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Adapalene vesicle and preparation method thereof, and preparation containing adapalene vesicle, and preparation method thereof

A technology of adapalene and vesicles, applied in the field of pharmaceutical preparations, can solve the problems of poor skin penetration, dry skin, skin discomfort and the like

Active Publication Date: 2018-03-06
BEIJING INCREASEPHARM CORP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adapalene is almost insoluble in water, and the marketed gel drug is dispersed in the matrix in a crystalline state, which has poor transdermal effect and often has adverse reactions. The main adverse reactions are dry skin, erythema, skin allergies and skin discomfort

Method used

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  • Adapalene vesicle and preparation method thereof, and preparation containing adapalene vesicle, and preparation method thereof
  • Adapalene vesicle and preparation method thereof, and preparation containing adapalene vesicle, and preparation method thereof
  • Adapalene vesicle and preparation method thereof, and preparation containing adapalene vesicle, and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0086] 1.1 Preparation of mouse skin

[0087] Male SD rats, 240-260g, were sacrificed by dislocation of the cervical vertebrae. The hair on the abdomen and surrounding area was removed with a razor, and the rat skin of the depilated part was peeled off with dissecting scissors, and placed in normal saline to stretch out (need 2-3min), use the filter paper to spread the mouse skin naturally, place the upper cover of the transdermal cup on the peeled skin, cut the mouse skin together with the filter paper (to ensure the natural shape of the mouse skin) and cut it out of the transdermal cup For small discs with a slightly larger layer, put the small discs into the prepared saline, cut off the fat tissue and mucosal tissue in the inner layer of the mouse skin with ophthalmic curved scissors (you can also scrape with a blade), and the treated mouse skin Wash it with normal saline, store it in a watch glass with filter paper moistened with normal saline, wrap it with plastic wrap, s...

Embodiment 1

[0109] Take adapalene 7.5mg, Span 60 45mg, polyethylene glycol monostearate 225㎎, sodium stearate 37.5㎎, cholesterol 131.25mg, add it to an appropriate amount of 95% ethanol, and heat it in a water bath at 85°C. After it is completely dissolved, inject it into an appropriate amount of water, stir at a constant temperature of 85°C for 30 minutes, lower the temperature to 55°C and continue stirring for hydration, evaporate the ethanol, add water to the prescribed amount, and shake well to obtain a vesicle suspension.

[0110] Carbomer 980 100㎎ add water to swell, ethylparaben 10㎎ is dispersed with 1000㎎ 10% glycerin, anhydrous sodium sulfite 50㎎ is dissolved in water, all are added to Carbomer 980, swell together overnight, add appropriate amount of hydrogen The pH of the sodium oxide solution was adjusted to 7.3 to obtain a gel matrix.

[0111] Mix the vesicle suspension with the gel matrix and stir evenly to obtain the vesicle gel.

Embodiment 2

[0113] Take Span 80 50㎎, Tween 60 100㎎, Cholesterol 100㎎, Adapalene 0.5㎎ dissolved in an appropriate amount of dichloromethane, heated to dissolve, and the solution is ready for use; under constant temperature stirring at 15°C, take the above solution and inject it into tartaric acid buffer at a constant speed solution (pH7.2), continue stirring after adding, until dichloromethane evaporates, add tartaric acid buffer solution (pH7.2) to the full amount, and process it once with a high-pressure milk homogenizer to obtain a vesicle suspension.

[0114] Add carbomer 971 10㎎ to swell with water, 80㎎ benzyl alcohol to disperse with 1800mg of hyaluronic acid: isopropanol (1:2) mixture, add tert-butyl p-hydroxyanisole 15㎎ to dissolve in water, then add to carbomer Mu 971, co-swell overnight, add an appropriate amount of sodium hydroxide solution to adjust the pH to 7.2, to obtain a gel matrix.

[0115] Mix the vesicle suspension with the gel matrix and stir evenly to obtain the vesic...

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Abstract

The invention discloses an adapalene vesicle and a preparation method thereof, and a preparation containing the adapalene vesicle, and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The adapalene vesicle is prepared from adapalene, a nonionic surfactant and an additive, and is preferably prepared in an external application gel dosage form. According to the present invention, the transdermal adapalene delivery external application preparation has the unique advantages; with the application of the novel vesicle delivery system, the transdermal absorption of drugs can be increased, the clinical treatment effect can be enhanced, and the toxic-side effect during the oral taking can be avoided; and the preparation can be used for treating comedo, papule, pustule and other acne.

Description

technical field [0001] The invention relates to adapalene vesicles and a preparation method thereof, a preparation containing adapalene vesicles and a preparation method thereof, and belongs to the field of pharmaceutical preparations. Background technique [0002] Adapalene, whose chemical name is 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, is a pure white powdery solid with a melting point of 319-322°C. Belonging to the third generation of retinoic acid drugs, it has a good anti-inflammatory effect and has a good curative effect on the treatment of acne. [0003] Non-ionic surfactant vesicles (also known as non-ionic surfactant liposomes) are called Non-ionic surfactant based vesicles in English, or niosomes for short. It uses various non-ionic surfactants as carrier materials, and is a bilayer micro or multi-locular vesicle carrier formed by self-closing. The use of non-ionic surfactant vesicles to encapsulate drugs can reduce the destruction of drugs before r...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/10A61K47/26A61K31/192A61K9/06A61K47/32A61P29/00A61P17/10
CPCA61K9/0014A61K9/06A61K9/1273A61K31/192A61K47/10A61K47/26A61K47/32
Inventor 张保献吴珍珍仇念平
Owner BEIJING INCREASEPHARM CORP LTD
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