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1.
《中国兽药杂志》2020,(7)
为研究牛蒡子粉中牛蒡苷元在仔猪体内的药物动力学特征,了解其在仔猪体内的吸收、分布、转化和排泄规律,为新兽药的研发和临床用药提供理论参考依据。选取健康仔猪8头(30.0±5.0 kg),以1.0 g/kg·bw的牛蒡子粉灌胃给药,不同时间点前腔静脉采血,采用HPLC法对猪血浆中牛蒡苷元的浓度进行分析。牛蒡子粉灌胃给药后,符合有吸收二室模型,主要药物动力学参数为:吸收半衰期(t_(1/2 ka))为0.274±0.102 h,分布半衰期(t_(1/2α))1.435±0.725 h;消除半衰期(t_(1/2β))63.467±29.115 h;表观分布容积(V_d)1.680±0.402 L/kg;清除率(CL_b)0.076±0.028 L/(h·kg);达峰时间(t_(max))为0.853±0.211 h,峰浓度(c_(max))为0.430±0.035μg/mL,药时曲线下面积(AUC)14.672±4.813μg·h/mL。试验表明:牛蒡子粉口灌后牛蒡苷元在仔猪体内吸收迅速、分布广泛、代谢消除缓慢,能够较长时间发挥药理作用。 相似文献
2.
为研究牛蒡苷元在仔猪体内的药物动力学特征,了解其在仔猪体内的吸收、分布、转化和排泄规律,为新兽药的研发和临床用药提供理论参考依据。选取健康仔猪8头(30.0±5.0 kg),以2.0 mg/kg.bw的牛蒡苷元静脉注射给药,不同时间点前腔静脉采血,采用HPLC法对猪血浆中牛蒡苷元的浓度进行分析。牛蒡苷元静脉注射后,符合无吸收二室模型,主要药动学参数为：分布半衰期(t1/2α)0.166±0.022 h;消除半衰期(t1/2β)3.161±0.296 h;表观分布容积(Vd)0.231±0.033 L/kg;清除率(CLb)0.057±0.003 L/(h·kg);药时曲线下面积(AUC)1.189±0.057 μg·h·mL-1。由此可知,牛蒡苷元静脉注射后在仔猪体内分布迅速、分布组织较少、代谢消除较快。 相似文献
3.
研究头孢噻呋钠在成年麻鸭体内的药动学特征及生物利用度,为临床制定合理的给药方案提供科学依据。选取24只健康的成年麻鸭(体重1.6?0.2kg),随机分为3组,以2mg.kg-1剂量分别单次肌内注射、静脉注射和内服头孢噻呋钠,采用HPLC法检测血药浓度,计算头孢噻呋的药动力学参数和肌注、内服的生物利用度。结果表明：静脉注射头孢噻呋钠后,血药浓度经时数据符合二室开放模型,主要动力学参数：t1/2α为0.19?0.22h,t1/2β为3.64?0.22h,Vd为0.48?0.06L.kg-1,CL为0.07?0.01 L.kg-1.h-1,AUC为27.09?2.84μg.mL-1.h-1;肌内注射后,血药浓度经时数据符合二室开放模型,主要动力学参数：t1/2α为0.38?0.02h,t1/2β为4.56?0.29h,Tmax为0.49?0.17h,Cmax为6.44?0.44μg.mL-1,AUC为26.88?0.48μg.mL-1.h-1,生物利用度为99.22%;内服后,血药浓度经时数据符合二室开放模型,主要动力学参数：t1/2α为0.77?0.14h,t1/2β为3.81?0.23h,Tmax为1.06?0.23h,Cmax为3.62?0.20μg.mL-1,AUC为21.47?0.44μg.mL-1.h-1,生物利用度为79.25%。头孢噻呋钠在成年麻鸭体内吸收迅速,半衰期较长,肌注的生物利用度高,内服吸收良好。 相似文献
4.
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
5.
为评价牛蒡苷元及牛蒡子提取物在兽医临床使用中的安全性,根据兽药急性毒性试验(LD50测定)指导原则的要求,开展了牛蒡苷元及牛蒡子提取物在SPF级昆明小鼠经口给药的急性毒性试验研究。试验结果表明:小鼠灌胃给予牛蒡苷元的半数致死量为219.8 mg/kg,死亡均发生在3 h以内,存活动物均正常生长;鼠灌胃给予牛蒡子提取物后采用最大耐受量法测定发现,给药组与对照组雌雄小鼠生长良好,在14 d观察期内均未出现明显中毒症状和死亡情况,药物急性经口MTD≥36 g/kg.bw;根据兽药指导原则经口给药急性毒性试验剂量分级标准,牛蒡苷元属中等毒级,牛蒡子提取物为实际无毒级。 相似文献
6.
健康仔猪单剂量内服左旋氧氟沙星的药动学研究 总被引：1，自引：0，他引：1
以20mg/kg剂量内服进行左旋氧氟沙星的辩证药动学研究。高效液相色谱法测定血浆药物浓度、3P97药代动力学程序处理药时数据。健康组药时数据符合一级吸收一室模型,其主要药动学参数为:吸收半衰期t1/2ka(0.42±0.08)h,消除半衰期t1/2ke(7.62±0.38)h,达峰时间tmax(1.85±0.25)h,峰浓度Cmax(6.99±0.92)mg/L,药时曲线下面积AUC(90.7±10.07)mg/L·h,生物相表观分布容积VF(s)(2.45±0.28)L/kg,平均滞留时间MRT(11.92±0.94)h。 相似文献
7.
6头成年健康黄牛按10 mg/kg剂量单次快速静注吡喹酮,另6头成年健康黄牛根据交叉试验设计法按10
mg/kg剂量单次肌注、30 mg/kg剂量内服吡喹酮进行药动学与生物利用度试验.利用高效液相色谱法测定血浆中吡喹酮原药的质量浓度,其检测限为25μg/L.房室模型分析表明,静注给药后的药时数据符合无吸收二室开放模型,其分布半衰期(t1/2a)、消除半衰期(t1/2β)、表观分布容积(Vd)、总体清除率(ClB)、药时曲线下面积(AUC)分别为(0.25±0.03)h、(1.28±0.20)h、(2.11±0.38)L/kg、(1.14±0.10)L/(kg·h)和(8.79±0.74)mg/(L·h).肌注的药时数据符合有吸收一室开放模型,主要药动学参数吸收半衰期(t
1/2ka)、消除半衰期(t1/2ke)、药时曲线下面积(AUC)、达峰时间(tmax)、峰浓度(Gmax)和生物利用度(F)分别为(0.40±0.17)h、(4.65±0.91)
h、(6.85±1.02)mg/(L·h)、(1.33±0.52)h、(0.83±0.08)mg/L和77.93%.内服给药后符合有吸收一室开放模型,吸收不规则,其药动学参数t
1/2ka、t1/2ke、AUC、tmax、Cmax和F分别为(1.08±0.13)h、(6.81±1.26)h、(8.51±1.78)mg/(L· 相似文献
8.
建立了超高效液相色谱-串联质谱法测定猪血浆中多西环素的浓度,探讨了猪内服和静脉给予多西环素水溶液后的药代动力学特征。结果表明：猪单次内服10 mg.kg-1体重多西环素饮水剂型水溶液后,MRTlast为12.82±3.34 h,T1/2为11.65±4.80 h,Tmax为4.13±1.89 h,Cmax为0.87±0.48 μg.mL-1,AUClast为11.07±4.19μg.h.mL-1。猪静注10 mg.kg-1体重多西环素水溶液后,AUClast为33.34±8.03μg.h.mL-1,T1/2为5.68±1.32 h,MRTlast为7.98±0.56 h。多西环素饮水剂水溶液的绝对生物利用度为33.2%。猪内服多西环素饮水剂后,具有体内吸收速度较快,达峰时间短,消除较慢,血中平均滞留时间较长等特点。 相似文献
9.
10头健康仔猪随机均分为健康组、脾虚组 ,按 2 0mg/kg的剂量进行内服左旋氧氟沙星的药动学研究。高效液相色谱法测定血浆中药物浓度 ,3P97药代动力学程序处理药时数据。健康组和脾虚组药动学数据适合一级吸收一室模型。健康组主要药动学数据为 :吸收半衰期 (t1 / 2ka)(0 42± 0 0 8)h ,消除半衰期 (t1 / 2ke) (7 62± 0 38)h ,达峰时间 (tmax) (1 85± 0 2 5)h ,达峰浓度 (Cmax) (6 99± 0 92 )mg/L ,药时曲线下面积 (AUC) (90 7± 1 0 0 7)mg·L- 1 ·h ,表观分布容积 (V/ F(s) ) (2 45± 0 2 8)L·kg,平均滞留时间 (MRT) (1 1 92± 0 94)h。脾虚组 :t1 / 2ka(1 1 7± 0 38)h ,t1 / 2ke (9 0 2± 1 1 8)h ,tmax (3 93± 1 0 5)h ,Cmax (4 2 8± 1 45)mg/L ,AUC (72 2 1± 1 6 0 7)mg·L- 1 ·h ,V/ F(s) (3 95±1 2 8)L·kg,MRT (1 3 74± 1 2 1 )h。结果表明 :仔猪脾虚状态下明显影响左旋氧氟沙星内服给药的药动学特征 相似文献
10.
为了研究泰地罗新注射液肌内注射和静脉注射在猪体内的药动学特征和绝对生物利用度,16只健康猪采用随机单剂量、平行试验设计,分别以4 mg/kg BW肌内注射和以1 mg/kg BW静脉注射泰地罗新注射液。采用超高效液相色谱-串联质谱法测定猪血浆中泰地罗新的浓度,以药动学分析软件WinNolin 6.4非房室模型计算药动学参数。结果显示,猪肌内注射泰地罗新注射液的药动学参数分别为Tmax(0.58±0.36)h,Cmax(0.88±0.17)μg/ml,AUClast(11.00±4.05)μg.h/mL,T1/2λz(33.58±22.01) h,MRTlast(35.60±10.00 )h。猪静脉注射泰地罗新注射液的药动学参数分别为AUClast(3.56±1.62)μg.h/mL,T1/2λz(50.91±23.47)h,MRTlast(37.53±4.52 )h,Vz(17.59±8.09)L/kg,Cl(0.31±0.14)L/h.kg。肌内注射泰地罗新注射液的绝对生物利用度77.15%,在猪体内的药动学特征是吸收迅速,血浆达峰时间短,消除半衰期长,绝对生物利用度高。 相似文献
11.
本试验按单剂量口服的方法对健康蛋鸡进行替米考星可溶性粉和替米考星溶液中主要组分替米考星的生物利用度和药代动力学研究。利用HPLC方法分析不同时间点试验鸡血浆中的药物浓度。药物的药动学参数结果显示,替米考星可溶性粉和替米考星溶液的平均血药浓度-时间曲线下面积(AUC0-48)分别为(16.947±0.624)μg/mL.h和(16.020±0.631)μg/mL.h,没有显著差异;二者AUC0-48比值为1.058,Cmax分别为(0.759±0.012)μg/mL和(0.764±0.012)μg/mL,比值为0.993;替米考星可溶性粉和替米考星溶液的t1/2β、C l(s)、t1/2 Ka和V/F(c)均没有显著差异;二者的tmax分别为(1.211±0.036)h和(1.030±0.063)h虽然有显著差异,但并不能以此说明二者生物学的非等效性。试验结果说明,单剂量口服替米考星可溶性粉和替米考星溶液后,替米考星被迅速吸收,消退缓慢,依据生物等效性的重要评判指标,得出替米考星可溶性粉和替米考星溶液在治疗中可以相互替代。 相似文献
12.
X. B. LI W. X. WU D. SU Z. J. WANG H. Y. JIANG J. Z. SHEN 《Journal of veterinary pharmacology and therapeutics》2008,31(6):523-527
A study on bioavailability and pharmacokinetics of cefquinome in piglets was conducted after intravenous (i.v.) and intramuscular (i.m.) administrations of 2.0 mg/kg of body weight, respectively. Plasma concentrations were measured by high‐performance liquid chromatography assay with UV detector at 268‐nm wavelength. Plasma concentration–time data after i.v. administration were best fit by a two‐compartment model. The pharmacokinetic values were distribution half‐life 0.27 ± 0.21 h, elimination half‐life 1.85 ± 1.11 h, total body clearance 0.26 ± 0.08 L/kg·h, area under curve 8.07 ± 1.91 μg·h/mL and volume of distribution at steady state 0.46 ± 0.10 L/kg. Plasma concentration–time data after i.m. administration were also best fit by a two‐compartment model. The pharmacokinetic parameters were distribution half‐life 0.88 ± 0.42 h, elimination half‐life 4.36 ± 2.35 h, peak concentration 4.01 ± 0.57 μg/mL and bioavailability 95.13 ± 9.93%. 相似文献
13.
1. The pharmacokinetics of cefquinome (CEQ) in chickens was determined after intravenous (IV) and intramuscular (IM) administration of 2?mg/kg body weight. Plasma concentrations were measured by high performance liquid chromatography assay with an ultraviolet detector at 265?nm wavelength. 2. Plasma concentration–time data after IV administration were best fitted by a two-compartment model. The pharmacokinetic parameters following IV injection were distribution half-life 0·43?±?0·19?h, elimination half-life 1·29?±?0·10?h, total body clearance 0·35?±?0·04?l/kg/h, area under curve 5·33?±?0·55?µg/h/ml and volume of distribution at steady state 0·49?±?0·05?l/kg. 3. Plasma concentration–time data after IM administration were best described by a two-compartment model. The pharmacokinetic parameters after IM administration were absorption half-life 0·07?±?0·02?h, distribution half-life 0·58?±?0·27?h, elimination half-life 1·35?±?0·20?h, peak concentration 3·04?±?0·71?µg/ml and bioavailability 95·81?±?5·81%. 4. Cefquinome kinetics in chicken and data from other species were summarised and analysed to provide a comprehensive understanding of CEQ pharmacokinetics. 相似文献
14.
D. GIROUX G. SIROIS G.-P. MARTINEAU‡ 《Journal of veterinary pharmacology and therapeutics》1995,18(6):407-412
The pharmacokinetics of gentamicin was investigated in six newborn male piglets, aged from 4 to 12 h at the time of administration of the drug, and six 42-day-old castrated male piglets, that had been weaned for 2 weeks following a single intravenous bolus of 5 mg/kg. Gentamicin was measured in serum and in urine by a fluorescence polarization immunoassay. The serum concentrationtime data were best described by a three-compartment open model. A rapid initial distribution phase (± phase) was observed in every animal. The serum β half-life (t1/2β) was significantly longer in the newborn piglets (mean ± SEM) (5.19 ± 0.30 h) than in the older group (3.50 ± 0.23 h) (P < 0.05). Mean residence time was similarly longer in younger piglets (6.62 ± 0.57 h) than in older animals (2.86 ± 0.11 h) (P < 0.05). The steady-state volume of distribution (Vills was significantly larger for younger pigs (0.785 ± 0.036 L/kg) than in elder pigs (0.474 ± 0.029 L/kg) (P < 0.05). Urinary γ half-life (t1/27u) was 72.66 ± 10.78 h in the newborn piglets and 69.20 ± 14.77 h in the 42-day-old animals. A urinary δ phase was observed in three of the 42-day-old piglets and gave a mean (t1/2δu of 232.01 ± 14.55 h. Percentages of urinary recovery of the administered dose after 144 h were 94.18 ± 1.01 and 94.04 ± 1.12 in the newborn and 42-day-old animals, respectively. Serum gentamicin clearance was significantly lower in younger animals (0.121 ± 0.007 L/h±kg) than in the 42-day-old group (0.166 ± 0.010 L/h·kg). It is suggested that in the newborn piglets, the increase of Vd(ss) could be explained by a higher proportion of extracellular water while the lower clearance could be attributed to a reduced glomerular filtration capacity. Gentamicin dosage requirement in the newborn piglets would therefore have to be adjusted, in order to take into consideration the observed differences in the mean values of these latter pharmacokinetic parameters. 相似文献
15.
本试验旨在探讨加丽素红中角黄素在鸡体内的药代动力学特征.选取19周龄的海兰蛋鸡12只,单次灌胃口服加丽素红9.6 mg/kg BW,在72 h内不同时间段分10次采集静脉血,用高效液相色谱法测定鸡血清中角黄素的质量浓度,并利用3P97药代动力学程序软件处理血药浓度-时间数据.结果如下:加丽素红经口服给药后,角黄素在鸡体内的血药浓度-时间数据符合一级吸收一室模型,其理论方程为C=0.471(e-0.036-e-0.190),主要药代动力学参数为:吸收半衰期t1/2(Ka)=(3.643±0.205)h,消除半衰期t1/2(Ke)=(19.263±1.312)h,达峰时间Tmax=(10.795±1.007)h,达峰浓度Cmax=(0.259±0.048)μg/mL,血药浓度-时间曲线下面积AUC=(10.607±1.029)μg/(mL·h),总体清除率CLB=(0.905±0.076)L/(kg·h),表观分布容积Vd=(2.515±0.133)L/kg.上述结果表明,角黄素在鸡体内血药浓度的变化表征了加丽素红在鸡体内代谢的变化规律,具有吸收分布较迅速、达峰快、体内分布广泛、消除速度较慢等特点. 相似文献
16.
克蚕菌的药物动力学研究 总被引：6，自引：4，他引：2
采用微生物法测定 5龄健康家蚕食下克蚕菌后的经时过程血药浓度。用药物动力学软件结合EXCEL程序拟和计算 ,克蚕菌在蚕体内的血药浓度—时间曲线符合一级吸收动力学和单室模型特征。其血药浓度随时间变化的单室模型关系式为C =16 .6 2 87(e-0 119t-e-0 742t) ,实测血药浓度—时间曲线与理论血药浓度—时间曲线的相关系数R2 =0 .96 33。求得克蚕菌的药物动力学参数分别为 :ka=(0 .74 2± 0 .12 3) /h ;k =(0 .119± 0 .0 0 3) /h ;t1/ 2 (a)=(0 95 8± 0 180 )h ;t1/ 2 =(5 82 1± 0 15 3)h ;Cmax=(9 70 7± 0 16 3) μg/mL ;Tmax=(2 .971± 0 .32 2 )h ;VD=(0 .5 4 3± 0 .0 2 5 )L ;CL =(0 .0 6 5± 0 .0 0 1)L/h ;AUC =(117.5 0 3± 3.30 6 )h·(μg/mL)。 相似文献
17.
为研究卡洛芬注射液在牛体内的药动学特征,将8头健康牛随机分为两组,每组4头,给药剂量为1.4 mg/kg BW,给药后按设计的采血点采集血样,采用超高液相色谱-串联质谱法(UPLC-MS/MS)测定血浆中卡洛芬的药物浓度,用WinNonlin8.1软件计算药动学参数。结果显示：牛单次皮下注射受试制剂卡洛芬注射液在牛体内主要药动学参数如下：平均最高血药浓度(Cmax)为(17473.30±2398.73)ng·mL-1,平均药时曲线下面积(AUClast)为(1052647.93±143055.37)h·ng·mL-1,平均达峰时间(Tmax)为8.00±2.62 h,平均消除半衰期(T1/2)为55.69±3.25 h;牛单次皮下注射参比制剂卡洛芬注射液的主要药动学参数如下：平均最高血药浓度(Cmax)为(15695.98±4865.73)ng·mL-1,平均药时曲线下面积(AUClast)为(1002858.15±297235.31)h·ng·mL-1,平均达峰时间(Tmax... 相似文献
18.
A method for the detection of curcumin in pig plasma by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was established firstly and the pharmacokinetics of curcumin solid dispersion and curcumin premix in piglets were studied. Sixteen healthy piglets (Yorkshire×Changbai), seven-week aged, half male and half female, were randomly divided into two groups receiving curcumin solid dispersant and curcumin premix orally at the dose of 100 mg·kg-1, respectively. Then plasma samples were collected at different time points, and the blood concentration of curcumin was determined by HPLC-MS/MS. The WinNonlin 5.2.1 software was used to analyze and calculate the pharmacokinetic parameters. The pharmacokinetic parameters of curcumin solid dispersion and curcumin premix were as follows: the area under the curve (AUC) was (104.53±38.67) and (37.82±11.48) h·ng·mL-1, time to peak concentration (Tmax) was (3.25±0.38) and (2.31±0.37) h, peak concentration (Cmax) was (26.65±9.65) and (9.55±2.75) ng·mL-1, respectively, elimination half-life time (t1/2β) was (3.55±2.17) and (6.93±0.86) h, mean residence time (MRT) was (5.23±0.53) and (4.26±0.47) h. The statistical analysis showed significant differentce (P<0.01) between curcumin solid dispersion and premix in parameters, the Tmax of curcumin solid dispersion was delayed significantly, the Cmax was increased obviously and the AUC was improved after the piglets were given curcumin solid dispersion. Compared with curcumin premix, the relative bioavailability of curcumin solid dispersion was 280.39%. The results showed that curcumin solid dispersion could improve the dissolution and absorption of curcumin in the intestinal tract and improve the relative bioavailability of curcumin, which provided a scientific basis for the development and clinical application of curcumin solid dispersions in the future. 相似文献
19.
Venkatathalam Dinakaran Vinod Kumar Dumka Bibhuti Ranjan Ramalingam Balaje Pritam Kaur Sidhu 《Tropical animal health and production》2013,45(7):1509-1512
Disposition following single intravenous injection (2 mg/kg) and pharmacodynamics of cefquinome were investigated in buffalo calves 6–8 months of age. Drug levels in plasma were estimated by high-performance liquid chromatography. The plasma concentration–time profile following intravenous administration was best described by a two-compartment open model. Rapid distribution of cefquinome was evident from the short distribution half-life (t ½α ?=?0.36?±?0.01 h), and small apparent volume of distribution (Vdarea?=?0.31?±?0.008 L/kg) indicated limited drug distribution in buffalo calves. The values of area under plasma concentration–time curve, elimination half-life (t ½β ), total body clearance (ClB), and mean residence time were 32.9?±?0.56 μg·h/mL, 3.56?±?0.05 h, 60.9?±?1.09 mL/h/kg, and 4.24?±?0.09 h, respectively. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration of cefquinome were 0.035–0.07 and 0.05–0.09 μg/mL, respectively. A single intravenous injection of 2 mg/kg may be effective to maintain the MIC up to 12 h in buffalo calves against the pathogens for which cefquinome is indicated. 相似文献