Introduction to Pharmaceutical Co-amorphous Systems Using a Green Co-milling Technique

Silva, Joana F. C.; Rosado, Mário T. S.; Maria, Teresa M. R.; Silva, Pedro S. Pereira; Silva, Manuela Ramos; Eusébio, M. Ermelinda S.

doi:10.1021/acs.jchemed.3c00036

Cited by 7 publications

(3 citation statements)

References 34 publications

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“…To the best of our knowledge, there are limited works in the literature that focus on laboratory educational experiment approaches to medicinal mechanochemical synthesis. Typical examples of application include the synthesis of a small library of sulfonylureas with antidiabetic properties, the synthesis of polymers and the dual-drug naproxen-cimetidine coamorphous system . Though the preparation of Zn-nalidixic acid ACF was first reported in 2018, its synthesis, chemical characterization, and antibacterial activity evaluation as an educative approach are herein described for the first time.…”

Section: Introductionmentioning

confidence: 99%

Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems

Domínguez-Martín,

Ntungwe,

Isca

et al. 2024

J. Chem. Educ.

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For decades, multiple varieties of antibiotics have been successfully used for therapeutic purposes. Nevertheless, antibiotic resistance is currently one of the major threats to global health. This work presents an innovative laboratory practice carried out in an inorganic medicinal chemistry course within the Degrees of Pharmacy and Biochemistry for undergraduate students. This experiment includes three classes of 2 h each. The first class consisted of the mechanochemical synthesis of an antibiotic coordination framework (ACF) using a known antibiotic (nalidixic acid) and zinc as the ligand. The prepared Zn-nalidixic acid ACF (Zn-ACF) was obtained in up to 82% yield with high purity. On the second day, the synthesized Zn-ACF was characterized by Fourier-transform infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD). Finally, during the last class, the antimicrobial activity was tested against Escherichia coli by the well diffusion method. The students verified the higher antimicrobial activity of Zn-ACF compared to nalidixic acid, proving that small changes in the chemical structure can result in great biological differences. In the end, the students presented their results in a poster format, encouraging the development of their soft skills and scientific results communication and dissemination. In the future, it is expected that such a laboratory experiment at the interface between medicinal chemistry, microbiology, analytical techniques, public health, and pharmacology will lead to the development and implementation of some service-learning practices and will serve as a model to look at for other courses and institutions.

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Section: Introductionmentioning

confidence: 99%

Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems

Domínguez-Martín,

Ntungwe,

Isca

et al. 2024

J. Chem. Educ.

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show abstract

“…7–9 These amorphous binary mixtures can be stabilized by different kinds of interactions, frequently hydrogen bonding, between the drug and the co-former, or segregation, avoiding recrystallization. 10–12 The co-amorphous drug systems may improve the apparent solubility and dissolution rates of the API. 13–15 The most common amorphization methodologies include milling and quench-cooling.…”

Section: Introductionmentioning

confidence: 99%

Avoiding pits on the energy landscape – alternative strategies for stabilizing nateglinide co-amorphous systems

Silva,

Jasiurkowska-Delaporte,

Pereira Silva

et al. 2024

CrystEngComm

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“…In the pharmaceutical industry, in vitro drug dissolution tests are typically performed with dissolution devices authorized by and following the standard protocol developed by the United States Pharmacopeia (USP) . Chemistry education studies have been conducted for implementing pharmaceutical analysis in teaching laboratories, particularly in the identification − and quantification of drug molecules − and introduction to drug design. − However, there are a limited number of laboratory experiments in dissolution testing developed for the undergraduate chemistry curriculum; , USP dissolution apparatuses are expensive, and it is not feasible to provide one instrument for each student group in the teaching lab. We decided to design a cost-effective apparatus and develop a dissolution protocol for the undergraduate teaching laboratory.…”

mentioning

confidence: 99%

Spectroscopic Monitoring and Modeling Drug Dissolution for Undergraduate Chemistry Curriculum

Guo,

Wendel,

Lee

et al. 2024

J. Chem. Educ.

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The pharmaceutical and medicine manufacturing industry has become the largest industrial sector for the employment of chemists, indicating a need for experiments with a pharmaceutical sciences context in the undergraduate chemistry curriculum. In the pharmaceutical industry, testing drug dissolution is a key analytical task for solid oral dosage forms that is performed in different phases of drug development to test the release behavior of new formulations, ensure consistency between manufacturing lots, and help predict the in vivo absorption of the drug substance after administration. However, there are a limited number of laboratory experiments in dissolution testing developed for the undergraduate chemistry curriculum. To help students obtain hands-on experience in dissolution testing, a protocol has been developed for an undergraduate chemistry laboratory course for students to build a dissolution apparatus, monitor dissolution processes, model the dissolution to extract kinetic parameters, and evaluate the consistency between dissolution curves with FDA regulated methods. Students successfully collected dissolution curves and completed the modeling analysis with nonlinear least-squares fitting. The designed dissolution protocol has been evaluated to have consistency and reproducibility to be implemented in the undergraduate chemistry laboratory curriculum.

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Introduction to Pharmaceutical Co-amorphous Systems Using a Green Co-milling Technique

Cited by 7 publications

References 34 publications

Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems

Antibiotic Coordination Frameworks against Antibiotic Resistance: How to Involve Students through Experimental Practices in the Search for Solutions to Public Health Problems

Avoiding pits on the energy landscape – alternative strategies for stabilizing nateglinide co-amorphous systems

Spectroscopic Monitoring and Modeling Drug Dissolution for Undergraduate Chemistry Curriculum

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