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1.
研究双氯芬酸钠注射液在猪体内的药物动力学特征和生物利用度,为其临床合理使用提供实验依据。选用8头健康猪,采用两周期随机交叉实验设计,单剂量静脉注射或肌内注射5%双氯芬酸钠注射液(2.5mg·kg~(-1)),高效液相色谱法(HPLC)检测猪血浆中双氯芬酸钠浓度,采用DAS 2.1.1软件对血药浓度-时间数据进行非房室模型分析,计算药动学参数。结果显示,猪静脉注射给药的药动学参数如下:消除半衰期(T_(1/2β))为(1.32±0.34)h,药-时曲线下面积(AUC)为(55.50±5.50)(μg·mL~(-1))·h,平均滞留时间(MRT)为(1.60±0.28)h,表观分布容积(V_d)为(0.50±0.05)L·kg~(-1),总体清除率(CL_B)为(0.26±0.04)L·(h·kg)-1。猪肌内注射给药的药动学参数如下:峰时(T_(max))为(1.19±0.26)h,峰浓度(C_(max))为(11.61±5.99)μg·mL~(-1),T_(1/2β)为(1.87±0.70)h,AUC为(43.17±7.77)(μg·mL~(-1))·h,MRT为(2.86±0.64)h,生物利用度(F)为(78.29±14.81)%。结果提示,双氯芬酸钠注射液肌注给药后在猪体内具有吸收良好、达峰迅速、血药峰浓度高、消除较快、生物利用度较高的药物动力学特征,临床推荐给药剂量为2.5mg·kg~(-1)。  相似文献   

2.
为研究六氢β-酸月桂酸酯在鸡体内的药动学,本试验选用12只健康鸡,随机分为2组,分别单剂量40mg/kg体重灌胃给药和1 mg/kg体重静脉注射给药。在给药前后不同时间点从前腔静脉采集血样,分离血浆,用高效液相色谱法测定血浆中六氢β-酸月桂酸酯的浓度。用Winnonlin 5.2.1的非房室模型处理血浆药物浓度-时间数据。单剂量口服六氢β-酸月桂酸酯的主要药动学参数:Cmax(0.04±0.01)μg/m L,tmax(1.00±0.15)h,T1/2(2.35±0.17)h,AUC(0.13±0.01)μg·h/m L,V(1024.1±98.4)L/kg,CLB(302.2±7.6)L/h·kg,MRT(3.55±0.27)h;单剂量静脉注射六氢β-酸月桂酸酯的主要药动学参数:C0(1.25±0.17)μg/m L,T1/2(1.10±0.25)h,AUC(0.82±0.14)μg·h/m L,V(1.93±0.13)L/kg,CLB(1.25±0.21)L/h·kg,MRT(1.27±0.31)h。结果表明:灌胃六氢β-酸月桂酸酯与静脉注射六氢β-酸月桂酸酯相比,鸡灌胃给药的生物利用度为0.4%,灌胃给药后吸收极少,静脉注射血药浓度较高,消除半衰期均较短。  相似文献   

3.
文中进行了六氢β-酸月桂酸酯在鸡体内的药动学研究。将12只健康鸡随机分为2组,分别单剂量每千克体重40 mg/kg灌胃给药和1 mg/kg静注给药。在给药前后不同时间点从前腔静脉采集血样,分离血浆,用高效液相色谱法测定血浆中六氢β-酸月桂酸酯的浓度。用Winnon-lin5.2.1的非房室模型处理血浆药物浓度-时间数据。单剂量口服六氢β-酸月桂酸酯的主要药动学参数:Cmax(0.04±0.01)μg/ml,Tmax(1.00±0.15)h,T1/2(2.35±0.17)h,AUC(0.13±0.01)(h·μg)/ml,V(1 024.1±98.4)L/kg,CLB(302.2±7.6)L/(kg·h),MRT(3.55±0.27)h;单剂量静注六氢β-酸月桂酸酯的主要药动学参数:C0(1.25±0.17)μg/ml,T1/2(1.10±0.25)h,AUC(0.82±0.14)(h·μg)/ml,V(1.93±0.13)L/kg,CLB(1.25±0.21)L/(kg·h),MRT(1.27±0.31)h。结果表明:灌胃六氢β-酸月桂酸酯[40mg/(kg·bw)]与静脉注射六氢β-酸月桂酸酯[1 mg/(kg·bw)]相比,鸡灌胃给药的生物利用度为0.4%,灌胃给药后吸收极少,静注浓度较高,消除半衰期均较短。  相似文献   

4.
为探究加米霉素在比格犬体内的药物代谢动力学特征,了解其在比格犬机体内的吸收、分布、转化以及排泄规律,选取6只比格犬,加米霉素以推荐剂量6 mg/kg皮下以及静脉分别单次给药,分别于不同时间点静脉采集犬血液,用高效液相色谱串联二级质谱法测定血液中药物浓度。用非房室模型对药时曲线进行分析,皮下注射药动学参数为:达峰时间(T_(max))为0.875 h±0.186 h,消除半衰期(T_(1/2β))为59.978 h±7.861 h,药时曲线下面积(AUC)为4.912μg·h/mL±0.738μg·h/mL。静脉注射药动学参数为:达峰时间(T_(max))为0.336 h±0.144 h,消除半衰期为(T_(1/2β))为49.028 h±5.012 h,药时曲线下面积(AUC)为3.774μg·h/mL±0.211μg·h/mL。试验结果表明,静脉或皮下注射加米霉素后,药物在比格犬体内的浓度较高,且皮下注射的生物利用度较高,推荐使用皮下注射的方式给药。  相似文献   

5.
本研究旨在考察国产麻保沙星溶液在健康犬体内的药动学特征及生物利用度.选用8只健康犬,按照随机拉丁方设计,进行单次不同单剂量(2.75 mg·kg-1)分别静注麻保沙星溶液和口服麻保沙星溶液制剂.血浆样品经乙腈沉淀血浆蛋白,高速离心,用反相高效液相色谱法测定犬血浆中麻保沙星的浓度,3P97药动学计算软件处理血浆药物浓度-时间数据.健康犬静注给药的药物动力学最佳数学模型为无吸收开放二室模型,主要药动学参数为:T1/2α(0.34±0.14)h,T1/2β(7.74±1.70)h,V(1.03±0.60)L·kg-1,CL(0.22±0.08)L·h-1;AUC(14.05±4.25)mg·mL-1·h.口服给药的药物动力学最佳数学模型为一级吸收二室模型.主要药动学参数为:T1/2α((2.82±1.86)h,T1/2β(16.03±9.27)h,V/F(2.25±0.34)L·kg-1,CL/F(0.21±0.05)L·h-1,Tmax(1.55±0.62)h,Cmax(0.89±0.21)μg·mL-1,AUC(13.66±2.77)mg·mL-1·h.肌注麻保沙星冻干粉针的生物利用度为97.22%.麻保沙星在健康犬体内口服的主要药动学特征为吸收较快,达峰时间短,半衰期较长,生物利用度高.  相似文献   

6.
为建立高效液相色谱法(HPLC)测定绵羊血浆中地昔尼尔的质量浓度,比较健康绵羊经皮肤浇泼地昔尼尔乳剂和进口地昔尼尔乳剂(Clik~)后的药动学特征及生物利用度,选用12头健康绵羊随机分为地昔尼尔乳剂组和Clik~组,公母各半,并以35 mg·kg-1的剂量于背正中线浇泼给药,在不同时间点内于颈静脉处采血,分离血浆,采用HPLC测定地昔尼尔的血药浓度。结果显示:地昔尼尔在20~10 000 ng·mL~(-1)浓度范围内线性良好,r~20.999,定量限(LOQ)为20 ng·mL~(-1);地昔尼尔以定量限、低、中、高(20、100、1 000、10 000 ng·mL~(-1))4个浓度添加水平的回收率均大于80%,精密度均小于15%;地昔尼尔乳剂组药动学参数:消除半衰期(T_(1/2λz))=(25.35±7.50)h,达峰时间(T_(max))=(46.00±4.90)h,达峰浓度(C_(max))=(473.73±102.53)ng·mL~(-1),药时曲线下面积(AUC_(0→t))=(20 856.38±4 178.93)ng·mL~(-1)·h;Clik~组药动学参数:T_(1/2λz)=(33.91±10.54)h,T_(max)=(44.00±6.20)h,C_(max)=(469.08±126.34)ng·mL~(-1),AUC0→t=(23 475.42±6 845.78)ng·mL~(-1)·h;地昔尼尔乳剂的相对生物利用度为88.84%。结果表明:该方法专属性强、重复性好、灵敏度高,适用于地昔尼尔在绵羊体内的药动学研究。  相似文献   

7.
为了考察国产马波沙星注射液在母猪体内的药动学数据,给临床用药提供依据。选用18头健康长白、大白母猪(体重222.0±31.9 kg),随机分为2组,分别以每千克体重2.0 mg的剂量静脉注射或肌肉注射马波沙星注射液。在给药前后按设计时间点从母猪前腔静脉采集血液,离心后取上清液,用反相高效液相色谱法(HPLC)测定血浆中药物的浓度,采用美国Pharsight公司药动学软件Winnonlin5.2.1的非房室模型来处理血浆药物浓度-时间数据。结果:主要药动学参数分别为:(1)肌肉注射马波沙星注射液:MRT(20.20±3.71)h;t_(1/2β)(21.09±5.18)h;AUC(32.94±4.41)μg/h·m L;t_(max)(1.72±0.97)h;C_(max)(1.90±0.69)μg/m L,生物利用度(F)为80.2%;(2)马波沙星注射液静注:MRT(18.94±4.10)h;t_(1/2β)(17.70±4.59)h;AUC(41.07±13.02)μg/h·m L;V_d(1.23±0.33)L/kg。表明:在健康母猪体内,马波沙星肌肉注射给药的主要药动学特征为:吸收迅速完全,消除缓慢,生物利用度高。  相似文献   

8.
研究新制剂三氮脒注射液在山羊体内的药动学特征。用三氮脒和三氮脒注射液给山羊单剂量(3.5mg·kg-1)肌内注射,采用高效液相色谱法测定山羊体内三氮脒含量,3P97软件拟合血药浓度-时间曲线,计算药动学参数。三氮脒和三氮脒注射液药动学参数符合一级吸收二室模型,主要药动学参数分别为:达峰浓度(Cmax)为(5.97±0.37)μg·mL-1和(7.63±0.41)μg·mL-1;达峰时间(Tmax)为(0.22±0.03)h和(0.40±0.10)h;吸收半衰期(t1/2ka)为(0.13±0.04)h和(0.04±0.01)h;药时曲线下面积(AUC)为(53.96±6.87)μg·mL-1*h和(77.43±6.71)μg·mL-1*h。三氮脒注射液与三氮脒相比,具有吸收缓慢、分布广、安全性好和作用时间长等特点,此结论为临床合理使用剂型提供依据和指导。  相似文献   

9.
《畜牧与兽医》2016,(5):122-125
为将绿原酸引入奶牛乳房炎的治疗,进行了绿原酸在奶山羊体内的药动学研究。本试验制备了奶山羊大肠杆菌性乳房炎病理模型,建立了反相高效液相色谱检测血清中绿原酸含量的方法,测定了静注、肌注绿原酸在健康奶山羊及乳房炎病理模型奶山羊体内的药动学参数,初步反映了绿原酸在奶山羊体内的动力学过程。经试验测定绿原酸在健康奶山羊体内,静注后呈二室开放模型,其药动学参数CO(μg/m L)为20.66±6.13,T1/2β(min)为7.27±1.19,CLB(L/kg·min-1)为0.27±0.34,AUC(mg/L·min-1)为81.83±14.87;肌注后呈一级吸收一室开放模型,其药动学参数Cmax(μg/m L)为0.40±0.11,AUC(mg/L·min-1)为41.54±17.16。绝对生物利用度平均为47。绿原酸在乳房炎奶山羊体内静注后呈二室开放模型,其药动学参数CO(μg/m L)为23.03±6.97,t1/2β(min)为9.01±4.16,AUC(mg/L·min)为96.68±16.93,CLB(L/kg·min-1)为0.10±0.02;肌注后呈一级吸收一室开放模型,其药动学参数Cmax(μg/m L)为0.48±0.37,AUC(mg/L·min)为38.02±23.69。绝对生物利用度平均为43%。  相似文献   

10.
建立了一种头孢维星在犬血浆中的高效液相色谱检测法,并研究了头孢维星在犬体内的药动学特征及生物利用度。选用健康家犬12只,按单剂量(8 mg/kg b.w.)分别静脉注射或皮下注射头孢维星,利用建立的方法对头孢维星在犬血浆中的浓度进行测定,采用Win Nonlin5.2.1程序的非房室模型处理药时数据。结果显示,静脉注射组的主要药动学参数为t1/2β=129.15±35.79 h;MRT=152.56±44.95 h;λz=0.0059±0.0023 h-1;Cl=1.24±0.56 m L/(h·kg);AUC=6942.88±2462.48μg獉h/m L;V=170.20±28.09 m L/kg。皮下注射组的主要药动学参数为t1/2β=136.94±20.96 h;MRT=167.77±28.15 h;Tmax=0.83±0.26 h;Cmax=59.51±7.99μg/m L;λz=0.0052±0.0009 h-1;Cl=1.05±0.21 m L/(h·kg);AUC=7332.58±1118.30μg·h/m L;V=203.81±30.09 m L/kg;F=105.61%。结果表明,头孢维星在家犬体内表现出吸收迅速、消除缓慢、表观分布容积大、生物利用度高等药动学特点。  相似文献   

11.
1-(2-Chloroethyl)3-cyclohexyl-1-nitrosourea (CCNU) is an alkylating agent in the nitrosourea subclass. A prospective evaluation of CCNU was done to determine the maximally tolerated dosage of CCNU in tumor-bearing cats. Response data were obtained when available. Twenty-five cats were treated with CCNU at a dosage of 50-60 mg/m3 body surface area. Complete hematologic data were available for 13 cats. Neutropenia was the acute dose-limiting toxicity. The median neutrophil count at the nadir was 1,000 cells/microL (mean, 2,433 cells/microL; range, 0-9,694 cells/microL). The time of neutrophil nadir was variable, occurring 7-28 days after treatment, and counts sometimes did not return to normal for up to 14 days after the nadir. Based on these findings, a 6-week dosing interval and weekly hematologic monitoring after the 1st treatment with CCNU are recommended. The nadir of the platelet count may occur 14-21 days after treatment. The median platelet count at the nadir was 43,500 cells/microL. No gastrointestinal, renal, or hepatic toxicities were observed after a single CCNU treatment, and additional studies to evaluate the potential for cumulative toxicity should be performed. Five cats with lymphoma and 1 cat with mast cell tumor had measurable responses to CCNU. Phase II studies to evaluate antitumor activity should be completed with a dosing regimen of 50-60 mg/m3 every 6 weeks.  相似文献   

12.
Human and equine athletes are reported to have a high prevalence of gastric disease, and anecdotal evidence suggests a similar phenomenon applies to racing sled dogs. To investigate the prevalence of gastric disease in racing sled dogs, we conducted 2 gastroscopy studies on dogs competing in the annual Iditarod Sled Dog Race. A pilot study of dogs that were either dropped from the 2000 Iditarod Sled Dog Race because of illness or that finished the race indicated that, approximately 5 days after competing, 10 of 28 dogs (35%) had endoscopic evidence of gastric ulceration, erosion, or hemorrhage. The next year, an endoscopic study of 73 dogs participating in the 2001 Iditarod race was performed in order to evaluate a larger population of dogs. Data from 70 of these dogs could be used; 34 (48.5%) had ulceration, erosion, gastric hemorrhage, or some combination of these findings. When this group of 70 dogs was compared retrospectively to a control group of 87 dogs presented to the Texas A&M University (TAMU) Veterinary Medical Teaching Hospital, the Iditarod sled dogs had a significantly higher prevalence (P = .049) of gastric lesions. These findings suggest that, similar to athletes of other species, elite canine athletes have an increased prevalence of gastric disease compared to the canine population at large.  相似文献   

13.
Continuous rate infusion (CRI) of furosemide in humans is considered superior to intermittent administration (IA). This study examined whether furosemide CRI, compared with IA, would increase diuretic efficacy with decreased fluid and electrolyte fluctuations and activation of the renin-angiotensin-aldosterone system (RAAS) in the horse. Five mares were used in a crossover-design study. During a 24-hour period, each horse received a total of 3 mg/kg furosemide by either CRI (0.12 mg/kg/h preceded by a loading dose of 0.12 mg/kg IV) or IA (1 mg/kg IV q8h). There was not a statistically significant difference in urine volume over 24 hours between methods; however, urine volume was significantly greater after CRI compared with IA during the first 8 hours ([median 25th percentile, 75th percentile]: 9.6 L [8.9, 14.4] for CRI versus 5.9 L [5.3, 6.0] for IA). CRI produced a more uniform urine flow, decreased fluctuations in plasma volume, and suppressed renal concentrating ability throughout the infusion period. Potassium, Ca, and Cl excretion was greater during CRI than IA (1,133 mmol [1.110, 1,229] versus 764 mmol [709, 904], 102.7 mmol [96.0, 117.2] versus 73.3 mmol [65.0, 73.5], and 1,776 mmol [1,657, 2.378] versus 1,596 mmol [1,457, 1,767], respectively). Elimination half-lives of furosemide were 1.35 and 0.47 hours for CRI and IA, respectively. The area under the excretion rate curve was 1,285.7 and 184.2 mL x mg/mL for CRI and IA, respectively. Furosemide CRI (0.12 mg/kg/h) for 8 hours, preceded by a loading dose (0.12 mg/kg), is recommended when profound diuresis is needed acutely in horses.  相似文献   

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The epidemiology of H. placei and of other gastrointestinal nematodes in yearling dairy cattle was examined on two farms in Kiambu District, central Kenya during each of 13 one-month periods from April 1993 to April 1994. On each farm, 32 newly weaned dairy calves were given a single dose of albendazole and then placed on experimental pastures. Twelve of the animals were designated for bi-monthly slaughter (n = 2) and analysis of worm population characteristics and 20 were designated for blood and faecal collection and for weighing. Two parasite-free tracer calves were grazed alongside the weaner calves each month throughout the study period and were also slaughtered for analysis of worm populations. Faecal egg counts, haematological and serum pepsinogen determinations, herbage larval counts, and animal live weight changes were recorded monthly. The study revealed that Haemonchus placei, Trichostrongylus axei, Cooperia spp. and Oesophagostomum radiatum were responsible for parasitic gastroenteritis and that H. placei was the predominant nematode present in the young cattle on both farms. Faecal egg counts from resident cattle and necropsy worm counts revealed that pasture larval levels were directly related to the amount of rainfall. The total worm burdens in the animals were highest during the rainy season (March–June and October–December) and lowest during the dry seasons (July–September and January–February). The very low recovery of immature larvae of H. placei from the tracer calves indicated that arrested development is not a feature of the life cycle of this parasite in central Kenya. The maintenance of the parasite population depended on continuous cycling of infection between the host and the pasture. The agroclimatic conditions of the study area were such that, in general, favourable weather conditions for the development and survival of the free-living stages of gastrointestinal nematodes existed all year round.  相似文献   

16.
The occurrence of ectoparasites in sheep flocks is frequently reported but seldom quantified. Sheep production used to be a predominantly family activity in the state of Sa~o Paulo (Brazil), but it began to become a commercial activity in the past decade. Thus, information about the ectoparasites existing in sheep flocks has become necessary. The present data were obtained by means of questionnaires sent to all sheep breeders belonging to the `Associaça~o Paulista de Criadores de Ovinos' (ASPACO; Sa~o Paulo State Association of Sheep Breeders). Response reliability was tested by means of random visits paid to 10.6% of the respondents. Most of the properties (89.5%) reported the presence of one or more ectoparasites. Screw-worm (Cochliomyia hominivorax) was the most frequent ectoparasite (72.5%), followed by bot fly larvae (Dermatobia hominis, 45.0%), ticks (Amblyomma cajennense) and Boophilus microplus, 31.3%) and finally lice (Damalinia ovis, 13.8%). Combined infestations also occurred, the most common one being screw-worm with bot fly larvae (36.0%) followed by bot fly larvae with ticks (13.9%), screw-worm with ticks (9.3%), bot fly larvae with lice (6.9%), and ticks with lice (5.0%). The most common triple combination was screw-worm, bot fly larvae and ticks (12.8%). Breeds raised for meat or wool were attacked by bot fly larvae and ticks more often than other breeds. Lice were only absent from animals of indigenous breeds. The relationships among these ectoparasites are discussed in terms of sheep breeds, flock size, seasonality and the ectoparasitic combinations on the host.  相似文献   

17.
Our particular attention in this article was given to natural mediators for macrophages isolated from the sites of tissue injury. A number of chemotactic factors, which may satisfy many criteria making them acceptable as inflammatory leucocyte chemotactic factors, has been separated. Among them, our laboratory has isolated three macrophage (monocyte) chemotactic factors (MCF-a, -b and -c). Their purification, characterization and functional specificity are discussed.  相似文献   

18.
19.
An experiment was conducted to study disappearance of C14 to C18 fatty acids, lag times and biohydrogenation (BH) rates of C18 fatty acids of ground soya bean and canola seeds in situ. Three ruminally fistulated Dallagh sheep were used to determine ruminal BH of unsaturated fatty acids (UFAs). Differences in the disappearance of fatty acids through the bags and lag times were observed between the oilseeds. We saw that the longer the incubation time of the oilseeds in the rumen, the lower the content of C18:2 and C18:3. Significantly higher lag times for both C18:2 and C18:3 were observed in ground canola compared to ground soya bean. BH rates of C18:2 and C18:3 fatty acids in soya bean were three times higher than those of canola. These results suggest that the fatty acid profile of fat source can affect the BH of UFAs by rumen micro‐organisms. So that UFAs of canola had higher ability to escape from ruminal BH. It seems that fatty acid profile of ruminant products is more affected by canola seed compared to soya bean seed.  相似文献   

20.
Serum biochemical values and the wet weight to dry weight ratios of tissues were determined in yaks in Shandan county of Gansu province. The liver, kidney, heart and muscle contents of seven elements in yaks were also analysed. Most serum biochemical values were similar to those of cattle, camels and sheep, but the calcium concentration was considerably above the normal range for other ruminants. The liver contained the highest concentrations of copper, manganese and cobalt and the kidney of selenium, iron and calcium.Abbreviations Alb albumin - ALT alanine aminotransferase - AST aspartate aminotransferase - BUN blood urea nitrogen - Chol cholesterol - Glob globulin - -GT -glutamyl transpeptidase - IP inorganic phosphorus - TP total protein  相似文献   

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