CN106075292A - A kind of curcumenol preparation treating hepatic fibrosis and preparation method thereof - Google Patents

A kind of curcumenol preparation treating hepatic fibrosis and preparation method thereof Download PDF

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CN106075292A
CN106075292A CN201610518481.4A CN201610518481A CN106075292A CN 106075292 A CN106075292 A CN 106075292A CN 201610518481 A CN201610518481 A CN 201610518481A CN 106075292 A CN106075292 A CN 106075292A
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radix
curcumenol
preparation
hepatic fibrosis
treating hepatic
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赵铁建
彭岳
段雪琳
黎桂玉
马静
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Guangxi University of Chinese Medicine
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Guangxi University of Chinese Medicine
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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    • A61K36/88—Liliopsida (monocotyledons)
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    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
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    • A61K36/18—Magnoliophyta (angiosperms)
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    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258—Panax (ginseng)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/484—Glycyrrhiza (licorice)
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    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
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    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/70—Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/708—Rheum (rhubarb)
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/71—Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
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    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
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    • A61K2236/30—Extraction of the material
    • A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
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    • A61K2236/50—Methods involving additional extraction steps
    • A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
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    • A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50—Methods involving additional extraction steps
    • A61K2236/55—Liquid-liquid separation; Phase separation

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Abstract

A kind of curcumenol preparation treating hepatic fibrosis and preparation method thereof, the present invention relates to treating liver fibrosis technical field；It comprises following weight constituent: Rhizoma Curcumae 10 20g, Rhizoma Sparganii 6 15g, Radix Et Rhizoma Rhei 6 15g, worm 15 25g, Carapax Trionycis 15 25g, Radix Glycyrrhizae 6 15g, Radix Ginseng 4 8g, Radix Angelicae Sinensis 6 15g, the Radix Paeoniae Alba 3 6g, Radix Bupleuri 6 15g, Oleum Curcumae 80 120g.No side effects, determined curative effect, fill up the shortage of existing anti-hepatic fibrosis medicines with not enough.

Description

A kind of curcumenol preparation treating hepatic fibrosis and preparation method thereof
Technical field
The present invention relates to treating liver fibrosis technical field, be specifically related to a kind of curcumenol preparation treating hepatic fibrosis and Its preparation method.
Background technology
Hepatic fibrosis is a pathophysiological process, refers to be increased by connective tissue in liver caused by various virulence factors is abnormal Raw.Any hepar damnification has the process of hepatic fibrosis during liver healing, if impairment factor for a long time can not Removing, Fibrotic process the most persistently will develop into liver cirrhosis.Therefore it is not an independent disease.
The prevention of existing hepatic fibrosis generally individually uses medicine to carry out with treatment, and " being three points of poison of medicine ", and be unfavorable for Patient's long-term taking, needs improvement badly.
Summary of the invention
Present invention aims to defect and the deficiency of prior art, it is provided that one is reasonable in design, technique is simple Curcumenol preparation for the treatment of hepatic fibrosis and preparation method thereof, no side effects, determined curative effect, fill up existing anti-hepatic fibrosis The shortage of medicine is with not enough.
For achieving the above object, the technical solution used in the present invention is: it comprises following weight constituent: Rhizoma Sparganii 6- 15g, Radix Et Rhizoma Rhei 6-15g, worm (Eupolyphaga Seu Steleophaga) 15-25g, Carapax Trionycis 15-25g, Radix Glycyrrhizae 6-15g, Radix Ginseng 4-8g, Radix Angelicae Sinensis 6-15g, the Radix Paeoniae Alba 3-6g, Radix Bupleuri 6-15g, Oleum Curcumae 80-120g.
Further, it comprises following weight constituent: Rhizoma Sparganii 10-15g, Radix Et Rhizoma Rhei 10-15g, worm 18-25g, Carapax Trionycis 18-25g, Radix Glycyrrhizae 10-15g, Radix Ginseng 5-8g, Radix Angelicae Sinensis 10-15g, Radix Paeoniae Alba 4-6g, Radix Bupleuri 10-15g, Oleum Curcumae 90-120g.
The processing technology of the present invention is as follows:
1, the preparation of Chinese medicine ultrafiltrate: (use ultrafiltrate method prepare Chinese medical concrete) select Rhizoma Sparganii 6-15g, Radix Et Rhizoma Rhei 6-15g, Worm (Eupolyphaga Seu Steleophaga) 15-25g, Carapax Trionycis 15-25g, Radix Glycyrrhizae 6-15g, Radix Ginseng 4-8g, Radix Angelicae Sinensis 6-15g, Radix Paeoniae Alba 3-6g, Radix Bupleuri 6- 15g, adds the water of 8～10 times of above-mentioned Chinese crude drug amounts, is heated to 100 DEG C, and the time is 1～2h, centrifuge separation medicinal residues, extracts Supernatant, then repeat to extract once with method, obtain extracting solution, at the beginning of carrying out in the filter that filter membrane aperture is 0.1～0.5 μm Filter, it is 3kg/cm that first filtrate is placed in pressure2Ultrafilter in ultrafiltration, obtain Chinese medicine ultrafiltrate, standby；
2, the preparation of curcumenol: from Oleum Curcumae isolated and purified go out curcumenol (in Oleum Curcumae containing 70% curcumenol):
2.1, silica gel column chromatography separates: take Oleum Curcumae 80-120g, mixes in 50g silica gel for chromatography, loads chromatographic column In, utilize petroleum ether (60～90 DEG C)-ethyl acetate (90: 10) eluting to obtain 45 parts, every part of eluent is all checked by thin layer, its In the 21st～45 part of eluent composition consistent, merged concentration；
2.2, weight crystalline substance purifies: after concentrated solution cold preservation (4～8 DEG C) to 6d, separates out crystal, and leaching crystallizes, the anhydrous second of frost Alcohol rinses crystallization, is recycled in stock solution by flushing liquor, and dehydrated alcohol is recrystallized to give curcumenol crystal, and (curcumenol purity reaches 90% Above)；
3, curcumenol ointment is prepared: gained curcumenol crystal and Chinese medicine ultrafiltrate are fully dissolved mixing, then at 40～50 ° Lower concentrating under reduced pressure becomes ointment；
4, curcumenol preparation is prepared: by above-mentioned ointment lyophilization (-5～-10 DEG C) 1d, obtain the dry paste formulation of medicine, according to Need to make different peroral dosage forms.
The drug particles prepared in described step 4 adds lubricant, filler, binding agent, disintegrating agent, preservative, rectifys Taste agent mix homogeneously.
The present invention can be prepared as the peroral dosage form of various needs neatly according to Western medicine preparation method, including pill, tablet, Capsule, granule etc., preferably pill.
Present invention have the beneficial effect that a kind of curcumenol preparation treating hepatic fibrosis of the present invention and preparation side thereof Method, no side effects, determined curative effect, fill up shortage and the deficiency of existing anti-hepatic fibrosis medicines, the present invention has structure letter Single, arrange rationally, the advantages such as cost of manufacture is low.
Detailed description of the invention
This detailed description of the invention (embodiment one) the technical scheme is that it comprises following weight constituent: Rhizoma Sparganii 10g, Radix Et Rhizoma Rhei 10g, worm (Eupolyphaga Seu Steleophaga) 20g, Carapax Trionycis 20g, Radix Glycyrrhizae 10g, Radix Ginseng 6g, Radix Angelicae Sinensis 10g, Radix Paeoniae Alba 5g, Radix Bupleuri 10g, cowherb Art oil 100g.
The processing technology of the present invention is as follows:
1, the preparation of Chinese medicine ultrafiltrate: (using ultrafiltrate method to prepare Chinese medical concrete) selects Rhizoma Sparganii 10g, Radix Et Rhizoma Rhei 10g, worm (Eupolyphaga Seu Steleophaga) 20g, Carapax Trionycis 20g, Radix Glycyrrhizae 10g, Radix Ginseng 6g, Radix Angelicae Sinensis 10g, Radix Paeoniae Alba 5g, Radix Bupleuri 10g, add 8 times of above-mentioned Chinese crude drugs The water of amount, is heated to 100 DEG C, and the time is 1h, centrifuge separation medicinal residues, extracts supernatant, then repeats to extract once with method, must carry Taking liquid, carry out initial filter in the filter that filter membrane aperture is 0.1 μm, it is 3kg/cm that first filtrate is placed in pressure2Ultrafilter Middle ultrafiltration, obtains Chinese medicine ultrafiltrate, standby；
2, the preparation of curcumenol: from Oleum Curcumae isolated and purified go out curcumenol (in Oleum Curcumae containing 70% curcumenol):
2.1, silica gel column chromatography separates: take Oleum Curcumae 100g, mixes in 50g silica gel for chromatography, loads in chromatographic column, profit Obtaining 45 parts with petroleum ether (60 DEG C)-ethyl acetate (90: 10) eluting, every part of eluent is all checked by thin layer, wherein the 21st～ 45 parts of eluent compositions are consistent, merged concentration；
2.2, weight crystalline substance purifies: after concentrated solution cold preservation (4 DEG C) to 6d, separates out crystal, and leaching crystallizes, the dehydrated alcohol punching of frost Wash crystallization, flushing liquor be recycled in stock solution, dehydrated alcohol be recrystallized to give curcumenol crystal (curcumenol purity reach 90% with On)；
3, curcumenol ointment is prepared: gained curcumenol crystal and Chinese medicine ultrafiltrate are fully dissolved mixing, then at 40～50 ° Lower concentrating under reduced pressure becomes ointment；
4, curcumenol preparation is prepared: by above-mentioned ointment lyophilization (-5 DEG C) 1d, obtain the dry paste formulation of medicine, by dry for medicine cream Preparation adds methylcellulose, lactose, crospolyvinylpyrrolidone, calcium stearate, xylitol mixing after being ground into coarse powder, i.e. Obtain granule.
This detailed description of the invention has the beneficial effect that a kind of curcumenol treating hepatic fibrosis described in this detailed description of the invention Preparation and preparation method thereof, no side effects, determined curative effect, fill up shortage and the deficiency of existing anti-hepatic fibrosis medicines, this Invention has simple in construction, arranges rationally, the advantages such as cost of manufacture is low.
Embodiment two:
The present embodiment the technical scheme is that it comprises following weight constituent: Rhizoma Sparganii 10g, Radix Et Rhizoma Rhei 12g, worm (Eupolyphaga Seu Steleophaga) 15g, Carapax Trionycis 15g, Radix Glycyrrhizae 8g, Radix Ginseng 6g, Radix Angelicae Sinensis 12g, Radix Paeoniae Alba 4g, Radix Bupleuri 8g, Oleum Curcumae 90g.
The processing technology of the present invention is as follows:
1, the preparation of Chinese medicine ultrafiltrate: (using ultrafiltrate method to prepare Chinese medical concrete) selects Rhizoma Sparganii 10g, Radix Et Rhizoma Rhei 12g, worm (Eupolyphaga Seu Steleophaga) 15g, Carapax Trionycis 15g, Radix Glycyrrhizae 8g, Radix Ginseng 6g, Radix Angelicae Sinensis 12g, Radix Paeoniae Alba 4g, Radix Bupleuri 8g, add 9 times of above-mentioned Chinese crude drug amounts Water, be heated to 100 DEG C, the time is 1h, centrifuge separation medicinal residues, extracts supernatant, then repeats to extract once with method, obtains extraction Liquid, carries out initial filter in the filter that filter membrane aperture is 0.4 μm, and it is 3kg/cm that first filtrate is placed in pressure2Ultrafilter in Ultrafiltration, obtains Chinese medicine ultrafiltrate, standby；
2, the preparation of curcumenol: from Oleum Curcumae isolated and purified go out curcumenol (in Oleum Curcumae containing 70% curcumenol):
2.1, silica gel column chromatography separates: take Oleum Curcumae 90g, mixes in 50g silica gel for chromatography, loads in chromatographic column, profit Obtaining 45 parts with petroleum ether (80 DEG C)-ethyl acetate (90: 10) eluting, every part of eluent is all checked by thin layer, wherein the 21st～ 45 parts of eluent compositions are consistent, merged concentration；
2.2, weight crystalline substance purifies: after concentrated solution cold preservation (4 DEG C) to 6d, separates out crystal, and leaching crystallizes, the dehydrated alcohol punching of frost Wash crystallization, flushing liquor be recycled in stock solution, dehydrated alcohol be recrystallized to give curcumenol crystal (curcumenol purity reach 90% with On)；
3, curcumenol ointment is prepared: gained curcumenol crystal and Chinese medicine ultrafiltrate are fully dissolved mixing, then at 40～50 ° Lower concentrating under reduced pressure becomes ointment；
4, prepare curcumenol preparation: by 10% lyophilization (-8 DEG C) 1d in above-mentioned ointment, be ground into medicated powder, add first Base cellulose, lactose, crospolyvinylpyrrolidone, calcium stearate, xylitol mix, and obtain powder, by remaining 90% ointment Send in pellet processing machine and make pill, more obtained pill is put in above-mentioned powder hit tight, round as a ball, finally by the medicine after round as a ball Ball sends into oven drying (90 DEG C, 10-20h), obtains pill.
The above, only in order to technical scheme to be described and unrestricted, those of ordinary skill in the art are to this Other amendment or equivalent that bright technical scheme is made, without departing from the spirit and scope of technical solution of the present invention, All should contain in the middle of scope of the presently claimed invention.

Claims (4)

1. the curcumenol preparation treating hepatic fibrosis, it is characterised in that: it comprises following weight constituent: Rhizoma Sparganii 6- 15g, Radix Et Rhizoma Rhei 6-15g, worm 15-25g, Carapax Trionycis 15-25g, Radix Glycyrrhizae 6-15g, Radix Ginseng 4-8g, Radix Angelicae Sinensis 6-15g, Radix Paeoniae Alba 3-6g, bavin 6-15g, Oleum Curcumae 80-120g recklessly.
2. the preparation method treating hepatic fibrosis, it is characterised in that: its processing technology is as follows:
(1), the preparation of Chinese medicine ultrafiltrate: select Rhizoma Sparganii 6-15g, Radix Et Rhizoma Rhei 6-15g, worm 15-25g, Carapax Trionycis 15-25g, Radix Glycyrrhizae 6- 15g, Radix Ginseng 4-8g, Radix Angelicae Sinensis 6-15g, Radix Paeoniae Alba 3-6g, Radix Bupleuri 6-15g, the water of 8～10 times of above-mentioned Chinese crude drug amounts of addition, heating To 100 DEG C, the time is 1～2h, centrifuge separation medicinal residues, extracts supernatant, then repeats to extract once with method, obtains extracting solution, in Filter membrane aperture be 0.1～0.5 μm filter in carry out initial filter, it is 3kg/cm that first filtrate is placed in pressure2Ultrafilter in Ultrafiltration, obtains Chinese medicine ultrafiltrate, standby；
(2), the preparation of curcumenol: from Oleum Curcumae isolated and purified go out curcumenol:
(2.1), silica gel column chromatography separates: takes Oleum Curcumae 80-120g, mixes in 50g silica gel for chromatography, loads in chromatographic column, Utilizing petroleum ether 60～90 DEG C-ethyl acetate 90: 10 eluting to obtain 45 parts, every part of eluent is all checked by thin layer, wherein the 21st ～45 parts of eluent compositions are consistent, merged concentration；
(2.2), weight crystalline substance purifies: after concentrated solution cold preservation 4～8 DEG C to 6d, separating out crystal, leaching crystallizes, the dehydrated alcohol punching of frost Washing crystallization, be recycled in stock solution by flushing liquor, dehydrated alcohol is recrystallized to give curcumenol crystal；
(3), curcumenol ointment is prepared: gained curcumenol crystal and Chinese medicine ultrafiltrate are fully dissolved mixing, then under 40～50 ° Concentrating under reduced pressure becomes ointment；
(4), curcumenol preparation is prepared: by above-mentioned ointment lyophilization-5～-10 DEG C, 1d, obtain the dry paste formulation of medicine, as required Make different peroral dosage forms.
A kind of curcumenol preparation treating hepatic fibrosis the most according to claim 1, it is characterised in that: it comprises following weight Amount constituent: Rhizoma Sparganii 10-15g, Radix Et Rhizoma Rhei 10-15g, worm 18-25g, Carapax Trionycis 18-25g, Radix Glycyrrhizae 10-15g, Radix Ginseng 5-8g, when Return 10-15g, Radix Paeoniae Alba 4-6g, Radix Bupleuri 10-15g, Oleum Curcumae 90-120g.
A kind of curcumenol preparation treating hepatic fibrosis the most according to claim 2 and preparation method thereof, it is characterised in that: In the drug particles prepared in described step (4), addition lubricant, filler, binding agent, disintegrating agent, preservative, correctives mix Close uniformly.
CN201610518481.4A 2016-07-05 2016-07-05 A kind of curcumenol preparation treating hepatic fibrosis and preparation method thereof Pending CN106075292A (en)

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CN110585190A (en) * 2019-08-20 2019-12-20 南方医科大学 Application of curzerene alcohol in preparation of medicine for preventing and treating hepatic fibrosis
CN116327937A (en) * 2022-09-20 2023-06-27 广西中医药大学赛恩斯新医药学院 Application of active ingredient of Zhuang medicine Beijing insect for iron death inducer

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110585190A (en) * 2019-08-20 2019-12-20 南方医科大学 Application of curzerene alcohol in preparation of medicine for preventing and treating hepatic fibrosis
CN110585190B (en) * 2019-08-20 2022-10-04 南方医科大学 Application of curzerene alcohol in preparation of medicine for preventing and treating hepatic fibrosis
CN116327937A (en) * 2022-09-20 2023-06-27 广西中医药大学赛恩斯新医药学院 Application of active ingredient of Zhuang medicine Beijing insect for iron death inducer

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Application publication date: 20161109