Development, recent advances, and updates in binary, ternary co-amorphous systems, and ternary solid dispersions

Saberi, Arezoo; Kouhjani, Maryam; Yari, Davood; Jahani, Afsaneh; Asare-Addo, Kofi; Kamali, Hossein; Nokhodchi, Ali

doi:10.1016/j.jddst.2023.104746

Cited by 9 publications

(1 citation statement)

References 247 publications

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“…Amorphous drugs are known to exhibit instability and a propensity to transform into a crystalline form, resulting in reduced solubility and bioavailability [4]. This phenomenon was especially evident when amorphous drugs were subjected to high temperature and humidity [5,6].…”

Section: Introductionmentioning

confidence: 99%

The Optimization of Pair Distribution Functions for the Evaluation of the Degree of Disorder and Physical Stability in Amorphous Solids

Yuan,

Li,

Luo

et al. 2024

Molecules

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The amorphous form of poorly soluble drugs is physically unstable and prone to crystallization, resulting in decreased solubility and bioavailability. However, the conventional accelerated stability test for amorphous drugs is time-consuming and inaccurate. Therefore, there is an urgent need to develop rapid and accurate stability assessment technology. This study used the antitumor drug nilotinib free base as a model drug. The degree of disorder and physical stability in the amorphous form was assessed by applying the pair distribution function (PDF) and principal component analysis (PCA) methods based on powder X-ray diffraction (PXRD) data. Specifically, the assessment conditions, such as the PDF interatomic distance range, PXRD detector type, and PXRD diffraction angle range were also optimized. The results showed that more reliable PCA data could be obtained when the PDF interatomic distance range was 0–15 Å. When the PXRD detector was a semiconductor-type detector, the PDF data obtained were more accurate than other detectors. When the PXRD diffraction angle range was 5–40°, the intermolecular arrangement of the amorphous drugs could be accurately predicted. Finally, the accelerated stability test also showed that under the above-optimized conditions, this method could accurately and rapidly assess the degree of disorder and physical stability in the amorphous form of drugs, which has obvious advantages compared with the accelerated stability test.

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Section: Introductionmentioning

confidence: 99%

The Optimization of Pair Distribution Functions for the Evaluation of the Degree of Disorder and Physical Stability in Amorphous Solids

Yuan,

Li,

Luo

et al. 2024

Molecules

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Novel nimesulide multicomponent solid forms: screening, synthesis, thermoanalytical study and characterization

de Almeida,

Ferreira,

Porto

et al. 2024

J Therm Anal Calorim

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Nimesulide (NMS) is a widely used non-steroidal anti-inflammatory drug, however, presents low aqueous solubility. One way to overcome the solubility issue of drugs is altering their solid forms through some approaches like cocrystals, coamorphous, and eutectic mixtures. The purpose of this work was to prospect new multicomponent solid forms of NMS. A virtual-experimental cocrystal screening was carried out through COSMOquick software and mechanochemical experiments. Alternatively, dual-drug coamorphous systems were investigated by quench cooling and/or cryomilling processes. All solid samples were characterized using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and infrared spectroscopy (FTIR). The results confirmed the successful synthesis of a NMS-piperazine cocrystal (NMS-PPZ), two new eutectic mixtures NMS-gentisic acid (NMS-GSA) and NMS-isoniazid (NMS-INH), as well as novel drug-drug coamorphous systems. The eutectic compositions were determined by binary solid–liquid phase diagram construction and Tamman’s triangle plot. Nimesulide-omeprazole (NMS-OMP) coamorphous system was found to be stable for at least 120 days in dry conditions. The coamorphous system with bicalutamide (NMS-BICA) prepared by quench cooling process is more stable than that obtained by cryomilling. Finally, the dissolution rate study demonstrated that NMS multicomponent systems are dissolved relatively faster than pure drug.

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Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

Patra,

Singha,

Sahu

et al. 2024

Biomedical Materials & Devices

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Development, recent advances, and updates in binary, ternary co-amorphous systems, and ternary solid dispersions

Cited by 9 publications

References 247 publications

The Optimization of Pair Distribution Functions for the Evaluation of the Degree of Disorder and Physical Stability in Amorphous Solids

The Optimization of Pair Distribution Functions for the Evaluation of the Degree of Disorder and Physical Stability in Amorphous Solids

Novel nimesulide multicomponent solid forms: screening, synthesis, thermoanalytical study and characterization

Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

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