A top coating strategy with highly bonding polymers to enable direct tableting of multiple unit pellet system (MUPS)

Frederick Osei-Yeboah; Yidan Lan; Changquan Calvin Sun

doi:10.1016/j.powtec.2016.10.039

A top coating strategy with highly bonding polymers to enable direct tableting of multiple unit pellet system (MUPS)

Frederick Osei-Yeboah, Yidan Lan, Changquan Calvin Sun

Pharmaceutics

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

Abstract

Multiple unit pellet system(s), MUPS, is one of the most commonly used means for achieving modified drug release through oral administration. MUPS is usually delivered as capsules that contain drug bearing beads coated with a release modulating functional layer. While the routine manufacture of tablets of MUPS by direct compression is highly desired, it is faced with the problem of poor tableting properties or altered drug release behavior due to the rupture of the functional coating layer. The use of a significant amount of cushion material alleviates these problems, but is also challenged with the problem of segregation and reduced drug loading. We hypothesize that top-coating the beads with a layer of highly bonding polymer can enable direct tableting of beads without compromising the functional coating layer and avoid segregation problem. Using functionally coated pyridoxine and caffeine beads, we confirmed that top coating with Polyvinylpyrrolidone sufficiently plasticized with water can enable the preparation of strong tablets at even low compaction pressures. Drug release profiles of tablets are comparable to those of uncompressed beads, indicating negligible amount of damage, if any, to the functional coating layer. In conclusion, it has been demonstrated that top polymer coating may provide a promising universally applicable strategy to realize the goal of delivering MUPS in the form of tablet.

Original language	English (US)
Pages (from-to)	591-596
Number of pages	6
Journal	Powder Technology
Volume	305
DOIs	https://doi.org/10.1016/j.powtec.2016.10.039
State	Published - Jan 1 2017

Bibliographical note

Funding Information:
This work is supported by a grant from the Dane O. Kildsig Center for Pharmaceutical Processing Research (CPPR) . F.O-Y is grateful for a David and Marilyn Grant Fellowship in Physical Pharmacy (2013–2014) and a University of Minnesota Graduate School Doctoral Dissertation Fellowship (2014–2015). We thank Upsher-Smith Laboratories for providing functionally coated pyridoxine beads.

Publisher Copyright:
© 2016 Elsevier B.V.

Keywords

Direct compression
Drug release
Mechanical strength
Multiple unit pellet system (MUPS)

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10.1016/j.powtec.2016.10.039

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abstract = "Multiple unit pellet system(s), MUPS, is one of the most commonly used means for achieving modified drug release through oral administration. MUPS is usually delivered as capsules that contain drug bearing beads coated with a release modulating functional layer. While the routine manufacture of tablets of MUPS by direct compression is highly desired, it is faced with the problem of poor tableting properties or altered drug release behavior due to the rupture of the functional coating layer. The use of a significant amount of cushion material alleviates these problems, but is also challenged with the problem of segregation and reduced drug loading. We hypothesize that top-coating the beads with a layer of highly bonding polymer can enable direct tableting of beads without compromising the functional coating layer and avoid segregation problem. Using functionally coated pyridoxine and caffeine beads, we confirmed that top coating with Polyvinylpyrrolidone sufficiently plasticized with water can enable the preparation of strong tablets at even low compaction pressures. Drug release profiles of tablets are comparable to those of uncompressed beads, indicating negligible amount of damage, if any, to the functional coating layer. In conclusion, it has been demonstrated that top polymer coating may provide a promising universally applicable strategy to realize the goal of delivering MUPS in the form of tablet.",

keywords = "Direct compression, Drug release, Mechanical strength, Multiple unit pellet system (MUPS)",

author = "Frederick Osei-Yeboah and Yidan Lan and Sun, {Changquan Calvin}",

note = "Funding Information: This work is supported by a grant from the Dane O. Kildsig Center for Pharmaceutical Processing Research (CPPR) . F.O-Y is grateful for a David and Marilyn Grant Fellowship in Physical Pharmacy (2013–2014) and a University of Minnesota Graduate School Doctoral Dissertation Fellowship (2014–2015). We thank Upsher-Smith Laboratories for providing functionally coated pyridoxine beads. Publisher Copyright: {\textcopyright} 2016 Elsevier B.V.",

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N2 - Multiple unit pellet system(s), MUPS, is one of the most commonly used means for achieving modified drug release through oral administration. MUPS is usually delivered as capsules that contain drug bearing beads coated with a release modulating functional layer. While the routine manufacture of tablets of MUPS by direct compression is highly desired, it is faced with the problem of poor tableting properties or altered drug release behavior due to the rupture of the functional coating layer. The use of a significant amount of cushion material alleviates these problems, but is also challenged with the problem of segregation and reduced drug loading. We hypothesize that top-coating the beads with a layer of highly bonding polymer can enable direct tableting of beads without compromising the functional coating layer and avoid segregation problem. Using functionally coated pyridoxine and caffeine beads, we confirmed that top coating with Polyvinylpyrrolidone sufficiently plasticized with water can enable the preparation of strong tablets at even low compaction pressures. Drug release profiles of tablets are comparable to those of uncompressed beads, indicating negligible amount of damage, if any, to the functional coating layer. In conclusion, it has been demonstrated that top polymer coating may provide a promising universally applicable strategy to realize the goal of delivering MUPS in the form of tablet.

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KW - Mechanical strength

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A top coating strategy with highly bonding polymers to enable direct tableting of multiple unit pellet system (MUPS)

Abstract

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