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老年人中苯恶洛芬的药代动力学。

The pharmacokinetics of benoxaprofen in elderly subjects.

作者信息

Hamdy R C, Murnane B, Perera N, Woodcock K, Koch I M

出版信息

Eur J Rheumatol Inflamm. 1982;5(2):69-75.

PMID:7084284
Abstract

Benoxaprofen plasma profiles were obtained in two groups of elderly female patients. A single dose of benoxaprofen, either 600 mg or 300 mg, was given and blood levels were measured daily to 120 hours. Mean peak plasma levels were reached at five hours following the 600-mg dose and at seven hours after the 300-mg dose. Elimination half-lives calculated from levels during 36-120 hours resulted in means of 111 hours and 86.4 hours for the 600-mg and 300-mg doses respectively. (Normal subjects, 30 to 35 hours.) Because of these extended half-lives, a further study was conducted following a single 600-mg dose to four more patients. Blood vessels were measured up to 504 hours (21 days). This resulted in a means half-life of 147.9 hours calculated from levels during 168-504 hours. Although serum creatinine levels ere not generally above the normal for this age group, calculated creatinine clearances were considerably reduced. It is concluded that the high plasma benoxaprofen levels achieved, combined with the slow clearance rates and long half-lives, indicate that it may be possible to work is needed to determine whether this prolonged half-life is matched by an equally prolonged therapeutic effect.

摘要

在两组老年女性患者中获取了贝诺洛芬的血浆浓度曲线。给予600毫克或300毫克的单剂量贝诺洛芬,并每日测量血药浓度直至120小时。600毫克剂量后5小时达到平均血浆峰浓度,300毫克剂量后7小时达到平均血浆峰浓度。根据36 - 120小时期间的血药浓度计算出的消除半衰期,600毫克剂量组的平均值为111小时,300毫克剂量组为86.4小时。(正常受试者为30至35小时。)由于这些半衰期延长,对另外4名患者给予600毫克单剂量后进行了进一步研究。测量血药浓度直至504小时(21天)。根据168 - 504小时期间的血药浓度计算出的平均半衰期为147.9小时。尽管血清肌酐水平一般未高于该年龄组的正常水平,但计算出的肌酐清除率显著降低。结论是,所达到的高血浆贝诺洛芬水平,加上清除率缓慢和半衰期长,表明可能需要开展工作来确定这种延长的半衰期是否与同样延长的治疗效果相匹配。

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