Tags

Type your tag names separated by a space and hit enter

A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery.
Int J Pharm. 2006 Feb 03; 308(1-2):52-60.IJ

Abstract

The aim of this study was to investigate the in vitro dissolution characteristics of pH-responsive polymers in a variety of simulated fluids. Prednisolone tablets were fabricated and coated with the following polymer systems: Eudragit S (organic solution), Eudragit S (aqueous dispersion), Eudragit FS (aqueous dispersion) and Eudragit P4135 (organic solution). Dissolution tests were conducted using a pH change method whereby tablets were transferred from acid to buffer. Three different buffer media were investigated: two compendial phosphate buffers (pH range 6.8-7.4) and a physiological buffer solution (Hanks buffer) with very similar ionic composition to intestinal fluid (pH 7.4). There was considerable drug release from tablets coated with Eudragit P4135 in acid, prompting discontinuation of further investigations of this polymer. Eudragit S (organic solution), Eudragit S (aqueous dispersion) and Eudragit FS on the other hand prevented drug release in acid, though subsequent drug release in the buffer media was found to be influenced by the duration of tablet exposure to acid. At pH 7.4 drug release rate from the polymer coated tablets was similar in the two compendial media, however in the physiological buffer, they were found to differ in the following order: Eudragit S (aqueous dispersion)>Eudragit FS>Eudragit S (organic solution). The results indicate that the tablets coated with the newer Eudragit FS polymer would be more appropriate for drug delivery to the ileo-colonic region in comparison to the more established Eudragit S. More importantly, however, dissolution in the physiological buffer was found to be markedly slower for all the coated tablets than in the two compendial buffers, a result akin to reported slower dissolution of enteric coated tablets in vivo. There is therefore the need to adequately simulate the ionic composition of the intestinal fluid in the dissolution media.

Authors+Show Affiliations

Department of Pharmaceutics, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

16356670

Citation

Ibekwe, Valentine C., et al. "A Comparative in Vitro Assessment of the Drug Release Performance of pH-responsive Polymers for Ileo-colonic Delivery." International Journal of Pharmaceutics, vol. 308, no. 1-2, 2006, pp. 52-60.
Ibekwe VC, Fadda HM, Parsons GE, et al. A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery. Int J Pharm. 2006;308(1-2):52-60.
Ibekwe, V. C., Fadda, H. M., Parsons, G. E., & Basit, A. W. (2006). A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery. International Journal of Pharmaceutics, 308(1-2), 52-60.
Ibekwe VC, et al. A Comparative in Vitro Assessment of the Drug Release Performance of pH-responsive Polymers for Ileo-colonic Delivery. Int J Pharm. 2006 Feb 3;308(1-2):52-60. PubMed PMID: 16356670.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery. AU - Ibekwe,Valentine C, AU - Fadda,Hala M, AU - Parsons,Gary E, AU - Basit,Abdul W, Y1 - 2005/12/13/ PY - 2005/04/10/received PY - 2005/10/17/revised PY - 2005/10/18/accepted PY - 2005/12/17/pubmed PY - 2006/4/21/medline PY - 2005/12/17/entrez SP - 52 EP - 60 JF - International journal of pharmaceutics JO - Int J Pharm VL - 308 IS - 1-2 N2 - The aim of this study was to investigate the in vitro dissolution characteristics of pH-responsive polymers in a variety of simulated fluids. Prednisolone tablets were fabricated and coated with the following polymer systems: Eudragit S (organic solution), Eudragit S (aqueous dispersion), Eudragit FS (aqueous dispersion) and Eudragit P4135 (organic solution). Dissolution tests were conducted using a pH change method whereby tablets were transferred from acid to buffer. Three different buffer media were investigated: two compendial phosphate buffers (pH range 6.8-7.4) and a physiological buffer solution (Hanks buffer) with very similar ionic composition to intestinal fluid (pH 7.4). There was considerable drug release from tablets coated with Eudragit P4135 in acid, prompting discontinuation of further investigations of this polymer. Eudragit S (organic solution), Eudragit S (aqueous dispersion) and Eudragit FS on the other hand prevented drug release in acid, though subsequent drug release in the buffer media was found to be influenced by the duration of tablet exposure to acid. At pH 7.4 drug release rate from the polymer coated tablets was similar in the two compendial media, however in the physiological buffer, they were found to differ in the following order: Eudragit S (aqueous dispersion)>Eudragit FS>Eudragit S (organic solution). The results indicate that the tablets coated with the newer Eudragit FS polymer would be more appropriate for drug delivery to the ileo-colonic region in comparison to the more established Eudragit S. More importantly, however, dissolution in the physiological buffer was found to be markedly slower for all the coated tablets than in the two compendial buffers, a result akin to reported slower dissolution of enteric coated tablets in vivo. There is therefore the need to adequately simulate the ionic composition of the intestinal fluid in the dissolution media. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16356670/A_comparative_in_vitro_assessment_of_the_drug_release_performance_of_pH_responsive_polymers_for_ileo_colonic_delivery_ DB - PRIME DP - Unbound Medicine ER -