Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai
Reexamination Certificate
1999-05-26
2001-02-06
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ether doai
C514S720000, C514S824000, C514S878000, C514S879000
Reexamination Certificate
active
06184255
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a medicinal composition with improved absorption after oral administration which comprises a coenzyme Q
10
of the following general formula (1-A) as an active ingredient.
BACKGROUND ART
Coenzyme Q
10
is a class of physiological substances occurring as component factors of the mitochondrial electron transfer system within the biological cell. Coenzyme Q
10
acts directly as an electron carrier in the oxidative phosphorylation reactions, through metabolic pathways, particularly aerobic pathways, to produce ATP and hence energy.
It seems that the demand for coenzyme Q
10
is increased in normal subjects in the state of severe physical fatigue and patients with cardiovascular disease, chronic debilitating disease, or on prolonged pharmacotherapy. It has been shown that a deficiency of coenzyme Q
10
occurs particularly in ischemic heart diseases, senile myocardial sclerosis, and hypertensive heart diseases. Therefore, it is a sound therapeutic choice to administer coenzyme Q
10
to those patients.
Moreover, coenzyme Q
10
has been used for non-therapeutic purposes as a nutrient or nutritional supplement just like vitamins.
In order that coenzyme Q
10
may express its therapeutic efficacy or nutritional effect, it is most important to increase the coenzyme Q
10
level within the patient's tissue cells.
Coenzyme Q
10
is a lipid-soluble and practically water-insoluble substance and, therefore, it is only sparingly soluble in gastric juice. Consequently, oral dosage forms containing coenzyme Q
Q
10
in solid state, such as tablets, granules, capsules, and suspensions for extemporaneous preparation, are not well absorbed after oral administration. This means that a considerably greater amount of coenzyme Q
10
than actually needed must be administered to the patient but such a practice tends to cause adverse gastrointestinal reactions such as epigastric discomfort, anorexia, nausea, and diarrheas.
Much research has heretofore been undertaken for overcoming those disadvantages. Japanese Kokai Publications Sho-55-81813 and Sho-61-221131, among others, disclose coenzyme Q
10
formulations of the solution type or the emulsion/dispersion type. However, such pharmaceutical devices are not sufficient to improve the absorption of coenzyme Q
10
in a satisfactory measure.
Japanese Kokai Publication Sho-56-18914 discloses a technology for accelerating the lymphatic absorption of coenzyme Q
10
. This technology has been demonstrated to increase the absorption of coenzyme Q
10
in a certain measure but has not proved practically useful as yet.
Japanese Kokai Publication Sho-60-89442 discloses a cyclodextrin-clathrated coenzyme Q
10
formulation. Japanese Kokai Publication Sho-60-1124 discloses a coenzyme Q
10
-containing ribosomal formulation. However, those coenzyme Q
10
preparations require a complicated pharmaceutical procedure for production and are not practically fully satisfactory.
Italian Patent 1190442 Specification discloses a technology which, instead of using coenzyme Q
10
as such, comprises converting a reduced form of coenzyme Q
10
to a derivative such as an acyl ester, a sulfuric acid ester, or a phosphoric acid ester and administering this coenzyme Q
10
derivative for enhanced absorption. However, the effect of the technology has not been supported by experimental data.
SUMMARY OF THE INVENTION
The present invention has for its object to provide a medicinal composition comprising coenzyme Q
10
as an active ingredient, which composition features an enhanced absorption after oral administration.
In the course of their intensive research for overcoming the above-mentioned disadvantages of the prior art, the inventors of the present invention discovered that when a medicinal composition containing a reduced form of coenzyme Q
10
was prepared and administered to patients by the oral route, a considerably higher bioavailability was surprisingly obtained as compared with the conventional medicinal composition containing only the oxidized form of coenzyme Q
10
. The present invention has been developed on the basis of the above finding.
The present invention, therefore, is directed to a medicinal composition comprising coenzyme Q
10
as an active ingredient with the reduced form of coenzyme Q
10
accounting for more than 20 weight % of said coenzyme Q
10
.
REFERENCES:
patent: 3349113 (1967-10-01), Gloor et al.
patent: 5312819 (1994-05-01), Fischer et al.
patent: 5648377 (1997-07-01), Bombardelli et al.
patent: 198839B (1989-02-01), None
patent: 1190442 (1985-11-01), None
patent: 59-47202A (1984-03-01), None
patent: 59-47202 (1984-03-01), None
patent: 4-89456 (1992-03-01), None
patent: 4-89456A (1992-03-01), None
“Effect of Dietary Coenzyme Q as an Antioxidant in Human Plasma”, Molec. Aspects. Med., vol. 15 (Supplement), pp. s97-s102, Dec. 1994.
Weber, C. et al., Molec. Aspects Med., (1994) vol. 15 (Supplement), pp. S97-S102.
Hidaka Takayoshi
Mae Tatsumasa
Morikawa Souichi
Sakamoto Yoshitomo
Kaneka Corporation
Krass Frederick
Pollock Vande Sande & Amernick
LandOfFree
Pharmaceutical composition comprising coenzyme Q10 does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical composition comprising coenzyme Q10, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical composition comprising coenzyme Q10 will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2603561