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s2ling

新虫 (小有名气)

[交流] 咪达唑仑的 理化性质,PKa值等

各位大虾,
我现在做液相,但是不了解咪达唑仑的结构特点,PKa值,蛋白结合率等。
不知道该怎么选择它的血样提取条件。另外里面加了地西泮。
希望各位高手给予指点啊!!!!
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lanwoco

铜虫 (小有名气)

★ ★
小木虫(金币+0.5):给个红包,谢谢回帖交流
ynmyx(金币+1,VIP+0):感谢参与交流!鼓励一下! 8-21 22:01
这篇文献应该对您有用,其中记载其pKa值为6.1
Reves, J.G., P. Newfield, and L.R. Smith, Influence of serum protein, serum albumin concentrations and dose on midazolam anaesthesia induction times. Can Anaesth Soc J, 1981. 28(6): p. 556-60.
Abstract:
Individual variation occurs in time to induction of anaesthesia with intravenous drugs. Less free drug is available to cross the blood-brain barrier when the drug is highly protein bound. Since this may prolong time to sleep, we correlated the induction time, serum albumin and total protein concentrations, and doses of midazolam, which is a highly protein bound intravenous anaesthetic. There is a poor correlation (r = 0.062) between induction time and serum protein, a weak (r = 0.524) but statistically significant (p = 0.026) correlation between induction time and serum albumin, and a highly significant (p = 0.003) negative correlation (r = -0.579) between drug dose and induction time. The administration of the appropriate dose of midazolam for induction, therefore, appears to affect induction time more significantly than does the serum albumin concentration.
2楼2009-08-21 12:04:18
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dujy

铜虫 (初入文坛)


小木虫(金币+0.5):给个红包,谢谢回帖交流
Human (5mg intranasal)
bioavailability - 0.83%

Human (5mg iv and intranasal)
t1/2alpha - 0.14hr; t1/2β - 1.32hr; Tmax - 0.23hr; Cmax - 71ng/ml; Vd - 1.11l/kg; Cl - 16.1ml/min/kg

from pharmaprojects V5
3楼2009-08-21 16:21:59
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