A (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer)-dispersed sustained-release tablet for imperialine to simultaneously prolong the drug release and improve the oral bioavailability

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Qing LinZhirong Zhang

Abstract

Imperialine, extracted from Bulbus Fritillariae Cirrhosae, is an efficient antitussive and expectorant medicine. However, its short half-life and stomach degradation limited imperialine from further clinical use. The current study was conducted to develop a sustained-release tablet for imperialine both to prolong absorption time and to improve the oral bioavailability of the drug. The tablets were prepared by a direct compression method formulated on optimized solid dispersion (SD) for imperialine based on polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus(®)) with imperialine/Soluplus(®) ratio of 1:8 (w/w). In order to obtain the optimized formulation, factors that affected the drug release were investigated by in vitro dissolution studies in the media of pH1.2, 5.8, 7.0 and 7.4. Powder X-ray diffraction and scanning electron microscope confirmed that the imperialine in SD was amorphous instead of crystalline, and still stayed amorphous even after the direct compression. And besides, pharmacokinetic study in Beagle dogs was performed to inspect the in vivo sustained release. Plasma concentration-time curves and pharmacokinetic parameters were gained. As a result, the Cmax of imperialine was o...Continue Reading

References

Jul 11, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yajaman SudhakarA K Bandyopadhyay
Aug 21, 2008·Drug Delivery·Subramania Nainar MeyyanathanBhojraj Suresh
Sep 1, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Mariana LandínP York
Dec 17, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Michael LinnClaus-Michael Lehr
Sep 24, 2013·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Qing LinZhirong Zhang
Jun 9, 2015·Acta Pharmacologica Sinica·Qing LinZhi-rong Zhang

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Citations

Dec 24, 2015·AAPS PharmSciTech·Thawatchai Phaechamud, Chai-Ek Choncheewa
Mar 3, 2018·Drug Delivery and Translational Research·Julien Maincent, Robert O Williams
Jul 8, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Li QiaoQingcong Wei
Jan 11, 2018·Bioconjugate Chemistry·Jeffrey M TingTheresa M Reineke

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