Slow release vehicles for minimizing skin irritancy of topical c

Details Slow release vehicles for minimizing skin irritancy of topical c Slow release vehicles for minimizing skin irritancy of topical c

1992-01-21

1998-02-24

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

514859, 514944, 424 7802, A61K 3120, A61K 3178

Patent

active

057212759

DESCRIPTION:

BRIEF SUMMARY
This application is the national share of PCT/US90/03219, filed Jun. 9, 1990, U.S. Ser. No. 07/362529, filed Jun. 7, 1989 abandoned and Ser. No. 07/429051, filed Oct. 30, 1989, abandoned.


FIELD OF THE INVENTION

The invention relates to stabilized, slow-release vehicles for normally irritating, non-water soluble active ingredients for topical application to the skin. More particularly, the invention is directed to aqueous emulsion formulations of retinoids for topical application to individuals who are sensitive to retinoids in other vehicles.


BACKGROUND OF THE INVENTION

Topical retinoids have been widely used for multiple cutaneous disorders, as reported in A. Haas et al. "Selected Therapeutic Applications of Topical Tretinoin," JAAD, 15:870 (1986) (See Table I below). In many instances, the application of tretinoin has alleviated or induced remission in many such conditions, although these disorders reflect a variety of pathogenic mechanisms.


TABLE I ______________________________________ Selected Therapeutic Application of Topical Tretinoin ______________________________________ Disorders with altered keratinization Acneiform follicular, or nevoid Nevus comdeonicus Senile comedones Steroid folliculitis Pseudofolliculitis Fox-Fordyce disease Hair casts Monilethrix Alopecia Thrichiostasis spinulosa Linear verrucous nevus Ichthyosiform Epidermolytic hyperkeratosis (congenital ichthyosiform erythroderma) Ichthyosis vulgaris Lamellar ichthyosis X-linked ichthyosis Psoriasiform, hyperkeratotic, or dyskeratotic Acanthosis and pseudoachanthosis nigricans Callosites Keratosis follicularis (Darier's) Keratosis palmaris et plantaris Kyrle's disease Psoriasis Reactive perforating collagenosis Infectious/inflammatory disorders Molluscum contagiosum Flat warts Plantar warts Tinea versicolor Leg ulcers Keloids and hypertrophic scars Mucocutaneous disorders Geographic tongue Lichen planus Leukoplakia Xerophthalmia (dry eye) Hairy leukoplakia Pigmentation disorders Ephelides Melasma Postinflammatory hyperpigmentation Malignant and premalignant disorders Actinic keratoses, photoaging Keratoacanthomas Melanomas Certival dysplasis Basal cell epithelioma ______________________________________
It has been demonstrated that prolonged topical application of Vitamin A acid (tretinoin or all-trans retinoic acid) is effective in the treatment of acne (See U.S. Pat. No. 3,729,568 and Kligman, A. M., "Topical Vitamin A Acid in Acne Vulgaris," Arch. Derm., 99: 469-476 (1969)). Kligman utilizes a composition in which Vitamin A acid is dispersed in a water miscible (substantially oil- and fat-free) liquid carrier having high solvating action. The topical application of this Vitamin A acid composition causes irritation of the skin in the treated areas. A presently available gel form with alcohol base or cream formulation also causes irritation. (See U.S. Pat. Nos. 3,906,108 and 4,247,547.)
A cream formulation of tretinoin is presently approved and is commercially available from Ortho Pharmaceutical Company under the trademark RETIN-A. It contains a therapeutically effective amount of tretinoin, a hydrophobic material selected from the liquid and solid fatty acids, fatty alcohols, fatty acid esters, pharmaceutical grades of waxes and hydrocarbons, the latter ranging from liquids through semisolids, such as petrolatum, to solids, and the like, a non-ionic emulsifier, xanthan gum, a preservative, an antioxidant and water. This formulation is more generally acceptable in a low dose 0.025% formulation, but it is still unacceptable to certain individuals with sensitive skin for continued daily applications.
Furthermore, the above tretinoin cream is relatively dense and pasty, and the pharmaceutical base is not elegant. The necessity to stabilize the cream with xanthan gum and to apply daily or twice daily a fatty substrate to the skin leaves a greasy film with a pasty residue.
Therefore, the problem has been to find vehicl

REFERENCES:
patent: 3729568 (1973-04-01), Kligman
patent: 3906108 (1975-09-01), Feltig
patent: 4021573 (1977-05-01), Lee
patent: 4214000 (1980-07-01), Papa
patent: 4247547 (1981-01-01), Marks
patent: 4950475 (1990-08-01), Vishnupad et al.
The Merck Index, 1976, Ninth Edition, p. 7961 Published by Merck & Co, Ind. Rahway, N.J., U.S.A..

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