Gallicano Keith, Foster Brian, Choudhri Shurjeel
Clinical Investigation Unit, The Ottawa Hospital-General Campus, Health Canada, Ottawa, Ontario, Canada.
Br J Clin Pharmacol. 2003 Feb;55(2):199-202. doi: 10.1046/j.1365-2125.2003.01736.x.
To evaluate the effect of acute dosing of garlic supplements on the single-dose pharmacokinetics of ritonavir.
Ten healthy volunteers (five male, five female) were equally randomized in a crossover design to receive 400 mg of a single dose of ritonavir within 10 min after eating breakfast either alone or with 10 mg of Natural Source Odourless Garlic. They received a total of eight doses of garlic extract (2 x 5 mg capsules) taken twice daily for 4 days. Ritonavir and the seventh garlic dose were administered simultaneously.
Coadministration of garlic nonsignificantly decreased area under the plasma concentration-time curve (AUC(0, infinity )) by -17% (90% confidence interval (CI), -31% to 0%; range -46% to 68%) and peak plasma concentration of ritonavir by -1% (90% CI, -25% to 31%; range -51% to 136%).
Acute dosing of the garlic capsules over 4 days did not significantly alter the single-dose pharmacokinetics of ritonavir in healthy volunteers. Given the complex effects of both ritonavir and garlic on drug metabolism, the results of our study should not be extrapolated to steady-state conditions, where the possibility of an interaction still needs to be evaluated.
评估急性服用大蒜补充剂对利托那韦单剂量药代动力学的影响。
10名健康志愿者（5名男性，5名女性）采用交叉设计平均随机分组，在早餐后10分钟内单独或与10毫克天然无臭大蒜一起服用400毫克单剂量利托那韦。他们总共服用8剂大蒜提取物（2×5毫克胶囊），每天服用两次，共4天。同时给予利托那韦和第七剂大蒜。
大蒜与利托那韦合用时，血浆浓度-时间曲线下面积（AUC(0,∞)）非显著性降低17%（90%置信区间（CI），-31%至0%；范围-46%至68%），利托那韦的血浆峰浓度非显著性降低1%（90%CI，-25%至31%；范围-51%至136%）。
在4天内急性服用大蒜胶囊未显著改变健康志愿者中利托那韦的单剂量药代动力学。鉴于利托那韦和大蒜对药物代谢的复杂影响，我们研究的结果不应外推至稳态情况，在稳态情况下相互作用的可能性仍需评估。
