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The Influence of High Drug Loading in Xanthan Tablets and Media with Different Physiological pH and Ionic Strength on Swelling and Release.
Mol Pharm. 2016 Mar 07; 13(3):1147-57.MP

Abstract

The formation of a gel coat around xanthan (Xan) tablets, empty or loaded with pentoxifylline (PF), and its release in media differing in pH and ionic strength by NMR, MR imaging, and two release methods were studied. The T1 and T2 NMR relaxation times in gels depend predominantly on Xan concentration; the presence of PF has negligible influence on them. It is interesting that the matrix swelling is primarily regulated by Xan despite high drug loading (25%, 50%). The gastric pH and high ionic strength of the media do not influence the position of the penetration and swelling fronts but do affect the erosion front and gel thickness. The different release profiles obtained in mixing and nonmixing in vitro methods are the consequence of matrix hydration level and erosion at the surface. In water and in diluted acid medium with low ionic strength, the main release mechanism is erosion, whereas in other media (pH 1.2, μ ≥ 0.20 M), anomalous transport dominates as was found out by fitting of measured data with theoretical model. Besides the in vitro investigation that mimics gastric conditions, mathematical modeling makes the product development more successful.

Authors+Show Affiliations

Jožef Stefan Institute, 1000 Ljubljana, Slovenia.Jožef Stefan Institute, 1000 Ljubljana, Slovenia.Faculty of Pharmacy, University of Ljubljana , 1000 Ljubljana, Slovenia.Faculty of Pharmacy, University of Ljubljana , 1000 Ljubljana, Slovenia.

Pub Type(s)

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

Language

eng

PubMed ID

26866780

Citation

Mikac, Urša, et al. "The Influence of High Drug Loading in Xanthan Tablets and Media With Different Physiological pH and Ionic Strength On Swelling and Release." Molecular Pharmaceutics, vol. 13, no. 3, 2016, pp. 1147-57.
Mikac U, Sepe A, Baumgartner S, et al. The Influence of High Drug Loading in Xanthan Tablets and Media with Different Physiological pH and Ionic Strength on Swelling and Release. Mol Pharm. 2016;13(3):1147-57.
Mikac, U., Sepe, A., Baumgartner, S., & Kristl, J. (2016). The Influence of High Drug Loading in Xanthan Tablets and Media with Different Physiological pH and Ionic Strength on Swelling and Release. Molecular Pharmaceutics, 13(3), 1147-57. https://doi.org/10.1021/acs.molpharmaceut.5b00955
Mikac U, et al. The Influence of High Drug Loading in Xanthan Tablets and Media With Different Physiological pH and Ionic Strength On Swelling and Release. Mol Pharm. 2016 Mar 7;13(3):1147-57. PubMed PMID: 26866780.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The Influence of High Drug Loading in Xanthan Tablets and Media with Different Physiological pH and Ionic Strength on Swelling and Release. AU - Mikac,Urša, AU - Sepe,Ana, AU - Baumgartner,Saša, AU - Kristl,Julijana, Y1 - 2016/02/24/ PY - 2016/2/12/entrez PY - 2016/2/13/pubmed PY - 2016/12/15/medline KW - drug release mechanisms KW - gel thickness KW - magnetic resonance imaging KW - mathematical modeling KW - matrix tablets KW - oral drug formulations KW - pH-controlled release SP - 1147 EP - 57 JF - Molecular pharmaceutics JO - Mol Pharm VL - 13 IS - 3 N2 - The formation of a gel coat around xanthan (Xan) tablets, empty or loaded with pentoxifylline (PF), and its release in media differing in pH and ionic strength by NMR, MR imaging, and two release methods were studied. The T1 and T2 NMR relaxation times in gels depend predominantly on Xan concentration; the presence of PF has negligible influence on them. It is interesting that the matrix swelling is primarily regulated by Xan despite high drug loading (25%, 50%). The gastric pH and high ionic strength of the media do not influence the position of the penetration and swelling fronts but do affect the erosion front and gel thickness. The different release profiles obtained in mixing and nonmixing in vitro methods are the consequence of matrix hydration level and erosion at the surface. In water and in diluted acid medium with low ionic strength, the main release mechanism is erosion, whereas in other media (pH 1.2, μ ≥ 0.20 M), anomalous transport dominates as was found out by fitting of measured data with theoretical model. Besides the in vitro investigation that mimics gastric conditions, mathematical modeling makes the product development more successful. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/26866780/The_Influence_of_High_Drug_Loading_in_Xanthan_Tablets_and_Media_with_Different_Physiological_pH_and_Ionic_Strength_on_Swelling_and_Release_ DB - PRIME DP - Unbound Medicine ER -