February 2023 and 30th June 2024. The study included 340 newly diagnosed acute AR patients aged 18 years and above from the ENT OPD. Participants were diagnosed by clinicians based on signs and symptoms such as nasal itching, sneezing, a runny nose, and nasal obstruction, with symptoms persisting for more than four consecutive weeks. Randomised participants received either Bilastine 20 mg daily or Bilastine combined with Famotidine 40 mg daily for 14 days. The primary outcomes were nasal and non nasal symptom scores, while secondary outcomes included serum IgE levels. Data were collected in an approved Case Report Form (CRF) and statistically analysed using the Independent t-test, Mann-Whitney U test, Wilcoxon signed-rank test, and Chi-square test. Results: The study included 340 participants aged between 18 and 80 years, comprising 178 (52.4%) males and 253 (74.4%) from urban areas. Rhinorrhea (83 cases, 24.4%) and nasal congestion (79 cases, 23.2%) were the most common symptoms. The combination therapy led to a significantly faster reduction in nasal symptoms (p-value=0.001). Serum IgE levels decreased in both groups (p-value=0.001 in Group A, p-value<0.001 in Group B), with a cut-off for serum IgE being <150 mg/dL. Adverse reactions were minimal, with two cases of nausea and bloating in Group A and two cases of nausea in Group B. Conclusion: AR predominantly affected younger adults (ages 21- 25 years). Combination therapy showed no adverse effects and provided faster symptom relief while reducing serum IgE levels.

Abstract licence: CC BY-NC-ND

Abstract For the treatment of rhinitis and asthma, a combination of Montelukast sodium and Bilastine has just been approved. Based on the first derivative of synchronous fluorescence, the current work developed a green, highly accurate, sensitive, and selective spectroscopic approach for estimating Montelukast sodium and Bilastine in pharmaceutical dosage form without previous separation. The selected technique focuses on measuring the synchronized fluorescence of the studied medications at a fixed wavelength range (Δλ) = 110 nm, and using the amplitude of the first derivative's peak at 381 and 324 nm, for quantitative estimation of Montelukast sodium and Bilastine, respectively. The impacts of different factors on the referred drugs' synchronized fluorescence intensity were investigated and adjusted. The calibration plots for were found to be linear over concentration ranges of 50–2000 ng mL −1 for Montelukast sodium and 50–1000 ng mL −1 for Bilastine. Montelukast sodium and Bilastine have LODs of 16.5 and 10.9 ng mL −1 , respectively. In addition, LOQs were: 49.9 and 33.0 ng mL −1 , for both drugs, respectively. The developed method was successfully employed to quantify the two drugs in synthetic tablets mixture and in laboratory prepared mixtures containing varied Montelukast and Bilastine ratios. To compare the results with the published analytical approach, a variance ratio F-test and a student t-test were used, which revealed no significant differences.

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Bilastine is a novel nonsedative H1-receptor antagonist, which may be used for the symptomatic treatment of chronic idiopathic urticaria (CU). This study describes the validation of an UV spectrophotometric method for quantitative determination of bilastine in tablets using 0.1 mol L-1 HCl as solvent. The method was specific, linear, precise, exact and robust at 210 nm, confirming that the method is fast and useful to the routine quality control of bilastine in tablets. The validate method was compared to liquid chromatography (HPLC), which was previously developed and validated to the same drug, and no significative difference between the methods using Student´s t test was found to bilastine quantitation.

Abstract licence: CC BY-NC-SA

• A novel method developed to measure the assay and related impurities in a single run. • Thirteen analytes separated within 20 minutes of runtime. • Forced degradation unknown impurities characterized by LCMS/MS. • Robustness study was designed by Quality by Design software. • The environmental impact was evaluated using green chemistry softwares. This study introduces a novel ultra-performance liquid chromatography (UPLC) method for the rapid, simple, and accurate detection of contaminants in bilastine (BLS) and montelukast (MTK) tablet formulations. The separation of BLS impurity-A, BLS impurity-B, BLS, MTK impurity-A, MTK, and MTK impurity-B was achieved using an Acquity BEH C18 column (50 × 2.1 mm, 1.7 μm) under gradient eluent conditions. The mobile phases consisted of 0.1% triethylamine in water with the pH adjusted to 2.5 using orthophosphoric acid (mobile phase A) and acetonitrile (mobile phase B). The ratio of mobile phase A to B was 70:30 (v/v). The column flow rate was set at 0.2 mL/min, and the photodiode array detector (PDA) was used to quantify the analytes. The detection wavelength was set to 224 nm. In a runtime of just 20 minutes, 13 analytes were successfully separated. The retention times for the target compounds and impurities were as follows: BLS impurity-A: 1509 min, BLS impurity-B: 3435 min, BLS: 5668 min, MTK impurity-A: 8137 min, MTK: 9784 min, MTK impurity-B: 11,853 min. The unspecified impurities in the degradation samples were detected at retention times of 2174, 2657, 3368, 4143, 8239, 11,722, and 12,436 minutes, and were characterized using liquid chromatography-mass spectrometry (LC-MS). The UPLC-based analytical method demonstrated in this study is an effective and efficient technique for the quantification of BLS, MTK, and their associated impurities in tablet formulations. This method has been validated in accordance with ICH Q2(R2) and USP <1225> guidelines. Cette étude présente une nouvelle méthode de chromatographie liquide ultra-performante (UPLC) pour la détection rapide, simple et précise des contaminants dans les formulations de comprimés de bilastine (BLS) et de montélukast (MTK). La séparation des impuretés BLS A, BLS BLS, BLS, MTK A, MTK et MTK B a été réalisée à l’aide d’une colonne Acquity BEH C18 (50 × 2,1 mm, 1,7 μm) dans des conditions d’éluant à gradient. Les phases mobiles étaient constituées de 0,1 % de triéthylamine dans l’eau avec un pH ajusté à 2,5 à l’aide d’acide orthophosphorique (phase mobile A) et d’acétonitrile (phase mobile B). Le rapport entre les phases mobiles A et B était de 70:30 (v/v). Le débit de la colonne a été fixé à 0,2 mL/min et le détecteur à barrette de photodiodes (PDA) a été utilisé pour quantifier les analytes. La longueur d’onde de détection a été fixée à 224 nm. En seulement 20 minutes, 13 analytes ont été séparés avec succès. Les temps de rétention des composés cibles et des impuretés étaient les suivants : BLS impureté-A : 1509 min, BLS impureté-B : 3435 min, BLS : 5668 min, MTK impureté-A : 8137 min, MTK : 9784 min, MTK impureté-B : 11 853 min. Les impuretés non spécifiées dans les échantillons de dégradation ont été détectées à des temps de rétention de 2174, 2657, 3368, 4143, 8239, 11 722 et 12 436 minutes, et ont été caractérisées par chromatographie liquide-spectrométrie de masse (LC-MS). La méthode d’analyse par UPLC démontrée dans cette étude est une technique efficace et efficiente pour la quantification des BLS, des MTK et de leurs impuretés associées dans les formulations de comprimés. Cette méthode a été validée conformément aux directives ICH Q2(R2) et USP <1225>.

Abstract licence: CC BY-NC-ND