USH1551H - Topical composition and method for reducing hair loss from human scalp - Google Patents

Topical composition and method for reducing hair loss from human scalp Download PDF

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Publication number
USH1551H
USH1551H US08/132,487 US13248793A USH1551H US H1551 H USH1551 H US H1551H US 13248793 A US13248793 A US 13248793A US H1551 H USH1551 H US H1551H
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US
United States
Prior art keywords
hair
hair loss
oxendolone
hairs
months
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
US08/132,487
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English (en)
Inventor
Wakoh Tsuchiya
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from JP4510382A external-priority patent/JPS58162512A/ja
Priority claimed from JP16619482A external-priority patent/JPS5959607A/ja
Priority claimed from JP16619382A external-priority patent/JPS5959606A/ja
Application filed by Individual filed Critical Individual
Priority to US08/132,487 priority Critical patent/USH1551H/en
Application granted granted Critical
Publication of USH1551H publication Critical patent/USH1551H/en
Abandoned legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • This invention relates to a hair grower which does not exhibit undesirable side-effects such as systemic hormonal activity but has an excellent hair growing effect by topical application.
  • Testosterone male hormone produced in the testicles and adrenal gland is carried in the blood stream and reaches the sebaceous gland where it is converted to 5 ⁇ -dihydrotestosterone (5 ⁇ -DHT), a more potent male hormone, by the reductase present in the cells of the sebaceous gland.
  • 5 ⁇ -DHT 5 ⁇ -dihydrotestosterone
  • Physiological symptoms such as male pattern baldness (MPB) and seborrhea are said to develop as a result of excessive androgen stimulation due to an excessive local accumulation of testosterone.
  • MPB male pattern baldness
  • seborrhea seborrhea
  • 5 ⁇ -DHT which is produced by reduction of testosterone in these organs by an enzyme called testosterone-5 ⁇ -reductase (briefly, reductase).
  • the mechanism involved in the pathogenesis of MPB may be postulated as follows. While 5 ⁇ -DHT, which is produced in the sebaceous tissue, combines with a receptor in the sebaceous cells and acts on the nucleus to promote the growth of the cells, 5 ⁇ -DHT itself comes out of the sebaceous gland cells and is carried in the blood stream and acts on the nearby cells, i.e. hair matrix to inhibit division of the hair matrix cells and prevent growth of the hair.
  • the present inventor has made extensive investigations in order to search for a substance which has no undesirable side-effect such as systemic hormonal activity, is safe, and shows an effect of inhibiting both the activity of the reductase and the binding of 5 ⁇ -DHT with the receptor protein by topical use.
  • these investigations have led to the discovery that the above object can be achieved by employing oxendolone.
  • the present invention was accomplished based on this discovery.
  • Oxendolone which is used in this invention, is chemically known as 16 ⁇ -ethyl-17 ⁇ -hydroxy-4-estren-3-one which is available as a white or pale yellowish white, odorless powder. It is available on the market as a drug for benign prostatic hypertrophy and while it is administered intramuscularly as an aqueous suspension containing 200 mg per 2 ml (Prostetin: Trade name of Takeda Chemical Industries, Ltd., U.S. Pat. No. 3,856,829), it has never been applied as a topical agent.
  • the present hair grower contains a maximum of about 2% of oxendolone in combination with a topically applicable vehicle or carrier, and if desired with further usual additives.
  • the grower may contain more than about 0.001% of oxendolone and, more desirably, 0.05 to 0.2% thereof in the total preparation.
  • Oxendolone is practically insoluble in water but soluble, for example, in ethanol, and, therefore, aqueous ethanol containing more than 30%, preferably 50% of ethanol may be employed as a suitable vehicle.
  • Oxendolone also may be dissolved totally or partially in vegetable oils such as sesame oil, cottonseed oil, castor oil, olive oil, corn oil, peanut oil, etc., carbohydrates such as squalane, squalene, liquid paraffin, vaseline, etc., alcohols such as palmityl alcohol, hexadecyl alcohol, stearyl alcohol, oleyl alcohol, propylene glycol, polyethylene glycol, polypropylene glycol, etc., fatty acids such as myristic acid, palmitic acid, stearic acid, oleic acid, etc., or silicone oils, lanoline, etc.
  • vegetable oils such as sesame oil, cottonseed oil, castor oil, olive oil, corn oil, peanut oil, etc.
  • carbohydrates such as squalane, squalene, liquid paraffin, vaseline, etc.
  • alcohols such as palmityl alcohol, hexadecyl alcohol, stearyl alcohol, oleyl alcohol, propylene glyco
  • the hair grower of the present invention may optionally contain any of those additives normally used in hair grower or hair tonics, for example germicides such as hinokitiol, surface active agents, refreshing agents such as menthol, perfumes, antioxidants, ultraviolet absorbers, dyes, moisturizers such as urea, salicylic acid, polyglyceride glycerol, etc.
  • the present hair grower may be used in the form of a liquid as well as emulsions, ointments, etc., prepared by a conventional method, and can be applied several times (1 to 6 times) a day in an amount of about 0.5-10 ml, preferably 1-5 ml.
  • the amount and application interval may vary with the conditions of the subject and may be used in a range of 0.1 mg to 100 mg per day, preferably 1 to 5 mg per day as oxendolone.
  • the regimen of this invention prescribes rubbing 0.05 ml/cm 2 of the present drug well into the bare or downy patches of the scalp several times (1 to 6 times) a day.
  • the grower is preferably used after a shampooing. It causes no particular side effect, but its use is preferably avoided in the presence of an open wound.
  • the systemic acute toxicity of oxendolone is as follows:
  • Rate of inhibition (%) (C-t/C) ⁇ 100
  • Rate of inhibition (%) (C-t/C) ⁇ 100
  • Oxendolone or 4-androsten-3-one-17 ⁇ -carboxylic acid and hardened castor oil/40 mole E0 adduct were added to 95% ethanol, and the mixture was stirred. Then, deionized water was added to the solution and mixed to obtain a transparent liquid hair grower.
  • Oxendolone 0.5 g
  • 2.0 g of polyoxyethylene (60 moles)/hardened castor oil 10.0 g of glycerol, 10.0 g of dipropylene glycol, 5.0 g of 1,3-butylene glycol, and 5.0 g of polyethylene glycol 1500 were dissolved by heating at 60° C.
  • Cetyl isooctanoate (10.0 g), 5.0 g of squalane, 2.0 g of vaseline and 2.0 g of propyl p-oxybenzoate were dissolved by heating at 60° C. (B).
  • Liquid paraffin (5.0 g), 5.5 g of cetostearyl alcohol, 5.5 g of vaseline, 3.0 g of glyceryl monostearate, 3.0 g of polyoxyethylene (20 moles) 2-octyl dodecyl ether, 0.05 g of vitamin E acetate, 0.3 g of propyl p-oxybenzoate and 0.05 g of a perfume were dissolved by heating.
  • MPB represents male pattern baldness.
  • FIGS. 1-6 depict clinical studies of the instant invention.
  • Prominent hair loss started 2 years ago, and marked hair loss occurred during the summer to fall of 1981, causing recession of the hairline in the anterior portions of the calvarium. He was examined at the Department of Dermatology, Kyoto University Hospital for about 2 months and was instructed to apply about 2 ml of the solution 1 to the affected area once a day at bedtime. As a result, the soft hairs in the borders became harder, and objectively also, the hairline at the anterior portions definitely descended.
  • Alopecia areata 29-year old female, living in Nagaokakyo City.
  • the hairline in the anterior region started to recede at the age of 21. Hair loss seemed prominent in the fall to winter season. He was examined at the Department of Dermatology, Kyoto University Hospital on Feb. 9, 1982. After he applied about 2 ml the solution 1 to the anterior region once a day for about 1 month, growth of new soft hairs in the same region became prominent. No side effect was observed.
  • the hair in the parietal portion was thin because of the scar of a trauma he received to the head in his childhood. For this reason he used to wear a wig.
  • the hair from the frontal to parietal portions became thinner as a whole about 5 years ago, and he was examined at the Dept. of Dermatology, Kyoto University Hospital on Jul. 22, 1982. He received 2 g each of cream 1 and embrocated it into the affected area 1-2 times a day. About one month later, a decrease in hair loss and regrowth of soft hairs were observed. When he visited the hospital about 4 months later his hair appeared thicker, and he told us that hardly any hairs adhered to his wig any more. He is under follow-up, and no side effect has been seen.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
US08/132,487 1982-03-20 1993-10-06 Topical composition and method for reducing hair loss from human scalp Abandoned USH1551H (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US08/132,487 USH1551H (en) 1982-03-20 1993-10-06 Topical composition and method for reducing hair loss from human scalp

Applications Claiming Priority (14)

Application Number Priority Date Filing Date Title
JP4510382A JPS58162512A (ja) 1982-03-20 1982-03-20 若禿及び円型脱毛の発毛剤
JP57-45103 1982-03-20
JP57-166193 1982-09-24
JP16619482A JPS5959607A (ja) 1982-09-24 1982-09-24 養毛料
JP16619382A JPS5959606A (ja) 1982-09-24 1982-09-24 老人性，脂漏性および「こう」糖性の脱毛症治療剤
JP57-166194 1982-09-24
US47592483A 1983-03-16 1983-03-16
US65987084A 1984-10-12 1984-10-12
US9176987A 1987-08-27 1987-08-27
US42652589A 1989-10-24 1989-10-24
US55941690A 1990-07-25 1990-07-25
US72986191A 1991-07-10 1991-07-10
US89959392A 1992-06-18 1992-06-18
US08/132,487 USH1551H (en) 1982-03-20 1993-10-06 Topical composition and method for reducing hair loss from human scalp

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
US89959392A Continuation 1982-03-20 1992-06-18

Publications (1)

Publication Number Publication Date
USH1551H true USH1551H (en) 1996-06-04

Family

ID=27292115

Family Applications (1)

Application Number Title Priority Date Filing Date
US08/132,487 Abandoned USH1551H (en) 1982-03-20 1993-10-06 Topical composition and method for reducing hair loss from human scalp

Country Status (13)

Country Link
US (1) USH1551H (enrdf_load_stackoverflow)
AU (1) AU559145B2 (enrdf_load_stackoverflow)
BE (1) BE896213A (enrdf_load_stackoverflow)
CA (1) CA1222460A (enrdf_load_stackoverflow)
CH (1) CH657774A5 (enrdf_load_stackoverflow)
DE (1) DE3309813A1 (enrdf_load_stackoverflow)
FR (1) FR2523440A1 (enrdf_load_stackoverflow)
GB (1) GB2122081B (enrdf_load_stackoverflow)
GR (1) GR77885B (enrdf_load_stackoverflow)
HK (1) HK57789A (enrdf_load_stackoverflow)
IT (1) IT1162843B (enrdf_load_stackoverflow)
NL (1) NL8300972A (enrdf_load_stackoverflow)
SG (1) SG2489G (enrdf_load_stackoverflow)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6348348B1 (en) 1998-04-07 2002-02-19 The Carnegie Institution Of Washington Human hairless gene and protein

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102008038242A1 (de) 2008-08-18 2010-02-25 Elife Mendes Mittel und Verfahren zur Behandlung des kreisrunden Haarausfalls

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3856829A (en) * 1970-01-07 1974-12-24 Takeda Chemical Industries Ltd 16{62 -hydrocarbon substituted estrane compounds
US4272508A (en) * 1979-03-30 1981-06-09 Jurgen Tamm Cosmetics for treatment of hair and skin

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2100319C3 (de) * 1970-01-07 1974-10-31 Takeda Chemical Industries, Ltd., Osaka (Japan) Neue Östranverbindungen, ihre Herstellung und sie enthaltende Arzneimittel
US3917829A (en) * 1971-11-08 1975-11-04 Research Corp Novel methods of inhibiting the activity of testosterone 5{60 -reductase

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3856829A (en) * 1970-01-07 1974-12-24 Takeda Chemical Industries Ltd 16{62 -hydrocarbon substituted estrane compounds
US4272508A (en) * 1979-03-30 1981-06-09 Jurgen Tamm Cosmetics for treatment of hair and skin

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Chemical Abstracts (1973) vol. 79 Par. 73,914s. *
Federal Register, 21CFR Part 310 Tues Jan. 15, 1985 pp. 2190 2198. *
Federal Register, 21CFR Part 310 Tues Jan. 15, 1985 pp. 2190-2198.

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6348348B1 (en) 1998-04-07 2002-02-19 The Carnegie Institution Of Washington Human hairless gene and protein
US20030027300A1 (en) * 1998-04-07 2003-02-06 Carnegie Institution Of Washington Human hairless gene and protein
US7416731B2 (en) 1998-04-07 2008-08-26 The Carnegie Institution Of Washington Human hairless antibodies

Also Published As

Publication number Publication date
GR77885B (enrdf_load_stackoverflow) 1984-09-25
DE3309813A1 (de) 1983-10-13
IT8367316A0 (it) 1983-03-21
GB2122081A (en) 1984-01-11
AU559145B2 (en) 1987-02-26
CA1222460A (en) 1987-06-02
BE896213A (fr) 1983-09-19
FR2523440A1 (fr) 1983-09-23
HK57789A (en) 1989-07-28
FR2523440B1 (enrdf_load_stackoverflow) 1984-12-14
DE3309813C2 (enrdf_load_stackoverflow) 1992-07-02
NL8300972A (nl) 1983-10-17
SG2489G (en) 1989-06-02
GB2122081B (en) 1986-04-03
AU1257383A (en) 1983-09-22
GB8307346D0 (en) 1983-04-27
IT1162843B (it) 1987-04-01
CH657774A5 (de) 1986-09-30

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