Pharmacokinetic and absolute bioavailability study of naloxone hydrochloride nasal sprays
LIU Ya-qin
SUN Jian-xu
ZHANG Xiao-yan
GAO Yong-liang
Abstract：Objective:To study the pharmacokinetics and bioavailability of naloxone hydrochloride nasal sprays in dogs.Methods:The HPLC method was developed to determine the concentration of naloxone hydrochloride in plasma.The two-period cross-over design was developed to study the pharmacokinetic and bioavailability of naloxone hydrochloride nasal sprays in dogs.Results:Good linearity was obtained in the range of 5～320 ng·mL~(-1)(r=0.999).The method recovery was 87%～97%.The absolute recovery was 71%～85%.Both of the intraday and inter-day RSDs were less than 9%.The concentration-time curve of naloxone hydrochloride nasal sprays was consistent with the two-compartment model.The main pharmacokinetic parameters were as follows:T_( max) 10 min,C_( max) (279.49±38.48)ng·mL~(-1),t_(1/2β) (176.94±30.14)min,CL×10~4(5.48±0.77)mL·min~(-1),AUC_(0～12h) (14 495.00±2 029.38)ng·min·mL~(-1),AUC_(0～∞) (15 749.63±2 177.48)ng·min·mL~(-1).The absolute bioavailability of naloxone hydroehloride nasal sprays in dogs was(87.88±6.37)%.Conclusion:Naloxone hydrochloride can be absorbed quickly after intranasal administration in dogs and the absolute bioavailability of Naloxone hydrochloride is high.
Keywords：snaloxone hydrochloridenasal spraysHPLCpharmacokineticbioavailability
Publication Date：2010-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)