Enteric polymers as acidifiers for the pH-independent sustained delivery of a weakly basic drug salt from coated pellets

Körber, Martin; Ciper, Mesut; Hoffart, Valérie; Pearnchob, Nantharat; Walther, Mathias; MacRae, Ross J.; Bodmeier, Roland

doi:10.1016/j.ejpb.2011.03.018

Cited by 11 publications

(2 citation statements)

References 18 publications

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“…A variety of polymers and manufacturing processes are used to alter and control drug release from coated pellets [ 22 , 23 , 24 , 25 , 26 , 27 ]. The chemical composition of the polymeric membrane, its thickness and inner structure, but also the type of core material can have a major impact on the relative importance of the involved physico-chemical phenomena [ 19 , 28 , 29 ].…”

Section: Introductionmentioning

confidence: 99%

Towards a Better Understanding of Verapamil Release from Kollicoat SR:IR Coated Pellets Using Non-Invasive Analytical Tools

et al. 2021

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The aim of this study was to gain deeper insight into the mass transport mechanisms controlling drug release from polymer-coated pellets using non-invasive analytical tools. Pellet starter cores loaded with verapamil HCl (10% loading, 45% lactose, 45% microcrystalline cellulose) were prepared by extrusion/spheronization and coated with 5% Kollicoat SR:IR 95:5 or 10% Kollicoat SR:IR 90:10. Drug release was measured from ensembles of pellets as well as from single pellets upon exposure to acetate buffer pH = 3.5 and phosphate buffer pH = 7.4. The swelling of single pellets was observed by optical microscopy, while dynamic changes in the pH in the pellet cores were monitored by fluorescence spectroscopy. Also, mathematical modeling using a mechanistically realistic theory as well as SEM and Raman imaging were applied to elucidate whether drug release mainly occurs by diffusion through the intact film coatings or whether crack formation in the film coatings plays a role. Interestingly, fluorescence spectroscopy revealed that the pH within the pellet cores substantially differed upon exposure to acetate buffer pH = 3.5 and phosphate buffer pH = 7.4, resulting in significant differences in drug solubility (verapamil being a weak base) and faster drug release at lower pH: from ensembles of pellets and single pellets. The monitoring of drug release from and the swelling of single pellets indicated that crack formation in the film coatings likely plays a major role, irrespective of the Kollicoat SR:IR ratio/coating level. This was confirmed by mathematical modeling, SEM and Raman imaging. Importantly, the latter technique allowed also for non-invasive measurements, reducing the risk of artifact creation associated with sample cutting with a scalpel.

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Section: Introductionmentioning

confidence: 99%

Towards a Better Understanding of Verapamil Release from Kollicoat SR:IR Coated Pellets Using Non-Invasive Analytical Tools

et al. 2021

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“…[8][9][10] However, few reports on the dissolution, absorption and taste of free acids or bases and salt forms are available. 11,12) In this study, P-4 was used as a model drug. Fine granules were prepared to decrease its intense bitterness, while the dissolution and absorption were equivalent with those of the marketed P-4 tablet (BUP-4 ® ).…”

Section: -3)mentioning

confidence: 99%

Taste Masking of Propiverine Hydrochloride by Conversion to Its Free Base

Ogata

Koide

Kinoshita

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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The aim of the present study was to mask the bitterness of propiverine hydrochloride (P-4) by converting it to propiverine free base. Fine granules comprising the free base, which was converted from P-4 by desalination, were prepared. By using Fourier transform infrared spectroscopy, thermogravimetry-differential thermal analysis, and powder X-ray diffraction spectra, we confirmed that P-4 had been converted into propiverine free base by desalination during the manufacturing process. Furthermore, the conversion into free base appeared to result in decreased solubility, and both the taste testing sensor and tasting volunteers determined that it masked the bitterness of P-4. On using the gustatory sensation test, the bitterness of the P-4 fine granules was confirmed to be weakened. The dissolution rate and bioavailability of fine granules of the free base were compared with tablets of P-4. The dissolution rate and bioavailability of the fine granules and tablets were almost the same. We successfully masked the taste of P-4 by converting it into free base using a manufacturing process that was suitable for commercial manufacturing.

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Novel method for screening of enteric film coatings properties with magnetic resonance imaging

Dorożyński¹,

Jamróz²,

Niwiński³

et al. 2013

International Journal of Pharmaceutics

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Enteric polymers as acidifiers for the pH-independent sustained delivery of a weakly basic drug salt from coated pellets

Cited by 11 publications

References 18 publications

Towards a Better Understanding of Verapamil Release from Kollicoat SR:IR Coated Pellets Using Non-Invasive Analytical Tools

Towards a Better Understanding of Verapamil Release from Kollicoat SR:IR Coated Pellets Using Non-Invasive Analytical Tools

Taste Masking of Propiverine Hydrochloride by Conversion to Its Free Base

Novel method for screening of enteric film coatings properties with magnetic resonance imaging

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