title: Determination of antazoline hydrochloride in rat plasma and excreta by reversed-phase ion-pair chromatography and its application to pharmacokinetics.
abstract: A reversed-phase ion pair chromatography method with liquid-liquid extraction analytical method was developed and validated for the determination of antazoline hydrochloride in plasma and excreta of rat. The aim of our study was to characterize the preclinical pharmacokinetics and excretion profiles of antazoline hydrochloride in rats after intravenous injection at the dose of 10 mg/kg. Plasma and excreta samples were extracted with ethyl acetate, and phenacetin was used as the internal standard. The result showed that the method is suitable for the quantification of antazoline hydrochloride in plasma and excreta samples. Analysis of accuracy (90.89-112.33%), imprecision (<7.1%) and recovery (>82.5%) showed adequate values. After a single intravenous administration at 10 mg/kg to rats, plasma concentration profile showed a relative fast elimination proceeding with a terminal elimination half-life of 3.53 h. Approximately 61.8 and 14.2% of the administered dose were recovered in urine and bile after 72 and 24 h post-dosing respectively; 5.9% of the administered dose was recovered in feces after 72 h post-dosing. The above results show that the major elimination route is urinary excretion.
authors.affiliation: Department of Pharmacy, Zhengzhou University, Zhengzhou, 450001, China; Luohe Central Hospital Affiliated to Luohe Medical College, Luohe, 462000, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
authors.forename: Yanle
authors.initials: Y
authors.lastname: Chu
authors.forename: Xiaotian
authors.initials: X
authors.lastname: Li
authors.forename: Baoluo
authors.initials: B
authors.lastname: Wan
authors.forename: Tong
authors.initials: T
authors.lastname: Yu
authors.forename: Linxi
authors.initials: L
authors.lastname: Wang
authors.forename: Lianqi
authors.initials: L
authors.lastname: Hao
authors.forename: Maowen
authors.initials: M
authors.lastname: Guo
mesh_terms: D000818:Animals; D000865:Antazoline / Q000032:analysis* / Q000737:chemistry / Q000493:pharmacokinetics; D001646:Bile / Q000737:chemistry; D056148:Chromatography, Reverse-Phase / Q000379:methods*; D005243:Feces / Q000737:chemistry; D005260:Female; D016014:Linear Models; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity
chemical_list: D000865:Antazoline
keywords: antazoline hydrochloride; excretion; pharmacokinetics; reversed-phase ion pair chromatography