CN108210462A - The preparation method of a kind of gram of vertical boron sieve local sustained release liposome and application - Google Patents
The preparation method of a kind of gram of vertical boron sieve local sustained release liposome and application Download PDFInfo
- Publication number
- CN108210462A CN108210462A CN201810269222.1A CN201810269222A CN108210462A CN 108210462 A CN108210462 A CN 108210462A CN 201810269222 A CN201810269222 A CN 201810269222A CN 108210462 A CN108210462 A CN 108210462A
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- CN
- China
- Prior art keywords
- gram
- liposome
- boron sieve
- vertical boron
- sustained release
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
-
- 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
- A61K31/69—Boron 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
Abstract
Application the invention discloses the preparation method of a kind of gram of vertical boron sieve local sustained release liposome and through from spray pattern to dermal topical application, it is liposome raw material that the Liposomal formulation, which selects phosphatide, cholesterol, select the stabilizer and film forming agent of polyethylene glycol and polyvinyl alcohol as corresponding liposome, the liposome that particle size dispersion is uniform and release profiles are stably and controllable can be obtained through high-pressure homogeneous, there is good transdermal enhancing effect to the drug of topical application, and the amount for entering blood is few, opposite targeting is shown to skin histology, so as to improve hold-up of the drug in skin histology.At the same time drug depot can be formed in epidermis and corium using liposome as the pharmaceutical carrier through dermal topical application, slow releasing pharmaceutical enduringly works to diseased region, especially suitable for certain skin diseases that are chronic, easily recurring.
Description
Technical field
The present invention relates to a kind of newtype drug sustained release usage more particularly to it is a kind of for skin disease, ox-hide moss be object
Medicament slow release method and its application.
Background technology
In numerous diseases, the disease such as small symptom such as ox-hide moss, topical ulcers in terms of skin is often not likely to draw
The extensive attention of people is played, therefore can in most cases be developed as one pleases until being difficult to the stage tidied up.To find out its cause,
Illness initial stage is not easy to find, and the processing means being lack of pertinence.Patient often has the trouble for fearing the process of seeking medical advice.
Under normal conditions, for sprain, collide with may be used erasing or spray Yunnan Baiyao mode emergency processing, for
The mode that attaching adhesive bandage may be used in small notch carries out emergency processing.Thus for above-mentioned dept. of dermatology's unmentionable disease, seek one
The rapidly processing mode of kind simply, with strong points is particularly important.
In recent years, a kind of entitled gram of vertical boron sieve（English is entitled：Crisaborole）New drug, on December 14th, 2016 obtain
U.S. FDA approval listing, by Anacor pharmaceutical developments and is responsible in U.S.'s list marketing, trade name Eucrisa；
Crisaborole is a kind of phosphodiesterase-4（PDE-4）Inhibitor, this inhibition lead to intracellular loops adenosine phosphate（cAMP）
Level increases；Eucrisa is a kind of office for 2 years old and the slight local treatment to moderate allergic dermatitis of above patient
Portion's externally-applied ointment.But traditional ointment contains big vaseline, has strong greasy feeling during use, easily makes clothing dirty, and damage
Significant component of active ingredient is lost, drug transdermal amount is not high, and smearing dosage and actual efficacy can not make the best of both worlds.
Invention content
Deficiency in view of the aforementioned technical background, the purpose of the present invention are directed to a kind of gram vertical boron sieve local sustained release liposome
Preparation method and application, solve the impression that uses of drug and higher skin hold-up be provided and reduces administration number of times.
The present invention realizes that the technical solution of said one purpose is the system of a kind of gram of vertical boron sieve local sustained release liposome
Method, it is characterised in that：
S1, phosphatide, cholesterol are selected as liposome raw material, alcohols material as stabilizer raw material, high molecular material be used as into
The ratio of film raw material, wherein phosphatide and cholesterol is 3:1-6:1, the ratio of phosphatide and gram vertical boron sieve is 10:1-20:1；
S2, phosphatide, cholesterol and vertical boron sieve of bulk pharmaceutical chemicals gram are dissolved in ethyl alcohol and form organic phase, stabilizer is added to the water,
It dissolves and adds in film forming solvent swell overnight as water phase, the ratio of water phase and organic phase is 2：1-4：1；
S3, organic phase is injected into water phase, it is 3-5 times high-pressure homogeneous, it obtains gram vertical boron sieve liposome, adds in filling after antioxidant
In spray special-purpose bottle.
Further, the phosphatide is at least egg yolk lecithin.
Further, the stabilizer is at least one or more combinations in PEG300, PEG400, glycerine, propylene glycol.
Further, the film forming agent is at least one in polyvinyl alcohol, povidone, copolyvidone, hydroxypropyl methylcellulose
Kind or multiple combinations.
Further, the antioxidant is one or both of vitamin E or butylated hydroxytoluene mixture.
Further, pressure is 400Mpa-800Mpa used by high pressure homogenization described in step S3.
The present invention realizes that the technical solution of another above-mentioned purpose is：A kind of gram of vertical boron sieve local sustained release liposome
Using, it is characterised in that：Utilize the spray special-purpose bottle for containing gram vertical boron sieve made from step S3, direct spraying film forming application.
Using the Liposomal formulation of the present invention, have prominent substantive distinguishing features and significant progress：By selecting to close
624D fits liposome formula and control high pressure homogenization parameter, can obtain the finished product that particle size dispersion is uniform and release profiles are stably and controllable
Drug has more good transdermal enhancing effect, opposite targeting is shown to skin histology, so as to improve drug in skin histology
Hold-up, reduce drug and enter blood generating unnecessary side effect, at the same time given using liposome as through local skin
The pharmaceutical carrier of medicine can form drug depot in epidermis and corium, and slow releasing pharmaceutical enduringly works to diseased region, for
Certain chronic, skin diseases for easily recurring improve the stability of pharmacological property release and the practicability of finished medicines.
Description of the drawings
Fig. 1 is gram vertical boron sieve liposome In-vitro release curves of the invention.
Specific embodiment
Just attached drawing in conjunction with the embodiments below, the embodiment of the present invention is described in further detail, so that of the invention
Technical solution is more readily understood, grasps, so as to make relatively sharp define to protection scope of the present invention.
Present invention innovation proposes preparation method and the application of a kind of gram of vertical boron sieve local sustained release liposome, the property summarized preparation method packet
Include following steps：S1, selecting phosphatide, cholesterol, alcohols material is as stabilizer raw material, high molecular material as liposome raw material
As film former base, the wherein ratio of phosphatide and cholesterol is 3:1-6:1, the ratio of phosphatide and gram vertical boron sieve is 10:1-20:
1；S2, phosphatide, cholesterol and vertical boron sieve of bulk pharmaceutical chemicals gram are dissolved in ethyl alcohol and form organic phase, stabilizer is added to the water, it is molten
It solves and adds in film forming solvent swell overnight as water phase, the ratio of water phase and organic phase is 2：1-4：1；S3, organic phase is injected into
It is 3-5 times high-pressure homogeneous in water phase, it obtains gram vertical boron sieve liposome, adds in filling in spray special-purpose bottle after antioxidant.
From the point of view of the selection of more specific raw material, which is at least egg yolk lecithin；Stabilizer be at least PEG300,
One or more combinations in PEG400, glycerine, propylene glycol；Film forming agent is at least polyvinyl alcohol, povidone, copolyvidone, hydroxyl
One or more combinations in third methylcellulose；Antioxidant is vitamin E or butylated hydroxytoluene（Hereinafter referred to as BHT）In
One or two kinds of mixtures.In addition, it is above-mentioned further, described in step S3 used by high pressure homogenization pressure be 400Mpa-
800Mpa。
Embodiment 1
150mg egg yolk lecithins and 50 cholesterol and 20mg grams of vertical boron sieve are dissolved in 4ml ethyl alcohol, form organic phase.It will
70mg polyvinyl alcohol addition 10ml is water-swellable overnight, as water phase.Organic phase is injected into water phase, the high-pressure homogeneous 3- of 800Mpa
5 times to get to gram vertical boron sieve liposome, adding in 0.1% antioxidant BHT, it is filling in spray special-purpose bottle to obtain the final product.
Embodiment 2
250mg egg yolk lecithins and 50 cholesterol and 20mg grams of vertical boron sieve are dissolved in 4ml ethyl alcohol, form organic phase.It will
200mg PEG300, which are added in 10ml water, to be dissolved, and adds in the swelling of 100mg copolyvidones overnight, as water phase.Organic phase is noted
Enter into water phase, high-pressure homogeneous 3-5 times of 800Mpa to get to gram vertical boron sieve liposome, adding in 0.1% antioxidant BHT, it is filling in
In spray special-purpose bottle to obtain the final product.
Embodiment 3
200mg egg yolk lecithins and 50 cholesterol and 20mg grams of vertical boron sieve are dissolved in 4ml ethyl alcohol, form organic phase.It will
200mg propylene glycol, which is added in 10ml water, to be dissolved, and adds in the swelling of 100mg copolyvidones overnight, as water phase.Organic phase is injected
Into water phase, high-pressure homogeneous 3-5 times of 400Mpa adds in 0.1% vitamin E to get to gram vertical boron sieve liposome, filling in spraying
In agent special-purpose bottle to obtain the final product.
As shown in Figure 1, be pH7.4PBS, 500ml by local sustained release liposome produced by the present invention in bag filter, 37
DEG C, the In-vitro release curves under the conditions of 100rpm/min.
Processing method and polynary application mode using the present invention, have prominent substantive distinguishing features and significant progress
Property：By select appropriate length ionic activating agent and control ultrasound intensity, can obtain particle size dispersion uniformly and release profiles
Stably and controllable final drug improves the stability of pharmacological property release and the practicability of finished medicines.
Claims (7)
1. the preparation method of a kind of gram of vertical boron sieve local sustained release liposome, it is characterised in that：
S1, phosphatide, cholesterol are selected as liposome raw material, alcohols material as stabilizer raw material, high molecular material be used as into
The ratio of film raw material, wherein phosphatide and cholesterol is 3:1-6:1, the ratio of phosphatide and gram vertical boron sieve is 10:1-20:1；
S2, phosphatide, cholesterol and vertical boron sieve of bulk pharmaceutical chemicals gram are dissolved in ethyl alcohol and form organic phase, stabilizer is added to the water,
It dissolves and adds in film forming solvent swell overnight as water phase, the ratio of water phase and organic phase is 2：1-4：1；
S3, organic phase is injected into water phase, it is 3-5 times high-pressure homogeneous, it obtains gram vertical boron sieve liposome, adds in filling after antioxidant
In spray special-purpose bottle.
2. the preparation method of gram vertical boron sieve local sustained release liposome according to claim 1, it is characterised in that：The phosphatide is at least
Egg yolk lecithin.
3. the preparation method of gram vertical boron sieve local sustained release liposome according to claim 1, it is characterised in that：The stabilizer is at least
For one or more combinations in PEG300, PEG400, glycerine, propylene glycol.
4. the preparation method of gram vertical boron sieve local sustained release liposome according to claim 1, it is characterised in that：The film forming agent is at least
For one or more combinations in polyvinyl alcohol, povidone, copolyvidone, hydroxypropyl methylcellulose.
5. the preparation method of gram vertical boron sieve local sustained release liposome according to claim 1, it is characterised in that：The antioxidant is dimension
Raw element one or both of E or butylated hydroxytoluene mixture.
6. the preparation method of gram vertical boron sieve local sustained release liposome according to claim 1, it is characterised in that：It is high described in step S3
It is 400Mpa-800Mpa to press homogeneous used pressure.
7. the application of a kind of gram of vertical boron sieve local sustained release liposome, it is characterised in that：Using made from step S3 contain gram vertical boron sieve
Spray special-purpose bottle, direct spraying film forming application.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810269222.1A CN108210462A (en) | 2018-03-29 | 2018-03-29 | The preparation method of a kind of gram of vertical boron sieve local sustained release liposome and application |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810269222.1A CN108210462A (en) | 2018-03-29 | 2018-03-29 | The preparation method of a kind of gram of vertical boron sieve local sustained release liposome and application |
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| Publication Number | Publication Date |
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| CN108210462A true CN108210462A (en) | 2018-06-29 |
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| CN201810269222.1A Withdrawn CN108210462A (en) | 2018-03-29 | 2018-03-29 | The preparation method of a kind of gram of vertical boron sieve local sustained release liposome and application |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113712977A (en) * | 2020-05-25 | 2021-11-30 | 南京帝昌医药科技有限公司 | Cliboroluo external preparation and preparation method and application thereof |
| CN116139085A (en) * | 2023-03-01 | 2023-05-23 | 深圳市贝美药业有限公司 | External aerosol and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1895225A (en) * | 2006-06-26 | 2007-01-17 | 裴泽军 | Brilliant mycomycin elaioplast preparation and its making method |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
-
2018
- 2018-03-29 CN CN201810269222.1A patent/CN108210462A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1895225A (en) * | 2006-06-26 | 2007-01-17 | 裴泽军 | Brilliant mycomycin elaioplast preparation and its making method |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
Non-Patent Citations (1)
| Title |
|---|
| 闫丽霞: "《药物制剂技术》", 31 August 2012, 华中科技大学出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113712977A (en) * | 2020-05-25 | 2021-11-30 | 南京帝昌医药科技有限公司 | Cliboroluo external preparation and preparation method and application thereof |
| CN116139085A (en) * | 2023-03-01 | 2023-05-23 | 深圳市贝美药业有限公司 | External aerosol and preparation method thereof |
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| PB01 | Publication | ||
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| WW01 | Invention patent application withdrawn after publication | ||
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Application publication date: 20180629 |