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1.
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   

2.
盐酸多西环素在猪体内的药物动力学及其残留   总被引:5,自引:0,他引:5  
试验建立了反相高效液相色谱(RT-HPLC)法测定盐酸多西环素的浓度,探讨了盐酸多西环素在猪体内的药物动力学和残留特征。结果表明,盐酸多西环素以2.5mg/kg单剂量肌内注射给猪(n=6),药物动力学模型符合有吸收一室模型,药物动力学参数:吸收半衰期(t1/2ka)、消除半衰期(t1/2ke)为(0.400±0.312)h、(9.530±0.956)h,药时曲线下面积(AUC)为(44.414±4.123)mg·h·L-1,最大血药浓度(Cmax)为(2.811±0.136)mg/L,达峰时间(Tp)为(1.910±0.213)h。另外,以相同剂量肌内注射给猪(n=6),每天1次,连续给药4d后,在不同时间测定盐酸多西环素在猪的肌肉、肝脏、肾脏、皮肤和脂肪中的残留量。在给药后16d,盐酸多西环素在各组织均能检测到,且残留均低于残留限量。盐酸多西环素注射液在猪体内消除缓慢,残留期较长,建议休药期不低于16d。  相似文献   

3.
《中国兽医学报》2015,(12):2002-2007
对麻鸭单次静脉注射、肌内注射和灌胃多西环素后进行药动学研究,给药剂量均为20 mg/kg。麻鸭给药后定点采血,分离血浆,然后以高效液相色谱法测定血浆中的药物浓度,并利用房室分析法计算3种不同给药途径下多西环素的药动学参数。结果显示:静脉注射后,多西环素分布广泛,其表观分布容积(V_d)为(768.50±119.61)m L·kg~(-1),且消除缓慢,消除半衰期(t_(1/2β))为(16.62±0.84)h;而灌胃和肌内注射后,多西环素均迅速吸收,峰浓度(C_(max))分别为(11.32±3.46),(19.70±2.79)mg·L~(-1),达峰时间(t_(max))分别为(2.51±0.23),(1.56±0.09)h,绝对生物利用度则分别为39.44%,77.67%。本研究结果证实多西环素在麻鸭体内具有优异的药动学特征,其吸收迅速、分布广泛、消除缓慢,但同时灌胃后其生物利用度较低。因此推荐多西环素在麻鸭感染性疾病治疗中的给药方案为灌胃或肌内注服给药,剂量均为20 mg·kg~(-1)·d~(-1),连用3 d。  相似文献   

4.
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   

5.
《畜牧与兽医》2014,(6):83-86
为了研究不同水温下多西环素在草金鱼体内过程,本试验采用对草金鱼以30 mg/kg的剂量单次口灌多西环素。结果显示:多西环素在草金鱼体内吸收迅速,分布广泛,消除半衰期长。房室模型分析表明,在2个水温条件下的药时数据均符合有吸收二室开放模型,15℃条件下的主要药物动力学参数为:吸收半衰期(T1/2ka)1.38 h;分布半衰期(T1/2α)2.06 h;达峰时间(Tmax)2.70 h;峰浓度(Cmax)4.57μg/mL;消除半衰期(T1/2β)62.57 h;药时曲线下面积(AUC)138.20μg·h/mL。25℃条件下的主要药物动力学参数为:吸收半衰期(T1/2ka)1.33 h;分布半衰期(T1/2α)0.77 h;达峰时间(Tmax)1.78 h;峰浓度(Cmax)4.06μg/mL;消除半衰期(T1/2β)25.73 h;药时曲线下面积(AUC)82.80μg·h/mL。  相似文献   

6.
分别用水中干燥法和油中干燥法制备盐酸多西环素微囊,比较各自制得的微囊质量参数及其体外释药特性,以期为盐酸多西环素缓释制剂提供科学依据.以乙基纤维素为囊材,通过正交设计分别考察各因素对微囊质量的影响,评定微囊的大小、形态、载药量、包封率等质量指标,以释放度实验研究其释药特性.结果显示,水中干燥法所制得微囊粒径20 ~ 30 μm,包封率为87.3%;油中干燥法微囊粒径范围为200~400μm,包封率为93.7%.上述结果表明油中干燥法所得微囊粒径较大,包封率、载药量均明显高于水中干燥法制得的微囊;体外释药实验表明,微囊化大大延缓了盐酸多西环素的释放时间.  相似文献   

7.
为研究盐酸多西环素注射液对家畜局部肌肉组织的刺激性,文章选用健康合格的新西兰家兔为试验动物,采用同体左右侧自身对比法,进行盐酸多西环素注射液局部刺激性试验。结果显示,盐酸多西环素注射液按5mg/kg及10mg/kg体重剂量对家兔肌注,刺激性较小,可用于肌肉注射,因此按临床推荐剂量肌注给药是安全的。  相似文献   

8.
目的 研究非布司他片在中国健康受试者体内单次及多次给药的药动学特征。方法 30名受试者随机分为3组,每组10人,男女各半,一组进行非布司他片中剂量(80 mg)的单/多次给药人体药动学试验,10名受试者每天服药1次,每次80mg,一共服药6次;一组进行非布司他片低剂量(40 mg)的单次给药人体药动学试验;一组进行非布司他片高剂量(120 mg)的单次给药人体药动学试验。血药浓度用LC-MS/MS快速测定。结果 单次空腹口服非布司他片40,80,120 mg后,其主要药动学参数如下:ρmax分别为(2 578±743),(4 522±1 376)和(6 407±2 463)ng·m L-1;tmax分别为(1.80±1.15),(1.78±1.18)和(2.28±1.57)h;t1/2分别为(6.21±2.11),(6.14±0.99)和(5.93±1.82)h;AUC0-36 h分别为(6 949±1 947),(14 875±4 200)和(23 881±6 225)ng·h·m L-1;AUC0-∞分别为(7 039±1 931),(14 995±4 287)和(24 056±6 236)ng·h·m L-1。多次口服80 mg非布司他片后,其主要药动学参数如下:tmax为(1.60±0.74)h,t1/2为(5.27±1.08)h,cSSmax为(4 326±1 477)ng·m L-1,cSSmin为(33.97±7.84)ng·m L-1,cSSav为(622.7±165.8)ng·m L-1,AUCSS为(14 945±3 979)ng·h·m L-1,AUC0-36 h为(15 196±4 119)ng·h·m L-1,AUC0-∞为(15 291±4 110)ng·h·m L-1。结论 非布司他片在剂量为40~120 mg内呈线性药代动力学特征,多次口服非布司他片每日1次,每次80 mg,不存在蓄积现象。  相似文献   

9.
比较国产和进口烯丙孕素口服液在健康母猪体内的药物代谢动力学。将16头健康苏姜商品母猪随机分为2组,分别单剂量灌服国产烯丙孕素口服液和进口烯丙孕素口服液,按体重给药量均为1.0 mg/kg,进行药动学比较研究。给药后按预定时间采集血样,采用液相色谱-串联四级杆质谱法测定血浆中烯丙孕素含量,实测血药浓度-时间数据采用WINNONLIN 6.3版药动学分析软件处理。国产制剂和进口制剂的达峰时间(Tmax)分别为(0.81±0.14)h、(1.59±0.80)h;达峰浓度(Cmax)分别为(175.19±58.12)ng/m L、(100.47±19.64)ng/m L;消除半哀期(t1/2)分别为(3.89±0.75)h、(3.14±0.24)h;平均滞留时间(MRT0~t)分别为(5.05±0.36)h、(5.06±0.71)h;药时曲线下面积(AUC0-t)分别为(729.82±179.76)ng·h·m L-1、(554.56±156.55)ng·h·m L-1。国产烯丙孕素口服液的相对生物利用度为131.60%。国产烯丙孕素口服液Cmax显著高于进口烯丙孕素口服液,而其它参数t1/2、Tmax、AUC0-t、MRT0~t无显著性差异。研究表明,国产烯丙孕素口服液在母猪体内具有吸收好、消除快、生物利用度高等优点。  相似文献   

10.
为了考察银翘药对配伍的科学性,利用高效液相色谱法分析检测了金银花注射液(A)、连翘注射液(B)、银翘药对注射液(C)以及金银花注射液、连翘注射液的混合液(D)主要成分绿原酸、连翘苷在家兔体内的药动学过程。结果A、C、D 3种注射液肌注后绿原酸在家兔体内药动学过程符合二室模型,其Cmax分别为:1.567、1.656、1.612 g.L-1;Tmax分别为:0.413、0.224、0.285 h;Tβ/2分别为1.164、1.227、1.132 h;AUC分别为1.905、2.623、2.114 mg.h.L-1;B、C、D 3种注射液肌注后连翘苷在家兔体内药动学过程符合一室模型,其Cmax分别为1.548 g.L-1、1.902、1.576 g.L-1;Tmax分别为:0.742、0.606、0.646 h;Tβ/2分别为1.272、1.212、1.220 h;AUC分别为2.80、3.216、2.881 mg.h.L-1。试验结果经统计学分析,配对能缩短绿原酸达峰时间Tmax,混合煎煮能提高连翘苷药峰浓度Cmax;配对并混合煎煮2种成分的药时曲线下面积(AUC)均显著提高,说明银翘配对并混合煎煮具有其科学依...  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   

14.
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   

15.
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   

16.
17.
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   

18.
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   

19.
正We are pleased to publish the second special issue on avian brood parasitism and to be responsible guest editors for the two special issues of Chinese Birds (Vol. 3, No. 4, 2012 and Vol. 4, No. 1, 2013), entitled "Avian Brood Parasitism - A Growing Research Area in Behavioral Ecology". The first issue was published in December 2012. The goal of the two special issues is to publish accumulated knowledge and some of the recent developments in  相似文献   

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