硫酸头孢喹肟乳房注入剂对泌乳期奶牛的安全性研究

为研究硫酸头孢喹肟乳房注入剂对泌乳期奶牛的安全性,试验选用12头健康泌乳奶牛(6头初产、6头经产),间隔12 h对每头奶牛的4个乳区分别注入硫酸头孢喹肟乳房注入剂(规格:8 g:75 mg/支)1支,连续给药3次,比较观察给药前后奶牛的临床症状、体细胞数、日产奶量及乳区病原菌变化情况。结果显示,与给药前相比,给药期间及停药后奶牛的临床症状、体细胞数、日产奶量、乳区病原菌检测结果均无显著性差异(P>0.05)。表明硫酸头孢喹肟乳房注入剂对泌乳期奶牛是安全的。     

Safety Study on Cefquinome Sulfate Intrauterine Infusion for Lactating Cows

The aim of this experiment was to study the safety of cefquinome sulfate intrauterine infusion for lactating cows.24 healthy lactating Chinese Holstein cows were randomly divided into four groups(6 cows in each group).Cows in groups Ⅰ, Ⅱ and Ⅲ were respectively injected different doses of cefquinome sulfate intrauterine infusion in uterus, and cows in the blank control group(group Ⅳ) were injected the dose of sterilized saline water.The cows were injected with the tested drug in uterus for twice and the interval was 72 h.The indicators including body temperature(rectal temperature), pulse rate, respiratory rate, blood physiological and biochemical indexes, mental state, daily milk yield and somatic cell count(SCC) in milk were respectively observed and measured on the day of first administration, the day of final administration and the 7th day after final administration.The results showed that injecting lactating cows cefquinome sulfate intrauterine infusion to lactating cows as recommended dosage was safe.The drug could be used to treat endometritis of lactating cows in clinical practice.     

头孢喹肟对金黄色葡萄球菌防突变浓度的研究

【目的】为兽医临床合理用药,进行头孢喹肟对金黄色葡萄球菌的最低抑菌浓度(MIC)和防突变浓度(MPC)研究.【方法】采用标准琼脂二倍稀释法,测定头孢喹肟对金黄色葡萄球菌的MIC和MIC99(抑制99%接种细菌生长的最低抑菌浓度);使用肉汤法富集1010CFU/mL金黄色葡萄球菌ATCC 29213和37株金黄色葡萄球菌临床分离菌,采用标准琼脂平板稀释法测定头孢喹肟对金黄色葡萄球菌的MPC,并计算选择指数(SI).【结果和结论】头孢喹肟对金黄色葡萄球菌ATCC 29213的MIC和MIC99分别是0.5和0.4μg/mL,MPC为1.6μg/mL,SI(MPC/MIC99)为4.头孢喹肟对37株临床分离的金黄色葡萄球菌的MIC50、MIC90和MPC90分别是0.50、1.00和5.12μg/mL;SI(MPC90/MIC90)为5.12.头孢喹肟对金黄色葡萄球菌具有较强的抗菌活性,SI也较小,通过调整给药方案可以减少耐药突变株的产生.     

硫酸头孢喹肟乳房注入剂在牛奶中的药代动力学研究

选取8头健康黑白花奶牛,每头牛随机选择两个乳区,以每个乳区1支(8g:75mg/支)的剂量进行单次乳房灌注给予硫酸头孢喹肟乳房注入剂。采用超高效液相色谱-串联质谱(UPLC-MS/MS)方法检测乳中头孢喹肟的浓度。结果表明,该制剂采用单次乳房灌注给药后,乳中药物能发挥较好抑菌效果的时间约为24～30小时,因此建议该制剂治疗奶牛临床型乳房炎的用药方案为：1支(8g:75mg)/(乳区.次),每天给药1次。     

Comparison of the clinical efficacy of cefquinome with the combination of penicillin G and gentamicin in equine patients

This prospective, randomised, nonblinded study compared the clinical efficacy of cefquinome to that of a combination of penicillin and gentamicin. Patients (374 horses and 13 donkeys) at the equine hospital of the Vetsuisse-Faculty of Zurich, presented from February-October 2007, were divided into prophylactic and therapeutic treatment groups. Equids from these groups were randomly treated either with cefquinome or with the combination of sodium penicillin and gentamicin. There was no significant difference between the 2 treatment groups for prophylactic indications. In the therapeutic group, cefquinome showed better efficacy, as demonstrated by fewer complications of wound healing and fewer treatment failures with subsequent change to another antibiotic. Side effects were very rare in both treatment groups. Cefquinome can be used with safety and efficacy in equids. Cefquinome had greater efficacy than the combination of penicillin and gentamicin in the therapeutic group. However, there was no difference between the 2 antibiotic treatments in the prophylactic group. In order to minimise the development of resistance, cefquinome should therefore not be used for routine prophylactic treatment.     

硫酸头孢喹肟乳膏剂临床疗效试验

为更好地防治奶牛乳房炎,河北农业大学动物科技学院自主研发了硫酸头孢喹肟乳膏剂,并对其临床疗效进行了考察。对河北4个地区临床分离的乳房炎致病菌进行鉴定,而后使用自制的乳膏进行体外抑菌试验和临床疗效试验。结果表明,分离的病原菌主要是链球菌、葡萄球菌和大肠杆菌,共占总菌株的95.11%;乳膏组对临床分离的致病菌抑菌效果优于青、链霉素对照组;乳膏在4个地区的治愈率和有效率均较高,分别为93.68%和98.95%;而青、链霉素对照组则分别只有57.84%,84.31%。因此,自主研发的硫酸头孢喹肟乳膏剂用于治疗临床奶牛乳房炎效果理想,为下一步的推广奠定良好的基础。     

硫酸头孢喹肟在鸭体内的药动学及生物利用度研究

试验将20只2月龄健康番鸭,随机分为2组,每组10只,雌雄各半,分别进行静脉注射和口服硫酸头孢喹肟给药的药动学研究。静脉注射和口服的给药剂量分别为10和20 mg/kg。以反相HPLC测定血浆中硫酸头孢喹肟的浓度,血药浓度—时间数据用3P97药动学程序软件处理。鸭单剂量静脉注射给药后,血药浓度—时间数据符合无吸收二室开放模型,其主要动力学参数分别为:V（c）,（1.146±0.02） L/kg;t_1/2α,（0.290±0.02）h;t_1/2β,（1.691±0.15）h;AUC （6.635±0.18）（mg·h）/L;CL（s）,（1.508±0.04）L/（kg·h）。鸭口服硫酸头孢喹肟的血药浓度—时间数据符合一级吸收一室开放模型,主要动力学参数分别为:t_1/2（ka）,（0.45±0.05）h;t_1/2（ke）,（0.96±0.29）h;T_（peak）,（0.91±0.09）h;C_（max）,（3.14±0.64）mg/L;AUC,（8.29±1.26）（mg·h）/L;F,（62.55±0.10）%。硫酸头孢喹肟在体内的药动学特征表现为吸收迅速、分布广泛、消除迅速。但口服给药在鸭体内生物利用度低,可能由于硫酸头孢喹肟的脂溶性低,其在消化道吸收率低所致。但8 h内能保持有效血药浓度范围（（0.14±0.03）~（3.14±0.64）μg/mL）,可抑制鸭疫里默氏杆菌及其他细菌感染。     

硫酸头孢喹肟脂质体的毒理学试验及安全性评价

采用急性毒性试验、局部刺激性试验和亚慢性毒性试验对硫酸头孢喹肟脂质体安全性进行评价,以期为临床用药提供参考。小鼠腹腔注射硫酸头孢喹肟脂质体半数致死量（LD₅₀）为639.73 mg/kg,95%可信限为573.06~714.17 mg/kg;该制剂对家兔股四头肌未见明显刺激作用;各给药剂量组家兔的体重、血液学指标、生化指标与对照组比较均无显著差异（P>0.05）;对肝脏和肾脏病理学观察表明,正常治疗剂量和中剂量组肝脏和肾脏组织结构清晰,但高剂量组出现肝细胞排列紊乱,肝血窦间出血,肾小球、肾间质有散在出血。以上结果表明硫酸头孢喹肟脂质体安全可靠,可应用于兽医临床。     

头孢喹诺的研究进展

头孢喹诺是动物专用的第 1个第 4代头孢菌素类抗生素 ,其抗菌谱广 ,抗菌活性强 ,对临床分离的各种 G 菌、G-菌的 MIC50 、MIC90 值均较小 ,而且对绿脓杆菌有很强的抗菌活性 ;其动力学特点优良 ,吸收快 ,达峰时间短 ,生物利用度较高 ,可以在肺、乳腺等组织达到较高的组织浓度 ;头孢喹诺毒性低 ,在动物的可食性组织中残留较少 ;国外已广泛应用于猪、牛的呼吸系统感染及奶牛乳房炎的临床治疗。因此 ,在我国兽医临床上具有广阔的应用前景。为了促进其在我国兽医临床上的合理应用、研制与开发 ,现对其抗菌活性、药动学、毒性及残留、临床应用等有关资料进行综述     

头孢喹诺的最新研究进展

作者综述了畜禽专用的第4代头孢菌素类抗生素—头孢喹诺的抗菌活性、药效学、药动学、临床应用和毒性及残留等方面的特性和研究概况。以促进其在我国的研制、开发与推广,从而更有效地使用该药。