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将阿普司特由片剂改为气雾剂:未来的构想。

Modification of Apremilast from Pills to Aerosol a Future Concept.

机构信息

Pulmonary Department, General Clinic, Euromedica Private Hospital, 546 45 Thessaloniki, Greece.

3rd Surgery Department, AHEPA University General Hospital, Aristotle University of Thessaloniki, 546 21 Thessaloniki, Greece.

出版信息

Int J Environ Res Public Health. 2021 Nov 4;18(21):11590. doi: 10.3390/ijerph182111590.

DOI:10.3390/ijerph182111590
PMID:34770103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8582726/
Abstract

BACKGROUND

Inhaled drugs have been available in the market for several years and for several diseases. Drugs for chronic obstructive pulmonary disease, cystic fibrosis, and diabetes have been used for several years. In the field of drug modification, these drugs range from tablets to aerosol.

METHODS

Milling as used to break down the tablets to powder and nebulisers are used to produce aerosol droplets. A mastersizer was used to measure the mass median aerodynamic diameter of the aerosol droplets.

RESULTS

Apremilast produced mmad diameters (2.43 μm) without any statistical difference between the different jet-nebulizers. The residual cup B contributed to greater mmad diameters as the 95% interval of mean values, based on those the ANOVA mean square clearly indicated, followed by cups C and F. The previous interval plot is much better clarified when the interaction means between drug and residual cap are plotted. The residual cups B, C and F produce mmad between (2.0-3.2).

CONCLUSION

In the current research study we demonstrated our methodology to create apremilast powder and produce apremilast aerosol droplets with different nebulisers and residual cups.

摘要

背景

吸入式药物已经在市场上存在多年,并且可用于多种疾病。用于慢性阻塞性肺疾病、囊性纤维化和糖尿病的药物已经使用了多年。在药物改性领域,这些药物的形式包括片剂和气雾剂。

方法

研磨用于将片剂粉碎成粉末,而喷雾器用于产生气溶胶液滴。使用 Mastersizer 测量气溶胶液滴的质量中值空气动力学直径。

结果

阿普米司特产生的 mmad 直径(2.43μm)在不同的射流喷雾器之间没有统计学差异。残留杯 B 导致更大的 mmad 直径,基于方差分析均方值的 95%间隔明显表明,其次是杯 C 和 F。当绘制药物和残留帽之间的交互均值图时,先前的间隔图得到了更好的澄清。残留杯 B、C 和 F 产生的 mmad 在(2.0-3.2)之间。

结论

在当前的研究中,我们展示了我们的方法来制备阿普米司特粉末,并使用不同的喷雾器和残留杯产生阿普米司特气溶胶液滴。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/efda8173444d/ijerph-18-11590-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/f3f4a0afb8fc/ijerph-18-11590-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/be8323bdd1d3/ijerph-18-11590-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/4487ff17139c/ijerph-18-11590-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/ea5857357b31/ijerph-18-11590-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/efda8173444d/ijerph-18-11590-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/f3f4a0afb8fc/ijerph-18-11590-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/be8323bdd1d3/ijerph-18-11590-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/4487ff17139c/ijerph-18-11590-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/ea5857357b31/ijerph-18-11590-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f80c/8582726/efda8173444d/ijerph-18-11590-g005.jpg

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本文引用的文献

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Apremilast monotherapy for long-term treatment of active psoriatic arthritis in DMARD-naïve patients.阿普米司特单药治疗初治的活动性银屑病关节炎患者的长期治疗。
Rheumatology (Oxford). 2022 Mar 2;61(3):1035-1043. doi: 10.1093/rheumatology/keab449.
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Long-Term Effectiveness and Drug Survival of Apremilast in Treating Psoriasis: A Real-World Experience.
阿普米司特治疗银屑病的长期疗效和药物生存:真实世界经验。
Dermatology. 2022;238(2):267-275. doi: 10.1159/000515763. Epub 2021 Jun 4.
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A Dose-Ranging Study of the Novel Inhaled Dual PDE 3 and 4 Inhibitor Ensifentrine in Patients with COPD Receiving Maintenance Tiotropium Therapy.一项新型吸入性双重 PDE3 和 4 抑制剂恩西特林在接受噻托溴铵维持治疗的 COPD 患者中的剂量范围研究。
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