Structural Characterisation and Dehydration Behaviour of Siramesine Hydrochloride

Zimmermann, Anne; Tian, Fang; Diego, Heidi Lopez de; Frydenvang, Karla; Rantanen, Jukka; Elema, Michiel Ringkjøbing; Hovgaard, Lars

doi:10.1002/jps.21679

Cited by 10 publications

(11 citation statements)

References 31 publications

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“… Hydrate examples for each classification. (a) Isolated site hydrate: siramesine hydrochloride [9] . (b) Channel hydrate: theophylline monohydrate (reference code THEOPH01) [10] .…”

Section: Hydrate As a Solid Formmentioning

confidence: 99%

“…The chloride ion is often bonded to amine moieties of the drug molecule, and the water molecules of hydrochloride hydrates tend to be extensively involved with any hydrogen bond donors and acceptors in the structure [31] . A specific example is siramesine hydrochloride [9] . In the anhydrate structure of this salt, the chloride ion is ionically bonded to the ammonium nitrogen.…”

Section: Examples Of Two Specific Hydrate Systemsmentioning

confidence: 99%

“…(a) Isolated site hydrate: siramesine hydrochloride. [9] (b) Channel hydrate: theophylline monohydrate (reference code THEOPH01). [10] (c) Ion-associated hydrate: risedronate sodium dihydrate (reference code WURPOO).…”

Section: Pharmaceutical Properties Affected By Hydrate Formationmentioning

confidence: 99%

“…[31] A specific example is siramesine hydrochloride. [9] In the anhydrate structure of this salt, the chloride ion is ionically bonded to the ammonium nitrogen. In the monohydrate, water is incorporated into the crystal packing through hydrogen bonds to the chloride ion.…”

Section: Structure and Bonding In Hydrates Of Pharmaceutical Saltsmentioning

confidence: 99%

“…[92,96] Siramesine hydrochloride is a poorly water soluble drug that can exist in an anhydrous and a monohydrate form. [9] The solubilities and the powder dissolution rates of the two salt forms have been determined at pH 3.4 (below pHmax) and 6.4 (above pHmax) to study the influence of solid form on the pH-dependent transformation of salt to its free base ( Figure 8). At pH 3.4, no transformation to the base was observed and the dissolution rates of the anhydrate and monohydrate salts were comparable.…”

Section: Influence Of Salt Hydrates On Pharmaceutical Manufacturing Amentioning

confidence: 99%

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Factors affecting crystallization of hydrates

Tian

Zimmermann

et al. 2010

Journal of Pharmacy and Pharmacology

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Objectives To provide a comprehensive understanding of the competing thermodynamic and kinetic factors governing the crystallization of various hydrate systems. The ultimate goal is to utilize this understanding to improve the control over the unit operations involving hydrate formation, as well as to optimize the bioavailability of a given drug product. Key findings The thermodynamic and kinetic factors that govern hydrate crystallization are introduced and the current status of the endeavour to gain a mechanistic understanding of the phenomena that occur during the crystallization of different hydrate systems is discussed. The importance of hydrate investigation in the pharmaceutical field is exemplified by examining two specific hydrate systems: the polymorphic hydrate system and hydrates of pharmaceutical salts. Summary This review identifies the factors that are of critical importance in the investigation of anhydrate/hydrate systems. This knowledge can be used to control the phase transformation during pharmaceutical processing and storage, as well as in building a desired functionality for the final formulation.

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“… Hydrate examples for each classification. (a) Isolated site hydrate: siramesine hydrochloride [9] . (b) Channel hydrate: theophylline monohydrate (reference code THEOPH01) [10] .…”

Section: Hydrate As a Solid Formmentioning

confidence: 99%

Section: Examples Of Two Specific Hydrate Systemsmentioning

confidence: 99%