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本研究以0.1 mg/kg体重的剂量研究美洛昔康片在比格犬中的药代动力学和生物利用度。HPLC分析血浆中的药物浓度,WinNonlin 6.4非房室模型计算药动学参数。比格犬内服美洛昔康片后测得0~48 h美洛昔康的T1/2、Cmax、Tmax和AUC0-t分别为14.55 ± 2.18 h、296.16 ± 74.15 ng·mL-1、6.0 ± 0.00 h和6356.79 ± 1089.78 ng·h·mL-1;比格犬静脉注射美洛昔康溶液后,测得0~48 h美洛昔康的T1/2和AUC0-t分别为11.54 ± 4.18 h和5510.68 ± 1075.29 ng·h·mL-1。内服美洛昔康片剂的绝对生物利用度为115.35%。美洛昔康片在比格犬体内消除速率较慢,消除半衰期较长,在体内滞留时间较长,绝对生物利用度高,药物在体内作用时间较长等药动学特征。 相似文献
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Pharmacokinetics of minocycline in crucian carp (Carassius auratus) after intravenous and oral administration 
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下载免费PDF全文 Fan Yang Fang Yang Yurong Yang Tao Kong Guoyong Wang Dongying Bai 《Aquaculture Research》2018,49(8):2782-2787
The pharmacokinetic of minocycline was studied after a single intravenous as well as oral dose (5 mg/kg body weight) in crucian carp (Carassius auratus) reared in freshwater at 10°C. Plasma samples were randomly collected from six fish at each sampling time. Plasma concentrations were determined by high‐performance liquid chromatography and further subjected to noncompartmental analysis. Initial concentration of minocycline just after intravenous administration was calculated as 7.320 μg/ml, while the other parameters after intravenous injection were determined as flows: apparent elimination rate constant (λz) of 0.064 per hr, apparent elimination half‐life () of 10.82 hr, total body clearance (Cl) of 142.72 ml/hr/kg, volume of distribution (Vz) of 2,227.38 ml/kg and volume of distribution at steady‐state (Vss) of 1,937.08 ml/kg. While after oral administration, the λz, , mean absorption time (MAT), absorption half‐life (t1/2ka) and bioavailability were determined as 0.059 per hr, 11.74, 5.55, 3.84 hr, and 81.98%, respectively, and the peak concentration was observed as 1.474 ± 0.362 μg/ml at 8 hr. It was shown that minocycline was slowly but relatively completely absorbed, extensively distributed, and slowly eliminated in crucian carp. Based on the ratios of AUC0–24 hr/MIC90, a minocycline dosage of 5 mg/kg body weight administered intravenously or orally would be only effective to successfully treat crucian carp infected by bacterium with MIC values ≤0.25 μg/ml. 相似文献
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【目的】研究抗球虫药盐酸氯苯胍在家兔体内的药物代谢动力学特征及内服给药的生物利用度。【方法】16只健康新西兰大白兔,公母各半,分为2组,一组以2.00 mg·kg~(-1)单次静脉注射给药,另一组以100.00 mg·kg~(-1)单次内服给药,通过耳部静脉采血,并用HPLC-UV法检测血浆中的盐酸氯苯胍浓度。使用WinnonlinTM药动学软件非房室模型计算相关药动学参数,采用SPSS 16.0软件得到药时曲线图。【结果】兔静脉注射盐酸氯苯胍(2.00mg·kg~(-1))后,药-时曲线下面积为1.72μg·h·m L~(-1),血浆清除率为1.17 L·h~(-1)·kg~(-1),表观分布容积为2.87L·kg~(-1),消除半衰期为1.72 h;内服盐酸氯苯胍(100.00 mg·kg~(-1))后,药-时曲线下面积为6.33μg·h·m L~(-1),消除半衰期为8.94 h。盐酸氯苯胍2种给药方式的药动学参数均存在显著差异(P0.05),内服给药的生物利用度较低,仅为7.36%。【结论】盐酸氯苯胍静脉注射给药的表观分布容积较大,药物在兔组织中分布广泛,并且消除迅速;内服盐酸氯苯胍后,药物经肠道吸收的量较少,体内药物残留较低。 相似文献
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Antibacterial efficacy and pharmacokinetic evaluation of sanguinarine in common carp (Cyprinus carpio) following a single intraperitoneal administration 下载免费PDF全文
下载免费PDF全文 Sanguinarine (SA), with antimicrobial and antiparasitic activities against fish pathogens, exhibits great potential commercial use in aquaculture. However, little information on pharmacokinetics of SA restricts further application in aquaculture. In this study, pharmacokinetics of SA in common carp (Cyprinus carpio) following a single intraperitoneal administration [10 mg kg?1 BW (body weight)] was evaluated by high‐performance liquid chromatography (HPLC). The peak concentration (Cmax) of SA in kidney was 11.8 μg g?1, which was higher than in other tissues and plasma. The terminal half‐life in fish tissue and plasma was as follows: 42.3 h (kidney) > 37.2 h (liver) > 20.1 h (gill) > 18.8 h (muscle) > 10.9 h (spleen) > 10.0 h (plasma). Additionally, we determined the bacterial loads in tissues of common carp infected with Aeromonas hydrophila after i.p. administration of SA at 0, 5, 10 and 20 mg kg?1 BW. The results showed that i.p. administration of SA at 10 mg kg?1 BW significantly enhanced antibacterial efficacy against A. hydrophila, where the antibacterial ratio in the gill, kidney, spleen and liver on day 5 was 95.13%, 93.33%, 90.09% and 92.82%, respectively. Overall, these results suggested the potential of SA to treat A. hydrophila infection in common carp farming industry. 相似文献
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通过建立体外药动模型的方法,研究诺氟沙星对嗜水气单胞菌Aerom onas hydrophila的药动-药效（简称PK-PD）参数。结果表明：在消除半衰期为3.4 h的模型内,2M IC（最小抑菌浓度）、4M IC和8M IC的诺氟沙星对嗜水气单胞菌能够抑制4 h,4 h后细菌出现再生长,而16M IC的诺氟沙星对嗜水气单胞菌能够起到持续的抑制作用;在消除半衰期为77 h的模型内,2M IC的诺氟沙星对嗜水气单胞菌能够抑制4 h,4 h后细菌出现再生长,而4M IC、8M IC和16M IC对嗜水气单胞菌能够起到持续的抑制作用。消除半衰期为3.4 h的模型内,当AUC0→24 h/M IC（药时曲线下面积与最小抑菌浓度的比值）〉42.43±9.21,Cm ax/M IC（峰浓度与最小抑菌浓度的比值）〉15.78±0.22时,诺氟沙星对嗜水气单胞菌能够起到持续的抑制作用;消除半衰期为77 h的模型内,当AUC0→24 h/M IC〉41.87±10.16,Cm ax/M IC〉4.79±0.11时,诺氟沙星对嗜水气单胞菌能够起到持续的抑制作用。 相似文献
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磺胺二甲嘧啶生理药动学模型种间类推的应用 总被引：1，自引：1，他引：0
本研究应用磺胺二甲嘧啶在猪的生理药动学模型来预测其在绵羊体内的动力学过程。利用文献中已经建立的猪的生理模型,采用动物种间类推原理,将模型外推至绵羊,模拟磺胺二甲嘧啶在绵羊体内的血药和组织浓度,并估算可食性组织残留休药期。结果模拟休药期和文献休药期基本趋于一致,表明生理药动学模型种间类推是可行的。 相似文献
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Wanhe Luo Dehai Wang Hua Qin Dongmei Chen Yuanhu Pan Wei Qu Lingli Huang Shuyu Xie 《Journal of veterinary science (Suw?n-si, Korea)》2021,22(6)
BackgroundOur previously prepared ceftiofur (CEF) hydrochloride oily suspension shows potential wide applications for controlling swine Streptococcus suis infections, while the irrational dose has not been formulated.ObjectivesThe rational dose regimens of CEF oily suspension against S. suis were systematically studied using a pharmacokinetic-pharmacodynamic model method.MethodsThe healthy and infected pigs were intramuscularly administered CEF hydrochloride oily suspension at a single dose of 5 mg/kg, and then the plasma and pulmonary epithelial lining fluid (PELF) were collected at different times. The minimum inhibitory concentration (MIC), minimal bactericidal concentration, mutant prevention concentration (MPC), post-antibiotic effect (PAE), and time-killing curves were determined. Subsequently, the area under the curve by the MIC (AUC0–24h/MIC) values of desfuroylceftiofur (DFC) in the PELF was obtained by integrating in vivo pharmacokinetic data of the infected pigs and ex vivo pharmacodynamic data using the sigmoid Emax (Hill) equation. The dose was calculated based on the AUC0–24h/MIC values for bacteriostatic action, bactericidal action, and bacterial elimination.ResultsThe peak concentration, the area under the concentration-time curve, and the time to peak for PELF''s DFC were 24.76 ± 0.92 µg/mL, 811.99 ± 54.70 μg·h/mL, and 8.00 h in healthy pigs, and 33.04 ± 0.99 µg/mL, 735.85 ± 26.20 μg·h/mL, and 8.00 h in infected pigs, respectively. The MIC of PELF''s DFC against S. suis strain was 0.25 µg/mL. There was strong concentration-dependent activity as determined by MPC, PAE, and the time-killing curves. The AUC0–24h/MIC values of PELF''s DFC for bacteriostatic activity, bactericidal activity, and virtual eradication of bacteria were 6.54 h, 9.69 h, and 11.49 h, respectively. Thus, a dosage regimen of 1.94 mg/kg every 72 h could be sufficient to reach bactericidal activity.ConclusionsA rational dosage regimen was recommended, and it could assist in increasing the treatment effectiveness of CEF hydrochloride oily suspension against S. Suis infections. 相似文献
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健康牙鲆口服剂量为100 mg/kg的甲氧苄氨嘧啶后,利用高效液相色谱测定药物在牙鲆肌肉、血液、肾脏、肝脏质量浓度变化,并通过3P87药动学软件分析数据。试验结果表明,甲氧苄氨嘧啶在肌肉、血液、肾脏、肝脏4种组织中均符合一级吸收二室开放模型,其在上述4种组织中的达峰时间(tmax)分别为18.72、12.942、3.13 h和19.49 h;达峰质量浓度分别为13.80、18.23、32.79、27.40μg/ml;消除半衰期分别为23.64、21.471、6.72 h和15.99 h。口服甲氧苄氨嘧啶,在牙鲆体内吸收与消除较慢,血药浓度高,维持时间长。 相似文献
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采用反溶剂法制备妥曲珠利微晶体,利用显微镜观察妥曲珠利微晶体与妥曲珠利原药显微特征差异,并在25℃条件下测定两者体外溶出速率差异。将12只家兔随机分为2组,每组6只,分别按药物剂量10mg/kg灌胃,单剂量给药,采用HPLC检测血药浓度;用DAS2.0药代动力学程序计算药代动力学参数。结果显示,成功制备了妥曲珠利微晶体,微晶体与原药的显微特征差异明显,体外溶出速率明显加快;家兔单剂量灌胃妥曲珠利和微晶体后,主要药动学参数Cmax分别为（8.925±0.360）mg/L和（12.510±0.525）mg/L,tmax均为24h,AUC（0-∞）分别为（411.605±20.918）mg/（L·h）和（578.650±11.664）mg/（L·h）,相对生物利用度为140.6%,药时数据符合一级吸收二室模型。结果表明,HPLC法适用于妥曲珠利血浆浓度的测定;妥曲珠利微晶体与妥曲珠利原药相比,体内吸收速率和吸收程度有较大的提高。 相似文献