CN101879195A - Process for preparing general flavone extract of effective part of hypericum ascyron linne and new medicament appliaciton - Google Patents
Process for preparing general flavone extract of effective part of hypericum ascyron linne and new medicament appliaciton Download PDFInfo
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- CN101879195A CN101879195A CN2009100150328A CN200910015032A CN101879195A CN 101879195 A CN101879195 A CN 101879195A CN 2009100150328 A CN2009100150328 A CN 2009100150328A CN 200910015032 A CN200910015032 A CN 200910015032A CN 101879195 A CN101879195 A CN 101879195A
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- herba hyperici
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Abstract
The invention relates to a process for preparing general flavone extract of effective part of Hypericum ascyron linne and new medicament appliaciton, in particular to application of the general flavone extract in preparation of medicaments for treating hepatitis B.
Description
Technical field
The invention belongs to biomedical sector, refer in particular to a kind of new medicine use of Herba Hyperici total flavone valid target, specifically be the purposes in the medicine of preparation treatment hepatitis B, comprise with the Herba Hyperici total flavone valid target being the purposes of pharmaceutical composition in the medicine of preparation treatment hepatitis B of active component.
Background technology
Herba Hyperici, for Hypericaceae hypericum Herba Hyperici Hypericum ascyron L., with all herbal medicine, another name Hunan Fructus Forsythiae, hypericum ascyron record in " national Chinese herbal medicine compilation ", and be cold in nature, mildly bitter flavor.Has cooling blood for hemostasis, heat-clearing and toxic substances removing.Be used for spitting blood spitting of blood, epistaxis, metrorrhagia, jaundice, hepatitis; Wound hemorrhage is controlled in external, burn and scald, eczema, jaundice, hepatitis.Herba Hyperici is a medicine commonly used among the people, among the peoplely is used for diseases such as hemostasis, the subcutaneous ulcer of harnessing the Yellow River, hepatitis and furuncle toxic swelling.Modern study shows that its chemical constituent mainly contains flavone compounds such as Quercetin, nimbecetin, hyperin, Isoquercitrin, globulariacitrin, and contains volatile oil, the main a-Flos Caryophylli alkene (a-caryophylene) that contains in the oil; Other has carotene, vitamin, riboflavin.Modern pharmacological research shows, its have relieving asthma, eliminate the phlegm, antitussive, antibacterial action, but not relevant for it in the application aspect the treating hepatitis B.Chinese patent 200610038949.6 discloses Herba Hyperici extractive of general flavone, its preparation method and application, provides this extract to be applied in preparation treatment cardiac-cerebral ischemia diseases.
We find that in the process that its composition is studied hyperin content is higher in the Herba Hyperici, and the medical material content of separate sources is on average between 1.1%-1.5%.Bibliographical information is arranged, and the single component hyperin has the effect of significant protection hepatic tissue, can promote to organize NO content to increase.Chinese patent 02146370.0 discloses preparation method and the new medicine use of a kind of hyperin, and the application of hyperin in the medicine of preparation treatment hepatitis B is provided.According to another report, hyperin infects the hepatic injury of DHBV model to duckling antiviral and protective effect preferably.Flavone component in the above-mentioned research data prompting Herba Hyperici has certain effect at tool aspect the treatment hepatitis.
In view of this, the extractive of general flavone of our extraction separation preparation from Herba Hyperici, this effective part extract contains the flavone component of kind of similar surplus in the of ten, wherein hyperin content accounts for more than 10%, general flavone content is up to more than 50%, composition is more comprehensive, infers that with this Herba Hyperici extractive of general flavone may have hepatitis virus resisting identical or better with hyperin and hepatoprotective effect.Therefore we have carried out the pharmacology prerun that antiviral activity is measured to the Herba Hyperici extractive of general flavone, and the HBsA blood clotting titre that the result handles with the Herba Hyperici total flavones reduces more than 2 times than positive controls, and is better than single component hyperin matched group; In addition, we have also carried out the preliminary experiment of duck hepatitis-B animal model, and 5 duckling base portions of treatment group as a result do not find the HBsAg of dhbv dna, and infect matched group the evidence that occurs positive infection in 3 duckling serum are arranged.The above results confirms that the Herba Hyperici total flavone valid target is aspect anti-hepatitis virus, effect is clearer and more definite than hyperin, have the advantage of special effect, and toxic and side effects is little, it is developed into Chinese medicine 2 kind new medicines, is expected to obtain the breakthrough of matter in the anti-hepatitis virus field.Thereby finished the present invention.
Summary of the invention
The new medicine use that the purpose of this invention is to provide a kind of Herba Hyperici total flavone valid target specifically is as the purposes in the medicine of preparation treatment hepatitis B.
Another object of the present invention provides a kind of pharmaceutical composition for the treatment of hepatitis B, contains the Herba Hyperici total flavone valid target and the pharmaceutical carrier for the treatment of effective dose.Described pharmaceutical composition, the Herba Hyperici total flavone valid target that can also contain dose therapeutically effective has the medicine of antiviral, hepatoprotective effect with other.
Aforementioned pharmaceutical compositions can adopt the conventional method of galenic pharmacy to be prepared into various dosage forms, as tablet, capsule, granule, oral liquid etc.
It is 100～500mg/ time that the suggestion clinical patients is used the dosage of Herba Hyperici total flavone valid target, three times on the one.
Essence for a better understanding of the present invention specifies the new purposes of Herba Hyperici total flavone valid target in pharmaceutical field below.
The specific embodiment
The preparation of embodiment 1 Herba Hyperici total flavone valid target
It is an amount of that Herba Hyperici is added 80% ethanol, extracts 1 time, extracted 2 hours, merge extractive liquid, filters, and relative density was 1.13～1.16 concentrated solution when filtrate was condensed into 60 ℃, add suitable quantity of water water precipitating 24h, sucking filtration is concentrated into respective volume, passes through macroporous adsorptive resins, adopt pure water gradient elution, 3 column volumes of water elution, 3 column volumes of each eluting of 10% and 30% ethanol, 1 column volume of 70% ethanol elution.Eluent concentrates, dry, obtain the Herba Hyperici extractive of general flavone after pulverizing, its general flavone content is 65%.
The capsular preparation of embodiment 2 Herba Hyperici total flavone valid targets
Get Herba Hyperici total flavone valid target extract 250g, magnesium stearate 50g crosses the abundant mixing of 80 mesh sieves, dry granulation, and 1000 of fill capsules, every contains Herba Hyperici total flavone valid target 250mg.Usage: each 2, every day three times.
The preparation of embodiment 3 Herba Hyperici total flavone valid target tablets
Get Herba Hyperici total flavone valid target extract 250g, microcrystalline Cellulose 45g, mixing, the ethanol wet granulation is crossed 20 mesh sieves.Add magnesium stearate 5g, mixing, compacting heavily is 1000 in the tablet of 0.3g/ sheet in flakes, every contains Herba Hyperici total flavone valid target 250mg.Usage: each 2, every day three times.
The preparation of embodiment 4 Herba Hyperici total flavone valid target granules
Get Herba Hyperici total flavone valid target extract 250g, dextrin 150g crosses the abundant mixing of 80 mesh sieves, and the ethanol wet granulation is packaged into 1000 bags of the granules of every bag of 4g, and every bag contains Herba Hyperici total flavone valid target 250mg.Usage: each 1～2 bag, every day three times.
The test of embodiment 5 anti-hepatitis virus
, utilize duck hepatitis B model to carry out the pharmacological action of Herba Hyperici extractive of general flavone and observe for following the trail of the objective with anti-HBV effect.
(1) the male 1 age in days sheldrake of animal model is 24, body weight 40～50g, all only through lower limb shin intravenous injection sheldrake DHBV-DN A strong positive serum 0.2ml/, raise to 2 ages in week as the duck hepatitis-B experimental animal model.
(2) experimental technique is divided into 4 groups at random with 24 of animal patterns, 6 every group.It is oral that administration group 1 and administration group 2 all give the suspension that the Herba Hyperici total flavones is made into, and dosage is respectively 50mg/kg/d and 100mg/kg/d; Virus control group starch solution; Positive drug group acycloguanosine (acyclovir, ACV group), dosage is 10mg/kg/d.Gavage every day 1 time, 10d is that 3d is observed in 1 course of treatment, drug withdrawal.Respectively at before the medication, medication 5d, medication 10d, drug withdrawal 3d blood sample collection from external jugular vein, separation of serum-20 ℃ preservation is to be checked.It is clear to get above-mentioned Sanguis Anas domestica, and every batch with the time point film, with P labelling DHBV NA probe, and makes the clear dot blot hybridization of Sanguis Anas domestica, and autoradiography diaphragm speckle is surveyed OD value (490nm) on enzyme connection instrument, calculating serum DHBV-DNA density.
Average suppression ratio (p on average suppresses)=(OD
Before the administration-OD
Administration nd) * OD
Before the administration -1* 100%.
(3) result
1. serum DHBV-DNA changes situation before and after the medication
All can significantly reduce DHBV infected duck serum DHBV-DNA level when Herba Hyperici extractive of general flavone 5d, 10d and drug withdrawal 3d.See Table 1.
The interior inhibitory action to DHBV-DNA of table 1 duck body (x ± s)
Annotate: adopt the t check.With comparison before the medication of this group,
*P＜0.05,
*P＜0.01; Compare with the concurrent control group,
#P＜0.05,
##P＜0.01; ACV organizes relatively with the same period.
△p＜0.05.
△△P＜0.01
2. the average suppression ratio of DHBV-DNA before and after treating
The Herba Hyperici extractive of general flavone all has remarkable inhibition DHBV effect when medication 5d, 10d and drug withdrawal 3d, the average suppression ratio of wherein administration group 2 and ACV group difference not statistically significant (P＞0.05), and do not have obvious rebound phenomenon during drug withdrawal 3d.See Table 2.
Table 2 Herba Hyperici extractive of general flavone is to the average suppression ratio (%) of DHBV-DNA
Annotate: adopt the t check.Compare with the concurrent control group.
*P＜005, #P＜0.01; ACV organizes relatively with the same period,
△P＜0.05.
☆P＜0.01
(5) conclusion:
Originally studies show that in the anti-dhbv dna test, the Herba Hyperici extractive of general flavone can significantly reduce DHBV infected duck serum DHBV-DNA level in the body, effect strengthens with using dosage.The anti-HBV effect and the potential research and development of pointing out this material to have significant are worth.
Claims (2)
1. Herba Hyperici total flavone valid target, it is characterized in that this effective site is made by following method: get the Herba Hyperici medical material, add 30～90% alcohol reflux, extracting solution concentrates, and water precipitating 24h filters, filtrate is passed through macroporous adsorptive resins, adopt pure water gradient elution, eluent is concentrated, dry, obtains Herba Hyperici effective site---extractive of general flavone.
2. Herba Hyperici total flavone valid target as claimed in claim 1, the purposes in the medicine of preparation treatment hepatitis B.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102805759A (en) * | 2011-12-02 | 2012-12-05 | 南昌大学 | Total flavone of Hypericum ascyron L and extraction method and application thereof |
| CN107569527A (en) * | 2017-10-31 | 2018-01-12 | 桂林纽泰生物科技有限公司 | The method that general flavone is extracted from hyperici,herba |
| CN109846831A (en) * | 2018-12-11 | 2019-06-07 | 江西赣隆药业有限公司 | A kind of hyperici,herba granule and preparation method thereof |
| CN110452110A (en) * | 2018-05-07 | 2019-11-15 | 中国医学科学院药物研究所 | A kind of phloroglucinol derivatives natural drug and its preparation method and application |
-
2009
- 2009-05-06 CN CN2009100150328A patent/CN101879195A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102805759A (en) * | 2011-12-02 | 2012-12-05 | 南昌大学 | Total flavone of Hypericum ascyron L and extraction method and application thereof |
| CN102805759B (en) * | 2011-12-02 | 2014-07-16 | 南昌大学 | Total flavone of Hypericum ascyron L and extraction method and application thereof |
| CN107569527A (en) * | 2017-10-31 | 2018-01-12 | 桂林纽泰生物科技有限公司 | The method that general flavone is extracted from hyperici,herba |
| CN110452110A (en) * | 2018-05-07 | 2019-11-15 | 中国医学科学院药物研究所 | A kind of phloroglucinol derivatives natural drug and its preparation method and application |
| CN109846831A (en) * | 2018-12-11 | 2019-06-07 | 江西赣隆药业有限公司 | A kind of hyperici,herba granule and preparation method thereof |
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Open date: 20101110 |