Modification of Apremilast from Pills to Aerosol a Future Concept.

Paul Zarogoulidis,Chrisanthi Sardeli,Nikolaos Kougkas,Lutz Freitag,Haidong Huang,Dimitris Petridis,Aimilios Lallas,Wolfgang Hohenforst-Schmidt,Christoforos Kosmidis

doi:10.3390/ijerph182111590

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.

Highlights

The mass median aerodynamic diameter (MMAD) variable was transformed to a log10 variabl size frequency distribution and the boxplot information suggested so
The residual cup B contributed to greater mmad diameters as4).the 95%
The analysis of drug mean values indicated that apremilast produced mmad diameters mean values based on the ANOVA mean square clearly indicated, followed

Summary

Introduction

Inhaled medications have been available in the market for several years. The most common drugs administered through inhalation are the drugs used for chronic obstructive pulmonary disease (COPD) or bronchoconstriction [1,2]. Inhaled antibiotics have been used and are in currently use for cystic fibrosis and copd patients [3]. Several efforts have been made to investigate different antibiotics as aerosol administration in the laboratory [4]

Methods

Results

Discussion

Conclusion