银杏叶滴丸剂与片剂的药动学及生物等效性评价  

Pharmacokinetics and bioequiavalence assessment of Ginkgo biloba extract dropping pills and tablets

作　　者：王长虹[1] 李宏 侴桂新[1] 程雪梅[1] 张芳[1] 王峥涛[1] 

机构地区：[1]上海中医药大学中药研究所 [2]浙江九旭药业有限公司,浙江金华321000

出　　处：《中国新药与临床杂志》2005年第12期946-950,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的:对银杏滴丸剂和片剂的药动学和生物等效性进行研究和评价。方法:10只新西兰家兔随机分成2组,先后单剂量口服受试制剂和参比制剂后,采用高效液相色谱质谱(HPLCMS)法测定家兔分别口服银杏叶滴丸剂与片剂后血中银杏内酯A(ginkgolideA,GA),银杏内酯B(ginkgolideB,GB),银杏内酯C(ginkgolideC,GC)及白果内酯(bilobalide,BB)的血药浓度。用3P97药动学程序计算GA,GB,GC及BB的药动学参数。以AUC0～12,tmax和cmax为指标,以双单侧t检验进行生物等效性判定。结果:家兔分别口服银杏叶滴丸剂及片剂后GA,GB,GC及BB均符合一房室模型。口服滴丸剂后GA,GB,GC及BB相对于口服片剂的生物利用度分别为104%,109%,112%和110%。2种制剂的药动学参数无显著差异。结论:银杏叶滴丸剂和对照剂型银杏叶片剂生物等效。AIM： To study the pharmacokinetics and bioequiavalence of Ginkgo biloba extract （GbE） dropping pills and tablets. METHODS： Ten rabbits enrolled were randomly divided into 2 groups. Group A first received orally single dose of the trial preparation GbE dropping pills, and then followed by the reference preparation GbE tablets in the same way, while group B received contrarily the reference preparation first, and followed by the trial preparation. Serum concentrations of ginkgolide A （GA）, ginkgolide B （GB）, ginkgolide C （GC）, and bilobalide （BB） were quantitatively measured by liquid chromatography/mass spectrometry using negative chemical ionization, by applying a very sensitive method which allowed serum concentrations as low as 20 μg·L^-1 for each compound （except 10 μg·L^-1 for GC） to be measured. The pharmacokinetic program of 3P97 was carried out to calculate the pharmacokinetic parametes of GA, GB, GC, and BB. ANOVA was utilized to check the differences of the means of the pharmacokinetic parameters between the two preparations. The pharmacokinetic parameters of AUC0-12, tmax, and cmax were used to determine bioequiavalence of GbE dropping pills and tablets by two one-sided t-tests. RESULTS： The dispositions of GA, GB, GC, and BB were conformed to onecompartment model in rabbits after orally administering GbE dropping pills and tablets. The relative bioavailabiliting of GA, GB, GC, and BB in GbE dropping pills vs tablets were 104 %, 109 %, 112 %, and 110 %, respectively. No significant differences were found among the main pharmacokinetic parameters. CONCLUSION： The GbE dropping pills are bioequivalent to GbE tablets.

关 键 词：二裂银杏 片剂 药动学 色谱法 高压液相 光谱法 质量 电喷雾电离 生物等效性 银杏内酯 白果内酯 滴丸剂 

分 类 号：R283.69[医药卫生—中药学] R945[医药卫生—中医学]