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Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging--effect of solubility of additives on HPMC matrix tablets.
Eur J Pharm Sci. 2009 May 12; 37(2):89-97.EJ

Abstract

Extensive studies of extended release tablets based on hydrophilic polymers have illuminated several aspects linked to their functionality. However, in some respects key factors affecting the mechanisms of release are yet unexplored. In the present study, a novel NMR-microimaging method has been used to study the influence of the solubility of additives in extended release hydroxypropyl methylcellulose (HPMC) matrix tablets. During the course of the tablet dissolution the movement of the swelling and erosion fronts were studied simultaneously to the release of both polymer and additives. Moreover, the focused beam reflectance measurement (FBRM) technology was for the first time assessed for both release and dissolution rate studies of poorly soluble particles. The studied formulations comprised solely HPMC, 40% HPMC and 60% mannitol (Cs=240 mg/ml) and 40% HPMC and 60% dicalcium phosphate (DCP) (Cs=0.05 mg/ml). The dissolution rate of the tablets was highest for the HPMC/mannitol formulation, followed by HPMC/DCP and plain HPMC tablet. A contrasting order was found regarding the degree and kinetics of swelling. The results were interpreted in light of how the mass transport in the gel layer is influenced by the solubility of additives. A mechanistic model, considering osmotic pressure gradient and the effective diffusion of the dissolution medium in the gel is proposed.

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Authors+Show Affiliations

Tajarobi F
AstraZeneca R&D, SE-431 83 Mölndal, Sweden. farhad@chalmers.se
Abrahmsén-Alami S
No affiliation info available
Carlsson AS
No affiliation info available
Larsson A
No affiliation info available

MeSH

Hypromellose DerivativesMagnetic Resonance SpectroscopyMannitolMethylcelluloseParticle SizeSolubilityTablets

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19429415

Citation

Tajarobi, Farhad, et al. "Simultaneous Probing of Swelling, Erosion and Dissolution By NMR-microimaging--effect of Solubility of Additives On HPMC Matrix Tablets." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 37, no. 2, 2009, pp. 89-97.
Tajarobi F, Abrahmsén-Alami S, Carlsson AS, et al. Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging--effect of solubility of additives on HPMC matrix tablets. Eur J Pharm Sci. 2009;37(2):89-97.
Tajarobi, F., Abrahmsén-Alami, S., Carlsson, A. S., & Larsson, A. (2009). Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging--effect of solubility of additives on HPMC matrix tablets. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 37(2), 89-97. https://doi.org/10.1016/j.ejps.2009.01.008
Tajarobi F, et al. Simultaneous Probing of Swelling, Erosion and Dissolution By NMR-microimaging--effect of Solubility of Additives On HPMC Matrix Tablets. Eur J Pharm Sci. 2009 May 12;37(2):89-97. PubMed PMID: 19429415.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging--effect of solubility of additives on HPMC matrix tablets. AU - Tajarobi,Farhad, AU - Abrahmsén-Alami,Susanna, AU - Carlsson,Anders S, AU - Larsson,Anette, Y1 - 2009/01/31/ PY - 2008/10/31/received PY - 2009/01/09/revised PY - 2009/01/13/accepted PY - 2009/5/12/entrez PY - 2009/5/12/pubmed PY - 2009/7/25/medline SP - 89 EP - 97 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 37 IS - 2 N2 - Extensive studies of extended release tablets based on hydrophilic polymers have illuminated several aspects linked to their functionality. However, in some respects key factors affecting the mechanisms of release are yet unexplored. In the present study, a novel NMR-microimaging method has been used to study the influence of the solubility of additives in extended release hydroxypropyl methylcellulose (HPMC) matrix tablets. During the course of the tablet dissolution the movement of the swelling and erosion fronts were studied simultaneously to the release of both polymer and additives. Moreover, the focused beam reflectance measurement (FBRM) technology was for the first time assessed for both release and dissolution rate studies of poorly soluble particles. The studied formulations comprised solely HPMC, 40% HPMC and 60% mannitol (Cs=240 mg/ml) and 40% HPMC and 60% dicalcium phosphate (DCP) (Cs=0.05 mg/ml). The dissolution rate of the tablets was highest for the HPMC/mannitol formulation, followed by HPMC/DCP and plain HPMC tablet. A contrasting order was found regarding the degree and kinetics of swelling. The results were interpreted in light of how the mass transport in the gel layer is influenced by the solubility of additives. A mechanistic model, considering osmotic pressure gradient and the effective diffusion of the dissolution medium in the gel is proposed. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/19429415/Simultaneous_probing_of_swelling_erosion_and_dissolution_by_NMR_microimaging__effect_of_solubility_of_additives_on_HPMC_matrix_tablets_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(09)00010-4 DB - PRIME DP - Unbound Medicine ER -