Dissolution and disintegration kinetics of high-active pharmaceutical granules produced at laboratory and manufacturing scale

Smrčka, David; Dohnal, Jiří; Štěpánek, František

doi:10.1016/j.ejpb.2016.04.005

Cited by 19 publications

(16 citation statements)

References 22 publications

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“…Because the deformability of the wet granules was low due to the low liquid content, the porosity of granules become high. 11,24) The high S.D. of individual granules with low L/S can be explained by non-uniform distribution of liquid, indicated by low G value.…”

Section: Comparison Of the Porosity Of Granules Measured By X-ray μCtmentioning

confidence: 99%

“…were low with high L/S due to the high deformability and high pore saturation condition of the wet granules. 11,24) Relationships between Porosity of Granules and Granule Properties Figure 11 illustrates the relationship between porosity of granules (X-ray μCT) and granule strength (friability). Good linear correlation was observed between the porosity of granules measured by X-ray μCT and the friability (R 2 = 0.9107).…”

Section: Comparison Of the Porosity Of Granules Measured By X-ray μCtmentioning

confidence: 99%

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Analysis of Microstructure of Granules Prepared by Continuous Twin Screw Granulator Using X-Ray Micro-computed Tomography

Matsui

Ando

Yamamoto

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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Granules prepared by a continuous twin screw granulator (TSG) were analyzed by X-ray micro-computed tomography (X-ray μCT) and the relationships between porosity of granules and granule properties were investigated. A model formulation containing ibuprofen, lactose monohydrate, microcrystalline cellulose, and hydroxypropyl cellulose was used. The porosity of granules was measured by X-ray μCT and mercury porosimetry. The data sets obtained by both methods showed linear correlation despite different values, which were attributed to the resolution of X-ray μCT and a low-signal-to-noise ratio of the original cross-sectional images. The porosity of granules measured by X-ray μCT decreased from 11-14 to 6-7% as liquid-to-solid ratio (L/S) increased, while the standard deviation (S.D.) of the porosity of individual granules decreased from 4-5 to 2%. L/S affected the porosity of granules. By contrast, the effect of screw speed was not significant. Pressure transmission, G, which indicates the liquid dispersion in wet kneaded masses, increased as the porosity of granules and the S.D. decreased. The cross-sectional images showed that granules were densified as L/S increased. Based on these results, the effect of L/S on the porosity of granules can be explained by liquid dispersion and densification of the wet granules. The porosity of granules measured by X-ray μCT showed good linear correlation with friability and drug dissolution rate (R 2 0.9107 and 0.8834, respectively). This study revealed that the drug dissolution rate was regulated by a disintegration step in which the porosity of granules plays an important role.

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Section: Comparison Of the Porosity Of Granules Measured By X-ray μCtmentioning

confidence: 99%

Section: Comparison Of the Porosity Of Granules Measured By X-ray μCtmentioning

confidence: 99%

Analysis of Microstructure of Granules Prepared by Continuous Twin Screw Granulator Using X-Ray Micro-computed Tomography

Matsui

Ando

Yamamoto

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…The bioavailability of a drug is determined by its dissolution over time. Before dissolution of the drug occurs, the granule and/or tablet must undergo wetting and disintegration (Smrčka et al,2016). Disintegration testing was done by placing 20 mg granules per 4g PBS solution of pH 7.4.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

3D printed elastic mould granulation

et al. 2019

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In the pharmaceutical industry, enhanced process understanding resulting in superior control of product attributes, has the potential to save up to 20 % of process engineering and product development costs during drug development. With the aim of achieving enhanced process understating, a novel approach for granulation of fine powders is presented. First, a mould with the desired particle shape and size is created using 3D printing followed by casting using elastomeric material. The formulation is prepared through wet massing and tested as a thin film on flat elastomeric membranes. The thin film itself can be a product but it also gives a good indication of coating performance before coating the patterned elastic membrane with the formulation i.e., 3D printed elastic mould granulation. Results show that following granulation and drying, granules of controlled size and shape (e.g. cubic and 500 μm), strength, friability and flowability can be formed. The method presented may allow for more robust process development in particle engineering.

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“…On the controversy, very few papers have reported the study of disintegration of porous powders [18,19], especially the mechanism. Researchers tried to define disintegration according to their scenarios.…”

Section: Introductionmentioning

confidence: 99%

Abrupt disintegration of highly porous particles in early stage dissolution

Karampalis

Caragay

et al. 2018

Powder Technology

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show abstract

Dissolution and disintegration kinetics of high-active pharmaceutical granules produced at laboratory and manufacturing scale

Cited by 19 publications

References 22 publications

Analysis of Microstructure of Granules Prepared by Continuous Twin Screw Granulator Using X-Ray Micro-computed Tomography

Analysis of Microstructure of Granules Prepared by Continuous Twin Screw Granulator Using X-Ray Micro-computed Tomography

3D printed elastic mould granulation

Abrupt disintegration of highly porous particles in early stage dissolution

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