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Pharmaceutics
Special Issues
Drugs-Excipients Interactions
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Drugs-Excipients Interactions

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

Deadline for manuscript submissions: closed (10 April 2024) | Viewed by 4268

Special Issue Editor

Prof. Dr. Titus Vlase

E-Mail Website
Guest Editor
Research Center for Thermal Analysis in Environmental Problems, Universitatea de Vest din Timisoara, Timisoara, Romania
Interests: thermal; spectroscopic and microscopic analysis; drugs-excipients interactions; thermal stability; materials and biomaterials synthesis and testing

Special Issue Information

Dear Colleagues,

Pharmaceutical dosage form is a combination of active pharmaceutical ingredients and excipients. Excipients are chemical compounds included in dosage forms to aid manufacture, administration, or absorption. They can initiate, propagate, or participate in chemical or physical interactions with drug compounds, which may compromise the effectiveness of a drug. Excipients can have functional groups that interact directly with active pharmaceutical ingredients. Alternatively, they may contain impurities or residues, or form degradation products that in turn cause the decomposition of the active substance.

Reporting examples of drug–excipients interactions on a marketed drug or a new mechanism study will be very helpful for highlighting side effects. This Special Issue has the aim of emphasizing the current progress in clinical or non-clinical interactions and elucidating the mechanism of drug–excipients interactions.

Prof. Dr. Titus Vlase
Guest Editor

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–excipients interactions
  • degradation products
  • decomposition
  • stability
  • investigation method
  • life time prediction
  • kinetics
  • solid–solid interactions

Published Papers (1 paper)

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Research

15 pages, 2940 KiB  
Article
Modeling the Impact of Excipients Selection on Nitrosamine Formation towards Risk Mitigation
by Alberto Berardi, Maarten Jaspers and Bastiaan H. J. Dickhoff
Pharmaceutics 2023, 15(8), 2015; https://doi.org/10.3390/pharmaceutics15082015 - 25 Jul 2023
Viewed by 4015
Abstract
Risk control for nitrosamine impurities in drug products is currently a major challenge in the industry. Nitrosamines can form during drug product manufacturing and storage through the reaction of nitrites with amine-containing APIs or impurities. The level of nitrites in excipients and the [...] Read more.
Risk control for nitrosamine impurities in drug products is currently a major challenge in the industry. Nitrosamines can form during drug product manufacturing and storage through the reaction of nitrites with amine-containing APIs or impurities. The level of nitrites in excipients and the rate of reaction often control the build-up of nitrosamine. Although the variability in nitrite levels across excipient types and suppliers is well recognized, the impact of excipient selection on the level of nitrosamine formed has not been systematically studied. This gap of knowledge is addressed in the current work. We present theoretical case studies of formulations where microcrystalline cellulose (MCC), or lactose supplier, or superdisintegrant type are changed in pursuit of lower levels of nitrite. The impact of the average, maximum, and minimum levels of nitrites in each excipient on nitrosamine formation in the dosage form is calculated. The input data for this calculation are the formulation composition, nitrosamine molecular weight (MW), percentage of conversion, and nitrite levels per excipient. The percentage of conversion (based on the formulation and manufacturing variables) and nitrite levels were taken from the recent literature. We show that changing the supplier of a single excipient, or of the three most critical excipients, can reduce nitrosamine formation by up to −59% and −89%, respectively. We also show that high-risk formulations, e.g., high MW nitrosamines, high dosage weights, and high percentages of conversion (e.g., wet granulation), can often be de-risked below regulatory acceptable daily intake via careful excipient selection. Finally, we provide an open-access tool that enables users to calculate the theoretical formation of nitrosamines in their specific formulations. This calculation template can be used for (i) the preliminary screening of the risk of nitrosamine formation in drug products and (ii) the preliminary assessment of the impact of excipient selection for risk mitigation. Full article
(This article belongs to the Special Issue Drugs-Excipients Interactions)
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