Pharmacokinetics and Bioequivalence Evaluation of Two Montelukast Sodium Chewable Tablets in Healthy Chinese Volunteers Under Fasted and Fed Conditions

Li, Weihong; Wang, Yanrong; Pei, Yingzi; Yue, Xia

doi:10.2147/dddt.s298355

Cited by 5 publications

(4 citation statements)

References 16 publications

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“…Montelukast sodium OSF and CT had numerically similar PK parameters. Generally, these parameters were consistent with previous studies of montelukast sodium CT (15)(16)(17). Additionally, we found that C max decreased and T max increased under the fed conditions compared with the fasting conditions.…”

Section: Discussionsupporting

confidence: 93%

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Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions

Zhu¹,

Wang²,

Han³

et al. 2023

Ann Transl Med

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Background The oral soluble film (OSF) is a new drug delivery system. Whether montelukast sodium OSF has similar pharmacokinetic (PK) properties and bioequivalence to chewable tablet (CT) should be investigated. Methods This study, conducted at Haikou People’s Hospital, consisted of two trials: a randomized, open-label, single-dose, 3-sequence, 3-period crossover trial under fasting conditions and a randomized, open-label, single-dose, 2-sequence, 2-period crossover trial under fed conditions. Healthy volunteers were randomized 1:1:1 to receive single-dose oral montelukast sodium OSF without water, OSF, or CT with water in the fasting trial, and 1:1 to receive OSF or CT with water in the fed trial in each period, with a 7-day washout period. Randomization was performed according to random number tables generated using computer. Blood samples were collected over a 24-h period. Plasma drug concentrations were tested using high-performance liquid chromatography-tandem mass spectrometry. The primary PK parameters were maximum plasma drug concentration (C max ), area under the plasma drug concentration-time curve (AUC) from t=0 to the last quantifiable concentration (AUC 0–t ), and AUC from t=0 to infinity (AUC 0–∞ ). The other PK parameters included time to C max (T max ), terminal elimination rate constant (λ z ), and half-life (t 1/2 ). Safety was also assessed. Analysis of variance on log-transformed primary PK parameters was applied to analyze the bioequivalence between the OSF and CT. The bioequivalence margin was 80–125%. Results From November 2018 to January 2019, 30 subjects were included in each trial. The PK parameters between OSF and CT were numerically similar. All 90% confidence intervals (CIs) of the geometric mean ratio (GMR) for the primary PK parameters fell within 80–125%, confirming the bioequivalence of montelukast sodium OSF and CT under fasting and fed conditions. In the fasting trial, 6 (20%) adverse events (AEs) were reported, including 3 (10%) cases after OSF administration without water and 3 (10%) after OSF administration with water, with no serious AEs. No AEs were recorded in the fed trial. Conclusions Montelukast sodium OSF is bioequivalent to CT, with acceptable safety. The OSF is an alternative option of CT. Trial Registration ClinicalTrials.gov identifiers: NCT05528198 (the fasting trial) and NCT05531994 (the fed trial).

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Section: Discussionsupporting

confidence: 93%

“…No AEs were observed in the fed trial. These safety results were consistent with previous data on montelukast sodium CT ( 15 - 17 ). There were two treatment-related AEs; one was in grade 1 and did not require treatment, while the other was in grade 2 and recovered after treatment.…”

Section: Discussionsupporting

confidence: 93%

Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions

Zhu¹,

Wang²,

Han³

et al. 2023

Ann Transl Med

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“…Montelukast sodium belongs to a type of leukotriene antagonist that is selective. [7][8][9] It can prevent leukotriene from attaching to receptors, thus regulating inflammation while compensating for budesonide's limitations. [10][11][12] Therefore, to further investigate the clinical therapeutic effect of budesonide combined with montelukast sodium in bronchial asthma, 86 children with bronchial asthma admitted to our hospital from January 2019 to December 2020 were selected for the following study and report.…”

Section: Introductionmentioning

confidence: 99%

Effect of budesonide combined with montelukast sodium on pulmonary function parameters and immunoglobulin levels in children with bronchial asthma

Chu

Liang

Chen

2023

Allergol Immunopathol

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Background and aim: Bronchial asthma is a prevalent type of respiratory disease that affects a large proportion of pediatric patients. The purpose of this study is to further investigate the clinical effects of budesonide combined with montelukast sodium in treating bronchial asthma. Methods: Eighty-six children with bronchial asthma were equally divided into study and control groups via randomized double-blind controlled trial. The control group was treated with aerosol inhalation of budesonide combined with placebo, while the study group was treated with budesonide combined with montelukast sodium. Pulmonary function parameters, immunoglobulin, and recovery of related symptoms, along with the adverse reaction rate, were observed and compared between both groups. Results: Before treatment, there was no marked difference in pulmonary function parameters and immunoglobulin indexes between both groups (P > 0.05). All pulmonary function indicators and immunoglobulin indexes in both groups improved following therapy, with the study group outperforming the control group (P < 0.05). The recovery time of related symptoms in the study group was shorter than that in the control group (P < 0.05). The incidence of adverse reactions in both groups was compared, with notable differences (P < 0.05). Conclusion: Budesonide combined with montelukast sodium in the treatment of bronchial asthma has the value of clinical application and promotion.

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“…MP-AzeFlu Nasal Spray consists of a fixed-dose combination of azelastine hydrochloride (AZE) and fluticasone propionate (FLU) that is used for the relief of symptoms of moderate to severe seasonal (SAR) and perennial allergic rhinitis (PAR). 1 , 2 Due to different primary mechanisms of action of the individual agents, MP-AzeFlu nasal spray provides greater efficacy than therapy with each agent (azelastine hydrochloride and fluticasone propionate) alone. The fixed drug combination has been approved in 65 countries worldwide and it has been marketed in the US since September 2012 and in Europe since March 2013 for use by adults and adolescents aged ≥12 years and in the US since February 2015 for children aged ≥6 years.…”

Section: Introductionmentioning

confidence: 99%

The Comparative Bioavailability of Fluticasone and Azelastine Delivered as a Single Fixed Dose Combination (MP-AzeFlu) in Comparison to Two Different Formulations of Azelastine and Fluticasone Propionate Following Intranasal Administration in Healthy Chinese Volunteers

Wei¹,

Liu²,

Xue³

et al. 2023

JAA

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Objective Two studies (Study I and Study II) were conducted in healthy Chinese volunteers to confirm that there was no pharmacokinetic drug interaction between AZE and FLU in MP-AzeFlu. The secondary objective was to evaluate the pharmacokinetic parameters of MP-AzeFlu compared with the commercially available mono-components. Methods Both studies were a randomized, open-label, three-period, six-sequence, single-dose cross-over trial (William’s design) conducted at Beijing Hospital (Beijing, China) in September and October of 2019 in 30 healthy adult male and female volunteers. The natural log transformed parameters: AUC 0-tlast , AUC 0-∞ and C max were analyzed. Results The comparison of PK parameters between MP-AzeFlu and Aze (commercially available) showed that the LS mean ratios (90% CI) values for, AUC 0–tlast , AUC 0–∞ and C max were 100.29% (94.31–106.66%), 100.76% (94.60–107.32%) and 93.14% (81.47–106.48%). The comparison of PK parameters between MP-AzeFlu and Flu (commercially available) for the bioavailability evaluation showed that the LS mean ratios (90% CI) values for, AUC 0–tlast , AUC 0–∞ and C max were 83.48% (69.81–99.82%), 100.19% (87.34–114.94%) and 81.91% (68.50–97.95%). Conclusion The study results confirm that neither the FLU or the AZE component in the combination product (MP-AzeFlu), nor the existing qualitative and quantitative differences in the formulation between the currently marketed AZE and FLU mono-product, display significant potential to impact the systemic exposure of AZE or FLU in Chinese subjects.

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Pharmacokinetics and Bioequivalence Evaluation of Two Montelukast Sodium Chewable Tablets in Healthy Chinese Volunteers Under Fasted and Fed Conditions

Cited by 5 publications

References 16 publications

Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions

Pharmacokinetics and bioequivalence study of montelukast sodium oral soluble film and chewable tablet in healthy Chinese volunteers: randomized trials under fasting and fed conditions

Effect of budesonide combined with montelukast sodium on pulmonary function parameters and immunoglobulin levels in children with bronchial asthma

The Comparative Bioavailability of Fluticasone and Azelastine Delivered as a Single Fixed Dose Combination (MP-AzeFlu) in Comparison to Two Different Formulations of Azelastine and Fluticasone Propionate Following Intranasal Administration in Healthy Chinese Volunteers

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