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1.
采用湿法制粒压片工艺,以崩解时间为指标,用正交试验L8(2^7)对制备工艺和处方进行筛选和优化,确定最佳工艺与处方。用紫外扫描仪在λ为200-400nm波长范围内,对甲磺酸培氟沙星辅料分别进行扫描,甲磺酸培氟沙星在271.5nm处有最大吸收并绘制出标准曲线,回归方程为:A=0.025+0.703C,r=0.9997,线性范围4.47-26.82mg/L,测出甲磺酸培氟沙星速溶片的回收率为99.5%,RSD为1.28%。对速溶片进行质量检查,结果表明:硬度、崩解时限度和重量差异均符合《中华人民共和国药典》2000年版规定。  相似文献   

2.
紫外分光光度法测定复方甲磺酸培氟沙星注射液含量   总被引:1,自引:0,他引:1  
建立了复方甲磺酸培氟沙星注射液中甲磺酸培氟沙星与安乃近的含量测定方法.用紫外分光光度法中倍率减差法消除安乃近干扰,测定甲磺酸培氟沙星含量,检测波长为287、299 nm,溶剂为0.1 mol/L盐酸溶液;用紫外分光光度法中等波长消去法消除甲磺酸培氟沙星干扰,测定安乃近含量,检测波长为261、291 nm,溶剂仍为0.1 mol/L盐酸溶液;整个过程采用棕色容量瓶避光操作.测定甲磺酸培氟沙星含量的回归方程为:ΔA1=0.089 936 C1,r1=0.999 6,平均回收率99.66%,RSD=0.61%;测定安用近含量的回归方程为:ΔA2=0.024 888 C2,r2=0.999 6,平均回收率99.81%,RSD=0.41%.本方法简单、快速、易于操作.  相似文献   

3.
测定甲磺酸培氟沙星在276nm波长处的紫外吸收系数,结果E1cm^1%为995,RSD为0.5%,用其测定甲磺酸培氟沙星制剂的含量,与《兽药质量标准》(1996年版)对照品法比较,结果令人满意。  相似文献   

4.
目的:制备优良的注射用甲磺酸培氟沙星。方法:采用正交设计试验,考察其影响因素,对工艺进行研究。结果:最佳甘露醇的量、活性炭的加入量和抗氧剂分别为0.1g/瓶、0.05%、0.01%亚硫酸氢钠和0.01%依地酸钙钠。结论:按该方法制备的注射用甲磺酸培氟沙星,完全符合质量标准。  相似文献   

5.
对人工感染鸡白痢的艾维茵雏鸡,采用"雏痢净"按高(0.5/只)、中(0.4/只)和低(0.3/只)三个剂量混饲治疗,用2%甲磺酸培氟沙星(药物对照组)、感染不用药(阳性对照组)、不感染不用药(阴性对照组)作为对照.结果"雏痢净"高、中、低剂量组与2%甲磺酸培氟沙星组对雏鸡白痢均有较高的疗效,其中"雏痢净"高、中剂量组与2%甲磺酸培氟沙星组的治疗效果最好,但三者差异不显著(P>0.05);"雏痢净"各组与2%甲磺酸培氟沙星组的相对增重率极显著高于感染不用药组(p0.01).表明"雏痢净"高、中剂量用药后症状明显减轻且渐恢复,体重也明显增加,其疗效与2%甲磺酸培氟沙星相当.  相似文献   

6.
对人工感染鸡白痢的艾维茵雏鸡采用"雏痢净"按高(0.5 g/只)、中(0.4 g/只)、低(0.3 g/只)三个剂量混饲治疗,用2%甲磺酸培氟沙星(药物对照)组、感染不用药(阳性对照)组、不感染不用药(阴性对照)组作为对照.结果:"雏痢净"高、中、低剂量组与2%甲磺酸培氟沙星组对雏鸡白痢均有较高的疗效,其中"雏痢净"高、中剂量组与2%甲磺酸培氟沙星组的治疗效果最好,但三者差异不显著(P>0.05);"雏痢净"各组与2%甲磺酸培氟沙星组的相对增重率极显著高于感染不用药组(P<0.01).研究表明,"雏痢净"高、中剂量组雏鸡用药后症状明显减轻且渐恢复,体重也明显增加,其疗效与2%甲磺酸培氟沙星相当.  相似文献   

7.
"雏痢净"对人工感染雏鸡白痢的疗效研究   总被引:1,自引:0,他引:1  
对人工感染鸡白痢的艾维茵雏鸡,采用“雏痢净”按高(0.5g/只)、中(0.4g/只)和低(0.3g/只)三个剂量混饲治疗,用2%甲磺酸培氟沙星(药物对照组)、感染不用药(阳性对照组)、不感染不用药(阴性对照组)作为对照。结果:“雏痢净”高、中、低剂量组与2%甲磺酸培氟沙星组对雏鸡白痢均有较高的疗效,其中“雏痢净”高、中剂量组与2%甲磺酸培氟沙星组的治疗效果最好,但三者差异不显著(P>0.05);“雏痢净”各组与2%甲磺酸培氟沙星组的相对增重率极显著高于感染不用药组(P<0.01)。表明:“雏痢净”高、中剂量用药后症状明显减轻且渐恢复,体重也明显增加,其疗效与2%甲磺酸培氟沙星相当。  相似文献   

8.
本文报道了甲磺酸培氟沙星注射液处方工艺的研究。研究表明:采用0.1%的亚硫酸氢钠作抗氧剂,并调节pH值为3.5~5.5时,本品见光不易发生氧化变色,具有较好的稳定性。  相似文献   

9.
为了选择敏感药物以避免抗药性的产生,选用新霉素、头孢噻肟钠、甲磺酸培氟沙星等8种抗菌药对东北地区主要养鸡场分离出的优势血清型致病性大肠埃希菌进行药敏试验.结果8种抗菌药的抑菌圈直径分别是氟苯尼考30 mm,头孢噻污钠28 mm,新霉素27 mm,甲磺酸培氟沙星21 mm,丁胺卡那25 mm ,磷霉素钙19 mm,庆大霉素6 mm,阿莫西林15 mm.根据药物敏感试验结果表明,抑菌作用较强的为氟苯尼考、头孢噻肟钠和新霉素.  相似文献   

10.
1%甲磺酸培氟沙星对犬胃肠炎的治疗效果黄玉庭闵华1黄劲虹兰贤文2广西南宁市畜牧兽医站南宁530001;1广西农业学校;2广西农大兽医系毕业实习生培氟沙星(pefloxacin)为一新型氟喹诺酮类药物,具有抗菌活性强、抗菌谱广,临床效果好等特点。对动物...  相似文献   

11.
1. In this study we investigated the residues of fluoroquinolone drugs (ciprofloxacin and pefloxacin) in the cloacal gland (a site of foam synthesis) and other tissues such as breast muscle, testes, brain, kidney and plasma. 2. Fifty-four healthy male Japanese quail were selected at random from a flock, maintained under uniform husbandry conditions and divided into three groups, each of 18 birds. Group I (control) received 1 ml vehicle (normal saline 0.9% (w/v) NaCl) daily for 12 d through the intraperitoneal route. Birds of groups II and III received ciprofloxacin and pefloxacin by the same route at the rate of 10 and 12 mg/kg body weight, respectively, every day for a similar period. 3. Birds from each group were killed, at 1, 5 and 10 d after the cessation of treatment, to collect the cloacal gland together with other tissues that were analysed for residual drugs. 4. Cloacal gland retained the maximum drug residues of ciprofloxacin (60%) and pefloxacin (80%) on d 10 compared with that on d 1 after drug withdrawal. The drug residues were found 60 and 80% in ciprofloxacin and pefloxacin groups, respectively, in the cloacal gland tissue even on d 10 after withdrawal of the treatment. 5. In the ciprofloxacin-treated group, all tissues except cloacal gland contained very small amounts of the drug residues on d 10 after treatment ended. In the pefloxacin group the cloacal gland, breast muscle and kidney retained a fairly high amount of drug even on d 10 after treatment ceased. No residues of pefloxacin were detectable in testes and brain throughout. 6. In conclusion, the cloacal gland in Japanese quail acted as the largest sink for the fluoroquinolone drugs. Ciprofloxacin was more widely distributed in different tissues and persisted for a shorter period than pefloxacin.  相似文献   

12.
建立了氟苯尼考注射液、柴胡注射液中非法添加培氟沙星、洛美沙星的HPLC-PDA检查方法。采用十八烷基硅烷键合硅胶为填充剂;以磷酸溶液-乙腈-甲醇(85.5∶7.0∶7.5)为流动相;二极管阵列检测器,提取波长为277 nm。通过液相色谱保留时间、峰纯度检查和光谱相似度检查对非法添加物进行确证。结果表明,该色谱条件下培氟沙星、洛美沙星与其他物质分离良好。培氟沙星在氟苯尼考注射液、柴胡注射液中的平均回收率分别为101.4%(RSD=0.2%)、100.0%(RSD=0.4%),洛美沙星在氟苯尼考注射液、柴胡注射液中的平均回收率分别为101.2%(RSD=0.1%)、99.8%(RSD=0.5%)。本方法简便、准确、可靠,可用于检查氟苯尼考注射液、柴胡注射液中非法添加的培氟沙星、洛美沙星。  相似文献   

13.
1. The pharmacokinetics of pefloxacin and its active metabolite norfloxacin were investigated in chickens after a single oral administration of pefloxacin at a dosage of 10 mg/kg. To characterise the residue pattern, another group of chickens was given 10 mg of pefloxacin/kg body once daily for 4 d by oral route; the tissue concentrations of pefloxacin and norfloxacin were determined at 1, 5 and 10 d after the last administration of the drug. 2. The concentrations of pefloxacin and norfloxacin in plasma and tissues were determined by HPLC assay. The limit of detection for pefloxacin and norfloxacin was 0.03 microg/ml in plasma or microg/g in tissue. 3. The plasma concentration-time data for pefloxacin and norfloxacin were characteristic of a one-compartment open model. The elimination half-life, maximum plasma drug concentration, time to reach maximum plasma drug concentration and mean residence time of pefloxacin were 8.74 +/- 1.48 h, 3.78 +/- 0.23 microg/ml, 3.33 +/- 0.21 h and 14.32 +/- 1.94 h, respectively, whereas the respective values of these variables for norfloxacin were 5.66 +/- 0.81 h, 0.80 +/- 0.07 microg/ml, 3.67 +/- 0.21 h and 14.44 +/- 0.97 h. 4. Pefloxacin was metabolised to norfloxacin to the extent of 22%. 5. The concentrations of pefloxacin (microg/g) 24 h after the fourth dose of the drug declined in the following order: liver (3.20 +/- 0.40) > muscle (1.42 +/- 0.18) > kidney (0.69 +/- 0.04) > skin and fat (0.06 +/- 0.02). Norfloxacin was also detectable in all the tissues analysed except muscle. No drug and/or its metabolite was detectable in tissues except skin and fat 5 d after the last administration. The concentrations of pefloxacin and norfloxacin in skin and fat 10 d after the last dose of pefloxacin were 0.04 +/- 0.02 and 0.03 +/- 0.01 microg/g, respectively.  相似文献   

14.
The clinical efficacy of the lazaroid, tirilazad mesylate, a new therapeutic agent for prophylaxis and treatment of endotoxemia, was evaluated in 24 neonatal Holstein calves. Endotoxemia was induced by IV infusion of commercial Escherichia coli lipopolysaccharide (3.25 micrograms/kg of body weight) over 3 hours. Group-1 calves were given endotoxin alone; group-2 calves were given an infusion of 0.9% sterile saline solution, then were treated with tirilazad mesylate (1.5 mg/kg) 1 hour after the infusion was started. Group-3 calves were treated with tirilazad mesylate 1 hour after the start of the endotoxin infusion, and group-4 calves were given tirilazad mesylate 1 hour before the start of the endotoxin infusion. Clinical signs of endotoxemia were mitigated by tirilazad mesylate. In addition, tirilazad mesylate protected calves from endotoxin-induced hyperglycemia; treatment after endotoxin infusion decreased the severity of hypoglycemia and prevented lactic acidosis. Treatment with tirilazad mesylate after initiation of endotoxin infusion was as protective as was pretreatment.  相似文献   

15.
采用荧光分光光度法测定了甲磺酸达氟沙星粉的含量。激发和发射波长分别为350nm和448 nm,平均回收率为102.5%,RSD为1.1%。在0.01~5μg/mL范围内,其荧光强度与浓度线性关系良好。  相似文献   

16.
This study evaluated the in vitro activity of masitinib mesylate against canine hemangiosarcoma (HSA) cell lines after treatment with increasing concentrations of masitinib mesylate (0.01-100?μM) for 24, 48 and 72 h. Results indicated that masitinib mesylate caused a dose- and time-dependent decrease in HSA cell proliferation. The 50% inhibitory concentration (IC(50) ) at 72 h for three HSA cell lines (DEN, Fitz and SB) was found to be 8.56, 9.41 and 10.65?μM, respectively. Further investigation demonstrated that masitinib mesylate induced apoptosis in all HSA cell lines, including activation of caspase-3/7. Measurement of VEGF levels in cell supernatant found a statistically significant increased VEGF in close proximity to the IC(50) of each cell line followed by a decline back towards baseline. These findings indicate that masitinib mesylate causes dose-dependent HSA cell death in vitro and supports future clinical trials of masitinib for canine HSA.  相似文献   

17.
The pharmacokinetics of orally administered pefloxacin were studied to evaluate the bio-enhancing effect of the herbal bio-enhancer, trikatu, in mountain Gaddi goats (n = 6). The findings of the study revealed a decreased plasma concentration (p > 0.05) of pefloxacin following trikatu administration during the absorption phase (10, 15, 20 min post pefloxacin administration). In contrast, the plasma concentrations of pefloxacin were significantly higher at 4, 6, 8 and 12 h (during the elimination phase) of the pefloxacin administration. The findings of the investigation revealed higher values for the area under the curve, the area under the first moment of the plasma drug concentration time curve, the mean residential time, the total duration of pharmacological action and bioavailability. Trikatu treatment, however, significantly reduced the elimination half life (t1/2β) and zero time intercept of the elimination phase. The apparent volume of distribution based on the total area under the plasma drug concentration curve [(Vd(area)] and the apparent volume of distribution based on the zero time plasma concentration intercept of the elimination phase [Vd(B)] were significantly higher in trikatu treated animals indicating a better penetration of the drug. Based on the MIC of 0.8 µg/ml of pefloxacin, a priming dose of 6.0 mg/kg and a maintenance dose of 2.21 mg/kg is required to be administered at 8 h intervals. For practical purposes in goats this would mean a priming dose of 6 mg/kg and a maintenance dose of 2 mg/kg given by the oral route, to be repeated at 8 h intervals.  相似文献   

18.
BACKGROUND: Imatinib mesylate is a small molecule targeted at dysregulated protein-tyrosine kinase. Mutation of c-kit exon 11, which induces constitutive phosphorylation of KIT, is one of the mechanisms for the development or progression of mast cell tumor (MCT) in dogs. The purpose of this study was to examine the therapeutic potential of imatinib mesylate in canine MCT. HYPOTHESIS: Imatinib mesylate has activity against MCT in dogs, and response to treatment can be correlated to presence of mutation within exon 11 of c-kit. ANIMALS: Twenty-one dogs with MCT with gross tumor burden and median tumor size of 7.2 cm (range, 1.0-25.3 cm) before treatment. METHODS: Tumors were analyzed for mutation of c-kit exon 11. Imatinib mesylate was administered PO to the dogs at a dose of 10 mg/kg daily for 1-9 weeks. RESULTS: Ten of 21 dogs (48%) had some beneficial response to imatinib mesylate treatment within 14 days of treatment initiation. All 5 dogs with a demonstrable c-kit mutation in exon 11 responded to the drug (1 complete remission, 4 partial remission). CONCLUSIONS AND CLINICAL IMPORTANCE: Imatinib mesylate has clinical activity against MCT in dogs. Response could not be predicted based on presence of absence of a mutation in exon 11 of c-kit.  相似文献   

19.
The plasma concentrations and pharmacokinetics of the fluoroquinolone antimicrobial agent pefloxacin, following the administration of a single intravenous (10 mg/kg) or oral (20 mg/kg) dose, were investigated in healthy female goats. The antimicrobial activity in plasma was measured at predetermined times after drug administration by an agar well diffusion microbiological assay, using Escherichia coli (ATCC 25922) as the test organism. Concentrations of the drug 0.25 g/ml were maintained in plasma for up to 6 and 10 h after intravenous (IV) or oral administration of pefloxacin, respectively. The concentration–time data for pefloxacin in plasma after IV or oral administration conformed to two- and one-compartment open models, respectively. Plasma pefloxacin concentrations decreased rapidly during the initial phase after IV injection, with a distribution half-life (t 1/2 ) of 0.10±0.01 h. The terminal phase had a half-life (t 1/2 ) of 1.12±0.21 h. The volume of distribution at steady state (V dss), mean residence time (MRT) and total systemic clearance (ClB) of pefloxacin were 1.08±0.09 L/kg, 1.39±0.23 h and 821±88 (ml/h)/kg, respectively. Following oral administration of pefloxacin, the maximum concentration in the plasma (C max) was 2.22±0.48 g/ml and the interval from administration until maximum concentration (t max) was 2.3±0.7 h. The absorption half-life (t 1/2 ka), mean absorption time (MAT) and elimination half-life of pefloxacin were 0.82±0.40, 4.2±1.0 and 2.91±0.50 h, respectively. The oral bioavailability of pefloxacin was 42%±5.8%. On the basis of the pharmacokinetic data, a dosage regimen of 20 mg/kg, IV at 8 h intervals or orally twice daily, is suggested for treating infections caused by drug-sensitive pathogens in goats.  相似文献   

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