背景:两类药物用于治疗阿尔茨海默病(AD);多奈哌齐,加兰他敏,卡巴拉汀是乙酰胆碱酯酶抑制剂,美金刚是N-甲基-D-天冬氨酸受体的非竞争性拮抗剂。虽然这些通常是口服的,有利伐斯的明和多奈哌齐的市售透皮治疗系统(TTS)。由于易于使用,因此对于监护人/护理人员来说,透皮途径是优选的。减少副作用,并改善对治疗的依从性。
目的:本研究旨在利用Espacenet平台获取这些药物特性的知识,并搜索与AD的TTS相关的专利。
方法:搜索词是“卡巴拉汀和透皮和皮肤给药和阿尔茨海默氏症”,改变药物\“美金刚\”,\"多奈哌齐\",和“加兰他敏”,2015年1月至2022年1月。标题和摘要用于选择专利。
结果:TTS在吸收方面存在一些限制因素,这是由于皮肤生理学和分子的大小而确定的经皮渗透极限(分子量为500g/mol,logP为5)。我们发现了加兰他敏的1、4、4和2项专利,利伐斯的明,多奈哌齐,还有美金刚,分别。由于分子量为287.35g/mol和logP为1.8,加兰他敏TTS似乎更具挑战性。吸收的渗透器是必要的。美金刚,利伐斯的明,多奈哌齐的logP为3.28、2.3和4.27,分子量为179.30、250.34和415.96g/mol,分别。
结论:TTS主要用于递送小分子。吸收增强剂和刺激缓解剂的使用对于增强性能是必要的。这些技术的发展对于患者和护理人员的便利至关重要。
BACKGROUND: 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.
OBJECTIVE: 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.
METHODS: 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.
RESULTS: 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.
CONCLUSIONS: 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.