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Treatment of skin disorders with topical tapinalov-EGFR inhibitor compositions

A composition and skin technology, applied in the direction of skin diseases, drug combinations, effective ingredients of hydroxyl compounds, etc., can solve problems such as mechanisms that are not fully understood

Pending Publication Date: 2022-03-18
SOL GEL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Tapinarov is a first-in-class drug whose mechanism is not fully understood

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0112] In some embodiments, there is provided a topical composition for treating, preventing or alleviating a skin or mucosal disorder selected from the group consisting of palmoplantar psoriasis, hereditary palmoplantar keratoderma, acquired palmoplantar angle Ichthyosis, suppurative edema, ichthyosis vulgaris, hereditary ichthyosis, acquired ichthyosis, actinic keratosis, keratotic dermatosis, keratomucosal disease, Goering syndrome, nail psoriasis, curved / Inverse psoriasis, non-melanoma skin cancer and precancerous skin, mucous membrane and nail lesions, the composition comprising about 0.01% to about 10% tapinarov and a carrier suitable for topical administration. In another embodiment, the topical composition comprises from about 0.01% to about 1% w / w, from about 1% to about 3% w / w, from about 3% to about 5% w / w, or from about 5% to about Tapinarov 10% and a vehicle suitable for topical application.

[0113] In some embodiments, there is provided a topical composition ...

Embodiment 1

[0149] Preparation of Encapsulated Tapinarov (15% E-Tapinarov) Dispersed in Water Preparation of Tapinarov Dispersion and Acidic Mixture

[0150] A tapinarov dispersion was prepared by mixing 378 grams of CTAC CT-429 (Cetrimonium Chloride 30%), 6,756 grams of tapinarov, and 18,855 grams of water under high shear. The dispersion was homogenized for 60 minutes at 33°C (not to exceed 45°C).

[0151] An acid mixture was prepared using 1013 grams of hydrochloric acid (37%), 215.3 grams of anhydrous citric acid, 322.3 grams of lactic acid (90%) and 1632 grams of water.

[0152] a) Coating cycle

[0153] By adding 953 g of ultrapure (28%) sodium silicate solution under high shear to the Tapinarov dispersion prepared in step a), followed by the acid mixture prepared in step (a), Then 1675 grams of Polyquaternium-7 (3%) solution was added to the mixture and the coating cycle was started. This cycle was repeated 5 more times. After 6 cycles, the pH of the mixture was adjusted to 5.0...

Embodiment 2

[0158] Preparation of Encapsulated Tapinarov (3.06% E-Tapinarov) Dispersed in Oil

[0159] a) oil phase

[0160] 45.9 grams of tapinarov were mixed in 129.3 grams of squalane. 86.16 grams of tetraethoxysilane (TEOS) was added and the resulting mixture was ground in a ball mill using an upper propeller mixer at 5000 rpm for 10 minutes, 250 rpm for 7 minutes and then 400 rpm for 3 minutes. 140.4 g of ground tapinarov in oil were aliquoted and heated to 60°C. Add 9.0 grams of beeswax and melt in the oil phase.

[0161] b) water phase

[0162] 3.3 grams of CTAC (cetrimonium chloride) was dissolved in 490.0 grams of water at 60°C. In all examples described herein, unless otherwise stated, the term "water" refers to sterile water (USP) for irrigation.

[0163] c) Core-shell step

[0164] 124.5 g of the oil phase prepared in step (a) were added to the water phase and homogenized at 4000 rpm for 1 minute. 17.9 grams of sodium silicate ultrapure solution (28%) was added to...

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Abstract

Disclosed are topical compositions and methods of treating a skin or mucosal disease selected from the group consisting of palmoplantar psoriasis, hereditary palmoplantar keratosis, hereditary palmoplantar keratosis, or the like by topically administering to a subject a composition comprising a therapeutically effective amount of tapinalov, at least one EGFR inhibitor, or a combination of tapinalov-EGFR inhibitor as an active agent, once or twice a day. Acquired palmoplantar keratosis, purulent edema, dermatitis, ichthyosis vulgaris, hereditary ichthyosis, acquired ichthyosis, actinic keratosis, keratodermatosis, keratomucosal disease, golin syndrome, psoriasis on nails, psoriasis curvilinear / reverse type, non-melanoma skin cancer and precancerous skin, mucosal and nail lesions.

Description

technical field [0001] The present invention in some embodiments thereof relates to topical compositions and methods of treating diseases of the skin or mucosa by topical administration of compositions comprising tapinarof, at least one EGFR inhibitor, or combinations thereof as active agents. [0002] The topical composition of the present invention is useful for the treatment, prevention or alleviation of skin or mucosal disorders selected from the group consisting of palmoplantar psoriasis, hereditary palmoplantar keratoderma, acquired palmoplantar keratoderma, suppurative edema, dermatitis , Ichthyosis vulgaris, Hereditary Ichthyosis, Acquired Ichthyosis, Actinic Keratosis, Keratinous Skin Disease, Keratinizing Mucosal Disease, Goering Syndrome, Nail Psoriasis, Curved / Inverted Psoriasis disease, non-melanoma skin cancer and precancerous skin, mucous membrane and nail lesions. Background technique [0003] Tapinarov (3,5-dihydroxy-4-isopropyl-trans-stilbene) is a pharmac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61P17/00A61P17/06A61P17/12A61K31/05A61K31/517A61K31/5377A61K39/395A61K31/506A61K9/06
CPCA61P17/00A61P17/12A61K39/395A61P17/06A61K31/05A61K9/0014A61K9/501A61K31/517A61K31/5377A61K45/06A61K2039/505A61K2300/00A61K47/186
Inventor 摩西·阿金马塞尔·兹格赫尔博伊姆奥利·诺夫O·托利达诺卡琳·奈曼希拉·哈卡克德杰比
Owner SOL GEL TECH
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