Process for dispersing adapalene in gel preparation

A gel preparation and dispersion technology, applied in the field of medicine, can solve the problems of poor preparation uniformity, poor appearance, and small batches

Inactive Publication Date: 2020-10-13
ZHAOKE GUANGZHOU OPTHALMIC DRUG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] These patents stipulate that the particle size of the preparation is less than 50um, but there is no systematic study on the particle size and pulverization process of adapalene and the detailed particle size distribution
Moreover, the dispersion processes disclosed in the above patents are small-scale stirring processes, and the batches are small, and the preparations are emulsified and dispersed after the preparation is completed. The preparations that require emulsification and dispersion are large in volume, so the emulsification and dispersion effect is not good, resulting in poor uniformity of the preparation. The appearance is poor, so the uniformity and stability of the preparations produced at this particle size cannot be guaranteed

Method used

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  • Process for dispersing adapalene in gel preparation
  • Process for dispersing adapalene in gel preparation
  • Process for dispersing adapalene in gel preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: the dispersion process of adapalene

[0028] 1. Raw material crushing and particle size control of adapalene

[0029] (1) Pulverization of adapalene raw material

[0030] Method: Adapalene was pulverized by jet mill to reach the target particle size.

[0031] Crushing parameters: Venturi tube pressure 8.0bar, annular pressure 8.0bar, feed speed 50rpm

[0032] (2) Particle size control:

[0033] Method: Take an appropriate amount of this product, and use a Malvern MS3000 laser particle size analyzer to detect it by dry method. The D50 should not be greater than 10um, and the D90 should not be greater than 30um.

[0034] 2. Dispersion process of adapalene

[0035] (1) Matrix preparation

[0036] Add 60Kg of purified water into the emulsification tank, start heating at 55±5°C, start homogenization and stirring, add 250g of methyl p-hydroxybenzoate, 10Kg of 1,2-propylene glycol, homogeneously stir for 10min, add 700g of Carbomer 980, 125g of ethyl alcohol...

Embodiment 2

[0047] 1. Raw material crushing and particle size control of adapalene

[0048] (1) Pulverization of adapalene raw material

[0049] Method: Adapalene was pulverized by jet mill to reach the target particle size.

[0050] Crushing parameters: Venturi tube pressure 9.0bar, annular pressure 9.0bar, feed speed 100rpm

[0051] (2) Particle size control:

[0052] Method: Take an appropriate amount of this product, and use a Malvern MS3000 laser particle size analyzer to detect it by dry method. The D50 should not be greater than 10um, and the D90 should not be greater than 30um.

[0053] 2. Dispersion process of adapalene

[0054] (1) Matrix preparation

[0055] Add 60Kg of purified water to the emulsification tank, start heating at 55±5°C, start homogenization and stirring, add 500g of methyl p-hydroxybenzoate 12Kg of 1,2-propylene glycol, stir for 10 minutes, add 750g of carbomer 980, 200g of ethylene glycol Disodium amine tetraacetate, homogeneously stirred for 20 minutes, ...

Embodiment 3

[0066] (1) Pulverization: After the adapalene raw material is pulverized, the D50 is not greater than 10um, and the D90 is not greater than 30um by dry method; the adapalene is pulverized with a jet mill to achieve the target particle size.

[0067] Pulverization parameters: Venturi tube pressure 10.0 bar, ring pressure 9.0 bar, feed rate 100 rpm.

[0068] (2) Matrix preparation:

[0069] Add methyl p-hydroxybenzoate and 1,2-propanediol to the purified water, stir evenly and continue heating, add Carbomer 980, disodium edetate, and stir until a uniform jelly-like matrix is ​​formed;

[0070] Specifically, add 60Kg of purified water to the emulsification tank, start heating at 55±5°C, start homogenization, stir, add 250g of methyl p-hydroxybenzoate, 10Kg of 1,2-propylene glycol, add 750g of carbomer 980, 125g of ethylenediaminetetra Disodium acetate, homogeneously stirred for 20 minutes, it was a uniform jelly-like matrix.

[0071] (3) Solution preparation:

[0072] Poloxame...

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PUM

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Abstract

The invention relates to the field of medicines, and particularly discloses a process for dispersing adapalene in a gel preparation. The process comprises the following steps: pulverizing an adapaleneraw material, and carrying out dry detection to obtain D50 of not more than 10 [mu]m and D90 of not more than 30 [mu]m; adding methyl p-hydroxybenzoate, 1,2-propylene glycol, carbomer 980 and ethylenediamine tetraacetic acid disodium salt into water, and continuously performing heating and stirring to obtain a uniform jelly-like matrix; adding poloxamer 188, propylene glycol and ethylene glycol phenyl ether into water, and performing stirring and heating to prepare a mixed solution; adding adapalene into the mixed solution, performing emulsifying at a high speed, adding emulsified material into the matrix, and fully performing stirring; and adding a triethanolamine aqueous solution, and performing homogenizing and stirring. The adapalene in the preparation prepared by the process disclosed by the invention is good in emulsifying and dispersing effects, can be used for large-scale expanded production, and has a good industrial application prospect.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a dispersion process of adapalene in a gel preparation. Background technique [0002] Adapalene is a white or off-white powder chemical. The chemical name is 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, the molecular formula is C28H28O3, the molecular weight is 412.52000, it is insoluble in water or ethanol, and slightly soluble in tetrahydrofuran. Adapalene is a drug used in dermatology, and it is clinically applicable to the skin treatment of acne vulgaris with acne, papules and pustules as the main manifestations. It can also be used to treat acne on the face, chest and back. [0003] Adapalene mainly binds to RARβ and RARγ, and has a weak binding force to RARα. In vitro, it can inhibit the glutamine converting enzyme of keratinocytes, inhibit the keratinization process, and regulate cell differentiation. Animal experiments have found that adapalene has acne-dissolving eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/10A61K47/14A61K47/32A61K47/18A61K31/192A61P17/10B01F3/08B02C19/06B01F23/70
CPCA61K9/0014A61K9/06A61K31/192A61K47/10A61K47/14A61K47/18A61K47/32A61K47/183A61P17/10B02C19/06B01F23/4105A61K47/34A61K31/7056B01F23/71B01F23/511B01F23/565B01F23/4146B01F2101/22A61K9/10A61K47/12
Inventor 刘婧李刚李小羿戴向荣殷雷凌娟
Owner ZHAOKE GUANGZHOU OPTHALMIC DRUG
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