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新型β-肾上腺素能受体阻滞剂倍他洛尔(SL 75212)多次口服给药后在人体的药代动力学

Pharmacokinetics of the new beta-adrenoceptor blocking agent betaxolol (SL 75212) in man after repeated oral administration.

作者信息

Bianchetti G, Blatrix C, Gomeni R, Kilborn J R, Larribaud J, Lücker P W, Thebault J J, Trocherie S, Morselli P L

出版信息

Arzneimittelforschung. 1980;30(11):1912-6.

PMID:6109538
Abstract

(+/-)-1-(Isopropylamino)-3-[p-(2-cyclopropyl-methoxyethyl)-phenoxy]-2-propanol HCl (betaxolol, SL 75212) was given to groups of healthy volunteers, 10 mg daily for 7 days followed by 20 mg daily 7 days in one group, and increasing daily doses up to 60 mg/day for a total of 15 days in the other group. The pharmacokinetics were studied during dosing and in the washout period. The pharmacokinetic characteristics were unchanged after repeated doses, T/2 16-22 h, Vd 7.7-8.8 l/kg; clearance 0.28-0.33 l/h/kg.

摘要

将(±)-1-(异丙氨基)-3-[对-(2-环丙基甲氧基乙基)-苯氧基]-2-丙醇盐酸盐(倍他洛尔,SL 75212)给予健康志愿者组,一组每天服用10mg,共7天,随后7天每天服用20mg;另一组每天剂量递增至60mg/天,共15天。在给药期间和洗脱期研究了其药代动力学。重复给药后药代动力学特征未改变,半衰期为16 - 22小时,分布容积为7.7 - 8.8升/千克;清除率为0.28 - 0.33升/小时/千克。

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