Cefuroxime axetil pharmacokinetic profile was investigated in 12 Beagle dogs after single intravenous and oral administration of tablets or suspension at a dose of 20 mg/kg, under both fasting and fed conditions. A three-period, three-treatment crossover study (IV, PO under fasting and fed condition) was applied. Blood samples were withdrawn at predetermined times over a 12-hr period. Cefuroxime plasma concentrations were determined by HPLC. Data were analyzed by compartmental analysis. No statistically significant differences were observed between formulations and feeding conditions on PK parameters. Independently of the feeding condition, absorption of cefuroxime axetil after tablet administration was low and erratic. The drug has been quantified in plasma in 3 out of 6 and 5 out of 6 dogs in the fasted and fed groups. For this formulation, the bioavailability (F), peak plasma concentration (Cmax ), and area under the concentration-time curve (AUC) of cefuroxime axetil were significantly enhanced (p < .05) by the concomitant ingestion of food (32.97 ± 13.47-14.08 ± 7.79%, 6.30 ± 2.62-2.74 ± 0.66 µg/ml, and 15.75 ± 3.98-7.82 ± 2.76 µg.hr/ml for F, Cmax, and AUC in fed and fasted dogs, respectively), while for cefuroxime axetil suspension, feeding conditions affected only the rate of absorption, as reflected by the significantly shorter absorption half-life (T½(a) ) and time to peak concentration (Tmax ) (0.55 ± 0.27-1.15 ± 0.19 hr and 1.21 ± 0.22-1.70 ± 0.30 for T½(a) and Tmax in fed and fasted dogs, respectively). For cefuroxime axetil tablets, T > MIC (≤1 µg/ml) was <2 hr in fasted and ≈4 hr in fed animals, and for cefuroxime axetil suspension, T > MIC (≤1 µg/ml) was ≈5 hr and for T >MIC (≤4 µg/ml) was ≈2.5 hr for fasted and fed dogs, respectively. Cefuroxime axetil as a suspension formulation seems to be a better option than tablets. However, its short permanence in plasma could reduce its clinical usefulness in dogs.

中文翻译：

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食物对狗中口服头孢呋辛肟酯的药代动力学的影响。

在禁食和进食条件下，以20 mg / kg的剂量单次静脉内和口服给予片剂或混悬剂后，在12只Beagle犬中研究了头孢呋辛酯的药代动力学概况。进行了三期，三处理交叉研究（IV，PO在禁食和进食条件下）。在12小时内的预定时间抽取血样。头孢呋辛血浆浓度通过HPLC测定。通过隔室分析对数据进行分析。在PK参数上，配方和进料条件之间没有观察到统计学上的显着差异。片剂喂养后，头孢呋辛酯的吸收率低且不稳定，与喂养条件无关。在禁食和进食组中，已经在6只狗中的3只和6只狗中的5只中对血浆中的药物进行了定量。对于此公式，通过同时摄入食物，头孢呋辛酯的生物利用度（F），血浆峰值浓度（Cmax）和浓度-时间曲线下面积（AUC）显着提高（p <.05）（32.97±13.47-14.08±7.79）分别为喂食和禁食狗的F，Cmax和AUC分别为％，6.30±2.62-2.74±0.66 µg / ml和15.75±3.98-7.82±2.76 µg.hr / ml），而对于头孢呋辛酯的混悬液，喂养条件仅影响吸收速率，这表现为明显缩短的吸收半衰期（T½（a））和达到峰浓度的时间（Tmax）（T½为0.55±0.27-1.15±0.19 hr和1.21±0.22-1.70±0.30 （a）分别为喂食和禁食狗的Tmax）。对于头孢呋辛酯锭，在禁食中，禁食<MIC（≤1µg / ml）<2小时，≈4小时；对于头孢呋辛酯混悬剂，MIC（≤1µg / ml）T> 禁食和喂养狗的MIC（≤1µg / ml）约为5小时，而T> MIC（≤4µg / ml）约为2.5小时。头孢呋辛酯作为悬浮剂似乎比片剂更好。但是，其在血浆中的持久性可能会降低其在犬中的临床实用性。