Conversion of solid dispersion prepared by acid-base interaction into free-flowing and tabletable powder by using Neusilin® US2

International Journal of Pharmaceutics
Ankita Shah, Abu T M Serajuddin

Abstract

A novel method of greatly increasing solubility and dissolution rate of a model basic drug, haloperidol, by interacting it with water-soluble weak organic acids in aqueous media was previously reported in the literature. Amorphous solid dispersion (SD) was formed when solutions containing haloperidol and various acids were dried. However, the SDs were semisolid, viscous and sticky, especially when the drug load was high, and could not be processed into tablets. The drug release from SD was also incomplete since the viscous material did not readily mix with aqueous media. In the present study, a mesoporous metalosilicate, Neusilin(®) US2, was incorporated in SDs prepared by using malic, tartaric and citric acids. The silicate constituted 40% w/w of the total solid mass. The addition of silicate converted SDs into powders, which were then characterized for flow properties, bulk and tap density, and tabletability. Their physical properties were found to be acceptable for the development of tablets. DSC and powder XRD showed that haloperidol and acids converted completely to amorphous forms, and they did not show any sign of crystallization during accelerated stability study at 40°C/75% RH and 25°C/60% RH for 9 months. Complete dru...Continue Reading

References

Sep 1, 1971·Journal of Pharmaceutical Sciences·W L Chiou, S Riegelman
May 1, 1970·Journal of Pharmaceutical Sciences·J T Fell, J M Newton
Oct 9, 1999·Journal of Pharmaceutical Sciences·T KristmundsdóttirH Thormar
Jun 7, 2000·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·C Leuner, J Dressman
Jan 5, 2002·Pharmaceutical Development and Technology·M K GuptaY C Tseng
Feb 15, 2003·Journal of Pharmaceutical Sciences·Manish K GuptaRobin H Bogner
Sep 2, 2005·Journal of Pharmaceutical Sciences·Shoufeng LiAbu T M Serajuddin
Jul 7, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Hiroshi MiuraKatsuhide Terada
Jan 4, 2012·Journal of Pharmaceutical Sciences·Kristyn Greco, Robin Bogner

❮ Previous
Next ❯

Citations

Oct 31, 2020·International Journal of Pharmaceutics·Barbora VraníkováMartin Kuentz
Sep 21, 2020·International Journal of Pharmaceutics·Xiaoning ShanVitaliy V Khutoryanskiy

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here