Yakasai I A
Department of Pharmaceutical and Medicinal Chemistry, Ahmadu Bello University, Zaria, Nigeria.
Eur J Drug Metab Pharmacokinet. 2003 Apr-Jun;28(2):93-9. doi: 10.1007/BF03190495.
The influence of sodium/potassium salt water extract incorporated in a traditional meal on the bioavailability of Ibuprofen tablets 400mg dose was studied in 6 healthy human volunteers. There was a statistically significant decrease in the plasma levels of ibuprofen, and its metabolites, hydroxy-ibuprofen and carboxy-ibuprofen, respectively, when the meal containing sodium/potassium salt extract was administered with the ibuprofen tablets than when taken under fasting state or with the meal without the fruit extract. The Cmax, AUC0-6hr and Ka for ibuprofen decreased from 38.04 +/- 0.70microg/ml to 20.06 +/- 1.21microg/ml (p<0.05); 28.030 +/- 2.40microg/ml.hr to 14.180 +/- 1.12microg/ml.hr (p<0.05) and 1.048 +/- 0.02hr(-1) to 0.602 +/- 0.03hr(-1). Similarly, the Cmax for hydroxy-ibuprofen and carboxy-ibuprofen decreases from 43.04 +/- 0.76microg/ml to 27.21 +/- 0.24microg/ml (p<0.05) and 48 +/- 0.71microg/ml to 31.08 +/- 0.12microg/ml (p<0.05) respectively; while AUC0-6hr for hydroxy-ibuprofen decreased from 34.120 +/- 0.49microg/ml.hr to 16.410 +/- 0.27microg/ml.hr while that of carboxy-ibuprofen decreased from 36.121 +/- 1.97microg/ml.hr to 19.278 +/- 0.92microg/ml.hr respectively. The Kel for hydroxy-ibuprofen increased from 0.71 +/- 0.94 hr(-1) to 0.81 +/- 0.21 hr(-1) (p<0.05) respectively. The study has indicated that sodium/potassium salt extract significantly decreased the bioavailability of ibuprofen.
在6名健康人类志愿者中研究了传统餐食中加入钠/钾盐水提取物对400毫克剂量布洛芬片剂生物利用度的影响。与在禁食状态下服用或与不含水果提取物的餐食一起服用布洛芬片剂相比,当含有钠/钾盐提取物的餐食与布洛芬片剂一起服用时,布洛芬及其代谢物羟基布洛芬和羧基布洛芬的血浆水平分别有统计学意义的下降。布洛芬的Cmax、AUC0 - 6hr和Ka分别从38.04±0.70微克/毫升降至20.06±1.21微克/毫升(p<0.05);从28.030±2.40微克/毫升·小时降至14.180±1.12微克/毫升·小时(p<0.05)以及从1.048±0.02小时-1降至0.602±0.03小时-1。同样,羟基布洛芬和羧基布洛芬的Cmax分别从43.04±0.76微克/毫升降至27.21±0.24微克/毫升(p<0.05)和从48±0.71微克/毫升降至31.08±0.12微克/毫升(p<0.05);而羟基布洛芬的AUC0 - 6hr从34.120±0.49微克/毫升·小时降至16.410±0.27微克/毫升·小时,羧基布洛芬的AUC0 - 6hr则分别从36.121±1.97微克/毫升·小时降至19.278±0.92微克/毫升·小时。羟基布洛芬的Kel分别从0.71±0.94小时-1升至0.81±0.21小时-1(p<0.05)。该研究表明,钠/钾盐提取物显著降低了布洛芬的生物利用度。