Formation of Mefenamic Acid Nanocrystals with Improved Dissolution Characteristics

An industrially feasible formulation approach combining media milling and spray‐drying was applied to improve dissolution characteristics of the poorly soluble drug mefenamic acid (MA). The approach was studied for two MA polymorphs at different stressing and pH conditions. It was found that final M...

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Bibliographic Details
Published inChemie ingenieur technik Vol. 89; no. 8; pp. 1060 - 1071
Main Authors Konnerth, Christoph, Braig, Veronika, Ito, Atsutoshi, Schmidt, Jochen, Lee, Geoffrey, Peukert, Wolfgang
Format Journal Article
LanguageEnglish
Published 01.08.2017
Subjects
Dissolution rate enhancement
Media milling
Nanocrystal
Polymorphism
Poorly water‐soluble drug
Spray drying
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Summary:An industrially feasible formulation approach combining media milling and spray‐drying was applied to improve dissolution characteristics of the poorly soluble drug mefenamic acid (MA). The approach was studied for two MA polymorphs at different stressing and pH conditions. It was found that final MA product particle sizes are rather determined by the solid‐liquid equilibrium than by mechanical fracture. Obtained drug particles are only composed of the most stable polymorph. Direct compressed tablets containing MA nanocrystals exhibit a significant improvement of in vitro dissolution kinetics as compared to tablets with micronized drug particles. A formulation approach combining media milling and spray‐drying was applied to produce nanocrystals of the poorly soluble drug mefenamic acid. Tablets prepared by direct compression containing the nanosized drug show significantly improved dissolutions characteristics as compared to the dosage form which contains micronised drug particles.
ISSN:0009-286X
1522-2640
DOI:10.1002/cite.201600190