CN107028918A - A kind of slow controlled release transdermal patch containing lisinopril - Google Patents
A kind of slow controlled release transdermal patch containing lisinopril Download PDFInfo
- Publication number
- CN107028918A CN107028918A CN201710210226.8A CN201710210226A CN107028918A CN 107028918 A CN107028918 A CN 107028918A CN 201710210226 A CN201710210226 A CN 201710210226A CN 107028918 A CN107028918 A CN 107028918A
- Authority
- CN
- China
- Prior art keywords
- lisinopril
- controlled release
- transdermal patch
- slow controlled
- layer
- 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.)
- Granted
Links
Classifications
-
- 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
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- 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
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of slow controlled release transdermal patch containing lisinopril, it is related to field of pharmaceutical preparations, including：Drug-reservoir layer, back sheet and protective layer; the drug-reservoir layer is made up of lisinopril, bank matrix and permeation enhancers; often paste lisinopril 10mg~80mg containing effective dose in the drug-reservoir layer of the slow controlled release transdermal patch; by mass percentage, lisinopril 2.5~25%, bank matrix 70%~97%, permeation enhancers 0.5%~5% are contained in the drug-reservoir layer.The slow controlled release transdermal patch containing lisinopril of the present invention is compared with lisinopril conventional tablet, capsule or oral slow-releasing preparation in the market, and insoluble drug release is uniform, and curative effect is determined, steady quality.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, and in particular to a kind of slow controlled release transdermal patch containing lisinopril.
Background technology
Lisinopril is angiotensin converting enzyme inhibitors of new generation, and it is mainly tight by suppressing adrenaline-blood vessel
Zhang Su-RAAS reduces blood pressure, and is mainly used in treating essential hypertension.Its structural formula is：
Molecular formula：C21H35N3O7。
The preparation of country's lisinopril is mainly the oral tablet of film coating, each oral 5~10mg, one day one now
It is secondary.Plasma peak concentration is general after it is oral occurs for 7 hours or so after the tablet has been ingested, but myocardial infarction patients plasma peaks are dense
Degree time of occurrence has slight delayed trend, and it is 12.6 hours that effective half-life is accumulated after multiple medication, the decay of its blood concentration
In extension end phase, but drug accumulation is not caused.
The characteristics of breaking-out of hypertensive patient has daily rhythmicity.Rhythm and pace of moving things change is presented in human blood-pressure in 24h, clear
Morning is rapidly increased to peak value, midnight to valley after waking up.Morning peak phenomenon is two key characters of blood pressure, therefore preferably depressor,
There should be preferable compliance, and should be steadily depressured in 24 hours periods, it is ensured that hyperpietic's degree of safety crosses cardiovascular and cerebrovascular
Each emergency case of event, and the effectively function of the target organs such as the protection heart, brain and kidney.For the blood pressure of human body as described above
The rhythm and pace of moving things changes, and selects suitable medicine and reasonable administration time, makes medicine effect consistent with the rhythm and pace of moving things that hypertension occurs, so as to reach
The emphasis paid close attention to optimal therapeutic effect and when reducing the purpose of adverse drug reaction as hypertension drug development.
Lisinopril preparation is conventional tablet and capsule in existing market, it cannot be guaranteed that sick in 24 hours after taking
People's blood concentration is stable, does not reach preferable antihypertensive effect.Chinese invention patent CN103006612 provides a kind of lisinopril
Slowbreak sustained-release tablet and preparation method thereof, it discloses a kind of sustained release preparation of lisinopril, said preparation is thin outside medicine
Punched in film coating tablet is made, and its principal component is discharged by the aperture of coating.The patent can reach 24
Steady antihypertensive effect in hour, but its complex process, technique associated technical parameters are difficult to control, poor reproducibility, rate of release
It is unstable.Its Compliance is bad for patients simultaneously, weekly there is still a need for multiple dosing.
The content of the invention
For defect present in prior art, it is an object of the invention to provide a kind of slow controlled release containing lisinopril is saturating
Skin patch, stable blood concentration can be maintained for a long time, and favorable reproducibility, rate of release is stable.
To achieve the above objectives, the present invention is adopted the technical scheme that：
A kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet and protective layer, the medicine
Storage layer is made up of lisinopril, bank matrix and permeation enhancers, by mass percentage, each component in the drug-reservoir layer
Content is as follows：
Lisinopril 2.5%~25%
Bank matrix 70%~97%
Permeation enhancers 0.5%~5%.
On the basis of above-mentioned technical proposal, the bank matrix is silicone pressure-sensitive adhesive, Medical PSA, acrylic acid
In ester pressure-sensitive, carbomer, triethanolamine, PVP, methylcellulose, ethyl cellulose or sodium carboxymethylcellulose at least
It is a kind of.
On the basis of above-mentioned technical proposal, the permeation enhancers are the compound of lecithin and azone, the rush infiltration
The ratio of mass percent shared by lecithin and azone is 1 in agent:2/3~3/2.
On the basis of above-mentioned technical proposal, the protective layer material be selected from polyethylene, polystyrene, politef or
The separate paper crossed by waxing/organosilicon isolation processing.
On the basis of above-mentioned technical proposal, the back sheet is by the impermeable flexible material of medicine is made, the back of the body
Lining is selected from the compound thin layer of non-woven fabrics, polyvinyl chloride, polyethylene, polystyrene, polyester or above-mentioned substance composition.
On the basis of above-mentioned technical proposal, the slow controlled release transdermal patch containing lisinopril also includes adhered layer, institute
Adhered layer is stated for blank pressure-sensitive adhesive layer.
On the basis of above-mentioned technical proposal, the adhered layer includes silicone pressure-sensitive adhesive, acrylate pressure-sensitive adhesive, natural rubber
One or more in glue and carbomer.
On the basis of above-mentioned technical proposal, contain effective agent in the drug-reservoir layer for often pasting the slow controlled release transdermal patch
The content of bank matrix is 50-150mg/cm2 in lisinopril 10mg~80mg of amount, the storage layer.
On the basis of above-mentioned technical proposal, the drug release rate of the slow controlled release transdermal patch containing lisinopril is
95-98%.
On the basis of above-mentioned technical proposal, lisinopril and quality percentage shared by permeation enhancers in the drug-reservoir layer
The ratio of ratio is 4:0.5~1.5.
Compared with prior art, the advantage of the invention is that：
(1) the slow controlled release transdermal patch containing lisinopril of the invention and lisinopril conventional tablet in the market,
Capsule or oral slow-releasing preparation are compared, and insoluble drug release is more uniform, favorable reproducibility, and curative effect is determined, steady quality.
(2) the slow controlled release transdermal patch containing lisinopril of the invention promotees to permeate by adding the compounding of lecithin and azone
Agent enables the continual and steady release of principal component in a long time, it is to avoid the first pass effect and intestines and stomach of liver during oral medication
Stimulate the reaction, more lisinopril conventional tablet, capsule or oral slow-releasing preparation the longer blood concentration stage of stable development can be provided,
Per 1-8 days only with being administered once, Compliance is preferable.
(3) the slow controlled release transdermal patch containing lisinopril of the invention is easy to use, and protective layer is torn and is affixed on skin
, during medication, such as occur drug side-effect, tear can terminate administration, it is necessary to when be further continued for sticking, improve
Patient medication security.
Embodiment
The present invention is described in further detail with reference to embodiments.
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet
And protective layer, drug-reservoir layer be made up of lisinopril, bank matrix and permeation enhancers, by mass percentage, drug-reservoir
Each component content is as follows in layer：
Lisinopril 2.5~25%
Bank matrix 70%~97%
Permeation enhancers 0.5%~5%.
Wherein, bank matrix can be silicone pressure-sensitive adhesive, Medical PSA, acrylate pressure-sensitive adhesive, carbomer, three second
One or more of mixtures in hydramine, PVP, methylcellulose, ethyl cellulose and sodium carboxymethylcellulose.Rush is oozed
Saturating agent can be lecithin and the compound of azone；The material of protective layer can select polyethylene, polystyrene, politef or make
With the separate paper crossed by waxing or organosilicon isolation processing；Back sheet can be by the impermeable flexible material of medicine be made, such as
It can select the compound thin layer of non-woven fabrics, polyvinyl chloride, polyethylene, polystyrene, polyester or above-mentioned substance composition.
The slow controlled release transdermal patch containing lisinopril in the embodiment of the present invention may also include adhered layer, and adhered layer can be sky
White pressure-sensitive adhesive layer.The material of adhered layer can be selected according to actual pharmacy demand, such as can select silicone pressure-sensitive adhesive, Acrylate pressure sensitive
One or more in glue, natural rubber and carbomer.
It is main in the present invention to make lisinopril release uniform by the interaction of lisinopril and permeation enhancers, so that
Reach the effect of the prolonged stabilization for maintaining blood concentration.In general, it is slow containing lisinopril in the embodiment of the present invention
The drug release time of controlled release transdermal patch is 1-8 days, and its burst size is 10mg/ days.Rely promise through testing in obtained drug-reservoir layer
The mass percent of Puli and permeation enhancers is 4:0.5-1.5, its preferred proportion scope can be 4:0.95-1.05, is demonstrate,proved through experiment
It is bright, more commonly matched somebody with somebody using its drug transdermal speed of the slow controlled release transdermal patch containing lisinopril of the invention matched in preferred scope
Than product increase by 5% or so, medicine adds up transit dose lifting 1-2%.
Often lose money in a business slow controlled release transdermal patch of the invention containing lisinopril drug release area be 1cm2~4cm2, skin penetration rate is
0.05mg/h·cm2~0.15mg/hcm2, sustained release drugs 1~8 day.Bank substrates quantity in the storage layer can be determined
For 50-150mg/cm2, preferably 80-120mg/cm2.The slow controlled release transdermal containing lisinopril in the obtained present invention is taken during administration
Patch is affixed on skin, is 10mg per consumption per day, the patch of various dose is selected according to time length.This administering mode was both
The effective dose that lisinopril during general treatment is used can be met, Treatment need is met；Again can as shown in rear test data,
Adjustment less on the premise of, significantly improve the blood medicine time to peak and plasma concentration half life of patient, play steadily in the long term to
The effect of medicine.
Below, by 6 embodiments, the present invention will be further described.
Embodiment 1
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet
And protective layer, the drug-reservoir layer is made up of lisinopril, bank matrix and permeation enhancers, often containing lisinopril described in patch
Slow controlled release transdermal patch contains the lisinopril 80mg of effective dose, by mass percentage, containing bad in the drug-reservoir layer
The content of bank matrix is 100mg/cm in promise Puli 16%, bank matrix 80%, permeation enhancers 4%, drug-reservoir layer2。
Contain in every 1000 patch embodiment in the drug-reservoir layer of transdermal patch：Lisinopril 80g, Polyisobutylene pressure sensitive
Glue 400g, lecithin 10g, azone 10g.Its back sheet is polyvinyl chloride, and protective layer is polyethylene.
Embodiment 2
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet,
Protective layer and adhered layer, the drug-reservoir layer are made up of lisinopril, bank matrix and permeation enhancers, often paste described containing bad promise
The slow controlled release transdermal patch of Puli contains the lisinopril 40mg of effective dose, by mass percentage, the drug-reservoir layer
In contain the content of bank matrix in lisinopril 10%, bank matrix 87.75%, permeation enhancers 2.25%, drug-reservoir layer and be
87.75mg/cm2。
Contain in every 1000 patch embodiment in the drug-reservoir layer of transdermal patch：Lisinopril 40g, silicone pressure-sensitive adhesive
320g, carbomer 15g, triethanolamine 16g, lecithin 4.5g, azone 4.5g.Its back sheet is non-woven fabrics, and protective layer is process
The separate paper that waxing or organosilicon isolation processing are crossed, adhered layer is silicone pressure-sensitive adhesive.
Embodiment 3
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet,
Protective layer, the drug-reservoir layer is made up of lisinopril, bank matrix and permeation enhancers, often pastes described slow containing lisinopril
Controlled release transdermal patch contains the lisinopril 80mg of effective dose, by mass percentage, containing bad promise in the drug-reservoir layer
The content of bank matrix is 50mg/cm in Puli 25%, bank matrix 70%, permeation enhancers 5%, drug-reservoir layer2。
Contain in every 1000 patch embodiment in the drug-reservoir layer of transdermal patch：Lisinopril 80g, silicone pressure-sensitive adhesive
287g, PVP 5g, methylcellulose 8g, lecithin 12g, azone 8g.Its back sheet is polyester film, and protective layer is poly- four chloroethene
Alkene film.
Embodiment 4
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet,
Protective layer and adhered layer, the drug-reservoir layer are made up of lisinopril, bank matrix and permeation enhancers, often paste described containing bad promise
The slow controlled release transdermal patch of Puli contains the lisinopril 80mg of effective dose, by mass percentage, the drug-reservoir layer
In contain lisinopril 25%, bank matrix 70%, permeation enhancers 5%, drug-reservoir layer in bank matrix content be 50mg/
cm2。
Contain in every 1000 patch embodiment in the drug-reservoir layer of transdermal patch：Lisinopril 80g, silicone pressure-sensitive adhesive
380g, PVP 12g, sodium carboxymethylcellulose 8g, lecithin 11g, azone 9g.Its back sheet be polyvinyl chloride, polyethylene and
The compound thin layer of polystyrene film composition, protective layer is polystyrene film, and adhered layer is silicone pressure-sensitive adhesive.
Embodiment 5
The embodiment of the present invention provides a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet,
Protective layer and adhered layer, the drug-reservoir layer are made up of lisinopril, bank matrix and permeation enhancers, often paste described containing bad promise
The slow controlled release transdermal patch of Puli contains the lisinopril 10mg of effective dose, by mass percentage, the drug-reservoir layer
In contain the content of bank matrix in lisinopril 2.5%, bank matrix 97%, permeation enhancers 0.5%, drug-reservoir layer and be
150mg/cm2。
Contain in every 1000 patch embodiment in the drug-reservoir layer of transdermal patch：Lisinopril 10g, Acrylate pressure sensitive
Glue 880g, ethyl cellulose 105g, lecithin 3g, azone 2g.Its back sheet is polyvinyl chloride, polyethylene and polystyrene film group
Into compound thin layer, protective layer is polyethylene film, and adhered layer is the mixture of acrylate pressure-sensitive adhesive and carbomer.
Embodiment 6
The difference of the embodiment of the present invention and embodiment 4 is：Without addition permeation enhancers in the present embodiment, and by adhered layer
It is changed to natural rubber.
The preparation method of pressure sensitive adhesive is transdermal patch in this area conventional method, each embodiment in various embodiments of the present invention
Preparation method is as follows：
S1, the bank matrix is taken, be mixed and heated to 70 DEG C of softenings with lecithin and azone, stir；
S2, take lisinopril plus suitable quantity of water to be added after dissolving in step S1 mixtures, stir, be well mixed；
S3, mixture obtained by step S2 is coated on protective layer, controls thickness, dried at 50 DEG C, be covered with backing
Layer, is cut into every 4cm2Produce.
For the Cutaneous permeation effect of the slow controlled release transdermal patch containing lisinopril in detection various embodiments of the present invention, carry out such as
Lower skin absorbs transmitance experiment：
Example 1-6 sample, determines its transmitance, and specific method is as follows：
Mouse 6 is taken, unhairing, mouse skin is peeled, remove oil layer.Mouse skin after processing is placed in Double-layered glass bottle
In, volume 100ml is filled in bottle, pH value is 6.8 phosphate buffer, is stirred using magnetic stirring apparatus, interlayer heating
Temperature is 32 DEG C, takes 4cm2Sample is affixed on mouse skin, respectively at 2h, 4h, 8h, 24h, 48h, 72h, 96h, 120h, 144h,
168h, 196h are sampled, and then supply sampling amount.Drugs through skin amount is detected, embodiment 2 is sampled to 96 hours, embodiment 5 takes
Sample was by 24 hours.
The detection method of lisinopril transit dose：
It is filler with octadecylsilane chemically bonded silica using chromatographic condition and system suitability；With acetonitrile-phosphorus
(0.02mol/L sodium dihydrogen phosphates adjust pH value to 5.0) (8 to phthalate buffer with sodium hydroxide test solution:92) it is flowing
Phase；Detection wavelength is 215nm；50 DEG C of column temperature.The separating degree of lisinopril should be greater than 5.0, and number of theoretical plate is based on lisinopril peak
Calculation is not less than 700.
During measure, take lisinopril reference substance, it is accurately weighed, dissolved with water and quantify dilution be made in every 1ml containing about
0.2mg solution, precision measures 20 μ l, injects liquid chromatograph, records chromatogram；Each sample separately is taken, filters, takes subsequent filtrate 20
μ l, inject liquid chromatograph, record chromatogram.By external standard method with calculated by peak area, the detection knot of lisinopril transit dose is produced
Really.
Transmitance testing result is as shown in the table：
Lisinopril transit dose in the embodiment 1-6 of table 1
It relies promise when the slow controlled release transdermal patch containing lisinopril is used in test data, various embodiments of the present invention
Puli's transit dose and accumulative release time are in good linear relationship.The rush being made up of in increase the compound of lecithin and azone
After bleeding agent, compared with control group (embodiment 6), the lisinopril transit dose in the unit interval adds 20% or so；Simultaneously
Can be seen that by transit dose-time graph, after increase permeation enhancers, lisinopril transit dose and accumulative release time more towards
Linear relationship, its insoluble drug release is more steady.
For the blood medicine content control effect of the slow controlled release transdermal patch containing lisinopril in detection various embodiments of the present invention, enter
The following experiment of row：
Example 1-3 sample, test group patient skin is affixed on by the slow controlled release transdermal patch sample containing lisinopril,
Calculated by every consumption per day 10mg, administration time and frequency are concluded according to the effective dose of lisinopril in each group sample, continuously given
Medicine 6 days；Control group uses the lisinopril oral tablet (name of an article bought on the market：Lisinopril Tablets in Chinese Volunteers (trade name Zestril), life
Production company：Britain AstraZeneca UK Limited, registration certificate number：H20091050,2009-12-02, medicine characteristic：Chemistry
Medicine, 10mg), using the amount tablet for taking lisinopril effective dose 10mg daily, mouth is carried out every the 12h modes for taking 5mg
Clothes, continuously take 6 days, and respectively at 2h after first time administration/medication, 4h, 8h, 12h, 16h, 24h, 36h, 48h, 60h, 72h,
84h, 96h, 108h, 120h, 132h, 144h, 156h, 168h, 180h, 192h, its blood concentration is determined using HPLC-MS/MS,
The blood medicine content of user is recorded, and pharmacokinetic model fitting and parameter are carried out to blood concentration-time data using DAS softwares
Calculate.
Each group blood medicine content detection result is as shown in the table：
The blood medicine content of patient in the embodiment 1-3 of table 2 and control group
From test data, its blood concentration change in continuous medication is in patch of the present invention with conventional oral tablets
Cyclic swing, the situation when blood concentration variation tendency after administration is substantially to single-dose for the last time is similar：Present invention patch
Blood concentration after agent administration slowly rises, up to peak after again slow decline；And the blood concentration of conventional oral tablets it is then quick on
Rise, up to peak after rapid decrease.Upon administration all there is marked difference, this hair in both corresponding time points in 3~24h blood concentration
Nearly 2 times of 12h concentration after 12h concentration is discontinued for conventional oral tablets after bright patch is discontinued, 24h after patch of the present invention is discontinued
Concentration is nearly 4 times of 12h concentration after conventional oral tablets are discontinued, and this marked difference shows the sustained release effect of patch of the present invention
Really.Knowable to plasma concentration and blood concentration in the contrast embodiment of the present invention and control group during stable state, the system of patch of the present invention
Agent technique has no effect on the absorption of medicine, simply plays regulating and controlling effect to its absorption rate, reaches controlled release dose, delay blood medicine dense
Spend the purpose of decay.
The present invention is not limited to the above-described embodiments, for those skilled in the art, is not departing from
On the premise of the principle of the invention, some improvements and modifications can also be made, these improvements and modifications are also considered as the protection of the present invention
Within the scope of.The content not being described in detail in this specification belongs to prior art known to professional and technical personnel in the field.
Claims (10)
1. a kind of slow controlled release transdermal patch containing lisinopril, including drug-reservoir layer, back sheet and protective layer, its feature exist
In：
The drug-reservoir layer is made up of lisinopril, bank matrix and permeation enhancers, by mass percentage, the medicine storage
Each component content is as follows in the layer of storehouse：
Lisinopril 2.5%~25%
Bank matrix 70%~97%
Permeation enhancers 0.5%~5%.
2. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：The bank matrix is silicon
Ketone pressure sensitive adhesive, Medical PSA, acrylate pressure-sensitive adhesive, carbomer, triethanolamine, PVP, methylcellulose, ethyl
At least one of cellulose or sodium carboxymethylcellulose.
3. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：The permeation enhancers are ovum
The ratio of mass percent shared by lecithin and azone is 1 in the compound of phosphatide and azone, the permeation enhancers:2/3~3/
2。
4. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：The protective layer material choosing
The separate paper crossed from polyethylene, polystyrene, politef or process waxing/organosilicon isolation processing.
5. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：The back sheet is by medicine
The impermeable flexible material of thing is made, the back sheet be selected from non-woven fabrics, polyvinyl chloride, polyethylene, polystyrene, polyester or on
State the compound thin layer of material composition.
6. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：It is described containing lisinopril
Slow controlled release transdermal patch also includes adhered layer, and the adhered layer is blank pressure-sensitive adhesive layer.
7. the slow controlled release transdermal patch as claimed in claim 6 containing lisinopril, it is characterised in that：The adhered layer includes silicon
One or more in ketone pressure sensitive adhesive, acrylate pressure-sensitive adhesive, natural rubber and carbomer.
8. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：Often paste the slow controlled release saturating
Bank matrix contains in lisinopril 10mg~80mg containing effective dose in the drug-reservoir layer of skin patch, the storage layer
Measure as 50-150mg/cm2。
9. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：It is described containing lisinopril
The drug release rate of slow controlled release transdermal patch is 95-98%.
10. the slow controlled release transdermal patch as claimed in claim 1 containing lisinopril, it is characterised in that：The drug-reservoir layer
The ratio of mass percent shared by middle lisinopril and permeation enhancers is 4:0.5~1.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710210226.8A CN107028918B (en) | 2017-03-31 | 2017-03-31 | Sustained-release transdermal patch containing lisinopril |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710210226.8A CN107028918B (en) | 2017-03-31 | 2017-03-31 | Sustained-release transdermal patch containing lisinopril |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107028918A true CN107028918A (en) | 2017-08-11 |
| CN107028918B CN107028918B (en) | 2020-08-25 |
Family
ID=59534804
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710210226.8A Active CN107028918B (en) | 2017-03-31 | 2017-03-31 | Sustained-release transdermal patch containing lisinopril |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107028918B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110694036A (en) * | 2019-08-21 | 2020-01-17 | 云南中医药大学 | Sanfu plaster with slow release function and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1633994A (en) * | 2004-11-04 | 2005-07-06 | 中国人民解放军总医院 | Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method |
| US20050203168A1 (en) * | 2004-03-11 | 2005-09-15 | The Regents Of The University Of Michigan | Angiotensin converting enzyme inhibitor use for treatment and prevention of gastrointestinal disorders |
| CN101653440A (en) * | 2008-08-18 | 2010-02-24 | 北京瑞康医药技术有限公司 | Treatment composition containing amlodipine series salt and pril medicament |
| CN104983723A (en) * | 2015-08-03 | 2015-10-21 | 徐静 | External application patch containing enalapril and application thereof |
| CN105213355A (en) * | 2015-11-09 | 2016-01-06 | 徐静 | A kind of external slow-release transdermal patch and application thereof containing ramipril |
-
2017
- 2017-03-31 CN CN201710210226.8A patent/CN107028918B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050203168A1 (en) * | 2004-03-11 | 2005-09-15 | The Regents Of The University Of Michigan | Angiotensin converting enzyme inhibitor use for treatment and prevention of gastrointestinal disorders |
| CN1633994A (en) * | 2004-11-04 | 2005-07-06 | 中国人民解放军总医院 | Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method |
| CN101653440A (en) * | 2008-08-18 | 2010-02-24 | 北京瑞康医药技术有限公司 | Treatment composition containing amlodipine series salt and pril medicament |
| CN104983723A (en) * | 2015-08-03 | 2015-10-21 | 徐静 | External application patch containing enalapril and application thereof |
| CN105213355A (en) * | 2015-11-09 | 2016-01-06 | 徐静 | A kind of external slow-release transdermal patch and application thereof containing ramipril |
Non-Patent Citations (1)
| Title |
|---|
| 刘福强 等: "《医师案头用药参考 中成药、化学药》", 31 March 2013, 中国中医药出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110694036A (en) * | 2019-08-21 | 2020-01-17 | 云南中医药大学 | Sanfu plaster with slow release function and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN107028918B (en) | 2020-08-25 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI411452B (en) | Transdermal therapeutic system for administering the active ingredient buprenorphine | |
| US8071125B2 (en) | Transdermal patch containing isosorbide dinitrate and bisoprolol | |
| RU2355387C2 (en) | Transdermal granisetron | |
| EP2062575B1 (en) | Adhesive preparation comprising desglymidodrine | |
| CN107669662A (en) | Transdermal delivery system comprising buprenorphine | |
| EP2233142A1 (en) | Transdermally absorptive preparation | |
| JP2011513287A (en) | Pharmaceutical composition | |
| CN107028918A (en) | A kind of slow controlled release transdermal patch containing lisinopril | |
| CA3079694A1 (en) | Transdermal therapeutic system for the transdermal administration of guanfacine comprising a silicone acrylic hybrid polymer | |
| JP2023506538A (en) | Transdermal therapeutic system containing agomelatine | |
| CN101822652B (en) | Vinpocetine transdermal patch and preparation method thereof | |
| JPH04150865A (en) | Medical pressure-sensitive tape and tape pharmaceutical preparation for therapy of disease | |
| BRPI0619419A2 (en) | matrix controlled transdermal systems comprising salts of the ac inhibitor dicarboxylic acids | |
| WO2012090322A1 (en) | Patch | |
| EP2062576B1 (en) | Adhesive preparation comprising desglymidodrine | |
| JP7005539B2 (en) | A transdermal delivery system containing methylphenidate or a salt thereof and a method thereof. | |
| JPH10265371A (en) | Transcutaneous absorption plaster | |
| JPH03123728A (en) | Medical system through skin having norpsoidephedrine as active ingredient | |
| CN106620644A (en) | Stable perindopril indapamide tablet and preparation technology | |
| CN105213355A (en) | A kind of external slow-release transdermal patch and application thereof containing ramipril | |
| CN109481423B (en) | Diclofenac salt transdermal patch and preparation method thereof | |
| WO1998046267A1 (en) | Base composition for percutaneous absorption and percutaneously absorbable preparation containing the base composition | |
| CN103800307A (en) | Medicinal composition for reducing blood pressure and preparation method thereof | |
| CN110115710A (en) | It is a kind of for treating the transdermal absorption formulation of asthma | |
| JPH10511972A (en) | Transdermal therapeutic system for the administration of (s) -3-methyl-5- (1-methyl-2-pyrrolidenyl) -isoxazole or one of its pharmaceutically acceptable salts |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |