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Week-acting transdermal pramipexole patch and preparation method thereof

A technology of pramipexole and transdermal patch, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of poor skin penetration and poor fat solubility. Achieve the effects of small hair follicle density, strong lipophilicity, and convenience for pharmacokinetic experiments

Active Publication Date: 2015-04-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the raw material drug used to make the patch is water-soluble pramipexole hydrochloride, which has poor fat solubility and poor skin penetration ability, and can only maintain an effective dose for three days

Method used

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  • Week-acting transdermal pramipexole patch and preparation method thereof
  • Week-acting transdermal pramipexole patch and preparation method thereof
  • Week-acting transdermal pramipexole patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Polyvinyl alcohol (PVA17-88) 1.5g, polyvinylpyrrolidone (PVP) 0.3g, propylene glycol 0.2g, glycerol 0.2g, ethylenediaminetetraacetic acid disodium 0.1g, pramipexole 40mg to prepare pramipexole paste sheet.

[0041] Polyvinyl alcohol (PVA17-88) 1.5g, polyvinylpyrrolidone (PVP) 0.3g, propylene glycol 0.2g, glycerol 0.2g, disodium edetate 0.1g, pramipexole hydrochloride 40mg, to prepare pramipexole hydrochloride paste sheet.

[0042] Preparation method: Fully swell polyvinyl alcohol and polyvinylpyrrolidone with 60% ethanol, add propylene glycol and glycerin, stir under a water bath at 70°C with magnetic stirring to fully dissolve and mix, add the drug solution when the temperature is lowered to 40°C, mix well, and let stand When the bubbles disappear, the film is laid by the casting method, and the composite is dried after forming and cooling, covering the polyethylene-aluminum-polyethylene composite film and the polyethylene anti-adhesive layer, and the divided dose is prepa...

Embodiment 2

[0045] Polyvinyl alcohol (PVA17-88) 1.6g, polyvinylpyrrolidone (PVP) 0.4g, eucalyptus oil 0.2g, glycerin 0.1g, ethylenediaminetetraacetic acid disodium 0.1g, pramipexole 100mg, to prepare pramipexole Agent.

[0046] Preparation method: Fully swell polyvinyl alcohol and polyvinylpyrrolidone with 60% ethanol, add glycerin and penetration enhancer, and stir under a water bath at 70°C with magnetic stirring to fully dissolve and mix. When the temperature is reduced to 40°C, add the drug solution and mix evenly. Leave it to stand until the bubbles disappear, spread the film by casting method, dry, form and cool and then compound, cover the polyethylene-aluminum-polyethylene composite film and the polyethylene anti-sticking layer, and prepare the divided dose to contain pramipexole 10.0mg / cm 2 Of the patch.

[0047] A modified Franz diffusion cell was used to measure the permeability of the transdermal patch on the inner skin of rabbit ears. The patch area used in the transdermal diffusi...

Embodiment 3

[0049] The first layer (one layer close to the release layer) composition: polyvinyl alcohol (PVA17-88) 2.8g, polyvinylpyrrolidone (PVP) 0.4g, eucalyptus oil 0.3g, propylene glycol 0.2g, glycerol 0.3g, ethylene dichloride Disodium aminetetraacetic acid 0.2g, pramipexole free base 40mg.

[0050] The second layer (close to the backing layer) composition: polyvinyl alcohol (PVA17-88) 1.6g, polyvinylpyrrolidone (PVP) 0.5g, eucalyptus oil 0.4g, propylene glycol 0.1g, glycerin 0.2g, ethylene diamine tetra Disodium acetate 0.1g, pramipexole free base 120mg.

[0051] Preparation method: Fully swell polyvinyl alcohol and polyvinylpyrrolidone with 60% ethanol, add propylene glycol and glycerin, stir under a water bath at 70°C with magnetic force to fully dissolve and mix. When the temperature is lowered to 40°C, add the drug and penetration enhancer solution and mix well. After that, let it stand until the bubbles disappear, cast the film, dry, form and cool and composite, cover the polyeth...

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Abstract

The invention particularly relates to a week-acting transdermal pramipexole patch and a preparation method thereof, and belongs to the field of pharmaceutic preparations. The week-acting transdermal pramipexole patch comprises a medicament storage bin, an anti-adhesion layer and a back lining layer. A double-layer patch is prepared by mixing a hydrophilic matrix with a penetration enhancer and adopting a laminated pouring method, so that the problems in multi-layer film preparation are effectively solved; furthermore, constant-speed release of a medicament within seven days can be guaranteed. An animal experiment shows that the week-acting transdermal pramipexole patch is non-irritative and non-allergenic to the skin. The patch disclosed by the invention has the advantages of definite treating effect, stable quality, high safety and convenience in use and is used for treating parkinsoncs disease.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pramipexole weekly transdermal patch and a preparation method thereof. In particular, it relates to the pramipexole transdermal patch that can continuously release the active ingredient pramipexole for a longer period of time, preferably within seven days. technical background [0002] Pramipexole, the chemical name is (S)-2-amino-4,5,6,7-tetrahydro-6-propylaminobenzothiazole, the active ingredient is chemically a base, and the current clinical dosage form Pramipexole hydrochloride immediate-release tablets ( ) And pramipexole hydrochloride sustained-release tablets ( ) Are in the form of its hydrochloride. Pramipexole is a new generation of non-ergot alkaloid selective dopamine D2 and D3 receptor agonists, approved by the FDA in 1997 for the treatment of primary Parkinson's disease (PD). Pramipexole is currently the first-line drug recommended by the PD diagnosis and ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/428A61K47/34A61K47/32A61P25/16
Inventor 刘建平陈彤
Owner CHINA PHARM UNIV
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