Effect of Spray Drying on Amorphization of Indomethacin Nicotinamide Cocrystals; Optimization, Characterization, and Stability Study

Tawfeek, Hesham M.; Chavan, Tejashri; Kunda, Nitesh K.

doi:10.1208/s12249-020-01732-x

Cited by 14 publications

(11 citation statements)

References 66 publications

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“…Apart from the above-mentioned co-former classes, other types of small molecules have been applied in the preparation of CAMS, for example urea [ 41 , 44 , 45 ] and nicotinamide [ 41 , 43 , 45 , 46 , 47 , 48 , 49 ]. These CAMS contribute 17.5% of the total.…”

Section: Classes Of Investigated Camsmentioning

confidence: 99%

“…Whilst this review will focus on the physical stability of CAMS, the chemical stability can be of interest, especially when using ball milling, which has been shown to be able to induce degradation. The reader is referred to several studies, which have investigated the chemical stability (either after preparation or after storage) [ 18 , 20 , 21 , 33 , 34 , 47 , 87 , 98 , 102 , 120 , 121 , 122 , 123 , 124 , 125 , 126 ].…”

Section: Physical Stability Of Investigated 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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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: Classes Of Investigated Camsmentioning

confidence: 99%

Section: Physical Stability Of Investigated Camsmentioning

confidence: 99%

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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“…As shown in Figure 6(C,D), it appears that NIF, despite the grinding, continued to present an important non-hygroscopic behavior. (Tawfeek et al 2020). Unlike milled NIF, any impact was observed on solubilization process as a function of the processes used and its different parameters.…”

Section: Dynamic Vapor Sorptionmentioning

confidence: 91%

Comparison study of physicochemical and biopharmaceutics properties of hydrophobic drugs ground by two dry milling processes

Dandignac

Lacerda

Chamayou

et al. 2022

Pharmaceutical Development and Technology

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This study focuses on the dry milling of biopharmaceutical classification system (BCS) class II molecules. These molecules have a limited bioavailability because of their low aqueous solubility, poor water wettability and low dissolution rate. In order to improve these properties, indomethacin (IND) and niflumic acid (NIF) were milled using two different types of equipment: Pulverisette 0 V R and CryoMill V R . Milled samples were characterized and compared to commercial molecules. IND shows a modified solid state, like surface crystallinity reduction and an increase in water vapor adsorption from to 2-up to 5-fold due to milling processes. The obtained solubility data resulted in an improvement in solubility up to 1.2-fold and an increase in initial dissolution kinetics: 2% of dissolved drug for original crystals against 25% for milled samples. For NIF no crystallinity reduction, no change of surface properties and no solubility improvement after milling were noticed. In addition, milled particles seemed more agglomerated resulting in no changes in dissolution rate compared to the original drug. IND solubility and dissolution enhancement can be attributed to the modification of surface area, drug crystallinity reduction, and water sorption increase due to specific behavior related to the drug crystal disorder induced by milling process.

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“…14,15 The crystal structure of these compounds can be tuned with the processing temperature, initial solute concentration, solvent evaporation rate, and solvent quality. 16–18 To increase the bioavailability of many of these actives, they are often co-spray dried with low molecular weight additives such as succinic acid 19 Indeed, many active ingredients including carbamazepine, 19,20 nicotinamide 20,21 and salbutamol sulfate 22,23 are co-spray dried with some excipients such as lactose 22,24 and mannitol. 25–28 Unfortunately, it becomes much more difficult to control the crystal structure and hence properties of active ingredients if they are co-spray-dried with excipients.…”

Section: Introductionmentioning

confidence: 99%

Controlling the crystal structure of succinic acid via microfluidic spray-drying

et al. 2023

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Effect of Spray Drying on Amorphization of Indomethacin Nicotinamide Cocrystals; Optimization, Characterization, and Stability Study

Cited by 14 publications

References 66 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

Comparison study of physicochemical and biopharmaceutics properties of hydrophobic drugs ground by two dry milling processes

Controlling the crystal structure of succinic acid via microfluidic spray-drying

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