用于吸入治疗的含布地奈德和阿福莫特罗的载体型干粉的配制和评估。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-23 DOI:10.1080/10837450.2024.2413145
Dong-Won Oh, Ji Hoon Choi, Gweon Hee Yu, Bo Kyung Kim, Sang Min Cho, Youn Woong Choi, Jin-Hyuk Jeong, Ji-Hyun Kang, Dong-Wook Kim, Chun-Woong Park
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引用次数: 0

摘要

哮喘和慢性阻塞性肺病(COPD)是全球主要的健康问题,吸入疗法是主要的治疗方法。然而,干粉吸入器(DPI)经常面临药物颗粒聚集的问题,这会降低药物输送效率。本研究旨在研究颗粒聚集问题,并优化内聚力-粘附力平衡,以提高吸入效率。研究采用了原子力显微镜和拉曼成像等先进技术来分析微粒的相互作用和聚集行为,重点关注乳糖比例、微粒形状以及药物与药物之间的相互作用。在哮喘模型中评估了含有布地奈德(BUD)和阿福莫特罗(AFT)的优化制剂的疗效。具体而言,与阳性对照组相比,sRAW、中性粒细胞计数和潮气量值均有明显改善,P 值均低于 0.01。AFT 的疗效相当于福莫特罗的一半剂量。此外,药代动力学(PK)研究表明,两种药物在体内的表现相似,证实了 AFT 的治疗优势。(AUC0-t和Cmax的p值分别为0.646和0.153)。主要研究结果表明,制剂优化可显著减少颗粒聚集,提高DPI的给药效率(AFT和BUD的FPF分别为39.4%和50.6%),这表明该制剂有望提高哮喘和慢性阻塞性肺病患者的临床疗效。这项研究为可吸入疗法的制剂开发提供了宝贵的见解。
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Formulation and evaluation of carrier-based dry powders containing budesonide and arformoterol for inhalation therapy.

Asthma and Chronic Obstructive Pulmonary Disease (COPD) are major global health concerns, with inhalation therapy being a primary treatment method. Dry powder inhalers (DPIs) often face challenges related to particle aggregation, which can diminish drug delivery efficiency. This study investigates particle aggregation and aims to optimize the cohesion-adhesion balance to improve inhalation efficiency. Advanced techniques like atomic force microscopy and Raman imaging were used to analyze particle interactions, focusing on lactose ratios, particle morphology, and drug-drug interactions. The therapeutic efficacy of optimized formulations containing budesonide (BUD) and Arformoterol (AFT) was assessed using an asthma model, showing significant improvements in sRAW, neutrophil count, and tidal volume compared to the positive control, with p-values below 0.01. AFT exhibited comparable efficacy to Formoterol at half the dose. Additionally, pharmacokinetic studies demonstrated similar in vivo behavior between the drugs, confirming the therapeutic advantage of AFT, with p-values for AUC0-t and Cmax of .646 and .153, respectively. The fine particle fractions for AFT and BUD were 39.4% and 50.6%, respectively, indicating improved drug delivery efficiency and potential for better clinical outcomes in asthma and COPD patients.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
期刊介绍: Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.
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