Pharamaceutical composition containing ubidecarenone

Details Pharamaceutical composition containing ubidecarenone Pharamaceutical composition containing ubidecarenone

1986-11-06

1989-09-26

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Enzyme or coenzyme containing

514458, 514682, 514946, A61K 3748

Patent

active

048699004

DESCRIPTION:

BRIEF SUMMARY
The present invention concerns a pharmaceutical composition containing Coenzyme Q.sub.10 as active ingredient and more particularly it concerns an orally adminsterable composition which ensures a high bioavailability of the active ingredient.
Coenzyme Q.sub.10 (ubidecarenone) of formula: ##STR1## is a substance naturally occuring in mammals and man wherein it plays an important role in the mitochondrial electron transport. Coenzyme Q.sub.10 (hereinafter referred to as CoQ.sub.10) proved to be clinically effective in the treatment of several cardiac affections such as cardiac deficiency, ischemic disease, etcetera. However, CoQ.sub.10 is very little soluble in water and in the gastric and intestinal juice; its absorption, notoriusoly scarce, takes place throught the lymphatic system.
Because of these characteristics, having available a pharmaceutical preparation ensuring an improved absorption of the drug is a very felt need.
Some pharmaceutical preparations or compositions having the scope of improving the absorption and thus the bioavailability of CoQ.sub.10 have been described in the literature.
Among these, may be cited compositions containing CoQ.sub.10 in association with a hydrophilic surfactant and a fatty acid (Japanese patent application No. 84/148718, Fujisawa Pharmaceutical Co. (Chemical Abstracts, 101, 226447c)), with an ester of a fatty acid with polyglycols and a water-soluble polymer (Japanese patent application No. 84/51214, Taiho Pharmaceutical Co. (Chemical Abstracts, 101, 137025k)) with a higher fatty acid and/or a monoglyceride of a higher fatty acid (European patent application No. 23349, Eisai Co.).
Liquid drinkable or injectable pharmaceutical compositions have also been described as well as aqueous emulsions containing CoQ.sub.10 in association with hydrogenated lecithin (European patent application No. 83108, Eisai Co.) and with lecithin and methanol (Japanese patent application No. 78/56315, Eisai Co. (Chemical Abstracts, 89, 95002b)).
However, because of the characteristics of the drug and for practical purposes in connection to the administration to the patient, solid orally administerable pharmaceutical preparations are preferred.
We have now found, and this is an object of the present invention, an orally administerable composition as below specified, which affords a high absorption of CoQ.sub.10.
The composition object of the present invention comprises (by weight) from 2 to 17% of CoQ.sub.10, from 50 to 70% of lecithin and from 20 to 48% of a surfactant agent as below defined, the total being 100%.
Specific examples of compositions according to the invention are reported in the following table 1.


TABLE 1

Compositions according to the invention.


______________________________________ Ingredient (% b.w.) a b c d e f ______________________________________ CoQ.sub.10 2 5 7 10 16.7 17 Lecithin 70 65 63 70 63.3 55 Surfactant agent 48 30 30 20 20 28 ______________________________________ surfactant agent in amounts of from 20 to 30% b.w.
As lecithin, soybean lecithin is generally used but it may also be used, with identical results, lecithin of other sources.
The surfactant agent useful in the compositions object of the invention consists of a physical or chemical association of a surfactant with a fat or with polyethyleneglycol; said surfactant agent being characterized by a melting point comprised between 35.degree. and 55.degree. C. and by a HLB value (hydrophilic-lipophilic balance) comprised between 12 and 15 but preferably between 12 and 14.
An example of a suitable surfactant agent is the product "Gelucire 50/13" (trademark of Gattefosse Company) consisting of a mixture of mono-, di- or triglycerides of hydrogenated palmil and palmitate-stearate esters of polyethyleneglycol having a molecular weight between 1000 and 2000, a melting point of 50.degree. C. and a HLB value of 13.
Another useful surfactant agent is the product "Glucire 44/14" (trademark of Gattefosse Company) consisting of glyceryl and polyethyleneglycol 1500 esters of copra hydroge

REFERENCES:
patent: 4325942 (1982-04-01), Taki et al.
patent: 4483873 (1984-11-01), Ohashi et al.
patent: 4525350 (1985-06-01), Casey et al.
Eisai Co., Ltd., cited in Chem. Abstracts, vol. 100:145017d, 1984.
Handbook of Pharmaceutical Excipients, pp. 209-213.

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