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Pharmaceutics
Special Issues
Pharmaceutical Dosage Forms: Drug Release, Solubility and Stability Evaluation
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Pharmaceutical Dosage Forms: Drug Release, Solubility and Stability Evaluation

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 5539

Special Issue Editors

Dr. Laura Sbârcea

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Guest Editor
Department of Drug Analysis, Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: drug solubility; cyclodextrin-based delivery systems; drug analysis and quality control; drug stability; drug–drug interactions; drug-excipient interactions
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Adriana Violeta Ledeți

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Guest Editor
Department of Analytical Chemistry, Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: drug stability and stabilization techniques; instrumental analysis of active pharmaceutical ingredients; heterogenous degradation of drugs; solid-state kinetics; supramolecular systems with increased biopharmaceutical profile
Special Issues, Collections and Topics in MDPI journals
Dr. Valentina Oana Buda

E-Mail Website
Guest Editor
Department of Clinical Pharmacy, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania
Interests: pharmacology; clinical pharmacy; pharmaceutical care; hypertension; endothelial dysfunction; elderly; heart failure; inappropriate medication; atherosclerosis; antipsychotics; phytotherapy; phytonutrients; black chokeberry; evening primrose; cannabidiol; black poplar; micronutrients; macronutrients
Dr. Denisa Laura Cîrcioban

E-Mail Website
Guest Editor
Department of Analytical Chemistry, Faculty of Pharmacy, “Victor Babeş” University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania
Interests: stability of drugs and compounds with potential biological activity; instrumental analysis of drugs as pure APIs and in pharmaceutical dosage forms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The release of drugs from the formulations is an important process in both immediate release and modified release dosage forms since it governs the efficiency of the pharmaceutical dosage forms. It also plays a crucial role in the design and optimization of modified release dosage forms including sustained, controlled, and delayed release forms and novel drug delivery systems. One of the most critical and important parameters impacting drug release is drug solubility, an essential property of a drug substance, vital for its bioavailability. Poor solubility can lead to low bioavailability and results in sub-optimal drug delivery, being a significant impediment to drug development efforts.

In the two past decades, the use of sophisticated experimental techniques, advanced computational methods, and complementary technologies in the drug discovery process has led to poor water solubility for nearly 60%‒90% of the developmental pipeline drugs and almost 40% of approved drugs. Nowadays, a lot of studies involve different approaches for enhancing the solubility of poorly water-soluble drugs and the design and development of modified drug delivery systems with optimized biopharmaceutics, pharmacokinetic and pharmacodynamics properties of drugs.

This Special Issue aims at collecting research covering drug solubility along with techniques and strategies addressing low solubility of active substances, drug release, modified drug delivery systems and issues related to drug stability, including drug-excipient interaction, being known the major importance in the selection of suitable excipients in the drug development process for the efficiency, quality, safety and stability of pharmaceutical dosage forms. In this Special Issue, original research articles and reviews are welcome.

We look forward to receiving your contributions.

Dr. Laura Sbârcea
Prof. Dr. Adriana Violeta Ledeți
Dr. Valentina Oana Buda
Dr. Denisa Laura Cîrcioban
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

  • drug solubility
  • drug release kinetics
  • dissolution
  • bioavailability
  • modified drug delivery systems
  • drug stability
  • drug-excipient interaction

Published Papers (2 papers)

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Research

14 pages, 2979 KiB  
Article
Using Nuclear Magnetic Resonance to Troubleshoot a Stability Issue in a Real-World Formulation Chassis—Application to Consumer Oral Healthcare
by Tomris Coban, Hannah Sykes, Shreedhar Kulkarni, Robert A. Lucas, Cameron Robertson and Adam Le Gresley
Pharmaceutics 2024, 16(3), 320; https://doi.org/10.3390/pharmaceutics16030320 - 24 Feb 2024
Viewed by 702
Abstract
With direct application to current and future consumer healthcare products, this research sheds light on the importance of packaging and its potential effects on both Active Pharmaceutical Ingredient (API) delivery and stability. Industrially sourced, proprietary experimental formulations (PEFs), specifically oral cleansers, based on [...] Read more.
With direct application to current and future consumer healthcare products, this research sheds light on the importance of packaging and its potential effects on both Active Pharmaceutical Ingredient (API) delivery and stability. Industrially sourced, proprietary experimental formulations (PEFs), specifically oral cleansers, based on salicylic acid and hydrogen peroxide, discolored over time at different rates, depending on packaging type used. This discoloration stemmed from an interplay of two factors, involving both spontaneous formulation degradation and the interaction of both degradants and salicylic acid with the internal surface of the packaging. This manuscript reports on the investigation to uncover the origins of discoloration. To investigate this real-world, industrial pipeline problem, we exploited the high dimensionality and simple sample preparation uniquely afforded by NMR. Using a combination of 1D/2D NMR and diffusion-ordered NMR spectroscopy (DOSY) to leverage molecular mass estimations from, we not only quickly confirmed the identities of these degradants, but also assessed their formation as a function of temperature and pH, providing insight into the mechanisms underlying their formation. We were able to identify catechol as the main source of discoloration over a period of several weeks, being formed at the ppm level. Furthermore, we evaluated the formulation–container interaction, employing NMR, ICP-MS, and ATR-IR. Despite this comprehensive analysis, the root causes of discoloration could only tentatively be assigned to a surface Ti complex of salicylic acid and other hydroxy carboxylic acids. Through the understanding of formulation degradation pathways, we were able to support further toxicology assessment, vital to both consumer safety and the manufacturer. This work underscores the invaluable role of NMR in the analysis of intricate proprietary mixtures with a consumer-centric purpose. Our findings demonstrate that conventional analytical techniques falter in the face of such complexity, requiring extensive preparation and pre-analytical processing, highlighting the novelty and crucial relevance of NMR research to manufacturers and consumers. Such an analysis is of value in the pursuit of materials within the consumer-healthcare space, which meet the requirements for successful recycling or re-use. Full article
(This article belongs to the Special Issue Pharmaceutical Dosage Forms: Drug Release, Solubility and Stability Evaluation)
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32 pages, 15734 KiB  
Article
Development of Clinically Optimized Sitagliptin and Dapagliflozin Complex Tablets: Pre-Formulation, Formulation, and Human Bioequivalence Studies
by So-Jin Kang and Joo-Eun Kim
Pharmaceutics 2023, 15(4), 1246; https://doi.org/10.3390/pharmaceutics15041246 - 14 Apr 2023
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Abstract
The purpose of this study is to derive an optimal drug release formulation with human clinical bioequivalence in developing a sitagliptin phosphate monohydrate-dapagliflozin propanediol hydrate fixed-dose combination (FDC) tablet as a treatment for type 2 diabetes mellitus. As a treatment for type 2 [...] Read more.
The purpose of this study is to derive an optimal drug release formulation with human clinical bioequivalence in developing a sitagliptin phosphate monohydrate-dapagliflozin propanediol hydrate fixed-dose combination (FDC) tablet as a treatment for type 2 diabetes mellitus. As a treatment for type 2 diabetes mellitus, the combined prescription of dipeptidyl peptidase-4 (DPP-4) inhibitors and sodium-glucose cotransporter-2 (SGLT-2) inhibitors is common. Therefore, this study simplified the number of individual drugs taken and improved drug compliance by developing FDC tablets containing sitagliptin phosphate monohydrate as a DPP-4 inhibitor and dapagliflozin propanediol hydrate as an SGLT-2 inhibitor. To derive the optimal dosage form, we prepared single-layer tablets, double-layer tablets, and dry-coated tablets and evaluated the drug control release ability, tableting manufacturability, quality, and stability. Single-layer tablets caused problems with stability and drug dissolution patterns. When the dissolution test was performed on the dry-coated tablets, a corning effect occurred, and the core tablet did not completely disintegrate. However, in the quality evaluation of the double-layer tablets, the hardness was 12–14 kilopond, the friability was 0.2%, and the disintegration was within 3 min. In addition, the stability test revealed that the double-layer tablet was stable for 9 months under room temperature storage conditions and 6 months under accelerated storage conditions. In the drug release test, only the FDC double-layer tablet showed the optimal drug release pattern that satisfied each drug release rate. In addition, the FDC double-layer tablet showed a high dissolution rate of over 80% in the form of immediate-release tablets within 30 min in a pH 6.8 dissolution solution. In the human clinical trial, we co-administered a single dose of a sitagliptin phosphate monohydrate-dapagliflozin propanediol hydrate FDC double-layered tablet and the reference drug (Forxiga®, Januvia®) in healthy adult volunteers. This study showed clinically equivalent results in the stability and pharmacodynamic characteristics between the two groups. Full article
(This article belongs to the Special Issue Pharmaceutical Dosage Forms: Drug Release, Solubility and Stability Evaluation)
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