Pharmacokinetics and safety of salbutamol/ambroxol fixed-dose combination granules in healthy Chinese subjects

Int J Clin Pharmacol Ther. 2018 Dec;56(12):597-603. doi: 10.5414/CP203212.

Abstract

Objectives: The aim of the study was to investigate the pharmacokinetics and tolerability of salbutamol/ambroxol fixed-dose combination granules following single and multiple dosing in healthy Chinese subjects.

Materials and methods: This was a randomized, open-label, two-period, one-sequence study (n = 12). Each subject received a single oral dose in period 1 and multiple doses in period 2. Plasma concentrations of these two components were determined using a validated LC-MS/MS method. Adverse events (AEs) were documented throughout the study. Investigators evaluated AEs in terms of frequency, duration, intensity, seriousness, outcome, and relationship to study drugs.

Results: Following single dosing, Cmax values were 8.07 ± 1.31 ng/mL and 25.7 ± 6.5 ng/mL for salbutamol and ambroxol, respectively. The corresponding T1/2 values were 8.15 ± 3.13 hours and 9.31 ± 2.27 hours, respectively. Moreover, no statistical differences in the pharmacokinetics of salbutamol and ambroxol in subjects receiving single or multiple dosage were observed. Single- and multiple-dose oral administration of fixed-dose combination granules were safe and well tolerated in healthy Chinese subjects. Drug hypersensitivity syndrome did not occur during our study.

Conclusion: The pharmacokinetics of salbutamol and ambroxol in the fixed-dose combination granules were not affected by dosing duration, and gender differences seemed to have no effect on the pharmacokinetics of salbutamol and ambroxol after a single dose and multiple doses of the medication. .

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adrenergic beta-2 Receptor Agonists / administration & dosage
  • Adrenergic beta-2 Receptor Agonists / adverse effects
  • Adrenergic beta-2 Receptor Agonists / blood
  • Adrenergic beta-2 Receptor Agonists / pharmacokinetics*
  • Adult
  • Albuterol / administration & dosage
  • Albuterol / adverse effects
  • Albuterol / blood
  • Albuterol / pharmacokinetics*
  • Ambroxol / administration & dosage
  • Ambroxol / adverse effects
  • Ambroxol / blood
  • Ambroxol / pharmacokinetics*
  • China
  • Chromatography, Liquid
  • Dosage Forms
  • Drug Administration Schedule
  • Expectorants / administration & dosage
  • Expectorants / adverse effects
  • Expectorants / pharmacokinetics*
  • Female
  • Healthy Volunteers
  • Humans
  • Male
  • Models, Biological
  • Tandem Mass Spectrometry
  • Young Adult

Substances

  • Adrenergic beta-2 Receptor Agonists
  • Dosage Forms
  • Expectorants
  • Ambroxol
  • Albuterol