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Tretinoin ethosomes gel and preparation method thereof

A technology of tretinoin and alcohol body, which is applied in the fields of pharmacy, cosmetic medicine and medicine, can solve the problems of small irritation of tretinoin alcohol body, poor transdermal absorption performance, easy to cause skin allergies, etc., so as to avoid skin irritation. Allergy, good fluidity, enhanced transdermal penetration effect

Active Publication Date: 2015-10-21
西安艾尔菲生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a retinoic acid ethosome gel, the retinoic acid ethosome gel in the gel has little irritation, small particle size, high permeability, high encapsulation efficiency, and solves the problem of existing Poor transdermal absorption of retinoic acid topical preparations and easy to cause skin allergies during use

Method used

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  • Tretinoin ethosomes gel and preparation method thereof
  • Tretinoin ethosomes gel and preparation method thereof
  • Tretinoin ethosomes gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Step 1, weigh 1000mg lecithin, 200mg vitamin E and 50mg retinoic acid and dissolve them in 32ml of dehydrated ethanol, in a light-proof environment, under the condition of a water bath at 30°C, stir at a speed of 800r / min for 15min to make it completely dissolved. Then transfer the solution into a round-bottomed flask, and carry out rotary evaporation of the solvent at 30° C. and a pressure of 0.1 MPa, the rotation speed is 35 r / min, and the time is 20 minutes to obtain a lipid film;

[0036]Step 2, weigh 200mg Tween-80, and dissolve it in 200ml of 10% ethanol aqueous solution (containing 20ml of absolute ethanol and 180ml of distilled water) to obtain a mixed solution; slowly add the mixed solution to the film obtained in step 1 In the process, after the film is completely dissolved; magnetic stirring is carried out under normal temperature conditions, the stirring speed is 800r / min, and the time is 60min to obtain a crude tretinoin ethosome suspension;

[0037] Step ...

Embodiment 2

[0042] Step 1, weigh 3500mg lecithin, 437mg vitamin E and 100mg retinoic acid and dissolve them in 40ml of dehydrated ethanol, in a light-proof environment, under the condition of a water bath at 35°C, stir at a speed of 900r / min for 12min to make it completely dissolved. Then transfer the solution into a round-bottomed flask, and carry out rotary evaporation of the solvent at 35° C. and a pressure of 0.15 MPa, with a rotation speed of 40 r / min and a time of 15 minutes to obtain a lipid film;

[0043] Step 2, weigh 700mg Tween-80, dissolve it into 110ml of 25% ethanol solution (containing 27.5ml of absolute ethanol, 82.5ml of phosphate buffer solution with pH=6.8), to obtain a mixed solution; The mixed solution was slowly added to the film obtained in step 1, and after the film was completely dissolved; magnetic stirring was carried out under normal temperature conditions, the stirring speed was 900r / min, and the time was 50min to obtain a crude tretinoin ethosome suspension; ...

Embodiment 3

[0049] Step 1, weigh 5000mg lecithin, 500mg vitamin E and 100mg retinoic acid and dissolve them in 45ml of absolute ethanol solution, and stir at a speed of 1000r / min for 10min in a light-proof environment at a water bath condition of 40°C to make It is completely dissolved, and then the solution is transferred into a round bottom flask, and the solvent is rotated to evaporate the solvent at 40°C and the pressure is 0.1MPa, the rotation speed is 45r / min, and the time is 10min to obtain a lipid film;

[0050] Step 2, weigh 1000mg Tween-80, and dissolve it in 67ml of 40% ethanol aqueous solution (which contains 30ml of absolute ethanol and 37ml of deionized water) to obtain a mixed solution; slowly add the mixed solution to the obtained product in step 1 In the film, after the film is completely dissolved; magnetic stirring is carried out under normal temperature conditions, the stirring speed is 1000r / min, and the time is 40min to obtain a crude tretinoin ethosome suspension;

...

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Abstract

The invention discloses tretinoin ethosomes gel. The particle size of a tretinoin ethosomes in the gel is 130200 nm, and the encapsulation efficiency of the tretinoin ethosomes is higher than 90%. The invention further discloses a preparation method of the gel. The preparation method comprises the specific steps of preparing a coarse tretinoin ethosomes suspension and conducting ultrasonic processing on the coarse tretinoin ethosomes suspension, using 0.22 microns of filter membrane to perform filtration so as to obtain the tretinoin ethosomes, preparing a gel body, mixing the tretinoin ethosomes and the gel body, and performing development to obtain the tretinoin ethosomes gel. The mode that the ethosomes is adopted to wrap tretinoin brings better stability and transdermal absorption compared with the mode that a lipidosome is adopted to wrap the tretinoin, the prepared tretinoin ethosomes gel is an externally-used transdermal delivery preparation, the transdermal permeation effect can be improved while skin irritation is reduced, and a certain amount of permeation promoting agent is contained in the gel, so that the transdermal permeation effect of the tretinoin ethosomes gel is further improved.

Description

technical field [0001] The invention belongs to the technical fields of medicine, pharmacy and cosmetic medicine, and specifically relates to a retinoic acid ethosome gel; the invention also relates to a preparation method of the retinoic acid ethosome gel. Background technique [0002] Acne is a chronic inflammatory skin disease of the pilosebaceous unit, and its clinical manifestations are characterized by pleomorphic skin lesions such as comedones, papules, pustules, and nodules on the face. The occurrence of acne is mainly closely related to factors such as excessive sebum secretion, pilosebaceous gland duct blockage, bacterial infection and inflammatory response. Although acne does not affect the physiological functions of the human body, it affects people's appearance and involves people's face. It is very important for beauty lovers to have smooth and undamaged skin. In the field of medicine, tretinoin is the first choice of topical drugs for acne treatment. [0003...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/127A61K31/19A61P17/10
Inventor 胡春梅刘艳王静李荣
Owner 西安艾尔菲生物科技有限公司
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