类黄酮的最新研究进展(Ⅲ)--吸收、代谢以及排泄

综述了不同类黄酮化合物的吸收、代谢以及生物效价的最新进展,包括黄烷酮、查尔酮以及二氢查尔酮、黄酮醇、黄酮以及黄烷醇。     

CONTINUOUS FERMENTATION OF GLUCOSE SOLUTIONS

Use of a continuous-flow plug fermentor to ferment glucose solutions was found to be possible only with unrefined commercial glucose and not with pure glucose. Even when the former was used problems were encountered due to a gradual increase in back pressure across the yeast bed. With the commencement of glucose metabolism in the yeast bed, ‘shock’ excretion of potassium and magnesium ions as well as of low molecular weight nitrogenous material was observed. The product from the fermentor contained an abnormally high level of α-diketones viz., 1–3 mg/litre.     

吸入铀化合物的内照射剂量估算

本文研究了单次吸入和连续均匀吸入铀化合物时,肺负荷、体负荷及尿铀排出速率与吸入量的关系。结果表明:(1)对于单次吸入,吸入物质从呼吸系统近乎全部清除的时间,对 D 类约为10天,W 类约为3年。吸入的 Y 类物质,一部分可能长期留在肺淋巴结内,肺负荷最终将趋于恒定。(2)连续均匀吸入铀化合物一段时间后,赖于化合物的吸入分类及吸入物质的 AMAD,肺负荷和尿铀排出速率将分别达到某个平衡值。(3)对于 D 类化合物的上述两种吸入类型以及连续均匀吸入 W 类化合物一年后,体负荷和尿铀排出速率与吸入物质的 AMAD 关系不大。(4)连续均匀吸入各种 AMAD 的 D,W 类化合物一段时间后,体负荷与吸入时间的关系可用幂函数表示。最后,讨论了吸入铀化合物的内照射剂量的估算方法。     

肾-膀胱排泄的剂量学模型

计算有效剂量时，膀胱有0．05的组织权重因子值，为计算摄入放射性物质对膀胱壁产生的当量剂量，需要放射性物质经肾－膀胱排泄的剂量学模型，ICRP53号出版物给出了该模型的数学表达式。不过，这些表达式只适用于能从体液直接经尿排泄的物质，本文导出了摄入放射性物质 经体内若干器官，组织依次转移然后经尿排出时，其在肾尿路，膀胱内容物中衰变数的计算式，并以吸入99mTc标记的DTPA气溶胶为例，说明计算式的实际应用。     

氚污染工作人员体内氚排出规律的观察

本文报告了由观察体内受到氚污染的工作人员而得到的氚代谢资料。主要介绍了氚以氧化氚形式入体后尿氚排泄的方程式和体内氧化氚的半排期。文中采用二区间代谢模式对氧化氚入体后的代谢动态作了分析。     

锕系元素钚、镅、镎年龄相关的生物动力学模式

本文根据ＩＣＲＰ６７号出版物提出的关于锕系元素年龄相关的生物动力学模式及相应的基本参数，说明涉及锕系元素钚、镅、镎年龄相关的代谢参数值导出过程，以便加深对现行模式的理解，进一步了解相关参数值其间的纵横联系。     

Pharmacokinetic, tissue distribution, and excretion of puerarin and puerarin-phospholipid complex in rats

Puerarin is a potential therapeutic agent for cardiovascular diseases. But its poor oral bioavailability restricts its clinical application. In present study, as an evaluation of a formulation to improve the bioavailability of the drug, puerarin and its phospholipid complex were given to rats by intragastrically (i.g.) administration to compare pharmacokinetic, tissue distribution, and excretion. Serum samples were obtained at designated times after a single oral dose of 400 mg/kg puerarin or its complex. Tissue samples (heart, liver, spleen, kidney, lung, and brain), urine, and feces were collected and analyzed by a sensitive and specific high performance liquid chromatography (HPLC) method after i.g. administration of puerarin or its phospholipid complex. Compartmental and non-compartmental analyses were applied to the serum concentration versus time data. Pharmacokinetic parameters were calculated using the 3P97 pharmacokinetic software package. An open two-compartment, first-order model was selected for pharmacokinetic modeling. The results showed that after i.g. administration of 400 mg/kg puerarin and its phospholipid complex (equivalent to 400 mg/kg of puerarin), the pharmacokinetic parameters of the two formulations were different. The serum concentrations reached peaks at 0.894 ± 0.521 h and 0.435 ± 0.261 h, respectively, indicating the complex was more readily absorbed in serum than puerarin. The maximum concentrations for puerarin and its complex were 1.367 ± 0.586 mg·L^-1 and 2.202 ± 1.28 mg·L^-1 and AUC were 5.779 ± 1.662 mg·h. L^-1 and 8.456 ± 0.44 mg·h L^-1, respectively, indicating a higher bioavailability for the complex. The widely distribution characteristics of puerarin and its complex in tissues post-i.g. administration was identical and in a descending order as follows: lung, kidney, liver, heart, spleen, and brain. However, the amount was different. Puerarin distribution was higher in heart, lung, and brain after administering the complex. The cumulative 72 h urinary excretion of puerarin after i.g. administration of puerarin and its complex accounted for 1.05%, 1.11% of the administered dose, respectively. The cumulative feces excretion of puerarin was 32.3% and 25.5%. To sum up, oral administration of puerarin phospholipid complex modified the pharmacokinetics and tissue distribution of puerarin and it could be an effective oral formulation for puerarin.     

五例内污染者~(137)Cs的滞留和排泄

在一次意外事件中,五人(例Z、C、Y、Q 和 W)摄入了~(137)Cs 放射性物质。在摄入后的15至290天期间,用全身计数器进行了活体测量和尿、粪排泄物的γ谱分析。活体测量结果表明,在自然排泄期这五例的有效半减期分别为124、54、61、36和36d。在促排期间,滞留规律仍可用单指数函数来描述,他们的有效半减期分别为38、39、25、17和16d。这五例的约定剂量当量估算结果分别为4、3、4、3和11mSv。尿、粪排泄物分析与活体测量所得的结果在合理的误差范围内是一致的。自然排泄期的尿排泄分数(?)_u=0.75,促排期间的尿排泄分数(?)_(?)=0.24。