This shouldn’t be a bitter pill to swallow.

So  the headline caught your attention ? No, oh well, I may try harder next time……..or not.  I thought I might talk about crystallizations today and more specifically about pharmaceutical co-crystals.  If you followed my previous website, PHARMNBIOFUEL.COM, I know that I had covered this topic before.  The gist of using a pharmaceutical co-crystal is to enhance solubility, bioavailability, etc. by adding another chemical entity (this isn’t a salt) that crystallizes with the pharmaceutical of interest.  You can take a look at the following review to read about pharmaceutical co-crystals.

M. Li et al, “Pharmaceutical co-crystals: An Overview”, International Journal of Pharmaceutics, 419 (2011) 1-11, doi: 10.1016/j.ijpharm.2011.07.037

I think it is a familiar story where the final drug product that you attain is as soluble as brick dust and is quite difficult to dissolve in solution.   In fact, the above article mentions that something like less than 1 % of the active pharmaceutical compounds appear in the marketplace.  That is a huge problem.  So I think co-crystals are definitely very important to aid in solubility, bioavailability, handling, filterability, etc.

I came across this paper in Crystal Growth and Design.  The title of the paper, which fascinated me is “Pharmaceutical Salts of Haloperidol with Some Carboxylic Acids and Artificial Sweeteners: Hydrate Formation, Polymorphism,and Physicochemical Properties” by S. Aitipamula, R. Tan et al, Crys. Growth Des., 2014, 14, 2542−2556, doi: 10.1021/cg500245e

Haloperiodal and some artificial sweeteners that were used as cocrystals

Haloperiodal and some artificial sweeteners that were used as cocrystals

This was the first time I had heard of using an artificial sweeteners as cocrystals and found that this idea was quite innovative.  Who hasn’t swallowed a bitter pill ?  Could you imagine how easily you might take your medicine if it had a sweetener in it to cut down on the bitter aftertaste ?

Although this paper talked about making other salts from common organic acids, such as succinic acid, oxalate acid, etc.  I was more interested if a salt could be made with the artificial sweeteners.  Two different polymorphs were made with saccharin in a 1:1 ratio as well as with acesulfame.   All sweeteners formed 1:1 salts, however only acesulfame and saccharin formed polymorphs with haloperidol.

The Acesulfame salt showed a dissolution rate that was 400 times that of the free base.  Really interesting stuff.

That’s all I have for now.  Stay tuned.  Feel free to comment.  Follow me on Twitter @DevelopProcess or Google+, Facebook or LinkedIn.


2 thoughts on “This shouldn’t be a bitter pill to swallow.

  1. Seems to be very intresting and looks tobe having a good role to play in Pharmaceutical administration…thougha lot of work has to be done with lot of insoluble drugs and also what happens to the ‘sweetener’..during drug actvity.


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