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几种复方制剂中硫酸庆大霉素含量的测定余莲广西兽药监察所５３０００１“抗菌退热灵”、“复方庆大霉素注射液”、“霍痢灵”和“炎痢净”都是硫酸庆大霉素的复方制剂，临床试验表明：ＴＭＰ、痢菌净等能减少硫酸庆大霉素的副作用，增强疗效，但严重影响制剂中硫酸庆大霉... 相似文献
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庆大霉素及复方庆大霉素在小猪体内的药物代谢动力学研究 总被引：4，自引：0，他引：4
本试验分别用硫酸庆大霉素及复方庆大霉索在14头小猪(体重16.71±4.2千克)进行单剂量给药的药代动力学研究。结果说明肌注该药吸收迅速而完全,第一小时末已吸收剂量的98.8％,表观生物利用度达92±6％。除吸收外静注及肌注表现的药代动力学特征无显著差别。复方制剂的庆大霉素从中央室消除明显加快。庆大霉素与TMP的生物半衰期分别为1.81±0.17及1.81±1.04小时,药代动力学参数说明这两种药物的配合是基本相适应的。本试验采用平衡透析法测定庆大霉素的血清蛋白结合率为46.5±5.2％,TMP共存时下降至25.0±2.8％。血药浓度表明庆大霉素肌注剂量3mg/kg是合适的,而静注建议酌减。本文还按病原菌不同的敏感性给出多剂量肌注给药方案。 相似文献
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将硫酸庆大霉素与大肠埃希菌血清抗体用化学修饰剂进行偶联,再经适当的化学方法处理,按照制剂学原理制备成靶向硫酸庆大霉素,经电镜检测,可以清楚的看到抗体球蛋白上附着的硫酸庆大霉素药物颗粒。应用间接ELISA法检测靶向硫酸庆大霉素结合物的免疫原性。结果表明,结合物存在微弱的免疫原性,但与大肠埃希菌血清抗体相比,免疫原性已经大为减弱,说明靶向硫酸庆大霉素复合物中,化学修饰剂不仅扮演偶联物的角色,还减弱了结合物中大肠埃希菌血清抗体的免疫原性,对靶向硫酸庆大霉素结合物的药动学和药效学几乎无影响。 相似文献
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应用药物累积法研究复方中药Ⅱ的药代动力学研究 总被引：1，自引：0，他引：1
中药药代动力学的研究对指导新药设计,改进药物剂型,改进给药方案,筛选高效、长效、低毒副作用的药物及指导临床用药等方面发挥重大作用。中药药代动力学的研究可分两部分:一部分为中药有效成分明确的药代动力学研究,另一部分是有效成分不明确的中药和中药制剂的药代动力学研究[1],方法有两种。第一种是药理效应法。第二种是药物累积法。用药物累积法研究药代动力学的方法有两种。第一种是以动物死亡率作为观察指标的“累积法”:即多组动物按不同间隔时间给药,求出不同时间体存百分率的动态变化情况,从而计算药动学参数[1]。赫梅生用此法对… 相似文献
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为分析硫酸庆大霉素在健康和鸡大肠杆菌感染鸡体内的药物动力学特征,试验通过给健康鸡腹腔注射大肠杆菌O157,以临床症状、病理剖检和微生物检查为指标,成功建立鸡大肠杆菌感染模型。选取健康鸡和患病鸡各8只,分别以20 mg/kg体重单剂量肌内注射硫酸庆大霉素,分别于0.167、0.25、0.5、0.75、1、2、3、4、6、8和12 h时间点采血,采用管碟法测定血浆中庆大霉素的浓度。结果显示:试验所建立的标准曲线相关性好,相关系数均达0.990以上,日内、日间变异系数均小于10%。肌注给药后,硫酸庆大霉素在鸡体内吸收迅速,房室模型分析表明,健康鸡与患病鸡药时数据均符合有二室开放模型,硫酸庆大霉素在健康鸡体内峰浓度(Cmax)为(15.01±3.51)μg/mL,药时曲线下面积(AUC)为(100.79±5.14)μg/mL·h,消除半衰期(t1/2β)为(4.41±1.32)h,达峰时间(Tp)为(1.27±0.50)h。硫酸庆大霉素在患病鸡体内峰浓度(Cmax)为(12.50±2.19)μg/mL,药时曲线下面积(AUC)为(83.38±4.19)μg/mL·h,消除半衰期(t1/2β)为(4.18±1.17)h,达峰时间(Tp)为(0.97±0.05)h。结果表明:硫酸庆大霉素在患病鸡体内的峰浓度和药时曲线下面积低于健康鸡(P<0.05),因此对于已感染大肠杆菌的病鸡可以考虑适当增加给药剂量。 相似文献
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自制药敏纸片对鸡致病性大肠杆菌的耐药性检验 总被引：5，自引：1，他引：4
用自行制备药敏试验纸片，对某中型鸡场的鸡源致病性大肠杆菌进行了９种抗菌药物的敏感性体外试验。结果表明：硫酸新霉素、盐酸环丙沙星为高度敏感；中草药制剂氯霉素为中度敏感；庆大霉素、卡那霉素、氟哌酸、大肠杆素菌净、氨苄青霉素为低度敏感性药物。 相似文献
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K F Bowman L P Dix J L Riond J E Riviere 《American journal of veterinary research》1986,47(7):1590-1596
Pharmacokinetics of ampicillin sodium (11 mg/kg), gentamicin sulfate (2.2 mg/kg), and combination ampicillin sodium-gentamicin sulfate were determined for serum and synovia of healthy horses given single-dose IV injection and were not found to be different from those from other reports; however, a prolonged terminal gamma-phase for gentamicin (8,498 +/- 1,842 minutes) in serum of horses was found to exist. Pharmacokinetic interaction between combination ampicillin sodium-gentamicin sulfate was not observed int he serum or synovia. Prediction of ampicillin sodium or gentamicin sulfate concentrations in synovia, based on serum-based pharmacokinetics, cannot be accomplished solely upon analysis of peripheral-compartment pharmacokinetics. However, once equilibrium is achieved between synovia and extracellular fluid in the peripheral compartment, the decrease in drug concentrations in synovia parallels that in serum. Therefore, after 6 hours, synovial concentrations of gentamicin sulfate can be predicted based on peripheral-compartment pharmacokinetics, using an appropriate correction factor. The significance of these findings need to be correlated with clinical conditions so that a pharmacostatistical model for the prediction of synovial concentrations of drug(s) during treatment of horses with septic arthritis can be developed. 相似文献
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抗菌增效剂属于人工合成的二氨基嘧啶类药物，此类药物与抗菌药物联合使用时会以特定的机制来增强抗菌药的药物活性。近年来，由于抗生素的广泛使用甚至滥用导致细菌耐药的问题日益显现，通过加入抗菌增效剂而研制出的新制剂可以提高抗菌药在动物体内的利用率、降低药物用量、增强药物疗效、降低兽药残留及减少细菌耐药性。文章分析了近年来甲氧苄啶、二甲氧苄啶和艾地普林与各类抗生素的联合使用制备的制剂产品，发现其对疾病的治疗效果普遍优于单独使用抗生素。同时，配合中药的使用对细菌耐药的问题有显著改善，为后期抗菌增效剂的研究打开新的局面。随着对兽药制剂的研究，其不再局限于简单的剂型，通过运用新技术、新材料研制出的制剂，针对不同的给药部位和给药途径可以对病患进行更精准的治疗，减少药物达到靶部位的时间，增加患病部位的药量，此思路可为后续的研发方向提供支持和参考。文章将对抗菌药-抗菌增效剂联用制剂的研发情况进行综述。 相似文献
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为研究制备壳聚糖-海藻酸钠载药微球的新方法,研究采用D相乳化法,结合微乳及胶体制备技术,以硫酸小檗碱为模型药物,以药物包封率为评价指标,应用单因素试验考察了氯化钙溶液浓度、海藻酸钠溶液浓度、壳聚糖溶液浓度,以及初次凝胶时间对微球性能的影响。应用响应面法筛选优化了载药微球的制备工艺。结果表明,在微球制备及药物包封率的影响因素中,海藻酸钠溶液浓度、氯化钙溶液浓度对评价指标的影响最大,其次是壳聚糖溶液浓度和初次凝胶时间,筛选优化的载药微球生产工艺条件为海藻酸钠溶液浓度1.57%,氯化钙溶液浓度2.13%,壳聚糖溶液浓度0.86%,初次凝胶时间30.71min,该条件下制备微球的平均粒径为329nm,药物包封率94.09%。验证试验证实,本工艺可制备优良的硫酸小檗碱壳聚糖-海藻酸钠微球,且制备工艺简便,生产效率高,本技术为微球制剂的产业化生产奠定了一定基础。 相似文献
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Conjugates of the Escherichia coli serum antibody (Ab) with the gentamicin sulfate (GM sulfate) have been evaluated for the assessment of their ability to eradicate E. coli in vitro. The combination of every component in the targeted drug is the amino of serum antibody and gentamicin sulfate combined with the hydroxyl of PEG6000 by hydrogen bond, which forms stable complexes. The half-life of this complex is 4.83 h, and it is non-toxic side effects and low immunogenic. After the combination of antibody and gentamicin sulfate, the targeting of antibody is quite good. In vitro anti-bacterial activity of gentamicin sulfate increased 1000 times, and the clinical curative effect enhanced 100 times, this means higher efficacy and safety. 相似文献
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S A Brown G L Coppoc J E Riviere V L Anderson 《American journal of veterinary research》1986,47(4):789-794
Dose-related changes in the pharmacokinetics of gentamicin sulfate were investigated in 9 sheep given 3, 10, or 20 mg/kg of body weight IV in a crossover design with a 24-day washout period. The pharmacokinetics of the 3 mg/kg single dose were compared with that of the terminal phase pharmacokinetics of 3 mg of gentamicin/kg IV every 8 hours for 7 days in 8 additional sheep. Serum concentrations were monitored for 21 to 24 days after the dose. Polyexponential equations were fit to each data set. The number of exponential terms was determined by optimizing the fit for each data set. The pharmacokinetics of the 3 mg/kg single dose were mainly described by triexponential equations. The 10 mg/kg and the 20 mg/kg single doses and the 3 mg/kg multiple-dose data were described by a tetraexponential equation. The elimination rate constant was significantly smaller (P less than 0.05) after the larger single doses, and the serum gentamicin clearance increased as the dose increased (P less than 0.05). The crossover design sequence had a significant effect on serum gentamicin clearance and the area under the curve normalized to unit dose (P less than 0.01). The final exponential phase was not detectable with the present assay sensitivity under the 3 mg/kg single dose. The triexponential equation underpredicted the terminal serum concentrations determined after the 3 mg/kg multiple dose, whereas the 4 phase equation overpredicted the same terminal serum concentrations, perhaps reflecting saturation of the tissue pools that were mirrored by the serum gentamicin concentrations after 24 hours. The present study emphasized the complexity of the terminal phase gentamicin. pharmacokinetics and acknowledged the need for a long-term washout period when using the crossover design for gentamicin pharmacokinetic studies. 相似文献
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《Research in veterinary science》2012,92(3):e136-e143
Conjugates of the Escherichia coli serum antibody (Ab) with the gentamicin sulfate (GM sulfate) have been evaluated for the assessment of their ability to eradicate E. coli in vitro. The combination of every component in the targeted drug is the amino of serum antibody and gentamicin sulfate combined with the hydroxyl of PEG6000 by hydrogen bond, which forms stable complexes. The half-life of this complex is 4.83 h, and it is non-toxic side effects and low immunogenic. After the combination of antibody and gentamicin sulfate, the targeting of antibody is quite good. In vitro anti-bacterial activity of gentamicin sulfate increased 1000 times, and the clinical curative effect enhanced 100 times, this means higher efficacy and safety. 相似文献
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C M Smith E P Steffey J D Baggot C I Dunlop T B Farver 《American journal of veterinary research》1988,49(1):19-22
Inhalation anesthetics decrease the clearance of some drugs that are eliminated by renal excretion. The purpose of the study reported here was to investigate the effects of halothane anesthesia on the pharmacokinetics and urinary excretion of gentamicin sulfate, using the horse as a model. Using a crossover design, pharmacokinetic values after a single IV dose of gentamicin (4 mg/kg) were compared in halothane-anesthetized and unanesthetized horses. Compared with unanesthetized horses, the anesthetized horses had significant decreases in total body clearance (P less than 0.01) and apparent volume of distribution (P less than 0.05), and a significant increase in half-life (P less than 0.05) of gentamicin. 相似文献