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1.
为研究海南霉素钠预混剂在鸡体内的药代动力学特征和生物利用度,将16只健康AA鸡随机分成2组,每组8只,采用平行试验设计对两组鸡分别进行单剂量口服给药和静脉注射给药药动学研究,给药量均为1.5 mg/kg bw(相当于7.5 mg/kg混饲给药)。按预定时间点采集血样,血样中海南霉素的含量采用高效液相色谱-串联质谱法(HPLC-MS/MS)测定,流动相为乙腈-0.1%甲酸水溶液(90:10,V/V)。实测血药浓度-时间数据使用Winnonlin 5.2药动学分析软件拟合药动学参数。鸡口服给药的药动学参数如下:平均消除半衰期为(T_(1/2β))约为30.44 h,平均滞留时间(MRT)约为36.40 h,在血浆中的达峰时间(T_(max))约为0.5 h,达峰浓度(C_(max))约为68.87 ng/mL,平均药时曲线下面积(AUC)约为654.95 ng·h/mL,平均生物利用度(F)约为32.82%。鸡静脉注射给药的药动学参数如下:平均消除半衰期约为(T_(1/2β))为46.40 h,平均滞留时间(MRT)约为30.91 h,平均血浆清除率(CL)约为1.59 L/(kg·h),平均表观分布容积(V_d)约为116.05 L/kg。结果表明海南霉素进入鸡体后分布广泛,消除缓慢,半衰期长;口服海南霉素钠预混剂吸收迅速,但吸收不完全。  相似文献   

2.
为研究帕托珠利混悬液在仔猪体内的药动学特征及生物利用度,采用平行实验设计方法,将16头 40 日龄健康仔猪随机分成两组,每组8头（公母各半）,分别进行单剂量静脉注射（6mg/kg bw）和单剂量口服给药（15mg/kg bw）,所有猪给药前禁食12h,给药2h后恢复正常饮食。给药后按预定的采血点采集血样,血浆中帕托珠利的含量采用经验证的 HPLC检测方法进行测定。实测血药浓度数据采用Graphad prism 8.0拟合药时曲线图,并用 Winnonlin5.2计算药动学参数。结果显示,单剂量静脉注射帕托珠利注射液后帕托珠利在仔猪体内主要药动学参数如下：平均消除半衰期（T1/2?）为136.98h,平均滞留时间（MRT）为165.92h,平均药时曲线下面积（AUC0-t）为1570.97 h?μg/mL,平均表观分布容积（Vz）为695.59 mL/kg,平均血浆清除率（CL）为3.77 mL/h?kg;单剂量口服帕托珠利混悬液后帕托珠利在仔猪体内主要药动学参数如下：平均消除半衰期（T1/2?）为134.05h,平均达峰时间（Tmax）为42.00h,平均峰浓度（Cmax）为14.03μg/mL,平均滞留时间（MRT）为173.19h,平均药时曲线下面积（AUC0-t）为2831.00 h?μg/mL,帕托珠利混悬液口服给药绝对生物利用度为72.08%。结果表明,帕托珠利在猪体内分布较差,消除缓慢;仔猪口服帕托珠利混悬液达峰时间较长,但吸收良好。  相似文献   

3.
目的为了了解四黄止痢泡腾颗粒相对生物利用度,分别给鸡灌胃四黄止痢泡腾颗粒和普通颗粒,采用HPLC法测定血浆中黄芩苷含量,采用DASS2.1.1软件计算相关药动学参数。结果鸡血浆中黄芩苷浓度出现双峰现象。泡腾颗粒和普通颗粒C1max分别为:1.03μg·ml-1和0.93μg·ml-1;C2max为0.95μg·ml-1和0.73μg·ml-1;T1max为0.47 h和0.39 h,T2max为2.43h和1.93 h;AUC为11.6μg·h·ml-1和10.63μg·h·ml-1;相对生物利用度为109.13%。结论 :四黄止痢泡腾颗粒相对生物利用度有所提高,值得推广。  相似文献   

4.
为研究氟苯尼考环糊精包合物的药代动力学及生物利用度,将健康白羽肉鸡24只,随机分为两组,每组12只,分别以20 mg/kg的剂量单次灌服20%普通氟苯尼考粉(A组)和20%氟苯尼考环糊精包合物(B组),并于给药后不同时间点从翅下静脉采血,采用已建立的UPLC-MS/MS测定血浆中的药物浓度,用WinNonlin 5.2.1药动学分析软件的非房室模型拟合血药浓度-时间数据。结果显示:A组达峰时间(T_(max))和达峰浓度(C_(max))分别为1.563±0.755 h、1043.15±391.42 ng/mL,平均消除半衰期(T_(1/2λz))约为4.814±3.058 h,平均曲线下面积(AUC_(last))为4283.53±2406.81 h·ng/mL;B组T_(max)、C_(max)分别为1.417±1.683 h、4691.95±1597.28 ng/mL,T_(1/2λz)约为2.106±1.476 h,AUC_(last)为14911.70±2976.22 h·ng/mL;相对生物利用度约为348.12%。试验表明,采用环糊精包合工艺的氟苯尼考粉的生物利用度显著高于普通工艺的氟苯尼考粉。  相似文献   

5.
本研究比较了口服复方替米考星可溶性粉与单独肌注替米考星注射液和静注磺胺二甲嘧啶钠注射液在鸡体内药物代谢动力学特征和相对生物利用度。36只健康鸡,随机分为3组,给药剂量均为20 mg/kg,翼下静脉采血,高效液相色谱法检测鸡血浆中的药物浓度。采用药动学软件Win Nonlin 6.1的非房室模型分析方法,计算出药物的动力学参数。鸡口服复方替米考星可溶性粉、肌注替米考星注射液和静注磺胺二甲嘧啶钠注射液后的药时曲线下面积(AUC)分别为:9.49±3.64、37.17±10.82、12.40±4.11、61.31±11.38μg×h/m L。复方替米考星可溶性中替米考星相对于肌肉注射的替米考星的生物利用度为75.98%,复方制剂中磺胺二甲嘧啶钠的绝对生物利用度为60.63%。复方替米考星可溶性粉和单方药物相比,药动学参数经t检验,t_(1/2)、T_(max)、C_(max)、AUC、MRT等存在显著性差异(P0.05)。结果表明复方替米考星可溶性粉单剂量口服给药吸收较慢,达峰时间显著延迟,平均驻留时间显著延长,有利于抗菌作用的发挥。  相似文献   

6.
《畜牧与兽医》2015,(6):125-127
16只体重较一致的健康断奶仔猪随机分成2组,采用单剂量平行随机对照试验设计,分别单剂量(20 mg/kg体重,以妥曲珠利计)经口内服国产(受试品)和进口(对照品)妥曲珠利混悬液。结果表明,与妥曲珠利混悬液对照品相比较,妥曲珠利触变混悬液受试品单剂量内服给药吸收和消除较慢,但药物吸收完全。给药后按预定时间采集血样,血浆中妥曲珠利含量采用HPLC紫外检测器进行分析。实测血药浓度-时间数据采用Winnonlin5.2药动学分析软件计算药代动力学参数。结果显示,妥曲珠利混悬液对照品单剂量内服后,其平均消除半衰期(T1/2β)约为40.806 h,达峰时间(Tmax)和峰值浓度(Cmax)分别为16.500 h和27.494 mg/L,平均药时曲线下面积(AUC)为1 375.738(μg/m L/h),平均滞留时间(MRT)为50.677 h;妥曲珠利触变混悬液受试品单剂量内服后,其T1/2β约为51.642 h,Tmax和Cmax分别为37.500 h和21.452mg/L,AUC为1 843.842μg/m L/h,MRT为64.058 h,相对生物利用度为134.02%。与妥曲珠利混悬液对照品相比,妥曲珠利触变混悬液受试品口服吸收AUC(P=0.020)、Tmax(P=0.001)、MRT(P=0.019)有显著性差异;但两种混悬剂的其他药动学参数,如T1/2β(P=0.224)、Cmax(P=0.146)无显著差异。  相似文献   

7.
<正>采用高效液相紫外检测法,测定了健康鸡灌服80 mg·kg-1阿德呋啉后血浆中药物浓度,药物浓度-时间数据用3P97药代动力学程序软件处理。血药浓度-时间数据符合一级吸收二室开放模型,其主要药代动力学参数分别为:血浆消除半衰期(T1/2β)(2.414±0.252)h,达峰时间(Tpeak)(1.429±0.053)h,达峰浓度(C max)(499.941±21.295)ng·m L-1,药时曲线下面积(AUC)(2624.528±124.690)ng·h·m L-1。阿德呋啉在试验鸡体内的相对生物利用度为61.94%。结果表明:阿德呋啉在健康鸡体内的药代  相似文献   

8.
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   

9.
健康白羽肉鸡20只,随机分为A、B两组,以20mg/kg的剂量单次灌服两种工艺的20%氟苯尼考粉。并于给药后不同时间点从翅下静脉采血,采用已建立的UPLC-MS/MS测定血浆中的药物浓度。采用 WinNonlin 5. 2. 1 药动学分析软件的非房室模型拟合血药浓度-时间数据。结果显示：A组达峰时间(Tmax)和达峰浓度(Cmax)分别为1.675±0.782 h、1073.20±425.72 ng/mL,平均消除半衰期T1/2λz约为4.729±3.347 h,平均曲线下面积 (AUClast) 为 4498.76±2596.16 h?ng/mL;B组达峰时间(Tmax)和达峰浓度(Cmax)分别为1.523±1.723 h、4654.64±1669.75 ng/mL,平均消除半衰期T1/2λz约为2.193±1.515 h,平均曲线下面积 (AUClast)为15392.84±2586.10 ng/mL;相对生物利用度约为342.16%。结果表明,采用环糊精包合工艺的氟苯尼考粉的生物利用度显著高于普通工艺的氟苯尼考粉。  相似文献   

10.
为了建立鸡血浆脱水穿心莲内酯的测定方法,给动物应用穿心莲后有效成分的吸收评价研究提供基础资料,试验以脱水穿心莲内酯为指标性成分,应用反相HPLC法测定岭南黄鸡内服穿心莲超微粉后血浆中脱水穿心莲内酯含量的变化.结果表明:内服给药后,在测定的时间段(0～10 h)内脱水穿心莲内酯在血浆中均有分布,给药后约40 min达到峰值,峰浓度约为1.542 μg/mL,给药后10 h的浓度为0.067 μg/mL;该方法的平均绝对回收率为90.44%～98.99%;最低定量限、最低检测限分别为0.04 μg/mL和0.02 μg/mL.  相似文献   

11.
The bioavailability and pharmacokinetics of ibuprofen, a nonsteroidal antiinflammatory drug, was studied in healthy Shetland ponies. Ibuprofen was administered IV, as a suspension, and as a solid solution oral paste to ponies from which food was withheld. The suspension paste was also administered to ponies that received hay and water ad libitum. Both formulations had an absolute bioavailability of about 80%. Bioavailability was not influenced by feeding.  相似文献   

12.
The pharmacokinetics of ampicillin and amoxicillin following intravenous administration at a dose rate of 15 and 10 mg/kg respectively were studied in four healthy adult horses. Pharmacokinetics of pivampicillin and amoxicillin were studied after oral administration to four healthy adult horses. Pivampicillin, a prodrug of ampicillin, was administered orally to starved and fed horses at a dose rate of 19.9 mg/kg, which is equivalent on a molecular basis to 15 mg/kg ampicillin. Amoxicillin was administered orally to starved horses only, at a dose rate of 20 mg/kg. Ampicillin and amoxicillin concentrations in plasma, synovial fluid and urine were determined. Mean biological half-life of intravenously administered ampicillin and amoxicillin was 1.72 and 1.43 h respectively, whilst the distribution volume (Vss) appeared to be 0.180 and 0.192 1/kg. Orally administered pivampicillin and amoxicillin were rapidly absorbed. A maximum concentration in plasma of 3.80 micrograms/ml was reached 2 h after administration of pivampicillin to starved horses; in fed horses a maximum concentration of 5.12 micrograms/ml was reached 1 h after administration. After oral administration of amoxicillin a maximum concentration of 2.03 micrograms/ml was reached after 1 h. The (absolute) bioavailability of pivampicillin administered orally was 30.9% in starved horses and 35.9% in fed horses. The bioavailability of amoxicillin administered orally was 5.3% in starved horses.  相似文献   

13.
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   

14.
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   

15.
The purpose of this study was to determine the effect of concurrent sucralfate (tablet or suspension) on doxycycline pharmacokinetics and to determine the effects of delaying sucralfate by 2 h on doxycycline absorption. Five dogs were included in a crossover study receiving: doxycycline alone; doxycycline concurrently with sucralfate tablet; doxycycline followed 2 h by sucralfate tablet; doxycycline concurrently with sucralfate suspension; and doxycycline followed 2 h by sucralfate suspension. Doxycycline plasma concentrations were evaluated with liquid chromatography with mass spectrometry. No interaction was seen when sucralfate was administered as a tablet. Sucralfate tablet fragments were frequently observed in some dogs' feces. The area under the curve (AUC) and maximum plasma concentration (CMAX) were significantly lower (P < 0.001) in the concurrent sucralfate suspension group (AUC 7.2 h·μg/mL, CMAX 0.43 μg/mL) than with doxycycline alone (AUC 36.0 h·μg/mL, CMAX 2.53 μg/mL) resulting in a relative bioavailability of 20%. Delaying sucralfate suspension by 2 h after doxycycline administration resulted in no difference in doxycycline absorption as compared with doxycycline administration alone with a relative bioavailability of 74%. The lack of an interaction with sucralfate tablets suggests sucralfate should be administered as a suspension rather than tablet in dogs.  相似文献   

16.
The pharmacokinetics and the influence of food on the kinetic profile and bioavailability of doxycycline was studied after a single intravenous (i.v.) and oral dose of 10.0 mg/kg body weight in 7-week-old broiler chickens. Following i.v. administration the drug was rapidly distributed in the body with a distribution half-life of 0.21 +/- 0.01 h. The elimination half-life of 6.78 +/- 0.06 h was relatively long and resulted from both a low total body clearance of 0.139 +/- 0.007 L/h.kg and a large volume of distribution of 1.36 +/- 0.06 L/kg. After oral administration to fasted chickens, the absorption of doxycycline was quite fast and substantial as shown by the absorption half-life of 0.39 +/- 0.03 h, the maximal plasma concentration of 4.47 +/- 0.16 micrograms/mL and the time to reach the Cmax of 1.73 +/- 0.06 h. The distribution and the final elimination of the drug were slower than after i.v. administration. The absolute bioavailability was 73.4 +/- 2.5%. The presence of food in the intestinal tract reduced and extended the absorption (t1/2a = 1.23 +/- 0.21 h; Cmax = 3.07 +/- 0.23 micrograms/mL; tmax = 3.34 +/- 0.21 h). The absolute bioavailability was reduced to 61.1% +/- 4.4%.  相似文献   

17.
Long-term oral treatment with cimetidine is recommended to reduce vomiting in dogs with chronic gastritis. Despite this, few studies have specifically examined the plasma disposition and pharmacokinetics of cimetidine in dogs, particularly following repeated oral administration. The pharmacokinetics of cimetidine following oral administration as tablets was investigated in healthy dogs. Cimetidine was absorbed rapidly post-treatment ( t max = 0.5 h). A mean absolute bioavailability of 75% was calculated following a single oral administration of 5 mg cimetidine/kg body weight. After intravenous administration, a plasma half-life of 1.6 h was calculated. Repeated oral administration at the recommended dose rate and regime (5 mg/kg body weight three times daily) for 30 consecutive days did not lead to any accumulation of cimetidine in plasma. Food intake concomitant with oral administration of cimetidine delayed ( t max = 2.25 h) and decreased the rate and extent of absorption ( AUC ) by about 40%. Cimetidine was well absorbed in fasted dogs. Administration of food decreased the bioavailability of cimetidine by 40%. Cimetidine does not accumulate over time in plasma when administered long term to dogs.  相似文献   

18.
The pharmacokinetics of oclacitinib maleate was evaluated in four separate studies. The absolute bioavailability study used a crossover design with 10 dogs. The effect of food on bioavailability was investigated in a crossover study with 18 dogs. The breed effect on pharmacokinetics was assessed in a crossover study in beagles and mongrels dogs. Dose proportionality and multiple dose pharmacokinetics were evaluated in a parallel design study with eight dogs per group. In all four studies, serial blood samples for plasma were collected. Oclacitinib maleate was rapidly and well absorbed following oral administration, with a time to peak plasma concentration of <1 h and an absolute bioavailability of 89%. The prandial state of dogs did not significantly affect the rate or extent of absorption of oclacitinib maleate when dosed orally, as demonstrated by the lack of significant differences in pharmacokinetic parameters between the oral fasted and oral fed treatment groups. The pharmacokinetics of oclacitinib in laboratory populations of beagles and mixed breed dogs also appeared similar. Following oral administration, the exposure of oclacitinib maleate increased dose proportionally from 0.6 to 3.0 mg/kg. Additionally, across the pharmacokinetic studies, there were no apparent differences in oclacitinib pharmacokinetics attributable to sex.  相似文献   

19.
Species differences in oral bioavailability, first-pass metabolism and pharmacokinetics of biopharmaceutics classification system (BCS) class I compound acetaminophen were studied. The absolute bioavailability was 42.2%, 39.0%, 44.5%, 75.5% and 91.0% in chickens, turkeys, dogs, pigs and horses, respectively. After hydrolysis of metabolites by β-glucuronidase/sulfatase, apparent bioavailability increased significantly in all species (turkeys: 72.4%, dogs: 100.5%, pigs: 102.2%), except horses (91.6%). Mean metabolic ratios of [acetaminophen glucuronide]/[acetaminophen] between 0 and 1 h were significantly higher after oral dosing in turkeys, dogs and pigs, revealing the role of first-pass metabolism in incomplete bioavailability. Evidence of species differences in acetaminophen metabolism is provided by differences in plasma clearance, which was inversely proportional to bioavailability. In conclusion, differences in BA appeared to originate predominantly from differences in first-pass metabolism, demonstrating that the BCS high permeability classification of acetaminophen is consistent across the mammalian species studied. In turkeys, however, incomplete absorption additionally seemed to contribute to the low BA.  相似文献   

20.
Ricobendazole (RBZ) was administered in sheep at the dose rate of 5 mg/kg by intravenous (i.v.) route as a 10% experimental solution, by the intraruminal (i.r.) route as a 10% experimental suspension, and by the subcutaneous (s.c.) route as a 10% commercial formulation available in Argentina. Blood samples were drawn during a 60 h period. Plasma concentrations of RBZ and its inactive metabolite albendazole sulphone (ABZSO2) were determined by high-performance liquid chromatography. The pharmacokinetic parameters were determined by compartmental analysis. The fitting of the data was done by weighted least-squares non-linear regression analysis. The pharmacokinetic parameters were estimated for every animal by simultaneous fitting of the plasma concentrations profiles of RBZ obtained after its administration by the three routes. The kinetic analysis of ABZSO2 was performed by a statistical moment approach. Ricobendazole bioavailability was poor after i.r. administration, whereas high and sustained plasma concentrations and higher bioavailability were obtained after s.c. administration. A simple two-compartment open model explains in a mechanical sense the pharmacokinetic behaviour of RBZ in sheep and allows us to estimate the real first-order constant rate of absorption and the loss of drug from the absorption site after its administration by s.c. and i.r. routes.  相似文献   

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