Novel Febuxostat-Telmisartan Cocrystal May Treat Comorbid Hyperuricemia/Gout and Hypertension

A novel drug-drug cocrystal of febuxostat and telmisartan may be used in the treatment of comorbid gout/hyperuricemia and hypertension, according to study findings published in Journal of Pharmaceutical Sciences.

Recent advancements in crystal engineering has resulted in the development of cocrystals for the treatment of comorbid conditions, such as gout and hypertension.

Researchers in Malaysia and India analyzed the novel cocrystal of febuxostat and telmisartan, using a methodical orthogonal framework.

They conducted a structural investigation using a single-crystal x-ray diffraction that confirmed heterosynthon formation between the carboxylic group of febuxostat and the benzimidazole group of telmisartan. Powder x-ray diffraction revealed the crystalline structure of the final product.

In addition, the researchers confirmed the noncovalent hydrogen bond formation in the heterosynthon using attenuated total reflectance Fourier transform infrared (ATR-FRIR) spectroscopy and Raman spectroscopy.

The researchers evaluated the physiochemical stability of the cocrystal using an accelerated stability study as well as an invitro biorelevant dissolution study. The cocrystal was found to be both physically and chemically stable, and demonstrated a slower dissolution rate compared with other drugs; however its melting point was closer to that of febuxostat than telmisartan.

“We…envisage that by doing appropriately designed clinical studies on the pathology and posology of the present cocrystal combination,” the study authors noted, “this work can offer a unique opportunity for developing a potential combination therapy for the patients [affected by] both the conditions — hypertension and gout.”

Reference

Ganesan T, Muthudoss P, Voguri RS, et al. A new febuxostat-telmisartan drug-drug cocrystal for gout-hypertension combination therapy. J Pharm Sci. Published online August 24, 2022. doi:10.1016/j.xphs.2022.08.022