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Slow release long-acting rasagiline transdermal patch with high bioavailability and preparation method thereof

A transdermal patch and utilization technology, applied in the direction of non-active ingredient medical preparations, sheet delivery, drug combination, etc., can solve the problems of undisclosed prescriptions and preparation methods, and avoid the first-pass effect of the liver, Smooth absorption and the effect of reducing blood pressure response

Inactive Publication Date: 2011-06-22
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] It is disclosed in WO2008076348 that rasagiline crystals can be used to prepare patches, but the prescription and preparation method are not disclosed

Method used

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  • Slow release long-acting rasagiline transdermal patch with high bioavailability and preparation method thereof
  • Slow release long-acting rasagiline transdermal patch with high bioavailability and preparation method thereof
  • Slow release long-acting rasagiline transdermal patch with high bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Patches based on DURO-TAK87-2677 pressure sensitive adhesive

[0060] prescription:

[0061]

[0062] Add the preparation intermediate to DURO-TAK87-2677, stir and mix well, coat 0.25mm thick on a 75μm thick translucent polyester film, dry at 60°C for 30 minutes, evaporate the organic solvent, and coat 75μm thick A polyethylene backing layer is available. The patch has a measured content of 923 μg / cm 2 . The patch was cut into a size containing 5 mg of rasagiline for human pharmacokinetic research.

Embodiment 2

[0064] Patches based on DURO-TAK87-4098 pressure-sensitive adhesive

[0065] prescription:

[0066]

[0067] Add the preparation intermediate and butyl hydroxytoluene (butyl hydroxytoluene is used as an antioxidant) to DURO-TAK 87-4098, stir and mix well, and coat 0.25 mm thick on a 75 μm thick translucent polyester film, Dry at 60°C for 30 minutes, evaporate the organic solvent, and cover with a polyethylene backing layer with a thickness of 75 μm. The patch measured content of 1080μg / cm 2 . The patch was cut into a size containing 5 mg of rasagiline for human pharmacokinetic research.

Embodiment 3

[0069] Patches based on silicone BIO-PSA7-4302 pressure-sensitive adhesive

[0070] prescription:

[0071]

[0072] Add rasagiline free base into BIO-PSA7-4302, stir and mix evenly, coat 0.2mm thick on a 75μm thick translucent polyester film, dry at 60°C for 30 minutes, evaporate the organic solvent, cover A polyethylene backing layer with a thickness of 75 μm is applied. The patch measured a content of 325 μg / cm 2 . The patch was cut into a size containing 5 mg of rasagiline for human pharmacokinetic research.

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Abstract

The invention relates to a slow release long-acting rasagiline transdermal patch with high bioavailability and a preparation method thereof. The patch is characterized in that effective amount of rasagiline and a substrate are contained, wherein the concentration of rasagiline is in the range of 0.1 mg / cm2 - 2 mg / cm2, every patch contains 1 mg - 10 mg of rasagiline, and the substrate contains one or more than two kinds of the following substances: acrylic polymers containing no carboxylic group and silicone polymers with silanol groups capped by alkyls. The time of maximum plasma drug concentration of the patch is prolonged to be 5 times or more that of oral tablets, and the bioavailability of the patch is 130 percent or more of that of oral tablets. The patch in the invention can be applied to effectively inhibit monoamine oxidase B (MAOB) for at least 3 days, in addition, the preparation method is simple and suitable for industrial production.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a high-bioavailability, slow-release and long-acting rasagiline transdermal patch and a preparation method thereof, which is characterized in that it contains an effective amount of rasagiline and a matrix, wherein, The patch contains 0.1mg / cm 2 ~2mg / cm 2 Rasagiline, each tablet contains 1mg to 10mg of rasagiline. After administration, rasagiline can be slowly released in the matrix and absorbed by the body, and its blood concentration can rise steadily to the therapeutic concentration. Compared with oral tablets, the time to reach the peak blood concentration is 5 times longer than that of oral tablets Above, the relative bioavailability is more than 130% of the oral tablet, and the application of the patch of the present invention can effectively inhibit monoamine oxidase B (MAOB) for at least 3 days, and the preparation method is simple, suitable for ind...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/135A61K47/32A61K47/34A61P25/16A61P25/28A61P25/24A61P25/00A61P25/30
Inventor 林佳亮邓杰李宏忠林羽张涛邹艳冶樊斌
Owner CHONGQING PHARMA RES INST
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