CN1252285A - Preparation of AIDS resisting medicine from indian stringbush root extract - Google Patents
Preparation of AIDS resisting medicine from indian stringbush root extract Download PDFInfo
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- CN1252285A CN1252285A CN 98114403 CN98114403A CN1252285A CN 1252285 A CN1252285 A CN 1252285A CN 98114403 CN98114403 CN 98114403 CN 98114403 A CN98114403 A CN 98114403A CN 1252285 A CN1252285 A CN 1252285A
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- radix wikstroemae
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Abstract
The extract of Wikstroemia indica is used as main material in preparing various AIDS-treating preparations. The said extract is prepared through one or several extraction processes of solvent extraction process, reversed phase column chromatographic process, etc. and in combination with conventional concentration drying process. The extract is used as AIDS-resisting active component in preparing oral medicine, injecta and external-use medicine for treating AIDS and various complications.
Description
The present invention relates to medical technical field, exactly it is the preparation method of AIDS resisting (AIDS) new drug Radix Wikstroemae extract.
Radix Wikstroemae (Wikstroemia indica) is a Rui Xiang Ke flower plant, is born in the shrubbery of the foot of the hill and hillside humidity, mainly is distributed in ground such as Guangdong, Guangxi, Fujian, Taiwan, Zhejiang, Jiangxi, Hunan, Sichuan.This stem leaves of plants, root and fruit all can be used as medicine, and have the effect of heat-clearing and toxic substances removing, dispersing swelling and dissipating binds, pain relieving, control carbuncle, rheumatalgia, traumatic injury [the new medical college in Jiangsu is compiled Chinese medicine voluminous dictionary (1977, the Shanghai People's Press), pp.51-53] .Among the people, normal and other Chinese herbal medicine compatibilities of Radix Wikstroemae are widely used in kinds of tumors [Wang Bing chief editor, Chinese medicine medicine for preventing Fang Xuan (1992, the People's Medical Officer Press), pp.16-17] such as treatment pulmonary carcinoma, cervical cancer, breast carcinoma, lymphatic cancer.Yet up to now, research to Radix Wikstroemae is less, be more common in the chemical constituent report, the rarely seen inhibition of activity research mice body endolymph cancer P-338 tumor strain effect [Kato et al., J.Nat.Prod., 1979,42:159-162] and PKC enzyme inhibition [Ko et al., Biochem.J., 1993,295:321-327; Wang et al., Euro.J.Pharm., 1995,288:341-348; Chen et al., Biochem.Pharm., 1996,52:1025-1032] .In addition, do not see any report about AIDS resisting (AIDS) or HIV (human immunodeficiency virus) HIV-1 and HIV-2.AIDS is the very high and extremely refractory disease of a kind of infectiousness, also finds no the report of the higher medicine of cure rate at present both at home and abroad.The inventor is upon the look in medical herbs AIDS resisting (AIDS) the active component process, find that Radix Wikstroemae extract has good AIDS resisting (AIDS) activity, and therefrom obtain a plurality of chemical compounds with multiple framework types such as the active dicoumarol of AIDS resisting (AIDS), lignanoid, flavone, flavonoid glycoside and bisflavones.
The objective of the invention is to systematically study AIDS resisting (AIDS) active component of Radix Wikstroemae, searching obtains AIDS resisting (AIDS) effective site, the new purposes of exploitation Radix Wikstroemae AIDS resisting (AIDS), a kind of AIDS resisting new drug Radix Wikstroemae extract is provided, and simple and practical process route is provided.
The present invention is achieved in that herb, root, stem and leaf or the fruit with Radix Wikstroemae (Wikstroemia indica) is raw material, adopt one or more technologies in the technologies such as solvent extraction method, solvent extraction, resin adsorption method, polyamide adsorpting column chromatography method, normal phase column chromatography, reversed-phase column chromatography, and be prepared into Radix Wikstroemae extract in conjunction with conventional drying method such as concentrate drying, lyophilization, spray dryinges.With the Radix Wikstroemae extract made as AIDS resisting (AIDS) active component, make it to combine and make dosage forms such as powder, granule, tablet, capsule, pill, suppository, enteric agents, injection, syrup, Emulsion, suspensoid, tincture, unguentum, spray, be used for the treatment of and comprise by HIV-1 and HIV-2 virus and other viral AIDS that causes (AIDS) and various complication thereof according to conventional method with suitable excipient.
Plant material Radix Wikstroemae (Wikstroemia indica) can be a herb, also can be root, stem and leaf or fruit.Raw material can be fresh collection, also can be through concocting.
The chemical compound that comprises wherein contained various types of coumarins, dicoumarol, lignanoid, flavone, flavonoid glycoside, bisflavone and other framework types as the Radix Wikstroemae extract of AIDS resisting (AIDS) active component.
In the solvent extraction method that is adopted, a kind of solvent in optional water, methanol, ethanol or other lower aliphatic alcohols, the also mixed solvent that can be formed with arbitrary proportion with any two or more solvents wherein, at room temperature soak into extraction or, perhaps under heated condition, soak into extraction or reflux, extract, with supersonic oscillations instrument supersound extract.Extraction time can be once also can be repeatedly.
In the solvent extraction that is adopted, a kind of solvent in water or lower aliphatic alcohols or mixed solvent can be extracted and the extract mixture through being obtained is suspended from the water, directly extract with in ethyl acetate, n-butyl alcohol, aquifer ethyl or the moisture n-butyl alcohol one or more.Perhaps after low polarity solvent (as petroleum ether) defat, one or more in reuse ethyl acetate, n-butyl alcohol, aquifer ethyl or the moisture n-butyl alcohol extract.Extraction times can be once also can be repeatedly.
In the resin adsorption method that is adopted, resin can be selected the adsorbent resin of D-101 type adsorbent resin, XAD-2 type adsorbent resin, CHP-20P adsorbent resin and other types for use, one or more in eluting solvent methanol, ethanol, acetone, aqueous methanol, aquiferous ethanol or the aqueous acetone.Can the isoconcentration eluting during eluting, also can gradient elution.
The eluting solvent is with methanol or aqueous acetone in the polyamide adsorpting column chromatography method that is adopted.Can the isoconcentration eluting during eluting, also can gradient elution.
In the normal phase column chromatography that is adopted, can select normal pressure or pressurized silica gel column chromatography for use, the optional column chromatography silica gel of used column packing, perhaps thin layer chromatography silica gel, eluant can be selected one or more in benzene/acetone, dichloromethane/acetone, chloroform/acetone, methylene chloride, chloroform/methanol, ethyl acetate/methanol, benzene/acetone, dichloromethane/acetone, chloroform/acetone, methylene chloride/water, chloroform/methanol or the ethyl acetate/methanol/water etc. for use.Can the isoconcentration eluting during eluting, also can gradient elution.
The reversed-phase column chromatography that is adopted can be selected normal pressure or pressurization reversed phase column chromatography for use, the optional octadecyl bonding of used column packing phase (ODS) or eight alkyl linked phases, and eluant is with aqueous methanol or contain water-acetonitrile.Can the isoconcentration eluting during eluting, also can gradient elution.
The drying means that is adopted comprises conventional drying method such as concentrate drying, lyophilization, spray drying.
As AIDS resisting (AIDS) active component, the consumption of Radix Wikstroemae extract is adult 1～1000mg every day, preferred 30～800mg/ days, takes every day 2～3 times.
Oral administration can be made into common formulations such as tablet, powder, granule, capsule, needs a kind of excipient at least, as starch, lactose, sucrose, mannose, hydroxy methocel etc., but tablet coating also.Except that these excipient, also can use magnesium stearate, sodium laurylsulfate, Pulvis Talci etc. as lubricant, dextrin, crystalline cellulose, polyvinylpyrrolidone, arabic gum, corn starch, gelatin etc. are as binding agent, and potato starch, hydroxy methocel are as disintegrating agent.In addition, also can be made into syrup, Emulsion, suspensoid etc.For these dosage forms, can add correctives, flavoring agent or coloring agent etc.
Exterior-applied formulation comprises suppository, ointment, external pulvis, spray, enema, Emulsion or the like.Here employed solid or liquid additive are often using in the art.For ointment, select the additive of the hydrophobic base formed by water, fat, fatty oil, lanoline, vaseline, glycerol, Cera Flava, paraffin, liquid paraffin, resin, higher alcohol, plastics, surfactant or hydrophilic matrix (comprising Emulsion substrate, water-soluble base suspended substrate) etc. for use.
When making injection, generally use distilled water for injection, normal saline, D/W, injection vegetable oil, propylene glycol, Polyethylene Glycol etc.In case of necessity, also can add suitable isotonic agent, cosolvent, antioxidant, antiseptic etc.
Advantage of the present invention is: for the Radix Wikstroemae plant provides new purposes, and features simple and practical process, the AIDS resisting curative effect is better, and has no side effect.
Below in conjunction with embodiment the present invention is done further detailed description.
Embodiment:
1, solvent extraction method/solvent extraction share and extracts the preparation Radix Wikstroemae extract
Radix Wikstroemae 1.2kg refluxes down at 90 ℃ with 90% ethanol (101 * 3), merge extractive liquid,, concentrate ethanol extraction.Ethanol extraction is suspended in the water, uses ethyl acetate extraction, can obtain Radix Wikstroemae extract through concentrate drying, yield is 6.6%.
2, the vitro inhibition HIV-1 of Radix Wikstroemae extract virus experiment
The XTT method is adopted in the vitro inhibition HIV-1 virus experiment of Radix Wikstroemae extract.1% DMSO specimen solution mixes on 96 orifice plates with the T4 lymphocyte of the isopyknic HIV-1 of infecing virus (CEM cell line) and dilutes successively with the 10 times of amounts in every hole, is cultivating 6 days in the PRMI-1640 culture medium that contains 10% calf serum (FCS) and 50 μ g/ml gentamicin under 37 ℃.1% DMSO specimen solution mixes with T4 lymphocyte (CEMcellline) liquid of isopyknic not infected by HIV-1 virus, cultivates in contrast under identical condition of culture.After cultivating in 6 days, every hole adds XTT, by microscopic examination existence cell number and estimate cell protection activity, and is calculated the IC of specimen by matched group
50, EC
50And TI
50(IC
50/ EC
50).The result shows, the IC of Radix Wikstroemae extract
50, EC
50And TI
50(IC
50/ EC
50) value is respectively 130 μ g/ml, 0.25 μ g/ml and 520.
3, Radix Wikstroemae extract 50g mixes with microcrystalline Cellulose 45g and magnesium stearate 5g, and mixture breaks into Ф 6mm with single punch tablet machine, the tablet of weight 300mg.Every contains Radix Wikstroemae extract 150mg in this tablet.In conjunction with symptom.Each 1～2 time, obey every day 2～3 times.
4, Radix Wikstroemae extract 10g mixes with corn starch 40g, adds water and makes soft material, crosses 12 mesh sieve pelletizes, and drying gets granule.In this granule, contain Radix Wikstroemae extract 100mg among every 500mg.In conjunction with symptom, each 0.5～1.0g takes 2～3 every day.
5, Radix Wikstroemae extract 80g and lactose 110g, magnesium stearate 10g mixes, with every 600mg filled capsules.In this capsule, each capsule contains Radix Wikstroemae extract 150mg.In conjunction with symptom, each 1～2, take every day 2～3 times.
6, Radix Wikstroemae extract 30g adds water 300ml dissolving, adds hesperidin 4ml, adds simple syrup and gets syrup to 100ml.Contain Radix Wikstroemae extract 30mg among this syrup 1ml.In conjunction with symptom, each 6～10ml takes 2～3 every day.
7, Radix Wikstroemae extract 50g mixes with microcrystalline Cellulose 90g and magnesium stearate 10g, and mixture breaks into the tablet of Ф 6mm with single punch tablet machine, and with CAP thin film bag table, makes the enteric coated preparation of weight 300mg.Every contains Radix Wikstroemae extract 100mg in this prescription.In conjunction with symptom, each 2～3, take every day 2～3 times.
8, Radix Wikstroemae extract 40g mixes with lactose 100g, magnesium stearate 10g, fills enteric coated capsule with every 600mg.In this enteric coated capsule, each capsule contains Radix Wikstroemae extract 160mg.In conjunction with symptom, each 1～2, take every day 2～3 times.
9, Radix Wikstroemae extract 25g dissolves with the distilled water for injection 1000ml that is heated to 60 ℃ with normal injection agent autofrettage, reconciles to wait with NaCl and opens, and encloses and pacifies bottle.Contain Radix Wikstroemae extract 250mg among this injection 10ml.In conjunction with symptom, each intramuscular injection 10ml injects 2～3 every day.
Claims (11)
1, the preparation method that a kind of AIDS resisting (AIDS) new drug Radix Wikstroemae extracts, it is characterized in that: (Wikstroemia indica) is raw material with Radix Wikstroemae, adopt solvent extraction method, solvent extraction, resin adsorption method, polyamide adsorpting column chromatography method, the normal phase column chromatography, one or more technologies in the technologies such as reversed-phase column chromatography, and in conjunction with concentrate drying, lyophilization, conventional drying method such as spray drying are prepared into Radix Wikstroemae extract, with the Radix Wikstroemae extract made as AIDS resisting (AIDS) active component, make it to combine with suitable excipient, the interior injection and the exterior-applied formulation with dosage form and non-oral administration of the oral administration of making according to conventional method used in AIDS (AIDS) and the treatment of various complication thereof.
2, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: plant material Radix Wikstroemae (Wikstroemia indica) can be a herb, also can be root, stem and leaf or fruit, raw material can be fresh collection, also can be through concocting.
3, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract is characterized in that: the chemical compound that comprises wherein contained various types of coumarins, dicoumarol, lignanoid, flavone, flavonoid glycoside, bisflavone and other framework types as the Radix Wikstroemae extract of anticancer active constituent.
4, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: in the solvent extraction method that is adopted, a kind of solvent in optional water, methanol, ethanol or other lower aliphatic alcohols, the mixed solvent that also can select for use any two or more solvents wherein to be formed with arbitrary proportion, at room temperature soak into to extract or with supersonic oscillations instrument supersound extract, perhaps under heated condition, soak into and extract or reflux, extract,, extraction time can be once also can be repeatedly.
5, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: in the solvent extraction that is adopted, a kind of solvent in water or lower aliphatic alcohols or mixed solvent can be extracted and the extract mixture through being obtained is suspended from the water, directly extract with in ethyl acetate, n-butyl alcohol, aquifer ethyl or the moisture n-butyl alcohol one or more.Perhaps after low polarity solvent (as petroleum ether) defat, one or more in reuse ethyl acetate, n-butyl alcohol, aquifer ethyl or the moisture n-butyl alcohol extract, and extraction times can be once also can be repeatedly.
6, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: in the resin adsorption method that is adopted, resin can be selected the adsorbent resin of D-101 type adsorbent resin, XAD-2 type adsorbent resin, CHP-20P adsorbent resin and other types for use, one or more in eluting solvent methanol, ethanol, acetone, aqueous methanol, aquiferous ethanol or the aqueous acetone.Can the isoconcentration eluting during eluting, also can gradient elution.
7, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract is characterized in that: the eluting solvent is with methanol or aqueous acetone in the polyamide adsorpting column chromatography method that is adopted.Can the isoconcentration eluting during eluting, also can gradient elution.
8, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: in the normal phase column chromatography that is adopted, can select normal pressure or pressurized silica gel column chromatography for use, the optional column chromatography silica gel of used column packing, perhaps thin layer chromatography silica gel, eluant can be selected benzene/acetone for use, dichloromethane/acetone, chloroform/acetone, methylene chloride, chloroform/methanol, ethyl acetate/methanol, benzene/acetone, dichloromethane/acetone, chloroform/acetone, methylene chloride/water, in chloroform/methanol or the ethyl acetate/methanol/water etc. one or more.Can the isoconcentration eluting during eluting, also can gradient elution.
9, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: the reversed-phase column chromatography that is adopted, can select normal pressure or pressurization reversed phase column chromatography for use, the optional octadecyl bonding of used column packing phase (ODS) or eight alkyl linked phases, eluant is with aqueous methanol or contain water-acetonitrile, can the isoconcentration eluting during eluting, also can gradient elution.
10, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract is characterized in that: distill the spissated organic solvent that reclaims simultaneously.
11, the preparation method of a kind of AIDS resisting as claimed in claim 1 (AIDS) new drug Radix Wikstroemae extract, it is characterized in that: made preparation comprises following dosage form: powder, granule, tablet, capsule, pill, suppository, enteric agents, injection, syrup, Emulsion, suspensoid, tincture, unguentum, spray.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB981144039A CN1181832C (en) | 1998-10-23 | 1998-10-23 | Preparation of AIDS resisting medicine from indian stringbush root extract |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB981144039A CN1181832C (en) | 1998-10-23 | 1998-10-23 | Preparation of AIDS resisting medicine from indian stringbush root extract |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1252285A true CN1252285A (en) | 2000-05-10 |
| CN1181832C CN1181832C (en) | 2004-12-29 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB981144039A Expired - Fee Related CN1181832C (en) | 1998-10-23 | 1998-10-23 | Preparation of AIDS resisting medicine from indian stringbush root extract |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006012779A1 (en) * | 2004-08-06 | 2006-02-09 | Nihon University | Wikstroemia indeca extract their production and use in the production of anti-inflammatory pharmaceutical |
| CN100463906C (en) * | 2007-03-07 | 2009-02-25 | 哈尔滨医科大学附属第二医院 | Extraction method for extraction and pharmaceutical containing the same |
| CN102000215A (en) * | 2010-12-03 | 2011-04-06 | 沈阳药科大学 | Method for preparing total lignans of Indian stringbush root |
| CN101601666B (en) * | 2009-07-10 | 2011-05-25 | 暨南大学 | Radix wikstroemae extractive and preparation method and application thereof |
| CN109512901A (en) * | 2018-12-31 | 2019-03-26 | 广东罗浮山国药股份有限公司 | Radix Wikstroemae extract and its preparing the application in antalgic and inflammation relieving drug |
| CN110538243A (en) * | 2018-05-29 | 2019-12-06 | 复旦大学 | Preparation method of active total diterpene in Thymelaeaceae plant and application thereof in pharmacy |
-
1998
- 1998-10-23 CN CNB981144039A patent/CN1181832C/en not_active Expired - Fee Related
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006012779A1 (en) * | 2004-08-06 | 2006-02-09 | Nihon University | Wikstroemia indeca extract their production and use in the production of anti-inflammatory pharmaceutical |
| CN101014560B (en) * | 2004-08-06 | 2010-04-28 | 学校法人日本大学 | Wikstroemia indeca extract, their production and use in the production of anti-inflammatory pharmaceutical |
| CN100463906C (en) * | 2007-03-07 | 2009-02-25 | 哈尔滨医科大学附属第二医院 | Extraction method for extraction and pharmaceutical containing the same |
| CN101601666B (en) * | 2009-07-10 | 2011-05-25 | 暨南大学 | Radix wikstroemae extractive and preparation method and application thereof |
| CN102000215A (en) * | 2010-12-03 | 2011-04-06 | 沈阳药科大学 | Method for preparing total lignans of Indian stringbush root |
| CN102000215B (en) * | 2010-12-03 | 2012-08-29 | 沈阳药科大学 | Method for preparing total lignans of Indian stringbush root |
| CN110538243A (en) * | 2018-05-29 | 2019-12-06 | 复旦大学 | Preparation method of active total diterpene in Thymelaeaceae plant and application thereof in pharmacy |
| CN109512901A (en) * | 2018-12-31 | 2019-03-26 | 广东罗浮山国药股份有限公司 | Radix Wikstroemae extract and its preparing the application in antalgic and inflammation relieving drug |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1181832C (en) | 2004-12-29 |
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