JPH01279818A - White hair blackening agent - Google Patents

Abstract

PURPOSE:To obtain a white hair blackening agent, containing idebenone and capable of blackening white hair. CONSTITUTION:The objective substance, containing idebenone as an active ingredient and obtained by mixing the idebenone with a normally used carrier, excipient, binder, diluent, etc., and preparing a pharmaceutical by a conventional method. The idebenone is blended in an amount of 0.1-15wt.%. The agent can be prepared in the form for oral administration of granule, powder, tablet, capsule or syrup or percutaneous administration of cosmetics, such as liquid, lotion, cream or ointment. The dose thereof for an adult per day is within the range of 10-150mg idebenone and about 1/10 based on the above-mentioned dose for percutaneous administration. The chemical name of the idebenone is 6-(10-hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Field of Application) The present invention is a composition containing idebenone, which is intended to darken gray hair.

(Prior art) Idebenone has an immune promoting effect and an in vivo tissue metabolism activating effect.
134), is commercially available as an agent for improving the aftereffects of cerebral infarction, cerebral hemorrhage, decreased motivation associated with cerebral artery sequelae, emotional disorders, and language disorders.

(Problems to be Solved by the Invention) The present invention aims to turn gray hair black by administering a composition containing idebenone to the human body.

(Means for solving problems) The present invention is a hair graying agent containing idebenone.

Idebenone is a common name, its chemical structure is represented by υ, and its chemical name is 6-(10-hydroxydecyl-2,3-dimethoxy-5-methyl-1°4-benzoquinone).

The gray hair blackening agent according to the present invention can darken the gray hair of mammals including humans.

The hair blackening agent of the present invention contains idebenone as an active ingredient, and this active ingredient may be used alone or in combination with other drugs and appropriate pharmacologically acceptable additives (fillers, diluents), etc. It can be made into a suitable pharmaceutical composition or cosmetic product.

The above pharmaceutical compositions can be prepared by mixing the active ingredient with physiologically acceptable carriers, excipients, binders, diluents, for example m granules, powder 1 tablet, li! Administer orally as capsules, soft capsules, syrups, or liquids. It can be administered transdermally as a cosmetic product such as a cream or ointment.

Orally administered dosage forms, such as powders, granules, 2 tablets, 5 hard capsules, soft capsules, and syrups, include carriers and excipients conveniently used in the formulation.

It can be adjusted by known methods using binders, diluents, etc. Preferred excipients, binders.

Examples of lubricants include lactose, starch, sucrose, and magnesium stearate.

Excipients for preparing soft capsules include, for example, pharmacologically acceptable animal oils and vegetable oils.

Mineral oil and the like are used, and the active ingredients are dissolved in these oils and fats and filled into soft capsules.

Liquid, Lone Gin. Transdermal preparations such as creams and ointments use solvents and suspending agents that are well known in the pharmaceutical field.

The emulsifier 5 can be prepared by a known method using a surfactant, an ointment base, and the like. Examples of the solvent include water, ethanol, glycerin, propylene glycol, and the like. Gum Arapia as a suspending and emulsifying agent. Examples include carboxymethylcellulose, methylcellulose, and sodium alginate. As a surfactant, Tween 80 (polysorbate 80), 5p
an 60 (sorbitan monostearate) and the like. Examples of ointment bases include petrolatum, paraffin, petroleum oil, animal oil, lanolin, waxes, and macrogol.

If necessary, preservatives (eg, butyl paraoxybenzoate, benzalkonium chloride), transdermal absorption enhancers (eg, Azone, 2-pyrrolidone), etc. may be added.

Idebenone is usually included in these preparations at 0.1-15% by weight.

The dosage of the composition of the present invention varies depending on the administration method, etc., but when used orally, 1 idebenone per day for adults.
It is administered in a range of 0 to 150 mg, preferably 30 to 901 mg. When used transdermally, the amount of 171O mentioned above is about the same.

The toxicity of idebenone is low in both cases, and LD in mice
,. is 1 O,000D/kg or more.

Example! (Tablets) Idebenone 30g Lactose 74g Starch
10.6mg starch (for paste production) 5 B Magnesium stearate
0.4 mg Calcium salt of carboquine methylcellulose 5 mg Total 150 mg The above components were mixed and made into tablets according to a conventional method.

Example 2 (Dragage-coated tablet) Tablet (Example 1) 150s+g talc 30 sg gum arabic 6 mg sucrose
74 B total 260 mg The tablets prepared in Example I were coated with the above ingredients in a conventional manner to make sugar-coated tablets.

Example 3 (Fine granules) Idebenone 20 mg Lactose 680 mg Starch
300 B total 1,000 mg The above components were mixed and prepared into fine granules according to a conventional method.

Example 4 (Capsule) Idebenone 10 mg Microcrystalline cellulose 30 mg Lactose
670 mg.

Magnenium stearate 3 mg meter
110 tng The above components were mixed according to a conventional method and filled into gelatin capsules to prepare capsules.

Example 5 (Soft capsule) Idebenone 15 a+g meter
150 mg The above ingredients were mixed and encapsulated in a film consisting of gelatin, glycerin, and sorbitol preservative according to a conventional method to form soft capsules.

Example 6 (Suppositories) Idebenone 30-g Carbon number 1
Triglycerides of saturated fatty acids of 1 to 17 (hydroxyl value 1
2) 1470 mg total 1500
mg The above components were mixed and made into a suppository according to a conventional method.

Example 7 (Carbowax ointment) Idebenone 1 g Macrogol 4G0 59 g Macrogol 400
0 40 g total 1 [)Og The above ingredients were heated and dissolved to form an ointment using a conventional method.

Example 8 (White Vaseline Ointment) Idebenone 1g Saran Beeswax 5g Purified Lanolin
5g white petrolatum
89 g of the above ingredients were dissolved by heating and made into an ointment using a conventional method.

Example 9 (Cream) Idebenone 1g stearyl alcohol 8g cetanol
13g propylene glycol
to g polysorbate 80 1
．． 5 g Methyl paraoxybenzoate 0.03
g Propyl paraoxybenzoate 0.01 g Purified water Total 100 g Idebenone, stearyl alcohol, cetanol.

A cream was prepared by heating and dissolving methyl parabenzoate and propyl parabenzoate, and adding purified water, propylene glycol, and polysorbate 80 dissolved under heating.

Experimental Example 1 One dose of idebenone was given to two men and one woman (all around 70 years of age) with cerebral arteriosclerosis who had almost half white and half black hair.
Oral administration was given daily at 90a+g. Three weeks later, the hair of all three patients became darker. The ratio of black hair to gray hair was approximately 7:3.

The hair was white on top and black on the bottom.

Experimental Example 2 A woman (75 years old) with gray hair due to cerebral arteriosclerosis received 1 dose of idebenone.
89 (1 mg was administered orally every day. The patient's hair began to turn black from about 3 weeks after administration.

Experimental Example 3 One dose of idebenone was administered to a 70-year-old man with gray hair due to sequelae of cerebral infarction.
Orally administered daily at 90-g/day. Two weeks after administration, the white hair turned black.

Experimental Example 4 Both idebenone (90 g/day) and vinpocetine (15 mg/day) were orally administered daily to a man with gray hair (80 years old with speech impairment due to cerebral infarction). In the second month, my gray hair turned a little black and the hair on my head started to grow little by little.

A woman with gray hair (84 years old, cerebral infarction patient) was given idebenone (90 mg/day) and vinpocetine (+5
mg/day) were orally administered daily. From around the first month of administration, black hair was visible among the gray hair.

(Effects of the Invention) The gray hair blackening agent containing idebenone of the present invention can darken gray hair.

Agent Patent Attorney Iwa 1) Hiroshi

Claims (1)

[Claims] A gray hair blackening agent containing idebenone.