Cyclodextrins in veterinary medicine (Part 1)

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It is well known, that cyclodextrins have many different applications. Can they be used in veterinary medicine? Well, yes and not “just” as excipients in several drug formulations…But first let’s talk a little about the “classic” cyclodextrin usage in veterinary formulations.

There are several drugs used both in human and veterinary medicine which is formulated with cyclodextrins to improve the pharmacokinetic properties. The most notable ones are antifungal agents, like voriconazole and itraconazole. Itraconazole is formulated with (2-hydroxypropyl)-beta-cyclodextrin and it is used in cats.

Now let’s see a few drug formulations that are used only in veterinary medicine and contain cyclodextrins.

1.) Pimobendan (Vetmedin™) is a calcium sensitizer and a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilator effects, used for the treatment of heart failure in dogs. A new patent by Boehringer Ingelheim describes a formulation that consists of modified cyclodextrins1

2.) Alfaxalone (Alfaxan™) is a neuroactive steroid molecule with general anesthetic effects. It is used only in veterinary practice. In the formulation, (2-hydroxypropyl)-beta-cyclodextrin is applied as a solubilizing agent.

3.) At last but not least, my personal favorite (based on experience): Maropitant (Cerenia™), a drug used for the treatment of motion sickness and vomiting in dogs (and cats). In the formulation of the injection, due to the low solubility of the compound, sulfobutyl-ether-beta-cyclodextrin is used as a solubilizing agent.

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These were just a few examples for cyclodextrin usages in veterinary products, but this is only the tip of the iceberg…A few keywords from the second part: cryopreservation, toxins, vaccines, essential oils…How come cyclodextrins to these?

 

1Boehringer Ingelheim Vetmedica Gmbh, Liquid preparation comprising pimobendan, 2015, US9107952 B2

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