Highly efficient miniaturized coprecipitation screening (MiCoS) for amorphous solid dispersion formulation development

Hu, Qingyan; Choi, Duk Soon; Chokshi, Hitesh; Shah, Navnit; Sandhu, Harpreet

doi:10.1016/j.ijpharm.2013.04.040

Cited by 37 publications

(20 citation statements)

References 17 publications

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“…The temperatures ranged from 2°C to 60°C and the relative humidity varied between 0% and 100%. The duration also varied significantly, with stability studies lasting from 24 h to two years (73,74,81,82,84,86,88,92,93,104,105,109,110,113,115,116,118,120,123,124,126,127,129,130,132,134,135,139,143,146,149,153,158,166,169,172,175,176). While most of the studies did not mention the container used for the physical stability test, a few specified, for example, whether a closed or open container was used (88,92,113,123,132,146).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…Ninety-two of the 101 studies reported solubility and dissolution studies (71–74,77–79,81–92,95,97–107,109–111,113–119,121,123,124,126–133,135–139,141–154,156,157,160,161,166,168–176). The USP in vitro dissolution type II apparatus was the most commonly used instrument (67%), followed by the USP type I apparatus (6%), while the remaining 27% used various other apparatuses, including modified versions of the USP type I only (148) or paired with confocal Raman microscopy (98), USP types I and II apparatus (72), USP type IV (152), closed loop of USP types II and IV (152), a perspex flow cell (73,142), a rotary mixer (131), a Chinese pharmacopoeia type III apparatus (118), an in-house miniaturized USP type II apparatus (175), Sirius T3 apparatus (146), μFLUX dissolution-permeation apparatus (141), Raman UV-Vis flow cell system (99), a centrifuge (88), high throughput screening using a 96-well plate (82,115,157), Wood’s apparatus (99,137), an orbital shaking incubator (156), and another shake-flask method (171) (Fig. 6).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…deionized, degassed, distilled, purified), HCl, and phosphate/acetate buffers at pHs ranging from 1.2 to 7.4 (71–74,77–79,81–88,90–92,95,100–107,109–111,113–119,121,126,127,129–133,135–139,149,150,153,154,156,160,161,166,168–177). Among the 88 studies that reported a dissolution assay, only sixteen (~18%) used a biorelevant dissolution medium (BDM) such as simulated gastrointestinal fluids and simulated saliva (77,79,82,97,121,123,130,135,136,145,152,154,160,169,170,176). These disparities in medium used affect the conclusions, which (as with the stability studies) make head-to-head comparison difficult.…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

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The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

See 1 more Smart Citation

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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“…Note that the co-precipitation route used here also deviated from recent publications [47][48][49][50][51] in that nonionic polymers were used and precipitation was induced using nonaqueous antisolvents, as opposed to ionic polymers and pH modified (depending on the polymer) aqueous antisolvents. Although this work focused on binary API-polymers, nonaqueous antisolvents can also readily allow for the incorporation of surfactants in ternary amorphous dispersions.…”

Section: Introductionmentioning

confidence: 99%

“…45,46 This method has been successfully used to formulate ASDs of poorly soluble drugs from this class. [47][48][49][50][51][52][53] The co-precipitation process relies on the rapid transition of the API and polymer from one solvent environment to another. Both the API and polymer are soluble in the first environment (common solvent), and both are insoluble in the second (common antisolvent).…”

Section: Introductionmentioning

confidence: 99%

Producing Amorphous Solid Dispersions via Co-Precipitation and Spray Drying: Impact to Physicochemical and Biopharmaceutical Properties

Mann¹,

Schenck²,

Koynov³

et al. 2018

Journal of Pharmaceutical Sciences

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Many small-molecule active pharmaceutical ingredients (APIs) exhibit low aqueous solubility and benefit from generation of amorphous dispersions of the API and polymer to improve their dissolution properties. Spray drying and hot-melt extrusion are 2 common methods to produce these dispersions; however, for some systems, these approaches may not be optimal, and it would be beneficial to have an alternative route. Herein, amorphous solid dispersions of compound A, a low-solubility weak acid, and copovidone were made by conventional spray drying and co-precipitation. The physicochemical properties of the 2 materials were assessed via X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis, and scanning electron microscopy. The amorphous dispersions were then formulated and tableted, and the performance was assessed in vivo and in vitro. In human dissolution studies, the co-precipitation tablets had slightly slower dissolution than the spray-dried dispersion, but both reached full release of compound A. In canine in vitro dissolution studies, the tablets showed comparable dissolution profiles. Finally, canine pharmacokinetic studies showed that the materials had comparable values for the area under the curve, bioavailability, and C. Based on the summarized data, we conclude that for some APIs, co-precipitation is a viable alternative to spray drying to make solid amorphous dispersions while maintaining desirable physicochemical and biopharmaceutical characteristics.

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Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

Hall

Chambers

Musa

et al. 2021

Handbook of Pyrrolidone and Caprolactam Based Materials

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The strongly interacting lactam functional group in both γand ε-lactams makes them of considerable interest in the formation of multicomponent solids including a hugely diverse range of cocrystals, coordination complexes with lactam ligands and coamorphous phases. Cocrystals are structurally homogenous crystalline substances that are comprised of two or more chemically different neutral molecules generally in stoichiometric amounts that are connected by non-ionic and non-covalent interactions [1]. The Food and Drug Administration (FDA) classifies cocrystals as crystalline materials composed of two or more different molecules, typically Active Pharmaceutical Ingredients (API) and approved, non-toxic cocrystal former (coformer), in the same crystal lattice [2].Cocrystals fall under the umbrella of multi-component molecular solids, which encompasses crystalline forms such as solvates, hydrates, and lattice inclusion compounds as well as coamorphous materials. The relationships between these various solid forms are illustrated in Figure 1. Also included under multi-component crystalline solids are solid solutions in which one component is randomly distributed in a crystal of another [4]. Salts are also multi-component molecular solids, with the main difference between a salt and a cocrystal often being proton transfer from an acid to a base that occurs to give a salt in contrast to neutral molecule cocrystals. However, the distinction is a fine one since, depending on the temperature, salts and cocrystals can interconvert [5]. Generally, true cocrystals are regarded as being formed from components that are solids at room temperature, a definition which excludes solvates and hydrates. However, this narrowing would mean that some materials involving low melting solids might be regarded as cocrystals in some labs and not others despite that fact that there is no fundamental structural difference between a cocrystal and a solvate [1,6,7].

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Highly efficient miniaturized coprecipitation screening (MiCoS) for amorphous solid dispersion formulation development

Cited by 37 publications

References 17 publications

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Producing Amorphous Solid Dispersions via Co-Precipitation and Spray Drying: Impact to Physicochemical and Biopharmaceutical Properties

Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

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