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RADIOISOTOPE LABELLED BIOLOGICAL COMPOSITIONS, AND THEIR USE IN ACCELERATOR MASS SPECTROMETRY

机译:放射性同位素标记的生物成分及其在加速器质谱中的应用

摘要

The invention provides a biological composition comprising a biological compound of formula I: (I) B-A* alone or together with B wherein B-A* is a biological compound or a derivative thereof formed as the product of reaction of the biological compound to introduce A*, A* is a radioisotopic moiety having MW in the range 10 to 500 comprising an AMS radioisotope * wherein the composition is characterised by a value for the percent incorporation of radioisotope which is a measure of maximum specific activity, wherein 100% incorporation is defined as the incorporation of one radioisotope per molecule, and wherein the percent incorporation is in the range from in excess of zero to 100%, wherein the quantity of organic radioisotope A* labelled molecules in a population of one thousand molecules is so low as to not alter the biological activity of the drag; a process for the preparation thereof; a method for AMS detection of one or more biological compositions as defined in any of claims 1 to 17 comprising B of same or different origin, comprising providing one or more biological compositions and optionally one or more control compositions comprising biological compound B, for dosing to at least one subject, obtaining metabolic samples from the subject(s) having been dosed with said biological(s) as hereinbefore defined and conducting AMS detection and obtaining AMS results for the or each biological; and the use of a biological composition or compound of formula I in AMS detection providing in vitro or in vivo metabolism characteristics thereof.
机译:本发明提供了一种生物组合物,其包含式I的生物化合物:(I)BA *单独或与B一起,其中BA *是作为生物化合物引入A *的反应产物而形成的生物化合物或其衍生物。 A *是具有10至500 MW的MW的放射性同位素部分,其包含AMS放射性同位素*,其中该组合物的特征在于放射性同位素掺入百分比的值,该值是最大比活的度量,其中100%掺入定义为每个分子掺入一个放射性同位素,并且其中掺入百分比在从零到100%的范围内,其中一千个分子群体中有机放射性同位素A *标记的分子的数量如此之低,以至于不会改变药物的生物活性;其制备方法; 18.一种用于AMS检测一种或多种如权利要求1至17中任一项所定义的包含相同或不同来源的B的生物组合物的方法,该方法包括提供一种或多种生物组合物以及任选地一种或多种包含生物化合物B的对照组合物,以用于至少一个受试者,从已被如前定义的所述生物剂量给药的受试者中获取代谢样品,并进行AMS检测并获得所述或每个生物的AMS结果;以及式I的生物组合物或化合物在AMS检测中的用途,可提供其体外或体内代谢特征。

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