Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Utility Patent
1997-05-22
2001-01-02
Jordan, Kimberly (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S578000, C514S725000, C514S734000, C514S947000
Utility Patent
active
06169110
ABSTRACT:
BACKGROUND OF THE INVENTION
Excessive sun exposure and exposure to the environment causes anatomical degradation of skin which accumulates over time. Every time the skin is photo-damaged or oxidized with therapeutic products such as benzoyl peroxide, the damage produces permanent effects on skin. Although the skin has an ability to repair such damage at an early age, with aging and the depression of the immune system, the ability of the skin to spontaneously repair itself is lost. Alterations in the skin resulting from such damage are apparent microscopically at an early age. As time goes by, the consequences of such degradation accumulate, with the effects being most pronounced at areas of excessive exposure, such as the skin around the eyes. The effects of the damage become visible to the unaided eye as more cells begin to degenerate. In adulthood, these degenerative effects may be seen clinically as blotchy hypo- and hyperpigmentation, keratoses, rhagades, (wrinkles), a general appearance of leathery skin, skin growths and finally, skin cancer. Red-haired and blond, blue-eyed individuals who are raised in the sunbelt are particularly sensitive to such skin damage.
It has been known for centuries that eating fruits and vegetables led to the improved appearance of skin. Early research showed that vitamin A was responsible for the benefits of fruits and vegetables and that it acted by stimulating new cell growth in the epithelium, producing softer, smoother skin. In the late 1930's and the early 1940's, vitamin A was synthesized and became available as a therapeutic agent. From that time forward, it has been recognized that vitamin A is an essential vitamin for the nutrient health of the skin.
In early skin treatments based on reaping the benefits of vitamin A, the vitamin was administered internally in large doses, usually in the form of an ester of vitamin A called vitamin A palmitate. However, internal administration of these esters proved toxic and produced hypervitaminosis A, a cluster of toxic symptoms such as hair loss, migraine headache, fatigue, bone pain and congenital defects.
U.S. Pat. No. 3,729,568 disclosed that repeated topical applications of vitamin A acids to areas of the skin alleviated these symptoms. Although the treatments disclosed in this patent were targeted predominately at the treatment of acne vulgaris, vitamin A became a general topical therapeutic agent well-known to the art of dermatology.
Later, U.S. Pat. No. 4,603,146 disclosed the beneficial effect of this vitamin A acid on retarding the effects of aging on skin. This patent disclosed that vitamin A acid results in a lightening of skin, diminished wrinkling and disappearance of early sun damaged spots such as actinic keratoses. However, treatment with this vitamin A acid causes excessive visible irritation and inflammation of the skin. During the initial months of this treatment, the skin exhibited an abnormal redness or erythema followed by painful, unpleasant peeling of the skin which could be severe. Large chunks of skin are sloughed from the surface, giving the appearance of peeling, or in the case of the scalp, dandruff. This is seen clinically as surface roughness along with abnormal redness. Not only is this cosmetically undesirable, but it is painfully uncomfortable to the patient. This discomfort is particularly amplified when used on skin that has been peeled from the daily use of vitamin A acid. As a consequence of this severe irritation, the use of vitamin A acid as a skin treatment has been limited and must be carefully monitored. Furthermore, the treatment is dispensed only at a physician's prescription request.
Simultaneous to these developments, Dr. Van Scott was developing alphahydroxy acids as skin care products. His initial U.S. Pat. No. 3,920,835 disclosed that the repeated topical application of alphahydroxy acids produced effects similar to those obtained with vitamin A acids. Topical administration of alphahydroxy acids produced an increase in the skin turnover, a general lightening of the skin, and a removal of skin keratoses.
The alphahydroxy acid treatments were not as effective as the vitamin A acid treatments. Using alphahydroxy acids, it was difficult to produce visible peeling and to slough out the acne impactions or to peel off the keratoses. In addition, the high concentrations of alphahydroxy acids required to produce such effects resulted in excessive burning, erosions, or even scarring when applied to the skin.
As a result of the above disclosures, it is known in the dermatologic community that either vitamin A acid or alphahydroxy acids induces skin proliferation and new cell growth. Because of the rapid stimulation of skin proliferation and new cell growth, these individual ingredients are effective in the treatment of acne and other hyperkeratotic skin conditions. Normally, the turnover of skin is 28 days for a new cell to form and then, finally, shed itself off at the surface. Both these compounds reduce this regenerative time to between 10 and 15 days. The regenerative portion of the skin, the epidermis, is doubled in thickness to compensate for this stimulation. However, the top layer of skin, the stratum corneum, is reduced from 14 layers of impacted cells to 8 or 9 layers of loosely woven cells. Deeper down in the skin, in the dermals, there is new collagen formation and new blood vessel formation puffing out the skin and reducing the visible signs of aging.
SUMMARY OF THE INVENTION
The present invention relates to improved methodologies and improved associated pharmaceutical compositions for therapeutically reducing the effects of skin damage and for the treatment of various dermatologic disorders such as acne without the abrasive and irritating characteristics of previous compounds such as vitamin A acid. Preferentially, the compositions of the present invention are applied topically in the form of lotions, including cream vehicles.
The combination of vitamin A and/or natural or synthetic derivatives of vitamin A, such as beta-carotene and retinoic acid, and alphahydroxy acids and/or hetahydroxy acid is effective for rejuvenation of human skin, treatment of skin disorders, and the general improvement of the quality and appearance of skin. Additionally, the combination provides an effective method to retard and reduce the effects of photoaging and environmental damage on skin. Particularly, the combination is effective in treating hyperkeratotic skin diseases such as acne vulgaris, disorders of keratinization such as ichthyosis, Darier's disease, acne, psoriasis and other similar conditions, early skin degenerations and precancerous conditions such as actinic keratoses, lentigos, lentigo malignas and melasma.
Preferably, the vitamin A or natural or synthetic derivative of vitamin A, such as betacarotene and retinoic acid, is covalently linked to an acid or an aldehyde through an esterbond.
Acids which can be ester linked to the vitamin A, or natural or synthetic derivative thereof, can comprise from 2-25 carbons, and can be linear, cyclic, or branched, and can be substituted or unsubstituted. Preferably the acid comprises 2-16 carbons. In especially preferred embodiments, the acid which is ester Iinked to the vitamin A or natural or synthetic derivative thereof is acetate, propionate, or pal mitate.
Preferred aldehydes which are suitable for covalent linkage to the vitamin A, or natural or synthetic derivative thereof, can comprise from 2-25 carbons, can be linear, cyclic, or branched, and can be substituted or unsubstituted. Preferably the aldehyde comprises 2-16 carbons.
The alphahydroxy acids used in the present formulations can comprise from 2-25 carbons, may be linear, cyclic, or branched, and may be substituted or unsubstituted. Preferably, the alphahydroxy acid comprises 2-10 carbons. More preferably, the alphahydroxy acid is citric acid, lactic acid, or glycolic acid.
Betahydroxy acids can also be included in the vitamin A formulation. The betahydroxy acids may comprise 2-25 carbons, may be linear, cyclic, or branched, an
Jordan Kimberly
Knobbe Martens Olson & Bear LLP
Vivant Pharmaceuticals
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