Kinetics of co-crystal formation with caffeine and citric acid via liquid-assisted grinding analyzed using the distinct element method

Shimono, Keisuke; Kadota, Kazunori; Tozuka, Yuichi; Shimosaka, Atsuko; Shirakawa, Yoshiyuki; Hidaka, Jusuke

doi:10.1016/j.ejps.2015.05.017

Cited by 38 publications

(16 citation statements)

References 54 publications

(51 reference statements)

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“…The speed of cocrystal formation increases with the grinding force. 98) However, grinding often encounters difficulties during scale-up because of its sensitivity to raw material quality and various process parameters. Related technologies such as solvent-added high-shear grinding 99) and polymer-assisted grinding 40) have also been explored.…”

Section: Manufacturing Of Cocrystalsmentioning

confidence: 99%

Characterization and Quality Control of Pharmaceutical Cocrystals

Izutsu¹,

Koide²,

Takata

et al. 2016

Chem. Pharm. Bull.

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Recent active research and new regulatory guidance on pharmaceutical cocrystals have increased the rate of their development as promising approaches to improve handling, storage stability, and bioavailability of poorly soluble active pharmaceutical ingredients (APIs). However, their complex structure and the limited amount of available information related to their performance may require development strategies that differ from those of single-component crystals to ensure their clinical safety and efficacy. This article highlights current methods of characterizing pharmaceutical cocrystals and approaches to controlling their quality. Different cocrystal regulatory approaches between regions are also discussed. The physical characterization of cocrystals should include elucidating the structure of their objective crystal form as well as their possible variations (e.g., polymorphs, hydrates). Some solids may also contain crystals of individual components. Multiple processes to prepare pharmaceutical cocrystals (e.g., crystallization from solutions, grinding) vary in their applicable ingredients, scalability, and characteristics of resulting solids. The choice of the manufacturing method affects the quality control of particular cocrystals and their formulations. In vitro evaluation of the properties that govern clinical performance is attracting increasing attention in the development of pharmaceutical cocrystals. Understanding and mitigating possible factors perturbing the dissolution and/ or dissolved states, including solution-mediated phase transformation (SMPT) and precipitation from supersaturated solutions, are important to ensure the bioavailability of orally administrated lower-solubility APIs. The effect of polymer excipients on the performance of APIs emphasizes the relevance of formulation design for appropriate use.

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Section: Manufacturing Of Cocrystalsmentioning

confidence: 99%

Characterization and Quality Control of Pharmaceutical Cocrystals

Izutsu¹,

Koide²,

Takata

et al. 2016

Chem. Pharm. Bull.

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“…To better understand the energy input during milling, the discrete element method (DEM) has been used to simulate milling experiments and calculate different parameters such as the impact energy transferred from balls to powder. 26,27 This method has been used for different types of mills, in a simple manner and with or without the addition of feed material.…”

Section: Introductionmentioning

confidence: 99%

Exploring the polymorphism of sofosbuvir via mechanochemistry: effect of milling jar geometry and material

et al. 2022

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“…Caffein 32 Citric Acid Liquid Assisting Grinding Caffeine-citric acid (1:1) and (2:1) cocrystal successfully formed, confirmed by PXRD, infrared spectroscopy, SEM and DSC analysis.…”

Section: Genistein 31mentioning

confidence: 69%

Traditional and Novel Methods for Cocrystal Formation: A Mini Review

Barikah¹

2018

SRP

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Pharmaceutical cocrystal is one of solid-state modification for drug substance, mainly for solubility improvement. Traditionally, cocrystal can be prepared by solvent evaporation method, grinding, and slurry method, but, every method has limitation for certain condition. The current trend for cocrystal formation uses the sophisticated method such as hot-melt extrusion method, spray drying method, supercritical fluid technology and the newest, and laser irradiation method. Development of new method is not only to overcome the limitation of traditional cocrystallization methods but also to generate a simpler step and continuous process for the production of cocrystal product. This article gives a brief explanation of each method that can be used to generate pharmaceutical cocrystals.

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Kinetics of co-crystal formation with caffeine and citric acid via liquid-assisted grinding analyzed using the distinct element method

Cited by 38 publications

References 54 publications

Characterization and Quality Control of Pharmaceutical Cocrystals

Characterization and Quality Control of Pharmaceutical Cocrystals

Exploring the polymorphism of sofosbuvir via mechanochemistry: effect of milling jar geometry and material

Traditional and Novel Methods for Cocrystal Formation: A Mini Review

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