摘要
１０名男性健康志愿者自身对照和随机交叉分别静脉滴果糖二磷酸三钠９ｇ（１，６－二磷酸果糖７．５４ｇ）、口服ＥｓａｆｏｓｆｉｎａＧｌｕｔａｍｍｉｃａ膜衣片６０片（钙盐制剂；１，６－二磷酸果糖７．５６ｇ）和果糖二磷酸三钠薄膜衣片３６片（１，６－二磷酸果糖７．５４ｇ）后，用酶法测定血中１，６－二磷酸果糖浓度，观察口服１，６－二磷酸果糖钙盐或钠盐的绝对生物利用度。结果，静滴给药后，１，６－二磷酸果糖Ｃｍａｘ为３６７．５±１７．０ｍｇ·Ｌ－１，Ｔｍａｘ为１２．４±２．０ｍｉｎ，ＡＵＣ为７１１９．９±１６２８．２ｍｇ·ｈ·Ｌ－１。口服果糖二磷酸三钠片和依沙福片后约３０ｍｉｎ在血中出现可检测到１，６－二磷酸果糖浓度（分别为３．６±４．２和６．８±５．６ｍｇ·Ｌ－１），９０～１２０ｍｉｎ已在检测限以下。Ｔｍａｘ分别为５１．０±１６．７和５５．５±１３．５ｍｉｎ达峰，Ｃｍａｘ分别为１０．１±４．１和７．１±２．８ｍｇ·Ｌ－１，果糖二磷酸钠盐片和钙盐片ＡＵＣ分别为３８７．５±１９１．９和２９８．１±１６０．２ｍｇ·Ｌ－１。两者的绝对生物利用度分别为５．８±３．２％和４．３±２．５％。实验结果表明，分别口服两种果糖二磷酸钠盐或钙盐?
Intravenous infusion of sodium fructose 1,6 diphosphate (FDP) 9 g (with FDP 7.54 g), oral administration of sodium fructose 1,6 -diphosphate 36 tablets (FDP 7.54 g) and Esafosfina Glutarlmmica 60 tablets (FDP calcium formulation; FDP 7.56 g) were given in 10 male health volunteers with randermized-cross and auto-pair method, respectively. Plasma FDP was detected by enzymatic method to observe absolute bioavailability of oral ingestion of calcium or sodium fructose 1,6- diphosphate tablets. Cmax, Tmax and AUC were 367.5±17.0 mg·L-1, 12.4±2.0 min and 7119.9±1628.2 mg·h·L-1 after iv infusion, respectively. Following ingestion of sodium fructose 1,6 diphosphate and esafosfina glutalmmica tablets, Cmax, Tmax and AUC were 10.1±4.1 and 7.1±2.8 mg·L-1; 51.0 ±16.7 and 55.5±13.5 min; 387.5±191.9 and 298.1±160.2 mg·h·L-1, respectively. Absolute bioavailability was 5.8±3.2% in sodium tablet formulation and 4.3±2.5% in calcium tablet formulation. The data showed that absolute bioavailability of oral ingestion of either FDP sodium formulation or FDP calcium formulation was extremely low, only below 10%, compared with intravenous infusion FDP.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1998年第1期30-34,共5页
The Chinese Journal of Clinical Pharmacology
