Preparation of Co-Amorphous Systems by Freeze-Drying

Wostry, Melvin; Plappert, Hanna; Grohganz, Holger

doi:10.3390/pharmaceutics12100941

Cited by 17 publications

(13 citation statements)

References 26 publications

(29 reference statements)

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“…Considerations of bioactivity, structural characteristics of drug and co-former, and physicochemical properties of co-formers on the one hand and consideration of combination therapy on the other hand accounted for 18.1% and 6.8%, respectively. However, a systematic co-former screening was only performed in 21.8% of the reported studies [ 29 , 36 , 41 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 ]. Therefore, systematic, predictive, and computational screening methods for co-former selections are still largely unexplored (see also a review: [ 27 ]).…”

Section: Co-former Selection Of Investigated Camsmentioning

confidence: 99%

“…Different co-formulated surfactants were investigated with naproxen–arginine and naproxen–lysine CAMS prepared by freeze-drying [ 57 ]. The results indicated that the formulation and the CQA of the CAMS were affected by the type of surfactant.…”

Section: Preparation Of Ternary Camsmentioning

confidence: 99%

“…To investigate the influence of the surfactant types Formation of a heterogeneous system; Improvement of sample physical stability [57] Naproxen-Meglumine Kollidon VA64 Polymer Reactive melt extrusion…”

Section: Acyclovirmentioning

confidence: 99%

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Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Grohganz

Hempel

2021

Pharmaceutics

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Co-amorphous drug delivery systems (CAMS) are characterized by the combination of two or more (initially crystalline) low molecular weight components that form a homogeneous single-phase amorphous system. Over the past decades, CAMS have been widely investigated as a promising approach to address the challenge of low water solubility of many active pharmaceutical ingredients. Most of the studies on CAMS were performed on a case-by-case basis, and only a few systematic studies are available. A quantitative analysis of the literature on CAMS under certain aspects highlights not only which aspects have been of great interest, but also which future developments are necessary to expand this research field. This review provides a comprehensive updated overview on the current published work on CAMS using a quantitative approach, focusing on three critical quality attributes of CAMS, i.e., co-formability, physical stability, and dissolution performance. Specifically, co-formability, molar ratio of drug and co-former, preparation methods, physical stability, and in vitro and in vivo performance were covered. For each aspect, a quantitative assessment on the current status was performed, allowing both recent advances and remaining research gaps to be identified. Furthermore, novel research aspects such as the design of ternary CAMS are discussed.

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Section: Co-former Selection Of Investigated Camsmentioning

confidence: 99%

Section: Preparation Of Ternary Camsmentioning

confidence: 99%

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Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Grohganz

Hempel

2021

Pharmaceutics

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“…In addition, many polymeric carriers are hygroscopic, which can lead to API recrystallisation while in some cases polymers can be unsuccessful in maintaining a good stability profile [123]. The applications and limitations of PASDs have been highlighted in a number of reviews [124][125][126]. PASDs incorporate low API loading within a compatible polymer to maintain the solubility advantage of amorphous systems through the formation of strong intermolecular attractions [120].…”

Section: The Design Of Carrier Free Formulations Using Coamorphous Solid Dispersions (Cacds)mentioning

confidence: 99%

Section: The Design Of Carrier Free Formulations Using Coamorphous Solid Dispersions (Cacds)mentioning

confidence: 99%

Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions

et al. 2021

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It is well established that currently available inhaled drug formulations are associated with extremely low lung deposition. Currently available technologies alleviate this low deposition problem via mixing the drug with inert larger particles, such as lactose monohydrate. Those inert particles are retained in the inhalation device or impacted in the throat and swallowed, allowing the smaller drug particles to continue their journey towards the lungs. While this seems like a practical approach, in some formulations, the ratio between the carrier to drug particles can be as much as 30 to 1. This limitation becomes more critical when treating lung conditions that inherently require large doses of the drug, such as antibiotics and antivirals that treat lung infections and anticancer drugs. The focus of this review article is to review the recent advancements in carrier free technologies that are based on coamorphous solid dispersions and cocrystals that can improve flow properties, and help with delivering larger doses of the drug to the lungs.

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Production of the Amorphous Form of Ibrutinib and Study of its Physicochemical Properties

Золотов¹,

Sazonov²,

Dain³

et al. 2023

Pharm Chem J

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Preparation of Co-Amorphous Systems by Freeze-Drying

Cited by 17 publications

References 26 publications

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions

Production of the Amorphous Form of Ibrutinib and Study of its Physicochemical Properties

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