CN109762163A

CN109762163A - It is a kind of carry Hyperoside synthesis and application method

Info

Publication number: CN109762163A
Application number: CN201910025750.7A
Authority: CN
Inventors: 张立竹; 赵玮; 章鹏轩; 陈天冬
Original assignee: Nanjing Surui Medical Technology Co Ltd
Current assignee: Nanjing Surui Medical Technology Co Ltd
Priority date: 2019-01-11
Filing date: 2019-01-11
Publication date: 2019-05-17

Abstract

The present invention provide it is a kind of carry Hyperoside synthesis and application method, and in particular to the γ-PGA (0.68g) of average molecular weight 2000 is dissolved in the 0.3N NaHCO of 60mL by Hyperoside field₃In solution, 1.8g EDCI is added, reacts 30min at 4oC；The Resocinol-phenol formaldehyde resin of 0.53g is added, ultrasonic dissolution assisting is protected from light 36h, and reaction solution dialysis 48h (Mw2000), freeze-drying obtains brown product, and is administered in a manner of oral or injection, present invention treatment colitis is not only quick, and Small side effects.

Description

It is a kind of carry Hyperoside synthesis and application method

Technical field

The invention belongs to Hyperoside fields, and in particular to it is a kind of carry Hyperoside synthesis and application method.

Background technique

Colitis (colitis) refers to that colitis venereal disease caused by a variety of causes becomes.Can by bacterium, fungi, virus, post The biologies such as infested, protozoon cause, and can also be caused by allergy and physical and chemical factor, according to cause of disease difference, can be divided into specific inflammation Venereal disease becomes and nonspecific inflammatory lesion.Existing drug therapy colitis generally passes through aminosalicylic acids, such drug side-effect It is small, but slow effect；Or glucocorticosteroid hormone is used, such effective medicine to inhibit the acute active stage inflammation of ulcerative colitis One of object, but side effect is larger；

In view of this, needing a kind of new method of new effective treatment colitis；Hyperoside also known as Quercetin -3-O- β - D- galactopyranoside.Belong to flavonols glycosides compound.Aglycon is Quercetin, and glycosyl is galactopyranose, by the 3 of Quercetin Position O atom is connected with β glycosidic bond with glycosyl, be clinically soothing liver-qi stagnation, honeysuckle in clearing heat and detoxicating prescription, Semen Cuscutae, pass through leaf The Main Flavonoids active component of Fructus Forsythiae, hawthorn etc..Hyperoside damages ischemic brain damage, myocardial damage, hepatic injury and kidney Wound has a significant protective effect, and mechanism is mainly antioxidation, Hyp in addition to it can directly remove ROS, chelated metal ions, It is also possible to increase the activity of the antioxygen enzymes such as GSH-Px, SOD, HO-1；

Summary of the invention

In view of the above deficiencies, the object of the present invention is to provide a kind of synthesis for carrying Hyperoside and application method, this method It is not only quick to treat colitis, and Small side effects.

The present invention provides the following technical solutions:

A kind of synthetic method carrying Hyperoside, its step are as follows,

S1, the γ-PGA (0.68g) by average molecular weight 2000, are dissolved in the 0.3N NaHCO of 60mL₃In solution, it is added 1.8g EDCI reacts 30min at 4 DEG C；

S2, the Resocinol-phenol formaldehyde resin that 0.53g is added, ultrasonic dissolution assisting are protected from light 36h, and reaction solution dialysis 48h (Mw2000), freeze-drying obtains brown product；

Its reactive chemistry equation is as follows:

A kind of application method carrying Hyperoside is as follows: using the agent for carrying Hyperoside treatment ulcerative colitis of synthesis Amount is 1-900mg/ days, and administration mode is oral or injection；

Preferably, the administration mode using tablet or capsule or granule or oral solution or sustained release agent is taken orally；

Preferably, wet granule compression tablet can be used in tablet；It is prepared by direct powder compression mode；It is direct that powder can be used in capsule It is encapsulated；It is prepared by the encapsulated mode of wet granulation；And the dosage of oral preparation is according to disease severity, the age of patient, body Weight, dosage 1mg between 900mg variation adjust and in single or divided doses；

Preferably, solid orally ingestible includes filler, disintegrating agent, lubricant, adhesive pharmaceutic adjuvant, and can be wrapped Clothing；

Preferably, the filler is using microcrystalline cellulose or pregelatinized starch or lactose or Icing Sugar or mannitol or phosphoric acid Hydrogen calcium or calcium sulfate；The disintegrating agent is using croscarmellose sodium or crosslinked polyvinylpyrrolidone or carboxymethyl starch Sodium or low-substituted hydroxypropyl cellulose or hydroxypropul starch or sodium bicarbonate；The lubricant is using talcum powder or stearic acid or firmly Fatty acid magnesium or calcium stearate or palmitinic acid or alumina silicate or stearmide or talcum powder.

Beneficial effects of the present invention:

This product can obviously inhibit mouse thymus index and spleen T, B to drench for internal dosage in 300mg/kg and 150mg/kg Bar cell Proliferation and Peritoneal Macrophage Phagocytosis；The increasing of mouse spleen T, bone-marrow-derived lymphocyte is then remarkably reinforced in 59mg/kg Grow the phagocytic function with peritoneal macrophage.The external dosage of Hyperoside can remarkably promote spleen T, B lymph in 50~6.25ml The proliferation of cell, enhancing T lymphocyte generates the ability of IL-2, and has apparent dose-effect relationship；When Hyperoside 6.25g/ml There is significant increasing action to Turnover of Mouse Peritoneal Macrophages phagocytosis neutrophil leucocyte ability, in 12.5~3.12 μ g/ml pair The ability that Turnover of Mouse Peritoneal Macrophages discharges NO has significant increasing action；This product has apparent guarantor to hepatic tissue and gastric mucosa Shield effect, mechanism of action and antioxidation and promote N0 level restore normally, raising SOD activity it is related；It is controlled using this product It is scorching to treat human colon, the more conducively absorption of human body is greatly improved drug effect, and Small side effects.

Specific embodiment

Embodiment 1

A kind of synthetic method carrying Hyperoside, its step are as follows,

Its reactive chemistry equation is as follows:

A kind of application method carrying Hyperoside is as follows: using the agent for carrying Hyperoside treatment ulcerative colitis of synthesis Amount is 1-900mg/ days, and administration mode is oral；It is oral to use tablet；Wet granule compression tablet can be used in tablet；Powder is directly pressed Sheet mode preparation；It is directly encapsulated that powder can be used in capsule；It is prepared by the encapsulated mode of wet granulation；And the dosage of oral preparation According to disease severity, the age of patient, weight, dosage is adjusted and one or many is given to variation between 900mg in 1mg Medicine；Solid orally ingestible includes filler, disintegrating agent, lubricant, adhesive pharmaceutic adjuvant, and can be coated；The filling Agent is using microcrystalline cellulose or pregelatinized starch or lactose or Icing Sugar or mannitol or calcium monohydrogen phosphate or calcium sulfate；The disintegrating agent Using croscarmellose sodium or crosslinked polyvinylpyrrolidone or sodium carboxymethyl starch or low-substituted hydroxypropyl cellulose Or hydroxypropul starch or sodium bicarbonate；The lubricant is using talcum powder or stearic acid or magnesium stearate or calcium stearate or palm Acid or alumina silicate or stearmide or talcum powder；

Embodiment 2

A kind of synthetic method carrying Hyperoside, its step are as follows,

Its reactive chemistry equation is as follows:

A kind of application method carrying Hyperoside is as follows: using the agent for carrying Hyperoside treatment ulcerative colitis of synthesis Amount is 1-900mg/ days, and administration mode is injection；Dose is administered to according to disease severity, the age of patient, weight, dosage 1mg between 900mg variation adjust and in single or divided doses；

This product can obviously inhibit mouse thymus index and spleen T, B to drench for internal dosage in 300mg/kg and 150mg/kg Bar cell Proliferation and Peritoneal Macrophage Phagocytosis；The increasing of mouse spleen T, bone-marrow-derived lymphocyte is then remarkably reinforced in 59mg/kg Grow the phagocytic function with peritoneal macrophage.The external dosage of Hyperoside can remarkably promote spleen T, B lymph in 50~6.25ml The proliferation of cell, enhancing T lymphocyte generates the ability of IL-2, and has apparent dose-effect relationship；When Hyperoside 6.25g/ml There is significant increasing action to Turnover of Mouse Peritoneal Macrophages phagocytosis neutrophil leucocyte ability, in 12.5~3.12 μ g/ml pair The ability that Turnover of Mouse Peritoneal Macrophages discharges NO has significant increasing action；This product has apparent guarantor to hepatic tissue and gastric mucosa Shield effect, mechanism of action and antioxidation and promote N0 level restore normally, raising SOD activity it is related；This method treatment Colitis is not only quick, and Small side effects.

These are only the preferred embodiment of the present invention, is not intended to restrict the invention, although with reference to the foregoing embodiments Invention is explained in detail, for those skilled in the art, still can be to foregoing embodiments institute The technical solution of record is modified or equivalent replacement of some of the technical features.It is all in spirit of the invention and Within principle, any modification, equivalent replacement, improvement and so on be should all be included in the protection scope of the present invention.

Claims

1. a kind of synthetic method for carrying Hyperoside, which is characterized in that synthesis step is as follows:

S1, the γ-PGA (0.68g) by average molecular weight 2000, are dissolved in the 0.3NNaHCO of 60mL₃In solution, it is added 1.8gEDCI reacts 30min at 4 DEG C；

Its reactive chemistry equation is as follows:

2. a kind of load Hyperoside application method, it is characterised in that: treat ulcerative colitis using the load Hyperoside of synthesis Dosage be 1-900mg/ days, administration mode is oral or injects.

3. a kind of load Hyperoside application method according to claim 2, it is characterised in that: oral to use tablet or capsule Or the administration mode of granule or oral solution or sustained release agent.

4. a kind of load Hyperoside application method according to claim 3, it is characterised in that: wet granulation can be used in tablet Tabletting；It is prepared by direct powder compression mode；It is directly encapsulated that powder can be used in capsule；It is prepared by the encapsulated mode of wet granulation；And The dosage of oral preparation is adjusted according to disease severity, the age of patient, weight, dosage in 1mg to variation between 900mg And in single or divided doses.

5. a kind of load Hyperoside application method according to claim 4, it is characterised in that: solid orally ingestible includes to fill out Agent, disintegrating agent, lubricant, adhesive pharmaceutic adjuvant are filled, and can be coated.

6. a kind of synthesis for carrying Hyperoside according to claim 5 and application method, it is characterised in that: the filler Using microcrystalline cellulose or pregelatinized starch or lactose or Icing Sugar or mannitol or calcium monohydrogen phosphate or calcium sulfate；The disintegrating agent is adopted With croscarmellose sodium or crosslinked polyvinylpyrrolidone or sodium carboxymethyl starch or low-substituted hydroxypropyl cellulose or Hydroxypropul starch or sodium bicarbonate；The lubricant is using talcum powder or stearic acid or magnesium stearate or calcium stearate or palmitinic acid Or alumina silicate or stearmide or talcum powder.