Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/40—Peroxides

Definitions

• the present invention relates to the topical treatment of papulo-pustules (pimples) and comedones of the human face. More particularly, the invention is directed to a spot therapy for rapid drying up of the papulo-pustules, a method for reducing scarring and hyperpigmentation owing to 10 more rapid resorption of the papulo-pustules, and to spot therapy for the treatment of comedones .
• Papulo-pustules commonly known as pimples or zits
• a pustule is a soft pimple full of neutrophiles. It is yellow
• Pustules are not infections, but are non ⁇ specific inflammatory reactions involving the disruption of the lining walls of the sebaceous follicles of the face.
• a pustule ensues when a comedo ruptures, dumping horn, bacteria, yeasts, hairs and sebum into the dermis.
• a papule is a deeper, larger inflammatory reaction which is more solid, but is still mainly made up of neutrophiles. A papule is more likely to scar and leave a pigmented spot. Papules are also quite common in blacks, who
• Papules and pustules differ essentially only in degree, and both types of lesions may be covered by the term “papulo-pustules" or more simply “pimples.”
• Papulo-pustules are obvious and spring up rapidly in less than 24 hours and even overnight. They may be quite sore and tender. These pimples take about 7-10 days to resorb or dry up without treatment. However, after resorption they may leave a long-lasting red spot in whites and in blacks a dark pigmented spot (hyperpigmentation) which may last for many months. This also happens in other dark-skinned persons, such as Orientals, and is considered to be a disquieting cosmetic defect .
• Benzoyl peroxide is widely used to treat acne based on its antibacterial properties especially in suppressing P. acnes in follicles. It is applied to the entire face and is not used for spot therapy. However, its capacity to dry up existing pimples, even in 10 percent formulations, is very limited.
• Glycolic acid is popular in many cosmetics and skin care treatments as a natural fruit acid. It is also a well- known exfoliant, widely used for light peels by dermatologists. Fruit acids, such as glycolic, citric or lactic, may be helpful as topical agents for spot therapy, but must be used at 40 percent peeling concentrations, usually in a physician's office. These are the so-called alpha-hydroxy acids which are currently the rage in women's magazines. At 50-75% concentrations, glycolic acid and other fruit acids are used by dermatologists to give a full face peel. Lactic and glycolic acids at commercial OTC concentrations of 5-10 percent simply do not resolve pimples.
• Salicylic acid is a standard keratolytic in OTC products to treat comedones, and is a well-known exfoliant widely used in light peels by dermatologists. Salicylic acid also has some anti-inflammatory effect and is often incorporated into topical drugs to reduce inflammation.
• the Quinoderm patent is based upon killing P. acnes in the follicles using a cream, lotion or gel containing hydrogen peroxide and maintained at an acid pH.
• the L'Oreal patent involves an anhydrous solution of hydrogen peroxide applied to the entire face and specifically directed to killing P. acnes, the main organism in acne.
• the present invention has nothing to do with killing P. acnes.
• papulo-pustules may be rapidly resorbed by a spot therapy which comprises application to the exterior surface of the papulo-pustules of an aqueous solution comprising hydrogen peroxide and optionally at least one of a fruit acid and salicylic acid, in an amount, at a concentration and at a frequency sufficient to effect resorption of the papulo-pustules within two to three days.
• the solution contains about 3 to 6 weight percent hydrogen peroxide, with or without a fruit acid such as glycolic acid and citric acid, present in a concentration equivalent to about 2 to 4 weight percent glycolic acid, and with or without 2 to 4 weight percent salicylic acid, and may be dabbed on the papulo-pustule in an amount sufficient to wet the surface 2 to 3 times daily for 1 to 3 days.
• the method of the invention is also effective to substantially lessen or avoid hyperpigmentation and scarring after resorption of the papulo-pustules.
• Another aspect of the invention is a method for spot therapy of comedones, including both open and closed comedones, comprising topically applying to the exterior surface of the comedone an aqueous solution as described above containing hydrogen peroxide, a fruit acid and salicylic acid, said solution being applied in an amount, at a concentration and at a frequency sufficient to provide a comedolytic effect within about 7 to 20 days of therapy.
• the solution may be dabbed on the comedone in an amount sufficient to wet the surface two or three times daily for about 10 to 20 days .
• Hydrogen peroxide is a well known antiseptic and bleaching agent . It is an OTC product which can be purchased readily for disinfection and cleaning of wounds. It is generally safe and carries no risks. However, the present invention is not based upon a debridement, cleaning or disinfection action, but rather a resorption and drying up of the papulo-pustules.
• the present invention has nothing to do with the antibacterial effect of hydrogen peroxide.
• hydrogen peroxide kills P. acnes in vitro
• I have found it to be completely ineffective in vivo.
• up to 10 weight percent aqueous solutions of hydrogen peroxide have been applied to skin with acne, but no reduction of the follicular population of P. acnes has been found.
• the mode of action of hydrogen peroxide in this instance is entirely different.
• Hydrogen peroxide is not used in OTC preparations for acne.
• benzoyl peroxide does suppress P. acnes in vivo and is commercially useful .
• the oxidizing property of hydrogen peroxide is probably important in the mechanism of the present invention. After application to the skin, the site whitens and gets frothy, which is almost certainly due to the release of oxygen. The latter is a highly reactive chemical which combines quickly and avidly with skin proteins, resulting in their coagulation. This is the probable mechanism of whitening. While concentrations of hydrogen peroxide in water up to about 10 percent by weight (w/v) have been found quite effective and act very quickly to resorb the papulo-pustules, such high concentrations are unnecessary and cause too much stinging and burning. Preferably, the concentration of hydrogen peroxide in water should be about 3-6 weight percent, and more preferably about 3-5 weight percent. This is a stable solution and requires no buffering.
• hydrogen peroxide is co-formulated with one or more of the adjuvants salicylic acid and fruit acid, wherein exemplary fruit acids are glycolic acid, citric acid, lactic acid, malic acid, pyruvic acid and mixtures thereof. Glycolic acid is a preferred fruit acid.
• said co- formulation affords benefits unavailable from the use of hydrogen peroxide alone.
• the presence of one or more adjuvants serves to stabilize the hydrogen peroxide, and therefore provides a longer self-life to the composition.
• the adjuvant (s) promote penetration of the composition into the tissue, and hence promote greater therapeutic effects. Deep-seated papules and even cysts are more likely to respond to the co-formulation of the invention. It is also observed that the co-formulation promotes faster resorption of the papulo-pustules by, it is hypothesized, speeding up the drying effect of the hydrogen peroxide.
• the co-formulation is more comedolytic than a formulation lacking the adjuvants of the invention: hydrogen peroxide alone has slight, if any, comedolytic effect. It is observed that when the composition of the invention is applied daily to large, ugly open comedones (also known as blackheads), the horny plugs fall out within 7 to 14 days. Closed comedones are also receptive to the inventive method, although the treatment typically takes longer, for example, up to about 20 days. The removal of comedones by spot therapy is a considerable improvement cosmetically. Elimination of comedones is prophylactic because all the inflammatory lesions in acne develop from the rupture of comedones.
• the combination of hydrogen peroxide, fruit acid and salicylic acid can be applied to the entire face as a general treatment for acne, as well as to selected areas which tend to be more prone to infection.
• the fruit acid is glycolic acid and it is present at a concentration of about 2 to 4 weight percent.
• said fruit acid(s) should be present in an amount equivalent to about 2 to 4 weight percent glycolic acid.
• Combinations of glycolic acid and one or more other fruit acids may also be used in the inventive co-formulations, where said combinations are present in a concentration equivalent to about 2 to 4 weight percent glycolic acid.
• salicylic acid is present in a concentration of about 2 to 4 weight percent.
• each adjuvant While higher adjuvant concentrations, for example above 5%, may be used, excessive peeling may result as well as chemical burns and irritation. Thus, it is preferred to keep each adjuvant at a concentration below 5 weight percent.
• a composition having either glycolic acid or salicylic acid present in the range of about 2 to 4 weight percent is only a mild, tolerable irritant. Of course, where fruit acid(s) weaker or less effective than glycolic acid are used, concentrations of such fruit acid may be higher than 5 weight percent .
• Either fruit acid or salicylic acid may be used alone with the hydrogen peroxide, however preferably both adjuvants are co-formulated with hydrogen peroxide in order to provide optimal stability and other desirable effects.
• Glycolic acid is a preferred fruit acid.
• Salicylic acid and fruit acids such as glycolic acid, are compatible with each other and with hydrogen peroxide, so that no special means are necessary in preparing the co-formulations.
• Thickeners, such as methyl cellulose, or gelling agents can be added, if desired, to facilitate delivery to the skin.
• the aqueous hydrogen peroxide solution with or without adjuvant may be simply applied in an amount sufficient to wet the surface of the papulo-pustule. Since the pimple will immediately turn white upon application of the solution, the whitening is a good indicator of whether enough solution has been applied. That is, just enough need be applied to produce whitening of the pimple. However, an excess will do no harm, and exactitude is not required. Any appropriate means of application which will wet the surface of the papulo-pustule may be used. A cotton tipped rod or stick has been found suitable, and preferred would be a cotton or felt tipped applicator which could be carried around in a small vial in a purse or pocket, since frequent application is desirable.
• the hydrogen peroxide solution with or without adjuvant should preferably be applied by dabbing or by other means on the papulo-pustules 2 to 3 times daily for 1 to 3 days, 2 to 3 days in the case of hydrogen peroxide alone.
• the pimples immediately turn white and then progressively dry up. The rapid resorption of the pimples is not only cosmetically useful, but also encourages compliance with the spot therapy treatment, since the patient sees the whitening and can perceive the drying process taking place.
• the hydrogen peroxide solution of the invention with or without adjuvant can preferably be applied as soon as the first red spot appears, which patients readily recognize. However, fully developed papulo-pustules will also dry up quickly. One can treat 20-30 pimples at a time, but usually the patient will be treating many fewer than this. While pimples will resolve spontaneously over a period of a week or more without treatment, early application is important in order to lessen scarring and hyperpigmentation which follow tissue-destroying inflammatory reactions. • Thus, the longer the pimple remains, the greater will be the hyperpigmentation and scarring.
• Another feature of this invention is prophylaxis which rapidly converts the earliest detectable lesion, usually only a red, flat spot, into a small pustule. This can happen in as little as 1 to 2 hours. Continued applications bring about a rapid drying up of these diminutive, abortive pustules, thus reducing their sequelae.
• This spot therapy as a two-stage process: (1) rapid evolution into an abortive pimple and (2) rapid resorption.
• Application to the earliest lesions will prevent the development of a larger papulo-pustule and reduce the possibility of scarring and hyperpigmentation.
• Papulo-pustular acne is increasing in post- menopausal women, particularly as they compete in the marketplace. They need a convenient way to abort pimples and to look well groomed.
• the spot therapy of the present invention provides a convenient, swift and exact targeting of the problem pimples .
• the treatments of the present invention are applicable to all types of papulo-pustules or pimples, they have been found to be particularly useful in the spot therapy of papulo-pustules in patients suffering from adolescent acne, post-adolescent female acne, peri-menopausal acne, acne cosmetica and in rosacea.
• follicular pustules of whatever origin, including bacterial infections will also resorb quickly when treated with the solution.
• the treatments of the present invention using hydrogen peroxide in combination with the above adjuvants are also applicable to comedones, including both open and closed comedones.
• spot therapy comprising topically applying to the exterior surface of a comedone an aqueous solution containing hydrogen peroxide, fruit acid and salicylic acid according to the invention
• a comedolytic effect is observed within 7 to 20 days of therapy.
• Glycolic acid is a preferred fruit acid according to this aspect of the invention.
• Open comedones generally require about 7 to 14 days of spot therapy, while closed comedones typically require spot therapy for about 10 to 20 days in order to achieve exfoliation of the horny plugs.
• each application of solution comprises dabbing with an applicator in an amount sufficient to wet the surface of the comedone with said solution, and the inventive therapy comprises topical applications of the solution to the comedone 2 to 3 times daily.

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• 1994
  • 1994-12-15 AU AU14382/95A patent/AU1438295A/en not_active Abandoned
  • 1994-12-15 CZ CZ961781A patent/CZ178196A3/cs unknown
  • 1994-12-15 WO PCT/US1994/014536 patent/WO1995016454A1/en not_active Application Discontinuation
  • 1994-12-15 EP EP95905978A patent/EP0739209A4/de not_active Withdrawn
  • 1994-12-15 CA CA 2179188 patent/CA2179188A1/en not_active Abandoned

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