CN106063797A - Phillyrin, phillyrin derivant, phillyrin and the application in preparing anti-oxidation medicine of the phillygenol compositions - Google Patents

Phillyrin, phillyrin derivant, phillyrin and the application in preparing anti-oxidation medicine of the phillygenol compositions Download PDF

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CN106063797A
CN106063797A CN201610247337.1A CN201610247337A CN106063797A CN 106063797 A CN106063797 A CN 106063797A CN 201610247337 A CN201610247337 A CN 201610247337A CN 106063797 A CN106063797 A CN 106063797A
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phillyrin
phillygenol
derivant
extract
medicine
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惠敏
富力
王凯乾
鲁明明
王硕
柳洋
冯雪
刘正贤
刘国友
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Abstract

The invention discloses a kind of phillyrin, phillyrin derivant, phillyrin and phillygenol compositions new opplication in preparing anti-oxidation medicine.Test proves, phillyrin, phillyrin derivant, phillyrin are notable with phillygenol compositions antioxidative effect, instant effect, toxic and side effects are little, be a kind of safe efficient, stable, simple anti-oxidation medicine of preparation technology, be suitable to industrialized production, it is easy to popularization.The present invention is that antioxidation provides a kind of new medicament sources.

Description

Phillyrin, phillyrin derivant, phillyrin and phillygenol compositions are preparing antioxygen Application in chemical medicine thing
Technical field
The present invention relates to field of medicaments, relate to a kind of antioxidative medicine or health food, particularly to a kind of Chinese medicine even Stick up and the application in preparing anti-oxidation medicine or health food of the Folium Forsythiae extract component.
Background technology
Aging be biosphere exist universal rule, be not with human will be transfer rule biology.Old and decline The concept being always correlated with but differ.Before more than 2,000 years, China's " Songs of the South " just has the saying of " year did not both wane always ".Decline An always biological process, and old being usually determines with the age as standard.According to global comprehensive condition, especially Being the situation looking after developing country, nineteen eighty-two determines 60 years old on the United Nations's aging problem world convention opens for senile Begin the age.In recent years, along with people's life and the raising of health level, increasing 60～65 years old old people's still health be good for Strong, energetic.To be born in mid-term 21 century in the peak of design population's aging, this means that 21 century gerontology research One content complexity of middle existence, difficulty are big, involve a wide range of knowledge aging and the new problem of research on anti-senescence, extend the longevity the most further How life, make the life quality of this long-lived crowd improve further, and this problem is the science that the world today has profound influence Forward position.
Aoxidize the chief-criminal that the biochemistry untoward reaction relevant to energy metabolism with nonenzymatic glycosylation the two is environmental injury Chief culprit, serves conclusive effect in human aging process, and therefore relevant research is just increasingly becoming Aging mechanism and grinding The focus and emphasis studied carefully.The physiology of the biomacromolecule that Free radicals injury--oxidative stress causes and pathologic damage and repair The accumulation of decorations is to cause organism pathological changes and an old and feeble modal biochemical reaction of class；Nonenzymatic glycosylation is modified and is and old and feeble phase The another kind of particularly important biochemical reaction closed, the aging and the disease that cause with diabetes are relevant, and this reaction is (non-without enzyme Enzyme) catalysis, can spontaneous carry out.Research shows that the oxidation nonenzymatic glycosylation effect of free radical mediated in aging course strengthens, and leads Cause the change of protein structure and function, accelerate old and feeble process.
Modern study finds that many herbal polysaccharides all have raising antioxidant enzyme activities, remove free radical, suppression lipid peroxy Change, thus protect biomembranous effect.
Chinese medicine anti-oxidation effect that is health care, long-standing, in " Sheng Nong's herbal classic " is classified as top grade all medicines, greatly Polyphyly is prolonged life, the oldest defying age health care medicine, such as Radix Ginseng, Fructus Ligustri Lucidi, Herba Cistanches, Radix Ophiopogonis, Fructus Lycii ... wait all Be loaded with " ... for a long time clothes make light of one's life by commiting suicide, prolong life, the most hungry, the oldest.”.Modern age it " Compendium of Materia Medica " contained tonic of Li Shizhen (1518-1593 A.D.) also reach 197 kinds it Many, and the most contained tonic prescription is thousands of, but to lie prostrate Siberian cocklebur, Radix Rehmanniae Preparata, Radix Ginseng, Semen Cuscutae, Herba Cistanches, Cortex Cinnamomi, The frequencies of occurrences such as Fructus Lycii, the Cortex Eucommiae, Rhizoma Dioscoreae, Radix Glycyrrhizae, Cornu Cervi Pantotrichum are higher, it was demonstrated that determined curative effect.
Fructus Forsythiae is that Chinese medicine clinic commonly uses one of conventional medicament, is widely used, and consumption is huge, and it has heat clearing away and " detoxifies " detumescence " removing the function of free radical, often Chinese herbal medicine with other makes formula use to eliminating stagnation clinically.Wherein concrete active component is the most not Clear, inventor is through arduous exploration, and preparation is extracted wherein active monomer compound phillyrin, and through chemosynthesis, preparation Corresponding derivant, has carried out a series of pharmacology activity research, finds phillyrin, phillyrin derivant, phillyrin and company Stick up acid value of lipids and the rising of peroxide value that fat promotor composition can delay High-Temperature Strengthening to preserve, can be as natural anti-oxidation Agent, illustrates that phillyrin, phillyrin derivant, phillyrin and phillygenol compositions have antioxidation, opens for patient New treatment by way of.
Phillyrin (phillyrin)
Phillygenol ((+)-phillygenin)
The present inventor passes through substantial amounts of modern scientific research, uses advanced separating and purifying technology from Fructus Forsythiae and Folium Forsythiae Extract its antioxidative effective ingredient phillyrin, and the most synthetically prepared phillyrin derivant.Can be patient The medicine of a kind of high-efficiency low-toxicity is provided.
Summary of the invention
The primary and foremost purpose of the present invention be to provide phillyrin, phillyrin derivant or phillyrin and phillygenol (i.e. phillyrin/ Phillygenol) for antioxidative new opplication, and provide phillyrin, phillyrin derivant or phillyrin and phillygenol for making The new application of standby antioxidative medication, i.e. new opplication in antioxidative medicine or health food.
For achieving the above object, one aspect of the present invention provides a kind of phillyrin, phillyrin derivant or phillyrin and Fructus Forsythiae The application in preparing anti-oxidation medicine or health product of the fat element.
During screening has the active skull cap components of antioxidation, inventor finds in the chemical composition of Fructus Forsythiae Phillyrin, phillyrin derivant, phillyrin/phillygenol compositions has strong antioxidative effect.
Wherein, described medicine or health product by phillyrin, phillyrin derivant or phillyrin and phillygenol compositions and Pharmaceutically acceptable carrier forms.
Particularly, described phillyrin derivant selects phillygenol glucal acid derivative.
Particularly, described phillyrin derivant includes 33-hydroxyl-phillygenol glucuronide (33-Hydroxy Phillygenin-8-O-β-D-glucuronide), 9-hydroxyl-phillygenol glucuronide (9-Hydroxy Phillygenin-8-O-β-D-glucuronide), 33,34-methylene dioxy-phillygenol glucuronide (33,34- Methylenedioxy phillygenin-8-O-β-D-glucuronide), phillygenol glucuronic acid methyl ester ((2R, 3R,4R,5S)-methyl6-(5-((1R,4S)-4-(3,4-dimethoxyphenyl)hexahydrofuro[3,4-c] furan-1-yl)-2-methoxyphenoxy)-3,4,5-trihydroxyte tra hydro-2H-pyran-2- Carboxylate), phillygenol D-Glucuronic acid sodium salt (sodium (2R, 3R, 4R, 5S)-6-(5-((1R, 4S)-4-(3,4- dimethoxyphenyl)hexahydrofuro[3,4-c]furan-1-yl)-2-methoxyphenoxy)-3,4,5- Trihydroxytetrahydro-2H-pyran-2-carboxylate), phillygenol glucuronic acid potassium (potassium (2R,3R,4R,5S)-6-(5-((1R,4S)-4-(3,4-dimethoxyphenyl)hexahydrofuro[3,4-c]furan- 1-yl)-2-methoxyphenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylate), even Stick up fat element glucuronic acid ((2R, 3R, 4R, 5S)-6-(5-((1R, 4S)-4-(3,4-dimethoxyphenyl) hexahydrofuro[3,4-c]furan-1-yl)-2-methoxyphenoxy)-3,4,5-trihydroxytetrahydro- 2H-pyran-2-carboxylic acid)；It is preferably 33-hydroxyl-phillygenol glucuronide, 9-hydroxyl-Fructus Forsythiae fat Element glucuronide, 33,34-methylene dioxy-phillygenol glucuronide, phillygenol glucuronic acid methyl ester, Phillygenol D-Glucuronic acid sodium salt or phillygenol glucuronic acid potassium.
Particularly, in described phillyrin and phillygenol compositions the weight of phillyrin and phillygenol be 2～ 98:2～98；It is preferably 2-10:90-98；More preferably 80:20 or 20:80, more preferably 90:10 or 10:90, Further it is preferably 98:2 or 2:98；Much further preferably from 98:2.
Wherein, described phillyrin, content >=1% of phillyrin derivant, it is preferably >=30%, more preferably >= 60%, further it is preferably >=80%, is more further preferably >=98%；Phillyrin and phillygenol composition levels >= 1%, it is preferably >=30%, more preferably >=60%, is further preferably >=80%, be more further preferably >= 98%.
Particularly, described phillyrin, phillyrin derivative content are 1%～98%；It is preferably 30～80%；Phillyrin It is 1%～98% with phillygenol composition levels；It is preferably 30～80%.
Particularly, pharmaceutically acceptable carrier generally by sanitarian's accreditation for this purpose and non-as medicament Active component.Compilation about pharmaceutically acceptable carrier can be at " handbook of pharmaceutical excipients " (Handbook of Pharmaceutical excipients, second edition, A.Wade and P.J.Weller edit；American Pharmaceutical Association publishes, Washington and The Pharmaceutical Press, London, 1994) etc. reference book finds.
Especially, described carrier includes excipient, such as starch, water etc.；Lubricant, such as magnesium stearate etc.；Disintegrating agent, as Microcrystalline Cellulose etc.；Filler, such as lactose etc.；Binding agent, such as pregelatinized Starch, dextrin etc.；Sweeting agent；Antioxidant；Anticorrosion Agent, correctives, spice etc.；
Wherein, described medicine exists with tablet, capsule, pill, powder, granule, syrup form.
Particularly, described phillyrin, phillyrin derivative content >=1%, it is preferably >=30%, more preferably >= 60%, further it is preferably >=80%, is more further preferably >=98%；Phillyrin and phillygenol composition levels >= 1%, it is preferably >=30%, more preferably >=60%, is further preferably >=80%, be more further preferably >= 98%.
Another aspect of the present invention provides one containing phillyrin, phillyrin derivant or phillyrin and phillygenol compositions Anti-oxidation medicine or health product.
Wherein, described phillyrin derivant selects phillygenol glucal acid derivative.
Particularly, described phillyrin derivant includes 33-hydroxyl-phillygenol glucuronide, 9-hydroxyl-Fructus Forsythiae fat Element glucuronide, 33,34-methylene dioxy-phillygenol glucuronide, phillygenol glucuronic acid methyl ester, Phillygenol D-Glucuronic acid sodium salt, phillygenol glucuronic acid potassium, phillygenol glucuronic acid；It is preferably 33-hydroxyl-company Stick up fat element glucuronide, 9-hydroxyl-phillygenol glucuronide, 33,34-methylene dioxy-phillygenol Fructus Vitis viniferae Glycuronide, phillygenol glucuronic acid methyl ester, phillygenol D-Glucuronic acid sodium salt or phillygenol glucuronic acid potassium.
Wherein, described phillyrin is 2～98 with the weight of phillyrin in phillygenol compositions with phillygenol: 2～98；It is preferably 2-10:90-98；More preferably 80:20 or 20:80, more preferably 90:10 or 10:90, more enter One step is preferably 98:2 or 2:98；Much further preferably from 98:2.
Particularly, described phillyrin, content >=1% of phillyrin derivant, it is preferably >=30%, more preferably >=60%, further it is preferably >=80%, is more further preferably >=98%；Phillyrin and phillygenol composition levels >=1%, it is preferably >=30%, more preferably >=60%, is further preferably >=80%, be more further preferably >= 98%.
Especially, described phillyrin, content >=1% of phillyrin derivant, preferably 1%～98%；It is preferably 30 ～80%, the most preferably 60%；Phillyrin and phillygenol composition levels >=1%, preferably 1%～98%；Excellent Elect 30～80%, the most preferably 60% as.
Particularly, the weight of described phillyrin, phillyrin derivant or phillyrin and phillygenol compositions and described medicine The ratio of the gross weight of thing or health product is 0.01-10:100, preferably 0.1～10:100, more preferably 1～10:100.
Wherein, described phillyrin/phillygenol compositions with monomer composition or uses solvent with phillyrin and phillygenol The phillygenol that heating extraction method is prepared from-phillyrin extracts compositions, or phillygenol and phillyrin and cyclodextrin or The derivant of cyclodextrin combines phillygenol-phillyrin-cyclodextrin composite.
Particularly, described phillygenol-phillyrin-cyclodextrin composite select phillygenol and phillyrin and α-, β-or The mixture that gamma-cyclodextrin or derivatives thereof mixes mutually, or phillygenol and phillyrin and α-, β-or gamma-cyclodextrin or The complex that its derivant is formed through physics, chemical method process.
Wherein, in described phillygenol-phillyrin-cyclodextrin composite phillyrin and phillygenol weight and cyclodextrin or The weight ratio of the derivant of cyclodextrin is 1:1-50.
Particularly, described cyclodextrin be α-or β-, gamma-cyclodextrin；Described cyclodextrin derivative be ethoxy-cyclodextrin, 2,6-dimethyl-cyclodextrin, 2,3,6-trimethyl-cyclodextrin, 2,6-diethyl-cyclodextrin, 2,3,6-triethyl group-cyclodextrin, Maltosyl-cyclodextrin or sulfobutyl ether beta-schardinger dextrin-, p-methyl benzene sulfonic chloride (p-TsCl) substituted beta-schardinger dextrin-, the replacement of 6-position β-CD p-methyl benzenesulfonic acid ester (beta-schardinger dextrin--6-OTs), 2-oxygen HP-β-CD, 2-position mono-substituted to methylbenzene Sulphonic acid ester (beta-schardinger dextrin--2-OTs), beta-schardinger dextrin-p-methyl benzenesulfonic acid ester (Tosyl-β-CD), the star of beta-schardinger dextrin-are divided greatly Sub-PCL-(Tos) 7-β-CD.
Particularly, described medicine or health product also include lying prostrate Siberian cocklebur extract, Radix Rehmanniae Preparata extract, Radix Ginseng extract, Herba cuscutae Seed extract, Herba Cistanches extract, Cortex Cinnamomi extract, Fructus Lycii extract, Cortex Eucommiae extract, Rhizoma Dioscoreae extract, Radix Glycyrrhizae are extracted Thing, Cornu Cervi Pantotrichum extract, vitamin C and derivant thereof or vitamin E and derivant thereof.
Compared with prior art, the present invention has a following obvious advantage:
1, known compound phillyrin, phillyrin derivant, phillyrin/phillygenol compositions have been excavated newly by the present invention Medical value, use it for antioxidation, and antioxidative medicine or health food can be prepared as, thus be Fructus Forsythiae and Folium Forsythiae A new field has been opened up in the application of medical material.
2, the campaign research of the present invention proves known compound phillyrin, phillyrin derivant, phillyrin/Fructus Forsythiae fat Promotor composition has notable antioxidative effect.
3, the known compound phillyrin of the present invention, phillyrin derivant, phillyrin/phillygenol compositions pharmacological action By force, notable for antioxidative effect, instant effect, toxic and side effects are little, safety good, it is possible to long-term taking, have good medicine Use prospect.
4, the products material abundance of the present invention, inexpensive, Clinical practice safety, preparation technology is simple, can be made into various Dosage form, and dosing is little, easy to use, it is thus susceptible to promote.
5, the present invention both can use the phillyrin of single component, phillyrin derivant or double-component phillyrin/phillygenol Compositions active component prepares antioxidative medicine, can use again phillyrin, phillyrin derivant and or phillyrin/phillygenol Compositions and other active component are (such as with volt Siberian cocklebur extract, Radix Rehmanniae Preparata extract, Radix Ginseng extract, Semen Cuscutae extract, meat desert Rong's extract, Cortex Cinnamomi extract, Fructus Lycii extract, Cortex Eucommiae extract, Rhizoma Dioscoreae extract, Radix Glycyrrhizae extract, Cornu Cervi Pantotrichum extract, Vitamin C and derivant thereof or vitamin E and derivant thereof.) common prescription, prepare antioxidative compound medicine.
Detailed description of the invention
The beneficial effect of formula of the present invention is further described, these embodiment bags below by detailed description of the invention Phillyrin and the capsule of phillyrin derivant, tablet, the pharmacodynamics test of soft capsule of the present invention are included.These embodiments are only It is exemplary, the scope of the present invention is not constituted any restriction.It will be understood by those skilled in the art that without departing from The details of technical solution of the present invention and form can be modified or replace under the formula thinking of the present invention, purposes scope, but These amendments and replacement each fall within protection scope of the present invention.
Heretofore described phillyrin derivant 33-hydroxyl-phillygenol glucuronide, 9-hydroxyl-phillygenol Glucuronide, 33,34-methylene dioxy-phillygenol glucuronide and patent application (application number: 201510319303.4, priority number: 201510164294.6) described in phillyrin derivant identical；Phillygenol glucose Aldehydic acid methyl ester, phillygenol D-Glucuronic acid sodium salt, phillygenol glucuronic acid potassium, phillygenol glucuronic acid and patent Shen Please identical in (application number: 201510320579.4, priority number: 201410825547.5).
Embodiment 1 phillyrin tablet
1, raw material is prepared according to following proportioning
2, granule will be made after phillyrin and starch mix homogeneously, suppress after adding Pulvis Talci and magnesium stearate mix homogeneously Become 10000.
Embodiment 2 phillyrin capsule
1, raw material is prepared according to following proportioning
Phillyrin (purity 94%) 200g
Starch 1000g
2, by encapsulated after phillyrin and starch mix homogeneously, 10000 are made.
Embodiment 3 phillyrin capsule
1, raw material is prepared according to following proportioning
Phillyrin (purity 98%) 500g
Starch 1000g
2, by encapsulated after phillyrin and starch mix homogeneously, 10000 are made.
Embodiment 4 phillyrin tablet
1, raw material is prepared according to following proportioning
2, by after phillyrin, Radix Ginseng extract, vitamin C and starch mix homogeneously, make granule, add Pulvis Talci with hard 10000 it are pressed into after fatty acid magnesium mix homogeneously.
Embodiment 5 phillyrin capsule
1, raw material is prepared according to following proportioning
2, by encapsulated after phillyrin, Poria extract, vitamin C and starch mix homogeneously, 10000 are made.
Embodiment 6 phillyrin granule
2, pack after phillyrin, Herba Cistanches extract, vitamin C and cane sugar powder mix homogeneously are made granule, make 10000 bags.
Embodiment 7 phillyrin oral liquid
1, raw material is prepared according to following proportioning
2, take phillyrin, Radix Rehmanniae Preparata extract, Rhizoma Dioscoreae extract, add dextrose syrup after dissolving with ethanol, finally add Ionized water, to 100ml, to obtain final product.
Embodiment 8 33-hydroxyl-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, by after 33-hydroxyl-phillygenol glucuronide and starch mix homogeneously, make granule, add Pulvis Talci Be pressed into 10000 after magnesium stearate mix homogeneously.
Embodiment 9 33-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
33-hydroxyl-phillygenol glucuronide (purity 60%) 200g
Starch 1000g
2, by encapsulated after 33-hydroxyl-phillygenol glucuronide and starch mix homogeneously, 10000 are made.
Embodiment 10 33-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
33-hydroxyl-phillygenol glucuronide (purity 98%) 500g
Starch 1000g
2, by encapsulated after 33-hydroxyl-phillygenol glucuronide and starch mix homogeneously, 10000 are made.
Embodiment 11 33-hydroxyl-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, will make after 33-hydroxyl-phillygenol glucuronide, Radix Glycyrrhizae extract, vitamin C and starch mix homogeneously Grain, is pressed into 10000 after adding Pulvis Talci and magnesium stearate mixing.
Embodiment 12 33-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
2, by after 33-hydroxyl-phillygenol glucuronide, Fructus Lycii extract, vitamin C and starch mix homogeneously Encapsulated, make 10000.
Embodiment 13 33-hydroxyl-phillygenol glucuronide granule
1, raw material is prepared according to following proportioning
2, by 33-hydroxyl-phillygenol glucuronide, Cortex Eucommiae extract, vitamin C and cane sugar powder mix homogeneously system Pack after becoming granule, make 10000 bags.
Embodiment 14 33-hydroxyl-phillygenol glucuronic acid glucoside oral liquid
1, raw material is prepared according to following proportioning
2, take 33-hydroxyl-phillygenol glucuronide, Cortex Eucommiae extract, Radix Glycyrrhizae extract, add after dissolving with ethanol Enter dextrose syrup, finally add deionized water to 100ml, to obtain final product.
Embodiment 15 9-hydroxyl-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, by after 9-hydroxyl-phillygenol glucuronide and starch mix homogeneously, make granule, add Pulvis Talci and 10000 it are pressed into after magnesium stearate mix homogeneously.
Embodiment 16 9-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
9-hydroxyl-phillygenol glucuronide (purity 97%) 200g
Starch 1000g
2, by encapsulated after 9-hydroxyl-phillygenol glucuronide and starch mix homogeneously, 10000 are made.
Embodiment 17 9-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
9-hydroxyl-phillygenol glucuronide (purity 98%) 500g
Starch 1000g
2, by encapsulated after 9-hydroxyl-phillygenol glucuronide and starch mix homogeneously, 10000 are made.
Embodiment 18 9-hydroxyl-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, will make after 9-hydroxyl-phillygenol glucuronide, Radix Glycyrrhizae extract, vitamin C and starch mix homogeneously Grain, is pressed into 10000 after adding Pulvis Talci and magnesium stearate mixing.
Embodiment 19 9-hydroxyl-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
2, by after 9-hydroxyl-phillygenol glucuronide, Semen Cuscutae extract, vitamin C and starch mix homogeneously Encapsulated, make 10000.
Embodiment 20 9-hydroxyl-phillygenol glucuronide granule
1, raw material is prepared according to following proportioning
2, by 9-hydroxyl-phillygenol glucuronide, Cortex Eucommiae extract, vitamin C and cane sugar powder mix homogeneously system Pack after becoming granule, make 10000 bags.
Embodiment 21 9-hydroxyl-phillygenol glucuronic acid glucoside oral liquid
1, raw material is prepared according to following proportioning
2, take 9-hydroxyl-phillygenol glucuronide, Cortex Eucommiae extract, Radix Rehmanniae Preparata extract, add after dissolving with ethanol Enter dextrose syrup, finally add deionized water to 100ml, to obtain final product.
Embodiment 22 33,34-methylene dioxy-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, by 33, after 34-methylene dioxy-phillygenol glucuronide and starch mix homogeneously, make granule, add It is pressed into 10000 after entering Pulvis Talci and magnesium stearate mix homogeneously.
Embodiment 23 33,34-methylene dioxy-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
33,34-methylene dioxies-phillygenol glucuronide (purity 97%) 200g
Starch 1000g
2, by 33, encapsulated after 34-methylene dioxy-phillygenol glucuronide and starch mix homogeneously, make 10000.
Embodiment 24 33,34-methylene dioxy-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
33,34-methylene dioxies-phillygenol glucuronide (purity 98%) 500g
Starch 1000g
2, by 33, encapsulated after 34-methylene dioxy-phillygenol glucuronide and starch mix homogeneously, make 10000.
Embodiment 25 33,34-methylene dioxy-phillygenol glucuronide tablet
1, raw material is prepared according to following proportioning
2, by 33,34-methylene dioxy-phillygenol glucuronide, Radix Rehmanniae Preparata extract, vitamin C and starch are mixed Pelletize after closing uniformly, after adding Pulvis Talci and magnesium stearate mixing, be pressed into 10000.
Embodiment 26 33,34-methylene dioxy-phillygenol glucuronide capsule
1, raw material is prepared according to following proportioning
2, by 33,34-methylene dioxy-phillygenol glucuronide, Semen Cuscutae extract, vitamin C and starch After mix homogeneously encapsulated, make 10000.
Embodiment 27 33,34-methylene dioxy-phillygenol glucuronide granule
1, raw material is prepared according to following proportioning
2, by 33,34-methylene dioxy-phillygenol glucuronide, Cortex Eucommiae extract, vitamin C and cane sugar powder Mix homogeneously packs after making granule, makes 10000 bags.
Embodiment 28 33,34-methylene dioxy-phillygenol glucuronide granule
1, raw material is prepared according to following proportioning
2, by 33,34-methylene dioxy-phillygenol glucuronide, Cortex Eucommiae extract, vitamin C and cane sugar powder Mix homogeneously packs after making granule, makes 10000 bags.
Embodiment 29 33,34-methylene dioxy-phillygenol glucuronic acid glucoside oral liquid
1, raw material is prepared according to following proportioning
2,33 are taken, 34-methylene dioxy-phillygenol glucuronide, Cortex Eucommiae extract, Radix Rehmanniae Preparata extract, use second Alcohol adds dextrose syrup after dissolving, and finally adds deionized water to 100ml, to obtain final product.
Prepared by embodiment 30 phillyrin and phillygenol composition tablet
1, the tablet of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, take phillyrin 490g, after phillygenol 10g mixs homogeneously with starch, make granule, add Pulvis Talci and tristearin It is pressed into 10000 after acid magnesium mix homogeneously.
Prepared by embodiment 31 phillyrins/phillygenol composition granule
1, the granule of phillyrin/phillygenol compositions is prepared according to following proportioning:
Phillyrin/phillygenol compositions (both weight ratios are 98:2) 100g
Microcrystalline Cellulose 10000g
2, take phillyrin 98g, after phillygenol 2g mixs homogeneously with microcrystalline Cellulose, make granule pack, make 10000 Bag.
Prepared by embodiment 32 phillyrins/phillygenol composition capsule
1, the capsule of phillyrin/phillygenol compositions is prepared according to following proportioning:
Phillyrin/phillygenol compositions (both weight ratios are 98:2) 250g
Starch 2500g
2, take phillyrin 245g, phillygenol 5g encapsulated after mixing homogeneously with starch, make 10000.
Prepared by embodiment 33-36 phillyrin/phillygenol composition capsule
In embodiment 33-36, after the weight ratio of phillyrin/phillygenol compositions according to the form below respectively is mixed homogeneously with starch Encapsulated, respectively make 10000 seed lac capsules.
Embodiment: prepared by 37-40 phillyrin/phillygenol composition granule
In embodiment 37-30, the weight ratio of phillyrin/phillygenol compositions according to the form below respectively mixes with microcrystalline Cellulose After Jun Yun, make granule pack, make 10000 bags.
Prepared by embodiment 41 phillyrins/phillygenol composition tablet
1, the tablet of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, weigh phillyrin 490g, phillygenol 10g is mixed homogeneously with Cortex Cinnamomi extract powder, then is mixed homogeneously with starch After make granule, be pressed into 10000 after adding Pulvis Talci and magnesium stearate mix homogeneously.
Prepared by embodiment 42 phillyrins/phillygenol composition granule
1, the granule of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, take phillyrin 245g, phillygenol 5 is mixed homogeneously with Rhizoma Dioscoreae extract, Cortex Cinnamomi extract powder, then with crystallite Make granule pack after cellulose mix homogeneously, make 10000 bags.
Prepared by embodiment 43 phillyrins/phillygenol composition capsule
1, the capsule of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, phillyrin 245g, phillygenol 5g mix all with Cornu Cervi Pantotrichum extract, Radix Ginseng extract, Herba Cistanches extract powder Even more encapsulated after mixing homogeneously with starch, make 10000.
Prepared by embodiment 44 phillyrins/phillygenol composition tablet
1, the tablet of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, take phillyrin 490g, phillygenol 10g is mixed homogeneously with Radix Ginseng extract powder, then after mixing homogeneously with starch Make granule, press after adding Pulvis Talci and magnesium stearate mix homogeneously, make 10000.
Prepared by embodiment 45 phillyrins/phillygenol composition granule
1, the granule of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, take phillyrin 900g, phillygenol 100g to mix homogeneously with said extracted thing (Radix Rehmanniae Preparata, Semen Cuscutae) powder, then with Make granule pack after microcrystalline Cellulose mix homogeneously, make 10000 bags.
Prepared by embodiment 46 phillyrins/phillygenol composition capsule
1, the capsule of phillyrin/phillygenol compositions is prepared according to following proportioning:
2, phillyrin 1880g, phillygenol 120g are mixed homogeneously with said extracted thing (Radix Rehmanniae Preparata, Rhizoma Smilacis Glabrae, Radix Ginseng) powder, After mixing homogeneously with starch more encapsulated, make 10000.
Test example 1 phillyrin, phillyrin derivant, phillyrin and the mensuration of phillygenol composition removing OH free radical
1 test material
1.1 medicines and reagent
Phillyrin, white powder, Dalian Fu Sheng natural drug development corporation, Ltd. produces, through high performance liquid chromatography two kinds inspection Surveying device UV-detector and evaporative light scattering detector area normalization method to measure, its purity is 99.5%, and with Chinese medicine Biological product assay phillyrin reference substance is demarcated and confirms that its content is 99.5%.Lot number: 20130303.
Phillygenol (content ＞ 98%), white powder, Dalian Fu Sheng natural drug development corporation, Ltd. produces, lot number: 20130301
33-hydroxyl-phillygenol glucuronide (phillyrin derivant A, content ＞ 98%), white powder, Dalian Fu Sheng natural drug development corporation, Ltd. produces, lot number: 20130301.Through two kinds of detector UV-detector of high performance liquid chromatography Measuring with evaporative light scattering detector area normalization method, its purity is 98.5%.
9-hydroxyl-phillygenol glucuronide (phillyrin derivant B, content ＞ 98%), white powder, Dalian is rich Raw natural drug development corporation, Ltd. produces, lot number: 20130302.Through two kinds of detector UV-detector of high performance liquid chromatography and Evaporative light scattering detector area normalization method measures, and its purity is 99.2%.
33,34-methylene dioxies-phillygenol glucuronide (phillyrin derivant C, content ＞ 98%), white Powder, Dalian Fu Sheng natural drug development corporation, Ltd. produces, lot number: 20130301.Through two kinds of detectors of high performance liquid chromatography UV-detector and evaporative light scattering detector area normalization method measure, and its purity is 98.7%.
Phillyrin/phillygenol compositions A, phillyrin (content ＞ 98%), white powder, richness raw natural drug in Dalian is opened Send out company limited to produce, lot number: 20130303；Phillygenol (content ＞ 98%), white powder, richness raw natural drug in Dalian is opened Send out company limited to produce, lot number: 20130301；Phillyrin is 98:2 with the weight ratio of phillygenol.
Phillyrin/phillygenol compositions B, phillyrin (content ＞ 98%), white powder, richness raw natural drug in Dalian is opened Send out company limited to produce, lot number: 20130303；Phillygenol (content ＞ 98%), white powder, richness raw natural drug in Dalian is opened Send out company limited to produce, lot number: 20130301；Phillyrin is 90:10 with the weight ratio of phillygenol.
Orthophenanthroline (is produced by Ke Miou chemical reagent development centre, Tianjin, lot number: GB1293-13)；Ferrous sulfate, H202Hydrogen peroxide, positive control VC etc. are domestic analytical pure.
2 test methods
Use H202/Fe2+System method [gold ring, dish Asia is glad. orthophenanthroline-Fe2+Oxidizing process detection H202/Fe2+The hydroxyl produced Free radical [J]. Progress in Biochemistry and Biophysics, 1996,23 (6): 553-555], phillyrin, phillygenol, phillyrin spread out Biological A, phillyrin derivant B, phillyrin derivant C, phillyrin and phillygenol compositions A, phillyrin and phillygenol group Compound B measures respectively.
Every kind of medicine takes 9 test tubes, is separately added into 0.75mmol/L orthophenanthroline solution 1mL, 150mmol/LPBS buffering Liquid (pH7.4) 1.5mL, 0.75mmol/LFeSO41mL, 0.01%H2021mL (wherein one is only used as not damaging pipe, is not added with H202), then it being separately added into variable concentrations drug solution (being wherein only used as damage pipe, be not added with medicine), damage is managed and is not damaged pipe Volume is supplemented with dehydrated alcohol.Wherein addition same volume 1mg/LVC is placed on 37 as positive drug control group, mix homogeneously Incubation 1h in DEG C water-bath, measures absorbance under 536nm wavelength after cooling.
Being calculated as follows of OH clearance rate: OH clearance rate=[(A2One A1)/(A0—A1)] in × 100% formula----formula 1,
A0: do not damage the absorbance of pipe, A1: the absorbance of damage pipe, A2: the absorbance of dosing group pipe.
OH free radical scavenging activity measurement result is shown in Table 1.
Table 1 phillyrin, phillyrin derivant, phillyrin and the phillygenol compositions scavenging action (x to hydroxyl radical free radical ± s, n=4)
Note: compared with positive drug control group, *: P < 0.05
In addition to phillygenol and other phillyrins and related compounds below substrate concentration 0.006/mL group, each dosage group and the positive The all removings to hydroxyl radical free radical of medicine group have certain effect, and along with the increase of drug level, clearance rate is in rising trend, through F Inspection, data difference significance, phillyrin derivant A and phillyrin derivant C are the strongest to hydroxyl radical free radical scavenging action.
Test example 2 phillyrin, phillyrin derivant, phillyrin and phillygenol composition removing O2 -The mensuration of free radical
1 test material
1.1 medicines and reagent
Phillyrin, phillyrin derivant, phillyrin and phillygenol compositions, phillygenol are with test example 1, hydrochloric acid hydroxyl Amine, Ammonium persulfate. (AP), p-aminobenzene sulfonic acid, α mono-naphthylamines, trishydroxymethylaminomethane (tris) and N, N, N,, N,-tetramethyl Ethylenediamine (TEMED), positive control VC etc. are domestic analytical pure.
2 test methods
Using AP-TEMED system of determination, each medicine is individually tested.Each medicine takes 8 and measures pipe, is separately added into A liquid (1mol/LHCL48ml, Tris36.6g, TEMED0.23mL, constant volume is in 100mL) 1mL, B liquid (140mg AP constant volume is in 100mL) 4mL, after reaction 1min, draws mixed liquor 2mL from often pipe, adds people's variable concentrations phillyrin, phillygenol, phillyrin derivant A, phillyrin derivant B, phillyrin derivant C, phillyrin and phillygenol compositions A, phillyrin and phillygenol compositions B The solution BHT of 2%0 concentration (positive drug control group add), mixing, with same volume dehydrated alcohol for comparison.Add to each pipe again Enter 10mmol/L oxammonium hydrochloride. 0.4mL, 25 DEG C of hybrid reactions 20min, add 17mmol/L p-aminobenzene sulfonic acid 2ml and 7mmol/ L alpha-naphthylamine 2mL, in 25 DEG C react 25min, add same volume n-butyl alcohol and fully shake up, stratification, draw n-butyl alcohol in Light absorption value is measured under 530nm wavelength.
O2 -Free radical scavenging activity (%)=[(A0One A1)/A0] × 100%-----formula 2
In formula: A0Absorbance for ethanol solution；A1Absorbance for dosing group
O2 -Free radical scavenging activity measurement result is as shown in table 2.
Table 2 phillyrin, phillyrin derivant, phillyrin and phillygenol compositions are to O2-Scavenging action (the x of free radical ± s, n=4)
Note: compared with positive drug control group, *: P < 0.05, * *: P < 0.01
Result of the test from table 2: the change reflection phillyrin of absorbance, phillyrin derivant and combinations thereof thing is each Dosage group is to O2 -Free radical is respectively provided with certain scavenging action, in addition to 12mg/mL medicine group, along with the increase of drug level, clearly Except rate is in rising trend, checking through F, data difference has significant and pole significant, and phillyrin derivant C is to O2 -From The strongest by base scavenging action, phillygenol has Synergistic almost without scavenging action, phillyrin and phillygenol use in conjunction Effect.

Claims (10)

1. phillyrin, phillyrin derivant, phillyrin are used for antioxidative medicine or health care with phillygenol compositions in preparation Application in product.
Application the most according to claim 1, it is characterized in that described medicine by phillyrin, phillyrin derivant or phillyrin with Phillygenol compositions and pharmaceutically acceptable carrier composition.
Application the most according to claim 1 and 2, is characterized in that described medicine is with tablet, capsule, pill, powder, granule Agent, syrup, solution form exist.
Application the most according to claim 1 and 2, it is characterized in that described phillyrin, phillyrin derivant purity for >= 1%；Phillyrin and content >=1% of phillygenol compositions.
Application the most according to claim 4, is characterized in that described phillyrin, the purity of phillyrin derivant are 1%～98%；Phillyrin is 1%～98% with the content of phillygenol compositions.
6. for antioxidative medicine or health product, it is characterized in that containing phillyrin, phillyrin derivant or phillyrin with Phillygenol compositions.
Medicine the most according to claim 6 or health product, is characterized in that described phillyrin, the purity of phillyrin derivant For >=1%；Phillyrin and content >=1% of phillygenol compositions.
Medicine the most according to claim 6 or health product, is characterized in that described phillyrin, phillyrin derivant or phillyrin It is 0.01-10:100 with the ratio of the weight of phillygenol compositions with the gross weight of described medicine or health product.
Medicine the most according to claim 6 or health product, is characterized in that described phillyrin selects with phillygenol compositions Phillygenol and phillyrin and α-, the mixture that mixes mutually of β-or gamma-cyclodextrin or derivatives thereof, or phillygenol and company Stick up glycosides and α-, the complex that formed through physics, chemical method process of β-or gamma-cyclodextrin or derivatives thereof.
Medicine the most according to claim 6 or health product, is characterized in that also including lying prostrate Siberian cocklebur extract, Radix Rehmanniae Preparata extract, people Conopsea extraction, Semen Cuscutae extract, Herba Cistanches extract, Cortex Cinnamomi extract, Fructus Lycii extract, Cortex Eucommiae extract, Rhizoma Dioscoreae carry Take thing, Radix Glycyrrhizae extract, Cornu Cervi Pantotrichum extract, vitamin C and derivant thereof or vitamin E and derivant thereof.
CN201610247337.1A 2015-04-23 2016-04-20 Phillyrin, phillyrin derivant, phillyrin and the application in preparing anti-oxidation medicine of the phillygenol compositions Pending CN106063797A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022048529A1 (en) * 2020-09-04 2022-03-10 大连富生天然药物开发有限公司 Forsythiae fructus component and optional ginseng component, and use thereof
CN117229338A (en) * 2023-11-13 2023-12-15 中泰(天津)生物科技有限公司 Method for comprehensively extracting forsythin, forsythoside, rutin and polysaccharide from forsythia leaves and application of method

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Publication number Priority date Publication date Assignee Title
CN1452973A (en) * 2003-05-23 2003-11-05 陕西师范大学 Orally taken antioxidant and antilipemic medicine
CN101537046A (en) * 2008-03-21 2009-09-23 河南大学 Blood lipid-lowing active fractions of forsythia suspensa and preparation method and use of same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1452973A (en) * 2003-05-23 2003-11-05 陕西师范大学 Orally taken antioxidant and antilipemic medicine
CN101537046A (en) * 2008-03-21 2009-09-23 河南大学 Blood lipid-lowing active fractions of forsythia suspensa and preparation method and use of same

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022048529A1 (en) * 2020-09-04 2022-03-10 大连富生天然药物开发有限公司 Forsythiae fructus component and optional ginseng component, and use thereof
CN117229338A (en) * 2023-11-13 2023-12-15 中泰(天津)生物科技有限公司 Method for comprehensively extracting forsythin, forsythoside, rutin and polysaccharide from forsythia leaves and application of method
CN117229338B (en) * 2023-11-13 2024-03-08 中泰(天津)生物科技有限公司 Method for comprehensively extracting forsythin, forsythoside, rutin and polysaccharide from forsythia leaves and application of method

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