CN107951937A - A kind of medicinal preparation for oral administration containing antidepressant activity component - Google Patents
A kind of medicinal preparation for oral administration containing antidepressant activity component Download PDFInfo
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- CN107951937A CN107951937A CN201711349764.1A CN201711349764A CN107951937A CN 107951937 A CN107951937 A CN 107951937A CN 201711349764 A CN201711349764 A CN 201711349764A CN 107951937 A CN107951937 A CN 107951937A
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- oral administration
- medicinal preparation
- antidepressant activity
- chinese medicine
- activity component
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- 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)
- A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
- A61K36/233—Bupleurum
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
- A61K31/08—Ethers or acetals acyclic, e.g. paraformaldehyde
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- 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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- 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)
- A61K36/65—Paeoniaceae (Peony family), e.g. Chinese peony
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- 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)
- A61K36/71—Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
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- 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)
- A61K36/72—Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
- A61K36/725—Ziziphus, e.g. jujube
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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Abstract
This case is related to a kind of medicinal preparation for oral administration containing antidepressant activity component, which contains traditional Chinese medicine composition extract liquid and antidepressant activity component；Traditional Chinese medicine composition extract liquid is obtained by radix bupleuri, radix glycyrrhizae, Chinese herbaceous peony, jujube by decocting and concentrating after specified weight proportioning；Antidepressant activity component is 3,7 dimethyl, 2,6 zinn diene aldehyde and 3,7 dimethyl, 2,6 zinn diene aldehyde dialkoxy acetal made from fatty alcohol condensation；The existing Chinese medicine warm of medicinal preparation for oral administration of the present invention and, few side effects and stimulate the advantages of small, also have the advantages that Western medicine it is rapid-action, can immunotherapy targeted autoantibody, and cost of material is relatively low, and the price of medicinal preparation for oral administration has competitiveness.
Description
Technical field
The present invention relates to antidepressant field, and in particular to a kind of oral medicine containing new antidepressant activity component
Agent.
Background technology
Depression belongs to one kind of mental state (emotion) obstacle, be mainly shown as significantly and enduringly present it is depressed, gently
Degree person shows as dysphoria, interest blank, severe patient can overwhelmed with sorrow, pessimistic despair, often have introgression.Depression is one
Class seriously endangers the common mental illness of human physical and mental health, the World Health Organization be classified as ten big heavy diseases it
One.With the fast development of social economy, the accelerating rhythm of life, the pressure increase of people, various emotion impacts increase, depressed
Disease incidence increases year by year.Depression is referred to as " epidemic disease of 21st century ".
Treating depression medication is divided into two major class of synthetic drug and natural drug, and synthetic drug includes tricyclic and Fourth Ring class resists
Depressant drug, monoamine oxidase inhibitors, lithium carbonate, Benzodiazepine etc.；Natural drug mainly under drug matching theoretical direction,
The Chinese herbal medicine that choosing has effects that soothing liver-qi stagnation is used as treatment depression after performance reconciliation.Wherein, there are anti-suppression for synthetic drug
The defects of strongly fragrant spectrum is narrow, side effect is big, medicine valency is high and easily recurs；Natural drug is there are complicated component, drug effect is slow, active ingredient and work
The problems such as being difficult to determine with mechanism.
The content of the invention
For the shortcoming of existing antidepressants, the present invention is with citral (3,7- dimethyl -2,6- zinn diene aldehyde)
Raw material, reacts to obtain ethylidene ether structure with the fatty alcohol containing 12~18 carbon atoms in acid condition, the ethylidene ether structure conduct
Antidepressant activity component achieves good antidepressant effect.
Antidepressant agent according to the present invention contains traditional Chinese medicine composition extract liquid and antidepressant activity component；Its
In, Chinese medicine composition by following components by weight ratio：
Antidepressant activity component for 3,7- dimethyl made from the condensation of 3,7- dimethyl -2,6- zinn diene aldehydes and fatty alcohol -
2,6- zinn diene aldehyde dialkoxy acetals.
Preferably, the preparation method of the traditional Chinese medicine composition extract liquid：Each taste Chinese medicine is cleaned into drying, coarse crushing and mistake
Sieve, adds water to cook after mixing, and the water for adding 8 times of medicinal material gross weight is carried in tank in water, when decoction 2 is small, repeats to decoct 3 times, mistake
Filter off filter residue, merging filtrate, be concentrated under reduced pressure to former filtrate volume 1/10~1/15.
Preferably, the preparation method of the antidepressant activity component：Will contain 3,7- dimethyl -2,6- zinn diene aldehydes,
The reaction solution of fatty alcohol, acetic acid and ethanol be heated to reflux 4~5 it is small when, 3,7- dimethyl -2,6- zinn diene aldehyde dialkoxies of generation
Base acetal is with reaction liquid layer and positioned at the bottom of reaction vessel, by 3,7- dimethyl -2,6- zinn diene aldehyde dialkoxy acetals
Washed three times with ethanol after separation, obtain antidepressant activity component.
Preferably, 3,7- dimethyl -2,6- zinn diene aldehyde containing 0.1mol, 0.2~0.22mol in the reaction solution
Fatty alcohol, the acetic acid of 2mL and the ethanol of 250mL.
Preferably, the fatty alcohol is the one or more in Decanol, dodecanol, tetradecanol.
Preferably, the traditional Chinese medicine composition extract liquid and the volume ratio of antidepressant activity component are 100: 8.
Preferably, honey is dissolved with the medicinal preparation for oral administration.
Beneficial effects of the present invention：Present invention selection radix bupleuri, radix glycyrrhizae, Chinese herbaceous peony, four taste Chinese medicine of jujube are combined, to Chinese medicine
Active ingredient carry out purification concentration, can act synergistically between Chinese medicine each component, pass through soothing the liver, invigorating the spleen, moistening lung etc. side
Formula achievees the purpose that Xie Yu；Addition is condensed by 3,7- dimethyl -2,6- zinn diene aldehydes and fatty alcohol in Chinese medical extract at the same time
Obtained by 3,7- dimethyl -2,6- zinn diene aldehyde dialkoxy acetals, the addition of acetal improves that the concentrated liquid of tradition Chinese medicine drug effect is slow, controls
Treat the cycle it is long the problem of, while can in adjusting and optimizing medicinal preparation for oral administration active ingredient content, in diseases such as treatment depression and anxiety
Aspect has significant curative effect；Compared with existing commercially available anti-depression Chinese medicament or Western medicine, the existing Chinese medicine warm of medicinal preparation for oral administration of the invention and,
Side effect and stimulate the advantages of few, also have the advantages that Western medicine it is rapid-action, can immunotherapy targeted autoantibody, and cost of material is relatively low, mouth
The price of medication agent has competitiveness.
Embodiment
With reference to embodiment, the present invention is described in further detail, to make those skilled in the art with reference to specification
Word can be implemented according to this.The present invention provides a kind of medicinal preparation for oral administration containing antidepressant activity component, pass through following embodiments
And comparative example is specifically described.
Embodiment 1
The preparation of Chinese medicine extract：(1) by 8 parts by weight radix bupleuri, 5 parts by weight radix glycyrrhizaes, 5 parts by weight Chinese herbaceous peonies, 3 parts by weight jujubes
Drying is cleaned, with spare；(2) by spare Chinese medicine coarse crushing and sieve, add medicinal material weight 8 after mixing in water lift tank
When water decoction 2 again is small, filtrate is collected；(3) repeat to decoct 3 times, filter off filter residue, the filtrate after each decoct is merged；(4)
The filtrate decompression of merging is concentrated to the 1/15 of original volume, is preserved stand-by.
The preparation of antidepressant activity component：By the 3,7- dimethyl -2,6- zinn diene aldehydes of 0.1mol, 0.22mol decyl alcohol,
The acetic acid of 2mL and the ethanol of 250mL are sequentially added in reaction vessel, be heated to reflux under nitrogen protection 4~5 it is small when, reaction hold
Occur obvious layering in device, isolate lower floor's liquid, washed three times with ethanol, obtain antidepressant activity component 3,7- diformazans
Base -2,6- zinn diene aldehyde dialkoxy acetals.
The preparation of medicinal preparation for oral administration：Traditional Chinese medicine composition extract liquid and 3,7- dimethyl -2,6- zinn diene aldehydes dialkoxy are contracted
Aldehyde is matched according to the amount of volume ratio 100: 8, then is obtained containing anti-suppression after preparing common process processing needed for medicinal preparation for oral administration
The medicinal preparation for oral administration of strongly fragrant active ingredient.
Embodiment 2
The dosage of four kinds of Chinese medicines in the preparation process of the Chinese medicine extract of embodiment 1 is adjusted to：6 parts by weight radix bupleuri, 4 weights
Part radix glycyrrhizae, 4 parts by weight Chinese herbaceous peonies, 2 parts by weight jujubes are measured, remaining preparation process is same as Example 1.
Embodiment 3
Decyl alcohol in the preparation process of the antidepressant activity component of embodiment 1 is replaced with tetradecanol, remaining preparation process
It is same as Example 1.
Comparative example 1
3,7- dimethyl -2,6- zinn diene aldehyde dialkoxy acetals are added without in the preparation process of medicinal preparation for oral administration, only with
Chinese medicine extract after concentration is as antidepressant agent.
Comparative example 2
3,7- dimethyl -2,6- zinn diene aldehyde dialkoxy the acetals of 8 parts by volume and the water proportioning of 100 parts by volume is dilute
Release, prepare the medicinal preparation for oral administration for comprising only acetal.
Comparative example 3
The depressed common bavin for the treatment of is blue or green to solve strongly fragrant soup.
The effect of for antidepressant agent in testing example 1~3 and comparative example 1~3, the present invention use rat
Forced swim test and Tail suspension test investigate each antidepressant medicament respectively.
The specific experiment method of rat forced swimming test：Choose weight and be put into the depth of water in 160g~180g male rats
The beaker (40cm high, 18cm diameter) of 15cm, 25 DEG C of water temperature；Dried after prerun 15min at 32 DEG C, 24 it is small when after rat again
Be put into above-mentioned environment went swimming, wherein before swimming 24 it is small when, 4 or 5 it is small when and 1 it is small when be administered three times, measure administration group and right
The floating motionless time is kept in 5min according to group；Rat is forced in the space went swimming of a limitation, they struggle first attempts
Escape, then in a kind of motionless state, this state is referred to as " behavioral despair ", and most antidepressants can be reduced effectively
The dead time of animal, and its drug effect and clinically drug effect are significantly correlated.
The operating method of Tail suspension test：Weight 20~24g male mices are selected, the position of its tail end 2cm is attached to
On one horizontal waddy, animal is set to separate the sight of animal with plate into projecting state, its head destage face about 5cm, suspension both sides,
Before experiment 24 it is small when, 4 or 5 it is small when and 1 it is small when be administered three times, compare the dead time of administration group and control group in 6min；It is outstanding
Tail mouse is overcomes abnormal position and struggle activity, but activity is after a certain period of time, and it is motionless discontinuity occur, shows " despair " shape
State, most antidepressants can shorten the quiescent time of mouse, and its drug effect and clinically drug effect are significantly correlated.
Table 1 describe respectively by the test group of animals to medicinal preparation for oral administration in embodiment 1~3 and comparative example 1~3 and not to
The dead time of the control animals of medicine in testing, every group of experiment are all repeated 3 times record average value；By to passing through embodiment 1
The animal of~3 antidepressant agent prepared, in rat forced swimming test and Tail suspension test, its behavior " despair "
State, that is, the control group that the time remained stationary as is not administered far smaller than, illustrates that antidepression medicinal preparation for oral administration exists in the present invention
Anti-depression aspect drug effect is notable；Without addition 3,7- dimethyl -2,6- zinn diene aldehyde dialkoxies in medicinal preparation for oral administration in comparative example 1
Base acetal, in testing it, animal " despair " state for time of administration is longer than " despair " state that animal is administered in embodiment 1
Time, illustrating that the acetal is being capable of antidepressant effective active component；Only by the use of acetal as oral liquid medicine in comparative example 2, although
The dead time of animal greatly reduces after administration, but still longer compared to the dead time in embodiment 1, this explanation contracting
There is synergistic effect between Chinese medicine extract in aldehyde and the present invention, which can strengthen the antidepressant effect of liquid；
Comparative example 3 is the currently used strongly fragrant Chinese medicine of solution, is easily learnt by being contrasted with embodiment 1, according to the present invention to contain specific contracting
The antidepressant effect of the medicinal preparation for oral administration of aldehyde is more preferable.
Table 1
Although embodiment of the present invention is disclosed as above, it is not restricted in specification and embodiment listed
With it can be applied to various suitable the field of the invention completely, can be easily for those skilled in the art
Realize other modification, therefore under the universal limited without departing substantially from claim and equivalency range, it is of the invention and unlimited
In specific details.
Claims (7)
1. a kind of medicinal preparation for oral administration containing antidepressant activity component, it is characterised in that the medicinal preparation for oral administration contains Chinese medicine composition
Extracting solution and antidepressant activity component；Wherein, the Chinese medicine composition by following components by weight ratio：
The antidepressant activity component for 3,7- dimethyl made from the condensation of 3,7- dimethyl -2,6- zinn diene aldehydes and fatty alcohol -
2,6- zinn diene aldehyde dialkoxy acetals.
2. medicinal preparation for oral administration according to claim 1, it is characterised in that the preparation method of the traditional Chinese medicine composition extract liquid：
Each taste Chinese medicine is cleaned into drying, coarse crushing is simultaneously sieved, added water to cook after mixing；The water for adding 8 times of medicinal material gross weight is carried in water
In tank, decoct 2 it is small when, repeat to decoct 3 times, filter off filter residue, merging filtrate, be concentrated under reduced pressure to former filtrate volume 1/10~1/
15。
3. medicinal preparation for oral administration according to claim 1, it is characterised in that the preparation method of the antidepressant activity component：Will
The reaction solution for containing 3,7- dimethyl -2,6- zinn diene aldehyde, fatty alcohol, acetic acid and ethanol be heated to reflux 4~5 it is small when, generation
3,7- dimethyl -2,6- zinn diene aldehyde dialkoxy acetals are with reaction liquid layer and positioned at the bottom of reaction vessel, by 3,7- bis-
Washed three times with ethanol after the separation of methyl -2,6- zinn diene aldehyde dialkoxy acetal, obtain antidepressant activity component.
4. medicinal preparation for oral administration according to claim 3, it is characterised in that 3, the 7- diformazans containing 0.1mol in the reaction solution
Base -2,6- zinn diene aldehydes, the fatty alcohol of 0.2~0.22mol, the ethanol of the acetic acid of 2mL and 250mL.
5. medicinal preparation for oral administration according to claim 1, it is characterised in that the fatty alcohol is Decanol, dodecanol, 14
One or more in alkanol.
6. medicinal preparation for oral administration according to claim 1, it is characterised in that the traditional Chinese medicine composition extract liquid and antidepressant activity
The volume ratio of component is 100: 8.
7. medicinal preparation for oral administration according to claim 1, it is characterised in that honey is dissolved with the medicinal preparation for oral administration.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711349764.1A CN107951937B (en) | 2017-12-15 | 2017-12-15 | Oral preparation containing antidepressant active ingredient |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711349764.1A CN107951937B (en) | 2017-12-15 | 2017-12-15 | Oral preparation containing antidepressant active ingredient |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107951937A true CN107951937A (en) | 2018-04-24 |
| CN107951937B CN107951937B (en) | 2021-04-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711349764.1A Expired - Fee Related CN107951937B (en) | 2017-12-15 | 2017-12-15 | Oral preparation containing antidepressant active ingredient |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1531951A (en) * | 2003-03-21 | 2004-09-29 | 贵阳新天药业股份有限公司 | Chinese medicine compound preparation for nourishing the heart to calm the mind and preparing method |
| CN1731931A (en) * | 2002-10-31 | 2006-02-08 | 弗朗茨·本契奇 | Acetals as insect repellant agents |
| CN1883638A (en) * | 2006-05-31 | 2006-12-27 | 朱鸿龙 | Compound medicine for treating depression and method for preparing same |
-
2017
- 2017-12-15 CN CN201711349764.1A patent/CN107951937B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1731931A (en) * | 2002-10-31 | 2006-02-08 | 弗朗茨·本契奇 | Acetals as insect repellant agents |
| CN1531951A (en) * | 2003-03-21 | 2004-09-29 | 贵阳新天药业股份有限公司 | Chinese medicine compound preparation for nourishing the heart to calm the mind and preparing method |
| CN1883638A (en) * | 2006-05-31 | 2006-12-27 | 朱鸿龙 | Compound medicine for treating depression and method for preparing same |
Non-Patent Citations (3)
| Title |
|---|
| 张玲等: ""抑郁平胶囊抗抑郁作用机理的研究"", 《哈尔滨商业大学学报（自然科学版）》 * |
| 曹竑: "《食品添加剂》", 31 July 2004, 甘肃民族出版社 * |
| 杜彩云等: "《有机化学》", 31 December 2015, 武汉大学出版社 * |
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Granted publication date: 20210402 Termination date: 20211215 |