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Pharmaceutics
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Advances in the Preparation and Technology of Pharmaceutical Solid Dosage...
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Advances in the Preparation and Technology of Pharmaceutical Solid Dosage Forms

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: 10 March 2025 | Viewed by 1968

Special Issue Editors

Dr. Inês C. B. Martins

E-Mail Website
Guest Editor
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen Universitetsparken 2, 2100 Copenhagen, Denmark
Interests: crystalline and amorphous pharmaceutical solid forms; poly(a)morphs; ball milling; solid-state characterization; crystal structure determination; X-ray diffraction; total scattering; molecular dynamics simulations
Special Issues, Collections and Topics in MDPI journals
Dr. Daniele Musumeci

E-Mail Website
Guest Editor
Department of Chemistry, School of Arts and Sciences, York College, New York, NY, USA
Interests: solid-state pharmaceutical chemistry and materials science; crystallization processes; polymorphs; co-crystals; amorphous solids; solid-state characterization

Special Issue Information

Dear Colleagues,

One of the most pressing issues in drug development is to find strategies with which to improve the aqueous solubility and thereby the oral bioavailability of poorly water-soluble drugs. Several strategies, including the preparation of both crystalline and amorphous multicomponent solid forms (i.e., the combination of a drug with a second biologically acceptable molecule), have been considered as promising routes with which to overcome the poor water solubility problem of drugs. For instance, the combination of amorphous drugs with polymers (amorphous solid dispersions—ASDs) and small molecules (co-amorphous systems) has received considerable attention, not only for offering the possibility to improve drug solubility (therefore decreasing the drug dosage) but also for allowing the design of more stable drugs in an amorphous state.

Despite all of these promising strategies to improve the aqueous solubility of poorly water-soluble drugs, only a few multicomponent solid forms (e.g., co-crystals, co-amorphous, and ASDs) have been developed into marketed products, mainly because of inadequate physical stability during storage and challenges during the scale-up of manufacturing processes.

This Special Issue aims to share the latest advances in the preparation and technological development of solid pharmaceutical dosage forms. To this end, we invite the submission of papers covering broad topics in pharmaceutics. Topics may range from the preparation and characterization of new solid forms to the development of new methods and technological strategies to improve the physical stability and manufacturing processes of more soluble solid dosage forms.

Dr. Inês C. B. Martins
Dr. Daniele Musumeci
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • pharmaceutics
  • solid dosage forms
  • amorphous systems
  • crystalline systems
  • drug delivery systems
  • solid-state characterization
  • pharmaceutical technology
  • manufacturing processes

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Published Papers (2 papers)

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Research

14 pages, 5518 KiB  
Article
In Vitro Analysis of Aerodynamic Properties and Co-Deposition of a Fixed-Dose Combination of Fluticasone Furoate, Umeclidinium Bromide, and Vilanterol Trifenatate
by Kittipong Maneechotesuwan, Somchai Sawatdee and Teerapol Srichana
Pharmaceutics 2024, 16(10), 1334; https://doi.org/10.3390/pharmaceutics16101334 - 18 Oct 2024
Viewed by 706
Abstract
Background/Objectives: Effective airway delivery of a fixed-dose combination of triple-aerosolized inhaled corticosteroid (ICS)/long-acting beta agonist (LABA)/long-acting muscarinic antagonist (LAMA) is likely to positively affect therapeutic responses predicted in patients with asthma and chronic obstructive pulmonary disease. This study aimed to conduct in vitro [...] Read more.
Background/Objectives: Effective airway delivery of a fixed-dose combination of triple-aerosolized inhaled corticosteroid (ICS)/long-acting beta agonist (LABA)/long-acting muscarinic antagonist (LAMA) is likely to positively affect therapeutic responses predicted in patients with asthma and chronic obstructive pulmonary disease. This study aimed to conduct in vitro fluticasone furoate, vilanterol trifenatate, and umeclidinium bromide depositions in a Next Generation Impactor. The aerodynamic properties of these inhaled medications influence the spatial distribution and drug abundance, particularly in the smaller airways, to reverse or alleviate disease pathology. Methods: The Next Generation Impactor was used to demonstrate the aerodynamic particle size distributions of fluticasone furoate, vilanterol trifenatate, and umeclidinium bromide delivered from a dry powder inhaler at different flow rates across all stages of the impactors. This in vitro study analyzed the distribution pattern of individual drug components to simulate mono-component deposition and co-deposition in the official model in the United States Pharmacopeia. An Andersen cascade impactor together with scanning electron microscope–energy-dispersive X-ray was employed to observe the drug deposition on each stage of the impactor. Results: We found that the distribution pattern of each component at the same cascade level was comparable, and the aerosol particles of the three drugs reached the in vitro representation of the lower airway compartment. The specified flow rates generated the desired fine particle fraction, fine particle dose, and mass median aerodynamic diameter. Our results also demonstrated visualized deposition patterns of the delivered drugs from different stages of the cascade impactor that may predict deposition as it occurs in vivo. Conclusions: Spatial distribution and abundance of ICS/LABA/LAMA in the same cascade levels were closely comparable, and the aerosol particles were able to reach the small aerosol-sized cascades at the lower levels to some extent. Full article
(This article belongs to the Special Issue Advances in the Preparation and Technology of Pharmaceutical Solid Dosage Forms)
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17 pages, 6082 KiB  
Article
Tailoring Crystallization Kinetics in Thin Sucrose Films during Convective Drying: Impact of Temperature and Humidity on Onset, Growth, and Nucleation Rate
by Martin Schugmann and Petra Foerst
Pharmaceutics 2024, 16(10), 1260; https://doi.org/10.3390/pharmaceutics16101260 - 27 Sep 2024
Viewed by 616
Abstract
Drying experiments with varying air temperature and humidity were conducted to investigate the influence of the drying process on the crystallization of thin sucrose films. For the first time, the effects of the nucleation onset, nucleation rate, and growth rate were investigated in [...] Read more.
Drying experiments with varying air temperature and humidity were conducted to investigate the influence of the drying process on the crystallization of thin sucrose films. For the first time, the effects of the nucleation onset, nucleation rate, and growth rate were investigated in situ and their differentiated influence on product crystallinity could be assessed. The growth rate was not influenced by air humidity but showed a strong dependence on temperature. It increased with drying temperature; however, at high temperatures, growth was inhibited when the water content falls below a critical level. Noticeable differences in nucleation behavior could be observed with regard to air humidity. Dry air led to crystallization onsets at lower levels of supersaturation, while moderately humid air retarded it. At higher temperatures, nucleation onset commenced at lower water contents but at a constant supersaturation level. The nucleation rate doubled in experiments with moderately humid air (15% RH), while an elevated drying temperature showed generally lower nucleation rates. The observed differences in the nucleation onset and rate could be explained by the film-internal concentration profile, which is strongly influenced by drying parameters. The insights therefore provide a differentiated understanding of the formation of the physical state and how it can be influenced during convective drying. Full article
(This article belongs to the Special Issue Advances in the Preparation and Technology of Pharmaceutical Solid Dosage Forms)
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