复方阿莫西林纳米乳制剂的安全性评价

通过急性毒性试验、皮肤刺激性试验和细胞毒性试验,对复方阿莫西林纳米乳(AMX-LH-NE)进行体内外安全性评价.结果表明,AMX-LH-NE毒性低,无法测出其半数致死量,小鼠的最大耐受量倍数为426倍;无论是单次给药,还是多次给药,AMX-LH-NE对完整皮肤和破损皮肤均无明显刺激性;AMX-LH-NE为10～150 mg.L-1时,对乳腺上皮细胞的生长和形态无明显影响,其毒性分级属于0或1级,即对乳腺上皮细胞无毒性作用.     

阿莫西林钠-酒石酸泰乐菌素复方药物治疗猪链球菌病的研究

为研究阿莫西林钠-酒石酸泰复方药物乐菌素治疗猪链球菌病的药效学,选用60只15g左右的昆明鼠,以多重耐药的临床分离猪链球菌为病原,以腹腔注射为感染途径,对猪链球菌的病理模型进行了复制,按照Reed-Munch法计算LD50为9.61×108cfu·mL-1。在此基础上,选用80只昆明鼠,接种LD50菌液,分别口服阿莫西林钠,酒石酸泰乐菌素及阿莫西林钠-酒石酸泰乐菌素复方药物。结果表明,阿莫西林钠-酒石酸泰乐菌素复方药物组的作用效果明显优于单药组,小鼠存活率为80%,阿莫西林钠组的小鼠存活率为70%,酒石酸泰乐菌素组为60%。     

The influence of growth and E. coli endotoxaemia on amoxicillin pharmacokinetics in turkeys

1. This experiment aimed to determine if the pharmacokinetics of amoxicillin (AMO) was affected by rapid growth or intravenous (i.v.) injection of Escherichia coli lipopolysaccharide (LPS).

2. Turkeys of 2.0, 5.5 and 12.0 kg were administered i.v. or orally with AMO sodium at the dose of 15 mg/kg. Another group (5.7 kg) was treated with LPS prior to i.v. AMO administration. Plasma drug concentrations were determined using high-performance liquid chromatography and pharmacokinetic parameters were calculated using a non-compartmental model. To assess the haemodynamic effects of endotoxaemia, turkeys were subjected to echocardiography.

3. During growth from 2.0 to 5.5 kg, the area under the drug concentration-time curve after i.v. AMO administration increased from 9.37 ± 2.43 to 21.29 ± 5.49 mg×h/ml. Total body clearance decreased from 1.72 ± 0.55 to 0.75 ± 0.12 l/h/kg. Growth to 12.0 kg did not further affect these parameters. Mean residence time and elimination half-life gradually increased. Pharmacokinetics of orally administered drug followed a similar pattern. LPS injection affected stroke volume, heart rate and resistance index. However, it did not affect the pharmacokinetic profile of AMO in survivors.

4. It is concluded that rapid growth in turkeys affects AMO pharmacokinetics. Endotoxaemia, on the other hand, does not affect AMO elimination if compensatory mechanisms develop.     

12批市售阿莫西林产品的监察思考

对市售12批阿莫西林产品进行监督检查,结果含量均不符合规定,并存在企业伪造GMP证、套用兽药产品批准文号、擅自使用未批准的商品名等违规现象。本文从兽药产品文号、主要成分含量、成分、标签和说明书等方面分析产生的原因,并提出了加强管理的意见。     

安普霉素及其联合用药对大肠杆菌的PAE研究

采用菌落计数法和中性粒细胞减少的小鼠股部感染模型,分别测定了安普霉素及其与阿莫西林或氨苄西林联用对大肠杆菌的体内、外PAE。当药物以2×MIC、4×MIC和8×MIC浓度作用于大肠杆菌时,安普霉素体外PAE分别为1.15、2.04、3.27 h,体内PAE分别为3.46、4.49、5.77 h;安普霉素与阿莫西林联用的体外PAE分别为1.53、3.06、4.75 h,体内PAE分别为4.95、6.50、8.47 h;安普霉素与和氨苄西林联用的体外PAE分别为1.95、3.57、5.58 h,体内PAE分别为5.24、6.95、9.28 h。结果表明：安普霉素在体内外对大肠杆菌均有较长的PAE,且随药物浓度的升高其PAE也相应的延长,呈明显的剂量依赖性。安普霉素与阿莫西林、氨苄西林联用对大肠杆菌体内、外PAE呈现相加或协同作用。