Preparation method of rotigotine pressure-sensitive adhesive dispersive type patch

A pressure-sensitive adhesive, dispersive technology, applied in nervous system diseases, sheet delivery, drug combination, etc., can solve problems such as the impact of percutaneous penetration that has not yet been seen, and achieve increased drug loading, easy operation, and simple method. Effect

Inactive Publication Date: 2017-03-22
SHAANXI EYOUNG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, domestic literature has reported its in vitro permeability, but it mainly focuses on the comparison between self-made patches and comme

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] A preparation method of rotigotine pressure-sensitive adhesive dispersion type patch, is characterized in that comprising the following steps:

[0016] (1) Titrate with hydrochloride solution to pH 5-8 with 0.1mol / L sodium hydroxide solution, its pKa value is 8.83, then extract with ethyl acetate, separate the organic phase and add anhydrous sodium sulfate for 12h ;

[0017] (2) After filtration, the ethyl acetate was removed by rotary evaporation, and the obtained white solid was transferred to a brown glass bottle, and placed in a vacuum drying oven. The drying temperature was 10-50°C and the pressure was 100Pa, and dried to constant weight, that is, Rotigotine original drug;

[0018] (3) Put about 50 mg of 3% pressure-sensitive adhesive weight and different types of pressure-sensitive adhesive ethyl acetate solution in a beaker, add 10 ml of ethyl acetate, stir for 2 hours to completely dissolve the drug, and let it stand for defoaming;

[0019] (4) Spread on the a...

Embodiment 2

[0021] A preparation method of rotigotine pressure-sensitive adhesive dispersion type patch, is characterized in that comprising the following steps:

[0022] (1) Titrate with hydrochloride solution to pH 5-8 with 0.1mol / L sodium hydroxide solution, its pKa value is 8.83, then extract with ethyl acetate, separate the organic phase and add anhydrous sodium sulfate for 12h ;

[0023] (2) After filtration, the ethyl acetate was removed by rotary evaporation, and the obtained white solid was transferred to a brown glass bottle, and placed in a vacuum drying oven. The drying temperature was 10-50°C and the pressure was 100Pa, and dried to constant weight, that is, Rotigotine original drug;

[0024] (3) Put about 50 mg of 3% pressure-sensitive adhesive weight and different types of pressure-sensitive adhesive ethyl acetate solution in a beaker, add 10 ml of ethyl acetate, stir for 2 hours to completely dissolve the drug, and let it stand for defoaming;

[0025] (4) Spread on the a...

Embodiment 3

[0028] A preparation method of rotigotine pressure-sensitive adhesive dispersion type patch, is characterized in that comprising the following steps:

[0029] (1) Titrate with hydrochloride solution to pH 5-8 with 0.1mol / L sodium hydroxide solution, its pKa value is 8.83, then extract with ethyl acetate, separate the organic phase, add anhydrous sodium sulfate and place it for 12h ;

[0030] (2) After filtration, ethyl acetate is removed by rotary evaporation, and the obtained white solid is transferred to a brown glass bottle, and placed in a vacuum drying oven, and the drying temperature is 10-50°C, and the pressure is 100Pa. Dry to constant weight, that is, Rotigotine original drug;

[0031] (3) Put about 50 mg of 3% pressure-sensitive adhesive weight and different types of pressure-sensitive adhesive ethyl acetate solution in a beaker, add 10 ml of ethyl acetate, stir for 2 hours to completely dissolve the drug, and let it stand for defoaming;

[0032] (4) Spread on the ...

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PUM

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Abstract

The invention relates to a preparation method of a rotigotine pressure-sensitive adhesive dispersive type patch. The preparation method is characterized by comprising the following steps that a hydrochloride solution is titrated to 5-8 in pH value through a sodium hydroxide solution with the molar concentration being 0.1 mol/L, and the pKa value of the hydrochloride solution is 8.83; and then extraction is conducted through ethyl acetate, and anhydrous sodium sulfate is added to be placed for 12 h after an organic phase is separated. The rotigotine pressure-sensitive adhesive dispersive type patch prepared through the preparation method is strong in adsorption capacity, the drug loading capacity can be increased, and the drug penetration amount of the rotigotine pressure-sensitive adhesive dispersive type patch is larger than that of a patch with a silicone pressure-sensitive adhesive as a matrix, and the preparation method is simple, easy to operate and good in economic benefit.

Description

technical field [0001] The invention relates to a preparation method of a rotigotine pressure-sensitive adhesive dispersed patch. Background technique [0002] Rotigotine is a non-ergot selective dopamine receptor agonist used for the adjuvant treatment of early and late Parkinson's disease (PD). It works by stimulating dopamine receptors in the body and simulating the neurotransmitter dopamine. Rotigotine has obvious hepatic first-pass effect and low oral bioavailability. The patch developed by German Schwartz Pharmaceutical Company can overcome the above-mentioned defects. It was first launched in the UK in 2006, and then in the United States, Germany, Italy, Spain and other countries, but it has not yet been launched in China. One Neupro patch per day, the initial dose is 2mg / patch, the maximum dose is 8mg / patch, it is used alone to treat PD in the early stage, and it can be used in combination with levodopa to treat PD in the late stage. [0003] At present, domestic l...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/381A61K47/34A61P25/16
CPCA61K31/381A61K9/7053
Inventor 张俊
Owner SHAANXI EYOUNG TECH
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