Pedraz J L, Calvo B, Bortolotti A, Celardo A, Bonati M
Laboratory of Clinical Pharmacology, Instituto di Ricerche Farmacologiche Mario Negri, Milano, Italy.
J Pharm Pharmacol. 1989 Jun;41(6):415-7. doi: 10.1111/j.2042-7158.1989.tb06490.x.
The bioavailability of alpha-tocopherol acetate and alpha-tocopherol (vitamin E) was assessed in male rabbits given 50 mg kg-1 doses according to a randomized design. After intramuscular injection of alpha-tocopherol acetate in colloidal aqueous solution, a mean absolute bioavailability of 65% was calculated for the acetate and 35% for the physiologically active compound, alpha-tocopherol. Comparison of the kinetic profiles after intravenous and intramuscular administration of the acetate and intravenous injection of alpha-tocopherol, revealed absorption of alpha-tocopherol acetate from the site of injection and hydrolysis of the acetate to be potential limiting steps in the bioavailability of alpha-tocopherol. Intramuscularly injected alpha-tocopherol acetate in olive oil (the only formulation available in a few European countries) proved completely bio-unavailable. It thus appears necessary to re-assess the utility of current vitamin E supplementation, since the only formulations available offer poor bioavailability.
按照随机设计，对给予50毫克/千克剂量的雄性兔子评估了醋酸生育酚和生育酚（维生素E）的生物利用度。在肌肉注射胶体水溶液中的醋酸生育酚后，计算出醋酸盐的平均绝对生物利用度为65%，生理活性化合物生育酚为35%。比较醋酸盐静脉注射和肌肉注射以及生育酚静脉注射后的动力学曲线，发现醋酸生育酚从注射部位的吸收以及醋酸盐的水解是生育酚生物利用度的潜在限制步骤。在橄榄油中肌肉注射醋酸生育酚（少数欧洲国家可用的唯一制剂）被证明完全没有生物利用性。因此，由于现有的唯一制剂生物利用度差，似乎有必要重新评估当前维生素E补充剂的效用。
