鼻内药物的药理动力学,仍然是一个错过的机会吗?
Maria Luisa Sardu1, Italo Poggesi2
1UCB Pharma SPA, Milano, Italy.
概括
鼻内药物输送是复杂的,并未完全理解,特别是在鼻子到大脑的途径. 需要进一步的研究来开发鼻内 (IN) 药物吸收和处置的预测模型.
科学领域:
- 药理动力学和药物输送方法
- 神经科学和药物发现
背景情况:
- 内鼻 (IN) 给药对于局部,全身和直接鼻至脑药物输送至关重要.
- IN吸收和鼻至大脑的分布是复杂的,受化合物特性和配方的影响.
- 目前对IN药物吸收决定因素的理解落后于口服,阻碍了药物开发.
研究的目的:
- 在IN剂量后审查药理动力学 (PK) 过程的生理学.
- 为研究鼻血通道和鼻脑通道的化合物提供示例.
- 确定研究缺口,以促进IN药物候选药物的开发.
主要方法:
- 关于鼻入药物管理的临床前和临床研究的文献综述.
- 对影响鼻内药物吸收和排放的因素的分析.
- 讨论现有知识,并确定需要改进的领域.
主要成果:
- 鼻内药物吸收和鼻至大脑输送机制是复杂的,并未完全阐明.
- 与口服途径相比,在预测IN化合物的PK特性方面存在显著的知识差距.
- 许多化合物已被探索用于IN输送,突出其治疗潜力.
结论:
- 鼻内注射仍然是一个开放的研究领域,用于开发可预测的PK模型.
- 进一步了解IN吸收决定因素对于推进药物开发至关重要.
- 需要翻译工具来从非临床IN研究中预测临床PK.
相关概念视频
Additional Routes of Drug Administration
2.7K
Choosing the appropriate route of drug administration is significantly influenced by two key factors: the therapeutic objectives and the inherent properties of the drug being used.
Administering drugs via inhalation allows for the direct delivery of gaseous, volatile substances or droplets to different parts of the respiratory tract. One of the advantages of the inhalation route is the rapid absorption of drugs into the circulatory system, which is possible because of the large surface area of...
Administering drugs via inhalation allows for the direct delivery of gaseous, volatile substances or droplets to different parts of the respiratory tract. One of the advantages of the inhalation route is the rapid absorption of drugs into the circulatory system, which is possible because of the large surface area of...
2.7K
Drug Delivery: Miscellaneous Routes
338
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
338
Non-Oral Extravascular Drug Absorption Routes
214
Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
214
Biopharmaceutics and Pharmacokinetics: Overview
2.0K
Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the...
2.0K
Drug Distribution as One-Compartment Model and Elimination by Nonlinear Pharmacokinetics: Overview
63
Drug administration can occur through various routes, each of which may result in a different process of elimination. This process is often mixed with nonlinear and linear processes. It's important to understand that a single drug can be metabolized into different metabolites through parallel processes.
For instance, consider the metabolism of sodium salicylate. This compound is metabolized into two distinct substances: a glucuronide and a glycine conjugate. The rate of conjugation depends...
For instance, consider the metabolism of sodium salicylate. This compound is metabolized into two distinct substances: a glucuronide and a glycine conjugate. The rate of conjugation depends...
63
Indirect-Acting Cholinergic Agonists: Pharmacokinetics
965
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...
965


