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Compositions comprising encapsulated tretinoin

A technology of composition and retinoic acid, which is applied in the direction of drug combination, effective ingredients of hydroxyl compounds, medical preparations containing active ingredients, etc., and can solve problems such as failure of retinoic acid/BPO to produce commercial products

Pending Publication Date: 2020-03-06
SOL GEL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] This view of the medical industry explains why all previous attempts to solve the stability problem of retinoic acid / BPO (such as microencapsulation technology) have so far failed to produce commercial products

Method used

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  • Compositions comprising encapsulated tretinoin
  • Compositions comprising encapsulated tretinoin
  • Compositions comprising encapsulated tretinoin

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0086] Preparation of formulations of encapsulated ATRA (0.05%) and encapsulated BPO (3%) oil phase:

[0087] 2000.0 grams of cyclomethicone 5N, 1500.0 grams of cetyl alcohol and 1500.0 grams of mono- and diglycerides were mixed and heated to 70°C until melted. 200.0 grams of Carbopol 980NF was added and the oil phase was mixed and heated until added to the main reactor.

[0088] water box:

[0089] Weight in 50L reactor (main reactor)

[0090] 50.0 grams of EDTA disodium salt, 1000.0 grams of polyethylene glycol stearate type I, 2000.0 grams of glycerin (99.5%) and 125.0 grams of imidazolidinyl urea were dissolved in 29.0 kilograms of water. The solution was mixed and heated to 65°C until the oil phase was added to the main reactor.

[0091] E-BPO / citric acid phase:

[0092] 100.0 grams of anhydrous citric acid were added to 10,000.0 grams of a 15% encapsulated aqueous suspension of benzoyl peroxide. The suspension was mixed and heated to 45-50°C until added to the main ...

example 2

[0096] Table 1 below shows the particle size distributions of eight E-ATRA suspensions (left side of the table) and their effect on the stability of cream formulations (right side of the table). Eight cream formulations were prepared from eight E-ATRA suspensions. The difference between the various suspensions is the manufacturer of key raw materials. As can be seen from the table, the particle size distribution of the suspension affects the percentage of ATRA degradant RRT 0.44 (all-trans 5,6-epoxyretinoic acid) and in the cream formulation after 2 weeks of stability at 40°C / 75%RH. Degradation % of ATRA.

[0097] Table 1. Effect of Particle Size Distribution (PSD) on the Stability of the Corresponding Creams

[0098]

[0099] PSD - Particle Size Distribution, TZ - Time - Zero, 2w 40°C - 2 weeks at 40°C

[0100] Table 2. Stability data of E-ATRA, 0.05% and E-BPO, 3% creams after storage for 3 months, 18 months or 24 months

[0101]

[0102] Table 3. Stability data of...

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Abstract

The present application is directed to compositions comprising microcapsules comprising encapsulated tretinoin, wherein the microcapsule size is less than 50 [mu]m; and to methods of use thereof.

Description

technical field [0001] The present application relates to compositions comprising encapsulated retinoic acid. Background technique [0002] Topical retinoids are keratinization inhibitors. It works by reducing the cohesion of follicular epithelial cells. This results in the inhibition of microcomedone formation, preventing the formation of mature comedones and inflammatory lesions (Gollnick and Cunliffe, J. Am. Acad. Dermatol 2003;49:S1-38). The use of retinoids promotes normal shedding of the follicular epithelium. The action of retinoids can enhance the penetration of other topical compounds used to treat acne. [0003] BPO is a topical antiseptic commonly used for acne, which is available in combination prescription or over-the-counter (OTC). BPO has been found to be lethal to Propionibacterium acnes (P.acne) and other bacteria that may reside on the skin. So far, no bacteria have been indicated to develop resistance to BPO. BPO has also been shown to have keratolyt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/203A61P17/10
CPCA61K31/203A61K9/0014A61K9/06A61K9/107A61K9/501A61K31/202
Inventor O·托利达诺卡琳·奈曼M·埃里奇多利特·马尔科
Owner SOL GEL TECH
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