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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: 28 February 2026 | Viewed by 5796

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 (5 papers)

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Research

23 pages, 5773 KiB  
Article
An Investigation into the Effect of Maltitol, Sorbitol, and Xylitol on the Formation of Carbamazepine Solid Dispersions Through Thermal Processing
by Madan Sai Poka, Marnus Milne, Anita Wessels and Marique Aucamp
Pharmaceutics 2025, 17(3), 321; https://doi.org/10.3390/pharmaceutics17030321 - 2 Mar 2025
Viewed by 650
Abstract
Background: Carbamazepine (CBZ) is a Biopharmaceutical Classification System (BCS) class II drug, that is practically insoluble in water, influencing the oral bioavailability. Polyols are highly hydrophilic crystalline carriers studied for their success in developing solid dispersions (SDs) for improved solubility and dissolution rate. [...] Read more.
Background: Carbamazepine (CBZ) is a Biopharmaceutical Classification System (BCS) class II drug, that is practically insoluble in water, influencing the oral bioavailability. Polyols are highly hydrophilic crystalline carriers studied for their success in developing solid dispersions (SDs) for improved solubility and dissolution rate. Polyols are generally regarded as safe (GRAS) and maltitol (MAL), xylitol (XYL) and sorbitol (SOR) are among the approved polyols for market use. While xylitol (XYL) and sorbitol, have shown promise in improving the solubility and dissolution rates of poorly soluble drugs, their full potential in the context of improving the solubility of carbamazepine have not been thoroughly investigated. To the best of our knowledge, maltitol (MAL) was not studied previously as a carrier for preparing SDs. Hence, the purpose of this study was to investigate their use in the preparation of CBZ SDs by the fusion method. Methods: CBZ-polyol SDs were prepared in varying molar ratios (2:1, 1:1 and 1:2) and characterised for solid-state nature, solubility and in-vitro dissolution rate. Results: Solid-state characterisation of the CBZ-polyol SDs revealed the existence of the SDs as continuous glass suspensions with fine CBZ crystallites suspended in the amorphous polyol carriers. Among the polyols studied, XYL exhibited good miscibility with CBZ and showed significant improvement in the solubility and dissolution rate. The prepared SDs showed a 2 to 6-folds increase in CBZ solubility and 1.4 to 1.9-folds increase in dissolution rate in comparison with pure CBZ. Conclusions: The study explains the possible use of polyols (XYL and SOR) based SDs of BCS Class II drugs with good glass forming ability for enhanced solubility and dissolution. 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, 4851 KiB  
Article
Mechanistic Investigation into Crystallization of Hydrated Co-Amorphous Systems of Flurbiprofen and Lidocaine
by Xiaoyue Xu, Holger Grohganz, Justyna Knapik-Kowalczuk, Marian Paluch and Thomas Rades
Pharmaceutics 2025, 17(2), 175; https://doi.org/10.3390/pharmaceutics17020175 - 30 Jan 2025
Viewed by 732
Abstract
Background: It is generally accepted that water as a plasticizer can decrease the glass transition temperatures (Tgs) of amorphous drugs and drug delivery systems, resulting in physical instabilities. However, a recent study has reported an anti-plasticizing effect of water on amorphous [...] Read more.
Background: It is generally accepted that water as a plasticizer can decrease the glass transition temperatures (Tgs) of amorphous drugs and drug delivery systems, resulting in physical instabilities. However, a recent study has reported an anti-plasticizing effect of water on amorphous lidocaine (LID). In co-amorphous systems, LID might be used as a co-former to impair the plasticizing effect of water. Method: Flurbiprofen (FLB) was used to form a co-amorphous system with a mole fraction of LID of 0.8. The effect of water on the stability of co-amorphous FLB-LID upon hydration was investigated. The crystallization behaviors of anhydrous and hydrated co-amorphous FLB-LID systems were measured by an isothermal modulated differential scanning calorimetric (iMDSC) method. The relaxation times of the co-amorphous FLB-LID system upon hydration were measured by a broadband dielectric spectroscopy (BDS), and the differences in Gibbs free energy (ΔG) and entropy (ΔS) between the amorphous and crystalline phases were determined by differential scanning calorimetry (DSC). Results: It was found that the crystallization tendency of co-amorphous FLB-LID decreased with the addition of water. Molecular mobility and thermodynamic factors were both investigated to explain the difference in crystallization tendencies of co-amorphous FLB-LID upon hydration. Conclusions: The results of the study showed that LID could be used as an effective co-former to decrease the crystallization tendency of co-amorphous FLB-LID upon hydration by enhancing the entropic (ΔS) and thermodynamic activation barriers (TΔS)3/ΔG2) to crystallization. Full article
(This article belongs to the Special Issue Advances in the Preparation and Technology of Pharmaceutical Solid Dosage Forms)
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14 pages, 3511 KiB  
Article
Drug–Phospholipid Co-Amorphous Formulations: The Role of Preparation Methods and Phospholipid Selection
by Keyoomars Khorami, Sam Darestani Farahani, Anette Müllertz and Thomas Rades
Pharmaceutics 2024, 16(12), 1602; https://doi.org/10.3390/pharmaceutics16121602 - 16 Dec 2024
Viewed by 904
Abstract
Background/Objectives: This study aims to broaden the knowledge on co-amorphous phospholipid systems (CAPSs) by exploring the formation of CAPSs with a broader range of poorly water-soluble drugs, celecoxib (CCX), furosemide (FUR), nilotinib (NIL), and ritonavir (RIT), combined with amphiphilic phospholipids (PLs), including [...] Read more.
Background/Objectives: This study aims to broaden the knowledge on co-amorphous phospholipid systems (CAPSs) by exploring the formation of CAPSs with a broader range of poorly water-soluble drugs, celecoxib (CCX), furosemide (FUR), nilotinib (NIL), and ritonavir (RIT), combined with amphiphilic phospholipids (PLs), including soybean phosphatidylcholine (SPC), hydrogenated phosphatidylcholine (HPC), and mono-acyl phosphatidylcholine (MAPC). Methods: The CAPSs were initially prepared at equimolar drug-to-phospholipid (PL) ratios by mechano-chemical activation-based, melt-based, and solvent-based preparation methods, i.e., ball milling (BM), quench cooling (QC), and solvent evaporation (SE), respectively. The solid state of the product was characterized by X-ray powder diffraction (XRPD), polarized light microscopy (PLM), and differential scanning calorimetry (DSC). The long-term physical stability of the CAPSs was investigated at room temperature under dry conditions (0% RH) and at 75% RH. The dissolution behavior of the CCX CAPS and RIT CAPS was studied. Results: Our findings indicate that SE consistently prepared CAPSs for CCX-PLs, FUR-PLs, and RIT-PLs, whereas the QC method could only form CAPSs for RIT-PLs, CCX-SPC, and CCX-MAPC. In contrast, the BM method failed to produce CAPSs, but all drugs alone could be fully amorphized. While the stability of each drug varied depending on the PLs used, the SE CAPS consistently demonstrated the highest stability by a significant margin. Initially, a 1:1 molar ratio was used for screening all systems, though the optimal molar ratio for drug stability remained uncertain. To address this, various molar ratios were investigated to determine the ratio yielding the highest amorphous drug stability. Our results indicate that all systems remained physically stable at a 1.5:1 ratio and with excess of PL. Furthermore, the CAPS formed by the SE significantly improves the dissolution behavior of CCX and RIT, whereas the PLs provide a slight precipitation inhibition for supersaturated CCX and RIT. Conclusions: These findings support the use of a 1:1 molar ratio in screening processes and suggest that CAPSs can be effectively prepared with relatively high drug loads compared to traditional drug–polymer systems. Furthermore, the study highlights the critical role of drug selection, the preparation method, and the PL type in developing stable and effective CAPSs. Full article
(This article belongs to the Special Issue Advances in the Preparation and Technology of Pharmaceutical Solid Dosage Forms)
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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 1490
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
Cited by 2 | Viewed by 984
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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