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氯雷他定。

Loratadine.

机构信息

Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; Department of Chemistry, Faculty of Science and Technology, Al-Neelain University, Khartoum, Sudan.

出版信息

Profiles Drug Subst Excip Relat Methodol. 2022;47:55-90. doi: 10.1016/bs.podrm.2021.10.002. Epub 2021 Dec 7.

DOI:10.1016/bs.podrm.2021.10.002
PMID:35396016
Abstract

Loratadine, 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester, is an antihistamine drug with long-acting effects and has limited selectivity for peripheral H1 receptors. It is widely used for the prevention of allergic diseases such as rhinitis chronic urticaria, and asthma. This chapter discusses, by a critical extensive review of the literature, the description of loratadine in terms of its names, formulae, elemental composition, appearance, methods of preparation. The profile contains physicochemical properties of Loratadine, including pKa value, solubility and X-ray powder diffraction. In addition, it involves Fourier transform infrared spectrometry, nuclear magnetic resonance spectroscopy and mass spectroscopy for functional groups and structural confirmation of. The chapter also includes methods of analysis of the drug such as compendial, titrimetric, electrochemical, spectroscopic, chromatographic and capillary electrophoretic methods. The chapter also covers clinical applications of the drug such as its uses, doses, ADME profiles and mechanism of action.

摘要

氯雷他定,4-(8-氯-5,6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)-1-哌啶羧酸乙酯,是一种长效抗组胺药物,对周围 H1 受体的选择性有限。它被广泛用于预防过敏性疾病,如鼻炎、慢性荨麻疹和哮喘。本章通过对文献的批判性广泛回顾,讨论了氯雷他定的名称、公式、元素组成、外观、制备方法。该概要包含了氯雷他定的物理化学性质,包括 pKa 值、溶解度和 X 射线粉末衍射。此外,它还涉及傅里叶变换红外光谱、核磁共振光谱和质谱法,用于官能团和结构的确认。本章还包括药物的分析方法,如药典、滴定、电化学、光谱、色谱和毛细管电泳方法。本章还涵盖了药物的临床应用,如用途、剂量、ADME 概况和作用机制。

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