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Timolol(Ⅰ)是β-肾上腺素能受体阻滞剂,对实验动物和人体在治疗剂量(5～15mg口服)相当低时即有效,在循环血浆中对此低浓度需要有很灵敏的专一检测方法。曾将药物转化成七氟丁基衍生物用电子捕获法可检测出人血浆中timolol的灵敏度接近2mg/ml。本文报道人血浆中未标记的以及用~(13)C_3标记的timolol的测定法,由于叔丁基的羟基化是timolol在人体中的代谢途径,因此选用~(13)C_3-标记的药物(Ⅱ)作为同时服药的化合物,并用9个氘原子标记的timolol(Ⅲ)作为内标,以测定timolol的生物利用度。测定时将已知量的内标加至血浆样品中,于C_(18)反相填充层析柱
Timolol (I) is a beta-adrenergic receptor blocker that works well in experimental animals and humans at relatively low therapeutic doses (5-15 mg orally), and is sensitive to this low concentration in circulating plasma A detection method. The drug has been transformed into heptafluorobutyl derivatives electron capture method can be detected in human plasma timolol sensitivity of nearly 2mg / ml. This paper reports the unlabeled and ~ (13) C_3 labeled timolol in human plasma. Since the hydroxylation of t-butyl is the metabolic pathway of timolol in human, 13 C_3-labeled drug ( II) as concurrently administered compounds and nine deuterium labeled timolol (III) as internal standard to determine the bioavailability of timolol. Determination of the known amount of internal standard added to the plasma sample in C_ (18) reversed-phase packed column