Enhanced oral bioavailability of paclitaxel by solid dispersion granulation

Drug Development and Industrial Pharmacy
Srinivasan ShanmugamJong Soo Woo

Abstract

The main objective of this study was to develop novel orally administrable tablets containing solid dispersion granules (SDG) of amorphous paclitaxel (PTX) prepared by fluid bed technology, and to evaluate its in vitro dissolution and in vivo pharmacokinetics (PK) in beagle dogs. The SDG were prepared using optimized composition by fluid bed technology, and characterized for solid-state properties. The release study of SDG tablet (SDG-T) in simulated gastric fluid showed a rapid release of PTX, reaching maximum dissolution within 20 min. Finally, the PK profile of SDG-T and a reference formulation Oraxol™ (oral solution formulation used in Phase I clinical study) at a dose of 60 mg orally with co-administration of P-gp inhibitor HM38101, and Taxol® at a dose of 10 mg intravenously (i.v.) was investigated in beagle dogs. The mean absolute BA% of PTX following SDG-T and Oraxol™ solution was 8.23 and 6.22% in comparison to i.v. administration of Taxol®. The relative BA% of PTX from SDG-T in comparison to Oraxol™ solution was 132.25% at a dose of 60 mg following oral administration. In conclusion, we have successfully prepared PTX tablets with solid dispersion granules (SDG) of amorphous PTX using fluid bed technology that could pr...Continue Reading

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Citations

Aug 21, 2015·Drug Development and Industrial Pharmacy·Maozhong LiYerong Xiong
Aug 13, 2015·Drug Development and Industrial Pharmacy·Maozhong LiYerong Xiong
Nov 5, 2019·Biochimica Et Biophysica Acta. Reviews on Cancer·Urvi H GalaRobert O Williams

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