Gonzalez J P, Valdivieso A, Calvo R, Rodríguez-Sasiaín J M, Jimenez R, Aguirre C, du Souich P
Department of Pharmacology, Faculty of Medicine, University of the Basque Country, Vizcaya, Spain.
Eur J Clin Pharmacol. 1995;48(3-4):295-7. doi: 10.1007/BF00198315.
The effect of ascorbic acid on the availability of propranolol has been examined. After oral administration of propranolol 80 mg with or without ascorbic acid pretreatment (2 g), the plasma concentrations and urinary excretion of propranolol and its metabolites, 4-hydroxy-propranolol and propranolol-conjugated, were determined by HPLC. Compared to controls, vitamin C decreased the maximum concentration of propranolol from 463 to 334 nmol.l-1, and the area under the propranolol concentration-time curve (from 0 to 24 hours) from 3.13 to 1.96 mumol.l-1.h. The time to reach maximum propranolol concentration was increased from 1.9 to 2.7. The total amount of drug recovered in urine has also significantly diminished (from 12.6 to 4.29 mg). No change in elimination rate was observed, indicating that ascorbic acid had affected both the absorption process and the first pass metabolism. The heart-rate decreased less when propranolol was administered with ascorbic acid in comparison to control subjects, although this interaction has little biological importance.
已研究了抗坏血酸对普萘洛尔生物利用度的影响。口服80毫克普萘洛尔，同时给予或不给予抗坏血酸预处理（2克），通过高效液相色谱法测定普萘洛尔及其代谢产物4-羟基普萘洛尔和普萘洛尔结合物的血浆浓度及尿排泄量。与对照组相比，维生素C使普萘洛尔的最大浓度从463纳摩尔/升降至334纳摩尔/升，普萘洛尔浓度-时间曲线下面积（0至24小时）从3.13微摩尔/升·小时降至1.96微摩尔/升·小时。达到普萘洛尔最大浓度的时间从1.9小时增加到2.7小时。尿中回收的药物总量也显著减少（从12.6毫克降至4.29毫克）。未观察到消除率的变化，表明抗坏血酸对吸收过程和首过代谢均有影响。与对照组相比，普萘洛尔与抗坏血酸合用时心率下降幅度较小，尽管这种相互作用的生物学意义不大。
