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Study of critical points of drugs with different solubilities in hydrophilic matrices.
Int J Pharm. 2010 Jan 04; 383(1-2):138-46.IJ

Abstract

Hydrophilic matrices are one of the most popular controlled release systems in the world. It is well known that drug solubility increases the osmotic stress in hydrophilic matrices, resulting in higher swelling through the creation of microcavities and influencing the release rate. Drug solubility also affects the drug release mechanism, favouring the diffusion against the erosion mechanism. Nevertheless it has not been studied whether this can modify the critical points of the hydrophilic matrices. The objective of the present work is to estimate the excipient percolation threshold in HPMC K4M hydrophilic matrices containing acetaminophen, theophiline and ranitidine.HCl, and to study the influence of the drug solubility on the excipient percolation threshold. Dissolution assays were performed using the paddle method. Water uptake was examined using the modified Enslin apparatus. In order to estimate the excipient percolation threshold, the behaviour of the kinetic parameters versus the excipient volume fraction plus initial porosity, was studied. The excipient percolation thresholds were situated between 24.8-25.8, 14.7-18.4 and around 31.2% (v/v) HPMC in theophiline, ranitidine.HCl and acetaminophen matrices, respectively. On the other hand, using these and some previously reported values no relation has been found between drug solubility and excipient percolation threshold in hydrophilic matrices.

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Authors+Show Affiliations

Fuertes I
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain.
Caraballo I
No affiliation info available
Miranda A
No affiliation info available
Millán M
No affiliation info available

MeSH

Chemistry, PharmaceuticalDiffusionPharmaceutical PreparationsSolubility

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

19766706

Citation

Fuertes, Inmaculada, et al. "Study of Critical Points of Drugs With Different Solubilities in Hydrophilic Matrices." International Journal of Pharmaceutics, vol. 383, no. 1-2, 2010, pp. 138-46.
Fuertes I, Caraballo I, Miranda A, et al. Study of critical points of drugs with different solubilities in hydrophilic matrices. Int J Pharm. 2010;383(1-2):138-46.
Fuertes, I., Caraballo, I., Miranda, A., & Millán, M. (2010). Study of critical points of drugs with different solubilities in hydrophilic matrices. International Journal of Pharmaceutics, 383(1-2), 138-46. https://doi.org/10.1016/j.ijpharm.2009.09.019
Fuertes I, et al. Study of Critical Points of Drugs With Different Solubilities in Hydrophilic Matrices. Int J Pharm. 2010 Jan 4;383(1-2):138-46. PubMed PMID: 19766706.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Study of critical points of drugs with different solubilities in hydrophilic matrices. AU - Fuertes,Inmaculada, AU - Caraballo,Isidoro, AU - Miranda,Antonia, AU - Millán,Mónica, Y1 - 2009/09/18/ PY - 2009/05/06/received PY - 2009/09/10/revised PY - 2009/09/11/accepted PY - 2009/9/22/entrez PY - 2009/9/22/pubmed PY - 2010/7/30/medline SP - 138 EP - 46 JF - International journal of pharmaceutics JO - Int J Pharm VL - 383 IS - 1-2 N2 - Hydrophilic matrices are one of the most popular controlled release systems in the world. It is well known that drug solubility increases the osmotic stress in hydrophilic matrices, resulting in higher swelling through the creation of microcavities and influencing the release rate. Drug solubility also affects the drug release mechanism, favouring the diffusion against the erosion mechanism. Nevertheless it has not been studied whether this can modify the critical points of the hydrophilic matrices. The objective of the present work is to estimate the excipient percolation threshold in HPMC K4M hydrophilic matrices containing acetaminophen, theophiline and ranitidine.HCl, and to study the influence of the drug solubility on the excipient percolation threshold. Dissolution assays were performed using the paddle method. Water uptake was examined using the modified Enslin apparatus. In order to estimate the excipient percolation threshold, the behaviour of the kinetic parameters versus the excipient volume fraction plus initial porosity, was studied. The excipient percolation thresholds were situated between 24.8-25.8, 14.7-18.4 and around 31.2% (v/v) HPMC in theophiline, ranitidine.HCl and acetaminophen matrices, respectively. On the other hand, using these and some previously reported values no relation has been found between drug solubility and excipient percolation threshold in hydrophilic matrices. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/19766706/Study_of_critical_points_of_drugs_with_different_solubilities_in_hydrophilic_matrices_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(09)00632-2 DB - PRIME DP - Unbound Medicine ER -