An investigation into water interactions with amorphous and milled salbutamol sulphate: The development of predictive models for uptake and recrystallization

Grisedale, Louise C.; Belton, Peter; Jamieson, Matthew J.; Barker, S. A.; Craig, Duncan Q.M.

doi:10.1016/j.ijpharm.2011.10.055

Cited by 10 publications

(8 citation statements)

References 20 publications

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“…The moisture uptake was larger for the amorphous form of the drug. A significant reduction in the crystallization temperature as the moisture content increased is reported (Grisedale et al, 2012). In this work, focus is on the appearance of the melting endotherm at different polymer ratios.…”

Section: Resultsmentioning

confidence: 99%

“…Water in the lyophilized mixture is more likely found in the amorphous part of the drug but its presence can induce crystallization. Such induction occurs due the greater mobility that the water gives to the amorphous form of the drug (Vlassios Andronis and George, 1996, Grisedale et al, 2012). For every SMX:Soluplus® ratio, single detectable T g was missing in lyophilized mixtures, which also indicates less efficient mixing of the two in the lyophilized mixtures.…”

Section: Resultsmentioning

confidence: 99%

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Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Altamimi

Neau

2017

Saudi Pharmaceutical Journal

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Altamimi

Neau

2017

Saudi Pharmaceutical Journal

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“…The importance and nature of the effect of moisture on amorphous materials are especially important when formulating amorphous products. Water can act as a plasticizer which increases molecular mobility and recrystallization rate . The samples were stored at 10% RH for 28 days and at 43 and 75% RH for 7 days.…”

Section: Resultsmentioning

confidence: 99%

“…Water can act as a plasticizer which increases molecular mobility and recrystallization rate. 46 The samples were stored at 10% RH for 28 days and at 43 and 75% RH for 7 days. NIR spectra were used to monitor the samples using PCA analysis.…”

Section: Milling Sulfathiazole With L-tartaric and Citricmentioning

confidence: 99%

Mechanochemical Reaction of Sulfathiazole with Carboxylic Acids: Formation of a Cocrystal, a Salt, and Coamorphous Solids

Gniado

Erxleben

et al. 2014

Crystal Growth & Design

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The anhydrous solvent-free mechanochemical reaction of sulfathiazole, STZ, polymorphs I, III, and V with 10 carboxylic acids was monitored by powder X-ray diffraction (PXRD), attenuated total reflectance infrared (ATR-IR), and near-infrared (NIR) spectroscopy. A 1:1 cocrystal was observed with glutaric acid and the strongest acid, oxalic acid, gave a 1:1 salt. A principal components analysis of the glutaric acid NIR data showed that forms I and V proceeded to the cocrystal, but that form III transformed to form IV before cocrystal formation. The oxalic acid salt was formed via complete amorphization. The crystal structures of the cocrystal and the salt were determined. Sulfathiazole comilled with l-tartaric and citric acids gave coamorphous systems that were stable at 10% RH for up to 28 days. Comilling sulfathiazole with dl-malic acid gave mixtures of form V and the amorphous form.

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“…This may be due to the fact that the dissolution behavior of GF ASDs is limited by the poor recrystallization inhibition of polyvinylpyrrolidone in the solution, 51 and amorphous GF recrystallizes during dissolution because it is hydrated in the dissolution media, 52,53 and water acts as a plasticizing agent, which leads to a concentration-dependent reduction in T g . 54 Recrystallization of amorphous GF leads to low dissolution rates and low final solution concentrations. Overall, the improvement of dissolution behavior with the increase of polymer loading could be ascribed to reduction in the recrystallization rate of GF during dissolution.…”

Section: Effect Of Polymer Loadingmentioning

confidence: 99%

Effect of Particle Size and Polymer Loading on Dissolution Behavior of Amorphous Griseofulvin Powder

Zheng

Lin

Capece

et al. 2019

Journal of Pharmaceutical Sciences

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The effect of particle size on the dissolution behavior of the particles of amorphous solid dispersions (ASDs) of griseofulvin (GF), with 0%-50% Kollidon ® VA 64 as a crystallization inhibitor is investigated. Both the final dissolved GF concentration and the dissolution rate of GF ASDs were found to be inversely proportional to the particle size. The solution concentrations for the smallest (45-75 mm) size group with different polymer loadings were significantly higher than those for the largest (250-355 mm) group regardless of the initial GF amount. Specifically, the dissolution rate of GF ASDs with 50% polymer loading for the finest group was 2.7 times higher than for the largest group under supersaturating conditions. The rates of dissolution and recrystallization were assessed through surface concentration (C s) and Avrami recrystallization rate kinetics, where the solid-state recrystallization was confirmed using Raman spectroscopy. Outcomes indicated that particle size reduction enhanced ASD drug loading by reducing the amount of polymer necessary as finest size ASDs initially dissolve faster, negating their higher recrystallization rate. Kollidon® VA 64 at 30% loading was sufficient to inhibit the GF recrystallization. Overall, the combination of particle size reduction and recrystallization inhibition is effective for improved dissolution behavior of GF ASDs.

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An investigation into water interactions with amorphous and milled salbutamol sulphate: The development of predictive models for uptake and recrystallization

Cited by 10 publications

References 20 publications

Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Mechanochemical Reaction of Sulfathiazole with Carboxylic Acids: Formation of a Cocrystal, a Salt, and Coamorphous Solids

Effect of Particle Size and Polymer Loading on Dissolution Behavior of Amorphous Griseofulvin Powder

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