CN107951868A - A kind of muskone patch and its preparation method and application - Google Patents
A kind of muskone patch and its preparation method and application Download PDFInfo
- Publication number
- CN107951868A CN107951868A CN201711450247.3A CN201711450247A CN107951868A CN 107951868 A CN107951868 A CN 107951868A CN 201711450247 A CN201711450247 A CN 201711450247A CN 107951868 A CN107951868 A CN 107951868A
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- muskone
- patch
- back sheet
- group
- adherent layer
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- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- 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
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of muskone patch and its preparation method and application.Including back sheet and adherent layer, include muskone and framework material between back sheet and adherent layer for the adhesion layer of drug containing, the adhesion layer of drug containing.Wherein framework material is silicone type pressure sensitive glue, and back sheet is polyethylene terephthalate, and adherent layer is the smooth ground paper crossed with Treating Cuttings with Paraffin Wax.Patch is made in muskone by the present invention, the defects of overcoming for oral administration and ejection preparation, and liver first-pass effect and stomach can be avoided to inactivate, and maintains constant blood concentration to strengthen therapeutic effect, reduces toxic side effect.The use of patch, can also reduce times for spraying, be suitable for the treatment of cerebral infarction especially recovery period of stroke.
Description
Technical field
The present invention relates to muskone medicine and applied technical field, more particularly to a kind of muskone patch and its preparation side
Method and application.
Background technology
Apoplexy is always to threaten a big serious disease of human health, and wherein ishemic stroke is the main Types of apoplexy.
Ishemic stroke is also known as ischemic cerebrovascular disease, and it is encephaledema, improvement brain blood circulation and brain protection that it, which treats key, so that extensive
The blood supply of multiple ischemic region, saves dying neuron.Its treatment means mainly has and reduces intracranial pressure, regulation and control blood pressure, anti-freezing, molten
Bolt, protection microcirculation and brain protection etc..
The conventional dosage forms for treating ishemic stroke are mainly decoction, capsule, oral liquid, tablet, injection.But these agent
All different degrees of, the time length big there are usage amount of type, clinical the shortcomings of being difficult to mate to all the time, and meeting during some patient's apoplexy
There is lockjaw symptom, therefore, in treatment need effective and safe pharmaceutical dosage form to improve method of administration.
Muskone (3- methylcyclopentadecanones) is the main active ingredient in natural musk and muscone, has fragrance
The effect having one's ideas straightened out.Muskone molecular weight is small, fusing point is low, easily enters central nervous system by skin and permeable blood-brain barrier.
The problem of lacking suitable formulations treatment for current ishemic stroke, the present invention needs to research and develop a kind of novel form, gram
The defects of taking for oral administration and ejection preparation, avoids liver first-pass effect and stomach from inactivating, and maintains constant blood concentration to strengthen
Therapeutic effect, reduces toxic side effect.
The content of the invention
The present invention provides a kind of muskone patch and its preparation method and application aiming at above-mentioned defect.This
Patch is made in muskone by invention, the defects of overcoming for oral administration and ejection preparation, and liver first-pass effect and stomach can be avoided to inactivate,
And maintain constant blood concentration to strengthen therapeutic effect, reduce toxic side effect.The use of patch, can also reduce times for spraying,
It is suitable for the treatment of cerebral infarction especially recovery period of stroke.
A kind of muskone patch and its preparation method and application technical solution of the present invention is：A kind of muskone patch, bag
Include back sheet and adherent layer, be the adhesion layer of drug containing between back sheet and adherent layer, the adhesion layer of drug containing include muskone and
Framework material (drug-reservoir material).
Wherein framework material is silicone type pressure sensitive glue (Bio PSA Low Tack Q7-2920), and back sheet is to be poly- to benzene two
Formic acid diethylester (PET FR530), adherent layer are the smooth ground paper crossed with Treating Cuttings with Paraffin Wax.
Muskone dosage 10.0-250.0mg, silicone type pressure sensitive glue dosage 15-40g, polyethylene terephthalate's dosage
150-400cm2, smooth ground paper 150-400cm that Treating Cuttings with Paraffin Wax is crossed2。
A kind of preparation method of muskone patch, comprises the following steps：
Mixed after 10.0-250.0mg muskones, 15-40g silicone type pressure sensitives glue are added the dissolving of 1-9mL ethyl acetate
Even, closed stirring 15min-1h, decompression degassing, is coated on 150-400cm2On polyethylene terephthalate's back sheet, formed
The adhesion layer of drug containing, adherent layer (150-400cm is covered after dry2), punching press cutting, obtains the muskone patch.
Application of the muskone patch in ishemic stroke is treated.
Beneficial effects of the present invention are：
(1) muskone patch of the invention can improve MCAO rat nerve functions, and it is in dosage correlation to improve degree；Musk deer
Ketone musk patch is obviously reduced MCAO rat cerebral infarction volumes, and muskone patch delivery group rat cerebral infarction index compares model group
Significantly reduce；SOD vigor is remarkably improved, reduces MDA contents in brain tissue.The present invention and traditional treatment medicine and traditional treatment
Formulation is compared, and is had identical even preferably drug action, can be substituted conventional medicament and conventional dosage forms completely, while it turn avoid
The peak valley phenomenon of blood concentration caused by oral, drug administration by injection, reduces toxicity during peak valley, secondly because patch
Active ingredient is absorbed through skin is directly entered " first pass effect " and gastrointestinal reaction that in vivo, can avoid medicine, and easy to use.
(2) medicine stability of the present invention is good, and preparation process is simple, expensive instrument and equipment is not required, and is adapted to industrialization big
Production.
Brief description of the drawings：
Fig. 1 show influence of the muskone patch to AICI rat model brain capillary permeabilities, wherein, with sham-operation
Group compares,#P<0.05,##P<0.01,###P<0.001；Compared with model group,*P<0.05,**P<0.01,***P<0.001；
Fig. 2 show influence of the muskone patch to MCAO rat model brain infarction areas；Wherein：1. sham-operation group
2.MCAO model group 3.MLD group 4.MMD group 5.MHD group 6.ND group 7.YKL groups, shadow region are normal blood supply area, white area
For infarcted region；
Fig. 3 show influence of the muskone patch to MCAO rat model cerebral infarction index of mortality.Wherein：With sham-operation group ratio
Compared with,#P<0.05,##P<0.01,###P<0.001；Compared with model group,*P<0.05,**P<0.01,***P<0.001。
Embodiment：
For a better understanding of the present invention, below with instantiation come the technical solution that the present invention will be described in detail, but this
Invention is not limited thereto.
Embodiment 1
52.5mg muskones, 25.0g silicone type pressure sensitives glue are added into 3mL ethyl acetate dissolving and mixings, it is closed to stir
Mix 0.5h, to suitable denseness after depressurize degassing, be coated on 200cm2On polyethylene terephthalate's back sheet, drug containing is formed
Adhesion layer, adherent layer (200cm is covered after dry2), punching press cutting, obtains load drug paste agent 200 and pastes.
Embodiment 2
105.0mg muskones, 25.0g silicone type pressure sensitives glue are added into 3mL ethyl acetate dissolving and mixings, it is closed to stir
1h is mixed, decompression degassing, is coated on 200cm2On polyethylene terephthalate's back sheet, the adhesion layer of drug containing is formed, after dry
Cover adherent layer (200cm2), punching press cutting, obtains load drug paste agent 200 and pastes.
Embodiment 3
The drug effect results of animal of muskone patch prepared by the present invention is as follows：
Dosage regimen：
Wistar rats 70 are taken, are randomly divided into sham-operation group, model group, muskone patch high dose group (MHD)
(4.20mg/kg), muskone patch middle dose group (MMD) (2.10mg/kg), muskone patch low dose group (MLD)
(1.05mg/kg), Nimodipine group (ND) (4mg/kg) and Gin Kgo Plus group (YKL) (40mg/kg), every group of 10 animals.Do evil through another person
On front side of the rat neck of art group and model group using physiological saline gavage and after being attached to unhairing with blank patch (at arteria carotis communis)；
Each dosage group of muskone patch using physiological saline gavage and the rat neck after being attached to unhairing with corresponding dosage patch at；Buddhist nun is not
The Nimodipine and Gin Kgo Plus of Horizon group and Gin Kgo Plus group difference gavage corresponding dosage, and it is big after being attached to unhairing with blank patch
At mouse neck, 1 time a day, continuous 7d.
Experiment one：Protective effect of the muskone patch to rat acute Incomplete cerebral ischemia (AICI) model
After successive administration 7 days, Banded Rats bilateral common carotid arteries establish rat acute Incomplete cerebral ischemia (AICI) mould
Type, after modeling 3h, broken end takes brain, measures cerebral index and brain water content.Measurement result is shown in Table 1, compared with sham-operation group,
AICI model groups cerebral index and the equal conspicuousness rise of brain water content；Compared with AICI model groups, high, medium and low dose of muskone patch
Amount group cerebral index and brain water content significantly reduce, and high, middle dosage action effect is better than Nimodipine and Gin Kgo Plus.Observe musk deer
Influence of the ketone musk patch to AICI group rat brain capillary permeabilities, the results show that compared with sham-operation group, AICI model groups
The brain capillary permeability of rat dramatically increases；Compared with AICI model groups, muskone patch can obviously reduce AICI models
Rat brain capillary permeability, and it is high, middle dosage effect is suitable with Nimodipine and Gin Kgo Plus, effect of high dosage effect compared with
It is good.The result is shown in influence of Figure of description Fig. 1 muskones to AICI rat model brain capillary permeabilities.
Influence (n=10) of the 1 muskone patch of table to AICI rat models cerebral index and water content
Note：Compared with sham-operation group,#P<0.05,##P<0.01,###P<0.001；Compared with MCAO model groups,*P<
0.05,**P<0.01。
Experiment two：Protective effect of the muskone patch to intraluminal middle cerebral artery occlusion in rats obstruction (MCAO) model
Successive administration 7d, after the last administration 1h, chloraldurate (300mg/kg) anesthetized rat, using internal carotid line brush
Slightly improvement prepares rat middle cerebral artery occlusion (MCAO) model.4h, 8h, 24h respectively carry out each group rat after modeling
The influence of neurobehavioral index is evaluated, and after modeling 24h, inferior caval vein takes blood, is measured for Biochemical Indices In Serum；Break immediately afterwards
Head takes brain, cuts off occipital bone inner wall, opens skull, takes out brain tissue, freezing microtome section, TTC dyeing, measures rat cerebral infarction area.
4h, 8h, 24h respectively carry out each group rat the influence evaluation of neurobehavioral index after modeling, the results are shown in Table 2, musk deer
4h can significantly improve MCAO rat nerve functions after ketone musk patch middle dosage, high dose modeling；Nimodipine, Gin Kgo Plus and musk deer
Nervous function scoring significantly reduces ketone musk patch low dosage compared with model group during 8h after modeling.The result shows that muskone can be shown
Writing improves MCAO rat nerve functions, and middle and high dosage is superior to Nimodipine and Yin Ke on responding time and improvement
The positive group of network two.
Observe influence of the muskone patch to MCAO rat cerebral infarction areas.The result is shown in Fig. 2, Fig. 3, cerebral infarction index results
Show, each administration group can reduce MCAO rat cerebral infarction indexes, and muskone patch effect is in dose dependent, high dose musk deer
Ketone musk patch is better than Nimodipine and Gin Kgo Plus.
Influence of the muskone patch to rat biochemical indicator is observed, the results are shown in Table 3, compared with MCAO model groups, muskone
3 dosage groups of patch and Nimodipine group, Gin Kgo Plus group are remarkably improved SOD vigor, reduce MDA in brain tissue, as a result table
Bright muskone patch has the function that to strengthen rat cerebral tissue's anti-oxidative damage.
Influence (n=10) of the 2 muskone patch of table to rat nerve behavioral indicator
Note：Compared with sham-operation group,#P<0.05,##P<0.01,###P<0.001；Compared with MCAO model groups,*P<
0.05,**P<0.01。
Influence (n=10) of the 3 muskone patch of table to MCAO rat model Biochemical Indices In Serums
Note：Compared with sham-operation group,#P<0.05,##P<0.01,###P<0.001；Compared with model group,*P<0.05,**P<
0.01,***P<0.001。
Experiment three：Protective effect of the muskone patch to Transient Forebrain Ischemia (GI) model
Successive administration 7d, after the last administration 1h, etherization, only separated after sham-operation group anesthesia right carotid without
Ligation；Remaining each group rat ligatures side arteria carotis communis, after 24h, rat is placed on 45min in low-oxygen box, causes rats
Global cerebral ischemia (GI) model.Influence of the muskone patch to GI hemorheology of rat indexs is observed, 4 are the results are shown in Table, with doing evil through another person
Art group is compared, and GI model group whole blood viscosity substantially increases, and blood is viscous, and red cell deformability reduces, high, middle dosage muskone
Patch group is compared with GI model groups, and whole blood viscosity, plasma viscosity substantially reduce, and red cell deformability is remarkably reinforced, and high agent
It is suitable with Nimodipine group and Gin Kgo Plus group to measure muskone patch therapeutic effect.
Influence (n=10) of the 4 muskone patch of table to GI rat model serum Hemorheological Indexes
Note：Compared with sham-operation group,#P<0.05,##P<0.01,###P<0.001；Compared with model group,*P<0.05,**P<
0.01,***P<0.001。
Claims (5)
1. a kind of muskone patch, it is characterised in that be drug containing between back sheet and adherent layer including back sheet and adherent layer
Adhesion layer, the adhesion layer of drug containing include muskone and framework material.
2. a kind of muskone patch according to claim 1, it is characterised in that framework material is silicone type pressure sensitive glue, the back of the body
Lining is polyethylene terephthalate, and adherent layer is the smooth ground paper crossed with Treating Cuttings with Paraffin Wax.
3. a kind of muskone patch according to claim 1, it is characterised in that muskone dosage 10.0-250.0mg, silicon
Ketone type pressure sensitive adhesive dosage 15-40g, polyethylene terephthalate's dosage 150-400cm2, smooth ground paper that Treating Cuttings with Paraffin Wax is crossed
150-400cm2。
4. a kind of preparation method of muskone patch as claimed in claim 1, it is characterised in that comprise the following steps：
10.0-250.0mg muskones, 15-40g silicone type pressure sensitives glue are added into 1-9mL ethyl acetate dissolving and mixings, it is close
Stirring 15min-1h is closed, decompression degassing, is coated on 150-400cm2On polyethylene terephthalate's back sheet, drug containing is formed
Adhesion layer, covers adherent layer, punching press cutting, obtains muskone patch after dry.
5. application of the muskone patch as claimed in claim 1 in ishemic stroke is treated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711450247.3A CN107951868B (en) | 2017-12-27 | 2017-12-27 | Muscone patch and preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711450247.3A CN107951868B (en) | 2017-12-27 | 2017-12-27 | Muscone patch and preparation method and application thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107951868A true CN107951868A (en) | 2018-04-24 |
| CN107951868B CN107951868B (en) | 2021-02-02 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711450247.3A Active CN107951868B (en) | 2017-12-27 | 2017-12-27 | Muscone patch and preparation method and application thereof |
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| Country | Link |
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| CN (1) | CN107951868B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110314224A (en) * | 2019-07-19 | 2019-10-11 | 西北大学 | A kind of pad pasting and its preparation method and application promoting skin injury healing |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102920766A (en) * | 2012-11-09 | 2013-02-13 | 杨军峰 | Drug composite for treating Chinese-medicine arthralgia syndromes and preparation of patch of drug composite |
| CN105056154A (en) * | 2015-09-17 | 2015-11-18 | 吉林大学 | Traditional Chinese medicine compound gel dispersible patch for curing rheumatic arthralgia |
-
2017
- 2017-12-27 CN CN201711450247.3A patent/CN107951868B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102920766A (en) * | 2012-11-09 | 2013-02-13 | 杨军峰 | Drug composite for treating Chinese-medicine arthralgia syndromes and preparation of patch of drug composite |
| CN105056154A (en) * | 2015-09-17 | 2015-11-18 | 吉林大学 | Traditional Chinese medicine compound gel dispersible patch for curing rheumatic arthralgia |
Non-Patent Citations (4)
| Title |
|---|
| 刘继勇: "痹痛宁透皮贴剂的研制", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑》 * |
| 潘卫三: "《药剂学》", 31 July 2017, 北京：化学工业出版社 * |
| 程怡，等: "麝香酮透皮吸收增强作用的体系研究", 《中药材》 * |
| 陈长勋: "《中药药理学 第2版》", 31 January 2015, 上海：上海科学技术出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110314224A (en) * | 2019-07-19 | 2019-10-11 | 西北大学 | A kind of pad pasting and its preparation method and application promoting skin injury healing |
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| CN107951868B (en) | 2021-02-02 |
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