Impact of polymeric excipient on cocrystal formation via hot-melt extrusion and subsequent downstream processing

Karimi-Jafari, Maryam; Ziaee, Ahmad; Iqbal, Javed; Croker, Denise M.; Walker, Gavin

doi:10.1016/j.ijpharm.2019.06.031

Cited by 23 publications

(19 citation statements)

References 43 publications

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“…Interestingly, by incorporating 5% Soluplus within the process, the extrusion process no longer exceeds the maximum torque limit and can now successfully process the co-crystals. The presence of Soluplus improved processability and facilitated the interaction between ARP and ADP to form co-crystals; as mention previously, Soluplus has successfully been used as a polymeric excipient for other co-crystals formation (82,94). The study again proves that extrusion temperature is critical for the successful formation of co-crystals.…”

Section: Recent Innovation Formulations Via Hot-melt Extrusionsupporting

confidence: 64%

“…It was shown that the presence of soluplus decreased the co-crystallization temperature as its presence enhances the interaction between the API and co-former. The study also proved that the mechanical and tabletting properties (tabletability, compactibility, and compressibility) were significantly improved with the presence of soluplus when being compared to purely ibuprofen-nicotinamide co-crystals only (94).…”

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 72%

“…Karimi-Jafari et al have also verified the advantageous effect of the presence of excipients in the co-crystal sample (94). Cocrystals of ibuprofen-nicotinamide were prepared using HME, and soluplus was added as the polymeric excipient.…”

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 93%

“…It was reported that processing above the eutectic point is required for the formation of co-crystals (92). Other reports showed that the screw design, temperature, feed rate, and screw speeds are the primary factors affecting the conversion of co-crystals (85,93,94). However, the barrel temperature in HME is still the most influential factor for co-crystal formation in the process (85,95,96).…”

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 99%

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Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

Tan

Davis

Miller³

et al. 2020

AAPS PharmSciTech

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Thermal processing has gained much interest in the pharmaceutical industry, particularly for the enhancement of solubility, bioavailability, and dissolution of active pharmaceutical ingredients (APIs) with poor aqueous solubility. Formulation scientists have developed various techniques which may include physical and chemical modifications to achieve solubility enhancement. One of the most commonly used methods for solubility enhancement is through the use of amorphous solid dispersions (ASDs). Examples of commercialized ASDs include Kaletra®, Kalydeco®, and Onmel®. Various technologies produce ASDs; some of the approaches, such as spray-drying, solvent evaporation, and lyophilization, involve the use of solvents, whereas thermal approaches often do not require solvents. Processes that do not require solvents are usually preferred, as some solvents may induce toxicity due to residual solvents and are often considered to be damaging to the environment. The purpose of this review is to provide an update on recent innovations reported for using hot-melt extrusion and KinetiSol® Dispersing technologies to formulate poorly water-soluble APIs in amorphous solid dispersions. We will address development challenges for poorly water-soluble APIs and how these two processes meet these challenges.

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Section: Recent Innovation Formulations Via Hot-melt Extrusionsupporting

confidence: 64%

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 72%

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 93%

Section: Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 99%

See 2 more Smart Citations

Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

Tan

Davis

Miller³

et al. 2020

AAPS PharmSciTech

View full text Add to dashboard Cite

show abstract

“…The combination of cocrystallisation and blending with excipients in a one-step process which would reduce the number of required unit operations is rarely reported. [27][28][29][30] Figure 1. Chemical structures of ctz and the coformers used in this study.…”

Section: Introductionmentioning

confidence: 99%

Influence of Excipients on Cocrystal Stability and Formation

Aljohani

McArdle

Erxleben

2020

Crystal Growth & Design

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Cocrystal formation is widely used to modify and optimise the physicochemical properties of an active pharmaceutical ingredient (API). However, the stability of cocrystals towards formulation with excipients is little investigated. In this work the effect of grinding in the presence of the common excipients polyvinylpyrrolidone (PVP) and microcrystalline cellulose (MCC) on 11 cocrystals and a salt of the sulfonamide diuretic chlorothiazide (ctz) was studied (ctz-bipy, ctzebipy, ctz-pbipy, ctz-pyr, ctz-hyp, ctz-hma, ctz-bza, ctz-nia, ctz-ina, ctz-cbz, ctz-aca, ctz-ppa, (bzamH + )(ctz -); bipy = 4,4'-bipyridine, ebipy = 1,2-di(4-pyridyl)ethylene, pbipy = 1,3-di(4pyridyl)propane, pyr = pyrazine, hyp = 2-hydroxypyridine, hma = hexamethylenetetramine, bza = benzamide, nia = nicotinamide, ina = isonicotinamide, cbz = carbamazepine, aca = acetamide, ppa = propionamide, bzamH + = benzamidinium). Except for ctz-ppa and ctz-aca, all cocrystals were stable towards milling with one weight equivalent PVP or MCC. It was also shown that the cocrystals ctz-bipy, ctz-ebipy, ctz-pbipy, ctz-pyr, ctz-hma, ctz-bza, ctz-ina, ctz-cbz and the salt (bzamH + )(ctz -) formed in situ, when ctz was milled with the respective coformer in the presence of PVP or MCC. The stability and formation of ctz-cbz, ctz-nia and htz-nia (htz = hydrochlorothiazide) towards grinding with a wider range of excipients (HPC, -lactose, deoxycholic acid and sodium taurocholate) was also investigated and the results are discussed with regard to the heterosynthons of the ctz cocrystals and competing H bonding with the excipients.

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Scalability of Pharmaceutical Co‐Crystal Formation by Mechanochemistry in Batch

Bodach,

Portet,

Winkelmann

et al. 2023

ChemSusChem

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The development of mechanochemistry is considerably growing. Benign by design, this technology complies with several principles of green chemistry, contributing to the achievement of the United Nations Sustainable Development Goals (UN SDGs) and the European Green Deal objectives. Herein, we report the use of mechanochemical processes in batch to prepare kilogram‐scale of the Active Pharmaceutical Ingredient (API): Ibuprofen‐Nicotinamide (rac‐IBP:NCT) co‐crystal in an industrial eccentric vibration mill. This scenario shows a sustainable approach to the industrial up‐scaling of pharmaceutical co‐crystals by a solvent‐free mechanochemical process in batch. The quantitative assessment of the greenness of the mechanochemical process against the Twelve Principles of Green Chemistry was performed using the DOZN 2.0 Green Chemistry Evaluator.

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Impact of polymeric excipient on cocrystal formation via hot-melt extrusion and subsequent downstream processing

Cited by 23 publications

References 43 publications

Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

Influence of Excipients on Cocrystal Stability and Formation

Scalability of Pharmaceutical Co‐Crystal Formation by Mechanochemistry in Batch

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