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1.
本文描述了阿维菌素长效注射液与阿维菌素普通注射液(阿福丁注射液)药物动力学的比较研究。绵羊血浆经提取、纯化、真空干燥和荧光衍生化后,用荧光高效液相色谱法进行检测。用3P87药代动力学分析软件对所测得的结果进行分析,得出以下药代动力学结果;阿维菌素长效注射液和阿福丁注射液在绵羊体内均呈二室代谢模型。长效注射液以1mg/kg体重进行颈部皮下注射得到以下药动学参数;吸收半衰期t_(1 2α)=9.59h,消除半衰期t_(1 2β)=292.97h,达峰时间t_(max)=47.46h,最大血药浓度C_(max)=13.91ng/mL,曲线下面积AUC=6235.48ng/(mL·h),消除率CLB=(0.034L/(kg·h),表观分布容积V_d=13.7L/kg。将阿福丁注射液以0.2mg/kg体重进行颈部皮下注射得到以下药动学参数:吸收半衰期t_(1 2α)=9.05h,消除半衰期t_(1 2β)=144.34h,达峰时间t_(max)=12.63h,最大血药浓度C_(max)=8.52ng/mL,曲线下面积AUC=1017.35ng/(mL·h),消除率CL_B=0.22L/(kg·h),表现分布容积V_d=14.5L/kg。研究结果表明:阿维菌素长效注射液比普通注射液吸收慢、消除慢,在体内维持有效血药浓度的时间长,长效注射液维持有效血药浓度(0.5ng/mL血浆)的时间长于49d,而阿福丁注射液不足21d。  相似文献   

2.
本文描述了阿维菌素长效注射液与阿维菌素普通注射液(阿福丁注射液)药物动力学的比较研究。绵羊血浆经提取、纯化、真空干燥和荧光衍生化后,用荧光高效液相色谱法进行检测。用3P87药代动力学分析软件对所测得的结果进行分析,得出以下药代动力学结果:阿维菌素长效注射液和阿福丁注射液在绵羊体内均呈二室代谢模型。长效注射液以1mg/kg体重进行颈部皮下注射得到以下药动学参数:吸收半衰期t1/2α=9.59h,消除半衰期t1/2β=292.97h,达峰时间tmax=47.46h,最大血药浓度Cmax=13.91ng/mL,曲线下面积AUC=6235.48ng/(mL·h),消除率ClB=0.034L/(kg·h),表观分布容积Vd=13.7L/kg。将阿福丁注射液以0.2mg/kg体重进行颈部皮下注射得到以下药动学参数:吸收半衰期t1/2α=9.05h,消除半衰期t1/2β=144.34h,达峰时间tmax=12.63h,最大血药浓度Cmax=8.52ng/mL,曲线下面积AUC=1017.35ng/(mL·h),消除率ClB=0.22L/(kg·h),表观分布容积Vd=14.5L/kg。研究结果表明:阿维菌素长效注射液比普通注射液吸收慢、消除慢,在体内维持有效血药浓度的时间长,长效注射液维持有效血药浓度(0.5ng/mL血浆)的时间长于49d,而阿福丁注射液不足21d。  相似文献   

3.
为了揭示复方银红涂膜在大鼠体内的药代动力学特性,试验采用高效液相色谱法(HPLC)测定大鼠血浆中复方银红涂膜指标成分羟基红花黄色素A的血药浓度。结果表明:当复方银红涂膜剂量为100 mg/kg时,分布半衰期(t1/2ɑ)=7.874 h,消除半衰期(t1/2β)=9.013 h,达峰时间(Tmax)=14.000 h,峰血药浓度(Cmax)=0.351μg/L,表观清除率(CL/F)=243.356 L/(h·kg),初始分布容积(V1/F)=182.438 L/kg,血药浓度-时间曲线下面积(AUC)=1.978 mg/(L·h)。说明复方银红涂膜中羟基红花黄色素A在大鼠体内呈二室模型分布。  相似文献   

4.
<正>采用高效液相紫外检测法,测定了健康鸡灌服80 mg·kg-1阿德呋啉后血浆中药物浓度,药物浓度-时间数据用3P97药代动力学程序软件处理。血药浓度-时间数据符合一级吸收二室开放模型,其主要药代动力学参数分别为:血浆消除半衰期(T1/2β)(2.414±0.252)h,达峰时间(Tpeak)(1.429±0.053)h,达峰浓度(C max)(499.941±21.295)ng·m L-1,药时曲线下面积(AUC)(2624.528±124.690)ng·h·m L-1。阿德呋啉在试验鸡体内的相对生物利用度为61.94%。结果表明:阿德呋啉在健康鸡体内的药代  相似文献   

5.
本试验旨在利用非房室模型统计矩原理研究角黄素在鸡体内的药代动力学特征。选用19周龄海蓝蛋鸡为研究对象,角黄素以0.96mg/kg体重单剂量经口服灌胃给药,不同时间点分10次采集鸡静脉血,高效液相色谱法测定鸡血清中角黄素的质量浓度,用3p(97)药代动力学软件的非房室模型统计矩原理分析药代动力学数据。结果显示,鸡单剂量口服角黄素的主要药动学参数分别为:T_(max)=10 h,C_(max)=0.362μg/mL,t_(1/2)=19.263,AUC_(0-t)=9.379μg/mL·h,AUC_(0-∞)=19.251μg/mL·h,MRT_(0-t)=27.964 h,MRT_(0-∞)=118.054h。上述研究表明,角黄素经口服后在鸡体内达峰快,在组织器官中分布广泛,但滞留时间很长,消除缓慢。  相似文献   

6.
《畜牧与兽医》2014,(7):73-76
为了解硫酸头孢喹肟口服和静注给药在鸡体内的动力学特征,用高效液相色谱法测定鸡血浆中的药物质量浓度,所得硫酸头孢喹肟血药浓度数据用3p97计算机软件处理。结果显示:硫酸头孢喹肟以每公斤体重10 mg单剂量静注给药,药物浓度-时间数据经药动学程序拟合符合无吸收二室开放动力学模型,主要药动学参数分别为:中央室分布容积V(c)(1.16±0.02)L·kg-1,分布半衰期T1/2α(0.29±0.03)h,消除半衰期T1/2β(1.69±0.24)h,曲线下面积AUC(6.57±0.18)mg·L-1·h,清除率CL/f(s)(1.53±0.04)mg·L-1·h。硫酸头孢喹肟以每公斤体重20 mg口服给药的血药浓度时间数据,符合一级吸收一室开放模型,主要动力学参数:吸收半衰期T1/2 ka(0.52±0.04)h,消除半衰期T1/2 ke(0.88±0.05)h,峰时Tmax(1.07±0.02)h,最高血药浓度Cmax(3.63±0.25)μg·mL-1,曲线下面积AUC(9.84±0.68)mg·L-1·h,表观分布容积V/f(c)(3.85±0.30)L·kg-1·h-1,生物利用度F(74.9±0.06)%。结果表明:硫酸头孢喹肟静注给药能迅速从血液分布进入组织中,在体液中具有良好的渗透和分布性能,体内分布广泛,能迅速从血液中消除。口服给药吸收迅速,达峰时间短。口服给药在鸡体内生物利用度稍低,可能由于硫酸头孢喹肟的脂溶性低,其在消化道吸收率低所致。但在8 h内能保持有效血药浓度范围(0.095.74μg·mL-1),可以有效控制常见细菌感染。  相似文献   

7.
氧氟沙星(Ofloxacin)在鲤鱼体内的药代动力学   总被引:3,自引:0,他引:3  
应用 HPL C法测定了单次混饲口服氧氟沙星 (10 mg/ kg)后 ,鲤鱼体内不同时间的血浆药物浓度。利用 MCPKP药代动力学软件分析数据 ,其药代动力学特征符合一级吸收一室开放模型 ,动力学方程为 C=3.2 94 31(e- 0 .0 4 34 1 t-e- 1 .1 1 474 t )。主要药代动力学参数 :吸收半衰期 (T1 /2 ka) 0 .6 2 16 7h,半衰期 (T1 /2 k) 15 .96 4 0 5 h,最高血药浓度 (Cmax)2 .775 89mg/ L ,出现最高血药浓度时间 (TPP,血药浓度时间曲线下面积 (AUC) 72 .934mg/ L· h,血浆治疗浓度维持时间 TCP(ther) 5 .4 4 10 h。结果表明 ,氧氟沙星在鲤鱼体内吸收较迅速 ,达峰时间较短 ,血药峰浓度高 ,消除缓慢 ,保持有效杀菌浓度时间长 ,适用于鱼类细菌性疾病的预防和治疗  相似文献   

8.
为研究海南霉素钠预混剂在鸡体内的药代动力学特征和生物利用度,将16只健康AA鸡随机分成2组,每组8只,采用平行试验设计对两组鸡分别进行单剂量口服给药和静脉注射给药药动学研究,给药量均为1.5 mg/kg bw(相当于7.5 mg/kg混饲给药)。按预定时间点采集血样,血样中海南霉素的含量采用高效液相色谱-串联质谱法(HPLC-MS/MS)测定,流动相为乙腈-0.1%甲酸水溶液(90:10,V/V)。实测血药浓度-时间数据使用Winnonlin 5.2药动学分析软件拟合药动学参数。鸡口服给药的药动学参数如下:平均消除半衰期为(T_(1/2β))约为30.44 h,平均滞留时间(MRT)约为36.40 h,在血浆中的达峰时间(T_(max))约为0.5 h,达峰浓度(C_(max))约为68.87 ng/mL,平均药时曲线下面积(AUC)约为654.95 ng·h/mL,平均生物利用度(F)约为32.82%。鸡静脉注射给药的药动学参数如下:平均消除半衰期约为(T_(1/2β))为46.40 h,平均滞留时间(MRT)约为30.91 h,平均血浆清除率(CL)约为1.59 L/(kg·h),平均表观分布容积(V_d)约为116.05 L/kg。结果表明海南霉素进入鸡体后分布广泛,消除缓慢,半衰期长;口服海南霉素钠预混剂吸收迅速,但吸收不完全。  相似文献   

9.
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   

10.
选取18头平均体重(15±5)kg、健康的杜长大三元杂交去势公猪,肌肉注射15 mg/kg阿莫西林三水合物水溶液,给药后分别于0.17、0.33、0.5、0.67、1、1.5、2、4、6、8、10、12和24 h采集前腔静脉血液,高效液相色谱法检测血浆中阿莫西林的含量。阿莫西林的血药浓度-时间数据采用Win Nonlin(Version 5.2.1)软件进行拟合,计算药动学参数。结果显示:末端消除速率常数λz=(0.40±0.04)h-1,消除半衰期T1/2λz=(1.74±0.16)h,峰时Tmax=(1.53±0.40)h,峰浓度Cmax=(5.62±0.74)μg·m L-1,药时曲线下面积AUCall=(25.35±2.25)h·μg·m L-1,表观分布容积Vz=(1.64±0.38)L·kg-1,消除速率常数CLz=(0.65±0.12)L·h-1·kg-1,平均滞留时间MRT=(3.20±0.41)h。结果表明:阿莫西林三水合物在健康猪体内的主要药动学特征为肌注给药吸收迅速、达峰时间短、消除迅速。  相似文献   

11.
喹烯酮及其主要代谢物在猪体内的药动学研究   总被引:1,自引:1,他引:0  
本试验旨在研究喹烯酮及其主要代谢物在猪体内的药物代谢动力学过程。将喹烯酮按40 mg/kg的剂量对7头猪进行灌胃给药,采用HPLC-MS/MS法测定血浆中喹烯酮及其主要代谢物的浓度,药代动力学软件WinNonlin 5.2处理血浆中药物浓度-时间数据。灌胃给药后猪血浆中能检测到原药和N1-脱氧喹烯酮、脱二氧喹烯酮及3-甲基喹噁啉-2-羧酸(MQCA)3种代谢物。喹烯酮的浓度-时间数据符合一级吸收一室开放模型,其主要药代动力学参数为:T1/2Ka=(0.97±0.08)h,T1/2λz=(2.79±0.16)h,CL=(26.03±0.65)L/h·kg,Cmax=(0.26±0.01)μg/mL,Tmax=(2.23±0.06)h,AUC=(1.54±0.04)h·μg/mL;采用统计矩法处理N1-脱氧喹烯酮和脱二氧喹烯酮的浓度-时间数据,N1-脱氧喹烯酮主要药代动力学参数为:Tmax=(6.33±1.37)h,Cmax=(8.81±2.08) ng/mL,T1/2λz=(3.03±1.27)h,AUC=(0.07±0.01)h·ng/mL,MRT=(6.58±0.40)h;脱二氧喹烯酮的主要药动学参数:Tmax=(10.29±0.29)h,Cmax=(6.20±1.11)ng/mL,T1/2λz=(5.84±2.78)h,AUC=(0.15±0.01)h·ng/mL,MRT=(3.64±0.72)h。同时,在少数时间点检测到代谢物MQCA。猪口服喹烯酮后,吸收较快,消除较慢。血浆中检测到N1-脱氧喹烯酮、脱二氧喹烯酮及3-甲基喹噁啉-2-羧酸3种代谢物,且浓度较低、消除缓慢。  相似文献   

12.
为分析硫酸庆大霉素在健康和鸡大肠杆菌感染鸡体内的药物动力学特征,试验通过给健康鸡腹腔注射大肠杆菌O157,以临床症状、病理剖检和微生物检查为指标,成功建立鸡大肠杆菌感染模型。选取健康鸡和患病鸡各8只,分别以20 mg/kg体重单剂量肌内注射硫酸庆大霉素,分别于0.167、0.25、0.5、0.75、1、2、3、4、6、8和12 h时间点采血,采用管碟法测定血浆中庆大霉素的浓度。结果显示:试验所建立的标准曲线相关性好,相关系数均达0.990以上,日内、日间变异系数均小于10%。肌注给药后,硫酸庆大霉素在鸡体内吸收迅速,房室模型分析表明,健康鸡与患病鸡药时数据均符合有二室开放模型,硫酸庆大霉素在健康鸡体内峰浓度(Cmax)为(15.01±3.51)μg/mL,药时曲线下面积(AUC)为(100.79±5.14)μg/mL·h,消除半衰期(t1/2β)为(4.41±1.32)h,达峰时间(Tp)为(1.27±0.50)h。硫酸庆大霉素在患病鸡体内峰浓度(Cmax)为(12.50±2.19)μg/mL,药时曲线下面积(AUC)为(83.38±4.19)μg/mL·h,消除半衰期(t1/2β)为(4.18±1.17)h,达峰时间(Tp)为(0.97±0.05)h。结果表明:硫酸庆大霉素在患病鸡体内的峰浓度和药时曲线下面积低于健康鸡(P<0.05),因此对于已感染大肠杆菌的病鸡可以考虑适当增加给药剂量。  相似文献   

13.
Ceftiofur, a third generation cephalosporin, demonstrates in vitro efficacy against microorganisms isolated from septicemic neonatal foals. This pharmacokinetic study evaluated the intravenous and subcutaneous administration of ceftiofur sodium (5 mg/kg body weight; n = 6 per group) and subcutaneous administration of ceftiofur crystalline free acid (6.6 mg/kg body weight; n = 6) in healthy foals. Plasma ceftiofur- and desfuroylceftiofur-related metabolite concentrations were measured using high performance liquid chromatography following drug administration. Mean (±SD) noncompartmental pharmacokinetic parameters for i.v. and s.c. ceftiofur sodium were: AUC(0→∝) (86.4 ± 8.5 and 91 ± 22 h·μg/mL for i.v. and s.c., respectively), terminal elimination half-life (5.82 ± 1.00 and 5.55 ± 0.81 h for i.v. and s.c., respectively), C(max(obs)) (13 ± 1.9 μg/mL s.c.), T(max(obs)) (0.75 ± 0.4 h for s.c.). Mean (± SD) noncompartmental pharmacokinetic parameters for s.c. ceftiofur crystalline free acid were: AUC(0→∝) (139.53 ± 22.63 h·μg/mL), terminal elimination half-life (39.7 ± 14.7), C(max(obs)) (2.52 ± 0.35 μg/mL) and t(max(obs)) (11.33 ± 1.63 h). No adverse effects attributed to drug administration were observed in any foal. Ceftiofur- and desfuroylceftiofur-related metabolites reached sufficient plasma concentrations to effectively treat common bacterial pathogens isolated from septicemic foals.  相似文献   

14.
The pharmacokinetics of florfenicol (FF) was studied in plasma after a single dose (40 mg/kg) of intramuscular (i.m.) or oral gavage (p.o.) administration to crucian carp (Carassius auratus cuvieri) in freshwater at 25 °C. Ten fish per sampling point were examined after treatment. The data were fitted to two-compartment open models follow both routes of administration. The estimates of total body clearance (CL(b) ), volume of distribution (V(d) /F), and absorption half-life (T(1/2(ka)) ) were 0.067 L/h/kg and 0.145 L/h/kg, 2.21 L/kg and 1.04 L/kg, 2.75 and 1.54/h following i.m. and p.o. administration, respectively. After i.m. injection, the elimination half-life (T(1/2(β)) ) was calculated to be 38.2h, the maximum plasma concentration (C(max) ) to be 16.82 μg/mL, the time to peak plasma FF concentration (T(max) ) to be 1.50 h, and the area under the plasma concentration-time curve (AUC) to be 597.4 μg/mL·h. Following p.o. administration, the corresponding estimates were 2.17 h, 29.32 μg/mL, 1.61 h, and 276.1 μg/mL·h.  相似文献   

15.
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   

16.
氟苯尼考(florfenicol,FFC)是新型动物广谱抗菌剂,抗菌效果好,广泛应用于牛、羊、猪、水产及禽类等动物细菌性疾病的防制.本试验旨在研究FFC和氟苯尼考纳米晶(florfenicol nanocrystal,FFC-NC)在鸡体内的生物利用度.采用交叉试验法,鸡用药后,在不同时间点翅下静脉采血,利用高效液相色...  相似文献   

17.
The pharmacokinetics of terbinafine was studied in six healthy fasted cats following a single intravenous and oral administration at a dose of 10 mg/kg and 30 mg/kg, respectively, according to a two-period crossover design. Plasma terbinafine concentrations were determined using a reverse phase liquid chromatographic method. The pharmacokinetic parameters were calculated by non-compartmental analysis with WinNonlin 5.2.1 software. After intravenous administration, the terminal half-life and area under the curve from time 0 to infinity were 10.40 ± 4.56 h, 15.20 ± 3.61 h·μg/ml, respectively. After oral dosing, the mean maximum concentration was 3.22 ± 0.60 μg/ml, reached at 1.33 ± 0.41 h. The terminal half-life, area under the curve from time 0 to infinity and apparent volume of distribution were 8.01 ± 3.46 h, 13.77 ± 4.99 h·μg/ml, 25.63 ± 6.29 l/kg, respectively. The absolute bioavailability of terbinafine hydrochloride tablets after oral administration was 31.00 ± 10.85%. Although bioavailability was low, excellent penetration at the site of infection and low minimum inhibitory concentrations values provided terbinafine with good efficacy against dermatophyte infections.  相似文献   

18.
为研究"一针肥"注射液中硒元素在山羊体内的血硒水平及药动学变化规律,采用单剂量肌肉注射"一针肥"注射液0.2mL/kg(相当于硒用量6μg/kg),用原子荧光法测定血硒浓度,通过3p97药物动力学程序软件分析药时数据。结果显示,肌注"一针肥"注射液后,血硒的药时数据符合二室开放模型,主要的药代动力学参数分别为:t1/2Ka(0.148 4±0.051 0)h,t1/2α(6.832 4±0.397 7)h,t1/2β(362.324 3±17.789 5)h,Kel(0.004 3±0.000 3)h,AUC(22 414.233 5±2 512.959 8)(μg/L).h。结果表明,肌注"一针肥"注射液后硒在山羊体内吸收迅速,消除缓慢。  相似文献   

19.
Pharmacokinetics of mequindox and one of its major metabolites (M) was determined in chickens after intravenous (i.v.), intramuscular (i.m.) and oral administration of mequindox at a single dose of 10 (i.v. and i.m.) or 20 mg/kg b.w. (oral). Plasma concentration profiles were analyzed by a non-compartmental pharmacokinetic method. Following i.v., i.m. and oral administration, the areas under the plasma concentration-time curve (AUC(0-∞)) were 0.71±0.15, 0.67±0.21, 0.25±0.10 μg h/mL (mequindox) and 37.24±7.98, 36.40±9.16, 86.39±16.01 μg h/mL (M), respectively. The terminal elimination half-lives (t(1/2λz)) were determined to be 0.15±0.06, 0.21±0.09, 0.49±0.23 h (mequindox) and 5.36±0.86, 5.39±0.52, 5.22±0.35 h (M), respectively. The bioavailabilities (F) of mequindox were 89.4% and 16.6% for i.m. and oral administration. Steady-state distribution volume (V(ss)) of 1.20±0.34 L/kg and total body clearance (Cl(B)) of 13.57±2.16 L/kg h were determined for mequindox after i.v. dosing. After single i.m. and oral administration, peak plasma concentrations (C(max)) of 3.04±1.32, 0.36±0.13 μg/mL (mequindox) and 3.81±0.92, 5.99±1.16 μg/mL (M) were observed at t(max) of 0.08±0.02, 0.32±0.12 h (mequindox) and 0.66±0.19, 6.67±1.03 h (M), respectively. The results showed that mequindox was rapidly absorbed after i.m. or p.o. administration and most of mequindox was transformed to metabolites in chickens, with much higher C(max)s and AUCs of metabolite (M) than those of mequindox in plasma.  相似文献   

20.
In a four-period, cross-over study, the fluoroquinolone antibacterial drug marbofloxacin (MB) was administered to calves, alone and in combination with the nonsteroidal anti-inflammatory drug tolfenamic acid (TA). Both drugs were administered intramuscularly (IM) at doses of 2 mg/kg. A tissue cage model of inflammation, based on the actions of the mild irritant carrageenan, was used to evaluate the pharmacokinetics (PK) of MB and MB in combination with TA. MB mean values of area under concentration-time curve (AUC) were 15.1 μg·h/mL for serum, 12.1 μg·h/mL for inflamed tissue cage fluid (exudate) and 9.6 μg·h/mL for noninflamed tissue cage fluid (transudate). Values of C(max) were 1.84, 0.35 and 0.31 μg/mL, respectively, for serum, exudate and transudate. Mean residence time (MRT) of 23.6 h (exudate) and 22.6 h (transudate) also differed significantly from serum MRT (8.6 h). Co-administration of TA did not affect the PK profile of MB. The pharmacodynamics of MB was investigated using a bovine strain of Mannheimia haemolytica. Time-kill curves were established ex vivo on serum, exudate and transudate samples. Modelling the ex vivo serum time-kill data to the sigmoid E(max) equation provided AUC(24 h) /MIC values required for bacteriostatic (18.3 h) and bactericidal actions (92 h) of MB and for virtual eradication of the organism was 139 h. Corresponding values for MB + TA were 20.1, 69 and 106 h. These data were used to predict once daily dosage schedules for a bactericidal action, assuming a MIC(90) value of 0.24 μg/mL, a dose of 2.6 mg/kg for MB and 2.19 mg/kg for MB + TA were determined, which are similar to the currently recommended dose of 2.0 mg/kg.  相似文献   

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