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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。
Objective To study the effects of pH adjusting agent on the bioavailability of breviscapine (the main active ingredient is scutellarin) in rats. Methods HPLC method was used to determine the concentration of baicalin in rat plasma. Rats under the following three kinds of programs gavage breviscapine 40 mg · kg -1 (with scutellarin dollars): (A) without pH regulator Breviscapine suspension; (B) pre-irrigation pH 6.2 sodium bicarbonate-citrate buffer, administration of a Breviscapine suspension without pH adjuster; (C) Breviscapine suspension pH-adjusted to pH 6.2 with sodium bicarbonate-citrate buffer , Gavage. The results of the program A as a reference, the relative bioavailability of programs B and C were 183.1% and 162.4%. The differences of AUC_ (0 → t) between B and C were not statistically significant. There was a 1 to 2 h delay in absorption when administered with protocol A, whereas the drug was rapidly absorbed with solutions B and C. The solubility-pH curve shows that baicalin is poorly soluble under acidic conditions and its solubility increases with increasing pH. Conclusion pH value is an important factor affecting the oral absorption of baicalin. Pre-irrigation or co-administration of pH adjusting agent to increase the pH value of gastric juice can increase the solubility of baicalin in the upper gastrointestinal tract, thus increasing the rate and extent of absorption , So that significantly reduced time lag, bioavailability significantly increased.