Melt extrusion and spray drying of carbamazepine and dipyridamole with polyvinylpyrrolidone/vinyl acetate copolymers

Drug Development and Industrial Pharmacy
James E PattersonThomas Rades

Abstract

Carbamazepine and dipyridamole are class II compounds (BCS) whose oral bioavailability is limited by poor solubility. The use of glass solutions to improve the bioavailability of this class of compound has been an area of research for a number of years. The influence of polymer parameters (Tg, hydrophilicity, solubility parameter, and ability to hydrogen bond) on glass solution properties is investigated. Carbamazepine and dipyridamole glass solutions are prepared with PVP/VA 64 and PVP/VA 37 by spray drying and melt extrusion. The products are then characterized by XRPD, thermal, and spectroscopic methods. Yield, physical stability, and dissolution profiles are also assessed. The properties of the polymer greatly influenced the ability to produce glass solutions. With decreases in Tg and hydrophilicity, melt extrusion became the more viable of the two preparative techniques. Although glass solutions were successfully prepared, the greater the difference in component solubility parameter, the less physically stable the formulation. Consideration must be given to the characteristics of the polymer when selecting for glass solution formulation. Although a number of process parameters can be varied for melt extrusion and spray dry...Continue Reading

References

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Jul 29, 2000·Drug Development and Industrial Pharmacy·F Zhang, J W McGinity
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Jul 30, 2005·Journal of Pharmaceutical Sciences·James E PattersonThomas Rades
Dec 19, 2006·International Journal of Pharmaceutics·James E PattersonThomas Rades

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Citations

Mar 23, 2011·Drug Development and Industrial Pharmacy·Fu JijunTang Xing
Jan 10, 2013·Drug Development and Industrial Pharmacy·Murali Mohan BommanaEmilio Squillante
Sep 16, 2010·Drug Development and Industrial Pharmacy·Mohanraj Palanisamy, Jasmina Khanam
Jul 24, 2012·International Journal of Pharmaceutics·Amrit PaudelGuy Van den Mooter
May 9, 2012·Advanced Drug Delivery Reviews·Amy J HallidayMark J Cook
Dec 27, 2015·Advanced Drug Delivery Reviews·Abhishek Singh, Guy Van den Mooter
Aug 25, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Saad M AlshahraniMichael A Repka
Jan 18, 2014·The Journal of Pharmacy and Pharmacology·Toshiro Sakai, Markus Thommes
Sep 21, 2013·International Journal of Pharmaceutics·Line Hagner NielsenAnette Müllertz
Oct 1, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Line Hagner NielsenAnette Müllertz
Jul 6, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Shrawan BaghelNiall J O'Reilly
Apr 23, 2017·Journal of Pharmaceutical Sciences·Rebecca A HalliwellAlastair J Florence
Sep 20, 2017·AAPS PharmSciTech·Siyuan Huang, Robert O Williams
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter
May 14, 2020·Pharmaceutics·Joanna Szafraniec-SzczęsnyRenata Jachowicz

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