Bioavailability and pharmacokinetics profile of helicid in beagle dogs using gradient elution high performance liquid chromatography electrospray ionization mass spectrometry.
A simple, sensitive and reliable gradient elution high performance liquid chromatography electrospray ionization mass spectrometry (HPLC-ESI-MS) method was developed for quantifying helicid in dog plasma. The limit of detection (LOD) and the lower limit of quantitation (LLOQ) were 0.3 and 1 ng/mL, respectively. This method was validated for selectivity, linearity, accuracy and precision, extraction recoveries, matrix effects, carry-over, cross-talk, dilution integrity, stability and incurred sample reanalysis (ISR). Bioavailability and pharmacokinetic parameters of helicid in beagle dogs were researched from a two period crossover design study. After intravenous administration (i.v.), helicid had a mean (± SD) AUC0-∞ of 12062.06 ± 2482.69 ng/mL h and terminal half-life (t1/2 z) of 2.91 ± 1.37 h, while Cmax was 35613.23 ± 8157.18 ng/mL. Following intragastric gavage administration (i.g.), AUC0-∞ was 7589.16 ± 1797.20 ng/mL h along with a longer t1/2 z of 4.10 ± 4.35 h. Cmax was researched at 0.58 ± 0.20 h. The absolute bioavailability (F) of helicid was 15.74 ± 1.87%.
Anhui Provincial Center for Drug Clinical Evaluation, Yijishan Hospital, Wannan Medical College, Wuhu 241001, Anhui, PR China.
Yuanwei
Y
Jia
Department of Clinical Pharmacy, Wannan Medical College, Wuhu 241001, Anhui, PR China.
Jie
J
Shen
Key Laboratory of Pharmacokinetics and Drug Metabolism, China Pharmaceutical University, 24# Tongjia Xiang Street, Nanjing 210009, Jiangsu, PR China.
Jianguo
J
Sun
Key Laboratory of Pharmacokinetics and Drug Metabolism, China Pharmaceutical University, 24# Tongjia Xiang Street, Nanjing 210009, Jiangsu, PR China.
Wei
W
Wang
Anhui Provincial Center for Drug Clinical Evaluation, Yijishan Hospital, Wannan Medical College, Wuhu 241001, Anhui, PR China. Electronic address: article2027@sohu.com.
Haitang
H
Xie
D061605:Administration, Intravenous; D000284:Administration, Oral; D000818:Animals; D001547:Benzaldehydes / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D018592:Cross-Over Studies; D004285:Dogs; D005260:Female; D057230:Limit of Detection; D016014:Linear Models; D008297:Male; D011897:Random Allocation; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*
D001547:Benzaldehydes; C055677:helicide
Bioavailability; HPLC–ESI-MS; Helicid; Pharmacokinetics