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Q: Coenzyme Q10 - bioavailability, pharmacokinetics ( Answered 3 out of 5 stars,   0 Comments )
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Subject: Coenzyme Q10 - bioavailability, pharmacokinetics
Category: Health > Fitness and Nutrition
Asked by: saregamapa-ga
List Price: $25.00
Posted: 04 Jul 2006 21:55 PDT
Expires: 03 Aug 2006 21:55 PDT
Question ID: 743427
What is the bioavailability of Coenzyme Q10 in humans upon oral
administration?  We seek details about its pharmacokinetics.
Answer  
Subject: Re: Coenzyme Q10 - bioavailability, pharmacokinetics
Answered By: bobbie7-ga on 05 Jul 2006 08:20 PDT
Rated:3 out of 5 stars
 
Hello Saregamapa,


DRUG NAME: Coenzyme Q10 (CoQ)
MANUFACTURER: Various

PHARMACOKINETICS 

?CoQ has a biphasic absorption following oral dosing with an initial
peak in plasma concentration at 5 to 6 hours, then a second peak at 24
hours. The second peak is believed to reflect tissue redistribution
(from the liver) back into the circulation. Using lipid formulations
and taking CoQ with food both increase absorption. The half-life of
CoQ is approximately 30-50 hours, meaning that the time to
pharmacological steady state is fairly prolonged (1-2 weeks).?

?Clearances in healthy adults have ranged from 0.0647-1.3062 L/hr. It
has been suggested that CoQ may have nonlinear absorption with
increasing doses absorbed to a lesser degree. For example, CoQ doses
of 30 mg and 100 mg have been estimated to increase the blood CoQ
concentration by 15 ?g/L/mg and 11 ?g/L/mg of CoQ ingested,
respectively.?

?In another study, single CoQ doses of 20 mg, 100 mg, and 500 mg
produced dose-normalized changes in peak plasma concentrations of 18,
5.4, and 1.6 ?g/L/mg. This suggests that individual dosage amounts may
affect absorption and that three times daily dosing may be preferred
if larger overall doses of CoQ are needed. Smoking has been cited to
increase plasma CoQ concentrations for some unknown reason. Age,
gender, weight, diet, and baseline CoQ concentrations have all have
been suggested as variables that might influence plasma CoQ
concentrations, although there is disagreement on this issue.?

BBB Permeability
?In order to effect a significant change in CoQ plasma concentration,
it appears that prolonged dosing will be needed. In rats given doses
of 200-500 mg/kg/day, 1-2 months of supplementation was needed to see
a significant increase in brain CoQ concentrations (i.e., 10-30%). In
addition, plasma concentrations may not adequately predict brain
concentrations.?

Source: THE HUNTINGTON PROJECT http://www.huntingtonproject.org/Portals/0/Coq10.pdf



================================================


Coenzyme Q10: Absorption, tissue uptake, metabolism and pharmacokinetics

Available data on the absorption, metabolism and pharmacokinetics of
coenzyme Q10 (CoQ10) are reviewed in this paper.

?Because of its hydrophobicity and large molecular weight, absorption
of dietary CoQ10 is slow and limited. In the case of dietary
supplements, solubilized CoQ10 formulations show enhanced
bioavailability. The Tmax is around 6 h, with an elimination half-life
of about 33 h. The reference intervals for plasma CoQ10 range from
0.40 to 1.91 µmol/l in healthy adults. With CoQ10 supplements there is
reasonable correlation between increase in plasma CoQ10 and ingested
dose up to a certain point.?
 
Publisher:   Taylor & Francis  
Issue:   Volume 40, Number 5 / May 2006  
Pages:   445 - 453  

http://taylorandfrancis.metapress.com/(0xraw2vlj4nz0b55bnrmig55)/app/home/contribution.asp?referrer=parent&backto=issue,1,13;journal,3,55;linkingpublicationresults,1:103554,1


Purchase a copy of the complete article here:

http://taylorandfrancis.metapress.com/(0xraw2vlj4nz0b55bnrmig55)/app/account/offerings.asp?referrer=contribution&offering=1678&id=J382563101123127&action=purchase&backto=contribution,1,1;searcharticlesresults,9,540


================================================



Total Coenzyme Q10 Concentrations in Asian Men Following Multiple Oral
50-mg Doses Administered as Coenzyme Q10 Sustained Release Tablets or
Regular Tablets,
Biol. Pharm. Bull., Vol. 26, 52-55 (2003)

?Twenty healthy male volunteers (19?23 years old) were divided into
two equal groups. Each subject in Group I received 50 mg oral doses of
coenzyme Q(10) as sustained release tablets once a day for fifteen
days, while subject in Group II received 50 mg doses of coenzyme Q(10)
regular tablets.?

?Following 1 week 50 mg/d dosing of CoQ(10), plasma CoQ(10)
concentrations increased to 1.85+/-1.03 mg/l for sustained release
tablets and up to 1.37+/-0.74mg/l for regular tablets. The net
increment proportion in AUC for sustained release and regular tablets
were 148.26+/-176.56%, 102.57+/-130.00%, respectively?

Download the complete article here:
http://www.jstage.jst.go.jp/article/bpb/26/1/52/_pdf


================================================


BioFactors  
Issue:   Volume 18, Numbers 1-4 / 2003  
Pages:   185 - 193  

?Serum coenzyme Q_{10} (Q_{10}) concentrations were evaluated in
healthy male volunteers supplemented with 30 mg or 100 mg Q_{10} or
placebo as a single daily dose for two months in a randomised,
double-blind, placebo-controlled study.?

?Median baseline serum Q_{10}concentration in 99 men was 1.26 mg/l
(10%, 90% fractiles: 0.82, 1.83). Baseline serum Q_{10} concentration
did not depend on age, while borderline significant positive
associations were found for body weight and smoking 1-10 cigarettes/d.
Supplementation with 30 mg or 100 mg Q_{10} resulted in median
increases in serum Q_{10} concentration of 0.55 mg/l and 1.36 mg/l,
respectively, compared with a median decrease of 0.23 mg/l with
placebo. The changes in the Q_{10} groups were significantly different
from that in the placebo group, and the increase in the 100 mg Q_{10}
group was significantly greater than that in the 30~mg Q_{10} group.
The change in serum Q_{10}concentration in the Q_{10} groups did not
depend on baseline serum _{10} concentration, age, or body weight.?

IOS Press
http://iospress.metapress.com/(zvcbql55cqnqjnfnb20pvg55)/app/home/contribution.asp?referrer=parent&backto=issue,21,36;journal,16,41;linkingpublicationresults,1:103144,1


================================================
 


?The absorptive properties of 4 different coenzyme Q10 preparations
(fast-melting, effervescent, soft gelatin, and powder-filled hard
shell) were studied in a randomized, single-dose, crossover study.
Twenty-four male subjects were given a 60 mg dose of coenzyme Q10 and
plasma coenzyme Q10 was measured over the next 12 hours.
Pharmacokinetic properties including area under the curve (AUC),
maximum plasma concentration (Cmax), time to maximum plasma
concentration (Tmax) and elimination half-life (t 1/2) were measured.?


RESULTS: 

?Area under the curve (microg/ml x h) for the fast-melting and
effervescent formulations, while marginally greater, was not
significantly different when compared to the soft gelatin and
powder-filled preparations, 5.4 +/- 1.04 (110%) and 5.5 +/- 0.589
(112%) versus 5.0 +/- 0.859 (102%) and 4.9 +/- 0.812 (100%),
respectively. Cmax for the 2 novel formulations was also not
statistically different from the soft gelatin or powder-filled
preparations, 0.87 +/- 0.14 and 0.86 +/- 0.074 versus 0.70 +/- 0.010
and 0.81 +/- 0.159 (microg/ml). Tmax however, was significantly
shorter for the fast-melting and effervescent formulations compared
with the soft gel and powder-filled forms, 1.3 +/- 0.348 and 2.0 +/-
0.552 versus 3.7 +/- 0.702 and 4.1 +/- 0.993 (h), respectively.?

International Journal of Clinical Pharmacology and Therapeutics,
Vol. 41, No. 1/2003 (42-48) 

http://www.dustri.com/ze/cp/33cp0301.htm#cp41_042



================================================


A New Coenzyme Q10 Tablet-Grade Formulation (all-Q®) Is Bioequivalent
to Q-Gel® and Both Have Better Bioavailability Properties than Q-SorB®


?Twelve healthy male subjects participated in a randomized,
three-period crossover bioequivalence study. Plasma CoQ10 was
determined from pre-dose until +36 hours. To compare bioavailability,
corrected maximum concentration (Cmax) and area under the curve from 0
to +14 hours [AUC(0-14 h)] were assessed and tested for
bioequivalence. The bioequivalence ranges of 0.8-1.25 hour x microg/mL
for AUC(0-14 h) and 0.75-1.33 microg/mL for Cmax were applied.?

?In summary, the kinetic profiles of all CoQ10 preparations revealed a
one-peak plasma concentration-time course. Highest Cmax values were
seen after Q-Gel application, whereas time to Cmax was nearly
identical across all treatments. The AUC(0-14 h) values were highest
for Q-Gel, narrowly followed by all-Q. The tests for bioequivalence
showed a bioequivalence between Q-Gel and all-Q, and both preparations
were found to have better bioavailability properties than Q-SorB.
Although all-Q and Q-Gel have equivalent bioavailability properties,
all-Q can be directly used in tablets, while this is not the case for
Q-Gel or other similar forms.?

Sep 2005, Vol. 8, No. 3: 397-399
Journal of Medicinal Food
http://www.liebertonline.com/doi/abs/10.1089/jmf.2005.8.397


Purchase a copy of the complete article here:
http://www.liebertonline.com/doi/pdf/10.1089/jmf.2005.8.397?cookieSet=1


================================================


The relative bioavailability of typical commercially available forms
of coenzyme Q10 (CoQ10) was compared with that of Q-Gel, a new
solubilized form of CoQ10, in human subjects in two separate trials.

?In the first, standard softgel capsules containing CoQ10 suspension
in oil, powder-filled hardshell capsules and powder-based tablets were
tested along with Q-Gel using a daily dosage of 120 mg for three
weeks. The baseline plasma CoQ10 values were all very tight (0.50-0.52
microgram/mL) and after three weeks the values were 1.37, 1.63 and
1.60 micrograms/mL for the first three products and 3.31 micrograms/mL
for Q-Gel. The relative bioavailability calculated using the areas
under the plasma CoQ10 curve (AUC) were (micrograms/mL x time in days)
7.16 (100%), 8.97 (125%), 9.19 (128%) and for Q-Gel 22.86 (319%).?

?The second trial, carried out to replicate the findings in the first,
employed only two groups, namely the standard softgel capsules
containing the suspension and Q-Gel, and the duration was extended to
four weeks. Plasma CoQ10 values were: baseline 0.40 and 0.38 and after
four weeks 1.26 and 2.80; the corresponding AUCs were: 8.33 (100%) and
22.75 (273%).?
 
PubMed - indexed for MEDLINE
Relative bioavailability of coenzyme Q10 formulations in human subjects.
Int J Vitam Nutr Res. 1998
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=abstract&list_uids=9565826&query_hl=5&itool=pubmed_docsum


================================================


Relative bioavailability and antioxidant potential of two coenzyme q10
preparations.
Kurowska EM, Dresser G, Deutsch L, Bassoo E, Freeman DJ.

??the bioavailability of CoQ10 supplements depends on the formulation
taken. We compared the bioavailability and antioxidant properties of
two commercial CoQ10 formulations, a commercial grade CoQ10 powder
(commercial grade CoQ) and a new BT-CoQ10 BIO-TRANSFORMED (BT-CoQ10)
obtained by fermentation of a soy-based, CoQ10-rich media with baker's
yeast.?

?Capsules containing 300 mg of either BT-CoQ10 or commercial grade
CoQ10 were given daily for 1 week and multiple blood samples were
taken for CoQ10, glutathione and glutathione peroxidase (GPx)
determination. In 3 subjects, baseline plasma CoQ10 levels were lower
prior to BT than prior to commercial grade CoQ treatment. In the
remaining participants, ingestion of BT vs. commercial grade CoQ
significantly increased maximum plasma CoQ10 concentration (+126%, p =
0.04) and tended to increase CoQ10 area under the curve from 0 to 24 h
(+160%, p = 0.07). One week of treatment with each formulation
increased plasma CoQ10 but did not alter plasma glutathione or GPx
activity. The enhanced bioavailability of the BT product might be due
to its predominantly reduced, hydrophilic membrane-complex form.?
http://content.karger.com/produktedb/produkte.asp?typ=fulltext&file=ANM47016

Purchase complete article here:
http://content.karger.com/produktedb/produkte.asp?typ=fulltext&file=ANM47016


================================================


Bioavailability of four oral coenzyme Q10 formulations in healthy volunteers. 

The abstract is available at the link below
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=abstract&list_uids=7752839&query_hl=5&itool=pubmed_docsum


================================================

Coenzyme Q10: Absorption, Antioxidative Properties, Determinants, and Plasma Levels

Read the abstract at the following link:
http://taylorandfrancis.metapress.com/(0xraw2vlj4nz0b55bnrmig55)/app/home/contribution.asp?referrer=parent&backto=searcharticlesresults,8,540;

================================================


Search terms:
Coenzyme Q10
Bioavailability  pharmacokinetics

I hope the information provided is helpful!

Best regards,
Bobbie7
saregamapa-ga rated this answer:3 out of 5 stars
Satisfactory

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