CoQ10 Bioavailability, Formulation (Co-operation, Competition in the CoQ10 Market)

Market Factors

Given its health-promoting effects, it is no wonder the market for CoQ10 is on the rise. ZMC-USA estimated there are approximately 6 million U.S. consumers supplementing with CoQ10 daily, and added retail sales data from IRI indicated there was a 19 percent increase in dollar sales volume and a 9 percent increase in unit sales of CoQ10 in 2007.

However, there are several considerations, including absorption, bioavailability, formulation and quality control. “Since CoQ10 is a rather large lipid molecule, it is not easily absorbed,” Koon noted. “CoQ10 is absorbed intestinally via a process known as passive facilitated diffusion. Absorption occurs on a molecular level, which means only single molecules can be absorbed at a time. But the CoQ10 material exists in a crystalline state, meaning it must be dissolved into single molecules in order to be absorbed.”

And the melting point of CoQ10 is almost 20-degrees higher than body temperature; therefore, the standard crystalline (powder) form of CoQ10 has always been poorly absorbed, with absorption of about 1 percent—for every 100 mg of CoQ10 capsule/tablet ingested, the body only absorbs 1 mg.

Raj Chopra, CEO, Tishcon, noted CoQ10’s lipophilic form presents absorption challenges, because it is almost insoluble in aqueous media. “The lack of adequate oral bioavailability of CoQ10 has led to the search for delivery technologies that would render it more water-friendly,” he said. Tishcon, for example, developed the patented BioSolv® process, which involves the use of a nonionic surfactant and a polyhydric alcohol to facilitate the hydrosolubility of CoQ10 (U.S. Patent No. 6,056,971). Other patented systems include the complexation of CoQ10 with cyclodextrins (U.S. Patent No. 6,861,447); the formulation of liposomal dispersions of CoQ10 (U.S. Patent No. 6,445,072); the formulation of self-emulsifying CoQ10 complexes; and numerous other processes.

Soft Gel Technologies Inc. (SGTI) developed its CoQsol® and CoQsol-CF™ formulations, using a lipid-based soft gel delivery system, to increase absorption. In a randomized, placebo-controlled study, researchers determined the differences in steady state absorption over a 30-day period (60 mg/d) and five-hour peak absorption characteristics (30 mg) between CoQsol and dry CoQ10 powder in a two-piece hard shell capsule. After 30 days supplementation, the average basal blood CoQ10 levels for the CoQsol group increased by 165 percent, compared to an 80 percent increase in the dry powder group. Further, in the five hour trial portion, 30 mg of CoQsol increased peak absolute CoQ10 levels by 0.48 µg/ml blood compared to an increase of 0.19 µg/ml for the subjects taking 30 mg dry CoQ10 powder. CoQsol-CF was the subject of a pilot clinical trial, in which supplementation with 60 mg/d increased mean CoQ10 plasma levels by 200 percent over 28 days.