葡萄内酯在大鼠体内的组织分布

Tissue Distribution of Auraptene in Rats

目的:探讨葡萄内酯软胶囊中药物在大鼠体内的组织分布情况。方法:采用大鼠灌胃给药法,依据大鼠灌胃给药后药物浓度-时间曲线,确定大鼠注射给药后于4个时间点依次采取组织样品,取各空白组织匀浆液,建立各组织中药物的标准曲线,计算该组织样品中葡萄内酯的含量,同时制备高、中、低浓度双样本质控(QC)样品,用以判断该批样品结果的可靠性。数据采用Analyst 1.6软件分析。结果:大鼠按100 mg·kg^(-1)灌胃给药后,大鼠灌胃给药30 min时,葡萄内酯在心、肝、脾、肺、肾、胃、小肠和肌肉中浓度达峰值。服药120 min时,小肠中葡萄内酯显著减少,脂肪和血液中药物浓度增加较为明显。6 h时除脑外,各脏器药物浓度均大幅度下降,小肠中药物浓度最高。8 h时各主要脏器药物浓度已显著降低。结论:灌胃葡萄内酯软胶囊内容物后能快速分布于大鼠各主要组织中,其中胃肠道的药物浓度一直较高,其他组织以肝脏、肺中药物浓度较高。脑组织中药物浓度一直维持在较高水平,这可能与葡萄内酯软胶囊对老年痴呆的活性靶向性存在一定的相关性。

Objective： To investigate tissue distribution of auraptene in rats. Method： Rat intragastric administration method was used. The content of auraptene in tissue sample was calculated after determining four time points with intragastric administration and taking tissue samples successively by establish a standard curve for drugs in various tissues. Meanwhile, two sample quality control（ QC） sample with high, medium and low concentrations were done for judging reliability of results of this batch of samples. Data were analyzed by Analyst1. 6 software. Result： With gastric administration by 100 mg·kg-1,auraptene was rapidly distributed in different tissues including heart,liver,spleen,lung,kidney,stomach,small intestine and muscle after 30 min. The concentration of auraptene in small intestine significantly decreased by 120 min,while drug concentrations in fat and blood mainly increased. The concentration of drug for other issues beside brain by 6 h were dropped greatly and then drug concentration of all main issues decreased significantly at 8 h. Conclusion： Auraptene soft capsule can be rapidly distributed in main tissues of rats after gastric administration,drug concentration in gastrointestinal tract is always high, its concentrations in liver and lung are higher than other tissues. In addition, the concentration of auraptene in brain tissue remains at a high level, which may be related to active targeting of auraptene soft capsule on senile dementia.