CN105997957A - Fucoxanthine hydrogel patch for preventing and treating obesity - Google Patents
Fucoxanthine hydrogel patch for preventing and treating obesity Download PDFInfo
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- CN105997957A CN105997957A CN201610534796.8A CN201610534796A CN105997957A CN 105997957 A CN105997957 A CN 105997957A CN 201610534796 A CN201610534796 A CN 201610534796A CN 105997957 A CN105997957 A CN 105997957A
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- fucoxanthine
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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
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
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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
- A61K47/30—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
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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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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Abstract
The invention discloses a fucoxanthine hydrogel patch for preventing and treating obesity. Fucoxanthine is used as a model drug, a hydrophilic high molecular material is used as a framework material, and the fucoxanthine hydrogel patch further contains a crosslinking agent, a crosslinking regulator, a thickener, a moisturizing agent, an antioxidant and a penetration enhancer. The prepared fucoxanthine hydrogel patch having excellent mechanical properties can maintain steady blood-drug concentration within a certain time range, avoids the shortcoming of a short half-life period after difficultly soluble fucoxanthine is taken orally, has small side effects and can prevent and treat the obesity.
Description
Technical field
The invention belongs to the technical field of natural product application, be specifically related to a kind of fucoxanthine hydrogel patch fat for prevention and treatment.
Background technology
Along with development and the raising of people's quality of life of China's economic level, the obesity that the diet structure of high lipid and the life style not got enough athletic exercise cause becomes global Dystrophy.And most method of weight-reducing all exists side effect such as affecting immunity of organisms, easily bounce-back, poor effect, from natural product, therefore seek safely and effectively anti-obesity activity material cause the concern of more and more scholar.
Fucoxanthine (fucoxanthin) is also known as pheophytin, and molecular formula is C42H58O6 ,It is a kind of rare oxygen-containing carotenoid being present in Phaeophyta biology.It is reported that title fucoxanthine has the strongest antioxidation and anticancer property, more particularly, its fat reducing effect is obvious, the desirable feedstock of preparation tool fat reducing functional health care food can be become, but being seldom related to patent report in this respect at present, have is also that fucoxanthine is made oral formulations, but it has the following disadvantages: through liver first-pass effect after fucoxanthine oral administration, half-life is short, and medicining times is many.
Summary of the invention
It is an object of the invention to for the deficiencies in the prior art, the cross-linking type fucoxanthine hydrogel patch that preparation mechanical property is more excellent, the blood drug level of stable state can be maintained in the range of certain time, the shortcoming that after avoiding slightly solubility fucoxanthine oral, the half-life is short, it is provided that a kind of side effect is little, can prevent and treat the fucoxanthine hydrogel patch of obesity.
In order to realize the purpose of the present invention, by the following technical solutions:
A kind of fucoxanthine hydrogel patch fat for prevention and treatment, it is characterized in that: with fucoxanthine as model drug, with hydrophilic high molecular material as framework material, also include cross-linking agent, cross-linking regulator, thickening agent, wetting agent, antioxidant and penetrating agent;
Wherein, one or more in dihydroxyaluminum aminoacetate, aluminium hydroxide or aluminium oxide of described cross-linking agent;
One or more in tartaric acid, citric acid, lactic acid, oleic acid or ethylenediaminetetraacetic acid of described cross-linking regulator;
One or more in polyvinyl alcohol, sodium alginate, hypromellose, sodium carboxymethyl cellulose, carbomer or gelatin of described thickening agent;
One or more in glycerol, Polyethylene Glycol, propylene glycol or sorbitol of described wetting agent;
One or more in azone, Oleum menthae, oleic acid or propylene glycol of described penetrating agent.
As preferably, described framework material selects hydrophilic high molecular material sodium polyacrylate.
As preferably, described antioxidant uses vitamin E.
Present invention also offers a kind of preferred implementation, a kind of fucoxanthine hydrogel patch fat for prevention and treatment, it is characterized in that: selection sodium polyacrylate is framework material, dihydroxyaluminum aminoacetate is cross-linking agent, tartaric acid be cross-linking regulator, polyvinyl alcohol and sodium carboxymethyl cellulose be thickening agent, glycerol is wetting agent, vitamin E is antioxidant, and azone is penetrating agent.
It is highly preferred that the content of each component of the described fucoxanthine hydrogel patch fat for prevention and treatment is: sodium polyacrylate 3g, dihydroxyaluminum aminoacetate 0.2g, 1.0% aqueous tartaric acid solution 25mL, polyvinyl alcohol 3g, sodium carboxymethyl cellulose 3g, glycerol 25g, the vitamin E solution that concentration is 10% of 1%, 2% azone.
The present invention also provides for the preparation method of a kind of described fucoxanthine hydrogel patch fat for prevention and treatment, it is characterised in that employing following steps:
A, the polyvinyl alcohol weighing recipe quantity add distilled water immersion overnight so that it is the most swelling, and heating in water bath to 90 DEG C makes it all be dissolved into glue, prepares A phase;
B, weigh the sodium carboxymethyl cellulose of recipe quantity, sodium polyacrylate adds in glycerol, after fully grinding well, add the tartaric acid after the dissolving of recipe quantity and dihydroxyaluminum aminoacetate, stir, prepare B phase;
B slowly is added in A phase stir by c, under agitation gradation, i.e. obtains patch bare substrate;
D, when temperature is down to 50 DEG C, the mixed liquor of the fucoxanthine of recipe quantity, antioxidant and penetrating agent and qs glycerin are ground well after, join in bare substrate, stir;
E, by obtained mixture through heating in water bath deaerate after, coat on the non-woven fabrics of certain area, solidify in vacuum drying oven, obtain fucoxanthine hydrogel patch.
Further, the solidification temperature of described fucoxanthine hydrogel patch is 50 DEG C.
Further, the hardening time of described fucoxanthine hydrogel patch is 12h.
The invention have the benefit that compared with prior art, fucoxanthine is made prevention or the cross-linking type hydrogel patch for the treatment of obesity by the present invention first, it has sustained releasing character, the blood drug level of stable state is maintained in the range of certain time, blood concentration fluctuation is little, reduce patient medication frequency, improve patient's compliance;Side effect is little, can effectively prevent and treat obesity.
Detailed description of the invention
Below by embodiment, the present invention is further elaborated:
The present invention is with fucoxanthine as model drug, by consulting literatures and preliminary experiment, optimization polypropylene acid sodium (NP-700) be framework material, dihydroxyaluminum aminoacetate be cross-linking agent, tartaric acid be cross-linking regulator, polyvinyl alcohol and sodium carboxymethyl cellulose be thickening agent, glycerol be wetting agent, vitamin E be antioxidant, azone is penetrating agent.
The present invention, using skin tracing ability, stretchability, mastic uniformity, plastic property etc. as evaluation index, uses L18(3)7The consumption of each adjuvant of optimization of orthogonal test, filters out optimum prescription: sodium polyacrylate (NP-700) 3g, dihydroxyaluminum aminoacetate 0.2g, 1.0% aqueous tartaric acid solution 25mL, polyvinyl alcohol 3g, sodium carboxymethyl cellulose 3g, glycerol 25g, the vitamin E solution that concentration is 10% of 1%.In fucoxanthine solution, add vitamin E, fucoxanthine stability can be effectively increased, suppress its oxidized decomposition.It addition, the present invention oozes multiple (ER) and (T lag time with unit are accumulation infiltration capacity (Q), infiltration rate (J), rushlag) as evaluation index, use Franz diffusion cell, using 15% ethanol-normal saline as receiving liquid, investigate the different penetrating agent impact on fucoxanthine Ligustrazine hydrochloride, final choice 2% azone, as penetrating agent, adds in above optimum prescription.
The present invention is as follows for the preparation method of prevention and the fucoxanthine hydrogel patch for the treatment of obesity:
A, the polyvinyl alcohol weighing recipe quantity add distilled water immersion overnight so that it is the most swelling, and heating in water bath to 90 DEG C makes it all be dissolved into glue, prepares A phase;
B, weigh the sodium carboxymethyl cellulose of recipe quantity, sodium polyacrylate adds in glycerol, after fully grinding well, add the tartaric acid after the dissolving of recipe quantity and dihydroxyaluminum aminoacetate, stir, prepare B phase;
B slowly is added in A phase stir by c, under agitation gradation, i.e. obtains patch bare substrate;
D, when temperature is down to 50 DEG C, the mixed liquor of the fucoxanthine of recipe quantity, antioxidant and penetrating agent and qs glycerin are ground well after, join in bare substrate, stir;
E, by obtained mixture through heating in water bath deaerate after, coat on the non-woven fabrics of certain area, solidify in vacuum drying oven, obtain fucoxanthine hydrogel patch.
Owing to fucoxanthine is to thermally labile, this research, with patch mouldability and medicament contg as index, optimizes patch solidification temperature and time, condition of cure is set to 50 DEG C, 12h.
Claims (8)
1. for prevention and treat fat fucoxanthine hydrogel patch for one kind, it is characterized in that: with fucoxanthine as model drug, with hydrophilic high molecular material as framework material, also include cross-linking agent, cross-linking regulator, thickening agent, wetting agent, antioxidant and penetrating agent;
Wherein, one or more in dihydroxyaluminum aminoacetate, aluminium hydroxide or aluminium oxide of described cross-linking agent;
One or more in tartaric acid, citric acid, lactic acid, oleic acid or ethylenediaminetetraacetic acid of described cross-linking regulator;
One or more in polyvinyl alcohol, sodium alginate, hypromellose, sodium carboxymethyl cellulose, carbomer or gelatin of described thickening agent;
One or more in glycerol, Polyethylene Glycol, propylene glycol or sorbitol of described wetting agent;
One or more in azone, Oleum menthae, oleic acid or propylene glycol of described penetrating agent.
The fucoxanthine hydrogel patch fat for prevention and treatment the most according to claim 1, it is characterised in that: described framework material selects hydrophilic high molecular material sodium polyacrylate.
The fucoxanthine hydrogel patch fat for prevention and treatment the most according to claim 1, it is characterised in that: described antioxidant uses vitamin E.
The fucoxanthine hydrogel patch fat for prevention and treatment the most according to claim 1, it is characterized in that: selection sodium polyacrylate is framework material, dihydroxyaluminum aminoacetate is cross-linking agent, tartaric acid is cross-linking regulator, polyvinyl alcohol and sodium carboxymethyl cellulose are thickening agent, glycerol is wetting agent, and vitamin E is antioxidant, and azone is penetrating agent.
The fucoxanthine hydrogel patch fat for prevention and treatment the most according to claim 4, it is characterized in that, the content of each component is: sodium polyacrylate 3g, dihydroxyaluminum aminoacetate 0.2g, 1.0% aqueous tartaric acid solution 25mL, polyvinyl alcohol 3g, sodium carboxymethyl cellulose 3g, glycerol 25g, the vitamin E solution that concentration is 10% of 1%, 2% azone.
6. the preparation method of a fucoxanthine hydrogel patch fat for prevention and treatment as claimed in claim 4, it is characterised in that employing following steps:
A, the polyvinyl alcohol weighing recipe quantity add distilled water immersion overnight so that it is the most swelling, and heating in water bath to 90 DEG C makes it all be dissolved into glue, prepares A phase;
B, weigh the sodium carboxymethyl cellulose of recipe quantity, sodium polyacrylate adds in glycerol, after fully grinding well, add the tartaric acid after the dissolving of recipe quantity and dihydroxyaluminum aminoacetate, stir, prepare B phase;
B slowly is added in A phase stir by c, under agitation gradation, i.e. obtains patch bare substrate;
D, when temperature is down to 50 DEG C, the mixed liquor of the fucoxanthine of recipe quantity, antioxidant and penetrating agent and qs glycerin are ground well after, join in bare substrate, stir;
E, by obtained mixture through heating in water bath deaerate after, coat on the non-woven fabrics of certain area, solidify in vacuum drying oven, obtain fucoxanthine hydrogel patch.
Preparation method the most according to claim 6, it is characterised in that: the solidification temperature of described fucoxanthine hydrogel patch is 50 DEG C.
Preparation method the most according to claim 6, it is characterised in that: the hardening time of described fucoxanthine hydrogel patch is 12h.
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CN201610534796.8A CN105997957A (en) | 2016-07-08 | 2016-07-08 | Fucoxanthine hydrogel patch for preventing and treating obesity |
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CN201610534796.8A CN105997957A (en) | 2016-07-08 | 2016-07-08 | Fucoxanthine hydrogel patch for preventing and treating obesity |
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108236646A (en) * | 2018-02-06 | 2018-07-03 | 贺建华 | Weight-reducing hydrogel patch and preparation method thereof |
CN109999205A (en) * | 2019-02-28 | 2019-07-12 | 北京三立慧评化妆品科技有限公司 | Gel combination, patch and its application |
CN110859793A (en) * | 2019-12-24 | 2020-03-06 | 广州市和一医疗科技有限公司 | High-affinity gel mask and preparation method thereof |
CN112807484A (en) * | 2021-03-12 | 2021-05-18 | 上海创始医疗科技(集团)有限公司 | Polymer hydrogel with slow release function and preparation method thereof |
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CN101045041A (en) * | 2007-04-29 | 2007-10-03 | 武汉兵兵药业有限公司 | Cataplasma containing ibuprofen its preparing method and application |
CN101801332A (en) * | 2007-09-20 | 2010-08-11 | 富士胶片株式会社 | Adhesive gel sheet for living organisms and sheet form cosmetics comprising the same |
WO2011152689A2 (en) * | 2010-06-03 | 2011-12-08 | 주식회사 리스토어랩스 | Method for purifying fucoxanthin derived from seaweed |
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2016
- 2016-07-08 CN CN201610534796.8A patent/CN105997957A/en active Pending
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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CN101045041A (en) * | 2007-04-29 | 2007-10-03 | 武汉兵兵药业有限公司 | Cataplasma containing ibuprofen its preparing method and application |
CN101801332A (en) * | 2007-09-20 | 2010-08-11 | 富士胶片株式会社 | Adhesive gel sheet for living organisms and sheet form cosmetics comprising the same |
WO2011152689A2 (en) * | 2010-06-03 | 2011-12-08 | 주식회사 리스토어랩스 | Method for purifying fucoxanthin derived from seaweed |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108236646A (en) * | 2018-02-06 | 2018-07-03 | 贺建华 | Weight-reducing hydrogel patch and preparation method thereof |
CN109999205A (en) * | 2019-02-28 | 2019-07-12 | 北京三立慧评化妆品科技有限公司 | Gel combination, patch and its application |
CN109999205B (en) * | 2019-02-28 | 2022-02-11 | 三立慧评(北京)检测技术有限公司 | Gel composition, spot patch and application thereof |
CN110859793A (en) * | 2019-12-24 | 2020-03-06 | 广州市和一医疗科技有限公司 | High-affinity gel mask and preparation method thereof |
CN110859793B (en) * | 2019-12-24 | 2022-01-14 | 广州市和一医疗科技有限公司 | High-affinity gel mask and preparation method thereof |
CN112807484A (en) * | 2021-03-12 | 2021-05-18 | 上海创始医疗科技(集团)有限公司 | Polymer hydrogel with slow release function and preparation method thereof |
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