通过基于囊的DPI输送的formoterol,glycopyrronium和tiotropium的比较体外沉积分析
Adam Sikora1,2, Joanna Chałupka1,2, Kinga Lewandowska1
1Department of Medicinal Chemistry, Faculty of Pharmacy, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Dr. A. Jurasza 2, 85-089 Bydgoszcz, Poland.
Pharmaceutics
|September 27, 2025
概括
干粉吸入器 (DPI) 的性能因设备和吸入力而异. 这项研究比较了三个DPI,发现虽然一些非专用吸入器在体外改善了细颗粒剂量,但已批准的药物设备组合确保了经过验证的临床疗效和安全性.
科学领域:
- 肺部药物输送 肺部药物输送
- 制药技术 制药技术 制药技术
- 呼吸系统医学 呼吸系统医学
背景情况:
- 干粉吸入器 (DPI) 对阻塞性肺部疾病至关重要.
- DPI性能对吸入器设备和患者的吸入力很敏感.
研究的目的:
- 为了比较三种基于囊的DPI药物的气溶化行为.
- 在不同的囊式吸入器中评估formoterol,glycopyrronium和tiotropium.
- 在不同的吸气流条件下评估性能.
主要方法:
- 使用下一代冲击器 (NGI) 和剂量单位采样装置 (DUSA) 评估空气动力学性能.
- 细颗粒剂量 (FPD) 和空气动力学颗粒大小分布 (APSD) 在各种流速 (15-100 L/min) 和4 kPa压力下降下测量.
- 通过验证的HPLC方法量化活性成分.
主要成果:
- 对所有DPI来说,细颗粒剂量 (FPD) 随着更高的流速而增加.
- 空气化剂和Breezhaler在4kPa时显示出比Handihaler更高的FPD.
- 非专用吸入器有时会产生比预期的设备更大的可呼吸分数.
- 较高的吸气流将药物沉积转移到较小的NGI阶段,表明增强肺部输送的潜力.
结论:
- 设备特征 (抗性,囊处理,穿孔) 显著影响药物的气溶化.
- 虽然体外FPD可能会通过非专用吸入器得到改善,但临床使用必须遵循经批准的药物-设备组合,以验证安全性和有效性.
相关概念视频
01:23Inhaled Medications
749
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...
749
01:18Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules
307
Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
307
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
151
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
151
01:09In Vitro Drug Dissolution: Compendial Testing Models II
257
Various dissolution methods are utilized to assess a drug’s dissolution rate, including the flow-through cell, paddle-over-disk, cylinder, and reciprocating disk methods.The flow-through cell apparatus (USP (United States Pharmacopeia) method 4) comprises a reservoir for the dissolution medium and a pump that propels the medium through the cell containing the test sample. This method is crucial for assessing modified-release dosage forms with minimally soluble active ingredients,...
257
01:30Asthma-IV: Diagnostic and Management
3.1K
The diagnosis and management of asthma are comprehensive, encompassing clinical assessments, lung function tests, and pharmacological interventions. Here's an overview:
Clinical Assessment for Asthma:
This is the first step in diagnosing and managing asthma. It includes:
Clinical Assessment for Asthma:
This is the first step in diagnosing and managing asthma. It includes:
3.1K
01:13In Vitro Drug Dissolution: Compendial Testing Models I
230
Compendial dissolution methods are standardized procedures defined by pharmacopeias to evaluate the rate at which a drug dissolves in a specific medium. These methods ensure batch-to-batch consistency, enable quality control, and support the prediction of drug bioavailability. They are critical for both immediate and modified-release drug products.The apparatuses used for dissolution testing differ in their design and mechanical function, but all aim to simulate the physiological environment of...
230