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.
Subject(s)
Ubiquinone/analogs & derivatives , Adult , Animals , Drug-Related Side Effects and Adverse Reactions , Female , Humans , Hydrophobic and Hydrophilic Interactions , Intestinal Absorption , Male , Rats , Rats, Sprague-Dawley , Solubility , Ubiquinone/administration & dosage , Ubiquinone/blood , Ubiquinone/toxicityABSTRACT
As part of a series of non-clinical studies to evaluate the safety of PureSorb-Q(TM)40 (Water-soluble type CoQ(10) powder, CoQ(10) content is 40 w/w%; hereinafter referred to as P40), male and female rats were treated orally by gavage with P40 once a day for 91 d, and its repeated dose toxicity was assessed. Control animals were treated with a 0.5 w/v% solution of methylcellulose, the vehicle for P40. Each test group consisted of 6 animals of each sex. No adverse effects of P40 were noted in general signs, body weight, food consumption, ophthalmological examination, urinalysis, hematological examination, blood chemical analysis, necropsy, organ weights, or histopathological examination in animals of either sex. From these results, the no observed adverse effect level of P40 was estimated at 2,000 mg/kg in both sexes of rats under the conditions of the present study, and P40 was confirmed to be a food material whose safety is high.
Subject(s)
Coenzymes/toxicity , Food Additives/toxicity , Administration, Oral , Animals , Blood Chemical Analysis , Body Weight/drug effects , Eating/drug effects , Female , Hematologic Tests , Histocytochemistry , Male , No-Observed-Adverse-Effect Level , Organ Size/drug effects , Organ Size/physiology , Rats , Rats, Sprague-Dawley , Ubiquinone , UrinalysisABSTRACT
PureSorb-Q40 (water-soluble type CoQ10 powder, CoQ10 content is 40 w/w%; hereinafter referred to as P40) is reported in the single-dose human and rat studies to have a greater absorption rate and absorbed volume of CoQ10 even taken postprandially, than those of regular CoQ10, which is lipid-soluble and generally taken in the form of soft-gel capsules. Thus, it was anticipated that the serum CoQ10 level might be higher with P40 tablets than with soft-gel capsules, even for the same dose of CoQ10. In the present study, in order to confirm the safety and measure the serum CoQ10 level for the case of an excessive dose of P40, a double-blinded Placebo controlled comparative study was conducted on 46 healthy volunteers and they were randomly divided into two groups. The P40 tablets or placebo were repeatedly taken by the volunteers. As the result of the study, for the group of taking 2250 mg/d of P40 (that is, 900 mg/d of CoQ10) for 4 consecutive wk, the serum CoQ10 level peaked at 2 wk after the start of intake at 8.79 +/- 3.34 microg/mL, and at 4 wk, it was at the level of 8.33 +/- 4.04 microg/mL. At 2 wk from withdrawal of intake, the serum CoQ10 level decreased to 1.30 +/- 0.49 microg/mL. The serum CoQ10 levels at these three points were significantly higher than those of the first day of intake and the Placebo group, which had no significant change throughout the study. Furthermore, P40 intake did not cause any significant changes in symptoms or clinical laboratory results as assessed by physical, hematological, blood biochemical or urinalysis tests. Physician examinations also did not reveal any abnormalities. These results confirm that P40 is an extremely safe material and it can produce better absorption of CoQ10.
Subject(s)
Coenzymes/toxicity , Ubiquinone/analogs & derivatives , Adult , Blood Cell Count , Blood Pressure/drug effects , Coenzymes/blood , Coenzymes/urine , Dose-Response Relationship, Drug , Double-Blind Method , Drug-Related Side Effects and Adverse Reactions , Electrocardiography/drug effects , Female , Heart Rate/drug effects , Hematocrit , Hemoglobins/drug effects , Humans , Male , Physical Examination , Reference Values , Tablets , Ubiquinone/bloodABSTRACT
Coenzyme Q10 (CoQ10) is a lipid-soluble antioxidant and essential component of the mitochondrial electron transfer system in the body, and is in wide use as a functional food material and cosmetic raw material. However, as CoQ10 is extremely lipid-soluble, absorption by the body is not easy. In general, people use soft-gel capsules in which CoQ10 is suspended in oil, and take these capsules with food. PureSorb-Q40 (P40) was developed to improve CoQ10 processability and absorption when taken without food, and the present study compared the effects of food on absorption between P40 and conventional lipid-soluble CoQ10 in rats and humans. The results of a rat study showed higher uptake when P40 was administered in the fasting state or with food compared to lipid-soluble CoQ10. The results of a human study showed that uptake was favorable when P40 was administered in the fasting state, and even when administered postprandially, a significant difference was noted in uptake rate up to 6 h after intake and uptake volume up to 8 h after intake when compared to lipid-soluble CoQ10. These results show that any CoQ10 product using P40 can be quickly and reliably absorbed by the body regardless of dosage form or intake time.
