共查询到20条相似文献，搜索用时 359 毫秒
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《科技视界》2014,(10)
目的:制备地氯雷他定片,并与原研市售制剂进行体外溶出行为一致性评价。方法:采用地氯雷他定原料药、乳糖、微晶纤维素和淀粉制备成地氯雷他定片后以欧巴代胃溶包衣液进行薄膜包衣。将自制的地氯雷他定片分别以pH=1.0的盐酸溶液,pH=4.5的醋酸盐缓冲液,pH=6.8的磷酸盐缓冲液及水为溶出介质,用浆法50r/min考察其在四种介质中的溶出行为,并采用f2相似因子评价其与原研片溶出行为的一致性。结果:自制地氯雷他定片与原研片在pH=1.0的盐酸溶液中15分钟溶出度均大于85%,在pH=4.5的醋酸盐缓冲液,pH=6.8的磷酸盐缓冲液及水中溶出曲线相似因子f2值分别为69,81及71。结论:自制地氯雷他定片与原研片在体外4种溶出介质中溶出行为均相似。 相似文献
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本试验旨在评价延胡索酸泰妙菌素口服固体受试制剂和参比制剂的体外溶出度。试验采用桨法测定溶出度,50rpm/min,溶出介质分别为pH1.2盐酸溶液、pH3.8醋酸盐缓冲液、pH4.8磷酸盐缓冲液、pH6.8磷酸盐缓冲液和水,温度37±0.5℃,参比制剂和受试制剂0.34g/杯,取样时间为第1、2、5、10、15、30、45和60min,高效液相色谱法检测药物成分含量。结果表明延胡索酸泰妙菌素在溶出介质中比较稳定,受试制剂和参比制剂在15min内的溶出率大于85%,在五个溶出介质中的差异因子(f1)小于15%。因此,受试制剂和参比制剂的溶出行为相似,生物利用度不受溶出行为的限制。 相似文献
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《畜牧兽医学报》2015,(6)
为研究头孢泊肟酯与牛至油在纳米水平的联合药效,首次制备复方头孢泊肟酯纳米乳并进行体外抑菌试验及急性毒性研究。在传统纳米乳制备方法筛选初步处方基础上,采用多指标正交试验法确定最优处方。以L9(34)正交表设计试验,以抑菌圈直径和纳米乳稳定常数Ke为考察指标,选择头孢泊肟酯和牛至油质量分数比(A)、纳米乳水相pH(B)、乳化温度(C)作为考察因素;体外抑菌试验采用微量肉汤稀释法;急性毒性试验采用最大耐受剂量法并进行了组织病理学检查。结果显示:针对致病性大肠杆菌、沙门菌最优处方为头孢泊肟酯0.33%、牛至油2.67%、1,2-丙二醇1.13%、EL-40 22.51%、蒸馏水73.36%,纳米乳pH值为6.17;与原料药相比,受试药物的最低抑菌浓度和最低杀菌浓度差异显著(P0.05);小鼠经口急性毒性最大耐受剂量大于1 800mg·kg-1,为低毒级药物,无肾、肠毒性,但可引起肝轻微病理损伤。结果表明,牛至油在纳米水平提高了致病性大肠杆菌、沙门菌、奇异变形杆菌、巴氏杆菌、痢疾杆菌、金黄色葡萄球菌、无乳链球菌对头孢泊肟酯敏感性。 相似文献
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HPLC法测定硫酸头孢喹肟冻干粉针中硫酸头孢喹肟含量 总被引：3，自引：0，他引：3
建立高效液相色谱法(HPLC法)测定硫酸头孢喹肟冻干粉针中硫酸头孢喹肟的含量。色谱条件为色谱柱Kromasil C18柱(250 mm×4.6 mm,5μm),以高氯酸钠-磷酸-三乙胺缓冲液(pH3.6):乙腈(体积比90∶10)为流动相,流速为0.8 mL/min,紫外检测波长为254 nm。结果表明,硫酸头孢喹肟在0.05~25μg/mL范围内呈良好的线性关系,r=0.99 96,平均回收率为100.34%(n=9),RSD为1.34%。该方法简便快速,结果准确可靠,可用于硫酸头孢喹肟冻干粉的质量控制研究。 相似文献
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对自制的硫酸头孢喹肟混悬剂进行质量检验和体外抑菌实验。按照筛选出的配方,应用分散法制备硫酸头孢喹肟混悬型制剂,检验混悬剂的质量并针对临床分离的奶牛乳房炎混合菌株进行体外抑菌实验。结果表明：制得的硫酸头孢喹肟混悬剂符合国家质量标准要求,体外抑菌实验效果明显。 相似文献
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通过考察3种替米考星颗粒制剂在酸性溶液和缓冲液中的释放情况，为新制剂的进一步研发和临床应用提供理论依据。采用高效液相色谱法对3种不同制剂中替米考星的含量及其体外溶出度进行测定。色谱柱选择Hypersil ODS-2 C18(4.6 mm×250 mm, 5μm),以水∶乙腈∶四氢呋喃∶磷酸二丁胺(790∶130∶55∶25)为流动相，流速1.0 mL/min,检测波长290 nm,柱温30℃。分别以盐酸溶液和磷酸盐缓冲液为溶出介质，测定3种新研制的替米考星不同制剂体外溶出曲线，溶出方法选用浆法，转速为75 r/min,温度为37℃±0.5℃。在所建立的方法学基础上，替米考星在10μg/mL～1000μg/mL范围内与峰面积呈良好的线性关系，在90 min时3种新研制的替米考星不同制剂在酸性溶液中的溶出度分别为100%、5.73%和8.29%,供试品1与供试品2、供试品3及对照品之间差异显著(P<0.05),供试品2、供试品3与对照品之间无明显差异；120 min时3种新研制的替米考星不同制剂在磷酸盐缓冲液中的累积溶出度分别为100%、97.53%和93.60%,3种供试品与对照品... 相似文献
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为研究国产和进口硫酸头孢喹肟注射液(7.5%)在猪体内的药代动力学特征和生物等效性,采用双处理、双周期随机交叉试验设计,将20头健康三元杂交猪随机分成2组,按3mg/kg体重分别单剂量肌内注射受试制剂和参比制剂。采用超高效液相色谱-串联质谱法测定血浆中头孢喹肟的浓度,利用Win Nonlin6.3软件计算主要药动学参数,并评价两种制剂的生物等效性。结果显示,受试制剂和参比制剂的Tmax分别为2.30±0.73h和2.25±0.55h;Cmax分别为2.37±0.34μg/mL和2.45±0.36μg/mL;AUC0-t分别为26.38±2.30μg·h·mL^-1和24.86±2.19μg·h·mL^-1;AUC0-∞分别为26.74±2.34μg·h·mL^-1和25.07±2.20μg·h·mL^-1。硫酸头孢喹肟注射液受试制剂和参比制剂的AUC0-t、AUC0-∞、Cmax、Tmax均无显著性差异(P>0.05)。双单侧t检验结果显示两种制剂生物等效,临床上可相互替代。该试验可为兽医临床合理用药提供参考。 相似文献
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Brown SA Boucher JF Hubbard VL Prough MJ Flook TF 《Journal of veterinary pharmacology and therapeutics》2007,30(4):320-326
The pharmacokinetic properties of cefpodoxime, and its prodrug, cefpodoxime proxetil, were evaluated in two separate studies, one following intravenous (i.v.) administration of cefpodoxime sodium and the second after oral (p.o.) administration of cefpodoxime proxetil to healthy dogs. After cefpodoxime administration, serial blood samples were collected and plasma concentrations were determined by high performance liquid chromatography (HPLC). A single i.v. administration of cefpodoxime sodium at a dose of 10 mg cefpodoxime/kg body weight resulted in a cefpodoxime average maximum plasma concentration (Cmax) of 91 (+/-17.7) microg/mL, measured at 0.5 h after drug administration, an average half-life (t1/2) of 4.67 (+/-0.680) h, an average AUC(0-infinity) of 454 (+/-83.1) h.microg/mL, an average V(d(ss)) of 151 (+/-27) mL/kg, an average Cl(B) of 22.7 (+/-4.2) mL/h/kg and an average MRT(0-infinity) of 5.97 (+/-0.573) h. When dose normalized to 10 mg cefpodoxime/kg body weight, cefpodoxime proxetil administered orally resulted in Cmax of 17.8 +/- 11.4 microg/mL for the tablet formulation and 20.1 +/- 6.20 microg/mL for the suspension formulation and an average AUC(0-LOQ) of 156 (+/-76.1) h.microg/mL for the tablet formulation and 162 (+/-48.6) h.microg/mL for the suspension formulation. Relative bioavailability of the two oral formulations was 1.04 (suspension compared with tablet), whereas the absolute bioavailability of both oral formulations was estimated to be approximately 35-36% in the cross-study comparison with the i.v. pharmacokinetics. Combined with previous studies, these results suggest that a single daily oral dose of 5-10 mg cefpodoxime/kg body weight as cefpodoxime proxetil maintains plasma concentrations effective for treatment of specified skin infections in dogs. 相似文献
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建立了德拉昔布咀嚼片溶出度测定的高效液相色谱法,并对德拉昔布咀嚼片和Deramaxx咀嚼片的溶出度进行比较。方法为浆法,转速为50 r/min,0.8%十二烷基硫酸钠为溶出介质,于5、10、15、20、30、40、50 min分别采样;采用Waters XSelect H88 C18(4.6 mm×250 mm,5μm)色谱柱,磷酸盐缓冲液(pH4.5)-乙腈(52∶48,V/V)为流动相,检测波长252 nm;柱温30℃;外标法定量。结果表明,德拉昔布在5~25μg/mL浓度范围内线性良好(r2=0.9992),检测限与定量限分别为0.81μg/mL、2.57μg/mL;平均回收率为101.8%±0.91%;德拉昔布咀嚼片与Deramaxx溶出度在30 min内分别为87.78%±1.91%和88.76%±2.05%,符合规定。试验所建立的方法简便、准确、专属性强,可用于德拉昔布咀嚼片的溶出度测定。 相似文献
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Carrillo NA Giguère S Gronwall RR Brown MP Merritt KA O'Kelley JJ 《American journal of veterinary research》2005,66(1):30-35
OBJECTIVES: To determine the disposition of orally administered cefpodoxime proxetil in foals and adult horses and measure the minimum inhibitory concentrations (MICs) of the drug against common bacterial pathogens of horses. ANIMALS: 6 healthy adult horses and 6 healthy foals at 7 to 14 days of age and again at 3 to 4 months of age. PROCEDURE: A single dose of cefpodoxime proxetil oral suspension was administered (10 mg/kg) to each horse by use of a nasogastric tube. In 7- to 14-day-old foals, 5 additional doses were administered intragastrically at 12-hour intervals. The MIC of cefpodoxime for each of 173 bacterial isolates was determined by use of a commercially available test. RESULTS: In 7- to 14-day-old foals, mean +/- SD time to peak serum concentration (Tmax) was 1.7 +/- 0.7 hours, maximum serum concentration (Cmax) was 0.81 +/- 0.22 microg/mL, and elimination half-life (harmonic mean) was 7.2 hours. Disposition of cefpodoxime in 3- to 4-month-old foals was not significantly different from that of neonates. Adult horses had significantly higher Cmax and significantly lower Tmax, compared with values for foals. The MIC of cefpodoxime required to inhibit growth of 90% of isolates for Salmonella enterica, Escherichia coli, Pasteurella spp, Klebsiella spp, and beta-hemolytic streptococci was 0.38, 1.00, 0.16, 0.19, and 0.09 microg/mL, respectively. CONCLUSIONS AND CLINICAL RELEVANCE: Oral administration at a dosage of 10 mg/kg every 6 to 12 hours would appear appropriate for the treatment of equine neonates with bacterial infections. 相似文献
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为了建立了维他昔布咀嚼片体外溶出度的测定方法,以0.8％十二烷基硫酸钠溶液为溶出介质,采用桨法(50 r/min),用紫外-可见分光光度法测定溶出度.结果显示,维他昔布浓度在0.002496 ～0.017472 mg/mL范围内,与吸收度呈良好的线性关系(r=0.9995),加样回收率为102.9％(RSD为1.36％),三批样品30 min时溶出度在80％以上.建立的溶出度测定方法重现性,均一性良好,样品溶出度大于80％,可用于维他昔布咀嚼片中溶出度的测定. 相似文献
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Kumar V Madabushi R Lucchesi MB Derendorf H 《Journal of veterinary pharmacology and therapeutics》2011,34(2):130-135
Kumar, V., Madabushi, R., Lucchesi, M. B. B., Derendorf, H. Pharmacokinetics of cefpodoxime in plasma and subcutaneous fluid following oral administration of cefpodoxime proxetil in male beagle dogs. J. vet. Pharmacol. Therap. 34 , 130–135. Pharmacokinetics of cefpodoxime in plasma (total concentration) and subcutaneous fluid (free concentration using microdialysis) was investigated in dogs following single oral administration of prodrug cefpodoxime proxetil (equivalent to 5 and 10 mg/kg of cefpodoxime). In a cross over study design, six dogs per dose were utilized after a 1 week washout period. Plasma, microdialysate, and urine samples were collected upto 24 h and analyzed using high performance liquid chromatography. The average maximum concentration (Cmax) of cefpodoxime in plasma was 13.66 (±6.30) and 27.14 (±4.56) μg/mL with elimination half‐life (t1/2) of 3.01 (±0.49) and 4.72 (±1.46) h following 5 and 10 mg/kg dose, respectively. The respective average area under the curve (AUC0–∞) was 82.94 (±30.17) and 107.71 (±30.79) μg·h/mL. Cefpodoxime was readily distributed to skin and average free Cmax in subcutaneous fluid was 1.70 (±0.55) and 3.06 (±0.93) μg/mL at the two doses. Urinary excretion (unchanged cefpodoxime) was the major elimination route. Comparison of subcutaneous fluid concentrations using pharmacokinetic/pharmacodynamic indices of fT>MIC indicated that at 10 mg/kg dose; cefpodoxime would yield good therapeutic outcome in skin infections for bacteria with MIC50 upto 0.5 μg/mL while higher doses (or more frequent dosing) may be needed for bacteria with higher MICs. High urine concentrations suggested cefpodoxime use for urinary infections in dogs. 相似文献
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R. G. COOKE A. KNIFTON D. B. MURDOCH I. S. YACOUB† 《Journal of veterinary pharmacology and therapeutics》1981,4(1):11-13
Plasma oxytetracycline concentrations were studied in four healthy beagles after oral administration of four different commercial preparations of oxytetracycline dihydrate tablets. Although no statistically significant differences were found in the biological availability between the four tablets, assessed by the peak plasma level and the area under the plasma concentration—time curve, there was great variation in the plasma concentrations of oxytetracycline achieved in the sixteen experiments. This variation was not related to the in vitro dissolution properties of the tablets. As the amount of oxytetracycline dihydrate administered in die experiments was almost the maximum recommended dose and the mean peak plasma concentrations were either below or at the lower end of the therapeutic concentration range, it is suggested that higher oral doses than those officially recommended are required to attain effective plasma levels. 相似文献
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K. Hamamoto R. Koike & Y. Machida 《Journal of veterinary pharmacology and therapeutics》2001,24(5):333-341
The effect of soybean oil refuse powder (SOR) when used as a vehicle on the absorption of oxolinic acid (OXA) powder in chicken, the dissolution profile of OXA and the correlation between in vivo and in vitro study were examined. To examine in vivo bioavailability, chickens fed or fasted were studied using a 2 x 2 crossover design. The OXA was administered OXA or OXA-SOR (1 : 9) mixture 20 mg OXA/kg. In vitro dissolution rates for OXA and OXA-SOR were measured using the paddle (PD) and the rotatory dialysis cell dissolution (PTSW) methods. Maximum plasma concentration (Cmax) and area under the curve (AUC) were significantly increased by the addition of SOR to OXA. Differences between OXA and OXA-SOR were more remarkable under fasted as compared with fed condition. In vitro dissolution rates of OXA-SOR pH 1.2, 6.5 and 7.2 as determined by the PD and the PTSW methods were increased in the presence of SOR vehicle. Differences between OXA and OXA-SOR in vitro dissolution rates were greater than in vivo bioavailability. Correlation between in vitro release (%) and in vivo absorption (%) showed good linearity (gamma=0.8805-0.9999). 相似文献
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为检测麻杏石甘散、氟苯尼考注射液中非法添加的盐酸溴己新,甘草颗粒中非法添加的吲哚美辛,以十八烷基键合硅胶为填充剂,磷酸盐缓冲液-乙腈(20∶80)为流动相检测盐酸溴己新,以乙腈-0.1mol/L冰醋酸溶液(50∶50)为流动相检测吲哚美辛,流速为1.0 m L/min,波长扫描范围为200~400 nm,建立了相应的HPLC-PAD检测方法,并采用峰纯度检查和光谱相似度检查辅助对照品比对方法,对非法添加药物进行确证。结果显示,麻杏石甘散和氟苯尼考注射液中盐酸溴己新的回收率分别为94.8%和98.5%,甘草颗粒中吲哚美辛回收率为95.2%;盐酸溴己新线性方程为y=14780200x-16476,R=0.9999,吲哚美辛线性方程为y=10995430x+13033,R=0.9999;麻杏石甘散中盐酸溴己新检测限为83 mg/kg,氟苯尼考注射液中盐酸溴己新检测限为1.6 g/L,甘草颗粒中吲哚美辛检测限为1 g/kg。 相似文献