Mannitol-coated hydroxypropyl methylcellulose as an alternative directly compressible controlled release excipient

[Display omitted] One of the most common forms of controlled release technology for oral drug delivery comprises an active ingredient dispersed in a hydrophilic matrix forming polymer such as hydroxypropyl methylcellulose (HPMC), which is tableted via direct compression. However, HPMC may pose probl...

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Published inInternational journal of pharmaceutics Vol. 660; p. 124298
Main Authors Kang, Christina Yong Xin, Foo, Wen Chin, Lam, Kwan Hang, Chow, Keat Theng, Lui, Yuan Siang, Goh, Hui Ping, Salome, Antoine, Boit, Baptiste, Lefevre, Philippe, Hiew, Tze Ning, Gokhale, Rajeev, Heng, Paul Wan Sia
Format Journal Article
LanguageEnglish
Published Netherlands Elsevier B.V 20.07.2024
Subjects
Chemistry, Pharmaceutical - methods
Co-processed
Controlled release
Delayed-Action Preparations - chemistry
Direct compression
Drug Compounding - methods
Drug Liberation
Excipients - chemistry
Hydroxypropyl methylcellulose
Hypromellose Derivatives - chemistry
Mannitol
Mannitol - chemistry
Powders
Solubility
Tablets
Co-processed
Hydroxypropyl methylcellulose
Direct compression
Controlled release
Mannitol
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Summary:[Display omitted] One of the most common forms of controlled release technology for oral drug delivery comprises an active ingredient dispersed in a hydrophilic matrix forming polymer such as hydroxypropyl methylcellulose (HPMC), which is tableted via direct compression. However, HPMC may pose problems in direct compression due to its poor flowability. Hence, mannitol syrup was spray-coated over fluidized HPMC particles to produce co-processed HPMC–mannitol at ratios of 20:80, 50:50, and 70:30. Particles of pure HPMC, co-processed HPMC–mannitol, and their respective physical mixtures were evaluated for powder flowability, compression profiles, and controlled release performance. It was found that co-processed HPMC–mannitol consisted of particles with improved flow compared to pure HPMC particles. Sufficiently strong tablets of >2 MPa could be produced at moderate to high compression forces of 150–200 MPa. The dissolution profile could be tuned to obtain desired release profiles by altering HPMC–mannitol ratios. Co-processed HPMC–mannitol offers an interesting addition to the formulator’s toolbox in the design of controlled release formulations for direct compression.
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ISSN:0378-5173
1873-3476
1873-3476
DOI:10.1016/j.ijpharm.2024.124298