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

Alhnan, MA; Cosi, D; Murdan, S; Basit, AW; (2010) Inhibiting the gastric burst release of drugs from enteric microparticles: the influence of drug molecular mass and solubility. J Pharm Sci , 99 (11) 4576 - 4583. 10.1002/jps.22174. Green open access

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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.

Type: Article
Title: Inhibiting the gastric burst release of drugs from enteric microparticles: the influence of drug molecular mass and solubility.
Location: United States
Open access status: An open access version is available from UCL Discovery
DOI: 10.1002/jps.22174
Publisher version: http://dx.doi.org./10.1002/jps.22174
Language: English
Additional information: The definitive version is available at www3.interscience.wiley.com
Keywords: Emulsions, Microspheres, Molecular Weight, Particle Size, Pharmaceutical Preparations, Polymethacrylic Acids, Solubility, Solvents, Tablets, Enteric-Coated
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
URI: https://discovery.ucl.ac.uk/id/eprint/1351094
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