Urolithin A Choline Salt

Urolithin A Choline Salt is a new patented compound product formulated as a novel salt form designed to break through absorption bottlenecks and advance anti-aging applications. 

Core Clinical Barriers of Free-State Urolithin A:

Only about 40% of the population possesses effective gut microbiota capable of converting dietary precursors (ellagitannins from pomegranates, berries, and nuts) into Urolithin A.

Free-state Urolithin A has extremely low solubility (below detection limits in pure water and 0.28 µg/mL in simulated intestinal fluid), leading to an oral bioavailability of less than 1% and sub-therapeutic plasma concentrations.

Uses a salt formation and crystal engineering strategy with choline as a counterion to disrupt the strong intermolecular hydrogen bond network of Urolithin A's phenolic hydroxyl groups, lowering lattice energy.

High-throughput crystallization screening identified "Type A" as the thermodynamically stable crystal form with optimal solubility and physicochemical stability.

In simulated intestinal fluid (FaSSIF, pH 6.5), the choline salt Type A reached a solubility of 3.6 µg/mL at 1 hour (about 13 times higher than the free state).

In pure water, it achieved an exponential leap to 1,542.3 µg/mL at 0.5 hours, whereas the free state remained below the detection limit.

• Rat pharmacokinetic studies confirmed a relative bioavailability of 216% (AUC increased from 18,626 to 40,219 ng h/mL).

• Peak concentration (Cmax) increased approximately 5-fold from 1,632 to 8,085 ng/mL.

• Time to peak (Tmax) was shortened from 4 hours to 1 hour, facilitating rapid onset.

Through the dual strategy of salt formation and crystal engineering, the Urolithin A choline salt Type A has restructured the drug's dissolution and absorption behavior at the molecular level. in vitro solubility improved by up to thousands of times in aqueous media and approximately 13-fold in simulated intestinal fluid, in vivo bioavailability increased by 216%, and Cmax increased approximately 5-fold. The complete evidence chain proves that this salt form is a novel solid form with high stability, high solubility, and high bioavailability, establishing a new benchmark for the efficient oral delivery of Urolithin A.