CN2323782Y - Constant release paster for metoprolol - Google Patents

Constant release paster for metoprolol Download PDF

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Publication number
CN2323782Y
CN2323782Y CN 98205051 CN98205051U CN2323782Y CN 2323782 Y CN2323782 Y CN 2323782Y CN 98205051 CN98205051 CN 98205051 CN 98205051 U CN98205051 U CN 98205051U CN 2323782 Y CN2323782 Y CN 2323782Y
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China
Prior art keywords
layer
paster
metoprolol
perseverance
released
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Expired - Fee Related
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CN 98205051
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Chinese (zh)
Inventor
王丽霞
李荣堂
郝金生
王婉云
尹成军
银燕
贾海莲
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Individual
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Individual
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Abstract

The utility model relates to a constant release paster for metoprolol, which is orderly composed of five layers of a protective layer, a contacting adhesion layer, a controlled release layer, a medicine storing layer and a surface pasting layer form inward to outward, wherein the medicine storing layer is dope which is formed by mixing and dissolving metoprolol, hydrogen ketone, povidone, hydroxypropylmenthyl cellulose, distilled water and chloroform; the controlled release layer is an expanding object which is formed by mixing and dissolving ethylene-vinyl acetate copolymer, tween-80, glycerine and the distilled water; the contacting adhesion layer is formed in the way that acrylate, benzoic acid, atolin and chloroform are mixed, dissolved and dried to be coated on a piece of siliconizing anti-pasting paper. The utility model has the advantages of convenient use, safety, good therapeutic effect, simple structure and easy production.

Description

The metoprolol perseverance is released paster
This utility model relates to pharmaceutical products, and concrete is that a kind of metoprolol perseverance is released paster.
Metoprolol (metoprolol) is a beta-blocker, be widely used in hypertension, coronary heart disease, heart disease and angioneurotic treatment of fainting mainly were oral and intravenously administrable dosage form in the past, be characterized in medicine onset rapidly, short time can reach higher blood drug level rapidly, but difficulty is kept equilibrium concentration, and the consumption of beta-blocker has tangible individual variation, same Genus Homo, the consumption of beta-blocker can differ several times.
Beta-blocker has tangible decreased heart rate, reduces myocardial oxygen consumption, the effect of bringing high blood pressure down, bradycardia can occur when excessive, clinical symptoms such as hypopiesia, and the individual variation of drug metabolism does not still have clear and definite method detection at present, therefore, initially give low dose of close observation, adjusting dosage at any time is the means that adopt at present.
The percutaneous controlled-release technology is a kind of medicine-feeding technology of up-to-date rise in the world, in the skin surface administration, medicine passes through each layer of skin with constant speed under the control of release-controlled film, enters the blood of human body circulation, produce the whole body therapeutic effect, and the metoprolol perseverance is released the paster product of this new technique just.
The purpose of this utility model provides a kind of metoprolol perseverance and releases paster, and is easy to use, safe, therapeutic effect good, and simple in structure, is easy to produce.
The purpose of this utility model is achieved in that
A kind of metoprolol perseverance is released paster, is effigurate bedded structure, it is characterized in that:
This paster successively by 1. protective layer, 2. contacts adhesion layer from the inside to the outside, 3. controlled release layer, 4. medicine storage layer, 5. appearance paste layer totally five layers of composition;
Wherein:
The medicine storage layer is for containing metoprolol.Hydrogen ketone, povidone, hydroxypropyl methylcellulose, the jelly that distilled water, chloroform mixed dissolution become;
Controlled release layer is the dilatant that contains ethylene one vinyl acetate co-polymer, tween 80, glycerol, distilled water mixed dissolution;
The contact adhesion layer volatilizes into pressure sensitive adhesive solution for containing acrylate, benzoic acid, liquid paraffin, chloroform mixed dissolution, is coated on the silication separate paper to constitute.
The purpose of this utility model can also realize by following measure:
Described appearance paste layer is plastic-coated/aluminium foil.
Described protective layer is a polyethylene film.
The face profile shape of described paster can be circular, oval, oblate, rectangle.
The face profile shape of described paster also comprises the lug of taking usefulness for finger off.
The metoprolol perseverance is released the slow release principle of paster:
Medicine see through skin enter the dosage form that produces whole body or local therapeutic effects in the body be called transdermal therapeutic system (transdermal therapeutil system, TTS).According to of the diffusion of ethylene one vinyl acetate co-polymer (EVA) film to some medicines, the principle of controlled release, we have developed the metoprolol perseverance and have released paster.
Medicine during by skin absorbs horny layer be main barrier, medicine passes through and determines the speed speed of drug transdermal absorption by passive diffusion principle in horny layer, when TTS drug release rate during greater than the diffusion velocity of medicine in horny layer, medicine be absorbed as the skin control release type, otherwise be the film controlling type of TTS, metoprolol has certain dissolubility in the EVA film, can spread to see through film, thereby available EVA film comes control drug release.
The metoprolol perseverance is released paster and has been compared following advantage with conventional administering mode:
1. Xian Jin percutaneous controlled-release treatment technology makes that constant speed continues to discharge in the medicine 72 hours, does not accumulate in vivo, and blood drug level remains on the valid density scope of equal perseverance always, pastes with once, and has greatly improved patient's treatment compliance in per 72 hours.
2. medicine absorbs through skin, entering body circulation directly acts on cardiovascular system and plays a role, avoided the first pass effect of liver, medicine is without digestive tract, eliminated medicine to GI irritation or infringement, avoided the decomposition of factors such as food digestion liquid and pH value to medicine, behind the removal paster, the medicine of storing in the local skin still can be kept effective blood drug concentration 12 hours.
3. formed blood drug level peak valley phenomenon when not having oral and intravenously administrable has been avoided the fluctuation of blood drug level, has avoided side effects of pharmaceutical drugs to greatest extent.
4. easy to use, it is painful not have injection, has avoided the trouble of oral drugs.
5. the metoprolol perseverance is released the paster scope of application:
1.. hypertension;
2.. arrhythmia;
3.. coronary heart disease;
4.. hypertrophic cardiomyopathy;
5.. the cardiovascular patient of heart rate variability sexual abnormality;
6.. angioneurotic treatment of fainting.
In a word, it is simple that the metoprolol perseverance is released paster structure, is easy to produce, safe in utilization, and convenient, clinical trial result is remarkable, for the treatment disease provides new route of administration.
Now in conjunction with the accompanying drawings:
Fig. 1 is the profile sketch map of this utility model one embodiment.
Fig. 2 is the A-A parting view of Fig. 1.
Please refer to Fig. 1, Fig. 2, constant release paster for metoprolol of the present utility model is made of following five layers of constituent from the inside to the outside successively,
1. protective layer: effect: prevent from contacting adhesion layer oxidation barrier and separate, remove in use this layer, exposure connects Touch adhesion layer.
2. contact adhesion layer: have adhesive attraction, this layer also is added with benzoic acid, can alleviate or eliminate the part The allergy of skin or inflammatory reaction.
3. controlled release layer can effective transdermal perseverance be released, and makes medicine under the effect of release-controlled film, with constant speed, See through skin, enter the body circulation, act on cardiovascular system and play a role.
4. medicine storage layer: to guarantee 72 hours constant-rate administrations, wherein be added with hydrogen ketone, can increase medicine thoroughly The skin ability promotes the infiltration of medicine.
5. appearance lining: be the support of paster.
Each forms the preparation of layer constant release paster for metoprolol:
The 3rd layer of controlled release layer:
Material: ethene one vinyl acetate co-polymer (EVA)
Tween-80 glycerol distillation water
Method for making: get a certain amount of EVA and add 5-7 distilled water doubly, soak and treat fully to expand rearmounted 85-90 ℃ water Heating lets cool its dissolving in the bath, slowly adds Tween-80, and glycerine after slowly stirring evenly, is added a cover, and places Night, treat that bubble eliminates, be poured on the glass plate that scribbles liquid paraffin, it is even to spread to thickness with the glass bar stand, The film that width equates, EVA release-controlled film one controlled release layer.
The 4th layer of medicine storage layer:
Material: metoprolol, hydrogen ketone, polyvinylpyrrolidone, HPMC, distilled water, chloroform.
Preparation: the above-mentioned substance mixed dissolution is become membranoid substance, be coated on the appearance lining, volatilize behind the chloroform The medicine storage layer.
The 2nd layer of contact adhesion layer:
Material: acrylate, benzoic acid, atoleine, chloroform, silication separate paper.
Preparation: with acrylate, liquid paraffin, benzoic acid, one reinstates chloroform dissolving, volatilizes behind the chloroform namely Become pressure sensitive adhesive solution, pressure-sensitive acid solution be coated on the silication separate paper, the contact adhesion layer.
The 1st layer of protective layer:
Material: polyethylene film.
The 5th layer of appearance lining:
Material: plastic-coated/aluminium foil.
During enforcement, the face profile shape of described paster can be circular, oval, oblate, square Shape (comprising square and rectangle).
The face profile shape of described paster can also include for finger and take the lug 6 of usefulness off (referring to figure 1).
Embodiment:
On circular plastic-coated/aluminium foil, put a certain amount of medicine storage film liquid, coated with release-controlled film, be coated with pressure sensitive adhesive solution behind the hot sealing edge, paste with the silication separate paper, again coated with polyethylene film, promptly make the metoprolol perseverance and release paster, this paster is the disk of radius 1.5cn, and every subsides contain the about 300mg of metoprolol, is affixed on the skin of chest to get final product.

Claims (5)

1, a kind of metoprolol perseverance is released paster, is effigurate bedded structure, it is characterized in that:
This paster successively by 1. protective layer, 2. contacts adhesion layer from the inside to the outside, 3. controlled release layer, 4. medicine storage layer, 5. appearance paste layer totally five layers of composition;
Wherein:
The medicine storage layer is for containing metoprolol.Hydrogen ketone, povidone, hydroxypropyl methylcellulose, the jelly that distilled water, chloroform mixed dissolution become;
Controlled release layer is the dilatant that contains ethylene-vinyl acetate copolymer, tween 80, glycerol, distilled water mixed dissolution;
The contact adhesion layer volatilizes into pressure sensitive adhesive solution for containing acrylate, benzoic acid, liquid paraffin, chloroform mixed dissolution, is coated on the silication separate paper to constitute.
2, metoprolol perseverance as claimed in claim 1 is released paster, it is characterized in that: described appearance paste layer is plastic-coated/aluminium foil.
3, metoprolol perseverance as claimed in claim 1 is released paster, it is characterized in that: described protective layer is a polyethylene film.
4, metoprolol perseverance as claimed in claim 1 is released paster, it is characterized in that: the face profile shape of described paster can be circular, oval, oblate, rectangle.
5, metoprolol perseverance as claimed in claim 1 is released paster, it is characterized in that: the face profile shape of described paster also comprises the lug of taking usefulness for finger off.
CN 98205051 1998-06-03 1998-06-03 Constant release paster for metoprolol Expired - Fee Related CN2323782Y (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 98205051 CN2323782Y (en) 1998-06-03 1998-06-03 Constant release paster for metoprolol

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 98205051 CN2323782Y (en) 1998-06-03 1998-06-03 Constant release paster for metoprolol

Publications (1)

Publication Number Publication Date
CN2323782Y true CN2323782Y (en) 1999-06-16

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Application Number Title Priority Date Filing Date
CN 98205051 Expired - Fee Related CN2323782Y (en) 1998-06-03 1998-06-03 Constant release paster for metoprolol

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101269056B (en) * 2007-03-19 2010-05-19 天津药物研究院 Metoprolol salt oral administration impulse pellet preparation

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101269056B (en) * 2007-03-19 2010-05-19 天津药物研究院 Metoprolol salt oral administration impulse pellet preparation

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GR01 Patent grant
C19 Lapse of patent right due to non-payment of the annual fee
CF01 Termination of patent right due to non-payment of annual fee