中国兽药杂志
中國獸藥雜誌
중국수약잡지
CHINESE JOURNAL OF VETERINARY DRUG
2012年
2期
10-15
,共6页
党晓林%祁长川%刘红艳%李英伦%杨锐
黨曉林%祁長川%劉紅豔%李英倫%楊銳
당효림%기장천%류홍염%리영륜%양예
头孢噻呋%鱼腥草%药代动力学
頭孢噻呋%魚腥草%藥代動力學
두포새부%어성초%약대동역학
cefliofur%Heartleaf Houttuynia Herb%pharmacokinetic
利用药物动力学的方法考察复方盐酸头孢噻呋混悬剂是否具备缓释长效的特点,同时研究鱼腥草油对头孢噻呋药代动力学的影响。36只SPF大鼠随机平均分成三组:A组单剂量注射复方盐酸头孢噻呋混悬剂,B组单剂量注射盐酸头孢噻呋混悬剂,C组单剂量注射头孢噻呋钠粉针;三组注射剂量均为50 mg/(kg.bw)。采用反相高效液相色谱内标法测定血浆药物浓度,并以DAS2.0药动学程序和SPSS(11.0)统计软件对所得数据进行分析。A、B、C组药时数据均符合一级吸收二室模型(权重=1/cc),主要动力学参数如下:A组:T1/2Ka=(1.253±0.100)h,Tpeak=(2.000±0.000)h,Cmax=(35.203±5.732)mg/L,AUC=(229.51±18.278)mg.h/L;B组:T1/2Ka=(0.341±0.090)h,Tpeak=(1.000±0.000)h,Cmax=(43.919±1.51)mg/L,AUC=(188.488±9.611)mg.h/L;C组:T1/2Ka=(0.044±0.012)h,Tpeak=(0.167±0.000)h,Cmax=(159.091±19.971)mg/L,AUC=(128.554±6.625)mg.h/L。实验数据表明,复方盐酸头孢噻呋混悬剂肌肉注射后,其药物动力学特征表现为吸收缓慢,血药浓度平稳,消除半衰期延长,生物利用度高等特点,在临床上注射1次,连用3 d,可以维持有效血液浓度。
利用藥物動力學的方法攷察複方鹽痠頭孢噻呋混懸劑是否具備緩釋長效的特點,同時研究魚腥草油對頭孢噻呋藥代動力學的影響。36隻SPF大鼠隨機平均分成三組:A組單劑量註射複方鹽痠頭孢噻呋混懸劑,B組單劑量註射鹽痠頭孢噻呋混懸劑,C組單劑量註射頭孢噻呋鈉粉針;三組註射劑量均為50 mg/(kg.bw)。採用反相高效液相色譜內標法測定血漿藥物濃度,併以DAS2.0藥動學程序和SPSS(11.0)統計軟件對所得數據進行分析。A、B、C組藥時數據均符閤一級吸收二室模型(權重=1/cc),主要動力學參數如下:A組:T1/2Ka=(1.253±0.100)h,Tpeak=(2.000±0.000)h,Cmax=(35.203±5.732)mg/L,AUC=(229.51±18.278)mg.h/L;B組:T1/2Ka=(0.341±0.090)h,Tpeak=(1.000±0.000)h,Cmax=(43.919±1.51)mg/L,AUC=(188.488±9.611)mg.h/L;C組:T1/2Ka=(0.044±0.012)h,Tpeak=(0.167±0.000)h,Cmax=(159.091±19.971)mg/L,AUC=(128.554±6.625)mg.h/L。實驗數據錶明,複方鹽痠頭孢噻呋混懸劑肌肉註射後,其藥物動力學特徵錶現為吸收緩慢,血藥濃度平穩,消除半衰期延長,生物利用度高等特點,在臨床上註射1次,連用3 d,可以維持有效血液濃度。
이용약물동역학적방법고찰복방염산두포새부혼현제시부구비완석장효적특점,동시연구어성초유대두포새부약대동역학적영향。36지SPF대서수궤평균분성삼조:A조단제량주사복방염산두포새부혼현제,B조단제량주사염산두포새부혼현제,C조단제량주사두포새부납분침;삼조주사제량균위50 mg/(kg.bw)。채용반상고효액상색보내표법측정혈장약물농도,병이DAS2.0약동학정서화SPSS(11.0)통계연건대소득수거진행분석。A、B、C조약시수거균부합일급흡수이실모형(권중=1/cc),주요동역학삼수여하:A조:T1/2Ka=(1.253±0.100)h,Tpeak=(2.000±0.000)h,Cmax=(35.203±5.732)mg/L,AUC=(229.51±18.278)mg.h/L;B조:T1/2Ka=(0.341±0.090)h,Tpeak=(1.000±0.000)h,Cmax=(43.919±1.51)mg/L,AUC=(188.488±9.611)mg.h/L;C조:T1/2Ka=(0.044±0.012)h,Tpeak=(0.167±0.000)h,Cmax=(159.091±19.971)mg/L,AUC=(128.554±6.625)mg.h/L。실험수거표명,복방염산두포새부혼현제기육주사후,기약물동역학특정표현위흡수완만,혈약농도평은,소제반쇠기연장,생물이용도고등특점,재림상상주사1차,련용3 d,가이유지유효혈액농도。
The delayed release characteristic of compound ceftiofur hydrochloride suspension was inspected based on pharmacokinetics, and the impact of Heartleaf Houttuynia Herb on pharmacokinetics was also studied. Thirtysix SPF rat were divided into 3 groups trabant equally. Group A was given compound ceftiofur hydrochloride suspension, group B was given ceftiofur hydrochloride suspension , group C was given ceftiofur sodium. The single injection dose were all 50 rag/( kg · bw). The ceftiofur concentrations in plasma were determined by reversed - phase HPLC. The pharmacokinetic variables were calculated by DAS2.0 PK program and SPSS(11.0) program. The model of group A, B and C all fit a two - compartment model with 1 st order absorption (weight = 1/cc). The main pharmacokinetics parameters were as follows: Group A: T1/2Ka : (1. 253 ±0. 100) h, Tpeak = 2.000 ± 0. 000) h, Cmax = (35. 203 ± 5. 732) rag/L, AUC = (229.51 ± 18. 278 ) mg · h/L; GroupB: T1/2K1 = (0.341 ± 0. 090) h, Tpeak = (1. 000 ± 0. 000) h, Cmax = (43. 919± 1. 51) rag/L, AUC=(188.488±9.611)mg · h/L; Group C: T1/2xa = (0.044±0.012)h, Tpeak = (0.167 ±0. 000)h, C = ( 159.091 ±0. 19.971 ) mg/L, AUC = ( 128. 554 - 6.625 ) mg · h/L. The compound ceftiofur hydrochloride suspension was more slowly absorbed in plasma, decreased the speed of absorption, but enhanced the degree of absorption, retarded the speed of elimination, increased the time of drug action; increased the bioavailability of ceftiofur. It suggested that the dose of compound ceftiofur hydrochloride suspension was once daily by intramuscular injection for 3 to 5 d, and it can keep utility haemoconcentration.