pH调节剂对野黄芩苷大鼠相对生物利用度的影响(英文)  

Effect of pH regulators on the oral bioavailability of scutellarin in rats

作　　者：李玉平[1] 张利斌[1] 田非非[2] 翁伟宇[2] 

机构地区：[1]同济大学医学院附属上海市肺科医院药剂科,上海200433 [2]华东理工大学药学院,上海200237

出　　处：《中国临床药学杂志》2010年第6期329-333,共5页Chinese Journal of Clinical Pharmacy

摘　　要：目的研究pH调节剂对大鼠灌胃灯盏花素(主要活性成分为野黄芩苷)后生物利用度的影响。方法采用HPLCUV法测定大鼠血浆中野黄芩苷的浓度。大鼠按以下3种方案灌胃灯盏花素40 mg·kg^(-1)(以野黄芩苷计):(A)不加pH调节剂的灯盏花素混悬剂;(B)预灌pH 6.2碳酸氢钠-柠檬酸缓冲液后,给予不加pH调节剂的灯盏花素混悬剂;(C)灯盏花素混悬剂以碳酸氢钠-柠檬酸缓冲液调节pH值至6.2后,灌胃。结果以方案A为参比,方案B和C的相对生物利用度分别为183.1%与162.4%。方案B和C间的AUC_(0→t)差异无统计学意义。以方案A给药时吸收存在1～2 h的时滞,而以方案B和C给药时药物吸收迅速。溶解度-pH曲线表明,野黄芩苷在酸性条件下难溶,随着pH值升高,其溶解度增大。结论 pH值是影响野黄芩苷口服吸收的一个重要因素,预灌或共服pH调节剂以提高胃液的pH值,可以增加野黄芩苷在胃肠道上段的溶解度,从而增加吸收的速率与程度,使时滞明显缩短、生物利用度显著提高。A/M To evaluate the effect of pH regulators on the oral bioavailability of scutellarin in rats. METHODS The plasma concentration of scutellarin, the primary active ingredient in breviscapine, was determined by an HPLC-UV method. Rats received the following 3 treatment regimens at an oral dose of 40mg·kg- 1 （ calculated with reference to scutellarin） ： （A） breviscapine suspension without pH regulators; （B） pre-administration with sodium bicarbonate-citric acid buffer （pH 6.2）, then breviscapine suspension without pH regulators; （C） breviscapine suspension adjusted to pH 6.2 with sodium bicarbonate-citric acid buffer. RESULTS The relative bioavailability to treatment regimen A was 183.1% and 162.4% for treatment B and C, respectively. No significant difference in AUC0→1 between treatments regimen B and regimen C was observed. In treatment regimen A, about 1 - 2 h of lag time was observed for each rat, while scutellarin was absorbed rapidly and reached the first peak concentration within 15 min in treatment regimen B and regimen C. The profile of the solubility of scutellarin versus pH showed that scutellarin was poorly soluble at low pH and the solubility rose as the pH increased. CONCLUSION The pH value is an important influencing factor in absorption of scutellarin after oral administration. Pre-administration and co-administration of pH regulators to elevate gastric pH could increase the solubility of scutellarin, which result in shorter lag time and higher bioavailability in rats.

关 键 词：野黄芩苷 灯盏花素 生物利用度 PH调节剂 

分 类 号：R285.5[医药卫生—中药学]