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洛地那非

Lodenafil.

作者信息

Alshehri Yahya M, Al-Majed Abdulrahman A, Attwa Mohamed W, Bakheit Ahmed H

机构信息

College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

出版信息

Profiles Drug Subst Excip Relat Methodol. 2022;47:113-147. doi: 10.1016/bs.podrm.2021.10.004. Epub 2021 Dec 7.

Abstract

Lodenafil is a class of drugs called an inhibitor of PDE5 which also include a wide range of other erectile medicines, such as sildenafil, tadalafil and vardenafil. It is part of a new generation of PDE5 inhibitors that includes udenafil and avanafil. Lodenafil is a prodrug manufactured in the form of lodenafil carbonate, the carbonate dimer that divides in the body into two active drug lodenafil molecules. The oral bioavailability of this formulation is higher than that of the parent drug. This article discusses, by a critical comprehensive review of the literature on lodenafil in terms of its description, names, formulae, elemental composition, appearance, and therapeutic uses. The article also discusses the methods for preparation of lodenafil, its physical-chemical properties, analytical methods for its determination, pharmacological-toxicological properties, and dosing information.

摘要

洛地那非是一类被称为磷酸二酯酶5(PDE5)抑制剂的药物,这类药物还包括多种其他勃起功能障碍治疗药物,如西地那非、他达拉非和伐地那非。它是新一代PDE5抑制剂的一部分,这新一代抑制剂还包括乌地那非和阿伐那非。洛地那非是以碳酸洛地那非的形式制造的前体药物,碳酸二聚体在体内分解为两个活性药物洛地那非分子。该制剂的口服生物利用度高于母体药物。本文通过对有关洛地那非的文献进行批判性综合回顾,讨论了其描述、名称、分子式、元素组成、外观和治疗用途。文章还讨论了洛地那非的制备方法、其物理化学性质、测定分析方法、药理毒理学性质和给药信息。

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