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Calcium Coordination Solids for pH‐Triggered Release of Olsalazine
Author(s) -
Levine Dana J.,
Gonzalez Miguel I.,
Legendre Christina M.,
Runčevski Tomče,
Oktawiec Julia,
Colwell Kristen A.,
Long Jeffrey R.
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700540
Subject(s) - calcium , chemistry , organic chemistry
Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H 4 olz), an anti‐inflammatory compound used for treatment of ulcerative colitis. The materials include one‐dimensional Ca(H 2 olz)⋅4 H 2 O chains, two‐dimensional Ca(H 2 olz)⋅2 H 2 O sheets, and a three‐dimensional metal‐organic framework Ca(H 2 olz)⋅2DMF (DMF= N , N ‐dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H 2 olz) phase when exposed to aqueous HCl. The compounds Ca(H 2 olz)⋅ x  H 2 O ( x =0, 2, 4) were each pressed into pellets and exposed to simulated gastrointestinal fluids to mimic the passage of a pill from the acidic stomach to the pH‐neutral intestines. All three calcium materials exhibited a delayed release of olsalazine relative to Na 2 (H 2 olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.

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