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Rivastigmine salt treating method and transdermal administration patch

A technology of rivastigmine salt and treatment method, applied in chemical instruments and methods, drug combination, carboxylate preparation and other directions, can solve the problem of inability to take into account the permeation efficiency and stable duration, and achieve long permeation duration, The effect of improving the utilization rate and ensuring the transmittance

Active Publication Date: 2017-09-08
BUSTER MEDICAL TECH CHANGZHOU CO LTD
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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 solve the above-mentioned problem that rivastigmine cannot be used as a patch when using it as a patch, so as to improve the utilization efficiency of the patch rivastigmine and provide the following technical solutions:

Method used

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  • Rivastigmine salt treating method and transdermal administration patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Treatment of Rivastigmine Salt:

[0059] After adding 2.4 grams of carpalatine tartrate into 1.0 gram of pure water for dissolving, add 0.25 gram of sodium hydroxide solution (0.25 gram of sodium hydroxide, dissolved in 0.5 gram of pure water), fully mix in a water bath at 5 degrees Celsius, Add 0.9 g of polyethyleneimine and mix well.

[0060] Preparation of the transdermal rivastigmine patch:

[0061] Add 0.05 grams of propyl gallate and 0.25 grams of ethanol to the above-treated rivastigmine salt, after fully mixing, add 1.0 grams of C5 resin and 0.2 g of mineral oil, mix well to allow C5 resin to fully dissolve, add 3.6 grams of polyisobutylene pressure-sensitive adhesive, after fully mixing, add 0.4 grams of cross-linked polyvinylpyrrolidone and 1.0 grams of n-hexane, after fully mixing, spread it into a gel of 5mm to 6mm, and heat it in an oven at 60 degrees Celsius For 1 hour to 2 hours, the drug layer is obtained by molding. The back protection layer, the dru...

Embodiment 2

[0064] Treatment of Rivastigmine Salt:

[0065] After adding 2.4 grams of carpalatine tartrate into 1.0 gram of pure water for dissolving, add 0.25 gram of sodium hydroxide solution (0.25 gram of sodium hydroxide, dissolved in 0.5 gram of pure water), fully mix in a water bath at 5 degrees Celsius, Add 0.9 g of polyethyleneimine and mix well.

[0066] Preparation of the transdermal rivastigmine patch:

[0067] Add 0.05 grams of propyl gallate and 0.25 grams of ethanol to the above-treated rivastigmine salt, after fully mixing, add 1.0 grams of C5 resin and 0.2 g of mineral oil, mix well to allow C5 resin to fully dissolve, add 3.6 grams of polyisobutylene pressure-sensitive adhesive, after fully mixing, add 0.4 grams of cross-linked polyvinylpyrrolidone and 1.0 grams of n-hexane, after fully mixing, spread it into a gel of 5mm to 6mm, and heat it in an oven at 60 degrees Celsius For 1 hour to 2 hours, the drug layer is obtained by molding. The same back protection layer as ...

Embodiment 3

[0070]After dissolving 3.0 g of carbaladin tartrate in 2.0 g of pure water, add 1.5 g of triethanolamine, and mix thoroughly in a water bath at 5°C.

[0071] Preparation of the transdermal rivastigmine patch:

[0072] Add 2.0 grams of C5 resin and 0.3 g of mineral oil to the above-treated rivastigmine salt, mix well to fully dissolve the C5 resin, add 9.0 g of polyisobutylene pressure-sensitive adhesive, and after fully mixing, add 1.0 g of cross-linking After polyvinylpyrrolidone and 1.0 g of n-hexane are fully mixed, coated to form a gel of 5 mm to 6 mm, heated in an oven at 60 degrees Celsius for 1 hour to 2 hours to form a drug layer. The same back protection layer as in Example 1, the same release liner as the drug layer in Example 1 were sequentially laminated into one, and then die-cut to prepare a transdermal rivastigmine patch.

[0073] The transdermal rivastigmine patch was tested for the transdermal transmission rate of rivastigmine, and the results are listed in T...

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Abstract

The invention particularly relates to a rivastigmine salt treating method and transdermal administration patch. According to the rivastigmine salt treating method provided by the invention, rivastigmine salt and alkaline substances are subjected to reaction treatment, and the rivastigmine salt treated by the method serves as patch, so the transmittance of the rivastigmine can be guaranteed, long penetrating duration time can be maintained stably, and the utilization rate is increased.

Description

[0001] This application claims the priority of the Chinese patent application submitted to the China Patent Office on March 1, 2016, the application number is 201610113139.6, and the invention name is "the conversion method of rivastigmine tartrate and the patch made of its product", all of which The contents are incorporated by reference in this application. technical field [0002] The invention belongs to the field of rivastigmine transdermal delivery, in particular to a rivastigmine salt treatment method and a transdermal drug delivery patch. Background technique [0003] Alzheimer's Disease (Alzheimer's Disease) is a progressive degenerative disease of the central nervous system, which mostly occurs in the elderly over 60 years old. Its clinical manifestations are short-term memory dysfunction first, followed by persistent mental decline, loss of judgment and reasoning ability, aphasia, and movement disorders. The main pathological features are brain atrophy, formation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C271/44C07C269/06C07C59/255C07C51/41A61K31/27A61K9/70A61P25/28
CPCA61K9/7053A61K31/27A61P25/28C07C269/06C07C271/44
Inventor 许宗民杨保新
Owner BUSTER MEDICAL TECH CHANGZHOU CO LTD
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