在健康志愿者中研究了每周一次的donepezil透皮系统与口服donepezil的生物等价性:一个简单的语言摘要
1Zevra Therapeutics, Inc., Celebration, FL, USA.
Neurodegenerative disease management
|September 6, 2023
概括
一个新的透皮输送系统 (TDS) 贴片每周输送多尼佩西尔,匹配每日药片水平. 这种阿尔茨海默氏症治疗方法显示了更少的胃肠道和神经系统副作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 神经学 神经学
- 药物输送系统 药物输送系统
背景情况:
- 阿尔茨海默病是一种与低乙胆水平相关的渐进性痴呆症.
- 多尼佩西尔是一种乙胆增强剂,通常被处方为口服药片.
- 口服多内佩西尔可能会引起显著的胃肠道副作用,导致治疗不坚持.
研究的目的:
- 为了比较每周一次的多尼透皮输送系统 (TDS) 和每天一次的口服多尼的药理学.
- 在健康志愿者中评估和比较多尼佩西尔TDS与口服多尼佩西尔的副作用概况.
主要方法:
- 对多尼佩西尔吸收和循环的药理动力学分析.
- 在多尼佩西尔TDS和口服多尼佩西尔配方之间的不良事件的比较.
- 在健康志愿者身上进行的研究,以评估药物输送和耐受性.
主要成果:
- 每周一次的多尼佩西尔TDS实现了与每天一次口服多尼佩西尔可比的全身药物水平.
- 与口服多尼佩西尔相比,多尼佩西尔TDS的胃肠道副作用 (腹,恶心,吐) 的发生率较低.
- 较少的神经系统副作用 (头,昏昏欲睡) 被观察到与donepezil TDS.
结论:
- 多尼西尔TDS为阿尔茨海默病痴呆症的口服多尼西尔提供了一个可行的替代方案.
- 透皮途径可以通过减少常见的副作用来提高耐受性.
- 这种输送方法支持患者在donepezil治疗中保持一致的坚持.
相关概念视频
Bioequivalence: Overview
1.1K
Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
1.1K
Factors Influencing Drug Absorption: Presystemic Elimination
260
The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
260
Direct-Acting Cholinergic Agonists: Pharmacokinetics
1.3K
Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
1.3K
Cholinergic Antagonists: Pharmacokinetics
515
Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations, while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
515
Dosage Regimen: Fixed Dose
1.9K
Fixed-dose regimens are a common approach to administer drugs to achieve and maintain desired levels of the drug in the body. In this dosing strategy, a specific amount of medication is given at regular intervals, often multiple times a day, to ensure a consistent drug concentration in the bloodstream.
Fixed-dose regimens can be used for various routes of administration, including intravenous (IV) injections and oral medications. For IV administration, a predetermined amount of the drug is...
Fixed-dose regimens can be used for various routes of administration, including intravenous (IV) injections and oral medications. For IV administration, a predetermined amount of the drug is...
1.9K
Indirect-Acting Cholinergic Agonists: Pharmacokinetics
1.0K
Indirect-acting cholinergic agonists, or anticholinesterases, enhance the body's cholinergic activity by inhibiting acetylcholine's breakdown. They are categorized as reversible or irreversible agents based on their mechanism of action. They are further classified into short-acting, intermediate-acting, and long-acting agents based on their duration of action.
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they...
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they...
1.0K


