Pharmacokinetics and safety of glycopyrrolate: An open-label, single-dose study in Chinese adult patients after general anesthesia surgery

Abstract

Background

Glycopyrrolate injection is an anticholinergic drug. The pharmacoeconomic advantages of glycopyrrolate, approved for marketing under the current Chinese health insurance payment model, are significant. The aim of this research was to characterize its pharmacokinetic properties and safety in Chinese adult patients after general anesthesia surgery.

Methods

An open-label, single-dose pharmacokinetics, safety and population pharmacokinetics of glycopyrrolate was performed in Chinese adult patients after general anesthesia surgery. Chinese adult patients after general anesthesia surgery were single intravenously administered by glycopyrrolate. Venous blood samples were drawn before and after administration and further quantified by a validated HPLC-MS/MS method. Safety was monitored during the whole stages. Population pharmacokinetics were performed by non-linear mixed-effects modelling.

Results

A total of 18 subjects were enrolled and evaluated. The principle pharmacokinetic parameters of C_max, t_1/2, AUC_0-t, AUC_0-∞, Vz and CL of glycopyrrolate were 45.8 ± 28.9 ng/mL, 1.7 ± 0.4 h, 10.3 ± 2.3 h∗ng/mL, 10.6 ± 2.4 h∗ng/mL, 1.9 ± 0.6 L/kg and 0.8 ± 0.2 L/h/kg, respectively. Safety was acceptable and no serious adverse events were detected. A three-compartment model and fitted concentration-time curve for glycopyrrolate were represented and validated, which was constant with published literatures.

Conclusions

Pharmacokinetics and safety of glycopyrrolate were investigated systemically with the help of this open-label, single-dose study in Chinese adult patients after general anesthesia surgery. Results of present study provide systemic data basis for improving the accessibility of the drug to Chinese patients and individualized and precise medication.

Clinical trial registration

No. CTR20170001 (Chinese Clinical Trial Registry, https://db.yaozh.com/linchuangshiyan/bJaRbmNnaGljlWRilJaYmA.html, Time of initial registration: 18 Feb 2017)