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Release of 5-Aminosalicylic Acid (5-ASA) from Mesalamine Formulations at Various pH Levels.
- Source :
-
Advances in therapy [Adv Ther] 2015 May; Vol. 32 (5), pp. 477-84. Date of Electronic Publication: 2015 May 08. - Publication Year :
- 2015
-
Abstract
- Introduction: Oral formulations of 5-aminosalicylic acid (5-ASA) for treatment of ulcerative colitis have been developed to minimize absorption prior to the drug reaching the colon. In this study, we investigate the release of 5-ASA from available oral mesalamine formulations in physiologically relevant pH conditions.<br />Methods: Release of 5-ASA from 6 mesalamine formulations (APRISO®, Salix Pharmaceuticals, Inc., USA; ASACOL® MR, Procter & Gamble Pharmaceuticals UK Ltd.; ASACOL® HD, Procter & Gamble Pharmaceuticals, USA; MEZAVANT XL®, Shire US Inc.; PENTASA®, Ferring Pharmaceuticals, Ltd., UK; SALOFALK®, Dr. Falk Pharma UK Ltd.) was evaluated using United States Pharmacopeia apparatus I and II at pH values of 1.0 (2 h), 6.0 (1 h), and 6.8 (8 h). Dissolution profiles were determined for each formulation, respectively.<br />Results: Of the tested formulations, only the PENTASA formulation demonstrated release of 5-ASA at pH 1.0 (48%), with 56% cumulative release after exposure to pH 6.0 and 92% 5-ASA release after 6-8 h at pH 6.8. No other mesalamine formulation showed >1% drug release at pH 1.0. The APRISO formulation revealed 36% 5-ASA release at pH 6.0, with 100% release after 3 h at pH 6.8. The SALOFALK formulation revealed 11% 5-ASA release at pH 6.0, with 100% release after 1 h at pH 6.8. No 5-ASA was released by the ASACOL MR, ASACOL HD, and MEZAVANT XL formulations at pH 6.0. At pH 6.8, the ASACOL MR and ASACOL HD formulations exhibited complete release of 5-ASA after 4 and 2 h, respectively, and the MEZAVANT XL formulation demonstrated complete 5-ASA release over 6-7 h.<br />Conclusion: 5-Aminosalicylic acid release profiles were variable among various commercially available formulations.<br />Funding: Shire Development LLC.
- Subjects :
- Administration, Oral
Anti-Inflammatory Agents, Non-Steroidal therapeutic use
Chemistry, Pharmaceutical
Colitis, Ulcerative drug therapy
Humans
Intestinal Mucosa metabolism
Mesalamine therapeutic use
Anti-Inflammatory Agents, Non-Steroidal pharmacokinetics
Hydrogen-Ion Concentration drug effects
Intestinal Mucosa drug effects
Mesalamine pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1865-8652
- Volume :
- 32
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Advances in therapy
- Publication Type :
- Academic Journal
- Accession number :
- 25951927
- Full Text :
- https://doi.org/10.1007/s12325-015-0206-4