title: Blood CoQ10 levels and safety profile after single-dose or chronic administration of PureSorb-Q40: animal and human studies.
abstract: Coenzyme Q10 (CoQ10) is known to be highly hydrophobic and, as such, insoluble in water: this leads to serious inconvenience when trying to incorporate it in food products. Its absorption is also known to be very limited. PureSorb-Q40 (P40) (Water-soluble type CoQ10 powder, CoQ10 content 40 w/w % was developed in order to improve its use with food products and to enhance its absorption. In the present study the absorption of this novel formulation was compared to a conventional lipid soluble CoQ10 by administering both products to rats and humans. Acute, single-administration studies in rats showed that P40 has a higher absorption, compared to lipid soluble CoQ10, both in prandial and fasting states. Similarly, single administration in humans revealed a higher absorption level for P40, taken in the fasting state or together with meals. In the rat study, no adverse effects were observed with P40 at doses up to 2,000 mg/kg in both sexes. In a double-blind, placebo controlled, comparative study conducted on 46 healthy volunteers and randomly divided into two groups, in the group receiving 900~mg of CoQ10 per day, for 4 consecutive weeks, the average level at two weeks was 8.79 +/- 3.34 microg/mL, similar to the corresponding level after 4 weeks (8.33 +/- 4.04 microg/mL). After 2 weeks of washout, serum CoQ10 level decreased to 1.30 +/- 0.49 microg/mL. P40 intake did not cause any significant changes in symptoms and clinical laboratory tests as assessed by physical, hematological, blood biochemical or urinalysis. Clinical examinations also did not reveal any abnormalities. The above blood (serum) CoQ10 level at 2 weeks after start of intake was compared with other reported values. The same dose of CoQ10 (900mg/day), when administered by softgel capsules yielded a plasma CoQ10 concentration of 3.6 microg/mL, while P40 levels were 8.79 +/- 3.34 microg/mL. These levels are remarkably high for instance when compared to the corresponding levels obtained, in patients affected by Parkinson's disease, with CoQ10 doses up to 2,400mg/day. A clinical study was conducted using doses of 300 mg/day and 600 mg/day, in patients affected by cardiovascular disease. Also in this case there was linearity in the response with the levels obtained by administering P40 at a dose of 100 and 900 mg/day.
authors.affiliation: Nisshin Pharma Inc., Tokyo, Japan.
authors.forename: Kazuki
authors.initials: K
authors.lastname: Nukui
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Yamagishi
authors.forename: Hiromi
authors.initials: H
authors.lastname: Miyawaki
authors.forename: Aikkarach
authors.initials: A
authors.lastname: Kettawan
authors.forename: Tadashi
authors.initials: T
authors.lastname: Okamoto
authors.forename: Romualdo
authors.initials: R
authors.lastname: Belardinelli
authors.forename: Luca
authors.initials: L
authors.lastname: Tiano
authors.forename: Gian Paulo
authors.initials: GP
authors.lastname: Littarru
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Sato
mesh_terms: D000328:Adult; D000818:Animals; D064420:Drug-Related Side Effects and Adverse Reactions; D005260:Female; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007408:Intestinal Absorption; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014451:Ubiquinone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000633:toxicity
chemical_list: C522292:PureSorb-Q40; D014451:Ubiquinone; C024989:coenzyme Q10