Ehrhardt J D
Biomed Mass Spectrom. 1985 Oct;12(10):593-5. doi: 10.1002/bms.1200121005.
The quantification in plasma and urine of 2-dicyclopropylmethylamino-2-oxazoline (S-3341), a new antihypertensive drug is described using a sensitive gas chromatographic negative ion mass spectrometric method with ammonia as moderating gas. After a two-step extraction, derivatization is carried out with 3,5-bis(trifluoromethyl)benzoyl chloride and the abundance of the molecular ion (m/z 420) obtained is compared with that of the tetradeuterated standard (m/z 424). The low background due to the high mass and negative ion detection provides a detection limit of about 1 pg per injection. Oral administration of 1 or 2 mg S-3341 to patients gives a maximum concentration of 3.3 +/- 0.7 ng ml-1 and 7.6 +/- 2.0 ng ml-1 at 1.8 +/- 0.6 h and 1.4 +/- 0.7 h and an average elimination half-life of 6.7 h.
采用以氨作为缓和气体的灵敏气相色谱负离子质谱法,对新型抗高血压药物2-二环丙基甲基氨基-2-恶唑啉(S-3341)在血浆和尿液中的含量进行了测定。经过两步萃取后,用3,5-双(三氟甲基)苯甲酰氯进行衍生化反应,并将所得分子离子(m/z 420)的丰度与四氘代标准品(m/z 424)的丰度进行比较。由于高质量和负离子检测导致的低背景,使得每次进样的检测限约为1皮克。给患者口服1或2毫克S-3341后,在1.8±0.6小时和1.4±0.7小时时的最大浓度分别为3.3±0.7纳克/毫升和7.6±2.0纳克/毫升,平均消除半衰期为6.7小时。