Pharmacokinetics of guaifenesin, pseudoephedrine and hydrocodone in a combination oral liquid formulation, administered as single and multiple doses in healthy Chinese volunteers, and comparison with data for individual compounds formulated as Antuss®.
1. A new oral liquid formulation combining guaifenesin, pseudoephedrine and hydrocodone is effective in improving the symptoms of common cold. The pharmacokinetic properties of the individual components were evaluated in a randomized, open-label, four-period study in 12 healthy Chinese volunteers following single and multiple doses. The data were compared with data for the individual ingredients in Antuss®. 2. In the single-dose period, exposure levels (AUC and Cmax) for guaifenesin, pseudoephedrine and hydrocodone increased directly as the dose of the oral liquid formulation increased from 5 to 15 mL. Only minor amounts of guaifenesin and hydrocodone were excreted in urine (∼0.10% and 4.66%, respectively). Pseudoephedrine was mainly excreted unchanged, with 44.95% of the dose excreted in urine within 24 h. After multiple dosing, there was no obvious accumulation of any drug, as assessed by AUC. When considering Cmax, there was a trend toward accumulation of hydrocodone and pseudoephedrine. The pharmacokinetic profiles of guaifenesin and pseudoephedrine in the oral liquid formulation were similar to those in the branded preparation, Antuss®. 3. The newly developed oral liquid formulation combining guaifenesin, pseudoephedrine and hydrocodone was safe and well tolerated and might provide a reliable alternative to the branded formulation for patients with common colds.
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Shuhua
S
Deng
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Wencan
W
Huang
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Xiaojia
X
Ni
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Ming
M
Zhang
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Haoyang
H
Lu
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Zhanzhang
Z
Wang
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Jinqing
J
Hu
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Xiuqing
X
Zhu
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Chang
C
Qiu
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Dewei
D
Shang
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Yuefeng
Y
Zhang
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Linghui
L
Xiong
a Institution of National Drug Clinical Trials, The Affiliated Brain Hospital of Guangzhou Medical University (Guangzhou Huiai Hospital) , Guangzhou , China.
Yuguan
Y
Wen
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D005260:Female; D006140:Guaifenesin / Q000493:pharmacokinetics*; D064368:Healthy Volunteers; D006801:Humans; D006853:Hydrocodone / Q000493:pharmacokinetics*; D008297:Male; D054199:Pseudoephedrine / Q000493:pharmacokinetics*
D006140:Guaifenesin; D006853:Hydrocodone; D054199:Pseudoephedrine
Combination oral liquid formulation; guaifenesin; hydrocodone; pharmacokinetic; pseudoephedrine