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目的研究在大鼠体内甘草次酸对橙皮素血浆浓度及组织分布的影响。方法将72只SD大鼠,体质量150~210g,随机分成4组,即实验高浓度组与低浓度组,对照组的高浓度组与低浓度组。每组中又包括三个小组即3,4,4.4 h。高浓度实验组灌胃20 mg/kg橙皮素+50 mg/kg甘草次酸,低浓度实验组灌胃10 mg/kg橙皮素+50mg/kg甘草次酸。对照组只灌胃橙皮素,剂量与实验组相同。灌胃给药后分别于3 h、4 h和4.4 h用摘眼球取血法取血,接着大鼠被断头处死,取出组织。血浆在85℃水浴中,加盐酸水解120 min,然后以乙腈为萃取剂,超声波为辅助提取,组织匀浆液用乙腈提取,利用高效液相色谱测定血浆及组织中橙皮素的浓度。结果血浆和组织中橙皮素测定的线性范围分别是0.05~10μg/ml和0.05~5μg/g,检测限分别是血浆0.012μg/ml和肝、肾0.005 7μg/g,肺0.011μg/g。测定回收率在是91%~104%之间。结论大鼠口服橙皮素后在血浆未能检测到游离橙皮素;灌胃20 mg/kg橙皮素时,甘草次酸对其药代动力学有影响(P<0.05);灌胃后橙皮素在大鼠体内分布特征是肝>肾>肺。
Objective To study the effect of glycyrrhetinic acid on the plasma concentration and tissue distribution of hesperetin in rats. Methods Seventy-two SD rats weighing 150-210 g were randomly divided into four groups: experimental high-concentration group and low-concentration group, and high-concentration group and low-concentration group. Each group also includes three groups that 3,4,4.4 h. The high concentration of experimental group was fed with 20 mg / kg hesperetin + 50 mg / kg glycyrrhetinic acid, and the low concentration of experimental group was orally administered 10 mg / kg hesperetin + 50 mg / kg glycyrrhetinic acid. The control group was only administered with hesperetin in the same dosage as the experimental group. After intragastric administration, blood was taken from the eyeballs at 3 h, 4 h and 4.4 h, respectively, and then the rats were sacrificed and their tissues removed. The plasma was hydrolyzed with hydrochloric acid for 120 min at 85 ℃ in water bath. Then acetonitrile was used as extractant, and ultrasound was used as auxiliary extraction. The homogenate was extracted with acetonitrile and the concentration of hesperetin in plasma and tissue was determined by HPLC. Results The linear ranges of hesperetin in plasma and tissue were 0.05 ~ 10μg / ml and 0.05 ~ 5μg / g respectively. The limits of detection were 0.012μg / ml in plasma and 0.005μg / g in liver and 0.011μg / ml in lung respectively. The recovery rate was between 91% and 104%. Conclusions Free hesperetin can not be detected in plasma after oral administration of hesperetin in rats. When glycyrrhizin 20 mg / kg is administered orally, glycyrrhetinic acid has effects on pharmacokinetics (P <0.05) Hesperetin distribution in rats is characterized by liver> kidney> lung.