CN110025603A - Application of the Bavachalcone compounds in the drug of preparation treatment obesity - Google Patents
Application of the Bavachalcone compounds in the drug of preparation treatment obesity Download PDFInfo
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- CN110025603A CN110025603A CN201910406258.4A CN201910406258A CN110025603A CN 110025603 A CN110025603 A CN 110025603A CN 201910406258 A CN201910406258 A CN 201910406258A CN 110025603 A CN110025603 A CN 110025603A
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- bavachalcone
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- corylifolinin
- drug
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- BLZGPHNVMRXDCB-UXBLZVDNSA-N Bavachalcone Chemical class C1=C(O)C(CC=C(C)C)=CC(C(=O)\C=C\C=2C=CC(O)=CC=2)=C1O BLZGPHNVMRXDCB-UXBLZVDNSA-N 0.000 title claims abstract description 68
- 239000003814 drug Substances 0.000 title claims abstract description 25
- 229940079593 drug Drugs 0.000 title claims abstract description 21
- 208000008589 Obesity Diseases 0.000 title claims abstract description 19
- 235000020824 obesity Nutrition 0.000 title claims abstract description 19
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- DUWPGRAKHMEPCM-IZZDOVSWSA-N isobavachalcone Chemical compound CC(C)=CCC1=C(O)C=CC(C(=O)\C=C\C=2C=CC(O)=CC=2)=C1O DUWPGRAKHMEPCM-IZZDOVSWSA-N 0.000 claims abstract description 75
- ZUGCRBMNFSAUOC-YRNVUSSQSA-N Bavachalcone Natural products C1=C(CC=C(C)C)C(OC)=CC(O)=C1C(=O)\C=C\C1=CC=C(O)C=C1 ZUGCRBMNFSAUOC-YRNVUSSQSA-N 0.000 claims abstract description 31
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 239000002775 capsule Substances 0.000 claims description 16
- 244000226566 Psoralea corylifolia Species 0.000 claims description 13
- 239000003826 tablet Substances 0.000 claims description 12
- -1 patch Substances 0.000 claims description 7
- 239000002552 dosage form Substances 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 4
- JEIPFZHSYJVQDO-UHFFFAOYSA-N iron(III) oxide Inorganic materials O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 claims description 4
- ZCCUUQDIBDJBTK-UHFFFAOYSA-N psoralen Chemical compound C1=C2OC(=O)C=CC2=CC2=C1OC=C2 ZCCUUQDIBDJBTK-UHFFFAOYSA-N 0.000 claims description 4
- 239000000243 solution Substances 0.000 claims description 4
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- VXGRJERITKFWPL-UHFFFAOYSA-N 4',5'-Dihydropsoralen Natural products C1=C2OC(=O)C=CC2=CC2=C1OCC2 VXGRJERITKFWPL-UHFFFAOYSA-N 0.000 claims description 2
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- DQFBYFPFKXHELB-UHFFFAOYSA-N Chalcone Natural products C=1C=CC=CC=1C(=O)C=CC1=CC=CC=C1 DQFBYFPFKXHELB-UHFFFAOYSA-N 0.000 claims 1
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- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical compound CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 description 2
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- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
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- ZYGHJZDHTFUPRJ-UHFFFAOYSA-N benzo-alpha-pyrone Natural products C1=CC=C2OC(=O)C=CC2=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 description 1
- IZTUINVRJSCOIR-UHFFFAOYSA-N benzylisoquinoline Chemical class N=1C=CC2=CC=CC=C2C=1CC1=CC=CC=C1 IZTUINVRJSCOIR-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- A61K31/12—Ketones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to application of the Bavachalcone compounds in the drug of preparation treatment obesity, and the Bavachalcone compounds include the combination of any one or at least two in Corylifolinin, Corylifolinin derivative, Corylifolinin officinal salt, Bavachalcone, Bavachalcone derivative or Bavachalcone officinal salt.The invention firstly discloses digestion and absorption that Bavachalcone compounds can reduce dietary fat and then efficiently inhibiting pancreatic lipase, play effect of reducing blood lipid and treatment obesity, its significant in efficacy, Small side effects, theoretical foundation is provided to study the therapeutic strategy of obesity, provides an insertion point to prepare the drug of new treatment obesity.
Description
Technical field
The invention belongs to biomedicine fields, are related to a kind of new opplication of Bavachalcone compounds, more particularly to
A kind of application of Bavachalcone compounds in the drug of preparation treatment obesity.
Background technique
Obesity is that energy absorption and energy consumption are unbalance for a long time as a result, and the fat and a variety of metabolic disease phases of human body
It closes, such as cardiovascular disease (hyperlipidemia, hypertension, artery sclerosis), type-2 diabetes mellitus, osteoarthritis, asthma and a variety of
The cancer (liver, kidney, gall-bladder and colon) of type.Thus, it is found that and preparation reducing blood lipid and slimming medicine it is very necessary, and wherein one
A important strategy is the digestion and absorption for reducing dietary fat in digestive organs.
Pancreatic lipase (triacylglycerol Acyl- hydrolase, PL) is a kind of serine hydrolysis of key in body metabolism system
Enzyme, the triglycerides being mainly responsible in hydrolysis diet, to adjust lipid absorption.Although there are many classes in the digestive organs of human body
The lipase (lingual lipase, gastric lipase and pancreatic lipase) of type, but pancreatic lipase plays the role of overriding, can decompose
70% dietary fat triglycerides.It is more and more to study in view of key effect of the pancreatic lipase in the absorption of human body lipid
The potent inhibitor of discovery pancreatic lipase is focused on, and then prevents and treats hyperlipidemia, obesity and its correlated metabolism disease
Disease.
Pancreatic lipase inhibitor orlistat is the antiadipositas drug object for going through to list at present, has extremely outstanding pancreas rouge
Fat enzyme inhibitory effect, but orlistat and its derivative can cause the side effect that can not ignore, such as gastrointestinal toxicity, liver damage
Wound, injury of pancreas, metabolic system be abnormal and high risk of cancer.
CN101836975A discloses purposes of the isopentene group flavonoid compound as pancreatic lipase inhibitor.The compound
Chemical name be (E) -2- (2,4- dihydroxy phenyl) -5,7- dihydroxy -3- (3- methyl-2-butene base) -6- (3- methyl -
1- cyclobutenyl) -4H- benzopyran-4-one, it can extract and obtain from Artocarpus nitidus.Pancreatic lipase activity test and animal body
Interior antiobesity action experiment shows: the compound has apparent pancreatic lipase inhibitory activity and antiobesity action, and it is new to can be used as development
Prevention or treatment obesity and correlated metabolism diseases drug lead compound, it can also be used to preparation prevention or treatment are clinical
The drug of common multiple obesity and correlated metabolism diseases.
CN103642866A discloses a kind of preparation work of catechin oxypolymer with pancreatic lipase inhibiting effect
Skill, using in vitro enzymatic oxidation model, the catalytic oxidation occurred when simulating tea leaf fermentation, preparation has pancreas fat
The catechin oxypolymer of enzyme inhibition, comprising the following steps: the preparation of catechin solution, the preparation of pear juice suspension,
The preparation of catechin oxypolymer, the purification of catechin oxypolymer.The reaction speed is easy to manually control, catechin oxygen
Fluidized polymer is also easy to detect.
It is derivative that CN104447544A discloses a kind of monobenzyl isoquinoline alkaloid with pancreatic lipase inhibitory activity
Object.Such compound passes through etherificate, Henry reaction, conjugated double bond reduction, acyl using different substituted benzaldehydes as starting material
Target product is obtained at salt after change, Bischler-Napieralski cyclization and carbon-to-nitrogen double bon reduction.Part of target produces
Object can be used as the target that richer substituent group can be obtained through demethylation, debenzylation, N-alkylation and acylation reaction again in intermediate and produce
Object.This law raw material sources are simple and easy to get, and reaction condition is mild, short preparation period, and vitro enzyme Activity Screening Test removes as the result is shown
The outer target compound of a few compounds has certain pancreatic lipase inhibitory activity.
But currently, for obesity therapeutic strategy it is also seldom, therefore, develop a kind of safe and efficient pancreatic lipase
Inhibitor is very significant as the drug for treating or preventing obesity.
Summary of the invention
In view of the deficiencies of the prior art, newly answering the purpose of the present invention is to provide a kind of Bavachalcone compounds
With more particularly to a kind of Bavachalcone compounds preparation treatment obesity drug in application.
In order to achieve that object of the invention, the invention adopts the following technical scheme:
The present invention provides a kind of application of Bavachalcone compounds in the drug of preparation treatment obesity.
Psoralea corylifolia is the dry mature fruit of legumes psoraleae, and property is pungent, bitter, and temperature returns kidney, the spleen channel, is important simply
Chinese traditional herbs, meanwhile, psoralea corylifolia is also one of the herbal medicine that can be used as health food ratified at present.Psoralea corylifolia has warm kidney
Supporing yang, gas of receiving is relievingd asthma, warming spleen and stopping diarrha, and external application disappears the function of wind nti-freckle.The main chemical compositions of psoralea corylifolia include flavonoids and look into
That ketone compounds.Chalcone compounds therein can be by inhibiting pancreatic lipase to reduce dietary fat in gastrointestinal tract
Digestion and absorption, play the effect of losing weight.
Preferably, the Bavachalcone compounds include Corylifolinin, Corylifolinin derivative, psoralea corylifolia
It is any one in B prime officinal salt, Bavachalcone, Bavachalcone derivative or Bavachalcone officinal salt
Kind or at least two combination, the described at least two combination combination of such as Corylifolinin and Bavachalcone, Psoralen
Combination, Bavachalcone and combination of Bavachalcone derivative of rouge B prime and Corylifolinin officinal salt etc..
The chemical structural formula of the Corylifolinin and the chemical structural formula of Bavachalcone are as follows:
Content of the Corylifolinin in psoralea corylifolia is more than 5.8mg/g (dry weight), according to Pharmacopoeia of People's Republic of China, is mended
Bone fat is 6-10g/d at human oral dosage form, shows that the dosage of Corylifolinin can reach 58mg/d, the office in gastronintestinal system
Portion's exposed amount reaches about 44.8 μM, much higher than Corylifolinin to the inhibition constant (K of pancreatic lipasei=1.43 μM), i.e. its body
Interior drug exposure concentrations can play its high efficiency inhibited to pancreatic lipase, and then improve the digestion and suction of body fat
It receives, to achieve the purpose that reducing blood lipid and weight-reducing.
The Corylifolinin officinal salt and Bavachalcone officinal salt refer to that Corylifolinin and psoralea corylifolia are looked into
Any one in the lithium salts of your ketone, sodium salt, sylvite, magnesium salts or calcium salt.
The Bavachalcone compounds are to obtain using psoralea corylifolia as raw material through simple extract, and purity exists
90% or more can reach preferable pharmacological effect, preferably 98% or more.
Preferably, the dosage form of the drug includes tablet, powder, suspension, granule, capsule, injection, is sprayed
Agent, solution, enema, emulsion, film, suppository, patch, nasal drop or pill.
Bavachalcone compounds of the present invention, which can be administered alone arrange in pairs or groups with auxiliary material, is made into appropriate dose
Type is administered, and the auxiliary material includes diluent, excipient, filler, adhesive, wetting agent, disintegrating agent, emulsifier, hydrotropy
Any one in agent, solubilizer, osmotic pressure regulator, surfactant, pH adjusting agent, antioxidant, bacteriostatic agent or buffer
Or at least two combination.The described at least two combination combination of such as diluent and excipient, emulsifier and cosolvent
Combination, filler and adhesive and the combination of wetting agent etc..
It may include having excipient when dosage form is tablet, such as microcrystalline cellulose, starch or calcium carbonate etc.；Also it can wrap
Containing disintegrating agent, such as croscarmellose sodium etc., the effective content of Bavachalcone compounds can in unitary tablet
To be adjusted according to the actual situation, it is typically chosen in 1mg-500mg, preferably 50mg.When dosage form is capsule, can prepare
As hard capsule or soft capsule, Bavachalcone compounds and auxiliary material can be prepared into powdered or particulate filler into
Enter in capsule.When dosage form is suspension, the flavor adjustments such as corrigent, suspending agent and mouthfeel can be added.When dosage form is emulsion,
Emulsifier, cosolvent can be properly added adjust solubility, emulsifiability is administered.
Preferably, the administration route of the drug includes intravenous injection, intraperitoneal injection, intramuscular injection, subcutaneous injection, takes orally
Administration, sublingual administration, nasal-cavity administration or percutaneous dosing, are preferably administered orally.
It is generally administered orally in a manner of tablet or capsule, in addition, being administered orally with tablet or capsule
When, it can be prepared into controlled release preparation or sustained release preparation, drug effect as needed and action time, select the controlled release of suitable dose auxiliary
Material or slow-release auxiliary material.
Preferably, the Bavachalcone compounds are the Bavachalcone class chemical combination being carried on pharmaceutical carrier
Object.
Preferably, the pharmaceutical carrier includes liposome, micella, dendritic macromole, microballoon or micro-capsule.
Preferably, the Bavachalcone compounds are the Bavachalcone class chemical combination contained in pharmaceutical composition
Object.
Bavachalcone compounds of the present invention can be with other natural products or day with blood fat reducing function
Right extract carries out collocation according to different proportion and forms pharmaceutical composition, and collective effect plays effect.Such as the carbohydrate that can arrange in pairs or groups
Natural products, Coumarins natural products, flavonoids natural products, alkaloids natural products etc.；Blood can also drop with other
Rouge Drug combination, such as linoleic acid, probucol, fibrate, Hydroxymethylglutaryl list acyl coenzyme A reductase inhibit
Statins etc. in drug.
Compared with the existing technology, the invention has the following advantages:
Bavachalcone compounds of the present invention can reduce dietary fat by potent inhibition pancreatic lipase
Digestion and absorption, play reducing blood lipid and treatment obesity the effect of, inhibitory activity is very strong, and Corylifolinin and psoralea corylifolia are looked into
Inhibition constant (K of that ketone to pancreatic lipasei) it is respectively 1.43 μM and 3.17 μM；Secondly, Bavachalcone compounds
Local exposed amount is very high, 44.8 μM reachable in the part exposure of gastronintestinal system, much higher than its inhibition constant to pancreatic lipase；
Its is highly-safe, Small side effects；In addition, Bavachalcone compounds can be obtained using psoralea corylifolia as raw material through simple extraction
?.
Detailed description of the invention
Fig. 1 be in embodiment 1 remaining enzyme activity with the variation diagram of Corylifolinin concentration；
Fig. 2 be in embodiment 1 remaining enzyme activity with the variation diagram of Bavachalcone concentration；
Fig. 3 be in embodiment 2 under various concentration Corylifolinin hydrolysis reaction with concentration of substrate variation diagram；
Fig. 4 be in embodiment 2 under various concentration Bavachalcone hydrolysis reaction with concentration of substrate variation diagram；
Fig. 5 is the biological activity combination conformational map of pancreatic lipase activity center and Corylifolinin；
Fig. 6 is the biological activity combination conformational map of pancreatic lipase activity center and Bavachalcone.
Specific embodiment
The technical scheme of the invention is further explained by means of specific implementation.Those skilled in the art should be bright
, the described embodiments are merely helpful in understanding the present invention, should not be regarded as a specific limitation of the invention.
Embodiment 1
The IC that the present embodiment measurement Corylifolinin and Bavachalcone inhibit pancreatic lipase50Value.
Method particularly includes: using to 4-methyl umbelliferone oleic acid ester hydrolysis metabolic response as probe reaction, by pancreas fat
Enzyme incubated in vitro system of determination IC50Value.Pancreatic lipase is added into the phosphate buffer of 200 μ L 0.1M pH=7.4, makes end
Concentration is 2 μ g/mL, and Corylifolinin is added, makes its final concentration of 0.1 μM -100 μM, and concussion incubates 10min in advance at 37 DEG C, is obtained
Pre- liquid is incubated to a series of.It is added into 96 orifice plates and incubates liquid and substrate 4-methyl umbelliferone oleate (final concentration of 10 μM) in advance, risen
Begin to react, continuously be detected in metabolism hydrolysate 4-methyl umbelliferone of the multi-function microplate reader to 4-methyl umbelliferone oleate
40min (excitation wavelength 340nm, launch wavelength 460nm).Using the concentration of Corylifolinin as abscissa, remaining enzyme activity is
Ordinate mapping, as shown in Figure 1, calculating IC using software50Value, obtains the IC of Corylifolinin50Value is 3.30 ± 1.17 μM.
The wherein calculation formula of remaining enzyme activity are as follows:
Remaining enzyme activity (%)=(F0-F1)/F0× 100%
F0The fluorescence intensity level measured when Corylifolinin being not added in liquid to incubate in advance, F1Each concentration benefit is added in liquid to incubate in advance
The fluorescence intensity level measured when bone fat B prime.
The IC that Bavachalcone inhibits pancreatic lipase50The measuring method of value is consistent with the above, with Bavachalcone
Concentration be abscissa, remaining enzyme activity be ordinate map, as shown in Fig. 2, use software calculating IC50Value, obtains psoralea corylifolia and looks into
The IC of your ketone50Value is 5.73 ± 1.11 μM.
Embodiment 2
The K that the present embodiment measurement Corylifolinin and Bavachalcone inhibit pancreatic lipaseiValue.
Method particularly includes: using to 4-methyl umbelliferone oleic acid ester hydrolysis metabolic response as probe reaction, by pancreas fat
Enzyme incubated in vitro system of determination KiValue.Pancreatic lipase is added into the phosphate buffer of 200 μ L 0.1M pH=7.4, makes end
Concentration is 2 μ g/mL, and Corylifolinin is added, makes its final concentration of 0 μM, 4 μM, 8 μM, 16 μM, shakes at 37 DEG C and incubate in advance
10min obtains a series of pre- incubating liquid.The substrate 4-methyl umbelliferone oleate for incubating liquid and various concentration in advance is added into 96 orifice plates
(be added in different concentration of substrate groups and a series of pre- incubate liquid), starting reaction, in multi-function microplate reader to 4-methyl umbelliferone oil
The metabolism hydrolysate 4-methyl umbelliferone of acid esters continuously detects 40min (excitation wavelength 340nm, launch wavelength 460nm).
Using the concentration of 4-methyl umbelliferone oleate as abscissa, reaction rate is ordinate mapping, as shown in figure 3, using software meter
Calculate KiValue, obtains the K of CorylifolininiValue is 1.43 ± 0.43 μM.The wherein calculation formula of reaction rate are as follows:
Reaction rate (μM/min/ μ g albumen)=[(F30-F10)/45656]/t/m
F30For the fluorescence intensity level detected when 30min, F10For the fluorescence intensity level detected when 10min, t is taken
20min, m are the gross mass for participating in the pancreatic lipase of reaction.
The K that Bavachalcone inhibits pancreatic lipaseiThe measuring method of value is consistent with the above, and Bavachalcone is pre-
Incubating the final concentration in liquid is respectively 0 μM, 6 μM, 12 μM, and the concentration of 4-methyl umbelliferone oleate is abscissa, and reaction rate is
Ordinate mapping, as shown in figure 4, calculating K using softwareiValue, obtains the K of BavachalconeiValue is 3.17 ± 0.58 μM.
Embodiment 3
The present embodiment carries out molecular simulation with pancreatic lipase respectively to Corylifolinin and Bavachalcone and docks.
Method particularly includes: by Surflex-Dock software package to pancreatic lipase and Corylifolinin or Bavachalcone
Between Interactions Mode and affinity studied, generate the life of pancreatic lipase and Corylifolinin or Bavachalcone
Object activity combination conformational map, as a result as shown in Figure 5 and Figure 6.As shown in Figure 5 and Figure 6: Corylifolinin (Fig. 5) and psoralea corylifolia are looked into
Your ketone (Fig. 6) can be docked to well in the catalysis lacuna of pancreatic lipase, two kinds of inhibitor can by hydrogen bond (Fig. 5 and
Dotted line refers to hydrogen bond action in Fig. 6) with the Ser-152 and Phe-77 of pancreatic lipase (in the catalytic triads of pancreatic lipase activity center
Two key amino acids) generate strong interaction, this shows Corylifolinin and Bavachalcone to pancreatic lipase
All have very high affinity (in Fig. 5 and Fig. 6 black wire region be pancreatic lipase activity center catalytic triads Ser-152,
Phe-77 and His263).
Embodiment 4
The present embodiment research Corylifolinin and Bavachalcone slow down effect to serum lipids in rats and obesity.
Method particularly includes: 30 Adult SD male rats (weight 180g-200g) are chosen, normal group, height are randomly divided into
Pionemia group, medicine group, every group of 10 rats.Normal group is fed with normal diet, other groups are formulated institute using equivalent D12492
Manufactured high-fat, high heat food carries out limitation feeding, and every mouse feeds 20g in the 1st week, increases 2g weekly later, daily
Raising supplies in two times, no longer adds after eating up, free water, until the 8th week.In addition, medicine group was pressed since the 4th week
200mg/kg (daily afternoon), dosage oral administration gavage gave the mixture (Corylifolinin of Corylifolinin and Bavachalcone
Mass ratio with Bavachalcone is 1:1), it is carried out continuously 5 weeks (i.e. 4-8 experiment week), every 2 weeks to rat weight.At the 8th week
After, blood is taken from rat aorta, measures the content of Triglycerides in Serum.
The changes of weight situation of each group rat is as shown in table 1, from the data in the table: compared with hyperlipidemia group, giving
The mixture of rat Bavachalcone compounds can significantly inhibit being excessively increased for rat body weight.
The content situation of triglycerides is as shown in table 2 in each group rat blood serum, from the data in the table: with hyperlipidemia group
It compares, the mixture for giving rat Bavachalcone compounds can significantly reduce containing for triglycerides in rat blood
Amount.
To sum up, Bavachalcone compounds can be by inhibiting pancreatic lipase to inhibit dietary fat in gastrointestinal tract
Digestion and absorption, and then prevent and treat fat and its related metabolic diseases.
Table 1
Table 2
| Group | Number of cases | Content of triglyceride (mmol/L) |
| Normal group | 10 | 3.34±0.71 |
| Hyperlipidemia group | 10 | 5.72±1.42 |
| Medicine group | 10 | 4.06±0.71 |
Embodiment 5
The present embodiment prepares Corylifolinin tablet
20g Corylifolinin (purity is greater than 98%) is accurately weighed, is added into medical starch 180g, the two is sufficiently mixed
After be made 400 tablets, every tablet weight 0.5g, every 50mg containing Corylifolinin.
Embodiment 6
The present embodiment prepares Bavachalcone tablet
20g Bavachalcone (purity is greater than 98%) is accurately weighed, medical starch 180g is added into, the two is sufficiently mixed
400 tablets, every tablet weight 0.5g, every 50mg containing Bavachalcone are made after conjunction.
Embodiment 7
The present embodiment prepares Corylifolinin capsule
20g Corylifolinin (purity is greater than 98%) is accurately weighed, is added into medical starch 180g, the two is sufficiently mixed
Particle is made with 20 meshes afterwards, dispenses and insert Capsules later, is distributed into 400 capsules, every capsule weight 0.5g, every
Capsule 50mg containing Corylifolinin.
Embodiment 8
The present embodiment prepares Bavachalcone capsule
20g Bavachalcone (purity is greater than 98%) is accurately weighed, medical starch 180g is added into, the two is sufficiently mixed
Particle is made with 20 meshes after conjunction, dispenses and insert Capsules later, is distributed into 400 capsules, every capsule weighs 0.5g, often
Grain capsule 50mg containing Bavachalcone.
The Applicant declares that the present invention is explained by the above embodiments prepared by Bavachalcone compounds of the present invention
The application in the drug of obesity is treated, but the present invention is not limited to the above embodiments, that is, does not mean that the present invention must be according to
Bad above-described embodiment could be implemented.It should be clear to those skilled in the art, any improvement in the present invention, to this hair
The equivalence replacement of bright each raw material of product and addition, the selection of concrete mode of auxiliary element etc., all fall within protection model of the invention
Enclose within the open scope.
The preferred embodiment of the present invention has been described above in detail, still, during present invention is not limited to the embodiments described above
Detail within the scope of the technical concept of the present invention can be with various simple variants of the technical solution of the present invention are made, this
A little simple variants all belong to the scope of protection of the present invention.
It is further to note that specific technical features described in the above specific embodiments, in not lance
In the case where shield, can be combined in any appropriate way, in order to avoid unnecessary repetition, the present invention to it is various can
No further explanation will be given for the combination of energy.
Claims (7)
1. application of the Bavachalcone compounds in the drug of preparation treatment obesity.
2. application as described in claim 1, which is characterized in that the Bavachalcone compounds include psoralea corylifolia second
Element, Corylifolinin derivative, Corylifolinin officinal salt, Bavachalcone, Bavachalcone derivative or Psoralen
In rouge chalcone officinal salt any one or at least two combination.
3. application as claimed in claim 1 or 2, which is characterized in that the dosage form of the drug include tablet, powder, suspension,
Granule, capsule, injection, spray, solution, enema, emulsion, film, suppository, patch, nasal drop or pill.
4. application as claimed in any one of claims 1-3, which is characterized in that the administration route of the drug includes vein note
Penetrate, be injected intraperitoneally, intramuscular injection, subcutaneous injection, oral administration, sublingual administration, nasal-cavity administration or percutaneous dosing, preferably take orally to
Medicine.
5. such as application of any of claims 1-4, which is characterized in that the Bavachalcone compounds are negative
The Bavachalcone compounds being loaded on pharmaceutical carrier.
6. application as claimed in claim 5, which is characterized in that the pharmaceutical carrier includes that liposome, micella, dendroid are divided greatly
Son, microballoon or micro-capsule.
7. such as application of any of claims 1-6, which is characterized in that the Bavachalcone compounds are medicine
The Bavachalcone compounds contained in compositions.
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