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Inhibiting the gastric burst release of drugs from enteric microparticles: the influence of drug molecular mass and solubility.

Authors
  • Alhnan, Mohamed A
  • Cosi, Daniele
  • Murdan, Sudaxshina
  • Basit, Abdul W
Type
Published Article
Journal
Journal of Pharmaceutical Sciences
Publisher
Elsevier
Publication Date
Nov 01, 2010
Volume
99
Issue
11
Pages
4576–4583
Identifiers
DOI: 10.1002/jps.22174
PMID: 20845456
Source
Medline
License
Unknown

Abstract

Undesired drug release in acid medium from enteric microparticles has been widely reported. In this paper, we investigate the relative contribution of microparticle and drug properties, specifically microsphere size and drug's molecular weight and acid solubility, on the extent of such undesired release. A series of nine drugs with different physicochemical properties were successfully encapsulated into Eudragit S and Eudragit L microparticles using a novel emulsion solvent evaporation process. The process yielded spherical microparticles with a narrow size distribution (27-60 and 36-56 µm for Eudragit L and Eudragit S microparticles, respectively). Upon incubation in acid medium (pH 1.2) for 2 h, the release of dipyridamole, cinnarizine, amprenavir, bendroflumethiazide, budesonide and prednisolone from both Eudragit microparticles was less than 10% of drug load and conformed with the USP specifications for enteric dosage forms. In contrast, more than 10% of the entrapped paracetamol, salicylic acid and ketoprofen were released. Multiple regression revealed that the drug's molecular weight was the most important factor that determined its extent of release in the acid medium, while its acid solubility and microsphere's size had minor influences.

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