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1.
Pharmacokinetic parameters of florfenicol were determined in 10 adult sheep (five wethers and five ewes) after a single 40 mg/kg intravenous (i.v.) dose, and three daily subcutaneous (s.c.) doses of 40 mg/kg of a commercial preparation (Nuflor((R))). The concentration of florfenicol in serum samples was assayed using a proprietary HPLC assay method, and pharmacokinetic parameters derived for individual animal data by each route using compartmental and noncompartmental approaches. Two animals (one male and one female) were excluded due to observed i.v. dosing problems, and a biexponential model was found to fit the i.v. data well for six of the other eight animals. Data from two males showed prolonged low concentrations of florfenicol in serum and were better fit by a three-compartment model. The mean +/- SD for the half-lives of the distribution and elimination phases for the six sheep best fit with a two-compartment model were 0.069 +/- 0.018 and 1.01 +/- 0.09 h respectively, and for the V(d(ss)) and clearances were 0.503 +/- 0.035 L/kg and 366 +/- 53 mL/h/kg respectively. The data collected during the s.c. multiple dose study were analyzed using noncompartmental methods only. The bioavailability (F%) after s.c. dosing was calculated in three ways to compare estimation methods as steady-state had not been reached and single dose s.c. data were not obtained past 24 h. Using the AUC(0--24) and AUC(0--> infinity ) from the first dose, the F% values averaged 27 and 40% respectively. Using the AUC(0--> infinity ) for all doses, the F% was 65%. Calculations of the mean time during which the serum concentration exceeded 0.5 and 1.0 microg/mL were 105 +/- 3.9 and 74.7 +/- 12.2 h respectively.  相似文献   

2.
Objective  To evaluate the circadian rhythms of intraocular pressure (IOP) and tear production in dog exposed to a natural photoperiod.
Animals studied  We used 12 clinically healthy Beagles dog housed under natural photoperiod at indoor temperature and humidity.
Procedure  Intraocular pressure and Schirmer tear test (STT) I were measured every 4 h over a 48-h period in both eyes in each animal. Statistical analysis of the data was performed by one-way repeated-measures anova , Student's t -test, and single cosinor method.
Results  On each day, there was a highly significant effect of time on both parameters. A statistically significant difference of STT I values was observed comparing left and right eyes ( P  < 0.0001). Robust daily rhythms were observed for both parameters, IOP values showed diurnal acrophase (left eye: 09:33 ± 00:50 h; right eye: 09:25 ± 00:22 h), while STT I values showed nocturnal acrophase (left eye: 20:27 ± 00:46 h; right eye: 20:00 ± 00:05 h).
Conclusion  This study has demonstrated circadian rhythms in both IOP and STT I.  相似文献   

3.
The aim of to the present study was to evaluate the effects of verapamil (VER) on plasma pharmacokinetics of ivermectin (IVM) and doramectin (DOR) in lactating Istrian Pramenka dairy sheep and to investigate the role of P-glycoprotein (P-gp) in transport of avermectins into milk. Pharmacokinetics of IVM and DOR following subcutaneous administration of 0.2mg/kg b.w. was evaluated in four groups of sheep. They were administered either IVM or DOR alone or in combination with verapamil (VER) at a dose of 3.0mg/kg b.w., 3 times at 12h intervals. Blood plasma and milk samples were collected at defined time intervals over 30 days post-treatment to determine IVM and DOR concentration levels. Pharmacokinetic parameters in sheep injected with IVM or DOR alone corresponded to previously published values. Comparison between sheep injected with IVM only, and sheep injected with IVM in combination with VER (IVM+VER) showed significant difference in pharmacokinetic parameters in blood plasma. Area under the concentration-time curve (AUC) truncated at 2 days (AUC(2)) was 15 and 28 μg day/L for group IVM and IVM+VER, respectively. With co-administration of VER, apparent plasma clearance (Cl/F) and mean residence time (MRT) of IVM decreased from 135 to 116 L/day and from 5.8 to 3.8 days, respectively. Similar trends were observed for DOR (AUC(2) 48 vs. 68 μg day/L, Cl/F 61 vs. 46 L/day, and MRT 5.6 vs. 4.4 days for groups DOR and DOR+VER, respectively). This study confirms that co-administration of VER has a significant effect on pharmacokinetic parameters of subcutaneously administered IVM in blood plasma. The influence on DOR pharmacokinetics is much weaker. This could be either due to the difference in lipophilicity or the difference in affinity towards P-gp as a result of structural differences. No significant influence of VER on AUC ratio of IVM and DOR between milk and plasma was observed suggesting that P-gp does not govern transport of avermectins into milk.  相似文献   

4.
In this investigation the pharmacokinetics of three commonly used antibiotics, ampicillin trihydrate (10 mg/kg), gentamicin sulphate (3 mg/kg) and oxytetracycline hydrochloride (5 mg/kg), given intravenously, were each studied in five Nubian goats and five desert sheep. The pharmacokinetic parameters were described by a two-compartment open model. The results indicated that there were significant differences between the two species in some kinetic parameters of ampicillin and oxytetracycline but not gentamicin. Ampicillin elimination half life ( t 1/2β) in goats (1.20 h) was shorter than that in sheep (2.48 h), and its clearance ( Cl ) significantly higher in goats (2921mL/h·kg) compared to sheep (262 mL/h·kg) ( P < 0.01). Ampicillin volume of distribution ( V darea) was found to be significantly larger in goats (5673 mL/kg) than in sheep (992 mL/kg) ( P < 0.01). For oxytetracycline, the t 1/2β in goats (3.89 h) was significantly shorter than that in sheep (6.30 h) and the Cl value in goats (437 mL/h·kg) was significantly higher than in sheep (281 mL/h·kg). The results suggest that when treating sheep and goats, the pharmacokinetic differences between the two species must be considered in order to optimize the therapeutic doses of ampicillin and oxytetracycline.  相似文献   

5.
The pharmacokinetics of diclofenac was investigated in sheep given diclofenac alone (1mgkg(-1), i.v. or i.m.) and in combination with enrofloxacin (5mgkg(-1), i.v.). The plasma concentration-time data following i.v. administration of diclofenac was best described by a two compartment open pharmacokinetic model. The elimination half-life (t(1/2beta)), area under concentration-time-curve (AUC), volume of distribution (Vd(area)), mean residence time (MRT) and total body clearance (Cl(B)) were 1.03+/-0.18h, 12.17+/-1.98microg h ml(-1), 0.14+/-0.02Lkg(-1), 1.36+/-0.16h and 0.10+/-0.02Lkg(-1)h(-1), respectively. Following i.m. administration of diclofenac alone and in conjunction with enrofloxacin, the plasma concentration-time data best fitted to a one compartment open model. The t(1/2beta), AUC, Vd(area), MRT and Cl(B) were 1.33+/-0.10h, 7.32+/-1.01microg h mL(-1), 0.13+/-0.01Lkg(-1) and 0.07+/-0.01Lkg(-1)h(-1), respectively. Co-administration of enrofloxacin did not affect Vd(area) and MRT but absorption rate constant (K(a)), beta, t1/2Ka, t1/2beta, AUC, AUMC, Cl(B) and bioavailability (F) were significantly increased. This may be due to direct inhibition of cytochrome P(450) isozymes by enrofloxacin. A dose of 1.4mgkg(-1) of diclofenac administered every 6h may be appropriate for use in sheep.  相似文献   

6.
The main goal of present study was to determine the effects of an Escherichia coli endotoxin-induced endotoxaemic status on disposition of enrofloxacin after a single intravenous dose (5 mg/kg) in rabbits. Septic shock was induced by the i.v. bolus administration at a single dose of E. coli lipopolysaccharide. Six adult New Zealand White rabbits were used. Concentrations of drug in plasma were determined by HPLC. The plasma pharmacokinetic values for enrofloxacin were best represented using a two-compartment open model. Total plasma clearance (Cl(T)) decreased from 2.11 (l/h/kg) in healthy animals to 1.50 (l/h/kg) in rabbits with septic shock, which is related to an increase in the AUC(0-->infinity). In endotoxaemic rabbits, volume of distribution at steady state (V(dss) = 3.61 l/kg) was significantly lower (P < 0.05) than in healthy animals (V(dss) = 4.97 l/kg). However, the elimination half-life of enrofloxacin was not affected by lipopolysaccharide administration.  相似文献   

7.
为阐明联合应用阿苯达唑(ABZ)和伊维菌素(IVM)在胃肠道线虫感染鄂尔多斯细毛羊体内的药动学互作关系,以感染胃肠道线虫的鄂尔多斯细毛羊为研究对象,比较研究了单独或联合应用阿苯达唑和伊维菌素后的药物动力学特征。通过粪便虫卵检查法,选取感染胃肠道线虫的鄂尔多斯细毛羊15只,随机分成3组,每组5只。第1组口服给予阿苯达唑(15mg/kg),第2组皮下注射伊维菌素(0.2mg/kg),第3组皮下注射伊维菌素(0.2mg/kg)的同时口服阿苯达唑(15mg/kg)。于给药后不同时间,由颈静脉采集血样,分离血浆,并用高效液相色谱法测定各时间点血浆阿苯达唑、阿苯达唑亚砜、阿苯达唑砜和伊维菌素浓度,并用PK Solution 2.0药物动力学软件计算出各药动学参数。结果表明,联合用药组绵羊血浆伊维菌素峰浓度(Cmax)、药时曲线下面积(AUC)和平均滞留时间(MRT)分别为44.80ng/mL±6.12ng/mL、5 007.46ng.h/mL±1 301.42ng.h/mL和85.47h±5.03h,均显著(P<0.05)小于单独用药组的对应参数值67.62ng/mL±9.06ng/mL、7 125.08ng.h/mL±908.52ng.h/mL和113.39h±9.00h。口服阿苯达唑组绵羊血浆中仅检测到了阿苯达唑砜和阿苯达唑亚砜,而未检测到阿苯达唑母药。联合用药后,除阿苯达唑砜的达峰时间(T max)显著推迟外,阿苯达唑砜和阿苯达唑亚砜的其他各参数之间均无显著性差异。因此,联合应用IVM和ABZ可影响它们在胃肠道线虫感染鄂尔多斯细毛羊体内的药动学特征,且对伊维菌素药动学特征的影响尤为明显,在临床联合用药过程中应予以重视。  相似文献   

8.
This study hypothesized that increased feeding frequency (FF) decreases problems with glucose homeostasis seen at high feeding levels (FL) in heavy veal calves. Effects of FF and FL on hormone and metabolite concentrations were studied in 15 heavy veal calves fed once (FF1; at 12:00), twice (FF2; at 12:00 and 24:00) or four times daily (FF4; at 06:00, 12:00, 18:00 and 24:00). In period 1, all calves were fed at a low FL (FL(low); 1.5 x metabolizable energy requirements for maintenance, ME(m)). In period 2, FF2 and FF4 calves were fed at high FL (FL(high); 2.5 x ME(m)), whereas FF1 calves were still fed at FL(low). Blood was sampled every 30 min from 12:00 to 18:00 and postprandial integrated plasma hormone and metabolite concentrations (AUC(12-18 h)) were calculated. Glucose AUC(12-18 h) increased with increasing FL, but decreased with increasing FF, urea AUC(12-18 h) increased with increasing FL, whereas non-esterified fatty acid AUC(12-18 h) were unaffected by FL and FF. Insulin AUC(12-18 h) decreased with increasing FF and decreasing FL. Glucagon AUC(12-18 h) increased with increasing FL and FF. Growth hormone AUC(12-18 h) decreased, whereas insulin-like growth factor-1 and leptin AUC(12-18 h) increased with increasing FL. Mean thyroxine and 3,5,3'-triiodothyronine concentrations were modified by FF and FL. There were no FF x FL interactions, except for plasma glucose. In conclusion, postprandial hormone and metabolite responses were differentially affected by FF and (or) FL. Glucose and insulin concentrations were maximally increased at high FL and low FF. Hyperglycemia, glucosuria and excessive insulinemia were prevented by increasing FF and decreasing FL.  相似文献   

9.
The pharmacokinetics and pharmacodynamics of A77 1726 and leflunomide after intravenous (i.v.) and oral (p.o.) administration were evaluated in adult cats. Three treatments were administered: a single i.v. dose of A77 1726 (4 mg/kg), a single oral dose of leflunomide (4 mg/kg), and multiple oral doses of leflunomide (2 mg/kg). Mean pharmacokinetic parameter values after a single i.v. dose of A77 1726 were distribution (A) and elimination (B) intercepts (15.2 μg/mL and 34.5 μg/mL, respectively), distribution and elimination half-lives (1.5 and 71.8 h, respectively), area under the curve (AUC(0 → ∞); 3723 μg*h/mL), mean residence time (MRT; 93 h), clearance (Cl(obs); 1.1 mL/kg/h), and volume of distribution at steady state (Vd(ss); 97 mL/kg). Mean pharmacokinetic parameter values after a single oral dose of leflunomide were absorption and elimination rate constants (0.3 1/h and 0.01 1/h, respectively), absorption and elimination half-lives (2.3 and 59.1 h, respectively), AUC(0 → ∞) (3966 μg*h/mL), and maximum observed plasma concentration (C(max); 38 μg/mL). The bioavailability after a single oral dose of leflunomide was 100%. The mean ± SD A77 1726 concentration that inhibited 50% lymphocytes (EC(50) ) was 16 ± 13.5 μg/mL. The mean ± SD maximum A77 1726 concentration (EC(max)) was 61.0 ± 23.9 μg/mL.  相似文献   

10.
OBJECTIVE: To determine pharmacokinetics of buprenorphine in dogs after i.v. administration. ANIMALS: 6 healthy adult dogs. PROCEDURES: 6 dogs received buprenorphine at 0.015 mg/kg, i.v. Blood samples were collected at time 0 prior to drug administration and at 2, 5, 10, 15, 20, 30, 40, 60, 90, 120, 180, 240, 360, 540, 720, 1,080, and 1,440 minutes after drug administration. Serum buprenorphine concentrations were determined by use of double-antibody radioimmunoassay. Data were subjected to noncompartmental analysis with area under the time-concentration curve to infinity (AUC) and area under the first moment curve calculated to infinity by use of a log-linear trapezoidal model. Other kinetic variables included terminal rate constant (k(el)) and elimination half-life (t(1/2)), plasma clearance (Cl), volume of distribution at steady state (Vd(ss)), and mean residence time (MRT). Time to maximal concentration (T(max)) and maximal serum concentration (C(max)) were measured. RESULTS: Median (range) values for T(max) and MRT were 2 minutes (2 to 5 minutes) and 264 minutes (199 to 600 minutes), respectively. Harmonic mean and pseudo SD for t(1/2) were 270+/-130 minutes; mean +/- SD values for remaining pharmacokinetic variables were as follows: C(max), 14+/-2.6 ng/mL; AUC, 3,082+/-1,047 ng x min/mL; Vd(ss), 1.59+/-0.285 L/kg; Cl, 5.4+/-1.9 mL/min/kg; and, k(el), 0.0026+/-0.0,012. CONCLUSIONS AND CLINICAL RELEVANCE: Pharmacokinetic variables of buprenorphine reported here differed from those previously reported for dogs. Wide variations in individual t(1/2) values suggested that dosing intervals be based on assessment of pain status rather than prescribed dosing intervals.  相似文献   

11.
The aims of this study were to describe and compare the pharmacokinetics of a single dose of cephalexin (10 mg/kg) after its intravenous (i.v.) administration to five goats in three different physiological status: nonpregnant nonlactating (NPNL), pregnant (P) and nonpregnant lactating (L). Blood samples were collected at predetermined times, and plasma concentrations of cephalexin were measured by microbiological assay. Relevant pharmacokinetic parameters were calculated using noncompartmental analysis. Statistical comparison was performed applying the nonparametric anova. No significant differences were found for cephalexin pharmacokinetic parameters between the L and the NPNL group. Median V(dss) was significantly lower in pregnant goats (0.09 [0.07-0.10] L/kg) compared with NPNL goats (0.16 [0.14-0.49] L/kg). Median total Cl and V(dz) were significantly lower in pregnant goats (0.25 [0.19-0.29] L/h·kg and 0.11 [0.10-0.13] L/kg, respectively) than in lactating goats (0.40 [0.32-0.57] L/h·kg and 0.20 [0.14-0.23] L/kg, respectively). Median AUC(0-∞) was significantly higher in pregnant goats (37.79 [34.75-52.10] μg·h/mL) than in lactating goats (25.11 [17.44-31.14] μg·h/mL). Our study showed that even though some pharmacokinetic parameters of cephalexin are altered in pregnant and lactating goats, these differences are unlikely to be of clinical importance; therefore, no dose adjustment would be necessary during pregnancy and lactation.  相似文献   

12.
The pharmacokinetic properties of the developmental Amino-Acetonitrile Derivative (AAD), monepantel and its sulfone metabolite, monepantel sulfone were investigated in sheep following intravenous (i.v.) and oral administrations. The sulfone metabolite was rapidly formed and predominated over monepantel 4 h after dosing, irrespective of the route of administration. The steady-state volume of distribution, total body clearance and mean residence time of monepantel were 7.4 L/kg, 1.49 L/(kg·h) and 4.9 h, respectively and 31.2 L/kg, 0.28 L/(kg·h) and 111 h, respectively for monepantel sulfone. The overall bioavailability of monepantel was 31%, but it was demonstrated that approximately the same amount of monepantel sulfone was produced whether monepantel was given intravenously or orally ( AUC (0–∞) oral/ AUC (0–∞) i.v. of 94% for monepantel sulfone), making oral administration a very efficient route of administration for monepantel in terms of the amount of sulfone metabolite generated. Because monepantel sulfone is the main chemical entity present in sheep blood after monepantel administration and because it is also an active metabolite, its pharmacokinetic properties are of primary importance for the interpretation of future residue and efficacy studies. Overall, these pharmacokinetic data aid in the evaluation of monepantel as an oral anthelmintic in sheep.  相似文献   

13.
The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in goats given enrofloxacin alone or in combination with probenecid. Enrofloxacin was administered i.m. at a dosage of 5 mg x kg(-1) alone or in conjunction with probenecid (40 mg x kg(-1), i.v.). Blood samples were drawn from the jugular vein at predetermined time intervals after drug injection. Plasma was separated and analysed simultaneously for enrofloxacin and ciprofloxacin by reverse-phase high performance liquid chromatography. The plasma concentration-time data for both enrofloxacin and ciprofloxacin were best described by a one-compartment open pharmacokinetic model. The elimination half-life (t(1/2beta)), area under the plasma concentration-time curve (AUC), volume of distribution (V(d(area))), mean residence time (MRT) and total systemic clearance (Cl(B)) were 1.39 h, 7.82 microg x h x mL, 1.52 L x kg(-1), 2.37 h and 802.9 mL x h(-1) x kg(-1), respectively. Enrofloxacin was metabolized to ciprofloxacin in goats and the ratio between the AUCs of ciprofloxacin and enrofloxacin was 0.34. The t(1/2beta), AUC and MRT of ciprofloxacin were 1.82 h, 2.55 microg x h x mL and 3.59 h, respectively. Following combined administration of probenecid and enrofloxacin in goats, the sum of concentrations of enrofloxacin and ciprofloxacin levels > or = 0.1 microg x mL(-1) persisted in plasma up to 12 h.Co-administration of probenecid did not affect the t(1/2beta), AUC, V(d (area)) and Cl(B) of enrofloxacin, whereas the values of t(1/2beta) (3.85 h), AUC (6.29 microg x h x mL), MRT (7.34 h) and metabolite ratio (0.86) of ciprofloxacin were significantly increased. The sum of both enrofloxacin and ciprofloxacin levels was > or = 0.1 microg x mL(-1) and was maintained in plasma up to 8 h in goats after i.m. administration of enrofloxacin alone. These data indicate that a 12 h dosing regime may be appropriate for use in goats.  相似文献   

14.
The objective of this study was to analyze the relationship between pharmacokinetic parameters and body weight (W) for orbifloxacin using reported pharmacokinetic data. The parameters of interest: clearance (Cl), volume of distribution at steady state (Vss) and elimination half-life were correlated across nine mammal species, including cattle, dog, rat, rabbit, goat, camel, horse, cat and sheep as a function of W using the conventional allometric equation Y = aW(b), where Y is the pharmacokinetic parameter, W is the body weight, a is the allometric coefficient (intercept) and b is the exponent that describes the relationship between the pharmacokinetic parameter and W. Our estimates (Cl=4.40 W(1.03); Vss=1.10W(1.05)) indicated that the increase in these parameters with W approximates a linear power relationship with slopes being very close to one. Overall, the results of this study indicated that it is possible to use allometry to predict pharmacokinetic variables of orbifloxacin based on W of mammal species.  相似文献   

15.
This study was conducted to confirm an interindividual variability in pharmacokinetic parameters of clomipramine in a large population of cats and to identify potential covariables that would explain the presence of such pharmacokinetic variability after a single dose of Clomicalm. Clomipramine hydrochloride was administered orally according to a weight-dose chart from 0.32 to 0.61 mg/kg, to 76 cats and five blood samples were then taken by direct venipuncture at 1, 3, 6, 12, and 24 h. Plasma concentrations of clomipramine and desmethylclomipramine (DCMP) were measured by LC-MS/MS. The Standard Two-Stage technique was used to assess differences and detect correlations between pharmacokinetic parameter estimates and individual covariables. A large interindividual variability in all pharmacokinetic parameters (CV% 64-124) was detected. Statistically significant gender-related differences were detected in MR and Cl/F, where female cats had a higher mean MR (0.53) and faster Cl/F (0.36 L/h.kg) than males (0.36 and 0.21 L/h.kg, respectively). No correlation could be found between clomipramine AUC0-24 h or DCMP AUC0-24 h and sedation scores. Further feline studies are required to assess these findings after multiple dosing of clomipramine and DCMP to allow clinical extrapolation.  相似文献   

16.
The efficacy of the pour-on formulation of eprinomectin, at a dose rate of 0.5 mg/kg bodyweight, was assessed in sheep against three main species of gastrointestinal nematodes and against the nasal bot fly, Oestrus ovis, and some pharmacokinetic parameters were determined for 21 days after the treatment. By comparison with untreated control sheep, infected experimentally with Haemonchus contortus, Teladorsagia circumcincta and Trichostrongylus colubriformis, eprinomectin was 100 per cent effective against the two abomasal species and 99.5 per cent effective against T. colubriformis. In ewes naturally infected with the nasal bot fly, the efficacy of the drug against O. ovis was 97.7 per cent. The mean (se) systemic area under the curve (AUC) was 56.0 (26.2) ng/day/ml and the mean residence time was 5.3 (1.0) days, but there were wide variations between individual sheep.  相似文献   

17.
本试验以蒙古羊、兰州大尾羊和陶寒杂交羊(无角陶赛特作为父本、小尾寒羊为母本的杂交F1代)为研究对象,每个群体选择3只3月龄去势公羔,集中饲喂至12月龄,对其血液生化指标及肉品质进行测定与分析。结果显示:陶寒杂交羊的白蛋白(ALB)含量和高密度脂蛋白(HDL)含量低于兰州大尾羊和蒙古羊(P<0.05),但葡萄糖(GLU)含量和低密度脂蛋白(LDL)含量高于二者(P<0.05);陶寒杂交羊的熟肉率低于兰州大尾羊和蒙古羊(P<0.05),但剪切力高于二者(P<0.05);蒙古羊的大理石纹高于兰州大尾羊和陶寒杂交羊(P<0.05);兰州大尾羊的眼肌面积高于蒙古羊和陶寒杂交羊(P<0.05);相关性分析显示,兰州大尾羊的GLU含量与熟肉率呈显著正相关(P<0.05);陶寒杂交羊的GLU含量与pH45min呈显著负相关(P<0.05),LDL含量与熟肉率呈显著正相关(P<0.05)。本文研究表明,兰州大尾羊具有很大的产肉力优势,蒙古羊肉质口感好,两者肝脏合成血清白蛋白能力较强,从而有助于这2个品种形成较强生活力和耐寒耐旱的生物学特性;陶寒杂交羊的肌肉嫩度小,但对脂肪沉积能力较强。  相似文献   

18.
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   

19.
喹烯酮在鸡体内的代谢及药物动力学研究   总被引:2,自引:0,他引:2  
以HPLC-MS/MS为定量手段,研究了喹烯酮经静脉注射(2.5 mg/kg)、口服(30 mg/kg)两种给药途径在鸡体内的代谢及药物动力学特征.鸡静脉注射喹烯酮后,血浆中检测到喹烯酮原药和1-脱氧喹烯酮;口服灌注喹烯酮后,血浆中检测到喹烯酮原药和3-甲基喹噁啉-2-羧酸(MQCA).喹烯酮在鸡体内的药动学数据采用统...  相似文献   

20.
Ketoprofen (KTP) and meloxicam (MLX) are non-steroidal anti-inflamatory drugs used extensively in veterinary medicine. The pharmacokinetics of these drugs were studied in eight dogs following a single oral dose of 1 mg/kg of KTP as a racemate or 0.2 mg/kg of MLX. The concentrations of the drugs in plasma were determined by high-performance liquid chromatography (HPLC). There were differences between the disposition curves of the KTP enantiomers, confirming that the pharmacokinetics of KTP is enantioselective. (S)-(+)-KTP was the predominant enantiomer; the S:R ratio in the plasma increased from 2.58 +/- 0.38 at 15 min to 5.72 +/- 2.35 at 1 h. The area under the concentration time curve (AUC) of (S)-(+)-KTP was approximately 6 times greater than that of (R)-(-)-KTP. The mean (+/- SD) pharmacokinetic parameters for (S)-(+)-KTP were characterized as Tmax = 0.76 +/- 0.19 h, Cmax = 2.02 +/- 0.41 microg/ml, t1/2el = 1.65 +/- 0.48 h, AUC = 6.06 +/- 1.16 microg.h/ml, Vd/F = 0.39 +/- 0.07 L/kg, Cl/F = 170 +/- 39 ml/(kg.h). The mean (+/- SD) pharmacokinetic parameters of MLX were Tmax = 8.5 +/- 1.91 h, Cmax = 0.82 +/- 0.29 microg/ml, t1/2lambda(z) = 12.13 +/- 2.15 h, AUCinf = 15.41 +/- 1.24 microg.h/ml, Vd/F = 0.23 +/- 0.03 L/ kg, and Cl/F = 10 +/- 1.4 ml/(kg.h). Our results indicate significant pharmacokinetic differences between MLX and KTP after therapeutic doses.  相似文献   

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