Pharmacokinetics of Amoxicillin Trihydrate in Desert Sheep and Nubian Goats

The pharmacokinetics of amoxicillin were studied in five Desert sheep and five Nubian goats after intravenous (i.v.) or intramuscular (i.m.) administration of a single dose of 10 mg/kg body weight. Following i.v. injection, the plasma concentration-versus-time data were best described by a two-compartment open model. The kinetic variables were similar in both species except for the volume of the central compartment (V_c), which was larger in sheep (p<0.05). Following i.m. injection, except for the longer half-life time of absorption in goats (p<0.05), there were no significant differences in other pharmacokinetic parameters between sheep and goats. The route of amoxicillin administration had no significant effect on the terminal elimination half-life in either species. The bioavailability of the drug (F) after i.m. administration was high (>0.90) in both species. These results indicate that the pharmacokinetics of amoxicillin did not differ between sheep and goats; furthermore, because of the high availability and short half-life of absorption, the i.m. route gives similar results to the i.v. route. Therefore, identical intramuscular and intravenous dose regimens should be applicable to both species.     

Factors Influencing the Bioavailability of Peroral Formulations of Drugs for Dogs

The oral route is presently the preferred route of drug delivery. Poor oral bioavailability results in variable concentrations of drugs in the plasma and variable pharmacological responses, in addition to higher product costs. The unique canine physiology, anatomy and biochemistry makes designing canine dosage forms a challenging exercise. This article reviews the physicochemical, physiological, pharmacokinetic, pharmacological and formulation factors that can influence the drug availability of the oral formulations in dogs in an effort to provide a source of data to aid development of canine drug products with superior bioavailability.     

Disposition Kinetics,Bioavailability and Renal Clearance of Cefepime in Calves

The pharmacokinetics of cefepime were studied following intravenous and intramuscular administration of 6.5 mg/kg in four female Friesian calves. Following single intravenous administration, the serum concentration-time curves of cefepime were best fitted using a two-compartment open model. The elimination half-life (t(1/2)beta) was 2.38+/-0.16 h, volume of distribution at steady state (Vdss) was 0.21 +/- 0.01 L/kg, and total body clearance (ClB) was 1.1 +/- 0.08 ml/min per kg. Following intramuscular administration, the drug was rapidly absorbed with an absorption half-life (t(1/2)ab) of 0.29+/-0.02 h; maximum serum concentration (Cmax) of 21.7 +/- 1.1 microg/ml was attained after (Tmax) 1.1 +/- 0.08 h; and the drug was eliminated with an elimination half-life (t(1/2)el) of 3.02 +/- 0.18 h. The systemic bioavailability (F) after intramuscular administration of cefepime in calves was 95.7% +/- 7.44%. The in vitro serum protein-binding tendency was 10.5-16.7%. Following administration by both routes, the drug was excreted in high concentrations in urine for 24 h post administration.     

土壤/沉积物中微量重金属的化学萃取方法研究进展

用化学萃取法，包括连续萃取法和单一萃取法，研究土壤 /沉积物中的微量重金属的活动性和生物可利用性是环境土壤化学领域内的热点问题之一。这里我们将对近年来该方法所取得的一些进展、存在的问题进行详细评述。     

恩诺沙星缓释溶液在猪体内的药物动力学及生物利用度

选用18头健康猪进行恩诺沙星普通溶液静脉注射、肌肉注射和恩诺沙星缓释溶液肌肉注射的药物动力学研究,比较了2种溶液在猪体内的药物动力学特征和生物利用度。结果表明:静脉注射给药的药时数据适合无吸收二室开放模型,主要药物动力学参数为t1/2α=0 726±0 164h,t1/2β=9 083±1 121h,Vd=4 364±0 565L/kg,ClB=0 336±0 053L/(kg·h),AUC=30 397±4 895mg·h/L。肌肉注射恩诺沙星缓释溶液和普通溶液的药时数据均符合一级吸收二室模型,其主要药物动力学参数分别为:t1/2ka=0 468±0 114h和t1/2α=0 415±0 195h;t1/2β=25 818±6 528h和t1/2β=9 460±2 946h(P<0 01);Tmax=1 498±0 194h和Tmax=1 347±0 393h;Cmax=2 206±0 555μg/mL和Cmax=2 561±0 152μg/mL;AUC=23 715±3 528mg·h/L和AUC=18 397±1 808mg·h/L(P<0 01);F=(78 02±11 61)%和F=(60 52±5 95)%。肌肉注射恩诺沙星缓释溶液和普通溶液的主要药物动力学参数t1/2β和AUC有显著性差异,其他指标均无显著性差异。恩诺沙星缓释溶液既有速释部分(与普通溶液相比吸收半衰期不变),又有缓释部分(消除半衰期延长),应用于临床其有速效和长效双重作用。     

土壤重金属污染的形态分析及生物有效性探讨

 土壤重金属污染已成为人们关注的全球性的环境问题之一,重金属生物有效性已成为污染生态学研究的前沿,污染土壤中重金属形态分析是土壤修复的关键所在。阐述了土壤重金属污染形态分析的研究进展,并对影响生物有效性的主要因素以及土壤重金属污染存在的问题进行了分析探讨,并指出了存在的问题和以后发展的方向,从而为重金属污染土壤经济、有效的修复提供理论依据。     

司帕沙星在E.coli-MG混合感染鸡的药动学与生物利用度研究

大肠杆菌-败血霉形体(Escherichia Coli.-Mycoplasma gallisepticu,E.coli-MG)疾病模型鸡单剂量(5mg.kg-1)内服和静注司帕沙星,研究其血液动力学特征和内服生物利用度。采用HPLC面积-内标法测定血浆中司帕沙星浓度,利用药动学分析软件MCPKP分析药-时数据。结果表明:疾病模型鸡内服司帕沙星血浆药-时数据符合一级吸收二室开放式模型,主要动力学参数如下:t1/2α1.7208h,t1/2β13.1773h,tm ax0.9083h,Cm ax0.6198μg.mL-1,AUC 3.8161mg.L-1.h-1。静注给药血浆中司帕沙星的经时数据符合无吸收二室开放式模型,主要动力学参数为:t1/2α0.4442h,t1/2β4.7557h,Kel0.5608h-1,Vd4.1204L.Kg-1,AUC 8.3274mg.L-1.h-1,C lB0.6004L.Kg-1.h-1。疾病模型鸡内服司帕沙星的生物利用度为47.03%。     

pH和有机质对土壤中镉和锌生物有效性影响研究*

 综述了土壤环境中重金属镉、锌生物有效性国内外研究态势，尤其是土壤pH、有机质和石灰对土壤中镉、锌生物有效性及镉、锌形态的影响机制。就目前研究状况，提出未来研究方向，为治理土壤镉、锌污染提供理论依据。     

河流底泥重金属不同形态的生物有效性

采用逐级连续化学浸提技术分析底泥重金属的形态 ,结合微生态系统生物暴露试验 ,通过线性回归的方法 ,评价了不同形态的生物有效性。结果表明 ,不同形态重金属的生物有效性 ,对不同吸收途径的生物是不同的。对于食腐屑的底栖动物而言 ,底泥Cu的水溶态、离子交换态、碳酸盐态、铁锰氧化态 ,Pb的水溶态 ,Mn的水溶态、离子交换态、有机 -部分硫化物态可被生物吸收利用 ;而底泥Cu的水溶态 ,Pb的水溶态对滤食性底栖动物具有生物有效性 ;底泥Cu的水溶态 ,Pb的水溶态 ,Zn的水溶态、离子交换态、碳酸盐态、有机 -部分硫化物态 ,Mn的水溶态、离子交换态、碳酸盐态、铁锰氧化物态对水生根系植物是有效的。     

1-site/2-pKa表面络合模型预测土壤中Cd2+的吸附及生物有效性

土壤中重金属的生物有效性与其在土壤中的吸附行为密切相关,本研究选取我国9个不同类型的非石灰性土壤,探究了Cd²⁺在土壤中的吸附过程。通过电位滴定获得土壤表面酸碱性质（pK_a1和pK_a2）,基于1-site/2-pK_a模型,使用ECOSAT和FIT拟合得到土壤与Cd²⁺的络合常数（lg K _{（SOCd⁺）}）,结果显示该模型能很好地描述Cd²⁺在土壤中的吸附过程。为了进一步探究土壤性质对Cd吸附固定的影响,通过逐步回归分析了pK_a1、pK_a2、lg K _{（SOCd⁺）}与土壤性质间的关系,发现土壤pH和CEC是pK_a1的主控因子,土壤pH同时也是pK_a2、lg K _{（SOCd⁺）}的主控因子。为了验证模型的可靠性,结合历史文献,基于土壤pH和CEC预测了历史文献中土壤表面酸碱性质和lg K _{（SOCd⁺）},利用得到的参数预测了Cd的吸附过程,发现预测值与实测值之间有很好的相关性,该模型能解释86%的变异。此外,利用回归模型得到的结合常数预测了历史文献中土壤溶液中的Cd含量,发现模型预测的Cd含量与蚯蚓体内Cd含量同样具有很好的相关性,能解释83%的变异。本研究基于Cd²⁺在不同性质土壤中的吸附行为,使用广义复合法建立的表面络合模型可以描述Cd²⁺在非石灰性土壤中的吸附与分配过程。