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Stable controlled-release rasagiline transdermal patch and preparation method thereof

A transdermal patch, stable technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, sheet-like delivery, etc., can solve the problems of unfavorable long-term storage and poor drug stability, and achieve Easy to prepare and long-lasting effect

Active Publication Date: 2009-12-23
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In CN101032474, a kind of rasagiline transdermal drug patch for the treatment or prevention of neurological diseases has been described, and the pH value of the patch remains in the alkaline range (greater than 7.0) in the embodiment, although good Transdermal penetration effect, but the study found that under the high temperature stability test conditions, the drug stability is not good, it may not be conducive to long-term storage, and some irritating solvents such as chloroform are used

Method used

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  • Stable controlled-release rasagiline transdermal patch and preparation method thereof
  • Stable controlled-release rasagiline transdermal patch and preparation method thereof
  • Stable controlled-release rasagiline transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1: A single-layer polyacrylate matrix patch containing rasagiline mesylate, using lauryl acid as a skin penetration promoting agent

[0067] 0.25 g of rasagiline mesylate was dissolved in 1 g of propylene glycol, and added to 20 g of polyacrylate glue (National Starch, 387-2287). Add 0.3 g of oleic acid, and after stirring evenly, use an automatic coating machine (Shanghai Kaikai Company, TB-04 type) to coat the mixed glue solution on the siliconized paper with a coating thickness of 0.6 mm. After drying at 60°C for 5 minutes, cover the support layer and transfer it, and then die-cut or cut the patch into the final sheet. The measured rasagiline content was 220ug / cm 2 , The measured pH is 4.4. The cross-sectional schematic diagram of the prepared patch is shown in figure 1 .

[0068] The penetration of the prepared patch was studied using a Franz cell and the depilated abdominal skin of two-month-old rats. Use high-performance liquid chromatography to measu...

Embodiment 2

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

[0072] Take 0.25 gram of rasagiline free base and dissolve it in 1 gram of propylene glycol, and then add it to 20 grams of silicone gel (3M Company, USA, PSA7-4302 type). Add 0.3 g of laurocaprazol, and after stirring evenly, take a small amount of glue as a sample (for stability research) and measure the pH value as 7.7. Prepare according to the above prescription and process, and add 0.15 g of methanesulfonic acid and stir evenly to obtain a glue solution. Take a small amount of the glue solution as a sample to measure (for stability research) and get a pH value of 4.0. Use an automatic coating machine (Shanghai Kaikai Company, TB-04 type) to coat the mixed glue solution on the siliconized paper with a coating thickness of 0.6 mm. After drying at 60°C for 5 minutes, cover the support layer and transfer it, and then die-cut or cut the patch...

Embodiment 3

[0077] Example 3: Single-layer polyvinylpyrrolidone-polyethylene glycol composite matrix patch containing rasagiline, using laurazozone as skin penetration promoting agent

[0078] Take 24 grams of polyvinylpyrrolidone PVP-K90D (ISP Technologies, INC) and sprinkle it into 120 grams of absolute ethanol, stir to make it swell completely, add 16 grams of polyethylene glycol 400 (Nanjing Weier Chemical Industry) into it, stir and mix Evenly, a blank glue is prepared. Take 15 grams of the prepared glue solution, add 1.0 grams of rasagiline free base, stir and ultrasonically dissolve it. Add 0.3 gram of azoxazone, and after stirring evenly, the measured pH value is 7.4. Prepare according to above-mentioned prescription, process, and add 0.6 gram of methanesulfonic acid, record pH value to be 4.7. Use an automatic coating machine (Shanghai Kaikai Company, TB-04 type) to coat the mixed glue solution on the siliconized paper with a coating thickness of 0.4 mm. After drying at 60°C f...

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Abstract

The invention relates to rasagiline for treating or preventing nervous system diseases and a transdermal patch of a pharmaceutically acceptable slat of rasagiline. The transdermal patch comprises the rasagiline or the pharmaceutically acceptable slat of rasagiline and at least one hydrophilic polymer substrate. And the pH value of the patch ranges from 3.5 to 6.5. The patch has the characteristics of excellent stability and good control over transdermal release of the rasagiline.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to transdermal drug patches of rasagiline and pharmaceutically acceptable salts thereof for treating or preventing neurological diseases, containing at least one hydrophilic polymer As for the substrate, the pH value of the patch is not greater than 7.0, especially between not less than 3.0 and not greater than 6.5. technical background [0002] Rasagiline (rasagiline) is a selective monoamine oxidase B inhibitor, used for the treatment of central nervous system diseases, such as Parkinson's disease (PD), depression, etc., has been listed in Europe. The chemical structural formula of rasagiline is as follows. [0003] [0004] Parkinson's disease is the result of degeneration of dopaminergic neurons in the central nervous system, a decrease in the release of the neurotransmitter dopamine. Due to the insufficient release of dopamine transmitters, the patient's muscle c...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/135A61K47/32A61K47/34A61K47/38A61P25/00A61P25/16A61P25/24
CPCA61K9/7084A61K9/7069A61K9/7061A61K9/703A61K9/7053A61P25/00A61P25/16A61P25/24A61P25/28A61P43/00
Inventor 林佳亮李群李宏忠张涛邓杰樊斌
Owner CHONGQING PHARMA RES INST
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