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1.
两种盐酸多西环素注射液在猪体内的药代动力学研究   总被引：1，自引：1，他引：0  
研究制备了两种稳定的20％盐酸多西环素注射液,按10 mg/kg的剂量分别给猪肌肉注射,观察两个制剂在猪体内单剂量肌注的药代动力学特征.结果表明,多西环素在猪体内的药物动力学特征均符合一级吸收二室开放模型,其主要的药物代谢动力学参数:消除半衰期(T1/2β)分别为(3.246±1.04)和(9.631±1.12)h,药时曲线下面积(AUC)为(10.462±0.28)和(17.525±0.14)(μg/mL)*h,达峰时间(Tpeak)及达峰浓度(Cmax)分别为(1.427±0.16)h、(1.465±0.20) μg/mL和(1.694±0.15)h、(1.058±0.09) μg/mL.其中制剂一的血药浓度在给药2h后迅速降低,为普通注射液;与制剂一相比,制剂二能够缓慢释放药物,为长效缓释盐酸多西环素注射液.  相似文献   

2.
本文比较了恩诺沙星注射剂和长效恩诺沙星注射液体外释药动力学和在山羊体内的药动学特征。采用紫外分光光度法测定了体外释放率;选用8头健康山羊进行肌注长效恩诺沙星注射液和恩诺沙星注射液的药物动力学研究,以反相高效液相色谱法测定血浆中恩诺沙星的浓度。恩诺沙星普通注射液1h体外累计释药百分率达83 22%,而长效恩诺沙星注射液10h释药仅80 56%。肌注长效恩诺沙星注射液和恩诺沙星注射液的药时数据符合一级吸收一室模型,主要药动学参数分别为:T1/2Ka1 76±0 12hand0 34±0 04h(P<0 01);T2/1Ke7 50±0 39hand1 15±0 10h(P<0 01);Tmax4 81±0 26hand0 85±0 09h(P<0 01)。两者的体外释药率和药代动力学参数有显著差异,前者的吸收半衰期、达峰时间及消除半衰期分别为后者的5 2、5 7和6 5倍。说明恩诺沙星注射液肌注后吸收缓慢、消除半衰期延长,具有缓释特征,能起到长效的作用。  相似文献   

3.
《中国兽医学报》2014,(10):1657-1662
研究并比较了头孢噻呋注射液和速解灵注射液在猪体内药物代谢动力学特征和相对生物利用度。20头健康猪,随机均分为2组,进行单次给药剂量(5mg/kg)肌注头孢噻呋注射液(洛阳惠中)和速解灵注射液(美国辉瑞),前腔静脉采血,高效液相色谱法检测猪血浆中头孢噻呋的浓度。采用药动学软件WinNonlin 5.2.1的非房室模型分析方法,计算出药物的动力学参数。猪肌注头孢噻呋注射液和速解灵注射液后的药动学参数分别为:达峰时间(Tmax):(2.63±0.74)、(3.38±1.92)h;峰质量浓度(Cmax):(14.06±2.21)、(9.48±1.84)mg/L;消除半衰期(t1/2β):(17.65±2.07)、(17.70±2.43)h;平均滞留时间(MRT):(23.21±2.68)、(22.11±2.50)h;药时曲线下面积(AUClast):(240.81±47.73)、(182.51±36.12)μg·h·mL-1。参数Cmax、AUClast统计差异极显著(P<0.01),头孢噻呋注射液较速解灵注射液吸收迅速、完全,达峰时间短,峰浓度显著升高;参数Tmax、t1/2β、MRT统计差异不显著(P>0.05),头孢噻呋注射液的相对生物利用度为132%,高于速解灵注射液。结果表明头孢噻呋注射液肌注后吸收迅速、完全,达峰时间短,峰浓度高,生物利用度高。  相似文献   

4.
恩诺沙星长效注射液肌注后在猪体内的药动学研究   总被引：2，自引：0，他引：2  
研究了恩诺沙星长效注射液给猪肌注后的药物动力学特征。将12只白猪随机分成两组,每组6只,分别肌注恩诺沙星注射液(5mg/kg)和长效恩诺沙星注射液(18.75mg/kg),并于给药后0.1, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 60h, 从前腔静脉采取5ml血,用HPLC分析各血浆样品中的药物浓度,用MCPKP软件计算药动学参数。结果表明:长效恩诺沙星注射液肌注后,经5.64h达到4.86μg/ml的最高浓度,吸收半衰期和消除半衰期分别为2.42h和19.47h,有效浓度维持时间为128.73h, AUC为166.96mg/L.h。吸收半衰期显著延长(p<0.05),达峰时间极显著推迟(p<0.01),消除半衰期也显著长于恩诺沙星注射液。  相似文献   

5.
盐酸多西环素缓释注射液在猪体内的药物动力学   总被引：2，自引：0，他引：2  
健康猪6头,体质量(17.85±1.3)kg,按拉丁方设计进行单剂量静注、肌注盐酸多西环素注射液(普通制剂)和肌注盐酸多西环素缓释注射液,注射剂量按多西环素计均为20 mg/kg,比较盐酸多西环素缓释注射液和盐酸多西环素注射液在猪体内的药动学特征和生物利用度.用高效液相色谱法测定其血药浓度,试验所得的血药浓度-时间数据采用非房室模型统计矩原理分析处理.猪静注盐酸多西环素注射液的主要药物动力学参数为AUC(108.15±13,25)mg·h·L-1,MRT(5.56±1.08)h,CI(0.19±0.02)L·h-1·kg-1,Vd(ss)(1.04±0.09)L·kg-1,t1/2(4.07±0.65)h.猪肌注盐酸多西环素注射液和盐酸多西环素缓释注射液的主要药物动力学参数分别为MRT(15.18±2.13)h和(22.25±3.49)h;Tmax(1.135±0.44)h和(2.0±0.63)h;Cmax(3.32±0.33)mg·L-1和(3.10±0.29)mg·L-1;AUC(38.91±4.35)mg·h·L-1和(61.72±10.16)mg·h·L-1;F(36.66±7.88)%和(57.66±10.75)%.比较盐酸多西环素注射液和盐酸多西环素缓释注射液的主要药动学参数,除了Cmax以外,MRT、Tmax、AUC、F等主要参数均有显著的统计学意义(P＜0.05).这表明盐酸多西环素缓释注射液肌注后吸收缓慢.消除半衰期延长,临床用药48 h给药1次仍能维持对常见病原菌的有效血药浓度.  相似文献   

6.
本实验采用高效液相色谱法测定猪血浆中阿莫西林的浓度,研究了丙磺舒对阿莫西林在健康猪体内药物动力学的影响。结果表明,单剂量肌肉注射阿莫西林后,阿莫西林吸收迅速,药峰时间为(0.19±0.11)h,药物浓度为(7.21±3.27)μg/mL,其动力学模型为一级速率一室模型。使用丙磺舒后,阿莫西林的半衰期由(0.86±0.18)h延长到(2.77±1.02)h(P<0.05),AUC由(12.38±5.69)μg/mL·h增加至(35.24±18.62)μg/mL·h,药峰时间为(0.42±0.32)h,药峰浓度为(6.24±3.43)μg/mL·h。  相似文献   

7.
研究秃疮花在山羊体内的药物动力学。结果表明,山羊肌注秃疮花针剂后,秃疮花提取物在山羊体内的药动学配置均符合有吸收因素二室开放模型特征,其最佳药-时曲线方程分别为:C=7.344 3e~(-0.148 8t)+1.803 3 e~(-0.058 3t)-9.147 6 e~(-1.628 3t)。主要药物动力学参数:制剂吸收半衰期t_(1/2ka)为(0.425 8±0.006 5)h,分布相半衰期t_(1/2α)为(4.680 6±0.358 2)h,消除半衰期t_(1/2β)为(12.684 8±3.685 0)h,药-时曲线下面积AUC为(73.307 0±0.732 9)μg/(mL·h)峰质量浓度为(6.753 8±0.060 8)μg/mL,达峰时间为(1.690 0±0.015 5)h。提示秃疮花提取物在山羊体内分布较广,吸收快,消除较慢,血药浓度维持时间较长。  相似文献   

8.
研究分析长效土霉素注射液作用于猪体内的生物等效性,为临床的进一步研究提供参考依据。方法:选取24头猪,将其随机分为两组,对照组1和对照组2,对照组1注射30%长效土霉素注射液;对照组2则注射20%长效土霉素注射液。采用高效液相色谱法对猪体内的血浆土霉素浓度进行测定,分析其生物等效性。结果:对照组1和对照组2的药动学参数为:药物吸收半衰期为(0.088±0.014)h和(0.140±0.076)h;消除半衰期为(52.489±21.885)h和(36.481±21.568)h;峰浓度为(4.986±1.786)μg/ml和(5.016±0.948)μg/ml;达峰时间为(0.609±0.110)h和(0.823±0.372)h;药时曲线下面积为(112.482±18.564)mg/L.h和(109.877±19.946)mg/L.h;以20%长效土霉素注射液作为对照,30%长效土霉素注射液相对生物利用度为(105.465±26.103)%。结论:研究结果表明,两种不同浓度的长效土霉素注射液的药动学参数不具有显著差异,由此看来两种药物具有生物等效性。  相似文献   

9.
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   

10.
为了探究泰地罗新在猪体内的药物动力学特征以及口服生物利用度,本试验通过给猪单次口服和静脉注射泰地罗新,来研究泰地罗新在猪体内的药物动力学特征以及生物利用度。试验结果显示,泰地罗新口服在猪体内吸收半衰期(t1/2ka)为1. 057 h,消除半衰期(t1/2β)为80. 9h,达峰时间(Tmax)为2. 10 h,峰浓度(Cmax)为0. 51μg/m L,其吸收快,消除半衰期长,单次口服给药可长时间维持较高的血药浓度,口服给药在猪体内的生物利用度为72. 9%。研究表明,说泰地罗新在猪体内的口服生物利用度较高,在猪体内分布广,口服和静注的消除半衰期无明显差异,较为适合口服给药。  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.
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   

13.
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   

14.
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   

15.
Comparison of different tests to diagnose feline infectious peritonitis   总被引：1，自引：0，他引：1  
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16.
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   

17.
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   

18.
A knowledge of the microbiological status of milk and of the different structures in the mammary glands has great importance in elucidating the pathogenesis of mammary gland infections. The objective of this study was to evaluate the microbiological status of various structures in the mammary glands from naturally infected dairy cows following slaughter. A total of 94 samples of milk, 184 samples of mammary parenchyma, 168 samples of gland cisterns, and 168 samples of teat cisterns were collected for microbiological examination. Microorganisms were detected in 59.9% of all samples, 67.0% of the milk samples, 70.1% of the mammary parenchymas, 55.9% of the gland cisterns and 48.8% of the teat cistern samples. When all samples were considered, coagulase-negative Staphylococcus were the most prevalent (35.7%) followed by coagulase-positive Staphylococcus (12.2%), Corynebacterium bovis (2.4%), Prototheca sp. (1.9%), and Streptococcus dysgalactiae (1.5%). There was a significantly higher occurrence of microorganisms in the milk and mammary parenchyma compared to the gland cisterns and teat cisterns. This revised version was published online in July 2006 with corrections to the Cover Date.  相似文献   

19.
Four grass plots were sequentially contaminated with goat faeces containing known numbers of unembryonated eggs of predominantly Haemonchus contortus and Trichostrongylus spp. between October 1982 and April 1983. Four other plots were similarly contaminated with sheep faeces between February and May 1987. An additional plot was repeatedly contaminated with sheep faeces from February to April 1987. Populations of free-living stages in faeces and of infective larvae (L3) in the herbage were subsequently monitored until the end of April and June of 1983 and 1987 respectively. During February and May 1987 two control cultures of sheep faeces were incubated in the laboratory at 25°C–30°C and at a constant temperature of 50°C and the free-living development was also monitored. L3 developed very readily in the faeces cultured at 25°C–30°C and in those spread on a grass plot in October, at the end of the wet season, but developed less on the plot contaminated in May at the start of the wet season. Worm eggs in faeces deposited on plots during the hot dry season (December to April) or incubated at 50°C died and disintegrated after 24–48 h exposure to the high environmental temperatures. The results indicate that it is unlikely that gastrointestinal nematodes of sheep and goats can develop or survive on open pasture during the dry season in the Nigerian derived savanna zone.  相似文献   

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