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烟酸占替诺长效制剂的生物利用度和耐受性。传统500毫克烟酸占替诺长效片剂与新型500毫克和1克长效片剂的比较

[Bioavailability and tolerance of xanthinol nicotinate depot preparations. Comparison of a conventional 500 mg xanthinol nicotinate depot tablet with new 500 mg and 1 g depot tablets].

作者信息

von Schrader H W, Buscher G, Dierdorf D, Freytag A, Mügge H, Wolf D

出版信息

Arzneimittelforschung. 1985;35(9):1468-72.

PMID:4084347
Abstract

Bioavailability (therapeutic blood levels) and tolerance of two 500-mg xanthinol nicotinate retard tablet forms and one 1-g xanthinol nicotinate retard tablet (Complamin special) were tested in 11 (12) healthy volunteers. Despite the fact that both 500-mg retard tablets had different in vitro release rates the blood levels in man were similar. These results suggest that in vitro release rates of tablets do not predict corresponding blood levels in man. The tablet with a lower release rate also showed a distinctly lower flush rate. In respect to bioavailability and tolerance the 1-g xanthinol nicotinate retard tablet was comparable with corresponding dosages of 500-mg retard tablets. The dosage given was 2 X 500 mg or 1 g xanthinol nicotinate t.i.d. over a period of 10 days each.

摘要

在11名(12名)健康志愿者中测试了两种500毫克缓释烟醇片剂型和一种1克缓释烟醇片(Complamin special)的生物利用度(治疗血药浓度)和耐受性。尽管两种500毫克缓释片的体外释放速率不同,但人体血药浓度相似。这些结果表明,片剂的体外释放速率并不能预测人体相应的血药浓度。释放速率较低的片剂潮红发生率也明显较低。就生物利用度和耐受性而言,1克缓释烟醇片与相应剂量的500毫克缓释片相当。给药剂量为每次2×500毫克或1克烟醇,每日三次,各持续10天。

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