Active substance-contained gel composite based on multilayer liquid crystal framework and method for producing same

A technology of gel composition and active substances, which is applied in the direction of drug combination, active ingredients of heterocyclic compounds, drug delivery, etc., and can solve problems such as accelerated transdermal water loss, skin vulnerable to external attacks, and low surfactant content , to achieve the effect of reducing skin irritation, improving moisturizing effect, and reducing the area of ​​administration

Active Publication Date: 2012-08-01
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above patents all need to be taken daily and for a long time, which cannot solve the shortcomings of poor compliance and high clinical drop-out rate of AD patients
Chinese patent CN101167697A discloses a long-acting sustained and controlled release composition of donepezil compound and its preparation method, but all of them are injection or oral preparations, which also have the above-mentioned defects
[0006] Chinese patent CN101460156B authorizes a patch-like transdermal therapeutic system containing donepezil with an adhesive as the matrix, but the closed patch is used for long-term medication, the patch area is large, and the skin tolerance is poor. Easy to precipitate in pressure sensitive adhesive
[0007] And the semi-solid composition that adopts

Method used

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  • Active substance-contained gel composite based on multilayer liquid crystal framework and method for producing same
  • Active substance-contained gel composite based on multilayer liquid crystal framework and method for producing same
  • Active substance-contained gel composite based on multilayer liquid crystal framework and method for producing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Prescription: (percentage by weight)

[0051]

[0052]

[0053] Preparation:

[0054] (1) Heat and melt polyoxyethylene polyoxypropylene block polymer, triacetin, and liquid paraffin at 75°C to obtain phase A;

[0055] (2) Swell PEO in water for 24 hours to obtain phase B;

[0056] (3) Dissolving donepezil hydrochloride in aqueous ethanol solution and mixing to obtain phase C;

[0057] (4) pyridoxamine hydrochloride, methylparaben and sodium hydroxide solution are mixed to obtain phase D;

[0058] At 25°C, add phase C to phase B, stir at 5000 rpm for 2 hours, mix and disperse to obtain a drug-containing hydrogel;

[0059] When the temperature drops to 35°C, add phase A to the above drug-containing hydrogel, stir at 20 rpm for 1 hour, and emulsify to form a liquid crystal gel;

[0060] Then add phase D and stir at 20 rpm for 30 minutes to obtain a gel composition based on a multilayer liquid crystal skeleton and containing active substances.

Embodiment 2

[0062] Prescription: (percentage by weight)

[0063]

[0064] Preparation:

[0065] (1) Heat and melt OW 340B, lauryl lactate, and liquid paraffin at 75°C to obtain phase A;

[0066] (2) Carbopol was swelled in water for 10 hours to obtain phase B;

[0067] (3) Dissolving donepezil hydrochloride in aqueous ethanol solution and mixing to obtain phase C;

[0068] (4) Sodium metabisulfite, ethylparaben and triethanolamine are mixed to obtain phase D;

[0069] At 35°C, add phase C to phase B, stir at 500rpm for 0.5 hours, mix and disperse to obtain a drug-containing hydrogel;

[0070] When the temperature drops to 20°C, add Phase A to the above drug-containing hydrogel, stir at 60 rpm for 0.5 hours, and emulsify to form a liquid crystal gel;

[0071] Then add phase D and stir at 60 rpm for 10 to obtain a gel composition based on a multilayer liquid crystal skeleton and containing active substances.

Embodiment 3

[0073] Prescription: (percentage by weight)

[0074] Arlatone LC 15%, isopropyl myristate 0.5%, liquid paraffin 15%, E-INSPIRE 343 (acrylate and acrylate copolymer) 1.5%, water 27%, donepezil hydrochloride 10%, absolute ethanol 27%, Sodium metabisulfite 1%, ethylparaben 1%, 2% sodium hydroxide solution 2%. The preparation method is the same as in Example 1.

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PUM

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Abstract

The invention discloses an active substance-contained gel composite based on a multilayer liquid crystal framework and a method for producing the same, wherein the gel composite comprises the following components in percentage by weight: 0.1-35% of liquid crystal gel surfactant, 0.2-30% of permeable skin penetration enhancer, 0.5-30% of liquid paraffin, 0.1-20% of gel host material, 3-90% of water, 0.1-15% of active substance and 3-90% of ethanol solution. The active substance-contained gel composite based on the multilayer liquid crystal framework not only has better efficiency, but also can reduce the medicine taking frequency, so the compliance of a user is increased; and meanwhile, a permeable skin way avoids the first-pass effect after the medicine is orally taken and then passes by gastrointestinal tract and liver, so higher bioavailability is obtained.

Description

technical field [0001] The invention relates to a gel composition based on a multilayer liquid crystal skeleton containing active substances and a preparation method. Background technique [0002] Alzheimer's disease, also known as Alzheimer's disease (AD), is a primary degenerative encephalopathy that occurs in old age and early old age, and its characteristic pathological changes are cerebral cortex atrophy, accompanied by β-Amyloid deposition, neurofibrillary tangles, loss of number of large memory neurons, and formation of senile plaques. The daily life ability of AD patients is reduced, which brings endless pain and troubles to themselves and the people around them. The average survival period of AD patients is 5.5 years. After cardiovascular disease, cerebrovascular disease and cancer, AD has become the "fourth killer" of the health of the elderly. In the near future, our country will enter an aging society, accompanied by a problem that cannot be ignored - the incid...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/445A61K47/44A61P25/28
Inventor 罗华菲侯惠民王浩武余波陈纯朱壮志马建芳
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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