Pharmacokinetic disposition of triclabendazole in cattle and sheep; discrimination of the order and the rate of the absorption process of its active metabolite triclabendazole sulfoxide

A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep. A commercial suspension of TCBZ (Biofasiolex, Biogénesis S.A., Argentina) was administered at a dose rate of 10 mg/kg by the oral route to six Holstein female calves and six Corriedale female sheep. The plasma concentration profiles of the metabolites triclabendazole sulfoxide (TCBZ-SO) and triclabendazole sulfone (TCBZ-SO₂) were analysed by means of the non-compartmental method. The order of the absorption process of the active metabolite, TCBZ-SO, was determined by construction of curves of cumulative absorbed fraction of the drug by means of the Wagner-Nelson method. The appearance of TCBZ-SO in plasma of cattle and sheep resembles the entry of a constant quantity of drug into the organism per unit time. This is explained by the reservoir effect of the rumen, which acts as a biological slow-release system for TCBZ-SO and its precursor TCBZ to the posterior digestive tract where they are absorbed. The plasma concentration profiles of TCBZ-SO in both species were well described by a one-compartment open model with zero-order process of absorption and first-order process of elimination. The values of AUC_0-∞ and C _max of TCBZ-SO did not differ between species, while other kinetic parameters except for λ _z had higher values in calves than in sheep. In the case of TCBZ-SO₂, t _max was the only parameter that did not differ between species, while other kinetic parameters except for λ _z had higher values in calves than in sheep.     

外源氯对番茄幼苗生长及养分吸收、利用的影响

 研究了不同水平外源氯处理对番茄(Lycopersicon esculentum L. ) 干物质积累、叶绿素含量、Cl^- 、NO₃^- 、氮、磷、钾、钙和镁含量的影响。结果表明: 一定范围( 6.25～100 nmol·L ^{- 1} ) 的外源氯处理, 不降低番茄生物量甚至促进生物量, 并可明显提高番茄幼苗对钾、镁、磷的吸收和氮素利用效率, 而200、300 mmol·L ^{- 1} Cl^- 处理的幼苗干物质积累极显著下降。     

A nonlinear, dynamic, simulation model for transport, and whole plant allocation of systemic xenobiotics following foliar application. IV: Physicochemical properties requirements for optimum absorption and translocation

The relationship between the physicochemical properties (molar volume, partition coefficient, and dissociation constant) of slow-acting systemic postemergence xenobiotics and their uptake and translocation to the sites of action was investigated using the nonlinear, dynamic simulation model ERMESSE. When the pK_a was held constant at 4.0, the model enables the prediction of the uptake of a systemic xenobiotic as a function of its partition coefficient and molar volume. The model also considered the effects of the physicochemical properties of a systemic xenobiotic on its long-distance translocation within the vascular tissues. For instance, when the log K_ow and pK_a were held constant at 1.5 and 6.0, respectively, the model predicted a higher translocation rate (55%) for molecules with a small (e.g., MV = 100 cm³ mol⁻¹) as opposed to a large (e.g., MV = 300 cm³ mol⁻¹, 33%) molar volume. In addition, the theoretical predictions from the ERMESSE model showed that any xenobiotic with a molar volume not exceeding 300 cm³ mol⁻¹ could provide an uptake ?50% and a translocation rate ?25% when its log K_ow is between −0.5 and 2.5 and its pK_a is between 0.0 and 8.0.     

Caco-2细胞模型及其在营养素小肠吸收机理研究中的应用

Caco-2细胞源自人结肠癌细胞,体外培养时能自发地进行类似肠道细胞的形态学和生化学上的分化,获得许多小肠吸收细胞的特性,如形成微绒毛结构;在细胞表面形成良好的刷状缘;在细胞间形成紧密连接;分泌水解酶以及合成转运糖、氨基酸和药物等的载体转运系统。由培养在微孔滤膜上的Caco-2细胞构建的模型为研究营养素在小肠的吸收机理提供了一个有效且易于操作的实验手段。本文主要综述了Caco-2细胞模型的建立、特征、检测及其在氨基酸、维生素、核苷和微量元素等营养素小肠吸收机理研究中的应用。     

Creep feed intake during lactation enhances net absorption in the small intestine after weaning

The aim of the study was to measure the effect of creep feeding during lactation on net absorption in the small intestine at 4 days after weaning. Intermittent suckling was used to increase creep feed intake during lactation. Creep feed containing chromic oxide was provided. Based on the colour of the faeces, piglets were classified as ‘eaters’ or ‘non-eaters’, respectively. At day 4 after weaning, an in vivo small intestine segment perfusion test was performed at 5 sites along the small intestine in 24 piglets (12 eaters and 12 non-eaters). At both sides of each intestinal segment a tube was fitted to perfuse and drain fluid in order to assess net absorption. Net absorption was higher in eaters than in non-eaters (P < 0.001). Net absorption varied greatly between and within piglets and was highest in the caudal segments of the small intestine (P < 0.001). These data suggest that creep feeding could be a useful tool in the prevention of post-weaning diarrhoea.     

白菜不同品种对硝酸盐吸收积累差异原因初探

 用两组积累硝酸盐不同的白菜品种作试材，测定其吸收硝酸盐的速率、动力学常数Km与V一、硝酸还原代谢库内硝酸根浓度(MPS)和硝酸还原酶活性(NRA)，结果表明，不同白菜品种吸收硝酸根的速率、Km与V 、MPS、NRA存在较大的差异；硝酸盐积累的差异主要是由于吸收硝酸根的速率不同，与硝酸根在其体内的运转、代谢并无显著直接相关。     

蔓生和矮生长豇豆氮磷钾吸收特性

研究了蔓生和矮生长豇豆的氮磷钾吸收特性。结果表明 ,两类长豇豆对氮磷钾的吸收 ,均以氮最多 ,钾次之 ,磷最少。蔓生类型的吸收比例为 2 .75～ 2 .92∶1∶2 .15～ 2 .75,矮生类型为4 .4 9∶1∶4 .2 1。蔓生类型比矮生类型的吸收量大 ,蔓生类型中白豆角比青豆角稍大。蔓生长豇豆营养生长期的吸收量微少 ,生殖生长期约占总吸收量的 98%。豆荚利用的氮磷钾逐渐增加 ,至结荚后期利用了氮磷的 6 5%～ 70 % ,钾的近 4 0 %。矮生长豇豆在营养生长期的吸收量约占 2 0 % ,生殖生长期约占 80 % ,豆荚只利用氮磷的 35%～ 4 0 %和钾的 30 %左右。     

^3H—BA不同溶解法对脐橙果实吸收^3H—BA的影响

＾３Ｈ－ＢＡ分别采用普通热酒精溶解法,加ＰＴ３９助溶剂的改进溶解法配成＾３Ｈ－ＢＡ＋ＧＡ３,于“清家”脐橙第一次重量落果高峰前涂果,改进溶解法使脐橙幼果在２４小时吸收＾３Ｈ－ＢＡ达２２３８８ｄｐｍ,果内＾３Ｈ－ＢＡ浓度达０．８８×１０＾－６,而普通热酒精溶解法仅分别为１２８９０ｄｍｐ和０．４５×１０＾－６,无论采用哪种方法溶解＾３Ｈ－ＢＡ脐橙幼果对＾３Ｈ－ＢＡ的吸收速度都是果后２４小时内最快,此后     

6-BA在葡萄植株体内的运转和分配

以葡萄为试材,研究了葡萄根、茎、叶、果等器官对6-苄基腺嘌呤(6-BA)的吸收及它在植株内的运转和分配。结果表明,对1年生葡萄幼苗茎部引入或叶片涂抹6-BA,1h后,在植株所有部位都有分布,其中以茎尖和根部浓度较高,表现为快速、非极性的运输特性。茎部引入5d之内,植株根内6-BA呈持续升高趋势,茎尖内6-BA虽然有波动,但是最后仍达到最大;而叶片涂抹则在涂抹后5h时,全株各部位6-BA浓度达到最大,5d后,除引入叶片外,其它部位几乎测不到6-BA。盛花后30d,果穗浸蘸和穗轴引入6-BA,2h后,果皮、果肉、种子中6-BA浓度达到高峰,以后逐渐下降,果穗浸蘸30d后,果实各部位均已测不到6-BA,穗轴引入30d后,果皮和果肉内仍能测到6-BA,但种子内已测不到。     

不同世代脱毒马铃薯氮磷钾吸收规律的研究

对不同世代脱毒马铃薯不同生长时期的氮、磷、钾吸收量及吸收速率的测定,结果表明,不同世代脱毒马铃薯对氮磷钾的吸收量显著不同,全生育期内以原种对氮磷钾的吸收量最大,商品薯的吸收量最小,原原种、生产种居中。不同世代脱毒马铃薯在幼苗期对氮磷钾的吸收速率差异较小,但在发棵期和块茎膨大期商品薯对氮、磷、钾的吸收速率显著低于其它3个处理,在块茎膨大期其吸收速率分别比原种降低了47.5%、45.8%和44.5%。而原原种、原种和生产种3个处理间在全生育期内差异不显著。