Coenzyme Q10 formulation and process methodology for soft...

Details Coenzyme Q10 formulation and process methodology for soft... Coenzyme Q10 formulation and process methodology for soft...

2000-03-28

2003-09-09

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Capsules

C514S863000

Reexamination Certificate

active

06616942

ABSTRACT:

BACKGROUND OF THE INVENTION
This invention relates to an improved formulation and process methodology of Coenzyme Q
10
in producing soft gel capsules of this formulation. Coenzyme Q
10
(CoQ
10
or Ubiquinone) is a large molecular weight (863.63 grams) lipid compound that is produced in the liver and perhaps other body organs. The total body content is estimated to be 1.4 to 1.8 grams, depending on the age and the physical fitness of the individual. Although CoQ
10
is found in the mitochondria and other organelles of every living cell, it appears to be most abundant in tissues with a high number of mitochondria and a high level of metabolic activity. For example, in the metabolically inactive blood there is approximately 4 mg, in the heart, and in the skeletal muscle 1000 mg. The blood acts as a CoQ
10
reservoir and transport media between endogenous CoQ
10
synthesis in the liver, exogenous CoQ
10
absorption from digested food substances in the intestinal tract, and the body cells. Endogenous synthesis appears to be responsible for 56 percent and exogenous sources for 44 percent of the body's CoQ
10
requirements. These numbers are currently being studied and endogenous CoQ
10
synthesis may be significantly deficient in the elderly. These deficiencies are not related to the total caloric intake, but rather to the vitamin content of ingested foods. The body requires multiple vitamins for the synthesis of CoQ
10
.
CoQ
10
requirements of the body are also variable between individuals and are dependent on age, physical activity, and disease. It is estimated that the body CoQ
10
utilization is between 5 and 9 mg per day. Intercellular CoQ
10
is required for the synthesis of energy and therefore essential for life. Energy synthesis occurs in the mitochondria, where CoQ
10
provides an electron for the electron transport chain in the cytochrome system, in which adenosine tripohosphate (ATP) is synthesized. As CoQ
10
gives up an electron for ATP synthesis, it gets oxidized. If CoQ
10
is used as an antioxidant, it gets oxidized and is no longer available to provide electrons and function in the synthesis of ATP. Under conditions of high metabolic stress, endogenous sources may become inadequate to meet the body's CoQ
10
requirement for ATP synthesis. Under such conditions, dietary CoQ
10
supplementation has been shown to be an effective source. An improved soft gel formulation and process of CoQ
10
soft gel capsule manufacturing has uses to treat heart failure, chronic fatigue and patients with psoriasis and planter warts. In all cases, it has been found that the improved soft gel formulation at ingestion rates of 30-100 mg/day of CoQ
10
have been proven to be superior to commercially available 60 mg dry powder capsules, and existing 100 mg/day CoQ
10
soft gel formulations.
An appropriate CoQ
10
dosage for a normal individual compared to the dosage necessary for a diseased individual has been difficult to ascertain. Recommended doses of 10 to 30 mg/day were found to be ineffective for patients with significant CoQ
10
deficiencies. In the past 15 years, it has become generally accepted that poor intestinal absorption of certain CoQ
10
formulations limits their effective use. For this reason, 50 and 150 mg CoQ
10
containing tablets or capsules are commercially available to the consumer, at a considerably higher cost.
Folkers et al (U.S. Pat. No. 4,824,669) addresses a soft gel capsule with CoQ
10
and at least one vegetable oil. This formulation was determined to increase blood CoQ
10
levels to 2.5 &mgr;g/ml compared to 1.6 &mgr;g/ml for an equivalent 100 mg dose of dry powder CoQ
10
. Many different CoQ
10
formulations have appeared which are claimed to increase intestinal absorption. However, intestinal absorption data, collected under near basal conditions, which compare CoQ
10
alone in oil with dry powder CoQ
10
, are conclusive that oil is a better delivery agent.
SUMMARY OF THE INVENTION
The present invention comprises a stable and nontoxic soft gel Coenzyme Q
10
formulation and process methodology of Coenzyme Q
10
for maximum Coenzyme Q
10
levels in the human body for a given input. A preferred soft gel formulation includes Coenzyme Q
10
(hereinafter CoQ
10
), Vitamin E, beta-carotene, bee's wax, medium chain triglycerides available as MCT Myglyol S12, and rice bran oil formulated to maximize the body's absorption by maintaining the CoQ
10
in what may be a supersaturated solution in easily absorbed materials, that can provide healthful effects, as opposed to just fillers. It is important as much of the supplied CoQ
10
be absorbed, rather than just taking megadoses at frequent intervals as the wholesale cost of CoQ
10
dry powder in quantity is as much as $2000 per kg. Not only is a relatively large percentage of the CoQ
10
absorbed, but the volume of the soft gel capsule is minimized, making it easier to swallow and requiring smaller shipping and storage space. Recent studies indicate the preferred soft gel CoQ
10
formulation should be administered twice a day in dosages of about 30 mg CoQ
10
in 220 mg capsules, as that amount of CoQ
10
is about the maximum the body of a healthy sedentary adult can use for maintenance of a preferred blood level. For those who have deficiencies of CoQ
10
, studies have shown that twice a day administration of about 60 mg CoQ
10
in 435 mg capsules is advantageous. In special instances of CoQ
10
deficiency, twice a day ingestion of 100 mg CoQ
10
containing soft gel capsules can be tolerated.
It is therefore an object of the present invention to provide a soft gel formulation of CoQ
10
and a methodology of formulation processing that produce a significantly greater bioavailability percentage of ingested CoQ
10
than existing soft or dry formulations.
Another object of the present invention is to provide a soft gel formulation of CoQ
10
and methodology of administration that produces greater absorption of CoQ
10
into the intestine.
Another object is to minimize the ingested volume required to maintain a given CoQ
10
blood content.
Another object is to provide a process that keeps CoQ
10
in solution in readily absorbed materials, that themselves have beneficial effects.


REFERENCES:
patent: 4824669 (1989-04-01), Folkers et al.
patent: 5500416 (1996-03-01), Miyazawa et al.
patent: 6020383 (2000-02-01), Stone et al.
patent: 6069167 (2000-05-01), Sokol
patent: 6203818 (2001-03-01), Vester

Affiliated with

Also associated with

Rating

Coenzyme Q10 formulation and process methodology for soft... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Coenzyme Q10 formulation and process methodology for soft..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Coenzyme Q10 formulation and process methodology for soft... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3004678