灵仙新苷在Beagle犬体内的药动学及其绝对生物利用度研究  被引量:3

Pharmacokinetics of clematichinenoside AR and its absolute bioavailability in Beagle dogs

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作  者:王大为[1] 李峰[2] 徐平[2] 周磊[2] 刘李[2] 刘晓东[2] 

机构地区:[1]江苏省中医药研究院 [2]中国药科大学药物代谢动力学重点实验室

出  处:《中国临床药理学与治疗学》2012年第11期1211-1215,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基  金:国家十一五新药创制重大专项基金(2009ZX09103-371);江苏省中医药局项目(LB09059);康缘中医药科技创新基金项目(HZ1014KY)

摘  要:目的:研究灵仙新苷在Beagle犬体内的药动学和绝对生物利用度。方法:采用四周期交叉设计,即Beagle犬8只,雌雄各半,随机等分为4组,分别采取单剂量静脉注射(0.75mg/kg)及灌胃(7.5、15和30mg/kg)两种给药方式,交叉给药,间隔1周。并于给药后不同时间点取血,采用LC-MS/MS测定血浆中灵仙新苷的浓度,利用DAS 2.0软件估算灵仙新苷在Beagle犬体内的药动学参数,并计算绝对生物利用度。结果:Beagle犬i.g.7.5、15和30mg/kg灵仙新苷后,估算的t1/2分别为(14.3±2.7)、(13.3±1.3)和(13.7±2.4)h,AUC0-36分别为(1.9±1.2)、(4.5±1.9)和(8.0±3.3)μg.h.mL-1,Cmax分别为(0.14±0.08)、(0.27±0.10)和(0.52±0.28)μg/mL。i.v.0.75mg/kg灵仙新苷后,估算的t1/2为(13.3±3.0)h,AUC0-36为(66.2±12.8)μg.h.mL-1。灌胃灵仙新苷在Beagle犬体内的绝对生物利用度分别为0.32%、0.35%和0.30%。结论:口服灵仙新苷后在Beagle犬体内绝对生物利用度很低,其药动学过程在研究剂量范围内是线性的。AIM: To investigate the pharma cokinetics and absolute bioavailability of clema tichinenoside AR (C-AR) in Beagle dogs. METHODS: By applying four cycle crossover de sign, a single dose of C-AR was administrated (i.v. 0.75 mg/kgori, g. 7.5, 15 or 30 mg/kg) to 8 Beagle dogs. Blood samples were collected before and at different intervals after C-AR ad ministration. The concentration of C-AR in dog plasma was determined by LC-MS/MS method. The pharmacokinetic parameters were estimated by DAS 2.0 pharmacokinetic program, and the absolute bioavailability was calculated. RE- SULTS:After single dose ig of 7.5, 15 and 30 mg/kg C-AR, the pharmacokinetics parameters were estimated as follows: tl/2 : (14.3 4±2.7), (13.3±1.3) and (13.7±2.4) h; AUC0-36:(1.9 ± 1.2), (4.5 ± 1.9) and (8.0 ± 3.3) μg · h· mL-1; Cmax. (0.14±0.08), (0.27±0.10) and (0.52±0.28) μg/mL. After single dose i. v. of 0.75 mg/kg C-AR, the pharmacoki- netics parameters were estimated as follows. tl/2. (13.3 ± 3.0) h, AUC0-36. (66.2 ± 12.8) μg · h · mL-1. The absolute bioavailabili- ty of C-AR following i. g. administration was 0.32%, 0.35% and 0.30%. CONCLUSION. The absolute bioavailability of C-AR in dogs is low, and the pharmacokinetic properties were linear in Beagle dogs.

关 键 词:灵仙新苷 LC—MS MS 药动学 绝对生 物利用度 Beagle犬 

分 类 号:R969.1[医药卫生—药理学]

 

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