Pharmacokinetics study of niclosamide in mouse plasma, muscle and skin
Objective To develop an LC/MS method for the quantitative analysis of niclosamide in plasma,muscle and skin of mice and apply to its pharmacokinetics,thus to provide experimental data support for the research of anti-cercaria new form of niclosamide and to establish the drug residues analysis approach.Methods Niclosamide in biological samples was extracted by acetone.The quasi-molecular ion peaks m/z 324.9788 and 138.0186 were selected as the fragment of single ion monitoring(SIM) for quantitative determination of niclosamide and p-nitrophenol (internal standard,IS) respectively for analysis of Cmax,T1/2 and AUC in plasma,muscle and skin of mice by HPLC/HRMS.Results The Cmax values of nicloasamide after oral administration at adose of 200mg/kgwere (2251.22±3138),(250.52±41.99) and (3663.01 ± 1279.52) ng/ml in plasma,muscle and skin respectively.The T1/2 was (11.07 ± 0.88),(45.57 ± 0.66) and (14.67 ± 0.31) h,respectively,and the AUC was (23 237 ± 544),(8 458 ± 581) and(79 093 ± 1 060) ng/(h·ml),respectively.Conclusion The results of Cmax and AUC in the skin indicated that niclosamide is more likely to be distributed in the skin,that is good for anti-invasion of schistosome cercariae.
NiclosamidePharmacokineticsLC/MSHigh resolution mass spectrum
NETL
NSTL
万方数据
维普
