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Pharmaceutical Cocrystals and Their Physicochemical Properties.

Schultheiss N, Newman A - Cryst Growth Des (2009)

Bottom Line: This review article will highlight and discuss the advances made over the last 10 years pertaining to physical and chemical property improvements through pharmaceutical cocrystals and, hopefully, draw closer the fields of crystal engineering and pharmaceutical sciences.

View Article: PubMed Central - PubMed

Affiliation: SSCI, Inc., A Division of Aptuit, West Lafayette, Indiana, and Seventh Street Development Group, Lafayette, Indiana.

ABSTRACT
This review article will highlight and discuss the advances made over the last 10 years pertaining to physical and chemical property improvements through pharmaceutical cocrystals and, hopefully, draw closer the fields of crystal engineering and pharmaceutical sciences.

No MeSH data available.


Intrinsic dissolution profile of fluoxetine HCl and its cocrystals measured in water at 10 °C. (Top ⧫) fluoxetine HCl/succunic acid cocrystal; (middle ◼) fluoxetine HCl; (middle ▲) fluoxetine HCl/fumaric acid cocrystal; (bottom ●) fluoxetine HCl/benzoic acid cocrystal. Figure modified from ref (12).
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fig8: Intrinsic dissolution profile of fluoxetine HCl and its cocrystals measured in water at 10 °C. (Top ⧫) fluoxetine HCl/succunic acid cocrystal; (middle ◼) fluoxetine HCl; (middle ▲) fluoxetine HCl/fumaric acid cocrystal; (bottom ●) fluoxetine HCl/benzoic acid cocrystal. Figure modified from ref (12).

Mentions: There are a limited number of intrinsic dissolution studies on cocrystals. Data for the glutaric acid cocrystal of 2-[4-(4-chloro-2-fluorphenoxy)phenyl]pyrimidine-4-carboxamide(48) were collected in water over 90 min and showed that the cocrystal dissolution was approximately 18 times faster than the parent compound. XRPD of the remaining solid showed mainly the glutaric acid cocrystal, with only minor peaks for the parent material, indicating that the results were not skewed by significant form changes over the course of the experiment. The intrinsic dissolution rates for fluoxetine HCl cocrystals were also measured in water, Figure 8.(12) The dissolution of the 2:1 fluoxetine HCl/succinic acid cocrystal was too fast to measure an accurate value for the dissolution rate, but a 3−fold increase over fluoxetine HCl was estimated based on early time points. The 1:1 fluoxetine HCl/benzoic acid cocrystal was roughly half-that of the API and the 2:1 fluoxetine HCl/fumaric acid cocrystal was approximately the same as that of the API. These results show that cocrystals can enhance the dissolution rate, but can also show no improvement or a slower dissolution rate. It was interesting to note that the aqueous solubility of the guest molecule appears to correlate with the aqueous dissolution rates of the corresponding cocrystal, with benzoic acid being the least soluble (0.34 g/100 g), fumaric acid being intermediate in solubility (0.61 g/100 g), and succinic acid being the most soluble (7.5 g/100 g). Other examples will be needed to determine if this is a general trend or specific to this system.


Pharmaceutical Cocrystals and Their Physicochemical Properties.

Schultheiss N, Newman A - Cryst Growth Des (2009)

Intrinsic dissolution profile of fluoxetine HCl and its cocrystals measured in water at 10 °C. (Top ⧫) fluoxetine HCl/succunic acid cocrystal; (middle ◼) fluoxetine HCl; (middle ▲) fluoxetine HCl/fumaric acid cocrystal; (bottom ●) fluoxetine HCl/benzoic acid cocrystal. Figure modified from ref (12).
© Copyright Policy - open-access - ccc-price
Related In: Results  -  Collection

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fig8: Intrinsic dissolution profile of fluoxetine HCl and its cocrystals measured in water at 10 °C. (Top ⧫) fluoxetine HCl/succunic acid cocrystal; (middle ◼) fluoxetine HCl; (middle ▲) fluoxetine HCl/fumaric acid cocrystal; (bottom ●) fluoxetine HCl/benzoic acid cocrystal. Figure modified from ref (12).
Mentions: There are a limited number of intrinsic dissolution studies on cocrystals. Data for the glutaric acid cocrystal of 2-[4-(4-chloro-2-fluorphenoxy)phenyl]pyrimidine-4-carboxamide(48) were collected in water over 90 min and showed that the cocrystal dissolution was approximately 18 times faster than the parent compound. XRPD of the remaining solid showed mainly the glutaric acid cocrystal, with only minor peaks for the parent material, indicating that the results were not skewed by significant form changes over the course of the experiment. The intrinsic dissolution rates for fluoxetine HCl cocrystals were also measured in water, Figure 8.(12) The dissolution of the 2:1 fluoxetine HCl/succinic acid cocrystal was too fast to measure an accurate value for the dissolution rate, but a 3−fold increase over fluoxetine HCl was estimated based on early time points. The 1:1 fluoxetine HCl/benzoic acid cocrystal was roughly half-that of the API and the 2:1 fluoxetine HCl/fumaric acid cocrystal was approximately the same as that of the API. These results show that cocrystals can enhance the dissolution rate, but can also show no improvement or a slower dissolution rate. It was interesting to note that the aqueous solubility of the guest molecule appears to correlate with the aqueous dissolution rates of the corresponding cocrystal, with benzoic acid being the least soluble (0.34 g/100 g), fumaric acid being intermediate in solubility (0.61 g/100 g), and succinic acid being the most soluble (7.5 g/100 g). Other examples will be needed to determine if this is a general trend or specific to this system.

Bottom Line: This review article will highlight and discuss the advances made over the last 10 years pertaining to physical and chemical property improvements through pharmaceutical cocrystals and, hopefully, draw closer the fields of crystal engineering and pharmaceutical sciences.

View Article: PubMed Central - PubMed

Affiliation: SSCI, Inc., A Division of Aptuit, West Lafayette, Indiana, and Seventh Street Development Group, Lafayette, Indiana.

ABSTRACT
This review article will highlight and discuss the advances made over the last 10 years pertaining to physical and chemical property improvements through pharmaceutical cocrystals and, hopefully, draw closer the fields of crystal engineering and pharmaceutical sciences.

No MeSH data available.