Comparative Bioequivalence Study of Two Marketed Formulation of Betamethasone Injectable Suspensions

Zakeri–Milani, Parvin; Ghanbarzadeh, Saeed; Basmenji, S.; Valizadeh, Hadi

doi:10.1055/s-0033-1348223

Cited by 2 publications

(2 citation statements)

References 24 publications

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“…Plasma BET concentrations after IM administration (Figure 5) were high during the first 24 h after administration and, then, decreased, being detected in all volunteers up to 96 h after administration at very low concentrations. Plasmatic concentrations obtained are in agreement with previous published data 29–31 . Different recovery profiles of CORT secretion were observed depending on the volunteer, starting for some of the volunteers in the period 72–96 h after administration, although for some volunteers, the complete recovery to basal values is achieved after 10–15 days (Figure S2).…”

Section: Discussionsupporting

confidence: 91%

Elimination profiles of betamethasone after different administration routes: Evaluation of the reporting level and washout periods to ensure safe therapeutic administrations

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Monfort

Alechaga

et al. 2020

Drug Testing and Analysis

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Betamethasone (BET) is prohibited in sports competitions when administered by systemic routes, and it is allowed by other routes for therapeutic purposes. In out‐of‐competition periods, there is no restriction of use. The present work aimed to assess the urinary excretion of BET and its metabolites after allowed and prohibited administrations to verify the suitability of the current reporting level of 30 ng/ml used to distinguish allowed and prohibited administrations and to establish washout periods for oral and intramuscular (IM) administrations when out‐of‐competition treatments are needed. BET was administered to healthy volunteers by different routes: topical (10 mg/day for 5 days, n = 6 males), intranasal (320 μg/day for 3 days, n = 4 males and 4 females), oral (0.5 mg, n = 8 males) or IM (6 mg, n = 6 males, or 12 mg, n = 4 males and 4 females). Urine and plasma samples collected before and after administration were analysed using liquid chromatography–tandem mass spectrometry. Among all studied metabolites, the parent drug was selected as the best discriminatory marker. After topical administration, BET concentrations were lower than 6.6 ng/ml. However, after intranasal treatment, some samples at concentrations close to or higher than 30 ng/ml were detected, suggesting the need to revise the current reporting level. Urinary concentrations after oral and intranasal administrations were similar, and after IM administration, concentrations were much higher. Taking into account all information, a urinary reporting level of 60 ng/ml is proposed. Washout periods of at least 48 and 96 h are recommended after oral and IM administrations, respectively.

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Section: Discussionsupporting

confidence: 91%

Elimination profiles of betamethasone after different administration routes: Evaluation of the reporting level and washout periods to ensure safe therapeutic administrations

Coll

Monfort

Alechaga

et al. 2020

Drug Testing and Analysis

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“…The kinetics of betamethasone obtained following i.m. administration of the dual formulation showed considerable interstudy variability: there was up to 5.8‐fold difference in drug exposure across four independent, healthy‐volunteer studies ( Table S4 ). One potential cause of the large interstudy variability is likely to be sample stability, as plasma samples needed to be stabilized with the addition of a phosphatase/esterase inhibitor .…”

Section: Methodsmentioning

confidence: 99%

Evaluation of Maternal Drug Exposure Following the Administration of Antenatal Corticosteroids During Late Pregnancy Using Physiologically‐Based Pharmacokinetic Modeling

Milad²

2019

Clin Pharma and Therapeutics

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Betamethasone and dexamethasone are the most widely studied antenatal corticosteroids (ACS) administered to pregnant women, just prior to the birth of a preterm neonate, to accelerate fetal lung maturation. Although betamethasone, predominantly used in developed countries, has been shown to be an effective and safe intervention for reducing neonatal mortality, the choice of ACS and optimal dosing in low and middle income countries (LMICs) remains unclear. This is primarily because the exposure-response relationships have not been established for ACS despite the long history of use. As the first step toward the optimal use of ACS in LMICs, we developed physiologically-based pharmacokinetic (PBPK) models to describe the kinetics of ACS following i.v., p.o., or i.m. dosing. In vitro data describing the cytochrome P450 3A4 enzyme contribution were incorporated and this was refined using clinical data. The models can be applied prospectively to predict kinetics of ACS in pregnant women receiving various dosing regimens.Preterm birth is a major cause of death and morbidity in newborns worldwide and the majority of preterm deliveries and deaths occur in sub-Saharan African and South Asian countries. 1 Respiratory morbidity, including respiratory distress syndrome (RDS), is a serious complication of preterm birth and the primary cause of early neonatal mortality and disability. The administration of antenatal corticosteroids (ACS) to a pregnant woman (who is at risk of imminent preterm birth) is recommended to promote fetal

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Comparative Bioequivalence Study of Two Marketed Formulation of Betamethasone Injectable Suspensions

Abstract: Based on the 90% CIs of Cmax, AUC0-t and AUC0-∞ in these healthy Iranian male subjects, the test and reference formulations of betamethasone injectable suspension met the regulatory requirements for bioequivalence.

Cited by 2 publications

References 24 publications

Elimination profiles of betamethasone after different administration routes: Evaluation of the reporting level and washout periods to ensure safe therapeutic administrations

Elimination profiles of betamethasone after different administration routes: Evaluation of the reporting level and washout periods to ensure safe therapeutic administrations

Evaluation of Maternal Drug Exposure Following the Administration of Antenatal Corticosteroids During Late Pregnancy Using Physiologically‐Based Pharmacokinetic Modeling

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