CN1927182A - Procyanidins nano milk-like liquid medicine and its preparation - Google Patents
Procyanidins nano milk-like liquid medicine and its preparation Download PDFInfo
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- CN1927182A CN1927182A CN 200610104619 CN200610104619A CN1927182A CN 1927182 A CN1927182 A CN 1927182A CN 200610104619 CN200610104619 CN 200610104619 CN 200610104619 A CN200610104619 A CN 200610104619A CN 1927182 A CN1927182 A CN 1927182A
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- procyanidins
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Abstract
The invention discloses a procyanidin nanoemulsion drugs the composition of which is procyanidin, non-ionic surfactant, oil, deionized water, its preparation method is surfactant is loaded and weighed according to the proportion formula, choosing oil phase, and make sure that the HLB for its emulsion is close to the HLB of surfactant, then well prepared surfactants and oil phase is mixed according to the original proportion formula, adding proportional anthocyanin, blending and stirring completely, slowly dropwising deionized water and stirring at room temperature until it has similar viscosity with water and become clear transparent solution which is procyanidin nanoemulsion drug. Nano-procyanidin significantly improves the solubility, dispersion of procyanidins in water and its bioavailability, improves the stability of procyanidins. The nano-emulsion can be widely used in cosmetics, pharmaceuticals, beverages, health care products, fodder and other fields.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of novel form of procyanidin medicine, particularly a kind of procyanidins nano milk-like liquid medicine and preparation method thereof.
Background technology
Procyanidin (proanthocyanidin, PC) be the general name of an extensive big class flavan-3-alcohol derivant that exists in the plant, be one of human up to now the most strong Natural antioxidant of finding from occurring in nature, have extremely strong antioxidation and remove free radical activity.Modern pharmacology studies show that procyanidin has cytoprotective, mutation, antiinflammatory, antiallergic, antiulcer, improves a series of good biopharmacology effects such as vision, microcirculation improvement, protection cardiovascular, defying age, antitumor.Procyanidin proves through extensively clinical, toxicology, pharmacokinetic study for many years, and it is nontoxic, non-carcinogenic, non-teratogenesis, and safety (oral acute toxicity LD
50>5000mg/kg.bw; Skin acute toxicity LD
50>2000mg/kg.bw).General Oligomeric Proanthocyanidins water soluble, but high poly-procyanidin generally is insoluble in water.The procyanidin product generally is the mixture of oligomeric and high poly-procyanidin, and its dissolubility in water is not very high.Grape pip procyanidin extract is easily degraded in human stomach, and grape pip procyanidin is deposited also unstable at normal temperatures, and activity easily reduces.
Summary of the invention
The present invention seeks to defective and deficiency at above-mentioned prior art, provide a kind of dissolubility good, stablize, viscosity is low, particle diameter Xiao Yi absorbs procyanidins nano milk-like liquid medicine.
The technical scheme that realizes the foregoing invention purpose is a kind of procyanidins nano milk-like liquid medicine, and it is made up of the following weight proportion raw material:
Surfactant 10%~40%
Oil 4%~20%
Water 40%~85%
Procyanidin 0.001%~3%
Total component of above-mentioned raw materials is 100%.
Described water is deionized water.
Rationale of the present invention: the preparation of O/W type nanometer emulsion needs the HLB value of surfactant between 8~18, and when the HLB value of the HLB value of the required surfactant of emulsifying oil phase and surfactant is close, easily form stabilized nano emulsion.The present invention selects the nonionic surfactant of HLB value between 9~15 of surfactant for use, and is perhaps composite with the non-ionic surface active agent of a kind of HLB<10.
The present invention selects green, hypotoxicity for use, haemolysis is less and the nonionic surfactant castor oil polyoxyethylene ether-40 of good biocompatibility (EL-40), castor oil polyoxyethylene ether-35 (EL-35).More than two kinds of surfactants can use separately, also can be respectively and the composite use of Arlacel-80 (Span-80).
The oil phase that the present invention selects for use: isopropyl myristate, isopropyl palmitate, Jojoba oil, liquid paraffin, one or more mixture of vitamin E wet goods.These oils and fatss are little to skin irritation, be in a liquid state, do not have bad abnormal smells from the patient under the room temperature, have good wetting property, and infiltration is made skin lubrication glossy by skin absorbs easily.
Another object of the present invention provides the method for preparing procyanidins nano milk-like liquid medicine, specifically comprises the following steps:
1) preparation of surfactant takes by weighing surfactant by formula proportion, use separately or with help surface activity composite in proportion, calculate the HLB value of this system, stir;
2) preparation of oil phase is selected one or more oil according to the HLB value of surfactant, regulates its ratio, makes the HLB of required HLB value of its emulsifying and surfactant close, and stirs;
3) surfactant and the oil phase that configures is mixed in proportion, the procyanidin that adds formula proportion again, abundant stirring and evenly mixing, at room temperature slowly drip deionized water and fully stirring, until forming the viscosity clear solution similar to aqueous solution, the critical water yield when record system becomes clarification by muddiness, what produced this moment promptly is O/W type procyanidins nano milk-like liquid medicine.
O/W type procyanidins nano milk-like liquid medicine of the present invention can be by the water infinite dilution.
Procyanidins nano milk-like liquid medicine of the present invention compared with prior art has the following advantages:
1) the present invention uses nanotechnology that procyanidin is made the procyanidins nano milk-like liquid medicine preparation can to improve its dissolubility, strengthens the stability of procyanidin.
2) the medicine dispersion that Nano medication breast viscosity of the present invention is low, particle diameter is little, contained improves, and promotes the external in vivo absorption of medicine, improves its bioavailability.
3) low, the good stability of Nano medication of the present invention breast safety, viscosity, particle diameter is little and even, and the procyanidin dispersion that is contained is improved, and promotes the external in vivo absorption of medicine.As procyanidins nano milk-like liquid medicine can being used for skin care, because of the generation of hard elastics protease capable of blocking and suppress its activity, keep skin elasticity, improve the health status of skin, than oral.
4) Nano medication breast of the present invention can be widely used in fields application such as cosmetics, medicine, beverage, health product, feedstuff.
Description of drawings
Fig. 1 is a procyanidins nano milk-like liquid medicine transmission electron microscope picture of the present invention.
The specific embodiment
The prepared procyanidins nano milk-like liquid medicine of the present invention detects through transmission electron microscope, and droplet diameter distribution is seen Fig. 1 between 10~100nm.
The prepared procyanidins nano milk-like liquid medicine of the present invention is through Detection of Stability, and the result is as follows:
1) strong illumination test
Procyanidins nano milk-like liquid medicine is placed under the illumination of 2000-4000lx, and in d5, d10 measures, and the result more still keeps clear before placing, do not see the profit layering.
2) high humility test
Procyanidins nano milk-like liquid medicine is placed under 25 ℃, 75 ℃ and 92.5 ℃ conditions of relative humidity in airtight vessel, and in d5, d10 measures, and the result more still keeps clear before placing, do not see the profit layering.
3) hot test
Procyanidins nano milk-like liquid medicine is placed respectively in 40 ℃, 60 ℃, 80 ℃ in airtight vessel, and in d5, d10 measures, and the result more still keeps clear before placing, do not see the profit layering.
4) accelerated test
Place high speed centrifuge in the centrifugal 10min of 5000r/min procyanidins nano milk-like liquid medicine, observe, keep clear, do not see the profit layering.
5) the room temperature investigation that keeps sample
Procyanidins nano milk-like liquid medicine was placed 0,1,2,3 months under 25 ℃ of room temperature/RH75 ℃ condition, still kept clear, do not see the profit layering.
Cross the transdermal test and show that this procyanidins nano milk-like liquid medicine transdermal effect is good.
Further specify its preparation method of procyanidins nano milk-like liquid medicine of the present invention below by the mode of embodiment, but do not limit the present invention in the described scope of embodiments.
Embodiment 1 preparation method
Accurately take by weighing castor oil polyoxyethylene ether-35 (EL-35) 4.5g, isopropyl myristate (IPM) 0.5g, procyanidin 0.5g, put into beaker, under 25 ℃ of room temperature conditions, manually stir its abundant mix homogeneously, to wherein slowly adding deionized water, the limit adds the waterside manually stirs then, and the system viscosity is less during beginning, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what obtained this moment is the transparent oil-in-water procyanidins nano milk-like liquid medicine of kermesinus oral liquid, claims that its gross weight is 25.00g.
Embodiment 2 preparation methoies
Accurately take by weighing castor oil polyoxyethylene ether-40 (EL-40) 4g, isopropyl myristate (IPM) 0.75g, liquid paraffin 0.25g, procyanidin 0.125g, put into beaker, under 25 ℃ of room temperature conditions, manually stir its abundant mix homogeneously, then to wherein slowly adding deionized water, the limit adds the waterside manually stirs, and the system viscosity is less during beginning, along with the increase of the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, unexpected when thinning when system, what obtained this moment is the transparent oil-in-water procyanidins nano milk-like liquid medicine of kermesinus oral liquid, continue to add water, making its final total weight is 25.00g.
Embodiment 3 preparation methoies
Accurately take by weighing castor oil polyoxyethylene ether-40 (EL-40) 7.2g, Arlacel-80 (Span-80) 1.8g, isopropyl myristate (IPM) 1g, procyanidin 0.5g, put into beaker, under 25 ℃ of room temperature conditions, manually stir its abundant mix homogeneously, then to wherein slowly adding deionized water, the limit adds the waterside manually stirs, and the system viscosity is less during beginning, along with the increase of the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, unexpected when thinning when system, what obtained this moment is the transparent oil-in-water procyanidins nano milk-like liquid medicine of kermesinus oral liquid, continue to add water, making its final total weight is 25.00g.
Embodiment 4 prescriptions
Castor oil polyoxyethylene ether-40 (EL-40) 4g
Isopropyl myristate (IPM) 0.9g
Liquid paraffin 0.175g
Vitamin E 0.175g
Deionized water 19.5g
Procyanidin 0.01g
Compound method is with implementing 1.
Embodiment 5 prescriptions
Castor oil polyoxyethylene ether-35 (EL-35) 5g
Arlacel-80 (Span-80) 1.25g
Isopropyl myristate (IPM) 1.25g
Deionized water 17.25g
Procyanidin 0.0625g
Compound method is with implementing 1.
Embodiment 6 prescriptions
Castor oil polyoxyethylene ether-35 (EL-35) 4g
Isopropyl myristate (IPM) 1g
Deionized water 17.495g
Procyanidin 0.005g
Compound method is with implementing 1.
Claims (8)
1, a kind of procyanidins nano milk-like liquid medicine is characterized in that it is made up of the following weight proportion raw material:
Surfactant 10%~40%
Oil 4%~20%
Water 50%~85%
Procyanidin 0.001%~3%
2, procyanidins nano milk-like liquid medicine according to claim 1 is characterized in that: described glass or plastic containers.
3, procyanidins nano milk-like liquid medicine according to claim 2 is characterized in that: described non-ionic surface active agent be in castor oil polyoxyethylene ether-40, the castor oil polyoxyethylene ether-35 any or any and the mixture of Arlacel-80.
4, procyanidins nano milk-like liquid medicine according to claim 1 is characterized in that: described oil is isopropyl myristate, isopropyl palmitate, liquid paraffin, any in the vitamin E oil or several mixture.
5, procyanidins nano milk-like liquid medicine according to claim 1 is characterized in that: described water is deionized water.
6, according to described any procyanidins nano milk-like liquid medicine of claim 1~5, it is characterized in that: described procyanidins nano milk-like liquid medicine particle diameter is 10nm~100nm.
7, according to the described procyanidins nano milk-like liquid medicine of claim 1~5, it is characterized in that: described procyanidins nano milk-like liquid medicine can be by the water infinite dilution.
8, the preparation method of the described procyanidins nano milk-like liquid medicine of claim 1 is characterized in that, comprises the following steps:
1) preparation of surfactant takes by weighing surfactant by formula proportion, use separately or with help surface activity composite in proportion, calculate the HLB value of this system, stir;
2) preparation of oil phase is selected one or more oil according to the HLB value of surfactant, regulates its ratio, makes the HLB of required HLB value of its emulsifying and surfactant close, and stirs;
3) surfactant and the oil phase that configures is mixed in proportion, the procyanidin that adds formula proportion again, abundant stirring and evenly mixing, at room temperature slowly drip deionized water and fully stirring, until forming the viscosity clear solution similar to aqueous solution, the critical water yield when record system becomes clarification by muddiness, what produced this moment promptly is O/W type procyanidins nano milk-like liquid medicine.
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105394521A (en) * | 2015-11-04 | 2016-03-16 | 天津科技大学 | Water-in-oil type purple sweet potato pigment micro-emulsion and preparation method thereof |
CN114437012A (en) * | 2022-02-10 | 2022-05-06 | 南宁荣港生物科技有限公司 | Extraction method and application of large-leaf protein chrysanthemum anthocyanin |
-
2006
- 2006-09-21 CN CN 200610104619 patent/CN1927182A/en active Pending
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105394521A (en) * | 2015-11-04 | 2016-03-16 | 天津科技大学 | Water-in-oil type purple sweet potato pigment micro-emulsion and preparation method thereof |
CN114437012A (en) * | 2022-02-10 | 2022-05-06 | 南宁荣港生物科技有限公司 | Extraction method and application of large-leaf protein chrysanthemum anthocyanin |
CN114437012B (en) * | 2022-02-10 | 2024-03-19 | 南宁荣港生物科技有限公司 | Extraction method and application of large leaf protein chrysanthemum anthocyanin |
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