CN1408396A - An Oral Medicine for Depression-Jinyukang - Google Patents
An Oral Medicine for Depression-Jinyukang Download PDFInfo
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- CN1408396A CN1408396A CN 01141431 CN01141431A CN1408396A CN 1408396 A CN1408396 A CN 1408396A CN 01141431 CN01141431 CN 01141431 CN 01141431 A CN01141431 A CN 01141431A CN 1408396 A CN1408396 A CN 1408396A
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- depression
- herba hyperici
- hyperici perforati
- jinyukang
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Abstract
The invention relates to a Jinyukang oral medicine for treating depression, which is extracted from the effective part of hypericum perforatum and is characterized in that: wherein the content of Hypericin and pseudohypericin is 0.15-48%, the content of rutin is 2.3-4%, the content of total flavone is 50-90%, and the content of Hyperforin is 2-46%. The oral preparation comprises tablets, capsules, powder and oral liquid. Can be directly extracted from herba Hyperici perforati, or further refined from the crude extract of herba Hyperici perforati.
Description
Technical field
The present invention relates to a kind of oral medicine-magnificent health for the treatment of depression, belong to International Classification of Patents medicament preparation A61K35/78 technical field.
Background technology
Depression is one of current social principal disease.Along with the aggravation of multiple stressors, accelerate as people's rhythm of life, aged tendency of population, social competition's aggravation etc., depression has become the commonly encountered diseases of modern society, high morbidity.Its incidence rate increases fast.According to statistics, whole world depressive patient has accounted for 3%～5% of world population.
Along with to the popular science propaganda of depression and the raising of people's living standard, to the raising that quality of life requires, depression more and more causes people's great attention.The medical expense that is used for the treatment of depression also sharply increases, and this type of medicine has huge market simultaneously, so the antidepressants of development of new, efficient, wide spectrum, low toxicity have become one of focus that every industry or trade researches and develops.According to statistics, the total sales volume of global CNS pharmaceutical market in 1997 is 26,000,000,000 US dollars, and annual rate of growth is 12%.The CNS medicine that surpasses 200,000,000 US dollars of sales volumes has 16 kinds more than.The sales volume in antidepressants market, nineteen ninety-five is 3,000,000,000 US dollars, 1998 is 6,000,000,000 US dollars.Arrange preceding 3 fluoxetine (23.56 hundred million US dollars) that is, Sertraline (13.37 hundred million US dollars), 11.01 hundred million US dollars of Pa Jinxiting are antidepressants.Development of new wide spectrum, antidepressants efficient, low toxicity are one of focuses of whole world pharmacy corporation concern.
World's antidepressants product mainly contains five classes: serotonin reuptake inhibitors (SSRTS) optionally, norepinephrine and specific serotonin reuptake inhibitors (NASSAS), tricyclic antidepressants (TCAS), oxidase inhibitor (MAOT) and serotonin and NRI (SNARI).Classical antidepressants are tricyclic antidepressant (TCA), and its determined curative effect, cheap is in leading position in decades clinically always.But because the toxicity that its cholinolytic effect reaches heart makes part patient and old people be difficult to accept.Fourth Ring class antidepressants have been done partly to improve on the TCA basis, but effect is not very good.Serotonin reuptake inhibitor (SSRI) has overcome the shortcoming of TCA, because its efficient, safety and good tolerability have obtained using widely abroad.Its characteristics are mainly few side effects and slight, essentially no cholinolytic effect of some medicine and cardiac toxicity.And instructions about how to take medicine are easy, and only need obey successively every day, and most patients must not adjust dosage basically, are easy to be accepted by the patient.But the SSRI preparation mostly is external or joint pharmaceutical factory is monopolized, and price is more expensive.All there are some shortcomings in above medicine, and is single as the mechanism of action, and price is more expensive, and side effect is big, the incidence rate height, as influence the universal and use that cardiac function, sexual function, xerostomia, constipation etc. have had a strong impact on these medicines.
The modern disease pharmacological research shows that the depression pathogenesis is very complicated, and induced factor is more.Medicine at certain single link often is difficult to obtain satisfied curative effect.Synthetic antidepressants great majority exist the antidepressant spectrum narrow, and side effect is big, defectives such as the high and easy recurrence of medicine valency.The utilization of plant amedica resource is more and more paid attention in the development of external antidepressants and exploitation aspect in the native land.Wherein the Herba Hyperici perforati treatment that is used for depression has caused global very big concern.
Antidepressants present Research commonly used at present is: 1, classical antidepressants, on behalf of medicine, it comprise imipramine, desmethylimipramine and amitriptyline etc.Its pharmacological action characteristics are heavily absorptions of monoamine neurotransmitter in the blocking-up brain, simultaneously the M-cholinergic in the brain and adrenal gland's nervous system etc. are all had in various degree cholinolytic side reaction and cardiac toxicity etc.For reducing side reaction and reducing toxicity.Once the seventies occurs some non-tricyclic antidepressants,, but do not overcome toxic and side effects yet fully as maprotiline and rice ammonia color woods etc.; 2, selectivity 5-hydroxy tryptamine cell reabsorption inhibitor, typical medicaments comprise fluoxetine, paroxetine, Sertraline and western general peptide orchid etc.Its pharmacology characteristics are that the specific inhibition 5-hydroxy tryptamine heavily absorbs, and are very low to the affinity of other neurotransmitter receptor in the brain, little than the tricyclic antidepressants toxicity, but still have certain side effect.3, oxidase inhibitor is just to find the effective medicine of treatment depression the fifties, and this class medicine belongs to non-selective inhibitor, and toxic and side effects is many, toxicity is big, is eliminated mostly, and what remain has: phenelzine, tranylcypromines etc. use very prudent clinically.
In view of the toxic and side effects and the shortcoming of above-mentioned Western medicine preparation, many researchs of extracting the antidepressant material from medical herbs are arranged at present, Chinese herbal medicine is abundant in china natural resources, is a field of being well worth doing.
Herba Hyperici perforati in Europe and the U.S. be extensive use of as medical herbs and food additive respectively.Herba Hyperici perforati is a kind of herbaceos perennial of Europe and Asia growth, in the clinical use history in existing thousands of years of this plant of Europe, is mainly used in wound, diuresis, peripheral neuralgia etc.Be used for the treatment of the history in existing hundreds of years of depression.
Herba Hyperici perforati is carried out more deep research abroad, illustrated the problem of its aspect such as resource, pharmacy, pharmacology, toxicity, clinical practice substantially.Progress is as follows:
1, to study the antidepressant main effective ingredient of this plant be benzo dianthrone class (comprising hypericin, pseudohypericin etc.), flavonoid (hyperin, rutin, Quercetin, isoquercitin etc.) to effective ingredient, phloroglucinol (hyperforine, pseudo-hyperforine) three major types.It is generally acknowledged that hypericin, pseudohypericin, hyperforine and some Flavonoid substances are the active component of treatment depression, are the coefficient results of these compositions.
2, Study on mechanism generally believes it is by suppressing the MAO enzyme, suppress 5-HT, DA, NA reuptake, making many-sided comprehensive functions such as 5-HT, DA, NA increase in the brain.
3, light, moderate depressive patients curative effect of clinical efficacy and safety Herba Hyperici perforati crude extract 900mg treatment and tricyclic antidepressants and fluoxetine are suitable, the side effect incidence rate is obvious low and slight than the latter, modal reaction is symptom of digestive tract (0.8), photosensitivity reaction (0.5), the side effect occurrence rate is 19.8%, and the side effect occurrence rate of common antidepressants is 35.9%, shows as mainly that cardiac function is unusual, sexual function is unusual and xerostomia etc.
4, dosage form, Quality Control, some pharmacy corporations of stability study are just being accelerated this plant is developed as prescription drugs, extensively utilize the crude extract treatment dysthymia of Herba Hyperici perforati (Hypericum perforatum L.).As spiritual class medicine is westerner's achievement in research in modern age.The preparation that is used for the treatment of depression on the American-European market is made " standard extract "-Herba Hyperici perforati crude extract, and the content of only stipulating total hypericin is 0.3% (HPLC method).Make capsule, tablet, steady quality.Taking dose is 300mg, tid..But in some patents or the preparation, on preparation technology, or only consider total hypericin content of (not comprising hyperforine), or only consider the content of hyperforine, clear and definite inadequately to the Flavonoid substances content requirement.
The exploitation of Herba Hyperici perforati has also caused the attention of more domestic units.Herba Hyperici perforati distributes very wide in China, be exactly a kind of Chinese herbal medicine since Gu, is used for astringing to arrest bleeding, regulating menstruation lactogenesis, heat-clearing and toxic substances removing, dampness removing etc.According to statistics, the domestic research paper of delivering about Herba Hyperici perforati has reached tens of pieces of writing, wherein mainly concentrates on Herba Hyperici perforati resource distribution, the process of preparing Chinese medicine, processing at home and reaches influence and basic researchs such as extracting method and analytical method to content.In recent years, because the foreign demand amount is bigger, domestic many manufacturers are many with the crude extract outlet, produce so that the form of extract is cheap.
Patent PCT/DE96/02444, propose " a kind of mixture; by one or more poly-ring diketone; from Hypericin, Pesudohypericin and salt thereof, select; concentration is between 0.05%-50%; and by another kind of or several other compositions in addition, concentration between 50%-99.95%, (for example: Quercetin), selection flavonoid candy glycoside, plant acid, hyperforine, tannin, phylloxanthin, fat and the waxiness etc. from bioflavonoids.Quality standard and wes' is similar, but fuzzy to the content requirement of hyperforine, and what is claimed is and be used for of this patent " treat a kind of by virus, the disease that particularly a kind of degeneration virus causes ", is not to be used for the treatment of depression.
Summary of the invention
The purpose of this invention is to provide a kind of this patent and propose a kind of novel formulation-magnificent health than the more purified treatment dysthymia of Herba Hyperici perforati crude extract.
Technical scheme of the present invention is as follows:
Obtain through refining the magnificent health oral drugs of treatment depression with the effective site of Herba Hyperici perforati, it is characterized in that: the total content of wherein contained hypericin (Hypericin) and pseudohypericin (Pesudohypericin) is 0.15-48%, the content of rutin is 2.3-4%, content of total flavone is 50-90%, and the content of hyperforine (Hyperforin) is 2-46%.
Oral formulations comprises tablet, capsule, powder and oral liquid etc.
The effective site of described Herba Hyperici perforati can directly be extracted from Herba Hyperici perforati, perhaps forms by the crude extract of Herba Hyperici perforati is further refining.
The crude extract of Herba Hyperici perforati refers to ethanol extraction, the spray drying method with about 70%, or directly extracts the mixture of after drying from the Herba Hyperici perforati crude drug with methods such as supercritical carbon dioxide extraction, except that active component, contains pigment and the carbohydrate material is higher.
To the research of central nervous system's influence,, prove that magnificent health is effective through animal experiment.Ergasia to animal has certain influence, can strengthen the exploratory behaviour of mice, and dose dependent prolongs the length of one's sleep of hypnotic, and the effect of antagonism reserpine is arranged in range of doses.Similar to most of antidepressants, can strengthen the runner mobility of mice, continuous use can reduce the aggressive behavior of male mice, prompting may to light, moderate depressive patients is effective.We have finished mouse tail suspension to the drug effect of magnificent Kang Jinhang, the rats'swimming test.The result is as follows:
According to new drug pharmacology guideline (Western medicine part), relevant antidepressant pharmacological evaluation teachings is carried out pharmacodynamic experiment.Now finished the mandatory swimming test of mouse tail suspension and rat.
Mouse tail suspension experiment: select 16 ~ 20g Kunming mouse male.After after the last administration one hour, mice to be hung by the feet in experimental box, head is hung 6 minutes time by the feet from end 5cm height, observes the mice dead time in 4 minutes.
Positive control drug shows for the desmethylimipramine result:
Annotate: increased gradually from 1 ~ 4 by the dosage of reagent, * and matched group are than P＜0.05
| Medicine | Dosage (mg/kg) | Dead time (S) | ??n |
| ?CMC-Na | ?85.6±29.8 | ?15 | |
| ?DMI | ?20 | ?60.7±29.4* | ?14 |
| Be subjected to reagent | ?1 | ?70.5±35.0 | ?15 |
| ?2 | ?74.1±38.7 | ?14 |
| ??3 | ??72.6±34.9 | ?15 | |
| ??4 | ??61.2±27.2* | ?13 |
The experiment of rat forced swimming: select 130 ~ 150gWistar rat, rat is put into diameter 20cm, in the glass circle cylinder that water is arranged of high 40cm, 1 in every cylinder.The control water temperature and the depth of water.Testing the previous day, every pre-trip 15 minutes of rat, test after 24 hours: rat is put into cylinder, observes 5 minutes, is accumulated at the dead time in the water.(stop to struggle, being floating state, only have limb motion once in a while persistent period of phenomenon such as to keep afloat to keep head) positive control drug is an amitriptyline.The result shows:
| Medicine | Dosage (mg/kg) | Dead time (S) | ?n |
| ?CMC-Na | ?68.0±35.3 | ?9 | |
| Amitriptyline | ?20 | ?8.60±18.3** | ?10 |
| Be subjected to reagent | ?1 | ?28.1±33.9* | ?10 |
| ?2 | ?36.2±31.6 | ?10 | |
| ?3 | ?21.0±13.2** | ?9 | |
| ?4 | ?9.10±9.8** | ?9 |
Annotate: increased gradually from 1 ~ 4 by the dosage of reagent, * and matched group are than P＜0.05**P＜0.01
Conclusion: be subjected to reagent in these two experiments, to show tangible antidepressant activity, the meaning of further exploitation is arranged.
Just carry out at present rat olfactory bulb removal and chronic depression Study of model, carrying out antidepressant mechanism researchs such as the mensuration of single 5-MT, DA, NA in the brain and MAO mensuration simultaneously.
The specific embodiment
Herba Hyperici perforati medicinal material extract three times, add for the first time 10 times of amount 55% ethanol soaking at room temperature and refluxed 2 hours after 12 hours, filter, add 6 times of amount 55% alcohol refluxs 1 hour for the second time, filter, add 6 times of amount 55% alcohol refluxs 1 hour for the third time, filter, merge three times filtrate, reclaim ethanol, be concentrated into relative density 1.35 (50-60 ℃), drying under reduced pressure (50-60 ℃) was pulverized the 80-100 mesh sieve and was promptly got the Herba Hyperici perforati crude extract.
The Herba Hyperici perforati crude extract extracts secondary, add for the first time 20 times of amount 15% ethanol and stir extraction 30 minutes for 60 ℃, extracting solution centrifugal (3000 rev/mins) 25 minutes, add for the second time 10 times of amount 15% ethanol, 60 ℃ are stirred extraction 20 minutes, centrifugal 25 minutes, merge the secondary supernatant, mixing is crossed the D-101 macroporous adsorptive resins, stops to go up sample after resin absorption is saturated, cross post with distilled water, till the effluent clarification (water consumption be the resin volume 4-5 doubly), use 70% ethanol elution, the collection eluent, reclaim ethanol and be concentrated into (50 ~ 55 ℃ of relative density 1.35 (50-60 ℃) drying under reduced pressure, vacuum: 0.09-0.1Mpa), pulverize, cross the 80-100 mesh sieve and promptly get Herba Hyperici perforati effective site.
Get Herba Hyperici perforati effective site 300g, add antioxidant (medicinal vitamin c powder) 4.5g, fluidizer (micropowder silica gel) 6.0g, mixing, encapsulated, obtain 1000 magnificent health.
Claims (3)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01141431 CN1261111C (en) | 2001-09-25 | 2001-09-25 | A preparation method of oral medicine for treating depression |
| CNB2006100811168A CN100534420C (en) | 2001-09-25 | 2001-09-25 | An oral administered medicine for treating depression-Jin Yu Kang |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01141431 CN1261111C (en) | 2001-09-25 | 2001-09-25 | A preparation method of oral medicine for treating depression |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100811168A Division CN100534420C (en) | 2001-09-25 | 2001-09-25 | An oral administered medicine for treating depression-Jin Yu Kang |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1408396A true CN1408396A (en) | 2003-04-09 |
| CN1261111C CN1261111C (en) | 2006-06-28 |
Family
ID=4676165
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100811168A Expired - Lifetime CN100534420C (en) | 2001-09-25 | 2001-09-25 | An oral administered medicine for treating depression-Jin Yu Kang |
| CN 01141431 Expired - Lifetime CN1261111C (en) | 2001-09-25 | 2001-09-25 | A preparation method of oral medicine for treating depression |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100811168A Expired - Lifetime CN100534420C (en) | 2001-09-25 | 2001-09-25 | An oral administered medicine for treating depression-Jin Yu Kang |
Country Status (1)
| Country | Link |
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| CN (2) | CN100534420C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100367976C (en) * | 2004-04-21 | 2008-02-13 | 上海市中药研究所 | Hypericum perforatum extract and preparation method thereof |
| CN101156835B (en) * | 2007-07-03 | 2010-10-06 | 中国农业科学院兰州畜牧与兽药研究所 | Preparation method of hypericin oral liquid |
| US8546342B2 (en) | 2005-02-28 | 2013-10-01 | Thomas Christian Lines | Composition for treating mental health disorders |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105832693A (en) * | 2016-03-18 | 2016-08-10 | 常州市阿曼特化工有限公司 | Preparation method for special hollow capsule used for depressant drug |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4239959A1 (en) * | 1992-11-27 | 1994-06-01 | Schwabe Willmar Gmbh & Co | St. John's wort dry extract, process for its preparation and its use |
| DE19646977A1 (en) * | 1995-09-29 | 1998-01-15 | Schwabe Willmar Gmbh & Co | Stable dry extract of Hypericum perforatum L., Saint John's wort |
| WO2000002455A1 (en) * | 1998-07-09 | 2000-01-20 | Cv Technologies Inc. | Hypericin and hypericum extract: specific t-type calcium channel blocker, and their use as t-type calcium channel targeted therapeutics |
-
2001
- 2001-09-25 CN CNB2006100811168A patent/CN100534420C/en not_active Expired - Lifetime
- 2001-09-25 CN CN 01141431 patent/CN1261111C/en not_active Expired - Lifetime
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100367976C (en) * | 2004-04-21 | 2008-02-13 | 上海市中药研究所 | Hypericum perforatum extract and preparation method thereof |
| US8546342B2 (en) | 2005-02-28 | 2013-10-01 | Thomas Christian Lines | Composition for treating mental health disorders |
| CN101156835B (en) * | 2007-07-03 | 2010-10-06 | 中国农业科学院兰州畜牧与兽药研究所 | Preparation method of hypericin oral liquid |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1261111C (en) | 2006-06-28 |
| CN1875954A (en) | 2006-12-13 |
| CN100534420C (en) | 2009-09-02 |
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Granted publication date: 20060628 |