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Compositions for topical application comprising benzoyl peroxide and adapalene

A technology of topical application of benzoyl peroxide, applied in the direction of active ingredients of peroxide compounds, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as scaling and itching, ATRA instability, etc.

Inactive Publication Date: 2018-05-11
SOL GEL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the two major obstacles to this combination are the instability of ATRA in the presence of BPO and serious adverse events such as erythema, irritation, burning, stinging, scaling, and itching

Method used

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  • Compositions for topical application comprising benzoyl peroxide and adapalene

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0101] According to one embodiment of the present invention, the method comprises:

[0102] (a) contacting the solid water-insoluble particulate material with a first cationic additive and an aqueous medium to obtain a dispersion of positively charged particulate material on its surface;

[0103] (b) subjecting the particulate material to a coating process comprising precipitating a metal oxide salt on the surface of the particulate material to form a metal oxide coating on the particulate material;

[0104] (b1) contacting the coated particulate material in an aqueous medium with a surface binding additive which is one or both of (i) a second cationic additive and (ii) a nonionic additive;

[0105] (b2) subjecting the granular material obtained in step (b1) to a coating process as in step (b);

[0106] (c) repeat steps (b1) and (b2) at least 3 times; and

[0107] (d) Aged metal oxide coating.

[0108] In addition, according to an embodiment of the present invention, the me...

Embodiment

[0161] In the following examples, all % values ​​referring to solutions are (w / w).

[0162] All % values ​​referring to dispersions (suspensions) are (w / w).

[0163] Unless otherwise stated, all solutions used in the following examples refer to aqueous solutions of the indicated components.

[0164] Example #1: Silica Encapsulation (Coating) of BPO

[0165] Step 1: Grinding: 110 g of 75% aqueous BPO (USP grade from Sigma, USA) was suspended in 152 g of 0.4% CTAC solution containing 0.001% silicon antifoam. BPO was ground using a rotor rotor mixer (IKA6100 operating at 15000 rpm). Grinding was stopped when the particle size distribution (PSD) of the suspension was d(0.9)≤35 μm or the temperature had reached 50°C. The final suspension was cooled to room temperature.

[0166] Step 2: Coating: During the coating process, the suspension was constantly stirred with a mechanical dissolver (60 mm, 500 RPM). The pH of the milled BPO suspension was corrected to 8 using NaOH 5...

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Abstract

The invention provides compositions comprising as active agents benzoyl peroxide (BPO) and adapalene, kits and uses thereof in methods for treating skin surface condition in a subject in need thereof.

Description

technical field [0001] The present invention relates to a composition comprising BPO and adapalene for topical application. Background technique [0002] Two of the most commonly used ingredients in topical treatments are benzoyl peroxide (BPO) and all-trans retinoic acid (retinoic acid (ATRA)), which are very effective in treating mild to moderate conditions of non-inflammatory acne. Benzoyl peroxide works by destroying P. acnes, the bacteria that cause the acne condition. It acts as an antiseptic and an oxidizing agent, reducing the number of blackheads or clogged pores. Tretinoin (ATRA) is a unique topical medication used in the treatment of acne that allows the keratin plugs of microcondone to be expelled so fewer lesions are able to rupture and cause the papules, pustules and nodules of inflammatory acne . Combination drugs of BPO and ATRA should have comedogenic and bacteriostatic effects in acne treatment. However, two major obstacles to this combination are the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P17/10A61P17/12A61K9/16
CPCA61K31/192A61K9/0014A61K9/501A61K9/5089A61K31/327A61P17/10A61P17/06A61P17/04A61K2300/00A61K9/16
Inventor 奥弗·托莱达诺阿隆·塞里-莱维克里内·奈曼奥里·诺乌
Owner SOL GEL TECH