草鱼体内双氟沙星药代动力学研究

为研究双氟沙星（Difloxacin,DIF）在草鱼（Ctenopharynodon idellus）体内的药代动力学以及在各组织中的残留量,采用高效液相色谱法测定在15℃水温状态下单次给草鱼灌喂20 mg/kg剂量的双氟沙星后,得出双氟沙星在各组织以及血液中的药时曲线均都符合二室开放性模型,双氟沙星能够在草鱼体内快速吸收,并且血液及各组织中均有分布,双氟沙星在草鱼体内的药物动力学方程为C=5.056e-0.012t+19.041e-0.011t,其中双氟沙星在血液、肌肉、肝脏、肾脏中吸收半衰期（T_1/2α）分别为0.176h、0.562h、4.562h和1.477h,消除半衰期分别为（T_1/2β）69.492h、65.303h、218.412h和163.937h,总体消除率（CL）分别为0.495、11.181、10.789和7.102 L/（h·kg）,药时曲线下面积（AUC）分别为81.550、1277.55、807.470和1432.150 μg/（L·h）。根据相关规定肌肉中双氟沙星最大残留量300 μg/kg为标准,建议休药期26d以上。     

浸泡条件下孔雀石绿及其代谢物隐色孔雀石绿在斑点叉尾 组织中分布及消除规律研究

以7 mg/L的孔雀石绿浸泡斑点叉尾 苗种5min后将其饲养于池塘的网箱中, 研究了在养殖模式下孔雀石绿及其代谢物隐色孔雀石绿在斑点叉尾 苗种各组织中的分布及消除规律。采用高效液相色谱串联质谱法(HPLC-MS/MS)分析孔雀石绿及其代谢物隐色孔雀石绿在斑点叉尾 血液、肌肉、皮肤、肝脏、肾脏组织中的浓度水平。采用药代动力学分析软件3p97对血药浓度时间数据进行分析。结果表明, 孔雀石绿和隐色孔雀石绿血药浓度时间曲线符合有吸收二室模型, 动力学方程分别为: C孔雀石绿 =683.063 e-0.248 t+ 11.176 e-0.006 t- 694.239e-0.333 t, C隐色孔雀石绿 =757.240 e-0.222 t + 14.474 e-0.007 t 771.714 e-0.382 t。血液中孔雀石绿和隐色孔雀石绿达峰时间Tpeak分别为3.480和3.623h, 峰浓度值Cmax分别为81.560和159.619 ng/mL, 表观分布容积Vd/F分别为37.689和21.125 L/kg, 分布相的一级速率常数分别为0.248和0.222/h, 消除相的一级速率常数分别为 0.006和0.007/h, 吸收半衰期T(1/2) 分别为2.794和3.124h, 消除半衰期T(1/2)分别为113.068和105.841h, 中央室向周边室转运的一级速率常数K12分别为0.020和0.015/h, 周边室向中央室转运的一级速率常数K21分别为0.159和0.121/h, 药-时曲线下面积AUC分别为2493.944和3601.863 ngh/mL。肌肉、皮肤、肝脏和肾脏组织中孔雀石绿和隐色孔雀石绿浓度水平的结果表明, 孔雀石绿在斑点叉尾 4种组织中浓度由高到低的顺序是皮肤肌肉肾脏肝脏, 其中斑点叉尾 皮肤组织易蓄积孔雀石绿, 其残留时间最长, 肝脏组织由于对孔雀石绿有极强的代谢转化功能而浓度较低。孔雀石绿在肌肉、皮肤、肝脏和肾脏组织中的消除方程分别为C=5.570 e-0.009t、C=6.302 e-0.007t、C=4.791 e-0.006t和C=4.591 e-0.002t, 相关系数r20.773, 消除半衰期T1/2肌肉、皮肤、肝脏和肾脏分别为3.2、4.1、4.8和14.4d。肌肉、皮肤、肝脏和肾脏组织中孔雀石绿分别在45、60、30和60d才未被检测到; 隐色孔雀石绿在斑点叉尾 4种组织中浓度由高到低的顺序是肝脏皮肤肌肉肾脏, 残留时间最长的组织也是皮肤组织。隐色孔雀石绿在肌肉、皮肤、肝脏和肾脏组织中的消除方程分别为C=6.491 e-0.004t、C=6.958 e-0.003t、C=6.722 e-0.007t和C=6.162 e-0.002t, 相关系数r20.673, 消除半衰期T1/2肌肉、皮肤、肝脏和肾脏分别为7.2、9.6、4.1和14.4d。肌肉、皮肤、肝脏和肾脏组织中隐色孔雀石绿分别在90、90、60和90d才未被检出。试验期间(2011年5月17日至7月15日)平均水温为26.4℃, 孔雀石绿和隐色孔雀石绿90d后在各组织中才未检测到, 因此, 使用7 mg/L孔雀石绿浸泡2龄斑点叉尾 苗种孔雀石绿及其代谢物隐色孔雀石绿至少应经过2376℃d后才能消除。       

强力霉素在斑点叉尾(鲴)体内药物动力学及残留消除规律研究

研究利用高效液相色谱法研究了强力霉素在斑点叉尾 (Ictalurus punctatus)体内的药物动力学与消除规律, 有助于制定合理用药方案和休药期, 为水产品质量安全提供理论依据。(1)单次口服剂量 20 mg/kg 强力霉素在斑点叉尾 体内的药时数据符合二室开放式模型。药-时曲线呈明显双峰现象: 第一次达峰时, 强力霉素在肾、血和肌肉中浓度迅速上升, 达峰时间 Tmax (1)出现在 30min, 强力霉素在肝脏中浓度上升缓慢, 出现在 1h; 肝、肾、血和肌肉第二次达峰的时间 Tmax (2)出现在 8h, 第二次达峰浓度 Cmax(2)大于第一次的浓度Cmax (1)。 药-时曲线下面积(AUC): 肾、肝、血和肌肉分别为 63.242、1282.077、142.379、62.348 μg·h /mL。消除半衰期[T1/2b]: 肾、肝、血和肌肉分别为 40.668、48.767、36.527、31.091h, 平均滞留时间(MRT): 肾、肝、血和肌肉分别为 46.585、56.989、48.859、42.428h; (2)连续口服剂量 20 mg/kg 的强力霉素 5d, 停药后强力霉素在斑点叉尾 肝脏中浓度最高, 肌肉+皮中浓度最低。在不同组织中强力霉素的消除速率不同(P<0.05), 药物消除速度由高到低依次为肌肉+皮、肾脏、肝脏。若以肝脏为靶组织, 最高残留限量 300 μg/kg,休药期不低于 30d; 若以可食组织肌肉+皮为靶组织, 最高残留限量 300 μg/kg, 休药期不低于 19d。     

肌注和药饵给药下诺氟沙星在南美白对虾血淋巴中药代动力学

本文分析了盐度1‰和15‰下诺氟沙星肌肉注射给药(剂量10mg/kg)和盐度15‰下药饵口服给药(剂量15mg/kg和30mg/kg)后南美白对虾血淋巴中药代动力学。在盐度1‰和15‰下,南美白对虾肌注给药后血药浓度的变化趋势基本相似,血药浓度与时间关系曲线适合用二室模型来描述,其药动学方程分别为C0=35.422×e-9.778t 4.363×e-0.165t和C0=35.144×e-13.335t 7.888×e-0.608t,但两盐度下部分药动学参数差别较大。药饵口服给药时,给药剂量与血药浓度未呈明显的正相关,且血药浓度—时间关系曲线均表现出双峰现象。以30mg/kg剂量药饵口服给药后,药峰出现的时间分别为给药后4h和12h,峰浓度分别为2.86μg/mL和2.04μg/mL;以15mg/kg剂量给药时也得到相似的双峰现象,但第二峰浓度出现的时间为8h。     

盐酸氯苯胍在斑点叉尾鮰体内的药代动力学及残留消除规律

在水温(28±1)℃条件下, 以20 mg/kg剂量的盐酸氯苯胍口灌斑点叉尾鮰(Ictalurus punctatus), 采用高效液相色谱-串联质谱法研究盐酸氯苯胍在斑点叉尾鮰体内的药代动力学和残留消除规律。结果显示, 在单次口灌给药后, 盐酸氯苯胍在斑点叉尾鮰血浆中的药时曲线符合二室模型特征, 其药动学方程为C= 7.69e–0.02t+ 0.13e–0.01t–7.82e–0.27t。盐酸氯苯胍在斑点叉尾鮰血浆、肌肉、皮、鳃、肝脏和肾脏中的T_(peak)分别为10.03、15.79、11.10、2.61、12.89、7.87h; C_max分别为5.76 μg/mL、2.91、2.90、3.05、3.04、0.42 mg/kg, 消除半衰期分别为58.63、23.57、35.37、19.74、29.34、43.30h; 药-时曲线下面积AUC分别为326.74 (μg/mL)/h、157.58、183.72、95.09、174.82、29.85 (mg/kg)/h。在连续口灌给药5d后, 停药后盐酸氯苯胍在斑点叉尾鮰肠道中的浓度最高, 肌肉中浓度最低, 盐酸氯苯胍在体内各组织中的消除速度由高到低依次为血浆、鳃、脑、肌肉、皮肤、肝脏、肾脏、肠。若将10 μg/kg作为盐酸氯苯胍的最高残留限量, 在试验条件下, 建议盐酸氯苯胍在斑点叉尾鮰体内的休药期至少应为23d。     

肌注和口服恩诺沙星在大菱鲆体内的药代动力学比较

在水温(16±0.6)℃条件下, 以20 mg/kg剂量给健康大菱鲆静注、肌注和口服恩诺沙星后, 用高效液相色谱法测定药物浓度,采用DAS2.0药动学软件对血药浓度进行分析,比较了肌注和口服两种给药方式下恩诺沙星在大菱鲆(Scophthalmus maximus)体内的药代动力学差异。结果显示,肌注和口服恩诺沙星后,在大菱鲆体内的代谢过程均符合一级吸收二室开放模型, 表达方程为C肌注=10.237e-0.702t+6.151e-0.01t-16.388e-25.796t和C口服=3.701e-0.072t+3.534e-0.007t-7.235e-0.364t。与口服给药后药代动力学参数比较, 肌注给药后的t1/2Ka(0.027h)、tmax(0.5h)、t1/2α(0.987h)和t1/2β(68.003h)均小于口服给药(1.904h、4h、9.621h和99.137h),且Cmax(21.7172μg/mL)和F(88.57%)均大于口服给药(5.3594μg/mL、66.42%)。结果表明, 肌注恩诺沙星在大菱鲆体内的吸收、消除均快于口服给药, 且比口服给药吸收完全。在试验条件下, 最佳给药方案为:肌注给药, 按鱼体重每次给药19.05 mg/kg,2天一次, 建议连续给药2-3次;口服给药,按鱼体重每次给药13.92mg/kg,1天一次, 建议连续给药3-5次, 建议休药期分别不低于30d和45d。       

给药剂量对氟苯尼考在中华绒鳌蟹体内的药物代谢动力学影响

在17℃水温下,单次肌肉注射给药,高效液相色谱法-荧光法测定中华绒螯蟹(Eriocheir sinensis)血淋巴、肌肉和肝中药物残留浓度,利用3P97药代动力学软件分析数据,研究不同剂量氟苯尼考在中华绒螯蟹血淋巴、肌肉和肝组织中的代谢规律及组织分布。结果表明,在3种(5.0、10.0、20.0mg/kg)给药剂量下,血淋巴和肌肉组织中氟苯尼考含量瞬时达到峰值,而肝中氟苯尼考含量则随给药时间,先上升后下降,各组织含量从大到小依次为:肌肉、血淋巴、肝。应用药代动力学计算软件3P97分析结果表明,血淋巴、肌肉、肝组织中氟苯尼考的代谢规律均符合二室开放模型,以3个浓度给药后,血淋巴中氟苯尼考的吸收半衰期(T1/2α)及消除半衰期(T1/2β)分别为0.04、0.21、0.87h和0.60、1.48、3.29h,整体清除率(CLs)分别是2.17、1.99和2.12ml/(kg·h),肌肉中氟苯尼考的T1/2α及T1/2β分别是1.38、0.93、0.47h和10.39、31.78、23.91h,CLs分别是0.07、0.03、0.03ml/(kg·h),肝中氟苯尼考的T1/2α及T1/2β分别是0.69、0.07、0.12h和0.73、4.90、4.49h,CLs分别是1.79、2.55、3.89ml/(kg·h)。     

达氟沙星在史氏鲟体内药物代谢动力学比较研究

采用高效液相色谱法测定以10mg/kg体重剂量静脉注射和口服给药后史氏鲟血浆中达氟沙星的浓度。该法采用C18色谱柱,流动相为乙腈-水相(15∶85),荧光激发波长和发射波长分别为280nm和450nm,样品用甲醇沉淀蛋白,离心取上清液进样。达氟沙星在0.005-1.0μg/mL范围内线性关系良好,本方法的最低检测限为0.005μg/mL。健康鱼单剂量静注达氟沙星(10mg/kg),其药时数据符合无吸收的三室开放模型,方程为C=5.830-5.582t+4.162-1.157t+0.852-0.029t,主要动力学参数如下:t1/2α0.552h;t1/2β22.186h;AUC34.226mg/(L.h);V 10.922L/kg;Vb10.144L/kg;ke 10.317h.Ah感染组的V1减小至0.290L/kg,静注感染组鱼体内达氟沙星的消除没有显著的改变。健康口服组数据结果符合一级吸收二室开放模型,血药浓度和时间方程为C=1.278e-0.073t+0.177e-0.089t-1.455e-0.329t。药动学常数分别为:t1/2ka9.491h,t1/2β78.267h,Tmax6.284h,Cmax0.791mg/mL;α0.073h。但Ah感染改变达氟沙星口服给药后在史氏鲟体内的吸收、分布和消除。分布速率常数降低为0.050/h。消除减慢,消除半哀期延长为93.988h,达峰时间延长为至9.060h,峰浓度降低为0.585mg/mL。口服达氟沙星水溶液,健康及感染组史氏鲟对达氟沙星生物利用度分别为96.503%和94.435%。本实验结果表明达氟沙星在健康史氏鲟体内分布广泛、吸收较完全。感染Ah对达氟沙星在史氏鲟体内的吸收、分布及消除规律均有不同程度的影响,其中口服给药的影响更为显著。达氟沙星可用于史氏鲟感染Ah的治疗。       

恩诺沙星在三疣梭子蟹主要组织中的代谢动力学

应用反相高效液相色谱法（RP-HPLC）研究了三疣梭子蟹（portunus trituberculatus）经口灌10 mg/kg恩诺沙星后体内的药代动力学规律。结果表明口灌给药后,三疣梭子蟹肝胰腺、肌肉和血淋巴组织中的恩诺沙星达峰速度快,肝胰腺和血淋巴在给药24h都有双峰现象出现。恩诺沙星在肝胰腺、肌肉、血淋巴中的Cmax分别为11.235μg/g、0.850μg/g和0.858μg/g,Vd/F为7.954 L/kg、10.367 L/kg和0.345 L/kg。t1/2β分别为283.361 h、47.869 h和17.681 h,AUC分别为245.618μg/g.h、24.753μg/g.h和20.111μg/g.h。给药后5 min在肝胰腺中即可检测到恩诺沙星的代谢产物环丙沙星,而肌肉和血淋巴在给药后2 h才能检测到,其含量均处于较低水平。用3P97软件对各组织中的药时数据进行房室模型拟合,结果显示：三疣梭子蟹口灌给药后,恩诺沙星在血淋巴、肌肉和肝胰腺中的代谢过程均符合一级吸收二室开放模型,而环丙沙星不能用房室模型来描述。     

双氟沙星及其代谢产物在中华绒螯蟹体内药物代谢及残留消除规律

采用高效液相色谱法,在口灌给药途径下,研究双氟沙星及其代谢产物沙拉沙星在中华绒螯蟹(Eriocheir sinensis)体内的药代动力学.中华绒螯蟹以20 mg/kg剂量给药双氟沙星后,其血淋巴、肌肉、肝胰腺、精巢和卵巢中药物-时间曲线关系符合开放性二室模型.双氟沙星在中华绒螯蟹体内吸收迅速,在不同组织中分布较广,达峰时间短.血淋巴、肌肉、肝胰腺、精巢和卵巢中的Vd分别为3.170 L/kg、2.122 L/kg、1.045 L/kg、1.051 L/kg和0.203 L/kg;双氟沙星在中华绒螯蟹体内消除缓慢,在血淋巴、肌肉、肝胰腺、精巢和卵巢中的消除半衰期t1/2β分别为96.316 h、88.228 h、137.524 h、67.021 h和124.679 h;总体清除率CLa分别为0.783 L/h·kg、0.040 L/h·kg、0.013 L/h·kg、0.011 L/h·kg和0.008 L/h·kg.代谢产物沙拉沙星在中华绒螯蟹血淋巴、肌肉、肝胰腺、精巢和卵巢中药物水平的变化趋势与双氟沙星相似,都呈现多峰现象.但肌肉、肝胰腺、精巢和卵巢4种组织中代谢产物沙拉沙星出现药峰的时候恰好是这4种组织中双氟沙星下降缓慢时期.鉴于双氟沙星及其代谢产物沙拉沙星在中华绒螯蟹体内消除缓慢,而可食组织中脂肪含量较高,因此若规定可食组织中双氟沙星的最大残留限量以脂肪中最大残留限量(100μg/kg)为标准,沙拉沙星的最大残留限量为30μg/kg,则建议双氟沙星在中华绒螯蟹中的休药期大于24d,才能保障食用者的安全.     

Plant-Parasitic Nematodes of South Viet Nam

Between 1974 and 1978, 2,842 identifications of plant-parasitic nematodes were made from more than 1,700 soil and plant samples collected in eight provinces of South Viet Nam. Species in nine genera—Helicotylenchus, Criconemoides, Meloidogyne, Pratylenchus, Tylenchorhynchus, Hoplolaimus, Hirschmanniella, Xiphinema, and Rotylenchulus—comprised 96.1% of the identifications; the remaining 3.9% were species of 11 genera. Fourteen genera were associated with rice which was grown on about 2,500,000 ha in 1970. Of these, Ditylenchus, Hirschmanniella, and Meloidogyne were most important. Ditylenchus angustus caused severe damage to about 50,000 ha of flooded rice in the Mekong Delta in 1976. Hirschmanniella spp. were found in all samples examined from flooded rice fields. Meloidogyne spp. were common in rice seedbeds, upland rice, and rice not kept flooded continuously. Meloidogyne and Pratylenchus spp. were found in roots of 22 of the 32 crop plants sampled. Little or no attempt was made in South Viet Nam to control nematodes.     

Identification key for European strand-forming house-rot fungi

An identification key for 20 common strand-forming indoor wood decay fungi is given. The key is based on observations of material from affected buildings and on wood samples that have been incubated in the laboratory. The key is with macro- and microscopic photographs.     

Semicircular canal system in early primates

Mammals with more rapid and agile locomotion have larger semicircular canals relative to body mass than species that move more slowly. Measurements of semicircular canals in extant mammals with known locomotor behaviours can provide a basis for testing hypotheses about locomotion in fossil primates that is independent of postcranial remains, and a means of reconstructing locomotor behaviour in species known only from cranial material. Semicircular canal radii were measured using ultra high resolution X-ray CT data for 9 stem primates (“plesiadapiforms”; n = 11), 7 adapoids (n = 12), 4 omomyoids (n = 5), and the possible omomyoid Rooneyia viejaensis (n = 1). These were compared with a modern sample (210 species including 91 primates) with known locomotor behaviours. The predicted locomotor agilities for extinct primates generally follow expectations based on known postcrania for those taxa. “Plesiadapiforms” and adapids have relatively small semicircular canals, suggesting they practiced less agile locomotion than other fossil primates in the sample, which is consistent with reconstructions of them as less specialized for leaping. The derived notharctid adapoids (excluding Cantius) and all omomyoids sampled have relatively larger semicircular canals, suggesting that they were more agile, with Microchoerus in particular being reconstructed as having had very jerky locomotion with relatively high magnitude accelerations of the head. Rooneyia viejaensis is reconstructed as having been similarly agile to omomyids and derived notharctid adapoids, which suggests that when postcranial material is found for this species it will exhibit features for some leaping behaviour, or for a locomotor mode requiring a similar degree of agility.     

Two common and problematic leucochrysine species – Leucochrysa (Leucochrysa) varia (Schneider) and L. (L.) pretiosa (Banks) (Neuroptera,Chrysopidae): redescriptions and synonymies

We dedicate this article to the memory of Sergio de Freitas, FCAV-UNESP, Jaboticabal, São Paulo, Brazil (deceased, 2012). He was an active and enthusiastic Neuropterist and the cherished mentor and friend of Francisco Sosa.Leucochrysa McLachlan is the largest genus in the Chrysopidae, yet it has received relatively little taxonomic attention. We treat two problematic and common Leucochrysa species – Leucochrysa (Leucochrysa) varia (Schneider, 1851) and Leucochrysa (Leucochrysa) pretiosa (Banks, 1910). Both are highly variable in coloration and were described before the systematic importance of chrysopid genitalia was recognized. Recent studies show that these species occur within a large complex of cryptic species and that they have accumulated a number of taxonomic problems. We identify new synonymies for each of the species–for Leucochrysa (Leucochrysa) varia: Leucochrysa (Leucochrysa) ampla (Walker, 1853), Leucochrysa internata (Walker, 1853), and Leucochrysa (Leucochrysa) walkerina Navás, 1913; for Leucochrysa (Leucochrysa) pretiosa: Leucochrysa (Leucochrysa) erminea Banks, 1946. The synonymy of Leucochrysa delicata Navás, 1925 with Leucochrysa (Leucochrysa) pretiosa is stabilized by the designation of a neotype. The following species, which were previously synonymized with Leucochrysa (Leucochrysa) varia or Leucochrysa (Leucochrysa) pretiosa, are reinstated as valid: Leucochrysa (Leucochrysa) phaeocephala Navás, 1929, Leucochrysa (Leucochrysa) angrandi (Navás, 1911), and Leucochrysa (Leucochrysa) variata (Navás, 1913). To help stabilize Leucochrysa taxonomy, lectotypes are designated for Allochrysa pretiosa and Allochrysa variata. Finally, Leucochrysa vegana Navás, 1917 is considered a nomen dubium.     

Multilocus phylogenetic analysis of the genus Aeromonas

A broad multilocus phylogenetic analysis (MLPA) of the representative diversity of a genus offers the opportunity to incorporate concatenated inter-species phylogenies into bacterial systematics. Recent analyses based on single housekeeping genes have provided coherent phylogenies of Aeromonas. However, to date, a multi-gene phylogenetic analysis has never been tackled. In the present study, the intra- and inter-species phylogenetic relationships of 115 strains representing all Aeromonas species described to date were investigated by MLPA. The study included the independent analysis of seven single gene fragments (gyrB, rpoD, recA, dnaJ, gyrA, dnaX, and atpD), and the tree resulting from the concatenated 4705 bp sequence. The phylogenies obtained were consistent with each other, and clustering agreed with the Aeromonas taxonomy recognized to date. The highest clustering robustness was found for the concatenated tree (i.e. all Aeromonas species split into 100% bootstrap clusters). Both possible chronometric distortions and poor resolution encountered when using single-gene analysis were buffered in the concatenated MLPA tree. However, reliable phylogenetic species delineation required an MLPA including several “bona fide” strains representing all described species.     

Bacterial flora in the alimentary tract of chickens infected with Eimeria brunetti and in chickens immunized with Eimeria maxima and cross-infected with Eimeria brunetti

Differential bacterial counts were made on the intestinal and caecal contents of chickens after inoculation with a standard dose of 320 000 freshly sporulated oocysts of Eimeria brunetti.