Applications of synchrotron powder X-ray diffractometry in drug substance and drug product characterization

Munjal, Bhushan; Suryanarayanan, Raj

doi:10.1016/j.trac.2021.116181

Cited by 14 publications

(7 citation statements)

References 56 publications

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“…The crystallinity of substances can be analyzed according to the position and intensity of the diffraction peaks in the PXRD ( Munjal and Suryanarayanan, 2021 ). The BAI profile exhibited obvious characteristic diffraction peaks, and Soluplus had no characteristic diffraction peaks, the same results were also found in the study of Yong and Fan et al ( Fan et al, 2017 ; Yong et al, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

The baicalein amorphous solid dispersion to enhance the dissolution and bioavailability and effects on growth performance, meat quality, antioxidant capacity and intestinal flora in Taihang chickens

Gao,

Fan,

et al. 2024

Poultry Science

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Section: Discussionmentioning

confidence: 99%

The baicalein amorphous solid dispersion to enhance the dissolution and bioavailability and effects on growth performance, meat quality, antioxidant capacity and intestinal flora in Taihang chickens

Gao,

Fan,

et al. 2024

Poultry Science

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“…The utility of conventional XRPD equipment in the characterization of such compounds is often limited by the appearance of numerous overlapping peaks with low intensities, posing challenges with respect to both resolution and sensitivity. The sensitivity is also limited by the low flux of the X-ray source (usually a sealed tub) (Munjal, Suryanarayanan 2021). In parallel, it is already known that thermograms can differ depending on the application of different parameters, for example, heating rates and amount of sample (Dedroog et al, 2020).…”

Section: Thermal Analysismentioning

confidence: 99%

Mechanical, optical, and physicochemical properties of HPMC-based doxazosin mesylate orodispersible films

Silva

Colucci

Silva

et al. 2023

Braz. J. Pharm. Sci.

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In this study, orodispersible films formed from hydroxypropyl methylcellulose (HPMC) E6 (2, 2.5, and 3%) and plasticizers ((glycerin (Gly), propylene glycol (PP), or polyethylene glycol (PEG)), containing doxazosin mesylate, were prepared by the solvent casting method and characterized. Design of experiments (DoE) was used as a statistical tool to facilitate the interpretation of the experimental data and allow the identification of optimal levels of factors for maximum formulation performance. Differential scanning calorimetry (DSC) curves and X-ray powder diffraction (XRPD) diffractograms showed doxazosin mesylate amorphization, probably due to complexation with the polymer (HPMC E6), and the glass transition temperature of the polymer was reduced by adding a plasticizer. Fourier transformed infrared (FTIR) spectroscopy results showed that the chemical structure of doxazosin mesylate was preserved when introduced into the polymer matrix, and the plasticizers, glycerin and PEG, affected the polymer matrix with high intensity. The addition of plasticizers increased the elongation at break and adhesiveness (Gly > PEG > PP), confirming the greater plasticizer effect of Gly observed in DSC and FTIR studies. Greater transparency was observed for the orodispersible films prepared using PP. The addition of citric acid as a pH modifier was fundamental for the release of doxazosin mesylate, and the desirability formulation had a release profile similar to that of the reference product.

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“…The presence of excipients can modulate the kinetics of solid-state reactions. 24 For example, mannitol enhanced the dehydration of theophylline monohydrate, while microcrystalline cellulose (MCC) exerted a minimal effect. 25 Therefore, it was of interest to assess the dehydration behavior of CBZDH in powder blends (meant for direct compression) in the CMT.…”

Section: Introductionmentioning

confidence: 99%

“…Pharmaceutical solid formulations are often multicomponent systems containing excipients to function as diluents, lubricants, binders, etc. The presence of excipients can modulate the kinetics of solid-state reactions . For example, mannitol enhanced the dehydration of theophylline monohydrate, while microcrystalline cellulose (MCC) exerted a minimal effect .…”

Section: Introductionmentioning

confidence: 99%

Drug Phase Transformation and Water Redistribution during Continuous Tablet Manufacturing: A Case Study of Carbamazepine Dihydrate

et al. 2023

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In recent years, continuous tablet manufacturing technology has been used to obtain regulatory approval of several new drug products. While a significant fraction of active pharmaceutical ingredients exists as hydrates (wherein water is incorporated stoichiometrically in the crystal lattice), the impact of processing conditions and formulation composition on the dehydration behavior of hydrates during continuous manufacturing has not been investigated. Using powder X-ray diffractometry, we monitored the dehydration kinetics of carbamazepine dihydrate in formulations containing dibasic calcium phosphate, anhydrous (DCPA), mannitol, or microcrystalline cellulose. The combined effect of nitrogen flow and vigorous mixing during the continuous mixing stage of tablet manufacture facilitated API dehydration. Dehydration was rapid and most pronounced in the presence of DCPA. The dehydration product, amorphous anhydrous carbamazepine, sorbed a significant fraction of the water released by dehydration. Thus, the dehydration process resulted in a redistribution of water in the powder blend. The unintended formation of an amorphous dehydrated phase, which tends to be much more reactive than its crystalline counterparts, is of concern and warrants further investigation.

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Applications of synchrotron powder X-ray diffractometry in drug substance and drug product characterization

Cited by 14 publications

References 56 publications

The baicalein amorphous solid dispersion to enhance the dissolution and bioavailability and effects on growth performance, meat quality, antioxidant capacity and intestinal flora in Taihang chickens

The baicalein amorphous solid dispersion to enhance the dissolution and bioavailability and effects on growth performance, meat quality, antioxidant capacity and intestinal flora in Taihang chickens

Mechanical, optical, and physicochemical properties of HPMC-based doxazosin mesylate orodispersible films

Drug Phase Transformation and Water Redistribution during Continuous Tablet Manufacturing: A Case Study of Carbamazepine Dihydrate

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