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机构地区:[1]兰州大学生命学院,甘肃兰州730000 [2]华侨大学教育部分子药物研究中心,福建泉州362021 [3]甘肃省中医学院动物实验中心,甘肃兰州730030
出 处:《药学学报》2010年第10期1279-1284,共6页Acta Pharmaceutica Sinica
基 金:甘肃省科技攻关项目(2GS064-A43-019-02);教育部科学基金107108资助;福建省自然科学基金(2008J0102);泉州市基金项目(2008Z21)资助;华侨大学人才引进启动项目(BS105)
摘 要:以砷酸(ATO)为对照,研究雄黄微生物溶解液(RBS)的药物动力学行为,探索雄黄溶解后,其中砷在大鼠体内吸收和分布的变化规律。以砷酸(腹腔注射,含砷量0.3mg·kg?1)为对照组,雄黄微生物溶解液(腹腔注射,含砷量0.3mg·kg?1)为给药组,测定药物中砷在大鼠血液中的浓度及在心、肝、脾、肺、肾和脑等组织中的浓度,并研究药代动力学参数的变化。RBS组药代动力学参数与ATO组接近,其中砷在大鼠各组织中蓄积量大幅度降低,与对照组相比具有显著差异。雄黄经生物溶解后,以无机砷或有机砷的形式存在,与对照组相比,砷的形态成分发生明显变化,药物生物利用度明显提高,砷在组织中几乎没有蓄积。这一结果可能为微生物技术在研究、开发雄黄的应用提供有力依据。The paper is to report the preparation of realgar bioleaching solution (RBS) by bacteria and the comparison of pharmacokinetics of RBS and H3AsO3 (ATO), and the study of its possible change of absorption and distribution of soluble arsenic in rat. The experiment was carried out on Wistar rats given peritoneal injection of RBS at a dose of 0.3 mg·kg^-1 (soluble arsenic content, 0.3 mg·kg^-1), and rats given ATO at the dose of 0.3 mg·kg^-1 (soluble arsenic content, 0.3 mg·kg^-1). The arsenic concentrations in many tissues including heart, liver, spleen, lung, renal and brain were determined. The changes of pharmacokinetic parameters and arsenic distribution in different tissues were detected and compared in these two groups of rats. The pharmacokinetic parameters of RBS and ATO are very similar. There is very few distribution of arsenic in the tissues in RBS group, compared with the ATO group. There is significant difference in the content of arsenic between two groups statistically (P 〈 0.01). It is feasible that we select the bacteria bioleaching solution as a candidate drug, which may be employed for primary change of arsenic compounds including dissolved inorganic arsenic and organic arsenic, in order to improve bioavailability and decrease the amount of arsenic accumulation in animal tissues. In addition, there is significant difference in the change of arsenic compounds between two groups. It can be concluded that, the investigation on application of microbial technology may provide a basis for exploratory research of realgar.
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