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将150μg1硝基芘(1NP)气管内或血管内给药后,对大鼠离体肺进行灌流,定时自灌流液中取样,以HPLC和GCMS测定并鉴定灌流液中未变的1NP及代谢物。经鉴定代谢物为单羟基硝基芘和二羟基硝基芘。两种途径给药后,1NP在灌流液中的浓度—时间数据符合一室药代动力学模型。预先以β萘黄酮,苯并蒽或苯巴比妥和β萘黄酮的混合物处理后的大鼠,肺灌流结果表明,显著降低1NP的平均保留时间(MRT),促进1NP的生物转化和气管给药后的吸收。以苯巴比妥预处理后的大鼠肺则对1NP的药代动力学参数无显著影响。
After intraperitoneal or intravascular administration of 150 μg of 1-nitropyrene (1NP), the isolated lungs of rats were perfused, and the samples were taken from the perfusate at regular intervals. The changes of perfusate in the perfusate were determined by HPLC and GCMS 1 NP and metabolites. The identified metabolites were monohydroxyl nitro pyrene and dihydroxy nitro pyrene. After the two routes of administration, the concentration-time data of 1-NP in the perfusate conformed to the one-compartment pharmacokinetic model. Pretreatment with β-naphthoflavone, benzanthracene or phenobarbital and β-naphthalene flavonoids in rats, pulmonary perfusion results showed that the mean retention time significantly reduced 1 NP (MRT), and promote 1 NP Biotransformation and absorption after tracheal administration. The rat lungs pretreated with phenobarbital had no significant effect on the pharmacokinetic parameters of 1-NP.