Curso de Farmácia, Universidade de Passo Fundo, Passo Fundo, BR 285 Bairro São José, CEP 99052-900, Brasil.
Programa de Pós-Graduação em Envelhecimento Humano, Universidade de Passo Fundo, Passo Fundo, BR 285 Bairro São José, CEP 99052-900, Brasil.
CNS Neurol Disord Drug Targets. 2024;23(9):1075-1084. doi: 10.2174/0118715273275957231102044934.
Two classes of medications are used to treat Alzheimer's disease (AD); donepezil, galantamine, and rivastigmine are acetylcholinesterase inhibitors, and memantine is a non-competitive antagonist of the N-methyl-D-aspartate receptor. Although these are typically taken orally, there are transdermal therapeutic systems (TTSs) commercially available for rivastigmine and donepezil. The transdermal route has been preferable for guardians/caregivers due to ease of use, reduced side effects, and improved adherence to therapy.
The study aimed to obtain knowledge of the properties of these drugs and to search for patents relating to the TTS for AD using the Espacenet platform.
The search terms were "rivastigmine AND transdermal AND skin delivery AND Alzheimer's", changing the drugs "memantine", "donepezil", and "galantamine", between January 2015 and January 2022. Title and abstract were used to choose patents.
TTSs present some limit factors in terms of absorption due to skin physiology and the size of the molecules with established limits of percutaneous penetration (molecular mass of 500 g/mol and log P of 5). We found 1, 4, 4, and 2 patents for galantamine, rivastigmine, donepezil, and memantine, respectively. Galantamine TTS seems to be more challenging due to the molecular mass of 287.35 g/mol and logP of 1.8. The permeator of absorption is necessary. Memantine, rivastigmine, and donepezil present logP of 3.28, 2.3, and 4.27 and molecular weights of 179.30, 250.34, and 415.96 g/mol, respectively.
TTSs are primarily effective for delivering small molecules. The use of absorption enhancers and irritation mitigators can be necessary to enhance the performance. The development of these technologies is essential for the convenience of patients and caregivers.
有两类药物可用于治疗阿尔茨海默病（AD）；多奈哌齐、加兰他敏和利伐斯的明是乙酰胆碱酯酶抑制剂，而美金刚是非竞争性 N-甲基-D-天冬氨酸受体拮抗剂。尽管这些药物通常口服，但利伐斯的明和多奈哌齐有商业用的透皮治疗系统（TTS）。由于使用方便、副作用减少和提高对治疗的依从性，透皮途径对监护者/照顾者来说是首选。
本研究旨在通过使用 Espacenet 平台获取有关这些药物特性的知识，并搜索与 AD 的 TTS 相关的专利。
检索词为“rivastigmine AND transdermal AND skin delivery AND Alzheimer's”，在 2015 年 1 月至 2022 年 1 月期间，将药物“memantine”、“donepezil”和“galantamine”进行替换。通过标题和摘要选择专利。
TTS 由于皮肤生理学和具有既定经皮渗透极限的分子大小（分子量 500g/mol 和 log P 5），在吸收方面存在一些限制因素。我们分别找到了 galantamine、rivastigmine、donepezil 和 memantine 的 1、4、4 和 2 项专利。由于 galantamine 的分子量为 287.35g/mol，log P 为 1.8，因此 TTS 似乎更具挑战性。吸收的透皮剂是必要的。Memantine、rivastigmine 和 donepezil 的 log P 分别为 3.28、2.3 和 4.27，分子量分别为 179.30、250.34 和 415.96g/mol。
TTS 主要适用于输送小分子。为了提高性能，可能需要使用吸收增强剂和刺激性缓解剂。这些技术的发展对于患者和护理人员的方便性至关重要。
