High-shear granulation as a manufacturing method for cocrystal granules

Rehder, Sönke; Christensen, Niels Peter Aae; Rantanen, Jukka; Rades, Thomas; Leopold, Claudia

doi:10.1016/j.ejpb.2013.04.022

Cited by 32 publications

(17 citation statements)

References 54 publications

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“…The diffraction pattern of the API and cocrystals showed that both were crystalline in nature as demonstrated by numerous distinct peaks of 2θ. Powder XRD pattern of lornoxicam cocrystals indicates formation of new crystalline phases, which can be attributed to cocrystal formation [39,40] .…”

Section: Resultsmentioning

confidence: 99%

Solubility Enhancement of Lornoxicam by Crystal Engineering

Gadade¹,

Kulkarni²,

Rathi³

et al. 2017

Journal of Pharmaceutical Sciences

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Gadade, et al.: Crystal Engineering of LornoxicamAn attempt was made to improve the solubility and physicochemical properties of the poorly soluble lornoxicam by crystal engineering with different coformers. Nineteen different coformers were screened during this study. Cocrystals were prepared by neat grinding method. The prepared cocrystals were evaluated for solubility, powder characteristics, assay and in vitro dissolution study. The solid state property was characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction analysis and Raman spectroscopy. Maximum solubility and dissolution rate were observed with cocrystal prepared using saccharin sodium. Cocrystallization leads to increased solubility and improved in vitro dissolution of lornoxicam.

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Section: Resultsmentioning

confidence: 99%

Solubility Enhancement of Lornoxicam by Crystal Engineering

Gadade¹,

Kulkarni²,

Rathi³

et al. 2017

Journal of Pharmaceutical Sciences

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“…HSG can also be considered a suitable method for the formation of cocrystal components on the batch scale. Granules formation is quite dependent upon the impeller speed, excipient used, and time of exposure of the granules ( Rehder et al, 2013 ). Proper selection of a liquid media for the granulate in order to get the desired product is absolutely necessary.…”

Section: Cocrystallization Techniquesmentioning

confidence: 99%

Recent Advances in Pharmaceutical Cocrystals: From Bench to Market

Bandaru¹,

Rout²,

Kenguva³

et al. 2021

Front. Pharmacol.

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The pharmacokinetics profile of active pharmaceutical ingredients (APIs) in the solid pharmaceutical dosage forms is largely dependent on the solid-state characteristics of the chemicals to understand the physicochemical properties by particle size, size distribution, surface area, solubility, stability, porosity, thermal properties, etc. The formation of salts, solvates, and polymorphs are the conventional strategies for altering the solid characteristics of pharmaceutical compounds, but they have their own limitations. Cocrystallization approach was established as an alternative method for tuning the solubility, permeability, and processability of APIs by introducing another compatible molecule/s into the crystal structure without affecting its therapeutic efficacy to successfully develop the formulation with the desired pharmacokinetic profile. In the present review, we have grossly focused on cocrystallization, particularly at different stages of development, from design to production. Furthermore, we have also discussed regulatory guidelines for pharmaceutical industries and challenges associated with the design, development and production of pharmaceutical cocrystals with commercially available cocrystal-based products.

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“…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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High-shear granulation as a manufacturing method for cocrystal granules

Cited by 32 publications

References 54 publications

Solubility Enhancement of Lornoxicam by Crystal Engineering

Solubility Enhancement of Lornoxicam by Crystal Engineering

Recent Advances in Pharmaceutical Cocrystals: From Bench to Market

Characterization and Quality Control of Pharmaceutical Cocrystals

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