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  • The search for various solid forms of an active pharmaceutical ingredient (API) is an important step in drug development. Our aim was to prepare co-crystals of trospium chloride, an anticholinergic drug used for the treatment of incontinence, and to investigate if they have advantageous properties for drug formulation. Phase identification was done by powder X-ray diffraction and single-crystal X-ray diffraction. The chemical composition was verified by solution NMR and the dissolution rate of the prepared phases was studied by IDR (intrinsic dissolution rate). For further analysis of phase stability and transitions, combined thermal analysis and temperature-resolved X-ray powder diffraction were used. Urea was selected as a co-crystallization partner. Trospium chloride urea (1:1) co-crystal was prepared by a solvent evaporation. from single-crystal data, the co-crystal structure was solved in a space group P2(1)/c and compared to previously published structures of trospium chloride. Intrinsic dissolution rate revealed that the co-crystal dissolves 32% faster than pure API. However, its low thermal and pressure stability makes it a challenging choice for the final drug formulation. (C) 2014 Elsevier By. All rights reserved.
  • The search for various solid forms of an active pharmaceutical ingredient (API) is an important step in drug development. Our aim was to prepare co-crystals of trospium chloride, an anticholinergic drug used for the treatment of incontinence, and to investigate if they have advantageous properties for drug formulation. Phase identification was done by powder X-ray diffraction and single-crystal X-ray diffraction. The chemical composition was verified by solution NMR and the dissolution rate of the prepared phases was studied by IDR (intrinsic dissolution rate). For further analysis of phase stability and transitions, combined thermal analysis and temperature-resolved X-ray powder diffraction were used. Urea was selected as a co-crystallization partner. Trospium chloride urea (1:1) co-crystal was prepared by a solvent evaporation. from single-crystal data, the co-crystal structure was solved in a space group P2(1)/c and compared to previously published structures of trospium chloride. Intrinsic dissolution rate revealed that the co-crystal dissolves 32% faster than pure API. However, its low thermal and pressure stability makes it a challenging choice for the final drug formulation. (C) 2014 Elsevier By. All rights reserved. (en)
Title
  • Increasing dissolution of trospium chloride by co-crystallization with urea
  • Increasing dissolution of trospium chloride by co-crystallization with urea (en)
skos:prefLabel
  • Increasing dissolution of trospium chloride by co-crystallization with urea
  • Increasing dissolution of trospium chloride by co-crystallization with urea (en)
skos:notation
  • RIV/60461373:22310/14:43897874!RIV15-GA0-22310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GA14-03636S), S
http://linked.open...iv/cisloPeriodika
  • AUG 1 2014
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 21152
http://linked.open...ai/riv/idVysledku
  • RIV/60461373:22310/14:43897874
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Organic compounds; Growth from solutions; X-ray diffraction; Solubility; Crystal structure (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • NL - Nizozemsko
http://linked.open...ontrolniKodProRIV
  • [ED7E64B994EB]
http://linked.open...i/riv/nazevZdroje
  • Journal Cryst.Growth
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 399
http://linked.open...iv/tvurceVysledku
  • Zámostný, Petr
  • Kratochvíl, Bohumil
  • Čejka, Jan
  • Skořepová, Eliška
  • Hušák, Michal
http://linked.open...ain/vavai/riv/wos
  • 000336432400004
issn
  • 0022-0248
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.jcrysgro.2014.04.018
http://localhost/t...ganizacniJednotka
  • 22310
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