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A skin external preparation containing rivastigmine and medicinal salt thereof and preparation method thereof

A technology for external preparations and medicinal salts, which is applied in the field of pharmaceutical preparations and can solve problems such as serious gastrointestinal side effects

Active Publication Date: 2020-05-12
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2000, Novartis imported rivastigmine capsules for clinical application in my country. In 2007, rivastigmine patches were launched. The disadvantage of oral preparations is that it needs to be taken twice a day, and the gastrointestinal side effects are serious, so it is more convenient to develop and use , drugs with fewer adverse reactions have become an inevitable
It can be seen from the existing literature that there is no report on how to prevent the oxidation of the raw material drug in the rivastigmine patch

Method used

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  • A skin external preparation containing rivastigmine and medicinal salt thereof and preparation method thereof
  • A skin external preparation containing rivastigmine and medicinal salt thereof and preparation method thereof
  • A skin external preparation containing rivastigmine and medicinal salt thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Backing layer: Thermal composite film of PET fiber and PET film

[0030] formula Dosage ratio rivastigmine 30.00% Silicone pressure sensitive adhesive 63.75% Tocopherol 0.25% lactic acid 6.00%

[0031] Preparation method: import 15% silicone pressure-sensitive adhesive into a container, add isopropanol to stir, add formula amount of lactic acid, prepare colloid A, stir evenly, seal for use; add tocopherol to the remaining silicone pressure-sensitive adhesive 1. Stir the active ingredients of the prescription amount evenly; adjust the coating machine to coat, first coat with colloid A, and then continue to coat the drug-containing colloid; cut the coated sample into strips and cut into required sizes .

Embodiment 2

[0033] Backing layer: Thermal composite film of PET fiber and PET film

[0034] formula Dosage ratio rivastigmine 20.0% Silicone pressure sensitive adhesive 69.8% Tocopherol 0.2% Oleic acid 10.0%

[0035] Preparation method: the same as in Example 1.

Embodiment 3

[0037] Backing layer: Thermal composite film of PET fiber and PET film

[0038] formula Dosage ratio rivastigmine 40.0% Silicone pressure sensitive adhesive 58.0% Tocopherol 1.0% polyoxyethylene monoglyceride 1.0%

[0039] Preparation method: the same as in Example 1.

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Abstract

The invention discloses an external skin preparation containing rivastigmine and pharmaceutical salt thereof. According to the formula, a stabilizer and tocopherol are added at special proportions; meanwhile, a backing layer, which is made from a special material is adopted; the selected backing layer can obviously reduce influence to active ingredients of the preparation and effectively inhibit the increase in an impurity content of the preparation; meanwhile, on the basis of the combined actions of the adopted special stabilizer and backing layer, the active ingredients of the medicine (thepreparation) are further prevented from getting oxidized, so that the generation of oxidation impurities is relieved; therefore, the external rivastigmine skin preparation provided by the invention ishigher in stability and longer in period of validity.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an external skin preparation of rivastigmine and a medicinal salt thereof for treating senile dementia symptoms and a preparation method thereof. Background technique [0002] At present, my country has entered an aging society, and Alzheimer's disease has become a disease that affects the lives and health of the people, especially the elderly. The current treatment methods cannot cure or even prevent the occurrence of Alzheimer's disease. The clinical drugs that can slow down the development of this disease include antioxidants, monoamine oxidase inhibitors, anti-inflammatory drugs and cholinease inhibitors, as well as biological agents that are still in the experimental stage. Engineered drugs such as brain nerve prosthetics. Cholinesterase inhibitors are currently internationally recognized and highly evaluated drugs for improving symptoms of Alzheimer's dementia. T...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K47/22A61K47/12A61K47/14A61K31/27A61P25/28
CPCA61K9/7076A61K31/27A61K47/12A61K47/14A61K47/22
Inventor 赵焰平卢迪纪明文申桂芬孙立欣张林林
Owner BEIJING TIDE PHARMA
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