不同水温下氟甲砜霉素在斑点叉尾鮰体内的药代动力学研究
PHARMACOKINETI CS OF FLORFENICOL IN CHANNEL CATFISH (ICTALURUS PUNCTATUS) AT D IFFERENTWATER TEM PERATURES
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摘要: 研究不同水温(18℃和28℃)条件下,单剂量(10mg/kgb·w)强饲氟甲砜霉素,在斑点叉尾鮰(Ictaluruspunc-tatus)体内药代动力学特征.采用高效液相色谱紫外检测法可以同时检测血浆中氟甲砜霉素及其代谢物氟甲砜霉素的浓度.用3p97药代动力学软件处理药时数据.结果表明:在不同水温条件下氟甲砜霉素在斑点叉尾鮰体内的药时数据均符合一室开放式模型.药时规律符合理论方程C血浆=71921(e-0.036t-e-0.18t)和C血浆=91061(e-0.081t-e-0.301t).18℃和28℃的条件下,主要药代动力学参数:吸收半衰期T1/2ka分别为31845h和21301h,消除半衰期T1/2ke分别为191118h和81519h,达峰时间Tpeak分别为111136h和51953h,最大血药浓度Cmax分别为41074μg/mL和41226μg/mL,曲线下面积AUC分别为1741547(μg/mL)/h和811279(μg/mL)/h,平均驻留时间MRT分别为271581h和121290h,相对表观分布容积V/F(c)分别为11580L/kg和115121L/kg.采用氟甲砜霉素防治斑点叉尾鮰细菌性疾病,建议在18℃左右口服10mg/kg体重剂量的氟甲砜霉素,2d给药1次;在28℃左右口服10mg/kg体重剂量的氟甲砜霉素,1d给药1次.试验过程中在斑点叉尾鮰血浆样品中未检测到氟甲砜霉素的主要代谢物氟甲砜霉素胺.Abstract: The pharmacokinetics of florfenicol (FF) was investigated with a single doe of.0mg/kg body weight after oral gavage administration in channel catfish (Ictalurus punctatus) at the water temperature of 18℃ and 28℃.Florfenicol and its metabolite FlorfenicolAmine (FFA) concentrations in fish p lasma were simultaneously determined using high-perform-ance liquid chromatography (HPLC) with UV detection.Pharmacokinetic parameters were calculated by using the 3p97 Practical Pharmacokinetic Program software.The results showed that the kinetics of the drug was found to be temperature dependent.Plasma concentration-time data of florfenicol were best fitted using a one-compartmental open model at both 18℃ and 28℃ water temperature.The kinetic equation were Cp lasma=7.921 (e -0.036t-e-0.180t) and Cp lasma=9.061 (e-0.08.t-e-0.30.1t) at 18℃ and 28℃ respectively.The major pharmacokinetic parameters atwater temperature of 18℃ and 28℃ were as follows: the absorp tion half-time (T1/2kα) 3.845h and 2.301h, respectively; the elimination half-time (T1/2ke) 19.118h and 8.519h, respectively; The time point of the maximum p lasma concentration (Tp) 1.1136h and 5.953h respectively, Peak p lasma concentration (Cmax) were 4.074μg/mL and 4.226μg/mL, respectively;Area under curve (AUC) 174.547μg/mL·h and 8.1279μg/mL·h, respectively; Mean residence time (MRT) were 27.58.h and 12.290h, respectively.Relatively apparent distributed volume V/F (c) were app roached that were 1.512L/kg and 1.580L/kg respectively.Florfenicol administration for p reventing and controlling bacterial disease of channel catfish which is recommended to be once two days at 18℃ or once a day at 28℃with a doe of 10mg/kg bodyweight by oral administration.The main metablite FFA of FF was-not detected in channel catfish p lasma samp le.
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