Optimising the release rate of naproxen liqui-pellet: a new technology for emerging novel oral dosage form
Issue Date
2019-07-08Subjects
solid-state analysisliqui-pellet
Liquisolid
dissolution enhancement
extrusion-spheronisation
liquid vehicle
liquisolid pellet
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Liqui-pellet is a new dosage form stemming from pelletisation technology and concept from liquisolid technology. In spite of liqui-pellet overcoming a major hurdle in liquisolid technology through achieving excellent flow property with high liquid load factor, the formulation requires to be optimised in order to improve drug release rate. Liqui-pellets of naproxen containing Tween 80, Primojel, Avicel and Aerosil were extruded and spheronised. Flowability test confirmed that all liqui-pellet formulations have excellent-good flow property (Carr’s index between 3.9–11.17%), including liqui-pellets with a high liquid load factor of 1.52, where 38% of the total mass is co-solvent. This shows a relatively high liquid load factor can be achieved in liqui-pellet without compromising the flowability, which is one of the key novelty of this work. It was found that the improved drug release rate was due to the remarkably improved disintegration of the supposedly non-disintegrating microcrystalline-based pellet; the optimised liqui-pellet seems to explode into fragments in the dissolution medium. At pH 1.2, the optimised formulation had ~ 10% more drug release than non-optimised formulation after 2 h, and at pH 7.4, the drug release of the optimised pellet was nearing 100% at ~ 15 min, whereas the none-optimised pellet only achieved ~ 79% drug release after 2 h. DSC and XRPD indicated an increase in the dissolution rate could be due to molecularly dispersion of naproxen in the pellets. Overall results showed that liqui-pellet exhibited an enhanced drug release and the capacity for high liquid load factor whilst maintaining excellent flowability, rendering it a potentially commercially feasible drug delivery system.Citation
Lam M, Ghafourian T, Nokhodchi A (2020) 'Optimising the release rate of naproxen liqui-pellet: a new technology for emerging novel oral dosage form', Drug Delivery and Translational Research, 10 (1), pp.43-58.Publisher
SpringerPubMed ID
31286452PubMed Central ID
PMC6978301Additional Links
https://link.springer.com/article/10.1007%2Fs13346-019-00659-6Type
ArticleLanguage
enISSN
2190-393Xae974a485f413a2113503eed53cd6c53
10.1007/s13346-019-00659-6
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