CN102342949B - Application of phlorhizin in preparation of drug for treating hyperuricemia - Google Patents
Application of phlorhizin in preparation of drug for treating hyperuricemia Download PDFInfo
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- CN102342949B CN102342949B CN201010246209A CN201010246209A CN102342949B CN 102342949 B CN102342949 B CN 102342949B CN 201010246209 A CN201010246209 A CN 201010246209A CN 201010246209 A CN201010246209 A CN 201010246209A CN 102342949 B CN102342949 B CN 102342949B
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Abstract
The invention belongs to the field of medicines, discloses application of phlorhizin in preparation of drug for treating hyperuricemia, and also discloses a pharmaceutical composition containing phlorhizin for treating hyperuricemia. The pharmaceutical effective ingredient of the pharmaceutical composition is a monomer compound; and at the same time, animal test shows that the compound has strong action on lowering mouse in-vivo uric acid content. The hyperuricemia animal model proves that the monomer compound (namely phlorhizin) has strong effect on lowering the uric acid level which is abnormally increased of model animals.
Description
Technical field:
The present invention relates to chemical field, relate in particular to the new purposes of dihydrochalcone glycoside monomeric compound phlorhizin (Phlorizin), the application of particularly a kind of phlorhizin in preparation treatment antihyperuricemic disease drug.
Background technology:
Gout is that long-term purine metabolism obstacle, blood uric acid increase the metabolic disease that causes; Hyperuricemia is the important biochemical basis of gout; Also become simultaneously the risk factor of numerous disease; Not only can bring out gouty arthritis like hyperuricemia, urinary calculus, urate nephropathy, and also disease such as serum uric acid level rising and abnormalities of sugar/lipid metabolism, obesity is closely related.
Should disease in Asia or Asians, compare rare in the past; Much more comparatively to see the America and Europe; But after the nineties in 20th century, regional economy such as Japan, Taiwan develop rapidly, and gout and hyperuricemia become commonly encountered diseases gradually; China the eighties in 20th century future trouble state of an illness condition also be ascendant trend year by year, hyperuricemia/gout has become the important diseases that threatens human health.
Phlorhizin structural formula, molecular formula and the american chemical article number of including (CASNo.) be as follows:
C
21H
24O
10 60-81-1
1-(2-(beta-D-Glucopyranose. oxygen base)-4,6-dihydroxy phenyl)-3-(4-hydroxy phenyl)-acetone
Phlorhizin is present in the Malus various plants, and distribution is all arranged in root, stem, leaf and fruit, belongs to the dihydrochalcone glycosides, is the higher natural non-sugar sweetener of a kind of sugariness, is a kind of ideal saccharide succedaneum for sweet food fan and diabetes patient.Phlorhizin has effect unique in the control of diabetes and complication thereof, have simultaneously the good resistance oxidant, anticancer, whiten, the blood lipid regulation effect, thereby cause people's extensive concern.But the compound monomer phlorhizin does not appear in the newspapers being used for preparation treatment antihyperuricemic disease drug and Composition Aspects thereof.
Summary of the invention:
The object of the present invention is to provide the application of a kind of phlorhizin in preparation treatment antihyperuricemic disease drug, the application of described this phlorhizin in preparation treatment antihyperuricemic disease drug will solve the single technical problem of phlorhizin purposes in the prior art.
The invention provides the application of phlorhizin in preparation treatment antihyperuricemic disease drug, phlorhizin is treated in the antihyperuricemic disease drug as unique active component in preparation.
Further, the present invention also provides the application of described phlorhizin in the medicine of the gout that preparation treatment is caused by hyperuricemia, phlorhizin in the medicine of the gout that the preparation treatment is caused by hyperuricemia as unique active component.
The present invention also provides a kind of pharmaceutical composition that is used to treat hyperuricemia, contains phlorhizin.
Further, also contain pharmaceutically acceptable carrier.
Further, described pharmaceutical dosage form is any dosage form of medically approving.
Further, described pharmaceutical dosage form is powder or injection or granule, capsule or tablet or oral liquid.
The present invention is used to prepare the pharmaceutical composition of treating hyperuricemia, and the phlorhizin chemical compound that contains the effective dose of preparation treatment hyperuricemia is an active component, and contains one or more pharmaceutically acceptable carriers; Prepare the preparation of treating hyperuricemia as active ingredient with this chemical compound, can be separately or combine with the acceptable excipient of pharmacy etc., process powder, oral liquid, capsule, granule, injection, tablets and other formulations according to conventional method.
Pharmaceutically acceptable carrier mentioned above is meant pharmaceutical carrier conventional in the pharmaceutical field, for example: diluent, excipient such as water, ethanol etc., filler such as starch, dextrin etc.; Binding agent such as cellulose derivative, alginate, gelatin and polyvinylpyrrolidone etc.; Wetting agent such as glycerol; Disintegrating agent such as calcium carbonate, sodium bicarbonate; Absorption enhancer such as quaternary ammonium compound; Surfactant such as hexadecanol; Absorption carrier such as Kaolin and soap clay; Lubricant such as Pulvis Talci, calcium stearate, magnesium stearate, Polyethylene Glycol etc.Can also in compositions, add other adjuvant in addition, like correctives etc.
The compounds of this invention can the composition forms administered through oral, snuffing is gone into, the mode of rectum or drug administration by injection is applied to the patient who needs this treatment.Be used for when oral, can be made into conventional solid preparation such as tablet, capsule, granule etc., process liquid preparation such as water or oil-suspending agent or other liquid preparation such as oral liquid, syrup etc.; When being used for rectally, can be made into unguentum, suppository etc.; When being used for drug administration by injection, can be made into injection or powder ampoule agent for injection.Preferred dosage form is tablet, capsule, suppository, spray and injection, the preparation that discharges particularly preferably in the specific part of intestinal.
The various preparations of pharmaceutical composition of the present invention can be according to the conventional production method preparation of pharmaceutical field.Active component is mixed with one or more carriers, be made into the required dosage form of preparation then.
The use amount of The compounds of this invention can be confirmed its daily dose according to variations such as the type of route of administration, patient's age, body weight, the disease of treating and the orders of severity, can use by one or many.
The present invention compares with prior art, and its effect is actively with tangible.Active ingredient of the present invention definite (monomeric compound), animal experiment shows that this chemical compound has uric acid content effect in the stronger reduction mice body simultaneously.The present invention utilizes the hyperuricemia animal model, has proved that the uric acid level that the monomeric compound phlorhizin increases the animal pattern abnormal expression has stronger reduction effect.
Description of drawings:
Fig. 1 be respectively organize uric acid in the mice after the phlorhizin administration concentration ratio than sketch map.
The specific embodiment:
Following embodiment can make those skilled in the art more fully understand the present invention, but does not limit the present invention in any way.
Laboratory animal: Kunming mouse, 24 ± 2g, male.
Medicine configuration: with purity is that 98%～100% natural product phlorhizin is dispersed in the normal saline, is used for gastric infusion, administration low dosage 15mg/kg, high dose 60mg/kg; Positive drug allopurinol 5mg/kg.
Experimental model: mice hyperuricemia model.
Experimental technique: get 50 of Kunming mouses, be divided into 5 groups at random, be respectively blank control group, model group, positive drug group, medicine high dose group, medicine low dose group.Positive drug group, medicine high dose group, medicine low dose group are distinguished administration 10 days, every day 1 time.After the last administration 1 hour, except that blank control group, all the other each treated animal lumbar injection oxonic acid potassium salt 300mg/kg cause the mice hyperuricemia.Behind the injection 1h, each treated animal is plucked eyeball and is got blood, gets determination of serum hematuria acid number, carries out group difference property relatively.
Experimental procedure:
1. kunming mice, adaptability were cultivated for 1 week (during accomplish grouping, labelling and weigh);
2. sun is distinguished administration 10 days, every day 1 time to group and each drug group; The normal control group gives solvent.
3. the last administration is after 1 hour, and except that blank control group, all the other each treated animal lumbar injection oxonic acid potassium salt 300mg/kg cause the mice hyperuricemia.Formulate inject time and strict execution of every animal of form plan.
4. inject back 1h, mice is plucked eyeball and gets blood, about 1ml.Room temperature leaves standstill more than the 1h, and 4 degree 2500r/min low-temperature centrifugations were got supernatant after 15 minutes, and are frozen in-20 degrees centigrade of refrigerators with the every pipe packing of 200ul.
5. serum uric acid concentration determination.
5.1 get serum as measuring sample;
Establish blank pipe, standard pipe and sample tube 5.2 measure, according to form liquid feeding in two steps;
5.3 each pipe of mixing, 37 ℃ of water-baths were cooled to room temperature after 5 minutes, in spectrophotometer 550nm wavelength colorimetric, with reagent blank pipe school zero, read the light absorption value of sample tube and standard pipe.
5.4, calculate the uric acid concentration of sample, uric acid (mg/L)=sample tube light absorption value/standard according to light absorption value
Pipe light absorption value * 100 (titer content)
Experimental result: the uric acid level of the low dose group of phlorhizin, high dose group, positive controls obviously reduces, and compares with model group, has significant differences
*P＜0.01, the result is as shown in Figure 1.
Claims (2)
1. the application of phlorhizin in preparation treatment antihyperuricemic disease drug, wherein phlorhizin is treated in the antihyperuricemic disease drug as unique active component in preparation.
2. the application of phlorhizin as claimed in claim 1 in preparation treatment antihyperuricemic disease drug; It is characterized in that: the application of described phlorhizin in the medicine of the gout that preparation treatment is caused by hyperuricemia, wherein phlorhizin in the medicine of the gout that the preparation treatment is caused by hyperuricemia as unique active component.
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| CN201010246209A CN102342949B (en) | 2010-08-05 | 2010-08-05 | Application of phlorhizin in preparation of drug for treating hyperuricemia |
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| CN201010246209A CN102342949B (en) | 2010-08-05 | 2010-08-05 | Application of phlorhizin in preparation of drug for treating hyperuricemia |
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| CN102342949A CN102342949A (en) | 2012-02-08 |
| CN102342949B true CN102342949B (en) | 2012-10-10 |
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| AU2014295000A1 (en) * | 2013-07-25 | 2016-02-18 | Fondazione Telethon | Inhibitors of FAPP2 and uses thereof |
| CN111533770A (en) * | 2020-05-14 | 2020-08-14 | 华侨大学 | Preparation method of arbutin in sparrow tea and application of arbutin in treating hyperuricemia |
| CN112972531A (en) * | 2021-02-23 | 2021-06-18 | 三峡大学 | Malus spectabilis tea water extract and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1880325A (en) * | 2006-04-21 | 2006-12-20 | 西斯汀财产有限公司 | Preparation and application of phlorizin composition |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1880325A (en) * | 2006-04-21 | 2006-12-20 | 西斯汀财产有限公司 | Preparation and application of phlorizin composition |
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