CN107028918B - Sustained-release transdermal patch containing lisinopril - Google Patents
Sustained-release transdermal patch containing lisinopril Download PDFInfo
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- CN107028918B CN107028918B CN201710210226.8A CN201710210226A CN107028918B CN 107028918 B CN107028918 B CN 107028918B CN 201710210226 A CN201710210226 A CN 201710210226A CN 107028918 B CN107028918 B CN 107028918B
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- lisinopril
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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
- 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
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- 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
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- 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
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- 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
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
Abstract
The invention discloses a sustained and controlled release transdermal patch containing lisinopril, which relates to the field of pharmaceutical preparations and comprises the following components: the sustained-release transdermal patch comprises a drug storage layer, a back lining layer and a protective layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a penetration enhancer, the drug storage layer of each sustained-release transdermal patch contains 10-80 mg of lisinopril with effective dose, and the drug storage layer contains 2.5-25% of lisinopril, 70-97% of the storage matrix and 0.5-5% of the penetration enhancer by mass percentage. Compared with the lisinopril common tablets, capsules or oral sustained-release preparations on the current market, the lisinopril-containing sustained-release transdermal patch has the advantages of uniform drug release, definite curative effect and stable quality.
Description
Technical Field
The invention relates to the field of pharmaceutical preparations, in particular to a sustained-release transdermal patch containing lisinopril.
Background
Lisinopril is a new generation angiotensin converting enzyme inhibitor, which is mainly used for reducing blood pressure by inhibiting an epinephrine-angiotensin-aldosterone system, and is mainly used for treating essential hypertension. The structural formula is as follows:
the molecular formula is as follows: c21H35N3O7。
At present, the preparation of lisinopril in China is mainly an oral tablet coated by a film, 5-10 mg is taken orally every time, and the preparation is taken once a day. After the oral administration, the peak plasma concentration generally appears about 7 hours after the administration, but the peak plasma concentration appearance time of patients suffering from acute myocardial infarction has a slight lag trend, the cumulative effective half-life period after the repeated administration is 12.6 hours, and the blood concentration attenuation of the patients shows an extension end, but the accumulation of the drugs is not caused.
The onset of hypertensive patients is characterized by circadian rhythmicity. The blood pressure of human body shows rhythmic change within 24h, and rapidly rises to a peak value after waking in the early morning and reaches a valley value in the middle night. The morning peak phenomenon is two important characteristics of blood pressure, so that an ideal antihypertensive drug has better compliance, can stably reduce blood pressure within a 24-hour period, ensures that a hypertensive safely crosses all emergencies of cardiovascular and cerebrovascular events, and effectively protects the functions of targeted organs such as heart, brain, kidney and the like. Aiming at the blood pressure rhythm change of the human body, proper medicines and reasonable administration time are selected, so that the medicine action is consistent with the rhythm of the hypertension, and the purposes of achieving the optimal treatment effect and reducing the adverse drug reactions become the key point of attention in the development of the hypertension medicine.
At present, lisinopril preparations in the market are common tablets and capsules, which can not ensure the blood concentration of patients to be stable within 24 hours after the lisinopril preparations are taken, and can not achieve ideal blood pressure reducing effect. The Chinese invention patent CN103006612 provides a lisinopril delayed-release tablet and a preparation method thereof, which discloses a lisinopril sustained-release preparation, wherein the preparation is prepared by punching holes on a film coating outside a medicament to prepare the tablet, and the main component of the tablet is released through the pore diameter of the coating. The patent can achieve the effect of stably reducing the pressure within 24 hours, but the process is complex, the related technical parameters of the process are not easy to control, the reproducibility is poor, and the release speed is unstable. Meanwhile, the medicine taking compliance of the medicine is poor for patients, and the medicine is still required to be taken for many times every week.
Disclosure of Invention
Aiming at the defects in the prior art, the invention aims to provide a lisinopril-containing sustained-release transdermal patch which can maintain stable blood concentration for a long time, has good reproducibility and stable release speed.
In order to achieve the above purposes, the technical scheme adopted by the invention is as follows:
a sustained and controlled release transdermal patch containing lisinopril comprises a drug storage layer, a back lining layer and a protective layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a penetration enhancer, and the content of each component in the drug storage layer is as follows according to mass percentage:
2.5 to 25 percent of lisinopril
70 to 97 percent of storage matrix
0.5 to 5 percent of penetration enhancer.
On the basis of the technical scheme, the storage matrix is at least one of silicone pressure-sensitive adhesive, polyisobutylene pressure-sensitive adhesive, acrylate pressure-sensitive adhesive, carbomer, triethanolamine, povidone, methyl cellulose, ethyl cellulose or sodium carboxymethyl cellulose.
On the basis of the technical scheme, the penetration enhancer is a compound of lecithin and azone, and the weight percentage of the lecithin and the azone in the penetration enhancer is 1: 2/3-3/2.
On the basis of the technical scheme, the protective layer material is selected from polyethylene, polystyrene, poly tetrachloroethylene or release paper which is coated with wax/organic silicon for isolation treatment.
On the basis of the technical scheme, the backing layer is made of a flexible material which is impermeable to the medicine, and is selected from non-woven fabrics, polyvinyl chloride, polyethylene, polystyrene, polyester or a composite thin layer consisting of the substances.
On the basis of the technical scheme, the lisinopril-containing sustained-release transdermal patch further comprises an adhesive layer, wherein the adhesive layer is a blank pressure-sensitive adhesive layer.
On the basis of the technical scheme, the sticking layer comprises one or more of silicone pressure-sensitive adhesive, acrylate pressure-sensitive adhesive, natural rubber and carbomer.
On the basis of the technical scheme, a drug storage layer of each sustained-release transdermal patch contains 10 mg-80 mg of lisinopril with effective dose, and the content of a storage matrix in the storage layer is 50-150mg/cm 2.
On the basis of the technical scheme, the drug release rate of the lisinopril-containing sustained-release transdermal patch is 95-98%.
On the basis of the technical scheme, the ratio of lisinopril to the penetration enhancer in the drug storage layer is 4:0.5-1.5 in percentage by mass.
Compared with the prior art, the invention has the advantages that:
(1) compared with the lisinopril ordinary tablets, capsules or oral sustained-release preparations on the market at present, the lisinopril-containing sustained-release transdermal patch has the advantages of more uniform drug release, good reproducibility, definite curative effect and stable quality.
(2) The sustained-release transdermal patch containing lisinopril has the advantages that the main component can be continuously and stably released for a long time by adding the compound penetration enhancer of lecithin and azone, the first pass effect of liver and gastrointestinal irritation reaction during oral administration are avoided, the sustained-release transdermal patch can provide a longer blood concentration stationary phase compared with the existing common tablet, capsule or oral sustained-release preparation of lisinopril, only once administration is needed every 1-8 days, and the administration compliance is better.
(3) The lisinopril-containing sustained-release transdermal patch is convenient to use, the protective layer is torn off and is pasted on the skin, the drug administration can be stopped when the protective layer is torn off and is continuously pasted when needed if side effects of the drug occur in the drug administration process, and the drug administration safety of patients is improved.
Detailed Description
The present invention will be described in further detail with reference to examples.
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer and a protective layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a penetration enhancer, and the content of each component in the drug storage layer is as follows by mass percent:
2.5 to 25 percent of lisinopril
70 to 97 percent of storage matrix
0.5 to 5 percent of penetration enhancer.
Wherein the reservoir matrix can be one or more of silicone pressure sensitive adhesive, polyisobutylene pressure sensitive adhesive, acrylate pressure sensitive adhesive, carbomer, triethanolamine, polyvidone, methylcellulose, ethylcellulose and sodium carboxymethylcellulose. The penetration enhancer can be a compound of lecithin and azone; the protective layer can be made of polyethylene, polystyrene, polytetrafluoroethylene or release paper which is coated with wax or subjected to organic silicon isolation treatment; the backing layer may be made of a flexible material impermeable to the drug, such as a nonwoven fabric, polyvinyl chloride, polyethylene, polystyrene, polyester, or a composite laminate of the foregoing.
The sustained and controlled release transdermal patch containing lisinopril in the embodiment of the invention also can comprise an adhesive layer, and the adhesive layer can be a blank pressure-sensitive adhesive layer. The material of the adhesive layer can be selected according to the actual pharmaceutical requirements, such as one or more of silicone pressure sensitive adhesive, acrylate pressure sensitive adhesive, natural rubber and carbomer.
The lisinopril is uniformly released mainly through the interaction of the lisinopril and the penetration enhancer, so that the effect of maintaining the blood concentration stably for a long time is achieved. Generally, the sustained-release transdermal patch containing lisinopril in the embodiment of the invention has the release time of 1 to 8 days and the release amount of 10 mg/day. The mass percentage of the lisinopril and the penetration enhancer in the drug storage layer obtained by tests is 4:0.5-1.5, the preferable proportion range can be 4:0.95-1.05, and tests prove that the drug transdermal rate of the sustained-release transdermal patch containing the lisinopril is increased by about 5% compared with that of a common proportioning product, and the cumulative drug permeation amount is increased by 1-2%.
The release area of each patch of the sustained and controlled release transdermal patch containing lisinopril is 1cm2～4cm2The transdermal speed is 0.05mg/h cm2～0.15mg/h·cm2And continuously releasing the medicine for 1-8 days. The amount of the reservoir matrix in the reservoir layer can be determined to be 50-150mg/cm2Preferably 80 to 120mg/cm2. The sustained-release transdermal patch containing lisinopril is applied to the skin when in administration, the daily dosage is 10mg, and patches with different dosages are selected according to the time length. The administration mode can meet the effective dosage of lisinopril in the general treatment process and meet the treatment requirement; and as shown in the test data, the blood drug peak time and the half-life period of the blood drug concentration of the patient are obviously improved on the premise of not being adjusted so as to achieve the effect of long-term stable drug administration.
The invention is further illustrated below by means of 6 examples.
Example 1
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer and a protective layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a penetration enhancer, each patch of the lisinopril-containing sustained-release transdermal patch contains 80mg of lisinopril with an effective dose, the drug storage layer contains 16% of lisinopril, 80% of the storage matrix and 4% of the penetration enhancer in percentage by mass, and the content of the storage matrix in the drug storage layer is 100mg/cm2。
The transdermal patch of this example contained within the drug reservoir layer per 1000 patches: 80g of lisinopril, 400g of polyisobutylene pressure-sensitive adhesive, 10g of lecithin and 10g of azone. The back lining layer is polyvinyl chloride and the protective layer is polyethylene.
Example 2
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer, a protective layer and an adhesive layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a permeation enhancer, each patch of the lisinopril-containing sustained-release transdermal patch contains 40mg of lisinopril with an effective dose, the drug storage layer contains 10% of lisinopril, 87.75% of the storage matrix and 2.25% of the permeation enhancer in percentage by mass, and the content of the storage matrix in the drug storage layer is 87.75mg/cm2。
The transdermal patch of this example contained within the drug reservoir layer per 1000 patches: the formula comprises 40g of lisinopril, 320g of silicone pressure-sensitive adhesive, 15g of carbomer, 16g of triethanolamine, 4.5g of lecithin and 4.5g of azone. The back lining layer is non-woven fabric, the protecting layer is anti-sticking paper which is coated with wax or is isolated by organic silicon, and the sticking layer is silicone pressure-sensitive adhesive.
Example 3
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer and a protective layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a penetration enhancer, each patch of the lisinopril-containing sustained-release transdermal patch contains 80mg of lisinopril with effective dose, and the drug storage layer contains lisinopril in percentage by mass25 percent of the total weight of the drug, 70 percent of the reservoir matrix and 5 percent of the penetration enhancer, wherein the content of the reservoir matrix in the drug reservoir layer is 50mg/cm2。
The transdermal patch of this example contained within the drug reservoir layer per 1000 patches: 80g of lisinopril, 287g of silicone pressure-sensitive adhesive, 5g of povidone, 8g of methyl cellulose, 12g of lecithin and 8g of azone. The back lining layer is polyester film and the protecting layer is polytetrafluoroethylene film.
Example 4
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer, a protective layer and an adhesive layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a permeation enhancer, each patch of the lisinopril-containing sustained-release transdermal patch contains 80mg of lisinopril with effective dose, the drug storage layer contains 25% of lisinopril, 70% of the storage matrix and 5% of the permeation enhancer in percentage by mass, and the content of the storage matrix in the drug storage layer is 50mg/cm2。
The transdermal patch of this example contained within the drug reservoir layer per 1000 patches: 80g of lisinopril, 380g of silicone pressure-sensitive adhesive, 12g of povidone, 8g of sodium carboxymethyl cellulose, 11g of lecithin and 9g of azone. The back lining layer is a composite thin layer composed of polyvinyl chloride, polyethylene and polystyrene film, the protective layer is polystyrene film, and the adhesive layer is silicone pressure-sensitive adhesive.
Example 5
The embodiment of the invention provides a lisinopril-containing sustained-release transdermal patch, which comprises a drug storage layer, a back lining layer, a protective layer and an adhesive layer, wherein the drug storage layer consists of lisinopril, a storage matrix and a permeation enhancer, each patch of the lisinopril-containing sustained-release transdermal patch contains 10mg of lisinopril with an effective dose, the drug storage layer contains 2.5% of lisinopril, 97% of the storage matrix and 0.5% of the permeation enhancer in percentage by mass, and the content of the storage matrix in the drug storage layer is 150mg/cm2。
The transdermal patch of this example contained within the drug reservoir layer per 1000 patches: 10g of lisinopril, 880g of acrylate pressure-sensitive adhesive, 105g of ethyl cellulose, 3g of lecithin and 2g of azone. The back lining layer is a composite thin layer composed of polyvinyl chloride, polyethylene and polystyrene film, the protective layer is a polyethylene film, and the adhesive layer is a mixture of acrylate pressure-sensitive adhesive and carbomer.
Example 6
The embodiment of the present invention is different from embodiment 4 in that: in this example, no permeation enhancer was added, and the adhesive layer was replaced with natural rubber.
The preparation method of the pressure-sensitive adhesive in each example of the present invention is a conventional method in the art, and the preparation method of the transdermal patch in each example is as follows:
s1, mixing the storage matrix with lecithin and azone, heating to 70 ℃ for softening, and uniformly stirring;
s2, dissolving lisinopril in a proper amount of water, adding the mixture into the mixture obtained in the step S1, stirring and uniformly mixing;
s3, coating the mixture obtained in the step S2 on a protective layer, controlling the thickness, drying at 50 ℃, covering a back lining layer, and cutting into pieces of 4cm2And (5) obtaining the product.
To examine the skin permeation effect of the lisinopril-containing sustained-release transdermal patch in each example of the present invention, the following skin absorption transmittance test was performed:
the samples of examples 1-6 were tested for transmittance by the following method:
6 mice were harvested, dehaired, and the mice were skinned and the lipid layer removed. Placing the treated mouse skin in a laminated glass bottle containing phosphate buffer solution with volume of 100ml and pH value of 6.8, stirring with a magnetic stirrer at interlayer heating temperature of 32 deg.C, and collecting 4cm2The sample is pasted on the mouse skin, the samples are respectively taken for 2h, 4h, 8h, 24h, 48h, 72h, 96h, 120h, 144h, 168h and 196h, and then the sampling amount is complemented. The amount of the drug penetrating the skin was measured by sampling for 96 hours in example 2 and 24 hours in example 5.
The method for detecting lisinopril permeation amount comprises the following steps:
chromatographic conditions and system applicability tests are adopted, and octadecylsilane chemically bonded silica is used as a filling agent; acetonitrile-phosphate buffer solution (0.02mol/L sodium dihydrogen phosphate solution, sodium hydroxide test solution to adjust pH value to 5.0) (8:92) is used as mobile phase; the detection wavelength is 215 nm; the column temperature was 50 ℃. The separation degree of lisinopril should be more than 5.0, and the number of theoretical plates is not less than 700 calculated according to the lisinopril peak.
During measurement, taking lisinopril reference substances, precisely weighing, dissolving with water, quantitatively diluting to prepare a solution containing about 0.2mg in each 1ml, precisely measuring 20 mu l, injecting into a liquid chromatograph, and recording a chromatogram; and taking another sample, filtering, taking 20 mu l of subsequent filtrate, injecting into a liquid chromatograph, and recording the chromatogram. And calculating by peak area according to an external standard method to obtain the detection result of lisinopril permeation.
The results of transmittance measurements are shown in the following table:
TABLE 1 lisinopril permeation in examples 1-6
From the experimental data, it can be seen that the lisinopril-containing sustained-release transdermal patch of each example of the present invention has a good linear relationship between the lisinopril permeation amount and the cumulative release time when applied. After the permeation enhancer consisting of the compound of lecithin and azone is added, the permeation amount of lisinopril in unit time is increased by about 20 percent compared with the control group (example 6); meanwhile, the permeation amount-time curve shows that after the permeation enhancer is added, the permeation amount of lisinopril and the accumulated release time are in a linear relationship, and the drug release is more stable.
In order to examine the blood content control effect of the lisinopril-containing sustained-release transdermal patch in each example of the invention, the following tests were performed:
taking the samples of the examples 1-3, applying the sustained-release transdermal patch sample containing lisinopril to the skin of the patients in the test group, and continuously administering for 6 days according to the effective dose and frequency of lisinopril in each group of samples and the calculation of the daily dosage of 10 mg; the control group used commercially available lisinopril oral tablets (trade name: lisinopril tablets (trade name: sinceri), company: AstraZeneca UK Limited, registration number: H20091050, 2009-12-02, pharmaceutical properties: chemicals, 10mg) and was orally administered in a manner of taking tablets with an effective dose of 10mg of lisinopril every day, 5mg every 12 hours for 6 consecutive days, and respectively measuring the blood concentration 2h, 4h, 8h, 12h, 16h, 24h, 36h, 48h, 60h, 72h, 84h, 96h, 108h, 120h, 132h, 144h, 156h, 168h, 180h and 192h after the first administration/administration by adopting HPLC-MS/MS, recording the blood content of a user, and performing pharmacokinetic model fitting and parameter calculation on the blood concentration-time data by using DAS software.
The results of the blood drug content test of each group are shown in the following table:
TABLE 2 blood levels of patients in examples 1-3 and control groups
According to the test data, the change of the blood concentration of the patch and the conventional oral tablet shows periodic fluctuation when the patch and the conventional oral tablet are continuously taken, and the change trend of the blood concentration after the last administration is basically similar to that of the patch after the single administration: after the patch is administrated, the blood concentration slowly rises and slowly falls after reaching the peak; the blood concentration of the conventional oral tablet rapidly rises and rapidly falls after reaching the peak. The blood concentrations of the drug and the drug at corresponding time points within 3-24 h after administration are obviously different, the concentration of the drug in 12h after the drug is stopped of the patch is nearly 2 times of the concentration of the drug in 12h after the drug is stopped of the conventional oral tablet, the concentration of the drug in 24h after the drug is stopped of the patch is nearly 4 times of the concentration of the drug in 12h after the drug is stopped of the conventional oral tablet, and the obvious difference indicates the slow release effect of the patch. Comparing the blood concentration value and the blood concentration value in a steady state in the embodiment of the invention and the control group, the preparation process of the patch of the invention does not influence the absorption of the medicine, but only plays a role in regulating and controlling the absorption rate of the medicine, and achieves the purposes of controlling the dosage and delaying the attenuation of the blood concentration.
The present invention is not limited to the above-described embodiments, and it will be apparent to those skilled in the art that various modifications and improvements can be made without departing from the principle of the present invention, and such modifications and improvements are also considered to be within the scope of the present invention. Those not described in detail in this specification are within the skill of the art.
Claims (8)
1. A sustained and controlled release transdermal patch containing lisinopril comprises a drug storage layer, a back lining layer and a protective layer, and is characterized in that:
the drug storage layer is composed of lisinopril, a storage matrix and a penetration enhancer, and the content of each component in the drug storage layer is as follows by mass percent:
2.5 to 25 percent of lisinopril
70 to 97 percent of storage matrix
0.5 to 5 percent of penetration enhancer;
wherein the penetration enhancer is a compound of lecithin and azone;
the penetration enhancer comprises lecithin and azone in a mass percentage ratio of 1: 1-3/2;
the mass percentage ratio of lisinopril to the penetration enhancer in the drug storage layer is 4: 0.95-1.05.
2. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the storage matrix is at least one of silicone pressure-sensitive adhesive, polyisobutylene pressure-sensitive adhesive, acrylate pressure-sensitive adhesive, carbomer, triethanolamine, povidone, methyl cellulose, ethyl cellulose or sodium carboxymethyl cellulose.
3. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the protective layer material is selected from polyethylene, polystyrene, poly tetrachloroethylene or release paper which is coated with wax/organic silicon for isolation treatment.
4. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the back lining layer is made of a flexible material which is impermeable to the medicine, and is selected from non-woven fabrics, polyvinyl chloride, polyethylene, polystyrene, polyester or a composite thin layer composed of the substances.
5. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the sustained and controlled release transdermal patch containing lisinopril also comprises an adhesive layer, wherein the adhesive layer is a blank pressure-sensitive adhesive layer.
6. The lisinopril-containing sustained or controlled release transdermal patch according to claim 5, wherein: the adhesive layer comprises one or more of silicone pressure-sensitive adhesive, acrylate pressure-sensitive adhesive, natural rubber and carbomer.
7. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the drug storage layer of each sustained-release transdermal patch contains 10 mg-80 mg of lisinopril with effective dose, and the content of the storage matrix in the storage layer is 50-150mg/cm2。
8. The lisinopril-containing sustained or controlled release transdermal patch according to claim 1, wherein: the drug release rate of the sustained and controlled release transdermal patch containing lisinopril is 95-98%.
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| CN100353934C (en) * | 2004-11-04 | 2007-12-12 | 王睿 | Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method |
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