Rasagiline transparent patch for curing and preventing neurological diseases and the preparing method thereof

A technique for nervous system diseases and patches, which is applied in the field of rasagiline transdermal drug patches and its preparation, protective foils or membranes, which can solve the problems of unsatisfactory transdermal penetration effects and inconvenient administration.

Active Publication Date: 2007-09-12
CHONGQING PHARMA RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The transdermal penetration enhancer is not particularly ideal for promoting the transdermal penetration of rasagiline, and it is absorbed through the skin by spraying, which is inconvenient for administration.

Method used

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  • Rasagiline transparent patch for curing and preventing neurological diseases and the preparing method thereof
  • Rasagiline transparent patch for curing and preventing neurological diseases and the preparing method thereof
  • Rasagiline transparent patch for curing and preventing neurological diseases and the preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1: Single-layer polyacrylate matrix patch containing rasagiline, with oleic acid as skin penetration promoting agent

[0061] Add 50 grams of 50% (w / w) Eudragit E100 solution in chloroform to a solution of 250 grams of fully swollen polyacrylate adhesive in water; add 50 grams of oleic acid (that is, a low amount of oleic acid) After that, stir to make it even.

[0062] Dissolve 50 grams of rasagiline in 200 ml of absolute ethanol at 50°C to 80°C, and then add it to the stirring solution above. Slowly add 1mol / l NaOH aqueous solution and stir while adding to make the pH value 7.5. After stirring evenly, apply it to the medical non-woven fabric with an appropriate scraper, and adjust the thickness of the wet film to make it in the The weight was 60 g / m2 after drying at 100°C for 60 minutes.

[0063] The dried base film was coated with a 23 μm thick polyester film; each patch was then die-cut into final sheets.

[0064] The amount of oleic acid added can be 150...

Embodiment 2

[0071] Example 2: A single-layer polyvinylpyrrolidone matrix patch containing rasagiline, using isopropyl myristate as a skin penetration promoting agent

[0072] 20 grams of sodium hydroxide and 15 grams of phosphoric acid are added to 500 grams of 25% (w / w) polyvinylpyrrolidone ethanol solution, and after stirring for 1 hour at 600 rpm, add 100 grams of colloid in batches successively Silicon dioxide, add 80 grams of rasagiline and 20 grams of isopropyl myristate (low amount of isopropyl myristate) in batches, continue stirring while slowly adding 1 mol / l NaOH aqueous solution to make the pH value 7.5 , after stirring for at least 1 hour to make it uniform, apply it to the medical non-woven fabric with an appropriate spatula, adjust the thickness of this wet film, and make it dry at 80°C for 60 minutes and have a weight of 60 g / m2 .

[0073] The dried base film was coated with a 23 μm thick polyester film; each patch was then die-cut into final sheets.

[0074] The amount ...

Embodiment 3

[0081] Example 3: Multi-layer polyisobutylene matrix patch containing rasagiline, using laurozozone as skin penetration promoting agent

[0082] Dissolve 50g of rasagiline in 200ml of absolute ethanol at 50°C~80°C, then add it to 74% silicone-containing polymer (40g BioPSA 7-4201+40g BioPSA 7-4301) In the heptane solution, after adding 100 grams of petroleum ether and 50 grams of laurozone (that is, a low amount of laurozone), the mixture was stirred for 1 hour at a speed of 600 rpm, while stirring Slowly add 1mol / l NaOH aqueous solution to make the pH value 7.5. After obtaining a uniform dispersion, apply it to the medical non-woven fabric with an appropriate scraper, adjust the thickness of the wet film, and make it dry at 60°C The weight after drying for 60 minutes was 60 g / m2. 150g, 250g

[0083] The dried base film was coated with a 23 μm thick polyester film; each patch was then die-cut into final sheets.

[0084] The amount of laurocapram added can be 150 grams (that...

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PUM

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Abstract

The present invention relates to one kind of transdermal rasagiline medicine plaster for preventing and treating neurological diseases and its preparation process. The transdermal rasagiline medicine plaster includes one support layer without chemical reaction with the matrix components, one matrix layer containing rasagiline or its pharmaceutically acceptable salt, and operate protecting layer being torn off before the plaster is used. It features the matrix layer with polymer as the basic material, adhering system with inorganic or organic filler, stored rasagiline and matter(s) to promote the transdermal absorption of rasagiline.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a rasagiline (ransagiline) transdermal drug patch for treating or preventing nervous system diseases and a preparation method thereof, the patch contains a support layer that does not react chemically with matrix components , a matrix layer containing an effective amount of rasagiline and pharmaceutically acceptable salts thereof, and a protective foil or membrane to be removed before use. technical background [0002] Rasagiline (ransagiline), a selective monoamine oxidase B inhibitor, is used for the treatment of central nervous system diseases, such as Parkinson's disease (PD), depression, etc., and has been launched in Europe. The chemical structural formula of rasagiline is as follows. [0003] [0004] Parkinson's disease is thought to be the result of degeneration of dopaminergic neurons in the central nervous system, a reduction in the release of the neurotr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/133A61K9/70A61P25/16A61P25/24A61P25/28A61P43/00
CPCA61K31/135A61K9/7053A61K9/7061A61K9/7069A61K9/7092A61P25/00A61P25/16A61P25/24A61P25/28A61P43/00
Inventor 林佳亮肖进迈邓杰
Owner CHONGQING PHARMA RES INST
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