Vinpocetine transdermal patch and preparation method thereof

A technology of vinpocetine and transdermal patch, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of drug and transdermal penetration enhancement In order to improve the sequelae of cerebral infarction, eliminate defects and improve the migration rate, etc.

Active Publication Date: 2010-09-08
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention changes the predecessors' method of directly mixing vinpocetine with adhesive as the skeleton material to prepare a skeleton transdermal patch, and solves the pr

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The transdermal patch described in this example is a reservoir-type drug patch, consisting of a five-layer structure of a protective layer, an adhesive layer, a release-controlling film layer, a drug reservoir, and a backing layer. The materials and components used in each layer as follows:

[0028] Backing layer: polyethylene film

[0029] Protective layer: PTFE film

[0030] Controlled release film layer: polyacetate cellulose film

[0031] Adhesive layer:

[0032] Vinpocetine: 2%

[0033] Polyacrylate pressure sensitive adhesive: 90%

[0034] Azone: 3%

[0035] Propylene Glycol: 5%

[0036] Drug storage:

[0037] Vinpocetine: 5%

[0038] Hypromellose: 10%

[0039] Azone: 5%

[0040] Propylene Glycol: 10%

[0041] Tween 80: 4%

[0042] Macrogol 400: 1%

[0043] Citric acid: 5%

[0044] Sodium hydroxide aqueous solution: appropriate amount

[0045] Water: Add to 100%

[0046] 1. Preparation of transdermal patch

[0047] 1) Preparation of drug reservoir...

Embodiment 2

[0067] The structural composition of the transdermal patch described in this embodiment is the same as in Example 1, consisting of five layers, and the materials and components used in each layer are as follows:

[0068] Backing layer: composite aluminum foil

[0069] Protective layer: polyester film

[0070] Controlled Release Membrane: Ethylene-vinyl acetate copolymer membrane

[0071] Adhesive layer: blank silicone pressure sensitive adhesive

[0072] Drug storage:

[0073] Vinpocetine: 2%

[0074] Carbomer: 5%

[0075] Azone: 5%

[0076] Ethanol: 20%

[0077] Eucalyptus Oil: 3%

[0078] Methylcellulose: 5%

[0079] Citric acid: 5%

[0080] Sodium hydroxide aqueous solution: appropriate amount

[0081] Water: Add to 100%

[0082] 1. Preparation of transdermal patch

[0083] 1) Preparation of drug reservoir:

[0084] Take an appropriate amount of water to fully swell the carbomer. After the carbomer is swollen, add different proportions of vinpocetine, azone, et...

Embodiment 3

[0101] The structure of the transdermal patch described in this embodiment is composed of the same as in Example 1, consisting of five layers, and the materials and components used in each layer are as follows:

[0102] Backing layer: polyester film

[0103] Protective layer: Polypropylene film

[0104] Controlled Release Membrane: Polysiloxane Membrane

[0105] Adhesive layer: blank polyisobutylene pressure sensitive adhesive

[0106] Drug storage:

[0107] Vinpocetine: 8%

[0108] Cellulose acetate: 5%

[0109] Azone: 8%

[0110] Ethanol: 30%

[0111] Polyvinylpyrrolidone: 5%

[0112] Citric acid: 10%

[0113] Sodium hydroxide aqueous solution: appropriate amount

[0114] Water: Add to 100%

[0115] 1. Preparation of transdermal patch

[0116] Preparation of the drug storehouse: Take an appropriate amount of water to dissolve and stir Vinpocetine, cellulose acetate, Azone, ethanol, polyvinylpyrrolidone and citric acid in different proportions to fully disperse and...

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PUM

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Abstract

The invention relates to a vinpocetine-contained transdermal patch and a preparation method thereof. The vinpocetine transdermal patch comprises five layers of a protecting layer, an adhesive layer, a release controlling film layer, a medicament reservoir and a back lining layer; the medicament reservoir contains 1-10 percent of vinpocetine or pharmaceutically acceptable salt of vinpocetine, 0-40percent of transdermal accelerating agent, a pH adjusting agent and the balance of reservoir substrate; the adhesive layer contains 0-8 percent of vinpocetine or pharmaceutically acceptable salt of vinpocetine, 0-40 percent of transdermal accelerating agent, a pH adjusting agent and the balance of pressure-sensitive adhesive; and pH values of the medicament reservoir and the adhesive layer are between 3.5 and 6.5. The invention solves the problems of less drug-loading amount, difficult formation of higher medicament concentration gradient and lower transmission rate of the traditional transdermal preparation by adopting a new preparation technology, has good transdermal effect and continuously releases medicaments for 1-7 days; and animal in-vivo tests show that the vinpocetine-contained transdermal patch has no simulating performance and sensitizing performance on skin.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a transdermal patch containing vinpocetine and a preparation method thereof. Background technique [0002] Vinpocetine (Vinpocetine), molecular formula C 22 h 26 N 2 o 2 , Molecular weight 350.46, Vinpocetine is a natural medicine obtained from periwinkle, belonging to indole alkaloids, widely used in the treatment and prevention of ischemic cerebrovascular diseases. Vinpocetine is a cerebral vasodilator, which can inhibit the activity of phosphodiesterase, increase the effect of c-GMP, the messenger of vascular smooth muscle relaxation, and selectively increase cerebral blood flow. In addition, it can also inhibit platelet aggregation, reduce human blood viscosity, enhance Red blood cell deformability, improve blood flow and microcirculation, promote brain tissue uptake of glucose, increase brain oxygen consumption, improve brain metabolism. Clinically, it is mainly used to improve var...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4375A61K47/38A61K47/34A61P9/10A61K47/10A61K47/32
Inventor 王向军郭殿武张涛吴耀东张旭文高渊
Owner HANGZHOU MINSHENG PHARM CO LTD
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