Bouraoui A, Toumi A, Ben Mustapha H, Brazier J L
Unit of Pharmacology Faculty of Pharmacy, Monastir, Tunisia.
Drug Nutr Interact. 1988;5(4):345-50.
Absorption and bioavailability of theophylline from a sustained-release gelatin capsule were investigated in 10 male rabbits after oral administration (20 mg/kg), with and without a ground capsicum fruit suspension. Comparison of pharmacokinetic parameters showed that the concomitant absorption of capsicum increases areas under plasma curves (from 86.06 +/- 9.78 mg H/liter to 138.32 +/- 17.27 mg H/liter, P less than 0.001), peak plasma levels (from 6.65 +/- 0.76 to 8.78 +/- 0.98 mg/liter, P less than 0.01), and mean residence times (from 14.94 +/- 2.97 to 20.98 +/- 5.75 H, P less than 0.001). A second administration of the capsicum suspension, 11 hours after dosing, produced a new rise of theophylline plasma levels in every rabbit. The variations in pharmacokinetic and bioavailability parameters are discussed in accordance with the mechanisms of action of capsaicin, an active compound present in capsicum fruit.
在10只雄性兔子口服(20毫克/千克)茶碱后,研究了含辣椒素悬浮液和不含辣椒素悬浮液时,缓释明胶胶囊中茶碱的吸收及生物利用度。药代动力学参数比较显示,同时服用辣椒素会增加血浆曲线下面积(从86.06±9.78毫克·时/升增至138.32±17.27毫克·时/升,P<0.001)、血浆峰值水平(从6.65±0.76毫克/升增至8.78±0.98毫克/升,P<0.01)和平均驻留时间(从14.94±2.97小时增至20.98±5.75小时,P<0.001)。给药11小时后再次给予辣椒素悬浮液,每只兔子的茶碱血浆水平均再次升高。根据辣椒果实中活性化合物辣椒素的作用机制,对药代动力学和生物利用度参数的变化进行了讨论。