摘要
目的：研究栀子苷（geniposide）经4种不同途径给药后在大鼠体内的药动学过程,比较各个途径的生物利用度,揭示栀子苷的体内动态变化规律,为栀子苷的临床应用提供理论依据。方法：分别灌胃（ig）、滴鼻（ns）、肌注（im）、尾静脉（iv）给予栀子苷50,8,8和8 mg·kg^-1,不同时间点眼眶取血。应用外标法和反相高效液相色谱法（RP-HPLC）测定血浆中栀子苷的含量,应用DAS统计软件模拟计算,得出相应的药动学参数。结果：ig及im给药符合一室模型,ns给药符合二室模型,iv给药符合三室模型。ig给药的t1/2,Cmax和AUC0－t与其他方式相比,存在显著性差异。不同给药途径的绝对生物利用度分别为F（ig）=9.74%,F（ns）=49.54%,F（im）=72.69%。结论：药动学参数及绝对生物利用度表明,栀子苷在ig,ns,im 3种给药途径的体内生物利用度为im〉ns〉ig。
Objective：In order to provide the basis for pharmaceutical applications in future,we studied the pharmacokinetics of geniposide after administration through 4 routes in rats,compared the properties of bioavailability and revealed the dynamic changes of geniposide in vivo.Methods：Geniposide（50,8,8 and 8 mg·kg^-1） was administered through oral（ig）,nasal（ns）,intramuscular（im） and intravenous（iv） routes.Blood samples were obtained by orbital bleeding at a series of time points.Plasma geniposide concentrations were measured by RP-HPLC determination using external standards.Pharmacokinetic parameters were calculated using DAS software.Results：The kinetics matched to one-compartment model after ig and im administration,to two-compartment model after ns administration,and to Room model after iv injection.There were great differences in t1/2,Cmax and AUC0-t between ig and other administrations.The absolute bioavailability was F（ig）=9.74%,F（ns）=49.54% or F（im）=72.69%,respectively.Conclusion：From pharmacokinetic parameters and absolute bioavailability of geniposide,the order of superiority is imnsig administration.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第9期746-749,754,共5页
Chinese Journal of New Drugs
基金
重大新药创制重大专项(2009ZX09103-393)
中药新型给药系统技术平台"十一五"重大新药创制项目(2009ZX09310-005)
江西省卫生厅科研计划(2009A060)
关键词
栀子苷
药动学
绝对生物利用度
geniposide
pharmacokinetics
absolute bioavailability
