CN107028944A - A kind of Western medicine compound for treating gout and its application - Google Patents
A kind of Western medicine compound for treating gout and its application Download PDFInfo
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- CN107028944A CN107028944A CN201710298025.8A CN201710298025A CN107028944A CN 107028944 A CN107028944 A CN 107028944A CN 201710298025 A CN201710298025 A CN 201710298025A CN 107028944 A CN107028944 A CN 107028944A
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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Abstract
The invention discloses a kind of Western medicine compound for treating gout and its application, the active component of the Western medicine compound is in parts by weight, composed of the following components:7 11 parts of ajmalicine, 59 parts of Kaempferol, 8 12 parts of eugenol, adult's dosage are 0.4 0.48mg/kg/ days.The present invention is using ajmalicine, Kaempferol and eugenol as raw material, and the symptom for significantly improving gout, the development for delaying gout are played in each component interaction altogether, so as to contribute to the recovery from illness of patient with gout, overall clinical efficacy rate is 98 100%.Western medicine compound consumption of the present invention is few, to human body without obvious adverse reaction and toxic side effect, and efficiently solves the Commpensation And Adaptation of gout treatment medicine, and its therapeutic effect to gout does not decline because of time lengthening.
Description
Technical field
The present invention relates to technical field of western medicines, specifically a kind of Western medicine compound for treating gout and its application.
Background technology
Gout is by monosodium urate salt(MSU)Deposition caused by crystal correlation arthropathy, with purine metabolic disturbance and
(Or)Hyperuricemia caused by underexcretion is directly related, refers in particular to acute characteristic arthritis and chronic gout stone disease
Disease, mainly includes acute attack arthritis, tophus formation, tophaceous chornic arthritis, urate nephropathy and uric acid
Lithangiuria, severe one may occur in which joint deformity and renal insufficiency.Gout is often with Central obesity, hyperlipidemia, hypertension, 2 types
Diabetes and cardiovascular disease etc. are showed.
The prerequisite of gout morbidity is hyperuricemia, and therefore, hyperuricemia is the most important biochemical basis of gout,
Next to that uric acid mineralization causes inflammatory reaction.As the improvement of people's living standards, in recent years due to the change of dietary structure,
The intake increase and the reduction of muscular labor momentum of alcohol especially beer class drink, cause hyperuricemia and primary gout
The incidence of disease present and become younger in ascendant trend year by year, and age of onset.Hypersaturated state is presented due to uric acid in the disease in blood,
In addition to directly infringement is caused to bone, joint, it can also be deposited on kidney and cause nephropathy, exist to the harm of health larger
Danger, receive the extensive concern of medical field.
Mitigate symptom more than modern medicine using colchicin, allopurinol, probenecid, Benzbromarone etc., reduce blood urine
Acid, but this class Western medicine can produce gastrointestinal reaction, influence hepatic and renal function, the side effects such as leucocyte be reduced, to human body side effect
Greatly.Therefore, doctor trained in Western medicine means clinical treatment gout receives a definite limitation.
The content of the invention
It is an object of the invention to provide a kind of evident in efficacy, treatment gout without obvious adverse reaction and toxic side effect
Western medicine compound and its application.
To achieve the above object, the present invention provides following technical scheme:
A kind of Western medicine compound for treating gout, its active component is in parts by weight, composed of the following components:Ajmalicine
7-11 parts, 5-9 parts of Kaempferol, 8-12 parts of eugenol.
It is used as further scheme of the invention:Its active component is in parts by weight, composed of the following components:In Armagh
New 8-10 parts, 6-8 parts of Kaempferol, 9-11 parts of eugenol.
It is used as further scheme of the invention:Its active component is in parts by weight, composed of the following components:In Armagh
New 9 parts, 7 parts of Kaempferol, 10 parts of eugenol.
It is used as further scheme of the invention:Adult's dosage of the active component of described Western medicine compound is 0.4-
0.48mg/kg/ days.
It is used as further scheme of the invention:Adult's dosage of the active component of described Western medicine compound is
0.44mg/kg/ days.
It is used as further scheme of the invention:Described Western medicine compound is peroral dosage form.
Application of the Western medicine compound of described treatment gout in terms for the treatment of gout medicine is prepared.
The effect of component used of the invention is as follows:
Ajmalicine:Prism-shaped crystallizes (methanol).Fusing point z57T (decomposition).Optical activity l } self-important-w0 of l (r=o.s, } imitate), 1
(' 2 0.5 adjoin ua), one 39 ' (' two.25, first is liquor-saturated).Its hydrochloride is that leaflet is brilliant (ethanol), melts x 290 and flies to decompose), optically-active
Spend fa " "-l70 (r=O.s, first is liquor-saturated);Its hydrogen wave hydrochlorate is diamond crystal (methanol) fusing point 295-2960.It is present in Apocynaceae
The root of plant snakewood (Rumcn " friend er/uevri Benrh), devilpepper CR vertici (iara (Lour.)
Bails.] hh7tl } there is anti-hypertension, antibacterial and sedation.
Kaempferol:Alias Kaempferol, Kaempferol, molecular formula are C15H10O6;Water is slightly soluble in, hot ethanol, second is dissolved in
Ether and alkali.Kaempferol belongs to flavonols, and yellow needles with anticancer, suppress fertility, anti-epileptic, anti-inflammatory, antioxidant, solution
Convulsion, antiulcer, cholagogic diuretics, cough-relieving.
Eugenol:Molecular formula is C10H12O2, it is colourless or pale yellow liquid, there is strong cloves fragrance, it is water insoluble.It is main
It is used for antibacterial, hypotensive;It can also be used in perfume fragrance and various cosmetic essences and fragrance for detergents formula, can be with
Allotment for flavoring essence.
Compared with prior art, the beneficial effects of the invention are as follows:The present invention is using ajmalicine, Kaempferol and eugenol as original
Material, each component synergy plays the symptom for significantly improving gout, the development for delaying gout altogether, so as to contribute to fullying recover from an illness for patient with gout
More.Verified through clinical test, Western medicine compound of the present invention has preferable curative effect for treatment gout, and overall clinical efficacy rate is 98-
100%.Western medicine compound consumption of the present invention is few, to human body without obvious adverse reaction and toxic side effect, especially for intestinal mucosa not
Any destruction is produced, and it is evident in efficacy, improve the compliance and quality of life of patient with gout.Effectively solution of the invention
Determine the Commpensation And Adaptation of gout treatment medicine, its therapeutic effect to gout does not decline because of time lengthening.
Embodiment
Below in conjunction with the embodiment of the present invention, the technical scheme in the embodiment of the present invention is clearly and completely described,
Obviously, described embodiment is only a part of embodiment of the invention, rather than whole embodiments.Based in the present invention
Embodiment, the every other embodiment that those of ordinary skill in the art are obtained under the premise of creative work is not made, all
Belong to the scope of protection of the invention.
Embodiment 1
In the embodiment of the present invention, a kind of Western medicine compound for treating gout, its active component in parts by weight, by with the following group
It is grouped into:7 parts of ajmalicine, 5 parts of Kaempferol, 12 parts of eugenol.
Embodiment 2
In the embodiment of the present invention, a kind of Western medicine compound for treating gout, its active component in parts by weight, by with the following group
It is grouped into:11 parts of ajmalicine, 9 parts of Kaempferol, 8 parts of eugenol.
Embodiment 3
In the embodiment of the present invention, a kind of Western medicine compound for treating gout, its active component in parts by weight, by with the following group
It is grouped into:8 parts of ajmalicine, 6 parts of Kaempferol, 11 parts of eugenol.
Embodiment 4
In the embodiment of the present invention, a kind of Western medicine compound for treating gout, its active component in parts by weight, by with the following group
It is grouped into:10 parts of ajmalicine, 8 parts of Kaempferol, 9 parts of eugenol.
Embodiment 5
In the embodiment of the present invention, a kind of Western medicine compound for treating gout, its active component in parts by weight, by with the following group
It is grouped into:9 parts of ajmalicine, 7 parts of Kaempferol, 10 parts of eugenol.
In above-described embodiment, the preparation process of the Western medicine compound of described treatment gout is:With ajmalicine, Kaempferol
It is active component with eugenol, using acceptable technique and auxiliary material in pharmacy, acceptable mouth in various pharmacies is made
Oral dosage form.
Drug toxicology is tested
1st, acute toxicity test
Using peroral dosage form made from the embodiment of the present invention 5 as experiment, using gastric infusion mode, successive administration 3 times in 24h,
Per minor tick 4h, 17.6mg active components are administered every time, accumulation medicine total amount reaches 52.8mg active components/kg, faced equivalent to people
120 times of bed consumption.After administration in 7d, mouse activity, feed, normal, the well-grown of excretion, hair color light, its average body
Weight increases with the extension of experimental period.Every mouse of post mortem at 8d, visually observe the heart, liver, spleen, lung, kidney, brain,
Thymus gland, stomach, intestines etc. do not find color and paramophia, fail to measure median lethal dose(LD50).As a result show:West of the invention
Drug composition is without acute toxic reaction.
2nd, long term toxicity test
Using peroral dosage form made from the embodiment of the present invention 5 as experiment, using gastric infusion mode, by Western medicine compound of the present invention point
For low dosage, middle dosage, three groups of high dose, the drug dose of each group is respectively 6.6,13.2,26.4mg active components/kg/d,
Equivalent to clinical dosage 15,30,60 times.After gastric infusion 12 weeks, general status, blood of the Western medicine compound of the present invention to animal
Liquid index, blood parameters are without obvious influence, and Systematic anatomy, organ coefficient and histopathological examination are not also found
Abnormal pathologic changes.Drug withdrawal also has no obvious change in 2 weeks.As a result show:Western medicine compound of the present invention in long term toxicity test,
Overt toxicity reaction and delayed toxicity reaction are not found.It can be seen that, Western medicine compound non-toxic reaction of the present invention, long-term prescription safety
Reliably.
Xanthine causes Studies on Animal Models of Hyperuricemic Mice experiment
1st, experiment material
Animal:Cleaning grade Kunming mouse 80, male, 20 ± 2g;
Medicine:Peroral dosage form made from the embodiment of the present invention 5;
Xanthine:Chemical Reagent Co., Ltd., Sinopharm Group, lot number WL20101109;
Blood urine acid detection kit:Shanghai Rongsheng Bioisystech Co., Ltd, lot number 20100406.
2nd, experimental method
Kunming mouse enters behind laboratory to be randomly divided into 5 groups, i.e. Normal group, model control group, high dose group, middle dosage
Group, low dose group, weigh and number by every group 16;After adaptability is fed 1 week, gavage gives distilled water, distillation to each group respectively
Water, peroral dosage form high dose suspension(Equivalent to active component 0.24g/60ml), peroral dosage form middle dosage suspension(Equivalent to
Active component 0.12g/60ml), peroral dosage form low dosage suspension(Equivalent to active component 0.06g/60ml);Press body weight
0.3ml/10g gavages, 2 times a day, for three days on end.
1h after last gavage, Normal group intraperitoneal injection of saline 0.1ml/10g, remaining 4 groups of intraperitoneal injection 10% are yellow
Purine suspension 0.1mL/10g carries out modeling, takes blood examination to survey uric acid level and united to measurement result with plucking eyeball method after 0.5h
Meter analysis, experimental result is as shown in table 1.
As can be seen from Table 1:Studies on Animal Models of Hyperuricemic Mice success, Western medicine compound of the present invention is to mouse hyperuricemia
Model has anti-trioxypurine effect, and especially middle dose group and the effect of high dose group is stronger.
Influence of each group medicine of table 1 to Studies on Animal Models of Hyperuricemic Mice blood uric acid(N=10,±s)
Note:Compared with Normal group,*Significant difference P < 0.05 are indicated,**Indicate significant differences P <
0.01;Compared with model control group,#Significant difference P < 0.05 are indicated,##Indicate significant differences P < 0.01.
Mice caused by dimethylbenzene xylene auricle edema model experiment
1st, experiment material
Animal:Cleaning grade Kunming mouse 80, male, 20 ± 2g;
Medicine:Peroral dosage form made from the embodiment of the present invention 5;
Colchicin:Guangdong Bidi Pharmaceutical Co., Ltd, lot number 20110102;
Dimethylbenzene:Hua Chang Chemical Co., Ltd.s of Shenzhen, lot number 20090812.
2nd, experimental method
Kunming mouse enters behind laboratory to be randomly divided into 5 groups, i.e. Normal group, composition high dose group, composition middle dosage
Group, composition low dose group, colchicin group, weigh and number by every group 16;After adaptability is fed 1 week, each group difference gavage
Give distilled water, peroral dosage form high dose suspension(Equivalent to active component 0.24g/60ml), peroral dosage form middle dosage be suspended
Liquid(Equivalent to active component 0.12g/60ml), peroral dosage form low dosage suspension(Equivalent to active component 0.06g/60ml)、
Colchicin suspension(1.2mg/60ml);Body weight 0.3ml/10g gavages are pressed, 2 times a day, for three days on end.
1h after last gavage, dislocation of cervical vertebra after two sides before and after mouse right ear, 1h is uniformly applied to dimethylbenzene and is put to death, with punching
Device(D=7mm)Auricle is removed in the same position of left and right ear, is weighed, using the difference of two ears as swelling, measurement result is carried out
Statistical analysis, experimental result is as shown in table 2.
As can be seen from Table 2:Substantially, model is successful for mice auricle swelling, colchicin and Western medicine compound pair of the present invention
Mice auricle swelling model has detumescence effect and action effect is similar.
The each group medicine paraxylene of table 2 causes the influence of mice auricle swelling model(N=10,±s)
Note:Compared with Normal group, * * indicate significant differences P < 0.01.
In summary, verified by animal experiment, result of the test shows that Western medicine compound of the present invention has for gout
There is good drug effect.
Clinical test
1st, basic document
Choose the ventilation patient 350 made a definite diagnosis, wherein male 187, women 163, age 30-65 Sui, average age 46.4
Year, the course of disease -8 years 2 months, average course of disease 4.2 years;Wherein the Metatarsophalangeal joint person of swelling and ache side 252, both sides 98;Wherein
Unilateral arthritis 240, two arthralgia inflammation persons 110;The person 49 that wherein has tophus.All cases pass through inspection
Look into, and 350 wholes have blood uric acid to increase, and all patients exclude medicine and other diseases are secondary.350 patients are random
It is divided into treatment 1-5 groups, totally seven groups of control 1-2 groups, every group 50, the nothing such as sex, age, the course of disease, state of an illness weight of each group patient
Significant difference, with comparativity.
2nd, treatment method
Treatment 1-5 groups take peroral dosage form made from 1-5 of the embodiment of the present invention respectively, and 2 times a day, and early, evening is each once, each taking
With the dosage equivalent to 0.22mg active components/kg, half an hour warm boiled water after meal.15 days are 1 course for the treatment of, continuously take 2-
24 courses for the treatment of.
Compare 1 group of peroral dosage form taken and only contain two kinds of components of Kaempferol and eugenol, remaining and the complete phase of embodiment 5
Together.2 times a day, and early, evening is each once, each taking the dosage equivalent to 0.22mg active components/kg, after meal half an hour warm water
Take after mixing it with water.15 days are 1 course for the treatment of, continuously take the 2-24 course for the treatment of.
Compare 2 groups of peroral dosage forms taken and only contain a kind of component of ajmalicine, remaining is identical with embodiment 5.Often
Days 2 times, early, evening is each once, each taking the dosage equivalent to 0.22mg active components/kg, after meal half an hour warm boiled water.
15 days are 1 course for the treatment of, continuously take the 2-24 course for the treatment of.
High purine food is not fed in few activity during treatment, abstinence from alcohol.
3rd, efficacy assessment standard
(1)Recovery from illness:Clinical symptoms all disappear, and freely, blood uric acid is down to normal range (NR) to joint motion;
(2)It is effective:Clinical symptoms take a turn for the better, and flexibly, blood uric acid reduces by more than 10% to joint motion earlier above;
(3)It is invalid:Symptom and laboratory examination are unchanged.
4th, treatment results
The comparitive study of each group of table 3
By the treatment of the 2-24 course for the treatment of, the curative effect of each group is as shown in table 3:The cure rate for the treatment of group is 86-92%, total effective rate
For 98-100%;The cure rate and total effective rate of control group well below treatment group, especially compare the healing of 1 group and 2 groups of control
Rate and total effective rate sum are still significantly less than the curative effect of 5 groups for the treatment of, and it is in the mutual of each raw material to illustrate Western medicine compound of the present invention
Just there is so high cure rate and total effective rate, Western medicine compound of the present invention is applied to the treatment of gout under compatibility effect.
5th, model case
Case 1:Meng, man, 39 years old, patient's left foot toe, instep repeatability swelled and ache 2 years.Patient after once drinking, dashed forward before 2 years
So occur the left foot back of the body, thumb to swell and ache, it is difficult to fall asleep, local scorching hot redness.Take after anti-inflammation analgesic, pain is delayed after one week
Solution.I.e. easily breaking-out, takes anti-inflammation analgesic certainly after drinking or catching a cold.Medication effect is not good in this year, and pain is fixed on a left side
Instep and left thumb.Cause this onste suffered from cold before January because being lying when sleeping after drinking again, have a medical check-up:It is flushing, quite go, the left foot back of the body and thumb
Red, swollen, tenderness, function limitation.Red tongue body, yellow and greasy fur, wiry and rolling pulse number.Chemical examination:Erythrocyte sedimentation rate 84mm/h, 647 μm of ol/L of blood uric acid.Clothes
Light, panic attacks number of times of keenly feeling after 1 course for the treatment of of peroral dosage form made from the embodiment of the present invention 5, during panic attacks is few, pain hair
Make interval time long.Adhere to taking after 4 courses for the treatment of, chemical examination Uric Acid Content of having a medical check-up is down to 350 μm of ol/L, blood uric acid is normal model
Enclose the high level level in value.Continue to take after 12 courses for the treatment of, gout is not sent out always, chemical examination blood uric acid of having a medical check-up is 258 μm of ol/L, blood
Uric acid is normal level, and without recurrence sign.
Case 2:Cen, female, 52 years old, patient was the most serious in occurring finger, toes painful swelling of joints, night pain before 6 years,
Right finger anchylosis ulceration 1 year.Result of having a medical check-up is:Right hand forefinger middle finger swell and ache ulceration, also swell and ache on the inside of left foot hallux toe, night
Between pain it is more serious.There is tophus tubercle on blood uric acid 690 μm of ol/L, bitter tastes, yellow and greasy fur, wiry and frequent pulse, the right side two.Take implementation of the present invention
After 3 courses for the treatment of of peroral dosage form made from example 5, finger, toes painful swelling of joints are relaxed, and night pain number of times is reduced.Continue to take 5
The course for the treatment of, chemical examination of having a medical check-up, blood uric acid is down to 391 μm of ol/L, adheres to taking after 24 courses for the treatment of, chemical examination of having a medical check-up, and blood uric acid is 268 μ
Mol/L, recovers to blood uric acid value normal range (NR), and without recurrence sign.
It is obvious to a person skilled in the art that the invention is not restricted to the details of above-mentioned one exemplary embodiment, Er Qie
In the case of without departing substantially from spirit or essential attributes of the invention, the present invention can be realized in other specific forms.Therefore, no matter
From the point of view of which point, embodiment all should be regarded as exemplary, and be nonrestrictive, the scope of the present invention is by appended power
Profit is required rather than described above is limited, it is intended that all in the implication and scope of the equivalency of claim by falling
Change is included in the present invention.
Moreover, it will be appreciated that although the present specification is described in terms of embodiments, not each embodiment is only wrapped
Containing an independent technical scheme, this narrating mode of specification is only that for clarity, those skilled in the art should
Using specification as an entirety, the technical solutions in the various embodiments may also be suitably combined, forms those skilled in the art
It may be appreciated other embodiment.
Claims (7)
1. a kind of Western medicine compound for treating gout, it is characterised in that its active component in parts by weight, by following components
Composition:7-11 parts of ajmalicine, 5-9 parts of Kaempferol, 8-12 parts of eugenol.
2. the Western medicine compound for the treatment of gout according to claim 1, it is characterised in that its active component is according to parts by weight
Number meter, it is composed of the following components:8-10 parts of ajmalicine, 6-8 parts of Kaempferol, 9-11 parts of eugenol.
3. the Western medicine compound for the treatment of gout according to claim 2, it is characterised in that its active component is according to parts by weight
Number meter, it is composed of the following components:9 parts of ajmalicine, 7 parts of Kaempferol, 10 parts of eugenol.
4. according to the Western medicine compound of any described treatment gouts of claim 1-3, it is characterised in that described Western medicine combination
Adult's dosage of the active component of thing is 0.4-0.48mg/kg/ days.
5. the Western medicine compound for the treatment of gout according to claim 4, it is characterised in that the work of described Western medicine compound
Property composition adult's dosage be 0.44mg/kg/ days.
6. the Western medicine compound for the treatment of gout according to claim 4, it is characterised in that described Western medicine compound is mouth
Oral dosage form.
7. the Western medicine compound of the treatment gout as described in claim 1-3 is any answering in terms for the treatment of gout medicine is prepared
With.
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108096275A (en) * | 2018-01-22 | 2018-06-01 | 马艳红 | A kind of Western medicine compound for treating gout |
CN109364094A (en) * | 2018-10-30 | 2019-02-22 | 青岛大学 | It is a kind of for treating the preparation method of the pharmaceutical composition of gout |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108096275A (en) * | 2018-01-22 | 2018-06-01 | 马艳红 | A kind of Western medicine compound for treating gout |
CN109364094A (en) * | 2018-10-30 | 2019-02-22 | 青岛大学 | It is a kind of for treating the preparation method of the pharmaceutical composition of gout |
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Application publication date: 20170811 |