CN1304019C - Compound artemisia rupestris capsule - Google Patents

Compound artemisia rupestris capsule Download PDF

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CN1304019C
CN1304019C CNB031379028A CN03137902A CN1304019C CN 1304019 C CN1304019 C CN 1304019C CN B031379028 A CNB031379028 A CN B031379028A CN 03137902 A CN03137902 A CN 03137902A CN 1304019 C CN1304019 C CN 1304019C
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capsule
herba
gram
concentrated
temperature
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CN1454663A (en
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斯拉甫·艾白
哈木拉提·吾甫尔
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Abstract

The present invention relates to a compound capsule for oral administration, which is prepared from ciliate desert-grass for treating viral hepatitis and hepatopathy according to the clinical experience of specialists in traditional Chinese medicine and national medicine for many years. The capsule is mainly prepared from ciliate desert-grass which is matched with Hypericum Perforatum and chicory. In the preparation method of the capsule, the ciliate desert-grass and the Hypericum Perforatum are firstly extracted, concentrated, settled, decompressed and concentrated into extractum; the drug dregs are decocted and filtered after being mixed with the chicory; the filtrate is combined with alcohol extract after being combined and concentrated; talcum powder is added after the combined filtrate is dried by spraying, sieved and baked, and then, the mixture is encapsulated after being uniformly blended and sieved. Indicated by antivirus tests in vivo and in vitro, the capsule has significant effects on treating viral hepatitis, hepatopathy, AIDS, etc., and also has obvious effects on treating viral hepatitis and hepatopathy in clinical application.

Description

The compound Artemisia rupestris capsule
Technical field
The present invention relates to a kind of compound Artemisia rupestris capsule oral medicine, be used for the treatment of the pure Chinese medicine of viral hepatitis and hepatopathy
Background technology
At present both at home and abroad the sickness rate of viral disease increases year by year, and new immunodeficiency such as acquired immune deficiency syndrome (AIDS) occurs.The types of drugs that is used for the treatment of this class disease is divided into two big classes substantially: 1. antiviral agents, and 2. immunomodulator, but himself problem is all arranged, and do not reach the healing purpose.Therefore develop the medicine that antiviral effect is good, side effect is little, make exigence of the world of medicine.
Viral hepatitis is a kind of global commonly encountered diseases, and China belongs to popular " severely afflicated area ".It is predicted that China infects the hepatitis B person and has more than 100,000,000 people; about 3,000 ten thousand people of the undesired patient of liver function that cause by hepatitis B; most in addition liver cancer patients have the chronic hepatitis medical history; the health that is threatening compatriots that various viral hepatitis are just serious is so the treatment of chronic hepatitis becomes a significant problem that urgently needs solution.The types of drugs that is used at present chronic hepatitis treatment both at home and abroad is divided three classes substantially: (1) antiviral agents, mainly contain interferon and several nucleoside analog, this type of medicine after drug withdrawal in about 6 months to 1 year most patients can recur and the medicine is expensive; (2) immunomodulator, as transfer factor, interleukin 1, thymosin etc., this type of Drug therapy chronic hepatitis curative effect waits certainly, and the medicine is expensive and side effect is arranged.(3) improve the liver function medicine, claim hepatoprotective or anti-hepatocyte injury medicine again, as glycyrrhizin, bifendate, silymarin etc., compound glycyrrhizin preparation.
Summary of the invention
The object of the invention is, developed a kind of oral medicine compound Artemisia rupestris capsule for the treatment of viral hepatitis and hepatopathy according to domestic and foreign literature data and the traditional Chinese medical science, national doctor expert clinical experience for many years, this medicine is based on Herba Achilleae, compatibility Herba Hyperici Monogyni, Herba Cichorii and form.Adopt and get Herba Achilleae, Herba Hyperici Monogyni alcohol reflux earlier, be concentrated into thick paste, leave standstill, precipitate, concentrating under reduced pressure is an extractum; Again medicinal residues are mixed with Herba Cichorii, decoct with water, filter, merging filtrate, filtrate decompression concentrates with alcohol-extracted extract and merges, spray drying, and with ethanol system soft material, wet grain is crossed net, and oven dry adds the Talcum grain, mixing, and crossing net can the fill capsule.This capsule is through the inside and outside antivirus test: the result, Herba Achilleae AR is 57.0 ± 22.1% at 5ug/ml to the average suppression ratio of HBV DNA, its IC 50Be 3.4 ± 0.5ug/ml, the lamivudine (3TC) of positive drug 1 μ M is 67.2 ± 16.4% to the suppression ratio of HBV DNA.Simultaneously the active component of Herba Hyperici Monogyni treatment depression, hepatitis and acquired immune deficiency syndrome (AIDS) and aspect tool such as anticancer important utilize prospect.
Compound Artemisia rupestris capsule of the present invention, this capsule be pure Chinese medicine based on Herba Achilleae, Herba Hyperici Monogyni, Herba Cichorii and form, wherein proportioning raw materials is: Herba Achilleae is 6-24 gram, Herba Hyperici Monogyni 3-16 gram, Herba Cichorii 3-18 gram; Get Herba Achilleae earlier, the Herba Hyperici Monogyni alcohol reflux, collecting decoction filters, be concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, temperature is 40~70 ℃ a extractum, again medicinal residues are mixed with Herba Cichorii, decoct with water 3 times, each 1 hour, filter, merging filtrate, filtrate decompression are concentrated into relative density 1.10~1.40, and temperature is 40~70 ℃, merge with alcohol-extracted extract, spray drying, and, cross 12 order nets for wet with 75%--95% ethanol system soft material, oven for drying, temperature is 45 ℃--65 ℃, dry granular adds Pulvis Talci, mixing in the 1%--2% ratio, cross 14 order wire gauzes, can the fill capsule after semi-finished product inspection is qualified.
A kind of preparation method of compound Artemisia rupestris capsule oral medicine follows these steps to carry out:
A, get Herba Achilleae 6-24 gram, Herba Hyperici Monogyni 3-16 gram, with alcohol reflux 3 times, collecting decoction, filter, be concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, and temperature is 40~70 ℃ a extractum.
B, with medicinal residues and Herba Cichorii 3-18 gram, mix, decoct with water 3 times, each 1 hour, filter merging filtrate, filtrate decompression is concentrated into relative density 1.10~1.40, and temperature is 40~70 ℃, merges with alcohol-extracted extract, spray drying, and, cross 12 order nets for wet with 75%--95% ethanol system soft material, oven for drying, temperature are 45 ℃--65 ℃, dry granular adds the Talcum grain in the 1%--2% ratio, mixing is crossed 14 order wire gauzes, can the fill capsule after semi-finished product inspection is qualified.
A kind of compound Artemisia rupestris capsule oral medicine is at the medicinal usage of preparation viral hepatitis and hepatopathy.This capsule be pure Chinese medicine based on Herba Achilleae, Herba Hyperici Monogyni, Herba Cichorii and form, wherein proportioning raw materials is: Herba Achilleae is 6-24 gram, Herba Hyperici Monogyni 3-16 gram, Herba Cichorii 3-18 gram; Get Herba Achilleae, Herba Hyperici Monogyni alcohol reflux earlier, collecting decoction filters, and is concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, and temperature is 40~70 ℃ a extractum.Again medicinal residues are mixed with Herba Cichorii, decoct with water 3 times, each 1 hour, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.10~1.40, temperature is 40~70 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 75%--95% ethanol system soft material, temperature is 45 ℃--65 ℃, dry granular adds Talcum grain, mixing in the 1%--2% ratio, cross 14 order wire gauzes, get final product the fill capsule after semi-finished product inspection is qualified; This medicine is used to treat the Chinese medicine of preventing and treating the viral hepatitis disease.
Clinical data shows, Herba Achilleae has effects such as detoxifcation, antibiotic, antiviral, the clinical diseases such as hepatitis, flu that are used for; Herba Hyperici Monogyni is the Guttiferae plant, and the exsiccant herb of Herba Hyperici Monogyni has softening cold-damp, and the diuresis of stimulating the menstrual flow is used for cold swelling and ache, urinary obstruction, and lung is unfavorable, lumbago and skelalgia, external application can be controlled burn and arthritis etc.; Herba Cichorii is the Uygur medicine medicinal herbs most in use, and Herba Cichorii (Carson) granule, the inflammation that Drug Standard of Ministry of Public Health of the Peoples Republic of China Uigurs medicine fascicle the is included main medicine that Di Naer syrup etc. is used for the treatment of viral disease that disappears is a Herba Cichorii.
Compound Artemisia rupestris capsule of the present invention, the inside and outside antivirus test of this capsule body is:
Summary: for studying the effect of its anti-hepatitis B virus, this experiment is studied the toxicity of its pair cell and to the excretory inhibition effect of HBV DNA in the Bel7402 2.2.15 of hepatitis B virogene transfection cell.Twice test shows: compound Artemisia rupestris capsule 320ug/ml begins 2 times of dilutions, adds cell culture 8 days, and pair cell median toxic concentration TC50 is 22.4ug/ml, and maximal non-toxic concentration TCO is 5ug/ml.Maximal non-toxic concentration 5ug/ml is 52.4 ± 6.6% to the suppression ratio of HBVDNA.
Material and method
One. medicine: the compound Artemisia rupestris capsule is a chocolate brown powder.Be made into 4 ℃ of preservations of 20mg/ml mother solution with DMSO during experiment, be made into desired concn with the 2.2.15 cell culture fluid during use.
Two .2.2.15 cells: the 2.2.15 cell line of hepatitis B virus (HBV) dna clone transfection human liver cancer cell (Hep G2), U.S. Mount Sinal medical center makes up, the cultivation of going down to posterity voluntarily after introduce my chamber.Cell is with containing hyclone 10%, 3% paddy ammonia phenol amine 1%, G418 380 μ g/ml, and Eagle ' the s MEM culture fluid of kanamycin 50U/ml is cultivated in 37 ℃ of 5%CO2 incubators, and an about week goes down to posterity once.
Three. reagent and instrument: radiosiotope α 32P dCTP is an inferior brightness biomedical engineering company, specific activity: 111TBq/nmol; The scarce day labelling kit that probe mark is used is available from Promerga company.Microplate reader: BIO-RAO 3550 types; γ-calculating instrument is a U.S. DPC company product.
Four. experimental technique:
1. medicine pair cell toxicity test
Medicaments compound Herba Achilleae capsule is a chocolate brown powder, be made into the 20mg/ml mother solution with DMSO, be made into desired concn with the 2.2.15 cell culture fluid during use, add to 2.5ug/ml with the culture fluid two-fold dilution from 320ug/ml then and add 96 porocyte culture plates, every concentration 3 holes, change same concentration liquid in per 4 days, and established no drug cell matched group.With the observation of cell pathological changes is index, 8 days microscopically observation of cell pathological changes, and destroying fully is 4; 75% is 3; 50% is 2; 25% is 1; Anosisly become 0.Calculate every concentration liquid average cell lesion degree and suppress %.Press Reed﹠amp; The Muench method is calculated the poisonous concentration of half (TC50) maximal non-toxic concentration (TC0)
2. medicine is to the inhibition test of HBV DNA
2.2.15 cell conditioned medium liquid each concentration group medicinal liquid and the cell matched group calculates suppression ratio after extracting the A value of its HBV DNA, each sample dot blot hybridization, autoradiography, each hybridization point of measurement by molecular cloning experimental technique method.
3, selection index (SI): SI=TC 50/ IC 50
The result
1. the cytotoxicity of compound Artemisia rupestris capsule in the 2.2.15 cell culture
Be to observe the toxicity of compound Artemisia rupestris capsule to people's hepatocarcinoma 2.2.15 cell of hepatitis B virogene transfection, behind inoculation 2.2.15 cell 24 hours, add two-fold dilution's medicinal liquid, experiment begins from 320ug/ml: 320; 160; 80; 40; 20; 10; 5; 2.5ug/ml, establish the normal cell contrast simultaneously.Change medicinal liquid in 4 days one time, kept 8 days, use the microscope observing cell pathological changes, by formula calculate the poisonous concentration (TC of half 50) and maximal non-toxic concentration (TC 0) be 5ug/ml.See Table 1.TC 50It is 22.4ug/ml that two batches of experiments divide in addition, 22.4ug/ml, the average poisonous concentration (TC of half 50) be 22.4ug/ml, maximal non-toxic concentration (TC 0) be 5ug/ml.
Table 1. compound Artemisia rupestris capsule, 2,3 toxicity in the 2.2.15 cell culture
The experiment batch Experimental technique Different pharmaceutical concentration mg/ml cytopathy TC 50 TC 0
320 160 80 40 20 10 5 2.5 (ug/ml)
1 CPE destroys % 4 4 4 100 4 4 4 100 4 4 4 100 4 4 4 100 1 1 1 25 1 1 1 25 0 0 0 0 0 0 0 0 22.4 5
2 CPE destroys % 4 4 4 100 4 4 4 100 4 4 4 100 4 4 4 100 1 1 1 25 1 1 1 25 0 0 0 0 0 0 0 0 22.4 5
Two batches average 22.4 5
The compound Artemisia rupestris capsule in the 2.2.15 cell culture to the inhibitory action of HBN DNA
Compound Artemisia rupestris capsule 5ug/ml; 2.5ug/ml; 1.25ug/ml; 0.625ug/ml; 0.313ug/ml add in the 2.2.15 cell and cultivate the 8th day suppression ratio to HBV DNA: compound Artemisia rupestris capsule Cmax 5ug/ml is 52.4 ± 6.6% to the suppression ratio of HBV DNA.
Table 2 compound Artemisia rupestris capsule is the 8th day inhibitory action to HBV DNA in the 2.2.15 cell
The experiment batch Drug level (ug/ml) The A value (X ± SD) Suppress % HBV DNA
IC 50(ug/ml)
I The contrast of 5 2.5 1.25 0.625 0.313 3TC, 1 μ M cell 0.279±0.015* 0.384±0.092 0.495±0.018 0.558±0.020 0.443±0.043 0.275±0.016* 0.681±0.062 59.0 43.6 27.3 18.1 34.9 59.6 2.10
II 5 2.5 1.25 0.625 0.313 3TC, 1 μ M cell contrast 5 0.279±0.015* 0.519±0.092 0.522±0.024 0.551±0.034 0.473±0.106 0.219±0.017** 0.583±0.061 45.9 - - - 8.2 57.5 >5.0
The result >3.55
Annotate: test group compares * * P<0.01, * P<0.05 with matched group
Conclusion:
1, the compound Artemisia rupestris capsule is to the toxicity of 2.2.15 cell culture: the compound Artemisia rupestris capsule adds in the 2.2.15 cell to be cultivated 8 days, was index with the cytopathy, two batches of empirical averages: median toxic concentration TC 50Be 22.4ug/ml, maximal non-toxic concentration TC 0Be 5ug/ml.
2, the compound Artemisia rupestris capsule in the 2.2.15 cell culture to the inhibitory action of HBV DNA: the compound Artemisia rupestris capsule was cultivated 8 days in the 2.2.15 cell, maximal non-toxic concentration 5ug/ml is 52.4 ± 6.6% to the suppression ratio of HBV DNA, and the lamivudine (3TC) of positive drug 1 μ M is 52.6 ± 1.1% to the suppression ratio of HBV DNA.
Table 3. compound Artemisia rupestris capsule is to the inhibitory action conclusive table of HBV DNA
Cytotoxicity (ug/ml) HBV DNA suppression ratio % 5.0ug/ml
TC50 TC0
22.4 5 52.4±6.6
The specific embodiment
Embodiment 1,
A, get Herba Achilleae 6 gram, Herba Hyperici Monogyni 16 grams with alcohol reflux 3 times, collecting decoction filters, and is concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10, and temperature is 40 ℃ a extractum.
B, medicinal residues and Herba Cichorii 3 grams are mixed, decoct with water each 1 hour 3 times, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.10, temperature is 40 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 75% ethanol system soft material, temperature is 45 ℃, dry granular adds Pulvis Talci in 1% ratio, and mixing is crossed 14 order wire gauzes.Get final product the fill capsule after semi-finished product inspection is qualified; This medicine is used to treat the Chinese medicine of viral hepatitis and hepatopathy.
Embodiment 2,
A, get Herba Achilleae 15 gram, Herba Hyperici Monogyni 3 grams with alcohol reflux 3 times, collecting decoction filters, and is concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.20, and temperature is 60 ℃ a extractum.
B, medicinal residues and Herba Cichorii 10 grams are mixed, decoct with water each 1 hour 3 times, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.20, temperature is 60 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 95% ethanol system soft material, temperature is 50 ℃, dry granular adds Pulvis Talci in 1.5% ratio, and mixing is crossed 14 order wire gauzes.Get final product the fill capsule after semi-finished product inspection is qualified; This medicine is used to treat the Chinese medicine of viral hepatitis and hepatopathy.
Embodiment 3,
A, get Herba Achilleae 24 gram, Herba Hyperici Monogyni 10 grams part with alcohol reflux 3 times, collecting decoction filters, and is concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.25, and temperature is 70 ℃ a extractum.
B, medicinal residues and Herba Cichorii 18 grams are mixed, decoct with water each 1 hour 3 times, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.40, temperature is 70 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 95% ethanol system soft material, temperature is 65 ℃, dry granular adds Pulvis Talci in 2% ratio, and mixing is crossed 14 order wire gauzes.Get final product the fill capsule after semi-finished product inspection is qualified; This medicine is used to treat the Chinese medicine of viral hepatitis and hepatopathy.
This product is the Uygur medicine new drug that utilizes Uygur's herb resource exploitation.Its exploitation will be removed slight illness to tens thousand of viral hepatitis and hepatopath, bring glad tidings to the patient.

Claims (3)

1, a kind of compound Artemisia rupestris capsule for the treatment of Type B viral hepatitis is characterized in that this capsule raw material ratio is: Herba Achilleae 6-24 gram, Herba Hyperici Monogyni 3-16 gram, Herba Cichorii 3--18 gram; Get Herba Achilleae earlier, the Herba Hyperici Monogyni alcohol reflux, collecting decoction filters, be concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, temperature is 40~70 ℃ a extractum, again medicinal residues are mixed with Herba Cichorii, decoct with water 3 times, each 1 hour, filter, merging filtrate, filtrate decompression are concentrated into relative density 1.10~1.40, and temperature is 40~70 ℃, merge with alcohol-extracted extract, spray drying, and, cross 12 order nets for wet with 75%--95% ethanol system soft material, oven for drying, temperature is 45 ℃--65 ℃, dry granular adds Talcum grain, mixing in the 1%--2% ratio, cross 14 order wire gauzes, can the fill capsule after semi-finished product inspection is qualified.
2, the capsular preparation method of a kind of compound Artemisia rupestris is characterized in that following these steps to carrying out:
A, get Herba Achilleae 6-24 gram, Herba Hyperici Monogyni 3-16 gram with alcohol reflux 3 times, collecting decoction, filter, be concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, and temperature is 40~70 ℃ a extractum.
B, medicinal residues and Herba Cichorii 3-18 gram is mixed, decoct with water each 1 hour 3 times, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.10~1.40, temperature is 40~70 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 75%--95% ethanol system soft material, temperature is 45 ℃--65 ℃, dry granular adds Talcum grain, mixing in the 1%--2% ratio, cross 14 order wire gauzes, can the fill capsule after semi-finished product inspection is qualified.
3, a kind of compound Artemisia rupestris capsule is in the purposes of the medicine of preparation treatment Type B viral hepatitis, and wherein this capsule raw material ratio is: Herba Achilleae 6-24 gram, Herba Hyperici Monogyni 3-16 gram, Herba Cichorii 3-18 gram; Get Herba Achilleae, Herba Hyperici Monogyni alcohol reflux earlier, collecting decoction filters, and is concentrated into 1: 1 thick paste, add ethanol equivalent, stir evenly, leave standstill and make precipitation more than the 24h, get the supernatant decompression recycling ethanol, being evaporated to relative density is 1.10~1.25, and temperature is 40~70 ℃ a extractum.Again medicinal residues are mixed with Herba Cichorii, decoct with water 3 times, each 1 hour, filter, merging filtrate, filtrate decompression is concentrated into relative density 1.10~1.40, temperature is 40~70 ℃, merges spray drying with alcohol-extracted extract, and, cross 12 order nets, oven for drying for wet with 75%--95% ethanol system soft material, temperature is 45 ℃--65 ℃, dry granular adds Talcum grain, mixing in the 1%--2% ratio, cross 14 order wire gauzes, can the fill capsule after semi-finished product inspection is qualified.
CNB031379028A 2003-05-29 2003-05-29 Compound artemisia rupestris capsule Expired - Fee Related CN1304019C (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1895453B (en) * 2006-06-27 2010-09-01 斯拉甫·艾白 Juyi oral preparation
CN101829185B (en) * 2010-06-02 2012-02-15 赵敬民 Medicinal composition for resisting influenza virus
CN103127273B (en) * 2013-03-12 2014-11-05 中国科学院新疆理化技术研究所 Compound medicament for treating chronic liver disease and preparation method thereof
CN106924313A (en) * 2015-12-30 2017-07-07 姚萍 Application of the witloof in the medicine for preparing treatment virus B hepatitis
CN106039277B (en) * 2016-08-05 2019-12-03 王豪鹏 Compound Ni Lupa cold granules and its production method

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1198097A (en) * 1995-09-29 1998-11-04 威廉施瓦布博士有限公司 Stable extract of hypericum perforatum L., process for preparing the same and pharmaceutical compositions

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1198097A (en) * 1995-09-29 1998-11-04 威廉施瓦布博士有限公司 Stable extract of hypericum perforatum L., process for preparing the same and pharmaceutical compositions

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