CN107929265A - A kind of preparation method of medicinal transdermal material - Google Patents
A kind of preparation method of medicinal transdermal material Download PDFInfo
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- CN107929265A CN107929265A CN201711090610.5A CN201711090610A CN107929265A CN 107929265 A CN107929265 A CN 107929265A CN 201711090610 A CN201711090610 A CN 201711090610A CN 107929265 A CN107929265 A CN 107929265A
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- transdermal
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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
- 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
- A61K47/02—Inorganic compounds
-
- 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
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
Abstract
The present invention relates to a kind of preparation method of medicinal transdermal material, belong to medical material tech field.The present invention is aided with myrrh again using Asian puccoon, the reinforcings such as peppermint promote Transdermal absorption, the transdermal Chinese medicine preparation for increasing space between cells is made in the mineral matter strong with osmosis again, and cubic liquid crystal is prepared by injection method, there is the closure lipid bilayer structure in co-continuous pool and lipid area using cubic liquid crystal, there is huge film surface product, the carrier that the medicine of opposed polarity can be wrapped up the characteristics of can simultaneously improving the stability of medicine as medicine, higher biology in situ adhesion properties are made, medicinal transdermal material with good Transdermal absorption performance, lipid arrangement between Chinese angelica volatile oil disorder corneocyte is cooperateed with by glyceryl monooleate, influence skin complete structure and further promote percutaneous drug absorption, deformation infiltrates into deep skin, it is effectively increased the transdermal amount of medicine, improve drug absorption rate, and improve therapeutic effect.
Description
Technical field
The present invention relates to a kind of preparation method of medicinal transdermal material, belong to medical material tech field.
Background technology
Transdermal drug delivery system is administered through skin plaster mode, makes medicine with certain speed by skin layers, by hair
Thin blood vessel is absorbed into body circulation and produces whole body or the preparation of local therapeutic effects.Transdermal drug delivery system goes out from the 1980s
After now, the research hotspot of medical personal in recent years is rapidly become with its unique advantage.
Cutaneous penetration technology, has gradually attracted numerous medical personals' note that and progressively becoming doctor
The research hotspot in medicine field.It is that medicine medication is made that great tribute as being administered orally with the alternative of drug administration by injection
Offer, cause the great interest of medical market.Preparation capable of permeating skin can weaken to gastrointestinal administration compared with other traditional pharmaceutical dosage forms
Side effect, extend medicine effective action time, less times for spraying and can according to administration area adjust dosage.
At present, as long as preparation capable of permeating skin is divided into Chinese medicine preparation capable of permeating skin and Western medicine preparation capable of permeating skin.There are many percutaneous dosing medicines in Chinese medicine preparation
Formulation, such as paste, cataplasm, creme etc..But Chinese medicine complicated component in itself, the drug absorption of Chinese medicine preparation capable of permeating skin are poor
The defects of limit the development of Chinese medicine transdermal patch always.Pharmaceutic adjuvant develops rapidly, new material, and new technology constantly goes out
It is existing, drive clinic and basic research that the Transdermal absorption of Chinese Traditional Medicine is administered.But also have with modern transdermal drug delivery system
A certain distance.Listed or come into the percutaneous administration patch of clinical research at present, mainly angiocardiopathy medicine,
Medicine for central nervous system, hormone medicine and Fei Liu body analgesic-antipyretic.
Therefore strengthen the correlative study of Chinese medicine transdermal patch and skin-tolerant, understand Chinese medicine transdermal patch and cause skin to pierce
Swash morbidity matrix and the prophylactic treatment measure of reaction, to reduce dermoreaction, the advantage for giving full play to Chinese medicine transdermal patch seems
It is particularly important that.
The content of the invention
The technical problems to be solved by the invention:It is low for the transdermal amount for the transdermal material medicine of Chinese medicine developed at present,
A kind of the problem of drug absorption rate is low, there is provided preparation method of medicinal transdermal material.
In order to solve the above technical problems, the technical solution adopted by the present invention is:
A kind of preparation method of medicinal transdermal material, specific preparation process are:
(1)Sodium chloride, sodium sulphate, magnesium sulfate, calcium sulfate, Asian puccoon, myrrh, peppermint, borneol, camphor are added in deionized water and protected
Temperature 1 ~ 2h of extraction, repeats merging filtrate after extracting 1 ~ 3 time and is concentrated by evaporation to stoste volume 20 ~ 30%, obtain transdermal Chinese medicine preparation;
(2)Glyceryl monooleate, Chinese angelica volatile oil, absolute ethyl alcohol are fitted into beaker, melt 20 ~ 30min simultaneously at 60 ~ 70 DEG C
20 ~ 30min of ultrasonic disperse, obtains organic phase;
(3)Transdermal Chinese medicine preparation is added in deionized water, 20 ~ 30min is stirred at 60 ~ 70 DEG C, obtains water phase;
(4)Water is mutually added dropwise in organic phase under vorticity, rear self-emulsifying is added dropwise 7 ~ 10 days, discharging is placed on brown
Bottle sealing, preserves at 0 ~ 4 DEG C, obtains medicinal transdermal material.
Step(1)The parts by weight of each raw material are 10 ~ 15 parts of sodium chloride in the transdermal Chinese medicine preparation, 10 ~ 15 parts of sodium sulphate,
5 ~ 10 parts of magnesium sulfate, 5 ~ 10 parts of calcium sulfate, 30 ~ 50 portions of Asian puccoons, 15 ~ 20 parts of myrrhs, 15 ~ 20 portions of peppermints, 5 ~ 10 parts of borneols, 5 ~ 10
Part camphor.
Step(1)The extraction process filters to get filtrate and filter residue, will filter to be heated to 95 ~ 100 DEG C of insulation 1 ~ 2h of boiling
Slag filters merging filtrate after repeating boiling 1 ~ 3 time.
Step(2)The glyceryl monooleate, Chinese angelica volatile oil, the parts by weight of absolute ethyl alcohol are sweet for 60 ~ 75 parts of single oleic acid
Grease, 20 ~ 25 parts of Chinese angelica volatile oils, 5 ~ 6 parts of absolute ethyl alcohols.
Step(3)The transdermal Chinese medicine preparation dosage is the 1 ~ 5% of glyceryl monooleate quality, the deionized water dosage
For the 1/3 of glyceryl monooleate quality.
Step(4)The drop rate is 1 ~ 2mL/min.
Compared with other methods, advantageous effects are the present invention:
The present invention utilizes the effect of the promotion Transdermal absorption of Asian puccoon, then is aided with myrrh, peppermint, borneol, camphor, and it is transdermal to strengthen promotion
Absorb, then the mineral matter strong with osmosis mixes, and is constructed to be improved cytoactive, increases the mobility of horn cell
By force, change the transdermal Chinese medicine preparation that skin epidermis structure increases space between cells, and cubic liquid crystal is prepared by injection method, utilize
Cubic liquid crystal has the closure lipid bilayer structure in co-continuous pool and lipid area, has huge film surface product, can wrap up difference
The medicine of polarity can simultaneously improve carrier of the characteristics of stability of medicine as medicine, and higher biology in situ is made and sticks spy
Property, there is the medicinal transdermal material of good Transdermal absorption performance, Chinese angelica volatile oil disorder angle is cooperateed with by glyceryl monooleate
Lipid arrangement between matter confluent monolayer cells, influences skin complete structure and further promotes percutaneous drug absorption, and deformation infiltrates into skin
Deep layer, is effectively increased the transdermal amount of medicine, improves drug absorption rate, and improve therapeutic effect.
Embodiment
Take 10 ~ 15g sodium chloride, 10 ~ 15g sodium sulphate, 5 ~ 10g magnesium sulfate, 5 ~ 10g calcium sulfate, 30 ~ 50g Asian puccoons, 15 ~ 20g
Myrrh, 15 ~ 20g peppermints, 5 ~ 10g borneols, 5 ~ 10g camphors, add in 1 ~ 2L deionized waters, are heated to 95 ~ 100 DEG C of insulation boilings
1 ~ 2h, filters to get filtrate and filter residue, is filtered after filter residue is repeated boiling 1 ~ 3 time, merging filtrate is simultaneously concentrated by evaporation to stoste volume
20 ~ 30%, transdermal Chinese medicine preparation is obtained, takes 60 ~ 75g glyceryl monooleates, 20 ~ 25g Chinese angelica volatile oils, 5 ~ 6g absolute ethyl alcohols load
In beaker, melt 20 ~ 30min under 60 ~ 70 DEG C of waters bath with thermostatic control, and 20 ~ 30min, whirlpool are disperseed with 100 ~ 300W ultrasonic echographies
5 ~ 8min is revolved, obtains organic phase, takes the transdermal Chinese medicine preparations of 1 ~ 3g, is added in 20 ~ 25g deionized waters, under 60 ~ 70 DEG C of waters bath with thermostatic control
20 ~ 30min is stirred with 300 ~ 400r/min, obtains water phase, water is mutually added dropwise to organic phase with 1 ~ 2mL/min under vorticity
In, rear self-emulsifying is added dropwise 7 ~ 10 days, discharging is placed on brown bottle sealing, is preserved at 0 ~ 4 DEG C, obtains medicinal transdermal material.
Example 1
Take 10g sodium chloride, 10g sodium sulphate, 5g magnesium sulfate, 5g calcium sulfate, 30g Asian puccoons, 15g myrrhs, 15g peppermints, 5g borneols, 5g
Camphor, adds in 1L deionized waters, is heated to 95 DEG C of insulation boiling 1h, filters to get filtrate and filter residue, filter residue is repeated boiling 1 time
After filter, merging filtrate is simultaneously concentrated by evaporation to stoste volume 20%, obtains transdermal Chinese medicine preparation, takes 60g glyceryl monooleates, and 20g works as
Return volatile oil, 5g absolute ethyl alcohols are fitted into beaker, melt 20min under 60 DEG C of waters bath with thermostatic control, and with 100W ultrasonic echographies point
20min is dissipated, vortex 5min, obtains organic phase, takes the transdermal Chinese medicine preparations of 1g, adds in 20g deionized waters, under 60 DEG C of waters bath with thermostatic control
20min is stirred with 300r/min, obtains water phase, water is mutually added dropwise in organic phase with 1mL/min under vorticity, is added dropwise
Self-emulsifying 7 days afterwards, discharging are placed on brown bottle sealing, are preserved at 0 DEG C, obtain medicinal transdermal material.
Example 2
Take 12g sodium chloride, 12g sodium sulphate, 7g magnesium sulfate, 7g calcium sulfate, 40g Asian puccoons, 17g myrrhs, 17g peppermints, 7g borneols, 7g
Camphor, adds in 1L deionized waters, is heated to 97 DEG C of insulation boiling 1h, filters to get filtrate and filter residue, filter residue is repeated boiling 2 times
After filter, merging filtrate is simultaneously concentrated by evaporation to stoste volume 25%, obtains transdermal Chinese medicine preparation, takes 70g glyceryl monooleates, and 22g works as
Return volatile oil, 5g absolute ethyl alcohols are fitted into beaker, melt 25min under 65 DEG C of waters bath with thermostatic control, and with 200W ultrasonic echographies point
25min is dissipated, vortex 6min, obtains organic phase, takes the transdermal Chinese medicine preparations of 2g, adds in 22g deionized waters, under 65 DEG C of waters bath with thermostatic control
25min is stirred with 350r/min, obtains water phase, water is mutually added dropwise in organic phase with 1mL/min under vorticity, is added dropwise
Self-emulsifying 8 days afterwards, discharging are placed on brown bottle sealing, are preserved at 2 DEG C, obtain medicinal transdermal material.
Example 3
Take 15g sodium chloride, 15g sodium sulphate, 10g magnesium sulfate, 10g calcium sulfate, 50g Asian puccoons, 20g myrrhs, 20g peppermints, 10g ice
Piece, 10g camphors, add in 2L deionized waters, are heated to 100 DEG C of insulation boiling 2h, filter to get filtrate and filter residue, filter residue is repeated
Filtered after boiling 3 times, merging filtrate is simultaneously concentrated by evaporation to stoste volume 30%, is obtained transdermal Chinese medicine preparation, is taken the mono- oleics of 75g
Ester, 25g Chinese angelica volatile oils, 6g absolute ethyl alcohols are fitted into beaker, melt 30min under 70 DEG C of waters bath with thermostatic control, and with 300W ultrasounds
Ripple ultrasonic disperse 30min, vortex 8min, obtains organic phase, takes the transdermal Chinese medicine preparations of 3g, adds in 25g deionized waters, in 70 DEG C of perseverances
30min is stirred with 400r/min under tepidarium, obtains water phase, is mutually added dropwise to water in organic phase with 2mL/min under vorticity,
Rear self-emulsifying is added dropwise 10 days, discharging is placed on brown bottle sealing, is preserved at 4 DEG C, obtains medicinal transdermal material.
Medicinal transdermal material prepared by the present invention and the medicinal transdermal material of Hebei company production are detected, specific inspection
Survey result such as following table table 1:
The medicinal transdermal material property characterization of table 1
The medicinal transdermal material that as shown in Table 1 prepared by the present invention, sustained release performance is good, and skin permeation rate improves, and drug absorption rate is good.
Claims (6)
1. a kind of preparation method of medicinal transdermal material, it is characterised in that specifically preparation process is:
(1)Sodium chloride, sodium sulphate, magnesium sulfate, calcium sulfate, Asian puccoon, myrrh, peppermint, borneol, camphor are added in deionized water and protected
Temperature 1 ~ 2h of extraction, repeats merging filtrate after extracting 1 ~ 3 time and is concentrated by evaporation to stoste volume 20 ~ 30%, obtain transdermal Chinese medicine preparation;
(2)Glyceryl monooleate, Chinese angelica volatile oil, absolute ethyl alcohol are fitted into beaker, melt 20 ~ 30min simultaneously at 60 ~ 70 DEG C
20 ~ 30min of ultrasonic disperse, obtains organic phase;
(3)Transdermal Chinese medicine preparation is added in deionized water, 20 ~ 30min is stirred at 60 ~ 70 DEG C, obtains water phase;
(4)Water is mutually added dropwise in organic phase under vorticity, rear self-emulsifying is added dropwise 7 ~ 10 days, discharging is placed on brown
Bottle sealing, preserves at 0 ~ 4 DEG C, obtains medicinal transdermal material.
A kind of 2. preparation method of medicinal transdermal material as claimed in claim 1, it is characterised in that step(1)It is described transdermal
The parts by weight of each raw material are 10 ~ 15 parts of sodium chloride in Chinese medicine preparation, 10 ~ 15 parts of sodium sulphate, 5 ~ 10 parts of magnesium sulfate, 5 ~ 10 parts of sulfuric acid
Calcium, 30 ~ 50 portions of Asian puccoons, 15 ~ 20 parts of myrrhs, 15 ~ 20 portions of peppermints, 5 ~ 10 parts of borneols, 5 ~ 10 parts of camphors.
A kind of 3. preparation method of medicinal transdermal material as claimed in claim 1, it is characterised in that step(1)The extraction
Process filters to get filtrate and filter residue to be heated to 95 ~ 100 DEG C of insulation 1 ~ 2h of boiling, and filter residue is repeated to filter after boiling 1 ~ 3 time to close
And filtrate.
A kind of 4. preparation method of medicinal transdermal material as claimed in claim 1, it is characterised in that step(2)Single oil
Acid glyceride, Chinese angelica volatile oil, the parts by weight of absolute ethyl alcohol are 60 ~ 75 parts of glyceryl monooleates, 20 ~ 25 parts of Chinese angelica volatile oils, 5
~ 6 parts of absolute ethyl alcohols.
A kind of 5. preparation method of medicinal transdermal material as claimed in claim 1, it is characterised in that step(3)It is described transdermal
Chinese medicine preparation dosage is the 1 ~ 5% of glyceryl monooleate quality, and the deionized water dosage is the 1/3 of glyceryl monooleate quality.
A kind of 6. preparation method of medicinal transdermal material as claimed in claim 1, it is characterised in that step(4)The dropwise addition
Speed is 1 ~ 2mL/min.
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109077958A (en) * | 2018-08-31 | 2018-12-25 | 蒋春霞 | A kind of antiperspirant composition and preparation method thereof |
Citations (1)
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US20070104783A1 (en) * | 2001-02-28 | 2007-05-10 | Axiomedic Ltd. | Double-Layered Absorbable Solid Compositions for the Topical Treatment of Oral Mucosal Disorders |
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2017
- 2017-11-08 CN CN201711090610.5A patent/CN107929265A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20070104783A1 (en) * | 2001-02-28 | 2007-05-10 | Axiomedic Ltd. | Double-Layered Absorbable Solid Compositions for the Topical Treatment of Oral Mucosal Disorders |
Non-Patent Citations (3)
Title |
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乔元等: ""当归挥发油的透皮特性及其作用机制研究"", 《中国药师》 * |
宋乃秋: "《中华民间百草良方》", 31 March 2008, 内蒙古人民出版社 * |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN109077958A (en) * | 2018-08-31 | 2018-12-25 | 蒋春霞 | A kind of antiperspirant composition and preparation method thereof |
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