Pharmacokinetics and ex vivo pharmacodynamics of cefquinome in porcine serum and tissue cage fluids

A tissue cage (TC) model was used to evaluate the pharmacokinetics and ex vivo pharmacodynamics of cefquinome after intravenous (IV) and intramuscular (IM) administration to piglets at 2 mg/kg bodyweight. The mean values of area under the concentration–time curve (AUC) were 21.28 (IV) and 21.37 (IM) μg h/mL for serum, and 17.40 (IV) and 16.57 (IM) μg h/mL for TC fluid (TCF), respectively. Values of maximum concentration (C_max) were 6.15 μg/mL (serum) and 1.15 μg/mL (TCF) after IM administration. The elimination half-lives (t_1/2β) in TCF (10.63 h IV and 11.81 h IM) were significantly higher than those in serum (2.33 h IV and 2.30 h IM) (P < 0.05). The values of AUC_TCF/AUC_serum (%) after IV and IM administration were 82.4% and 80.7%, respectively.The ex vivo time-kill curves were established for serum and TCF samples using Escherichia coli ATCC 25922. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration values of cefquinome against E. coli were 0.030 and 0.060 μg/mL in Mueller–Hinton broth, and 0.032 and 0.064 μg/mL in both serum and TCF, respectively. The ex vivo growth inhibition data of TCF after IM administration were fitted to the sigmoid E_max model; AUC_24h/MIC was 35.01 h for bactericidal activity and 44.28 h for virtual eradication, respectively. The findings from this study suggest that cefquinome may be therapeutically effective in diseases of pigs caused by E. coli when used at a dose rate of 1.33 mg/kg administered every 24 h for organisms with MIC₉₀ ⩽ 0.50 μg/mL.     

柱塞式两次喷油泵驱动凸轮的设计及其运动特性分析

参考一次喷油泵的设计手册,进行了两次喷油泵的驱动凸轮的改型设计,对凸轮的运动特性进行了分析,驱动凸轮能两次推动柱塞完成两次喷油的过程。     

Injection stauntoniae inhibits chronic inflammatory pain responses by changing COX-2 expression in carrageenan-inflamed mice

AIM：To investigate the effect of injection stauntoniae (IS) on inflammatory pain responses in mice. METHODS：The carrageenan test was used to determine the anti-inflammatory and analgesic effects of IS. Except for control group, the mice in other groups received an injection of λ-carrageenan solution (1%, 50 μL) into the plantar region of the left hind paws, followed by a subcutaneous injection of IS at doses of 12.5%, 50% and 100% or equal volume of 0.9% NaCl. Both paw edema and hyperalgesia to thermal stimulation were measured 4 h, 12 h, 24 h and 48 h after the injection of λ-carrageenan solution. The lumbar-5 (L5) dorsal root ganglions (DRGs) of the mice were taken to investigate the cyclooxygenase 2 (COX-2) expression by immunohistochemical staining. RESULTS：Subcutaneous injection of IS potently inhibited paw edema and hyperalgesia induced by λ-carrageenan in the mice accompanied with the inhibition of COX-2 protein expression in L5 DRGs. CONCLUSION：IS exerts the anti-inflammatory and analgesic effects on the inflammatory responses by inhibiting the protein expression of COX-2 in DRGs.     

Differences in aluminium tolerance of ryegrass and white clover plants grown from seed or propagated vegetatively

The effect of aluminium (Al) on the relative yield of plants grown from seeds of ryegrass (Lolium perenne L.) or white clover (Trifolium repens L.) and either tillers (ryegrass) or stolon tip cuttings (white clover) were investigated using a low ionic strength (2.7 x 10^‐3 M) solution culture technique. In ryegrass, plants grown from tillers had higher relative yields than plants grown from seedlings in the tops when solution Al concentrations were greater than 16 μM and in the roots when solution Al concentrations were greater than 7 μM. In white clover, relative yields in the tops and roots plants were higher in plants grown from stolon tip cuttings than from seedlings when solution Al concentrations were greater than 10 μM. There were no significant cultivar effects. The results indicate that plants used in Al‐tolerance experiments can be grown from seed or vegetatively propagated, provided solution Al rates are adjusted to reflect differences in Al tolerance.     

4种兽用注射液中非法添加倍他米松UPLC-PDA检查方法的建立

为了建立柴胡注射液、维生素C注射液、盐酸林可霉素注射液、黄芪多糖注射液中非法添加倍他米松的超高效液相色谱检查方法,采用Waters ACQUITY UPLCBEH C18色谱柱(2.1 mm×50 mm,1.7μm),以0.75%三乙胺溶液(用磷酸调节p H为3.0)-甲醇-乙腈(50∶45∶5)为流动相;流速为0.3 m L·min-1;二极管阵列检测器,波长采集范围为190~400 nm,记录色谱图波长242 nm。柱温25℃,进样量10μL。倍他米松质量浓度在20.0~180.0 mg·L-1内峰面积呈良好线性关系(R2=0.9997,n=7),在柴胡注射液、盐酸林可霉素注射液、维生素C注射液、黄芪多糖注射液中倍他米松的平均回收率分别为103.5%(RSD=0.2%)、101.2%(RSD=0.8%)、100.4%(RSD=1.7%)、99.2%(RSD=1.7%)。本方法简便、快速、准确,可用于柴胡注射液等四种兽用注射液中非法添加倍他米松的检测。     

三类中药制剂对急性肾衰影响的比较

为了研究瘟清注射液、香丹注射液和术苓注射液对内毒素所致急性肾衰家兔的防治作用。将40只健康哈尔滨白兔随机分为阴性对照组、模型组、瘟清组、香丹组和术苓组,每组8只。模型组和各防治组家兔一次性静脉注射大肠杆菌O111B4内毒素生理盐水溶液;三防治组家兔在注射内毒素后立即静脉注射相应的中药注射液;阴性对照组静注生理盐水。各组家兔静注液体的总量相等。注射内毒素（或生理盐水）1 h后开始通过膀胱瘘管收集尿液,每小时收集1次,共收集6 h。末次收集尿液后心脏采血。对各组家兔的肾功能指标进行动态测定。结果显示：模型组家兔发生了急性肾功能衰竭。和模型组比较,瘟清组家兔的肌酐、尿素氮排出量显著或极显著增加（P〈0.05,P〈0.01）,肾衰指数和钠排泄分数显著或极显著降低（P〈0.05,P〈0.01）,内生性肌酐清除率显著或极显著升高（P〈0.05,P〈0.01）。除肾衰指数和钠排泄分数之外,香丹组家兔绝大多数肾功能指标的变化趋势与瘟清组相似。试验结果表明：瘟清注射液对急性肾衰具有确实的防治作用;香丹注射液亦有良好的防治急性肾衰作用;术苓组家兔肾功能衰竭状况并未得到根本好转。     

高效凝胶渗透色谱法测定人参糖肽注射液的重均分子量

建立人参糖肽注射液分子量分布测定方法。色谱柱为多糖专用凝胶柱OHpak SB-802HQ（8mm×300mm）,以0．9％氯化钠为流动相,流速0.5mL／min,示差折光检测器。人参糖肽注射液重均分子量为900—1100u。本实验建立的多糖分子量测定方法具有简便、快速和重现性好的特点,为提高和完善该制剂的质量标准提供了依据,同时可作为指纹图谱从多糖肽分子量角度来控制该产品的内在质量。     

Effects of phosphogypsum or calcium sulfate on aluminon reactive aluminum in solutions at varying pH

Abstract

Growing evidence of positive crop responses to gypsum or phosphogypsum (PG) application in acid soils strongly support the use of these amendments as an ameliorant of subsoil acidity. Although gypsum improves Ca availability in subsoils, its role in alleviation of Al toxicity needs careful attention. In the current study, either PG, CaSO₄.2H₂O or CaCl₂.2H₂O was added (to supply 12 mM Ca) to solutions containing 40 μM Al at pH 4.1 + 0.1. Solution pH was gradually raised to 4.5, 4.8 and then to 5.3 at various time intervals during 25 d aging of the solutions at 25 + 1^OC.

Concentration of Al measured by aluminon method without preacidification and preheating, referred to as “reactive Al”; in this paper, was 16 μM in 2 g L^‐1PG solution without added Al. This accounted 38% of total soluble Al in PG solution. Addition of 2 g L^‐1PG to solution containing 40 μM Al, resulted in only 42% of total Al in solution present in forms reactive with aluminon. According to MINTEQ speciation model, Al in solution was present as an entirely complexed form with F^‐. An increase in solution pH up to 5.3 had no effect on measured concentration of reactive Al or predicted distribution of Al species.

Addition of CaSO₄.2H₂O to 40 μMAl solutions had no effect on the concentration of reactive Al within pH 4.1 ‐4.8, however, up to 62% of total Al was in a form complexed with SO₄ ^2‐, as predicted by MINTEQ model. The concentration of reactive Al decreased by 60% at pH 5.3. Addition of CaCl₂.2H₂O also had no effect on the concentration of reactive Al within pH 4.1 ‐ 4.8. Nearly 73 ‐ 94% of total Al was present in Al³⁺form. An increase in pH to 5.3, decreased the concentration of reactive Al by 27%. The results suggest that ion‐pairing of Al with F^‐would appear to be a possible mechanism for alleviation of Al toxicity by PG at pH range 4.1 ‐ 5.3. With regard to CaSO₄.2H₂O, at pH 4.1 ‐ 4.8 ion‐pairing with SO.₄ ^2‐appears to be possible mechanism for the alleviation of Al toxicity. In addition, at pH 5.3 a considerable decrease in reactive Al was evident which would further alleviate Al toxicity.     

参麦注射液对高血压心衰大鼠血浆代谢组学的影响

目的 研究参麦注射液对高血压心衰大鼠血浆代谢组学的影响。方法 通过8% NaCl高盐饲料喂养Dahl盐敏感性大鼠制造高血压心衰模型,成模大鼠分为模型组、参麦注射液组,并同时设置正常组,干预15 d后,采集正常组、模型组和参麦注射液组大鼠的血浆样本,运用气相色谱-质谱（GC-MS）联用技术及多元统计分析进行研究。结果 3组的代谢图谱存在显著差异。与正常组相比,模型组19种代谢物水平紊乱;经参麦注射液干预后,亮氨酸、鸟氨酸、丙氨酸、4-羟基-脯氨酸、苏氨酸、天冬酰胺、苏糖醇、丙酮酸、尿素浓度向正常方向显著回调,苏糖酸、半胱氨酸、色氨酸、甲基半胱氨酸、花生四烯酸、胆固醇、木糖醇、核糖醇、焦谷氨酸、丙二酸浓度无显著改变,此外还发现异亮氨酸浓度上升。结论 高血压心衰大鼠血浆代谢组学出现变化,参麦注射液能有效改善部分紊乱的代谢物水平,其作用机制与改善糖代谢、氨基酸代谢紊乱,调节支链氨基酸水平相关,未发现有改善脂代谢紊乱的作用。     

复方麝香注射液联合尼莫地平治疗高血压性脑出血微创清除术后患者的疗效观察

目的 观察复方麝香注射液联合尼莫地平治疗微创清除术后高血压性脑出血患者的临床疗效,探讨其临床应用价值。方法 选取2018年5月至2019年5月本院收治的96例高血压脑出血患者,随机分为观察组和对照组,每组48例。对照组在基础治疗及护理的基础上给予尼莫地平注射液14 d,后改用尼莫地平片继续服用14 d;观察组在对照组的基础上加用复方麝香注射液静脉滴注28 d。观察两组患者治疗前后的血肿量、水肿量、神经功能缺损程度[美国国立卫生研究院卒中量表（national institute of health stroke scale,NIHSS）评定]、血清学相关指标[白细胞介素-6（interleukin-6,IL-6）、肿瘤坏死因子-a（tumor necrosis factor-a,TNF-a）、基质金属蛋白酶-9（matrix metalloprotein-9, MMP-9）],以及治疗后临床疗效。结果 （1）治疗后,两组患者的血肿量、水肿量均较本组治疗前减少,NIHSS评分均较本组治疗前降低,差异均有统计学意义（P<0.05）,且观察组低于对照组（P<0.05）;（2）治疗后,两组患者的血清IL-6、TNF-a、MMP-9均较本组治疗前下降（P<0.05）,且观察组低于对照组（P<0.05）;（3）治疗后观察组患者的总有效率为95.83%,高于对照组的81.25%（P<0.05）。结论 采用复方麝香注射液联合尼莫地平治疗微创清除术后高血压性脑出血患者,可促进患者颅内血肿吸收,改善神经功能缺损,疗效显著,值得临床推广。