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首页> 外文期刊>Drug development and industrial pharmacy >Tissues distribution of R-(-)- and S-(+)-m-nisoldipine after single enantiomer administration in rats.
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Tissues distribution of R-(-)- and S-(+)-m-nisoldipine after single enantiomer administration in rats.

机译：在大鼠中单一对映体给药后，R-（-）-和S-（+）-m-尼索地平的组织分布。

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摘要

Rapid, sensitive, and selective high-performance liquid chromatography methods were developed and validated for determination of m-nisoldipine enantiomers in rat tissues. All of the samples were prepared based on a simple and efficient liquid-liquid extraction method. After validating that no racemation occurred by ULTRON ES-OVM (Japan), m-nisoldipine enantiomers were determined, respectively, on a reverse-phase C(18) column (5 microm, 250 x 4.6 mm). This method was applied to study tissue distribution of m-nisoldipine enantiomers in rats after a single administration of m-nisoldipine enantiomers. By the two-sample t test, there were basically no significant differences between the two enantiomers in each tissue ( p > .05), which indicates that they may have the same potency in rats. In small intestine, lung, liver, and spleen, the concentrations of R-(-)- and S-(+)-m-nisoldipine were high at 30 and 150 min than that at 90 min, which showed that m-nisoldipine enantiomers may have the phenomenon of hepatoenteral circulation. A small quantity of the prototype of R-(-)- and S-(+)-m-nisoldipine in brain showed that they can cross the blood-brain barrier to arrive at the brain tissue. The high quantity of distribution in lung and brain implied that the lipophilicity of the drug was powerful.
机译：开发了快速，灵敏和选择性的高效液相色谱方法，并验证了其在大鼠组织中测定间尼索地平对映体的能力。所有样品均基于简单有效的液-液萃取方法制备。在确认ULTRON ES-OVM（日本）未发生消旋作用后，分别在反相C（18）色谱柱（5微米，250 x 4.6毫米）上测定了m-尼索地平对映体。该方法用于研究单次施用尼索地平对映体后大鼠体内尼索地平对映体的组织分布。通过两次样本t检验，每个组织中的两种对映异构体之间基本上没有显着差异（p> .05），这表明它们在大鼠中可能具有相同的效力。在小肠，肺，肝和脾中，R-（-）-和S-（+）-m-尼索地平的浓度在90和30分钟时都比90分钟时高，这表明m-尼索地平对映体可能有肝肠循环现象。大脑中的少量R-（-）-和S-（+）-m-尼索地平原型表明它们可以穿过血脑屏障到达大脑组织。在肺和脑中的大量分布表明该药物的亲脂性很强。

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