Concomitant food intake can increase the bioavailability of propranolol by transient inhibition of its presystemic primary conjugation
Concomitant food intake can increase the bioavailability of propranolol by transient inhibition of its presystemic primary conjugation
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同时摄入食物可以通过短暂抑制其系统前初级结合来增加普萘洛尔的生物利用度
DOI：
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发表时间：
1986
期刊：
影响因子：
--
通讯作者：
A. Melander
中科院分区：
文献类型：
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作者：
H. Liedholm;A. Melander
在11名健康女性中研究了伴随食物摄入对普萘洛尔（80 mg）的生物利用度和系统前主要结合的影响。食物增加了普萘洛尔的血药浓度和AUC（P < 0.05），降低了结合型普萘洛尔的血药浓度和AUC（P < 0.05）。结合型普萘洛尔/原型普萘洛尔的平均AUC比在空腹状态下为13：1，而在非空腹状态下仅约为6：1（P < 0.001）。至最大血清浓度的时间和t½不受食物影响。当使用缓释制剂时，食物对普萘洛尔或结合普萘洛尔的任何动力学参数均无影响。我们得出结论，伴随食物摄入可引起普萘洛尔的系统前初级结合的短暂、递送速率依赖性抑制。这是一个，但不是唯一的，机制，食物可以提高普萘洛尔的生物利用度。
The influence of concomitant food intake on the bioavailability and presystemic primary conjugation of propranolol (80 mg) was studied in 11 healthy women. Food increased the maximum serum concentration and serum AUC of propranolol (P < 0.05) and reduced those of conjugated propranolol (P < 0.05). The mean AUC ratio of conjugated/unchanged propranolol was 13:1 in the fasting state but only about 6:1 in the nonfasting state (P < 0.001). The time to maximum serum concentration and the t½ were not affected by food. There was no influence of food on any kinetic parameter of propranolol or conjugated propranolol when a slow‐release formulation was used. We conclude that concomitant food intake can evoke a short‐lasting, delivery rate—dependent inhibition of the presystemic primary conjugation of propranolol. This is one, but not the sole, mechanism by which food can enhance propranolol bioavailability.
人体内普萘洛尔的立体选择性环氧化。
影响因子：
3.4
作者：
Walle,T;Walle,UK;Wilson,MJ;Fagan,TC;Gaffney,TE
通讯作者：
Gaffney,TE