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Some Pharmacokinetic Parameters of R-(–)- and S-(+)-Ketoprofen: The Influence of Age and Differing Physiological Status in Dairy Cattle

机译:R-(–)-和S-(+)-酮洛芬的一些药代动力学参数:年龄和奶牛生理状况的不同影响

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The pharmacokinetic parameters of ketoprofen have previously been studied in cattle, but no studies have been performed on differing ages and metabolic situations in these animals. The aim of this work was to study the possible modifictions of the pharmacokinetics of ketoprofen enantiomers that may result from age, lactation or gestation in dairy cattle. Three groups of Holando Argentino cattle contained, respectively, 8 cows in early lactation, 8 pregnant cows and 8 newborn calves. Four animals from each group received the enantiomer R-(–)-ketoprofen, the other four animals received the S-(+) enantiomer, all by intravenous injection at a dose of 0.5 mg/kg. Significant differences between the three categories of animals were obtained in elimination half-life (t 1/2) (1.52, 0.87 and 0.31 and 1.71, 0.69 and 0.26 in newborn calves, cows in early lactation and cows in gestation, respectively), mean residence time (MRT) (0.45, 1.25, 2.20 and 0.38, 0.99, 2.47 h, in cows in gestation, cows in early lactation and newborn calves, respectively) and area under the plasma concentration-time curve (AUC) (0.87, 2.93, 3.24, and 0.67, 2.78, 5.13 (μg/h)/ml in cows in gestation, cows in early lactation and newborn calves, respectively, for the R-(–) and S-(+) enantiomer, respectively. In calves, there was a significant difference in AUC (3.24 vs 5.13 (μg h)/ml between R-(–)- and S-(+)-ketoprofen. In view of the differences between calves and adult cattle in the pharmacokinetic results for ketoprofen, the effects of age and physiological status (lactation, gestation) should be taken into account for therapeutic regimens.
机译:酮洛芬的药代动力学参数先前已在牛中进行过研究,但尚未针对这些动物的不同年龄和代谢情况进行过研究。这项工作的目的是研究奶牛年龄,泌乳或妊娠可能导致的酮洛芬对映体药代动力学的可能变化。三组阿根廷霍兰多牛分别包含8头泌乳早期的母牛,8头怀孕的母牛和8头新生的犊牛。每组的四只动物接受对映体R-(-)-酮洛芬,其他四只动物接受S-(+)对映体,全部通过静脉内注射,剂量为0.5 mg / kg。这三类动物的消除半衰期(t 1/2 )有显着差异(新生儿犊牛,哺乳初期的母牛和妊娠母牛的1.52、0.87和0.31和1.71、0.69和0.26), ),平均停留时间(MRT)(分别在妊娠母牛,早期泌乳母牛和新生犊牛中为0.45、1.25、2.20和0.38、0.99、2.47 h)和血浆浓度-时间曲线下的面积(AUC) (R-(–)和S-(+)对映异构体分别在妊娠母牛,泌乳早期母牛和新生犊牛中分别为0.87、2.93、3.24和0.67、2.78、5.13(μg/ h)/ ml,在犊牛中,R-(–)-和S-(+)-酮洛芬之间的AUC有显着差异(3.24比5.13(μgh)/ ml)。酮洛芬的药代动力学结果,年龄和生理状况(泌乳,妊娠)的影响都应考虑到治疗方案中。

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