Rivastigmine transdermal patch and preparation method thereof

A technology of transdermal patch and spray drying method, which is applied in the directions of osmotic delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc. Skin release rate and other issues, to achieve the effect of less drug irritation, simple preparation process, and improved transdermal release rate

Active Publication Date: 2018-10-23
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the aforementioned prior art, since the active drug rivastigmine actually exists in a supersaturated dissolved state in the system of the present invention, it is easy to cause crystallization of the active drug, which in turn affects the transdermal release rate of the active drug rivastigmine, making the drug loading Quantity limited

Method used

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  • Rivastigmine transdermal patch and preparation method thereof
  • Rivastigmine transdermal patch and preparation method thereof
  • Rivastigmine transdermal patch and preparation method thereof

Examples

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Embodiment 1

[0035] A preparation method of rivastigmine transdermal patch, comprising:

[0036] (1) The preparation method of the powder of rivastigmine or its salt, it is by rivastigmine or its salt, and phospholipid and water-soluble adjuvant are dispersed in dehydrated alcohol, and described phospholipid is selected from soybean lecithin; Sexual excipients are selected from polyvinylpyrrolidone, which is prepared by spray drying method. The weight ratio of rivastigmine to phospholipids and water-soluble excipients is 70:25:5. The spray drying process is nitrogen flow pressure: 600L / h; Temperature: 90°C; Outlet temperature: 43°C; Feed rate: 5mL / min; Needle pass frequency: 15 seconds / time;

[0037] (2) The preparation method of the adhesive layer of transdermal patch: the adhesive layer is liquid paraffin (mass ratio 80%) and styrene-isoprene-styrene block copolymer (mass ratio 20%), in acetic acid Disperse and mix in an ethyl ester solvent, prepare an adhesive layer according to the th...

Embodiment 2

[0040] A preparation method of rivastigmine transdermal patch, comprising:

[0041] (1) The preparation method of the powder of rivastigmine or its salt, it is by rivastigmine or its salt, and phospholipid and water-soluble adjuvant are dispersed in dehydrated alcohol, and described phospholipid is selected from soybean lecithin; Sexual excipients are selected from polyethylene glycol 6000, which is prepared by spray drying method. The weight ratio of rivastigmine to phospholipids and water-soluble excipients is 70:25:5. The spray drying process is nitrogen flow pressure: 600L / h; Inlet air temperature: 90°C; Outlet air temperature: 43°C; Feed rate: 5mL / min; Needle pass frequency: 15 seconds / time;

[0042](2) The preparation method of the adhesive layer of transdermal patch: the adhesive layer is liquid paraffin (mass ratio 80%) and styrene-isoprene-styrene block copolymer (mass ratio 20%), in acetic acid Disperse and mix in an ethyl ester solvent, prepare an adhesive layer ac...

Embodiment 3

[0045] A preparation method of rivastigmine transdermal patch, comprising:

[0046] (1) The preparation method of the powder of rivastigmine or its salt, it is by rivastigmine or its salt, and phospholipid and water-soluble adjuvant are dispersed in dehydrated alcohol, and described phospholipid is selected from soybean lecithin; Sexual excipients are selected from polyvinylpyrrolidone, which is prepared by spray drying method. The weight ratio of rivastigmine to phospholipids and water-soluble excipients is 70:25:5. The spray drying process is nitrogen flow pressure: 600L / h; Temperature: 90°C; Outlet temperature: 43°C; Feed rate: 5mL / min; Needle pass frequency: 15 seconds / time;

[0047] (2) The preparation method of the adhesive layer of transdermal patch: adhesive layer is liquid paraffin (mass ratio 70%) and styrene-isoprene-styrene block copolymer (mass ratio 30%), in acetic acid Disperse and mix in an ethyl ester solvent, prepare an adhesive layer according to the thickn...

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Abstract

The invention discloses a rivastigmine transdermal patch and a preparation method thereof. The method includes: dispersing rivastigmine or salt thereof, phospholipid and water-soluble auxiliary materials into an organic solvent, and using a spray drying method or a reduced-pressure drying method to remove the solvent to obtain powder; preparing an adhesive layer comprising liquid paraffin and styrene-isoprene-styrene block copolymer, heating the adhesive layer under 55-70 DEG C for 2-10 hours, evenly attaching the powder to the surface of the adhesive layer, and cooling to normal temperature at the cooling speed of 1-15 DEG C/h to obtain the transdermal patch. The transdermal patch has the advantages that the separating out of active drug crystals in the high-drug-loading-capacity patch can be inhibited as much as possible, the transdermal release rate of the active drug rivastigmine can be increased, and the patch is low in irritation.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a rivastigmine transdermal patch and a preparation method thereof. Background technique [0002] Rivastigmine, English name: rivastigmine, chemical name (S)-N-ethyl-N-methyl-3-[1-(dimethylamino)ethyl]-phenylcarbamate, mostly use its tartrate Mostly medicinal substances, also known as rivastigmine, the chemical structure of rivastigmine is as follows: [0003] [0004] It is a carbamate brain-selective cholinesterase inhibitor, which can specifically inhibit the degradation of brain acetylcholine and butyrylcholine, and increase the level of choline in the cerebral cortex. The existing dosage forms are oral liquid and capsules developed by Novartis Pharmaceuticals. The capsules have been imported under the trade name Exelon, but they are expensive and are administered twice a day. Due to the single dosage form of rivastigmine, there is a large hepatic firs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/32A61K31/27A61P25/28
CPCA61K9/0004A61K9/7053A61K31/27A61P25/28
Inventor 贾文强黄伟棠闫鹏李莹廖峰
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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