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Title:
SKIN REJUVINATING SUPPLEMENT
Document Type and Number:
WIPO Patent Application WO/2007/050423
Kind Code:
A3
Abstract:
A skin rejuvenating supplement composition for treating age spots, darkening of the skin, dry skin, calcium amino acid deficiencies, osteoporosis and eye site deficiencies. The composition contains 100 to 1,500mg of pearl powder, 0.6 to 50µg Vitamin D, 1.5 to 20.0mg of astaxanthin and 20 to 750mg of bilberry extract. The composition can be administered in a tablet, also containing glycerol in an amount of about 500mg, once or two times per day.

Inventors:
ITAGAKI YASUHIRO (US)
KANAYAMA NOBUKO (US)
IIDA YASUHISA (US)
NAKANISHI JUN (US)
Application Number:
PCT/US2006/040879
Publication Date:
October 11, 2007
Filing Date:
October 18, 2006
Export Citation:
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Assignee:
ITAGAKI YASUHIRO (US)
KANAYAMA NOBUKO (US)
IIDA YASUHISA (US)
NAKANISHI JUN (US)
International Classes:
A61K8/65; A61K35/618
Domestic Patent References:
WO2003013556A12003-02-20
Foreign References:
FR2865354A12005-07-29
US20050226830A12005-10-13
JP2003304846A2003-10-28
Other References:
PIZZORNO J.E. ET AL.: "Textbook of Natural Medicine", vol. 2ND ED., 1999, pages: 994
KATIYAR ET AL.: "Green tea polyphenol ()-epigallocatechin-3-gallate treatment of human skin inhibits ultraviolet radiation-induced oxidative stress", CARCINOGENESIS, vol. 22, no. 2, February 2001 (2001-02-01), pages 287 - 294
CAMIRE M.E. ET AL.: "Phytochemicals in Vaccinium family: bilberries, blueberries and cranberries", PHYTOCHEMICALS IN NUTRITION AND HEALTH, vol. 19, 2002
Attorney, Agent or Firm:
ARMSTRONG, IV, James E. (KRATZ QUINTOS, HANSON & BROOKS, LLP,1725 K Street, Nw,Suite 100, Washington District Of Columbia, US)
Download PDF:
Claims:

CLAIMS

What is claimed is:

1. An oral supplement composition for maintaining and improving skin condition

comprising the following ingredients:

a) conchiolin protein

b) Vitamin D, and

c) an antioxidant.

2. The composition of claim 1, wherein the antioxidant is astaxanthin.

3. The composition of claim 1, wherein the conchiolin protein is provided in the

composition in the form of pearl powder which incorporates the conchiolin protein.

4. The composition of claim 1 further comprising a polyphenol.

5. The composition of claim 1 further comprising a polyphenol different from the

antioxidant.

6. The composition of claim 5, comprising bilberry extract as the source of the

polyphenol.

7. An oral supplement composition for maintaining and improving skin condition

comprising:

a) 100 to l,500mg of pearl powder as the conchiolin protein,

b) 0.6 to 50μg Vitamin D, and

c) 1.5 to 20.0mg of astaxanthin as the antioxidant.

8. The composition of claim 7 further comprising 20 to 750mg of bilberry extract.

9. An oral supplement dosage unit for maintaining and improving skin condition

comprising:

a) 100 to 300mg of pearl powder,

b) 0.6 to 1.25μg Vitamin D, and

c) 1.5 to lO.Omg of astaxanthin.

10. The dosage unit of claim 9, having 250mg of pearl powder, 1.25μg Vitamin D and

3.3mg of astaxanthin.

11. The dosage unit of claim 9, wherein the ingredients are contained in a capsule with

500mg of glycerol.

12. The dosage unit of claim 9, wherein the pearl powder has an average particle

diameter size of 1 μm.

13. The dosage unit of claim 9, further comprising 20 to 150mg of bilberry extract.

14. The dosage unit of claim 13 for maintaining and improving skin condition having:

a) 250mg of pearl powder,

b) 1.25μg Vitamin D,

c) 3.3mg of astaxanthin, and

d) lOOmg bilberry extract.

15. The dosage unit of claim 14, wherein the ingredients are contained in a capsule with

500mg of glycerol.

16. A method of preventing osteoporosis comprising:

taking at least one oral supplement dosage unit comprising:

a) 100 to l,500mg of pearl powder,

b) 0.6 to 50μg Vitamin D, and

c) 1.5 to 20.0mg of astaxanthin.

17. The method of claim 16, wherein the oral supplement dosage unit further comprises

0 to 750mg of bilberry extract.

Description:

TITLE

SKIN REJUVINATING SUPPLEMENT

BACKGROUND OF THE INVENTION

The skin is the body's outer covering and the body's largest organ. Skin protects

the body against heat, light, injury, and infection. It regulates body temperature and

stores water, fat, and vitamin D. Damage to the skin from normal environmental

exposures has been well documented. The skin is considered a highly stressed organ. It

is subject to chemical attack and also to constant exposure to ultraviolet radiation.

Prolonged exposure to ultraviolet light is linked to skin damage characterized by

sunburn, aging and cancer. The production of free radicals from oxygen in the presence

of ultraviolet light is linked to degradation of collagen and other structural components

of the skin in addition to DNA mutation and structural changes which impair the skin's

ability to heal itself. In recent years the demand for cosmetic compositions and

cosmetic methods for improving the appearance and condition of skin has grown

enormously.

Consumers are increasingly seeking "anti-ageing" skin care products that treat

or delay the visible signs of chronoageing and photoageing skin, such as wrinkles, lines,

sagging, hyperpigmentation and age spots.

Consumers also frequently seek other benefits from skin care products in

addition to anti-ageing. The concept of "sensitive skin" has also raised the consumer

demand for skin care products that improve the appearance and condition of sensitive,

dry and/or flaky skin and to soothe red, and/or irritated skin.

In China, pearl powder has been known for thousands of years as traditional

medicine. It is used to treat cataract and ringing in the ear, bronchitis, high blood

pressure, inflammation of the liver (hepatitis), angina, autonomic imbalance, etc. It is

also used in its raw form as a skin whitener/rejuvenator, anti-aging agent, as well as an

anti-inflammatory agent.

Conchiolin is a protein extracted from pearl powder. There are several patents

based on conchiolin, or its hydrolyzate, made from shells and pearls of pearl oysters, sea

mussels, etc. Patent JP-H06-17123 recognizes conchiolin- vitamin E compound to be a

potent antioxidant. Patent JP-H06-211640 recognizes conchiolin as an active oxygen

suppressor. Patent JP 2003-292447 recognizes pearl powder compound as

anti-diabetes supplement.

Other patent literature includes an astaxanthin-bilberry extract compound

which has been reported in patent JP-2002- 17295 showing effectiveness against eye

diseases while helping to maintain optical functions. Patent JP-2002-335668 recognizes

astaxanthin-tocotrienol compound as a skin-beautifying agent. Patent JP-2004-210725

recognizes astaxanthin to have cyclooxygenase inhibitory function.

DETAILED DESCRIPTION OF THE INVENTION

The present invention is a formulation including at least three ingredients:

conchiolin protein, vitamin D and an antioxidant. The formulation of the present

invention is intended for human health care, in particular skin care. Specifically, it

may be used for treating age spots, darkening of the skin (pigmentary deposits) and dry

skin. It may also be used for treating calcium/amino acid deficiencies, osteoporosis

and for improving eyesight. In fact, the present invention is the first invention that

rejuvenates the skin and at the same time prevents osteoporosis.

Conchiolin protein is the protein that gives pearl the rainbow-like or iridescent

glow. Conchiolin protein can be found in pearls produced by bivalve shellfishes such

as pearl oysters, abalone, silver-lipped pearl oysters (pinctada maxima), black-lipped

pearl oysters (pinctada margaritifera), etc. It is woven into the pearl's calcium. To

extract the protein from a pearl, which is primarily calcium, the pearl needs to be

dissolved first with acid that reacts with calcium carbonate such as hydrochloric acid.

However, for use with this invention, conchiolin protein or its hydrolysate need not be

extracted and purified. Rather, it can be used in a form (powder, liquid etc.) that can

be absorbed readily by the body via internal organs such as the stomach and intestines.

One such form is pearl powder. Pearls that are ground into powder provide an

adequate source of conchiolin protein or its hydrolysate. Pearl powder can be made

fine so that the powder particles have an average diameter of 1 to lOμm.

Vitamin D is an agent good for aiding the digestion function of the human body.

It assists the body in digesting not only Vitamin D itself but other substances as well.

For example, in combination with pearl powder, Vitamin D aids the body in digesting

and absorbing conchiolin protein and calcium. Used in the solid form, Vitamin D

creates an easily absorbed effective agent for helping the body digest and absorb

surrounding ingredients.

Antioxidant is a classification of substances which are inhibitors, effective in

preventing or slowing down oxidation by singlet oxygen and/or various forms of

radicals. Anitoxidants include vitamins C and E, vitamin A (which is converted from

beta-carotene), selenium (a mineral), lycopene, and a group known as the carotenoids.

One antioxidant for the present invention is astaxanthin, which is the main carotenoid

pigment found in aquatic animals and algae. Additional antioxidants that can be used

for the present invention include carnosine, cartenoid, co-en2yme QlO, Vitamins A, B,

C and E, selenium, soy isoflavones, and zinc. Astaxanthin is used because of its

properties as a strong antioxidant and an effective compound against UV radiation on

the skin.

The formulation of the present invention is generally administered orally. It

may be administered in an individual dosage form such as capsule form, in which case

there will be additional ingredients, generally considered to be inactive ingredients, such

as fillers. Glycerol may be used as such an inactive ingredient.

Generally one dosage unit of the present invention will have the following

amounts of compounds: the amount of conchiolin found in 100 to l,500mg of pearl

powder, 0.6 to 50μg of Vitamin D, and an amount of an antioxidant, such as 1.5 to

20.0mg of a strong antioxidant like astaxanthin or several more times (2 to 10 times

more) of a weaker antioxidant.

Within the total ranges of amounts of each ingredient, smaller amounts are

possible, for example, the amount of conchiolin found in 200, 400, 600, 900, 1,000 or

l,200mg of pearl powder, 2.5, 5, 10, 20, 30, or 40 μg of Vitamin D and 2, 4, 6, 8, 10, 12,

15, 17 or 18mg of a strong antioxidant like astaxanthin. Combinations of these

amounts may be used to create a dosage unit for administering the present invention.

Preferably, when in an individual dosage form, the content of a typical daily

dosage will be 100 to 300mg of pearl powder, 0.6 to 1.25μg of Vitamin D and 1.5 to

lO.Omg of astaxanthin, with Vitamin D not exceeding 100 IU. Glycerol, or other

inactive ingredients, can be combined with the above active ingredients in a variable

amount to formulate a capsule or tablet for taking orally. Typically, the formulation

will be designed for administration twice a day, so the amounts of components in a

dosage unit would be 50 to 150 mg of pearl powder; 0.3 to 0.63 μg of Vitamin D and

0.75 to 2.0mg of astaxanthin.

The upper limit of the general dosage amount of each ingredient represents an

amount, assuming the present invention is taken twice a day (in other words a dosage of

2X), that will not exceed the US Food and Drug Administration recommended daily

allowance for an adult human.

The lower limit of the effective dosage amount of each ingredient represents

the lower limit of half of the daily amount necessary to achieve the objective of the

present invention.

Polyphenols, a class of phytochemicals found in high concentrations in wine,

tea, grapes and a wide variety of other plants, may also be added to the above

formulation to further improve the present invention, as polyphenols are good protectors

against UV radiation on the skin. Polyphenols can also act as antioxidants. Bilberry

extract may be used as an ingredient because it is an excellent source of polyphenols in

addition to being an antioxidant. In fact, by using astaxanthin and bilberry extract,

both of which are a 100-1,000 times more effective antioxidant as compared to vitamin

E, the age-spot prevention/skin restoration functions, at least one objective of this

invention, has been dramatically improved.

Thus, when in an individual dosage form, the content of a typical dosage unit

of the present invention will be 100 to 300mg of pearl powder, 0.6 to 1.25μg of Vitamin

D, 1.5 to 4.0mg of astaxanthin, and 20 to 750mg of bilberry extract, with Vitamin D not

exceeding 100 IU/day. Within the range of amount of bilberry extract, smaller amounts

are possible like 150, 300, 450, 500, and 650mg. However for a typical daily dosage

150mg of bilberry extract will be sufficient. Glycerol can be combined with the above

ingredients in a variable amount to formulate a capsule or tablet for taking orally.

Typically, the formulation will be designed for administration twice a day, so the

amount of Vitamin D will typically not exceed 50 IU per dosage unit.

Example

An example will be given of an embodiment of the present invention. For this

example, pearl powder in powder form (super-fine Nano Tec Pearl Powder with an

average particle diameter size of lμm) was purchased from Lucoral Inc. and astaxanthin

in solid form, Vitamin D in solid form, bilberry extract in solid form, and glycerol were

purchased from Sigma-Aldrich, Inc.

The ingredients were then combined as follows: 250mg super-fine pearl

powder; 3.3mg astaxanthin; lOOmg bilberry extract; 1.25μg of Vitamin D and 500mg

glycerol were placed in a glass flask and homogenized with a magnetic stirrer. The

temperature was kept at about 5O 0 C using a hot water bath. The ingredients were

mixed until a thick syrup-like liquid was produced. This liquid was poured into a

capsule for oral consumption.

To prove the effects of the present invention, the above formulated capsules

were taken by 10 subjects (Sub), male (M) and female (F) (Sub 1 to Sub 10; M and F

below) ranging from 30"s to 50's in age, for a period of two months. Each subject

took approximately two capsules a day. The results are summarized below in the table.

hi the clinical trials, nine categories (categ.) were measured:

White = feels white/more transparent

Finer = feels finer

AS age spots vanished/fading

Firm = feels firmer

Moist = feels more moist

Mk-up = makeup spreads better

LessC = needs less concealer

Body = entire body feels whiter

Eyes = eyes feel less strained

Table

The following is a summary of the clinical trials:

• • = very much

• = somewhat

Several visual observations were made about the clinical trials. First, age

spots on older subjects, male and female, became smaller in size (the area the covered

on the face) and they also became lighter or more white. Second, other types of spots

on the skin, perhaps due to sun damage or other skin problems, became smaller, whiter

and some completely disappeared. Thus the total number of spots on the skin of the

face became fewer. When spots on the face disappeared, the skin color returned to a

smoother, consistent color from a more motley color.

In the clinical trials, it took one month to two months for the results to appear,

which coincides with the normal skin-regeneration cycle of 28 days to 60 days. A

person should take the invention daily as long as the person wishes to benefit from its

effectiveness. Dosage interruption or stoppage may cause undesired conditions, such

as age spots and dry skin, to reappear.

We have now found that effective treatment and prevention of normal, but

cosmetically undesirable, skin conditions, due to chronoageing or photoageing, such as

wrinkles, lines, sagging, hyperpigmentation and age spots, may be obtained through the

use of the present invention for the skin. We have also found that the use of such

cosmetic compositions advantageously provides further skin care benefits in addition to

anti-ageing such as soothing sensitive and/or irritated skin, controlling oil/sebum

secretion and for lightening the skin.

hi addition the present invention can be used to prevent osteoporosis. If

dosage units of the present invention are taken regularly, for example once or twice a

day for 3 months, 6 months, 1 year, 2 years, 5 years or more, the invention can

effectively deliver calcium to the body, which will help prevent osteoporosis.

While there have been illustrated and described several embodiments of the

present invention, it will be apparent that various changes and modifications thereof will

occur to those skilled in the art. It is intended in the appended claims to cover all such

changes and modifications that fall within the true spirit and scope of the present

invention.