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食物、抗酸剂和剂型对健康志愿者中舍吲哚药代动力学及相对生物利用度的影响。

Effects of food, antacid, and dosage form on the pharmacokinetics and relative bioavailability of sertindole in healthy volunteers.

作者信息

Wong S L, Linnen P, Mack R, Granneman G R

机构信息

Department of Pharmacokinetics and Biopharmaceutics, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.

出版信息

Biopharm Drug Dispos. 1997 Aug;18(6):533-41. doi: 10.1002/(sici)1099-081x(199708)18:6<533::aid-bdd42>3.0.co;2-j.

DOI:10.1002/(sici)1099-081x(199708)18:6<533::aid-bdd42>3.0.co;2-j
PMID:9267685
Abstract

The pharmacokinetic disposition and relative bioavailability of sertindole administered as a tablet dosage form under fasting conditions, in the presence of food, in the presence of antacid, and as solution was studied in a four-way crossover in young healthy male volunteers. Overall, tablet dosing after a meal or Maalox had no effect on t1/2 or AUC values when compared to fasting conditions, but increased the tmax and decreased the Cmax values slightly. The mean relative bioavailabilities of sertindole administered as tablets after fasting, with food, and with Maalox are 99, 104, and 98%, respectively, compared to sertindole solution. Therefore, sertindole can be administered with and without food and without regard to coadministration of antacids.

摘要

在年轻健康男性志愿者中进行了一项四交叉试验,研究了在禁食条件下、进食时、同时服用抗酸剂时以及制成溶液时,舍吲哚片剂型的药代动力学特征和相对生物利用度。总体而言,与禁食条件相比,餐后或服用氢氧化铝镁后服用片剂对t1/2或AUC值没有影响,但使tmax增加,Cmax值略有降低。与舍吲哚溶液相比,禁食后、进食时和同时服用氢氧化铝镁后服用舍吲哚片的平均相对生物利用度分别为99%、104%和98%。因此,舍吲哚可以与食物同服或不同服,且无需考虑抗酸剂的同时服用情况。

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