开发可吸入喷雾干燥的纳尔布芬化粉末的开发
Waiting Tai1, Hong-Jaan Wang2, Dipesh Khanal1
1Advanced Drug Delivery Group, Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, Sydney, NSW 2006, Australia.
International journal of pharmaceutics
|July 11, 2025
概括
这项研究使用喷雾干燥开发了可吸入的纳布芬化 (NAL) 粉末. 氨酸和人血清白蛋白 (HSA) 增强了NAL粉末的吸入,改善了微粒分数,以更好地传递到肺部.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 肺部医学 肺部医学
背景情况:
- 纳尔布芬化 (NAL) 是一种有效的阿片类止痛药,但目前的输送方法有局限性.
- 低生物可用性和侵入性途径需要替代NAL.
- 肺部输送提供了高生物可用性和快速作用的潜力,具有局部肺部益处.
研究的目的:
- 通过喷雾干燥开发可吸入的纳布芬化 (NAL) 粉末.
- 为了评估白和人血清白蛋白 (HSA) 作为NAL肺部输送的分散增强剂的疗效.
- 评估开发的可吸入NAL配方的稳定性.
主要方法:
- 使用喷雾干燥方法制造无形NAL粉末,其残留溶剂含量低 (<4%).
- 分析了颗粒的大小,形态和吸入能力 (细颗粒分数,FPF).
- 研究了不同度的白和HSA对FPF的影响.
- 在受控的湿度和温度下测试了最佳配方的化学和物理稳定性.
主要成果:
- 喷雾干燥的NAL颗粒是球形的,尺寸为3-4微米,表面带有波纹.
- 仅NAL一个人就实现了25%的FPF.
- 添加HSA增加了FPF的33-37%,而白则将其提升到39-47%.
- 这种含有20%白的配方在储存一个月后表现出极好的稳定性.
结论:
- 喷雾干燥是一种生产可吸入NAL粉末的可行方法.
- 氨酸和HSA显著提高了NAL粉末的可吸入性.
- 这些稳定,可吸入的NAL配方代表了用于肺部药物输送止痛药的有希望的平台.
相关概念视频
Inhaled Medications
396
Inhaled medications are crucial for managing chronic obstructive pulmonary disease (COPD) and asthma. They are essential for effective treatment and control, ensuring optimal respiratory health and well-being. Inhaled medication delivers drugs directly to the lungs, providing a rapid onset of action and reducing systemic side effects compared to oral or injectable medications. Three primary types of inhalation devices are used to administer these medications: nebulizers, metered-dose inhalers...
396
Drug Delivery: Miscellaneous Routes
471
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...
471
Additional Routes of Drug Administration
3.1K
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...
3.1K
Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.0K
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
1.0K
Factors Influencing Drug Absorption: Pharmaceutical Parameters
195
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
195
Inhalational Anesthetics: Overview
525
Inhalation anesthetics are drugs that induce general anesthesia upon inhalation. They work by increasing the sensitivity of GABAA receptors or inhibiting NMDA receptors, leading to a decrease in central nervous system activity. The depth of anesthesia can be rapidly adjusted by changing the concentration of the inhaled gas. Some common examples of inhalational anesthetics include volatile liquids like isoflurane, desflurane, sevoflurane and gases like xenon and nitrous oxide. Isoflurane, a...
525


