Beattie Kevin, Phadke Geeta, Novakovic Jasmina
Apotex Inc., Toronto, Ontario, Canada.
Profiles Drug Subst Excip Relat Methodol. 2013;38:113-57. doi: 10.1016/B978-0-12-407691-4.00004-6.
Carvedilol ((2RS)-1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]propan-2-ol), a β1-, β2-, and α1-adrenoreceptor blocker drug with antioxidant and antiproliferative effects, is indicated for treatment of hypertension, stable angina pectoris, and congestive heart failure. A profile of this drug substance is provided in this chapter and includes physical characteristics of Carvedilol (e.g., UV-vis, IR, NMR, and mass spectra). Details regarding the stability of Carvedilol in the solid state and solution phase are presented and methods of analysis (compendial and literature) are summarized. Furthermore, an account of the pharmacokinetics (ADME) and synthesis of Carvedilol are presented.
卡维地洛((2RS)-1-(9H-咔唑-4-基氧基)-3-[[2-(2-甲氧基苯氧基)乙基]氨基]丙-2-醇),一种具有抗氧化和抗增殖作用的β1、β2和α1肾上腺素能受体阻滞剂药物,适用于治疗高血压、稳定型心绞痛和充血性心力衰竭。本章提供了该药物的概况,包括卡维地洛的物理特性(如紫外可见光谱、红外光谱、核磁共振光谱和质谱)。介绍了卡维地洛在固态和溶液相中的稳定性细节,并总结了分析方法(药典方法和文献方法)。此外,还介绍了卡维地洛的药代动力学(吸收、分布、代谢和排泄)及合成情况。