MXPA92006239A - Treatment of acne or of pseudo folliculitis barbae - Google Patents
Treatment of acne or of pseudo folliculitis barbaeInfo
- Publication number
- MXPA92006239A MXPA92006239A MXPA/A/1992/006239A MX9206239A MXPA92006239A MX PA92006239 A MXPA92006239 A MX PA92006239A MX 9206239 A MX9206239 A MX 9206239A MX PA92006239 A MXPA92006239 A MX PA92006239A
- Authority
- MX
- Mexico
- Prior art keywords
- treatment
- acne
- inhibitor
- beard
- pseudofolliculitis
- Prior art date
Links
- 206010000496 Acne Diseases 0.000 title claims abstract description 23
- 208000001818 Pseudofolliculitis Barbae Diseases 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 17
- 239000003112 inhibitor Substances 0.000 claims abstract description 16
- 210000003491 Skin Anatomy 0.000 claims abstract description 7
- 102000028557 Ornithine Decarboxylase Human genes 0.000 claims abstract description 6
- 108091022025 Ornithine Decarboxylase Proteins 0.000 claims abstract description 6
- 239000000203 mixture Substances 0.000 claims description 14
- VLCYCQAOQCDTCN-UHFFFAOYSA-N Eflornithine Chemical group NCCCC(N)(C(F)F)C(O)=O VLCYCQAOQCDTCN-UHFFFAOYSA-N 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 6
- 102000004190 Enzymes Human genes 0.000 claims description 5
- 108090000790 Enzymes Proteins 0.000 claims description 5
- 230000003000 nontoxic Effects 0.000 claims description 4
- 231100000252 nontoxic Toxicity 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002588 toxic Effects 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002280 anti-androgenic Effects 0.000 description 4
- 239000000051 antiandrogen Substances 0.000 description 4
- 231100000486 side effect Toxicity 0.000 description 4
- 229960003104 Ornithine Drugs 0.000 description 3
- 229940030495 ANTIANDROGEN SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Drugs 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- LZSOOHLAZHOTHJ-GUCLMQHLSA-N Topterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@](CCC)(O)[C@@]1(C)CC2 LZSOOHLAZHOTHJ-GUCLMQHLSA-N 0.000 description 2
- SHGAZHPCJJPHSC-NWVFGJFESA-N Tretinoin Chemical compound OC(=O)/C=C(\C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NWVFGJFESA-N 0.000 description 2
- 229960001727 Tretinoin Drugs 0.000 description 2
- -1 alpha-ethynyl ornithine Chemical compound 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 230000000750 progressive Effects 0.000 description 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
- 150000004492 retinoid derivatives Chemical class 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- WZNYARWXMBARIC-AOHMHTKGSA-N 17β-Acetoxy-4α,5-cyclo-a-homo-b-nor-5α-androst-1-en-3-one Chemical compound O=C([C@@H]1C[C@@]11C2)C=C[C@]1(C)[C@@H]1C2[C@@H]2CC[C@H](OC(=O)C)[C@@]2(C)CC1 WZNYARWXMBARIC-AOHMHTKGSA-N 0.000 description 1
- 229940061720 Alpha Hydroxy Acids Drugs 0.000 description 1
- 229940064005 Antibiotic throat preparations Drugs 0.000 description 1
- 229940083879 Antibiotics FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Drugs 0.000 description 1
- 229940042052 Antibiotics for systemic use Drugs 0.000 description 1
- 229940042786 Antitubercular Antibiotics Drugs 0.000 description 1
- 239000004342 Benzoyl peroxide Substances 0.000 description 1
- 229960001616 Chlormadinone Acetate Drugs 0.000 description 1
- QMBJSIBWORFWQT-DFXBJWIESA-N Chlormadinone acetate Chemical compound C1=C(Cl)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 QMBJSIBWORFWQT-DFXBJWIESA-N 0.000 description 1
- WDFKMLRRRCGAKS-UHFFFAOYSA-N Chloroxine Chemical compound C1=CN=C2C(O)=C(Cl)C=C(Cl)C2=C1 WDFKMLRRRCGAKS-UHFFFAOYSA-N 0.000 description 1
- 230000037250 Clearance Effects 0.000 description 1
- 229960000978 Cyproterone Acetate Drugs 0.000 description 1
- UWFYSQMTEOIJJG-FDTZYFLXSA-N Cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 description 1
- 206010012455 Dermatitis exfoliative Diseases 0.000 description 1
- SZXQTJUDPRGNJN-UHFFFAOYSA-N Dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 1
- 208000004526 Exfoliative Dermatitis Diseases 0.000 description 1
- 229940065521 Glucocorticoid inhalants for obstructive airway disease Drugs 0.000 description 1
- 229940093922 Gynecological Antibiotics Drugs 0.000 description 1
- OMPJBNCRMGITSC-UHFFFAOYSA-N Incidol Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 description 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 1
- 229940067631 Phospholipids Drugs 0.000 description 1
- RUOJZAUFBMNUDX-UHFFFAOYSA-N Propylene carbonate Chemical compound CC1COC(=O)O1 RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 description 1
- 206010037888 Rash pustular Diseases 0.000 description 1
- 229940002683 Retin-A Drugs 0.000 description 1
- SHGAZHPCJJPHSC-YCNIQYBTSA-N Retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 1
- LXMSZDCAJNLERA-ZHYRCANASA-N Spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 1
- 229940037128 Systemic Glucocorticoids Drugs 0.000 description 1
- 229940024982 Topical Antifungal Antibiotics Drugs 0.000 description 1
- 210000003934 Vacuoles Anatomy 0.000 description 1
- 229940046009 Vitamin E Drugs 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000001280 alpha hydroxy acids Chemical class 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 235000019400 benzoyl peroxide Nutrition 0.000 description 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 1
- 230000003115 biocidal Effects 0.000 description 1
- 238000005352 clarification Methods 0.000 description 1
- 230000035512 clearance Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000012050 conventional carrier Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000000824 cytostatic agent Substances 0.000 description 1
- 201000004624 dermatitis Diseases 0.000 description 1
- 231100000406 dermatitis Toxicity 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 229940079866 intestinal antibiotics Drugs 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000003211 malignant Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229940005935 ophthalmologic Antibiotics Drugs 0.000 description 1
- 239000002818 ornithine decarboxylase inhibitor Substances 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 201000004681 psoriasis Diseases 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 229960002256 spironolactone Drugs 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 150000003712 vitamin E derivatives Chemical class 0.000 description 1
- 238000004018 waxing Methods 0.000 description 1
- 239000010497 wheat germ oil Substances 0.000 description 1
Abstract
Patients suffering from acne and/or pseudofolliculitis barbae are treated by applying to the skin of the patient an inhibitor of ornithine decarboxylase.
Description
"METHOD TO PRODUCE A USEFUL COMPOSITION FOR THE TREATMENT OF ACNE"
Inventors: DOUGLAS SHANDER, North American, domiciled at 16112 Howard Landing Drive, Gaithersburgh, Maryland, E.U.A .; F. EUGENE HARRINGTON, North American, domiciled in Address New Market, Maryland, E.U.A. and MARY CLAIRE HITMORE, North American, domiciled at 1 Vista Avenue, Lynchburg, Virginia, E.U.A.
Causaire: THE GILLETTE COMPANY, Delaware State Corporation, E.U.A. domiciled in Prudential Tower Building, Boston, Massachusetts, E.U.A.
EXTRACT OF THE INVENTION
The present invention relates to a process for treating patients suffering from acne or pseudofolululitis of the beard, which comprises applying to the skin of the patient a composition comprising an inhibitor of the dendrimerylase of the enzyme, in a pharmacologically acceptable, non-toxic vehicle.
DESCRIPTION OF THE INVENTION
This invention relates to the treatment of acne and pseudo-folliculitis of the beard (PFB) by the local application of compositions containing materials capable of inhibiting the action of the dendronic acid deficiency of the enzyme (ODC). In a preferred embodiment of this invention, such inhibitors are applied in the presence of an anti-androgen or a retinoid. Although the exact mechanisms that lead to acne are unknown, antiandrogens, retinoic acid, steroids and antibiotics, inter alia, have been proposed in a general manner for their treatment, as described in US Patents Nos. 4,139,638; 4,161,540; 4,191,775; 4,344,943; and in the OLS patent of East Germany No. 2,840,144. The PFB is related to the elimination of hair by shaving or waxing. The same has been processed by procedures such as the use of electric hair removal machines or hair removal machines, or by local treatment with tretinoin (Retin-A), benzoyl peroxide, chlorohydroxyquinoline, chloroalkylphenoles, phospholipids in combination with a wheat germ oil and vitamin E, alpha-hydroxy acids, salicylic acid in combination with glucocorticoids and sulfur, as shown for example in U.S. Patent Nos. 4,228,163, 4,463,016; 4,525,344; 4,775,530; and 4,944,939; and in Klingman et al., Arch. Dermatol., volume 107, 551-552 (1973). Most PFB treatments, and particularly for acne, produce side effects so serious that treatment can only be justified in the most severe cases; other treatments are of limited effectiveness. The compound of 2- (difluoromethyl) ornithine (DFMO, 2-difluoromethyl-2,5-diaminopentanoic acid) and other inhibitors of ornithine decarboxylase, have been proposed for use in the treatment of cancer and certain non-malignant diseases such as erythroderma. , psoriasis, and some forms of dermatitis, etc., as described in Splinter et al., Eur. J. Cancer and Clin. Oncology, Volume 22: I-E, 61-67 (1985); McCullough et al., J. Investig. Dermatology, Volume 85, 518-521 (1985); McCullough et al., J. Investig, Dermatology, Volume 81, 388-392 (1983); Kousa et al., Acta Dermatovener (Stockholm) Volume 62, 221-224 (1982); and U.S. Patent No. 4,207,315. It has now been discovered that lo-cal administration of a nontoxic, cytostatic agent, such as 2 (difluoromethyl) -2,5-diaminopentanoic acid (d-difluoroethyl ornithine, DFMO) which inhibits the decarboxylase activity of ornithine of the enzyme, can be used to effectively improve or to effectively control acne and / or PFB in patients, without side effects or with unwanted, side effects. The DFMO can be used in combination with a locally active sebosuperative agent, such as an antiandrogen or a retinoid, to take advantage of the benefits of such agents for treatment. Among the preferred inhibitors of ornithine decarboxylase, in addition to DFMO, which can be used in the present invention, are alpha-ethynyl ornithine.; 6-heptin-2, 5-diamine; and esters of (E) -2-fluoromethyldehydroornithine. In the choice of ODC inhibitors for use in the practice of the present invention, it is important to avoid those that have undesirable side-effects, such as 5-hexin-1,4-diamine. The ornithine decarboxylase inhibitors are employed by dissolving or dispersing them in a pharmacologically acceptable, non-toxic, conventional carrier vehicle, which may be in the form of a lotion, cream, poultice, ointment, or stick composition although the Accurate concentration of inhibitor in the carrier or carrier is not critical, it is generally desired that the composition contain from 1 to 20% inhibitor by weight, so that it can be applied to the affected areas of the skin of patients suffering from of acne or PFB, particularly to pimples or inflamed areas of the skin, at a speed of 40 to 800 micrograms per square centimeter. The composition is preferably applied only to the pustules, vacuoles or inflamed areas of the skin, although it is not necessary to avoid application to adjacent areas. Among the antiandrogens that can be used in the company of the ODC inhibitor are cyproterone acetate, chlormadinone acetate, 17-alpha-propyltestosterone, 17-alpha-allyltestosterone, alpha-alpha-alpha-trifluoro-2-methyl -4'-nitro-m-propionotoluidine, 6alfa-bromo-17beta-hydroxy-17alpha-methyl-4-oxa-5alpha-androstan-3-one, 17beta-acetoxy-4alpha, 5-cyclo-A-homo-B- nor-5alpha-androst-1 -en-3-one, and spironolactone, For minimal alterations of the other functions of the body with androgen intermediation, through systematic action, 17-alpha-propyltestosterone or 17 -alpha-aliltestosterone. The following examples will serve to further illustrate the nature of the invention without acting as a limitation on its scope.
EXAMPLE 1
Ten women suffering from moderately severe to mild degrees of acne, treat themselves twice a day for a period of 6 months with a water-based vehicle (68% water, 16% ethanol, 5% propylene glycol, 5% dipropylene glycol, 4% benzoyl alcohol, and 2% propylene carbonate) containing 10 g of DFMO per 100 ml of the total composition. The dermatological observations were recorded by a dermatologist who indicated the conditions of the skin prior to treatment, at 12 and 24 weeks after treatment, and 12 months after the suspension of treatment. Of the 10 women who are in treatment 9 showed a significant improvement in their acne condition. Of the 9 that responded, 4 showed a complete resolution of acne during the 12-week interval, and a fifth subject, for whom 12-week observation was not available, exhibited complete clarity at week 24. The 4 subjects in which acne was completely erased, showed markedly progressive improvements through the course of treatment. After ceson of treatment at 12 weeks, observations were continued on 9 of the 10 original subjects, including the 8 who responded to the treatment. This continuous after-treatment revealed that 7 of 8 exhibited a recurrence of acne after withdrawal of treatment. The total clarity or marked improvement in acne in 9 out of 10 subjects after treatment with elfluornitin and its recurrence after ceson of treatment demonstrated the efficacy of DFMO.
EXAMPLE 2
Nine women suffering from pseudofoliculi-tis treated themselves and were evaluated as described in Example 1. Five exhibited complete clarity, four of them cleared within 12 weeks. Four additional women showed progressive improvements during the 24 weeks of treatment. Of the nine women with pseudofolliculitis, six were women from group 10 of Example 1, who also suffered from acne. In the six women with both acne and PFB, three showed a complete clearance of both conditions and the other three exhibited a substantial erasure or clarification of both conditions.
It is noted that in relation to this date the best method known to the applicant to carry out the aforementioned invention is that which is clear from the present description of the invention.
Having described the invention as above, the content of the following is claimed as property
Claims (10)
1. The process for the treatment of patients suffering from acne or pseudofolliculitis of the beard, characterized in that it comprises applying to the skin of the patient a composition comprising an inhibitor of the enzyme ornithine decarboxylase, in a pharmacologically acceptable vehicle, not toxic.
2. The process according to claim 1, characterized in that the inhibitor is 2- (difluoromethyl) -2,5-diaminopentanoic acid.
3. The process according to any of claims 1 or 2, characterized in that the patients suffer from acne.
4. The process according to claim 1 or claim 2, characterized in that the patients suffer from pseudofolliculitis of the beard.
5. A method for producing a composition useful for the treatment of acne or pseudofolliculitis of the beard, characterized in that it comprises selecting an inhibitor of the ornithine decarboxylase of the enzyme, and combining the inhibitor in an effective amount for treatment with a vehicle pharmacologically acceptable, non-toxic.
6. The method according to claim 5, characterized in that it comprises using as the inhibitor 2- (difluoromethyl) -2,5-diaminopentanoic acid.
7. The method according to claim 5 or 6, characterized in that the composition produced is useful for the treatment of acne.
8. The method according to claim 5 or 6, characterized in that the composition produced is useful for treating pseudofolliculitis of the beard.
9. The novel use of an inhibitor of the ornithine decarboxylase of the enzyme, for the treatment of acne or pseudofolliculitis of the beard.
10. The novel use according to claim 9, characterized in that the inhibitor is 2- (difluoromethyl) -2,5-diaminopentanoic acid. In testimony of which I sign this in
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/785,032 US5328686A (en) | 1991-10-30 | 1991-10-30 | Treatment of acne or of pseudofolliculitis barbae |
| US07785032 | 1991-10-30 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX9206239A MX9206239A (en) | 1998-11-30 |
| MXPA92006239A true MXPA92006239A (en) | 1999-01-15 |
Family
ID=
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US5328686A (en) | Treatment of acne or of pseudofolliculitis barbae | |
| AU723723B2 (en) | Reduction of hair growth | |
| EP1614430B1 (en) | Compositions containing anti-acne agents and the use thereof | |
| US6071543A (en) | Pyridine-thiols reverse mucocutaneous aging | |
| EP0700282B1 (en) | Inhibition of hair growth | |
| US6932963B2 (en) | Treatment of skin wounds using polyenylphosphatidylcholine and alkanolamines | |
| US5962482A (en) | Method of reducing cellulite in mamalian skin | |
| AU694274B2 (en) | Compositions for the treatment of skin disorders | |
| Milton et al. | Treatment of nevus comedonicus with ammonium lactate lotion | |
| US5444091A (en) | Method of applying alpha hydroxy acids for treating striae distensae | |
| MXPA05013032A (en) | Novel dermatological composition. | |
| US5730992A (en) | Compositions for the treatment of skin disorders | |
| MXPA92006239A (en) | Treatment of acne or of pseudo folliculitis barbae | |
| US5240945A (en) | Method and compositions for treating acne | |
| JPH03118318A (en) | Synergistic depigmentation composition for skin pigmentation | |
| US5861432A (en) | Glycolic acid and tretinoin formulation for the treatment of acne | |
| MX2007014761A (en) | Composition comprising wortmannin and its topical use for reducing human hair growth. | |
| Steinsapir | The chemical peel | |
| Giam et al. | Effect of 13-cis retinoic acid on cystic acne in Singapore. | |
| Vaswani | Management of Acne Vulgaris | |
| MXPA00005078A (en) | Use of a mixture of a diol and an alpha-hydroxy acid for the treatment of hyperkeratotic skin diseases | |
| MXPA01004124A (en) | Reduction of hair growth |