Pharmaceutical cocrystals: Structural and physicochemical property studies

Pharmaceutical cocrystals are an emerging class of crystal forms in the pharmaceutical industry. Crystal engineering of an active pharmaceutical ingredient (API) offers a number of routes to improved solubility and dissolution rate, which can be adopted through an in-depth knowledge of crystal interactions. Pharmaceutical cocrystals that are obtained by design (crystal engineering) can enhance the solubility, bioavailability, release rates and/or stability of API crystal forms. Crystal engineering of pharmaceutical entities with poor solubility and permeability (class IV) have shown appreciable enhancements in the two properties thus paving the way for highly bioavailable drugs. Crystal engineering also allows the possibility of designing combinations of drugs that have multiple therapeutic benefits which exhibit higher bioavailablity and release properties than mixed drugs.

 

API-Final

                    

Ref.

  1. Sanphui, P.; Devi, VK.; Mathew, D.; Malviya, N.; Ganguly, S.; Desiraju, GR. Mol. Pharmaceutics 2015, in Press.
  2. Rajput, L. Cryst. Growth Des. 2014, 14, 5196-5205.
  3. Sanphui, P.; Tothadi, S.; Ganguly, S.; Desiraju, GR. Mol. Pharmaceutics 2013, 10, 4687−4697.
  4. Rajput, L.; Sanphui. P.; Desiraju, GR. Cryst. Growth Des. 2013, 13, 3681-3690.
  5. P. Sanphui. and L. Rajput., Acta Crystallogr., Sect. B 2013, 70, 81-90.

Indian Patent Filed in 2013

  1. Title of the invention: Sildenafil-cocrystals and salts and uses thereof; Assignee: Indian Institute of Science