CN107028920A - Brufen bar cloth patch - Google Patents
Brufen bar cloth patch Download PDFInfo
- Publication number
- CN107028920A CN107028920A CN201710343235.4A CN201710343235A CN107028920A CN 107028920 A CN107028920 A CN 107028920A CN 201710343235 A CN201710343235 A CN 201710343235A CN 107028920 A CN107028920 A CN 107028920A
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- CN
- China
- Prior art keywords
- brufen
- phase component
- bar cloth
- oil
- cloth patch
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
A kind of brufen bar cloth patch, it is characterized in that the bar cloth patch is made up of back sheet, protective layer and drug-reservoir, the drug-reservoir is consisted of the following components in percentage by weight：It is used as the brufen 3%~5% of active component；Oil-phase component 5~10%, the oil-phase component is 1 by mass ratio:0.3~0.4 Glycerin, mixed triester with caprylic acid capric acid and octadecyl alcolol composition, brufen is scattered in oil phase；Sodium Polyacrylate 5 10% is neutralized as the part of water-phase component, Dihydroxyaluminium Aminoacetate 0.2%~0.4%, glycerine 10~15%, carbomer 934 1%~1.5%, sodium carboxymethylcellulose (CMC Na) 1.5~3%, mosatil 0.1%~0.3%, the water of pH adjusting agent, Tween 80 1%~1.5%, mannitol 10~15%, filler 1~3% and surplus.The pH adjusting agent is to adjust water-phase component pH to 5~6.5 sodium hydroxide solution.
Description
Technical field
The present invention relates to brufen bar cloth patch.
Background technology
Brufen (CAS：It is 15687-27-1) Alpha-Methyl -4- (2- methyl-propyls) phenylacetic acid, is that one kind has anti-inflammatory, town
Bitterly, the NSAIDs of refrigeration function.It is usually used in headache and arthritic treatment, when for rheumatoid arthritis, bone pass
When saving the treatment of the local inflammation such as inflammation, traditional Oral administration has that drug availability is low, and stomach and systemic side effects are big
Shortcoming.The chronic local inflammations such as arthritis need persistently to be treated, but existing brufen external preparation such as cream etc.
It is difficult to continual and steady release active ingredient and have impact on therapeutic effect, shares the clinical needs of medicine.Bar cloth patch
(Cataplasm) mean and medicine is dissolved or is mixed in water-soluble high-molecular material matrix, be coated on by lining material, for skin
Skin sticks a kind of New Percutaneous form of administration used.Bar cloth patch has drugloading rate compared with common external medicine preparation
Greatly；Water content is higher can to strengthen the aquation in skin to promote drug percutaneous to pass through, and to skin without allergic reaction and
Stimulation, without drawing pain and the advantages of noresidue during stripping, but also big just because of bar cloth patch drugloading rate, the application time compared with
It is long, need to take into account promotion Drug Percutaneous Absorption in progress prescription screening and make its insoluble drug release uniform, therefore offer one kind can
Quick acting, and realize that the brufen bar cloth patch for stablizing drug release for a long time turns into urgently to be resolved hurrily in the prior art and asked
Topic.
The content of the invention
To solve aforementioned technical problem, the invention provides a kind of brufen bar cloth patch, it is characterized in that the bar cloth is pasted
Agent is made up of back sheet, protective layer and drug-reservoir, and the drug-reservoir is consisted of the following components in percentage by weight：
It is used as the brufen 3%~5% of active component；Oil-phase component 5~10%, the oil-phase component is 1 by mass ratio:
0.3~0.4 Glycerin, mixed triester with caprylic acid capric acid and octadecyl alcolol composition, brufen is scattered in oil phase；
As water-phase component part neutralize Sodium Polyacrylate 5-10%, Dihydroxyaluminium Aminoacetate 0.2%~0.4%, glycerine 10~
15%, carbomer 934 1%~1.5%, sodium carboxymethylcellulose (CMC-Na) 1.5~3%, mosatil 0.1%~
0.3%, pH adjusting agent, Tween 80 1%~1.5%, mannitol 10~15%, the water of filler 1~3% and surplus.It is described
PH adjusting agent is to adjust water-phase component pH to 5~6.5 sodium hydroxide solution.
It is preferably NP700 that the part, which neutralizes Sodium Polyacrylate,；The filler is kaolin.
A kind of described brufen bar cloth patch, it is characterized in that glycerol content is preferably 10%, mannitol content is preferred
For 10%.
Find under study for action, the brufen bar cloth patch provided is provided, can make system by screening obtained optimizing prescriptions
Standby obtained brufen cataplasm patch can take into account quick release active ingredient and sustained release has within the 12h application time
Imitate composition two kinds of performances, in studying prescription it was found that currently preferred oil-phase component proportioning and aqueous phase into
Glycerine and mannitol proportioning are the decision components of decision active ingredient release characteristics in point.The exactly cooperation of said components, solution
Determine quick acting and long-acting release problem of the brufen Babu cream in the case where long-time is applied.
Embodiment
Brufen cataplasm in the embodiment of the present invention is prepared in accordance with the following methods
1) oil-phase component is prepared, and the raw material of oil-phase component is heated into 50-70 DEG C, adds brufen micro mist, dispersed with stirring
Obtain oil phase liquid (1)
2) water-phase component is scattered in water and obtains hydrogel, hydrogel is heated to after 50~70 DEG C to stir with uniform mixer
While to add temperature be 50-70 DEG C of oil phase liquid (1), oil phase is added after filler after adding and stirred；It is true through standing
The drug-reservoir of paste is obtained after sky degassing；
3) drug-reservoir is coated on back sheet, and protective layer is attached in upper surface.Obtain brufen bar cloth patch.Obtain
Brufen cataplasm specification be 5g drug-reservoirs/40cm2Back sheet
In all embodiments, it is NP700 (Showa Denko kk productions), filler that the part, which neutralizes Sodium Polyacrylate,
For 2% kaolin, NMF is glycerine.
The formula of embodiment 1~6 see the table below
The formula of reference examples 1~6 see the table below
Do not add mannitol (reference examples 1,2) compared with embodiment 1~6, in the formula of reference examples 1~6 or do not add third
Triol (reference examples 3,4) or the proportioning (reference examples 5,6) for changing two kinds of components of oil-phase component
By being investigated to the cataplasm that embodiment 1~6 is obtained, it is known that its flat appearance, uniform, drug-reservoir lotion
It is smooth；Mouldability, paste containing amount, initial bonding strength, adhesiveness and film residual quantity meet the requirements.
The extracorporeal releasing experiment of Pharmacological Examples 1
According to the 3rd method (oar dish method, for transdermal in drug release determination method in second annex XD of Chinese Pharmacopoeia 2010 edition
Patch) in the Ba Bu that is obtained to embodiment 1~6 of method that provides be adjacent to anxious drug release determination.Specific method is as follows
Experiment adds dissolution medium in stripping rotor using physiological saline as dissolution medium, and pre-temperature to (32 ± 0.5 DEG C) is by bar
Cloth cream removes protective layer, is cut into 2.5cmx7.5cm sizes, keeps flat into bag filter (molecular cut off 14,000), emission surface
Upward, it is placed between two layers of disk, disc edge is clamped bag filter two ends, then be fastened with rubber band, fixes disk.In
10min, 20min, 30min, 45min, 60min, 90min, 2h, 2.5h, 3h and 4h sample 6mL out of stripping rotor respectively, and mend
Fill isometric (32+0.5) DEG C fresh dissolution medium, parallel test 6, calculating of averaging.Show by detection, the application is real
The vitro release for applying the Babu cream in example reaches more than 90% in 2h.
Pharmacological Examples 2, percutaneous penetration
Using improved Fontan, using in vitro 3 months old rats skin of abdomen as barrier, with embodiment 1~6 and right
1~6 bar cloth patch prepared carries out carry out permeation test in vitro as usual.Specific experiment method is：
Take after the anesthesia execution of 3 monthly age healthy rats, eliminate belly wool with scissors, remove undamaged skin, remove subcutaneous
Tissue, is individually fixed in addition pH7.4 phosphate buffers work release in the liberation port of Franz diffusion cells, receiving chamber and is situated between after cleaning
Matter, keeps endodermis and solution close contact.The cataplasm for throwing off protective layer is affixed on skin, regulation water-bath makes outer layer jacket layer
Temperature is constant at (32 ± 0.5) DEG C, and mixing speed is 100rpm, and release was drawn respectively at 0,1h, 2h, 4h, 6h, 8h, 12h hours
Medium 4ml, while adding equivalent PBS liquid.Calculating accumulative absorption percentage, (brufen for adding up to pass through accounts for cloth in drug-reservoir
The fractions of ibuprofen total amount) result such as following table
The above results show, the brufen Babu cream that the present invention is provided, when carrying out Transdermal Absorption experiment, 12h's
Accumulative medicine transmitance is above 80%, and drug release rate is used with time more uniform, the explanation present invention that gathers way
In technical scheme, by the composition of preferred oil-phase component and water-phase component respectively, the transdermal suction of brufen cataplasm had both been improved
Speed is received, medicine more uniform release within the entirely application period can be controlled again, the balance of two kinds of characteristics is realized.
We have found that it is preferred that the proportioning of Glycerin, mixed triester with caprylic acid capric acid and octadecyl alcolol during prescription screening, and recipe quantity is added in aqueous phase simultaneously
After glycerine and mannitol, the effect of brufen Quick uniform release could be realized.By being shown with the control experiment of comparative example,
Change the proportioning of two kinds of components in oil-phase component, or be individually added into the brufen release that glycerine or mannitol can influence
Effect, the and it was also found that accessory formula and the relevant property of brufen in further experiment, when changing active component
When, even if using same accessory formula, can not also produce the Quick uniform that the brufen cataplasm of the invention provided has
Release the drug effect.
Claims (3)
1. a kind of brufen bar cloth patch, it is characterized in that the bar cloth patch is made up of back sheet, protective layer and drug-reservoir, institute
Drug-reservoir is stated to consist of the following components in percentage by weight：
It is used as the brufen 3%~5% of active component；Oil-phase component 5~10%, the oil-phase component is 1 by mass ratio:0.3
~0.4 Glycerin, mixed triester with caprylic acid capric acid and octadecyl alcolol composition, brufen is scattered in oil phase；
As water-phase component part neutralize Sodium Polyacrylate 5-10%, Dihydroxyaluminium Aminoacetate 0.2%~0.4%, glycerine 10~15%,
Carbomer 934 1%~1.5%, sodium carboxymethylcellulose (CMC-Na) 1.5~3%, mosatil 0.1%~0.3%, pH
The water of conditioning agent, Tween 80 1%~1.5%, mannitol 10~15%, filler 1~3% and surplus.
2. a kind of brufen bar cloth patch as claimed in claim 1, it is characterized in that the part neutralizes Sodium Polyacrylate
Preferably NP700；The filler is kaolin.
3. a kind of brufen bar cloth patch as claimed in claim 1, it is characterized in that glycerol content is preferably 10%, mannitol
Content is preferably 10%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710343235.4A CN107028920A (en) | 2017-05-16 | 2017-05-16 | Brufen bar cloth patch |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710343235.4A CN107028920A (en) | 2017-05-16 | 2017-05-16 | Brufen bar cloth patch |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107028920A true CN107028920A (en) | 2017-08-11 |
Family
ID=59538580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710343235.4A Pending CN107028920A (en) | 2017-05-16 | 2017-05-16 | Brufen bar cloth patch |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107028920A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995031193A1 (en) * | 1994-05-11 | 1995-11-23 | Laboratoires D'hygiene Et De Dietetique | Matrix system for the transdermal delivery of ibuprofen, and method for preparing same |
| CN101045041A (en) * | 2007-04-29 | 2007-10-03 | 武汉兵兵药业有限公司 | Cataplasma containing ibuprofen its preparing method and application |
| CN101502499A (en) * | 2009-03-13 | 2009-08-12 | 北京化工大学 | Ibuprofen percutaneous release patch and preparation method thereof |
| CN105287361A (en) * | 2015-11-13 | 2016-02-03 | 北京泰德制药股份有限公司 | External preparation containing non-steroid anti-inflammatory drug microemulsion and used for skin |
-
2017
- 2017-05-16 CN CN201710343235.4A patent/CN107028920A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995031193A1 (en) * | 1994-05-11 | 1995-11-23 | Laboratoires D'hygiene Et De Dietetique | Matrix system for the transdermal delivery of ibuprofen, and method for preparing same |
| CN101045041A (en) * | 2007-04-29 | 2007-10-03 | 武汉兵兵药业有限公司 | Cataplasma containing ibuprofen its preparing method and application |
| CN101502499A (en) * | 2009-03-13 | 2009-08-12 | 北京化工大学 | Ibuprofen percutaneous release patch and preparation method thereof |
| CN105287361A (en) * | 2015-11-13 | 2016-02-03 | 北京泰德制药股份有限公司 | External preparation containing non-steroid anti-inflammatory drug microemulsion and used for skin |
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| PB01 | Publication | ||
| PB01 | Publication | ||
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| TA01 | Transfer of patent application right | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20190531 Address after: 102629 Second Floor and Third Floor of Building 12, No. 50 Huatuo Road, Daxing Biomedical Base, Beijing (Liandong U Valley Biomedical Science and Technology Park) Applicant after: BEIJING MINGZE ZHONGHE MEDICAMENT RESEARCH CO., LTD. Address before: 528139 No. 20, Dushugang New Village Team, Lubao Town, Sanshui District, Foshan City, Guangdong Province Applicant before: Cai Zhihao |
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| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170811 |