title: Amorphous Protic Ionic Systems as Promising Active Pharmaceutical Ingredients: The Case of the Sumatriptan Succinate Drug.
abstract: In this article, we highlight the benefits coming from the application of amorphous protic ionic systems as active pharmaceutical ingredients (APIs). Using the case of the sumatriptan (STR) drug, we show that the conversion of nonionic API to partially ionized amorphous protic succinate salt (STR SUCC) brings a substantial improvement in apparent solubility. Since in general the disordered systems reveal a tendency to self-arrangement during storage, the dominant part of this article is dedicated to the physical stability issue of sumatriptan and its ionic counterpart. To recognize the crystallization tendency of the studied systems, the calorimetric measurements were performed. Additionally, the role of ion dynamics in spontaneous nucleation of amorphous sumatriptan succinate is discussed. The differential scanning calorimetry analysis of ionic and nonionic sumatriptan reveals many similarities in thermal properties of these APIs as well as distinct differences in their resistance against crystallization in the supercooled liquid state. To determine the long-term physical stability of STR SUCC at room temperature conditions, the time scale of structural relaxation below their glass transition temperatures is estimated. We show that in contrast to nonionic materials, τα predictions of STR SUCC are much more complex and require aging experiments.
authors.affiliation: Institute of Physics, University of Silesia , Uniwersytecka 4, 40-007 Katowice, Poland.|SMCEBI , 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.
authors.forename: Z
authors.initials: Z
authors.lastname: Wojnarowska
authors.affiliation: Institute of Physics, University of Silesia , Uniwersytecka 4, 40-007 Katowice, Poland.|SMCEBI , 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.
authors.forename: J
authors.initials: J
authors.lastname: Knapik
authors.affiliation: Institute of Physics, University of Silesia , Uniwersytecka 4, 40-007 Katowice, Poland.|SMCEBI , 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.
authors.forename: M
authors.initials: M
authors.lastname: Rams-Baron
authors.affiliation: Institute of Physics, University of Silesia , Uniwersytecka 4, 40-007 Katowice, Poland.|SMCEBI , 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.
authors.forename: A
authors.initials: A
authors.lastname: Jedrzejowska
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences , Grunwaldzka 6, 60-780 Poznań, Poland.
authors.forename: M
authors.initials: M
authors.lastname: Paczkowska
authors.affiliation: PozLab sp. z.o.o. Parkowa 2, 60-775 Poznań, Poland.
authors.forename: A
authors.initials: A
authors.lastname: Krause
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences , Grunwaldzka 6, 60-780 Poznań, Poland.
authors.forename: J
authors.initials: J
authors.lastname: Cielecka-Piontek
authors.affiliation: Institute of Chemistry, Department of Theoretical Chemistry, University of Silesia , Szkolna 9, 40-006 Katowice, Poland.
authors.forename: M
authors.initials: M
authors.lastname: Jaworska
authors.affiliation: Institute of Chemistry, Department of Theoretical Chemistry, University of Silesia , Szkolna 9, 40-006 Katowice, Poland.
authors.forename: P
authors.initials: P
authors.lastname: Lodowski
authors.affiliation: Institute of Physics, University of Silesia , Uniwersytecka 4, 40-007 Katowice, Poland.|SMCEBI , 75 Pulku Piechoty 1A, 41-500 Chorzow, Poland.
authors.forename: M
authors.initials: M
authors.lastname: Paluch
mesh_terms: D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D004355:Drug Stability; D052578:Ionic Liquids; D012995:Solubility; D019802:Succinic Acid / Q000737:chemistry*; D018170:Sumatriptan / Q000737:chemistry*; D044366:Transition Temperature; D014961:X-Ray Diffraction
chemical_list: D052578:Ionic Liquids; D018170:Sumatriptan; D019802:Succinic Acid
keywords: amorphous active pharmaceutical ingredients; dielectric spectroscopy; glass transition; molecular dynamics; protic ionic systems