Equilibrium state at supersaturated drug concentration achieved by hydroxypropyl methylcellulose acetate succinate: molecular characterization using (1)H NMR technique

Molecular Pharmaceutics
Keisuke UedaKunikazu Moribe

Abstract

The maintenance mechanism of the supersaturated state of poorly water-soluble drugs, glibenclamide (GLB) and chlorthalidone (CLT), in hydroxypropyl methylcellulose acetate succinate (HPMC-AS) solution was investigated at a molecular level. HPMC-AS suppressed drug crystallization from supersaturated drug solution and maintained high supersaturated level of drugs with small amount of HPMC-AS for 24 h. However, the dissolution of crystalline GLB into HPMC-AS solution failed to produce supersaturated concentrations, although supersaturated concentrations were achieved by adding amorphous GLB to HPMC-AS solution. HPMC-AS did not improve drug dissolution and/or solubility but efficiently inhibited drug crystallization from supersaturated drug solutions. Such an inhibiting effect led to the long-term maintenance of the amorphous state of GLB in HPMC-AS solution. NMR measurements showed that HPMC-AS suppressed the molecular mobility of CLT depending on their supersaturation level. Highly supersaturated CLT in HPMC-AS solution formed a gel-like structure with HPMC-AS in which the molecular mobility of the CLT was strongly suppressed. The gel-like structure of HPMC-AS could inhibit the reorganization from drug prenuclear aggregates to th...Continue Reading

References

Sep 1, 1971·Journal of Pharmaceutical Sciences·W L Chiou, S Riegelman
Sep 30, 1999·International Journal of Pharmaceutics·J Y JungK H Lee
Jun 28, 2000·Pharmaceutical Research·B C Hancock, M Parks
Feb 13, 2001·International Journal of Pharmaceutics·S L RaghavanJ Hadgraft
Sep 21, 2002·Pharmaceutical Research·Timothy Scott WiedmannLamya Kamel
Jun 2, 2005·Journal of the American Chemical Society·Paul Schanda, Bernhard Brutscher
Sep 14, 2006·Pharmaceutical Research·Adchara PongpeerapatKeiji Yamamoto
Jun 19, 2007·The Journal of Physical Chemistry. B·Tejwant Singh, Arvind Kumar
Jul 10, 2007·Advanced Drug Delivery Reviews·David J Hauss
Jun 26, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Hajime KonnoLynne S Taylor
Dec 2, 2008·Molecular Pharmaceutics·Dwayne T FriesenJ A S Nightingale
Jan 22, 2009·Angewandte Chemie·Jamshed AnwarSheetal Odedra
May 1, 2009·Accounts of Chemical Research·Deniz ErdemirAllan S Myerson
May 13, 2010·Molecular Pharmaceutics·Kristyn Greco, Robin Bogner
Aug 26, 2010·Journal of Pharmaceutical Sciences·Kenjirou HigashiKeiji Yamamoto
Dec 6, 2011·International Journal of Pharmaceutics·Junying ZhangKeiji Yamamoto
May 18, 2013·International Journal of Pharmaceutics·Sen Xu, Wei-Guo Dai
Jan 21, 2014·International Journal of Pharmaceutics·Keisuke UedaKunikazu Moribe
Apr 9, 2014·Molecular Pharmaceutics·Prateek K Jha, Ronald G Larson
Apr 22, 2014·International Journal of Pharmaceutics·Kunikazu MoribeKeiji Yamamoto

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Citations

Jan 22, 2018·Carbohydrate Polymers·Juliana Munari Oliveira PintoHellen Karine Stulzer

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