Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

Liang, Zhengxuan; Chen, Hongbo; Wang, Chenguang; Sun, Changquan Calvin

doi:10.3390/cryst10110996

Cited by 5 publications

(2 citation statements)

References 39 publications

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“…The concept of supramolecular synthon or hydrogen-bonded building units was later developed by Desiraju . Cocrystal formation has become a powerful tool for enhancing key pharmaceutical properties, including stability, dissolution, , bioavailability, and manufacturability in the industry. Other applications, such as taste masking and toxicity reduction, have also been reported.…”

Section: Introductionmentioning

confidence: 99%

Bioavailability-Enhancing Cocrystals: Screening, In Vivo Predictive Dissolution, and Supersaturation Maintenance

Chen

Huang

Zhang

et al. 2022

Crystal Growth & Design

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Cocrystal engineering for bioavailability enhancement is still a serendipitous process, which requires systematic solution crystallization, in vivo predictive dissolution, and biopharmaceutical simulation. The purpose of this study is to improve bioavailability through cocrystal engineering, with a focus on understanding the mechanism of supersaturation maintenance during dissolution. BI 639667 is a poorly soluble and fast precipitating compound. The ability of its cocrystal with salicylic acid (SA) to maintain supersaturation was assessed using a modified two-step dissolution method, and its bioavailability was determined in rats. Biopharmaceutical simulation and dissolution modeling were performed to predict the in vivo performance in humans. Conductor-like screening model for realistic solvents and molecular dynamics (MD) simulation were used to study the interactions between the active pharmaceutical ingredient (API) and coformers in vacuum and aqueous media, respectively. A high melting cocrystal with SA, crystallized in dichloromethane, showed moderate solubility enhancement with prolonged supersaturation during dissolution, which was able to enhance bioavailability with reduced C max , compared to amorphous dispersion. The radial distribution function (RDF) between the API and selected coformers was calculated using MD simulation to determine the mean distance between the API and coformer molecules in aqueous media. The result suggests that SA could better compete against water for interactions with the API and could penetrate the API molecular clusters to inhibit nucleation. Thus, the RDF by MD simulation may be used to determine the disruptive effect of water on the interaction between the API and coformer and improve cocrystal engineering for bioavailability enhancement.

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Section: Introductionmentioning

confidence: 99%

Bioavailability-Enhancing Cocrystals: Screening, In Vivo Predictive Dissolution, and Supersaturation Maintenance

Chen

Huang

Zhang

et al. 2022

Crystal Growth & Design

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“…, mikroemulsi [4], nanopartikel [5], kokristal [6] dan dispersi padat [7]. Pembentukan garam merupakan metode termudah dalam upaya peningkatan kelarutan suatu senyawa, namun metode ini menjadi kurang efektif karena pengaplikasiannya yang hanya berlaku pada beberapa zat aktif tertentu.…”

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Pemilihan Jenis Koformer dan Metode Preparasi dalam Sistem Penghantaran Sediaan Ko-Amorf

2021

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Ko-amorf adalah suatu sistem multikomponen padat yang mengandung zat aktif dan molekul dengan berat molekul rendah lainnya (koformer) yang dapat berupa eksipien atau zat aktif yang relevan secara farmakologis. Formulasi ko-amorf yang dibuat dengan metode preparasi dan jenis koformer yang berbeda dapat menghasilkan perbedaan yang signifikan dalam stabilitas fisik dan profil disolusi suatu bentuk ko-amorf. Tujuan penulisan dari artikel review ini adalah untuk menggali informasi lebih dalam tentang sistem ko-amorf, klasifikasi ko-amorf, karakterisasi ko-amorf serta pengaruh jenis koformer dan metode preparasi ko-amorf terhadap pembentukan ko-amorf. Artikel review ini disusun dengan literature search melalui PubMed, MDPI dan Science Direct dengan memasukkan kata kunci co-amorphous, co-amorphous formulations, co-amorphous stabilizers, co-amorphous drug formulations. Dari review ini ditemukan terdapat beberapa jenis koformer yang dapat digunakan untuk pembentukan ko-amorf yaitu dapat berupa zat aktif yang relevan secara farmakologis dan eksipien seperti diantaranya yaitu asam amino, asam karboksilat, asam tanat, quercetin, sakarin dan nikotinamid. Dan untuk metode preparasi ko-amorf yang dapat digunakan diantaranya yaitu ball milling, cryomilling, melt quenching/ quench cooling, hot melt extrusion, solvent evaporation, spray drying, freeze drying hingga teknologi seperti supercritical antisolvent dan microwave technique. Keberhasilan pembentukan ko-amorf ditentukan diantaranya oleh pemilihan jenis koformer yang melibatkan berbagai sifat yang perlu dipertimbangkan, seperti Tg, potensial ikatan hidrogen, ketercampuran/ miscibility, atau perilaku kristalisasi. Sifat zat aktif dan eksipien seperti stabilitas termal, suhu leleh dan kecenderungan kristalisasi zat aktif dan eksipien, menjadi faktor yang perlu diperhatikan dalam pemilihan metode preparasi ko-amorf.

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A comprehensive review of recent advances in the applications and biosynthesis of oxalic acid from bio-derived substrates

Amenaghawon,

Ayere,

Amune

et al. 2024

Environmental Research

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Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

Cited by 5 publications

References 39 publications

Bioavailability-Enhancing Cocrystals: Screening, In Vivo Predictive Dissolution, and Supersaturation Maintenance

Bioavailability-Enhancing Cocrystals: Screening, In Vivo Predictive Dissolution, and Supersaturation Maintenance

Pemilihan Jenis Koformer dan Metode Preparasi dalam Sistem Penghantaran Sediaan Ko-Amorf

A comprehensive review of recent advances in the applications and biosynthesis of oxalic acid from bio-derived substrates

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