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

• Published in: International journal of clinical pharmacology and therapeutics Vol. 56; no. 12; pp. 597 - 603
• Main Authors: Wang, Yan, Lu, Jin, Li, Tengfei, Zhao, Shunbo, Yang, Wen, Liu, Lingye, Shi, Xing, Michael, Mtalimanja, Ding, Li
• Format: Journal Article
• Language: English
• Published: Germany Dustri - Verlag Dr. Karl Feistle GmbH & Co. KG 01.12.2018
• Subjects: 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; Drug dosages; Expectorants - administration & dosage; Expectorants - adverse effects; Expectorants - pharmacokinetics; Female; Gender differences; Healthy Volunteers; Humans; Laboratories; Male; Models, Biological; Pharmaceuticals; Pharmacokinetics; Prescription drugs; Quality control; Tandem Mass Spectrometry; Young Adult; China
• DOI: 10.5414/CP203212
• ISSN: 0946-1965

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. 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. Following single dosing, C values were 8.07 ± 1.31 ng/mL and 25.7 ± 6.5 ng/mL for salbutamol and ambroxol, respectively. The corresponding T 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. 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.
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