Preparation Technologies and Dissolution Behaviour of Oral Solids

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (31 May 2025) | Viewed by 4063

Special Issue Editors


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Guest Editor
Department of Pharmacy and Pharmaceutical Sciences, Faculty of Science, National University of Singapore, Singapore, Singapore
Interests: pharmaceutical technology; in areas of coating; pelletization; microencapsulation; powder technology; preparation of botanicals; controlled release formulations; process science

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Guest Editor
Department of Pharmacy and Pharmaceutical Sciences, Faculty of Science, National University of Singapore, Singapore, Singapore
Interests: oral solids; stability testing; formulation design; excipients; tableting

Special Issue Information

Dear Colleagues,

You are invited to submit manuscripts in this special issue “Preparation Technologies and Dissolution Behavior of Oral Solids”. Oral solids are ubiquitous as dosage forms to treat all the ills and chills by patients. Despite the many preparation methods in use for oral solids, there is still the search for innovative preparation technologies to overcome the limitations of the commonly used methods such as high shear wet granulation. Improvements in preparation methods such as the use of continuous manufacturing methods have improved productivity in the drug development process.  There is also a great interest in the technology and formulation design to improve the oral bioavailability or release properties of poorly water-soluble drugs. In another spectrum, the release properties of fast dissolving drugs could be extended over a wider time span or be released at the desired site in the gastrointestinal tract through the use of specialized preparation technologies that confer the requisite properties to the oral solid dosage form. Clearly, preparation technologies of oral solids can impact the dissolubility of the oral solid dosage form. Additionally, properties of the drug itself like particle size and crystal form have their influence on the dissolution behaviors of oral solids. We look forward to manuscripts related to preparation technologies, dissolution and sustained release oral solids. 

Dr. Paul Wan Sia Heng
Dr. Natalia Veronica
Guest Editors

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Keywords

  • granulation
  • oral solids
  • dissolution
  • sustain release
  • solubility
  • oral bioavailability

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Published Papers (1 paper)

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Research

17 pages, 2672 KiB  
Article
Mannitol-Coated Hydroxypropyl Methylcellulose as a Directly Compressible Controlled Release Excipient for Moisture-Sensitive Drugs: A Stability Perspective
by Christina Yong Xin Kang, Keat Theng Chow, Yuan Siang Lui, Antoine Salome, Baptiste Boit, Philippe Lefevre, Tze Ning Hiew, Rajeev Gokhale and Paul Wan Sia Heng
Pharmaceuticals 2024, 17(9), 1167; https://doi.org/10.3390/ph17091167 - 4 Sep 2024
Cited by 3 | Viewed by 3565
Abstract
Background/Objectives: Hydroxypropyl methylcellulose (HPMC) is one of the most commonly used hydrophilic polymers in formulations of matrix tablets for controlled release applications. However, HPMC attracts moisture and poses issues with drug stability in formulations containing moisture-sensitive drugs. Methods: Herein, the moisture sorption behavior [...] Read more.
Background/Objectives: Hydroxypropyl methylcellulose (HPMC) is one of the most commonly used hydrophilic polymers in formulations of matrix tablets for controlled release applications. However, HPMC attracts moisture and poses issues with drug stability in formulations containing moisture-sensitive drugs. Methods: Herein, the moisture sorption behavior of excipients and drug stability using aspirin as the model drug in matrix tablets were evaluated, using HPMC and the newly developed mannitol-coated HPMC, under accelerated stability conditions (40 °C, 75% relative humidity) with open and closed dishes. Results: Tablets prepared with mannitol-coated HPMC showed a slower drug degradation rate compared to tablets prepared with directly compressible HPMC. Initial moisture content and hygroscopicity were stronger predictors of drug stability compared to water activity when comparing samples without similar moisture content. In the early stage (day 0 to 30), the aspirin degradation rate was similar in both open and closed conditions, as moisture content is the main degradation contributor. In the later stage (day 30 to 90), aspirin degradation was faster under closed conditions than under open conditions, likely due to autocatalytic effects caused by the volatile acidic by-product entrapped in the closed environment. Conclusions: The findings from this study reinforced the importance of judicious excipient selection based on the understanding of excipient–moisture interactions to maximize the chemical stability of moisture-sensitive drugs. Mannitol-coated HPMC is a promising addition to the formulator’s toolbox for the formulation of controlled release dosage forms by direct compression. Full article
(This article belongs to the Special Issue Preparation Technologies and Dissolution Behaviour of Oral Solids)
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