Ibuprofen percutaneous release patch and preparation method thereof

A technology of patch and transdermal penetration enhancer, which is applied in the field of medicine, can solve the problems of short biological half-life of ibuprofen, frequent medication, kidney damage, etc., achieve good sweat resistance and repeated peeling, and overcome insufficient dosage. Determination, the effect of a large amount of accumulated transdermal release

Inactive Publication Date: 2011-07-27
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the oral dosage form is easy to cause gastrointestinal adverse reactions, and due to the short biological half-life of ibuprofen, frequent medication is required to maintain the therapeutic concentration, which aggravates gastrointestinal reactions, even causes gastrointestinal bleeding, and also damages the kidneys
However, the administration error of ointment and gel is relatively large, and the medication is frequent, easy to lose, and pollute clothes
[0004] Because of its small molecular weight, low melting point, suitable oil-water partition coefficient and small dosage, ibuprofen basically meets the properties that patch drugs should have. However, there is no ibuprofen transdermal patch at present.

Method used

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  • Ibuprofen percutaneous release patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1) Combine IBU, SIS, medical grade terpene resin, compound transdermal accelerator (72-6:1, 2-propanediol mass ratio=1:1) and compound antioxidant (antioxidant 1010: antioxidant 264 Mass ratio=2: 1) is to carry out back-up by mass percent respectively at 10%, 50%, 33%, 5% and 2%; The consumption of organic solvent (cyclohexane: ethyl acetate mass ratio=3: 1) is 20ml / g IBU;

[0027] 2) Add the SIS and tackifying terpene resin into the organic solvent, add the drug ibuprofen, compound transdermal penetration enhancer and compound antioxidant after complete swelling, stir evenly, and use a film coater to coat after removing air bubbles by ultrasonic waves Put it on the polytetrafluoroethylene film of the anti-adhesive layer, dry it naturally, put it in a vacuum drying oven at 50 ° C for 1.5 hours, remove the solvent completely, obtain the drug storage layer, and then cover the backing layer aluminum foil-polyethylene composite film on the on the drug storage layer and tr...

Embodiment 2

[0029] 1) Combine IBU, SIS, medical grade terpene resin, compound transdermal accelerator (72-6:1, 2-propanediol mass ratio=1:0.1) and compound antioxidant (antioxidant 1010: antioxidant 264 Mass ratio=1: 5) is to carry out back-up respectively by mass percent as 15%, 28.5%, 54%, 1% and 1.5%; The consumption of organic solvent (cyclohexane: ethyl acetate mass ratio=1: 1) is 20ml / g IBU;

[0030] 2) Same as step 2) in Example 1.

Embodiment 3

[0032] 1) Combine IBU, SIS, medical grade terpene resin, compound transdermal accelerator (72-6:1, 2-propanediol mass ratio=1:0.5) and compound antioxidant (antioxidant 1010: antioxidant 264 Mass ratio=1: 0.1) is carried out back-up according to mass percentage respectively at 5%, 65%, 25%, 4% and 1%; The consumption of organic solvent (cyclohexane: ethyl acetate mass ratio=1: 0.1) is 20ml / g IBU;

[0033] 2) Same as step 2) in Example 1.

[0034] 1. Drug release test

[0035] Get the ibuprofen transdermal release patch prepared in embodiment 1-3 and carry out in vitro guinea pig permeability test, concrete steps are as follows:

[0036] Fix the pretreated guinea pig skin between the supply chamber and the receiving chamber of the Franz diffusion cell, the cuticle faces the supply chamber, and the supply liquid is close to the cuticle, and a freshly prepared phosphate buffer solution with a pH of 7.4 is added to the receiving chamber When it is full, the dermis side is in f...

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Abstract

The invention provides an ibuprofen (IBU) percutaneous-release paster and a preparation method thereof, belonging to the technical field of medicine. No ibuprofen percutaneous-release paster is available in the prior art. The paster of the invention comprises an anti-sticking layer, a drug-storing layer and a backing layer, wherein, the drug-storing layer comprises the following components: 5wt% to 15wt% of IBU, 28.5wt% to 65wt% of SIS, 25wt% to 54% of tackifying resin, 1wt% to 5wt% of compound penetration enhancer and 1wt% to 2wt% of compound anti-oxidant. The preparation method of the IBU percutaneous-release paster comprises the following steps: adding the other components after the SIS and the tackifying terpine resin swell in the organic solvent; agitating on an ultrasound basis; coating the anti-sticking layer; air drying and vacuum drying; and covering the backing layer. The percutaneous-release paster has the advantages that the paster is not irritant or allergic to skins, the drug release can be easily controlled and the duration of the drug effect is long.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a transdermal release patch containing ibuprofen and a preparation method thereof. Background technique [0002] Ibuprofen (IBU) is a phenylpropionic acid non-steroidal anti-inflammatory drug widely used in clinical practice. For the treatment of rheumatoid arthritis, ankylosing spondylitis, osteoarthritis and rheumatoid arthritis, etc.; for somatic pain and dysmenorrhea, such as joint pain, muscle pain, headache, toothache, neuralgia, etc.; can also be used for Antipyretic of high fever and cold caused by various reasons. [0003] Currently used ibuprofen dosage form exists tablet, sustained-release tablet, sustained-release capsule, granule, oral liquid, suppository, cream, liniment and compound preparation. Among them, the oral dosage form is easy to cause gastrointestinal adverse reactions, and due to the short biological half-life of ibuprofen, frequent medication is requ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K47/32A61K31/192A61P29/00
Inventor 王秀芬邱亮
Owner BEIJING UNIV OF CHEM TECH
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