CN107137421A - Dextran sulfate is preparing the application in suppressing corneal vascularization medicine - Google Patents
Dextran sulfate is preparing the application in suppressing corneal vascularization medicine Download PDFInfo
- Publication number
- CN107137421A CN107137421A CN201710376482.4A CN201710376482A CN107137421A CN 107137421 A CN107137421 A CN 107137421A CN 201710376482 A CN201710376482 A CN 201710376482A CN 107137421 A CN107137421 A CN 107137421A
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- CN
- China
- Prior art keywords
- medicine
- dextran sulfate
- corneal vascularization
- application
- active component
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/716—Glucans
Abstract
The application in suppressing corneal vascularization medicine is being prepared the invention discloses dextran sulfate, a kind of medicine for treating corneal vascularization is disclosed simultaneously, active component is dextran sulfate or its pharmaceutically acceptable salt, ester, solvate, and the valid density of active component is 2 80%.The present invention proves that dextran sulfate is a kind of potential medicine for suppressing corneal vascularization by system's test.Whole animal experiment confirms that the medicine can substantially suppress corneal vascularization, and the poisonous side effect of medicine of conventional treatment corneal vascularization is very big, limits its application, dextran sulfate has no toxic side effect.
Description
Technical field
The present invention relates to the new application of dextran sulfate, more particularly to answering in suppression corneal vascularization medicine is prepared
With.
Background technology
The formation of new vessels is the severe complication of many ophthalmic diseases, proliferative diabetic retinopathy, view
Film blood vessel blocking disease, senile macular disciform degeneration, corneal transplantation, glaucoma can cause the positions such as retina, cornea
Angiogenesis, it is associated with it ooze out, bleeding, a series of pathological changes such as hyperplasia can heavy damage eye 26S Proteasome Structure and Function,
Visual function is set to suffer damage, serious causes blindness.
The newborn active drug of ocular angiogenesis and method are not treated still clinically at present.The laser photocoagulation clinically used
Therapy can cause the serious irreversible damage of retina.Once someone was considered as dexamethasone in treatment, but effect is not obvious, and
Toxic side effect is very big, limits its application.Therefore searching can prevent and treat ocular angiogenesis new life and the small medicine of toxic side effect has
Great society and economic implications.
Dextran sulfate, molecular weight 2KD ~ 600KD, it is the polyanionically-derivatised thing of glucan, by glucan and
The esterification of chlorosulfonic acid is formed, at present, and it is mainly used in reducing blood lipid and antiatherosclerotic.
The content of the invention
The technical problem to be solved in the present invention is to provide a kind of new application of dextran sulfate, is to prepare suppression cornea
Application in angiogenesis medicament.
One new application of dextran sulfate provided by the present invention is：Dextran sulfate or its is pharmaceutically acceptable
The application of salt, ester, solvate in corneal vascularization medicine is suppressed
The present invention also provides a kind of medicine for treating corneal vascularization, its active component be dextran sulfate or its pharmaceutically may be used
Salt, ester, solvate of receiving etc..
The valid density of the active component of said medicine is 2-80%.It is preferred that, the valid density of active component is 5-30%.
Further, the valid density of active component is 10-15%.Described concentration is mass fraction, and solvent is distilled water.
The prevention that is prepared using dextran sulfate or its pharmaceutically acceptable salt, ester, solvate as active ingredient and/or
The medicine of corneal vascularization is treated, protection scope of the present invention is fallen within.
The medicine of prevention and/or the treatment corneal vascularization can pass through injection, injection, collunarium, eye drip, infiltration, suction
The method receive, physically or chemically mediated imports body such as muscle, intracutaneous, subcutaneous, vein, mucosal tissue；Or by other materials
Body is imported after mixing or parcel.
When needs, one or more pharmaceutically acceptable carriers can also be added in said medicine.It is described to carry
Body includes the conventional diluent of pharmaceutical field, excipient, filler, adhesive, wetting agent, disintegrant, sorbefacient, surface
Activating agent, absorption carrier, lubricant etc..
It is a variety of that parenteral solution, tablet, pulvis, granule, capsule, oral liquid, paste, creme etc. can be made in described medicine
Form.The medicine of above-mentioned various formulations can be prepared according to the conventional method of pharmaceutical field.
Beneficial effects of the present invention：
The present invention proves that dextran sulfate is a kind of potential medicine for suppressing corneal vascularization by system's test.Whole animal
Experiment confirms that the medicine can substantially suppress corneal vascularization.The poisonous side effect of medicine of conventional treatment corneal vascularization
It is very big, its application is limited, dextran sulfate has no toxic side effect.
Embodiment
The inhibitory action experiment of the dextran sulfate corneal angiogenesis of embodiment 1, its main experimental procedure and operation
Report in prior art CN1424030A is carried out.
1. materials and methods
1.1 material
Dextran sulfate, with the dextran sulphate solution that distilled water configuration quality fraction is 15%.
Large ear rabbit, weight 2.5-3.0kg.Two carry out cornea seam money, under anesthetic anesthesia, with 1-0 silk threads at angle
3 pins of seam above film.Rabbit is randomly divided into 2 groups, every group 10.Control group gavage distilled water, administration group gavage mass fraction is 15%
Dextran sulphate solution.3 times a day, and the volume of each gavage is 100ml.
Wistar rats, weight 280-330g, corneal central area implements alkali burns after general anesthesia, with a diameter of 5mm circle
Shape filter paper, is dipped in the 1M μ L of sodium hydroxide solution 10, is subsequently placed in cornea of rats center, is removed after 10 seconds, sterile life is used immediately
Manage normal saline washing l/min.Control group eye drip distilled water, 3 times a day, every time O.2ml；Administration component penetrates eye drip mass fraction and is
15% dextran sulphate solution, 3 times a day, each 0.2mL.
1.2 result
（1）Rabbit corneal angiogenesis is now examined with operating loupe, the number and total length of new vessels is measured.It was found that corneal suture
The 3rd day afterwards, conjunctival hyperemia, and there is new vessels to stretch into corneal limbus, there is 2-9 branch new vesselses, length in every suture upper end
Between 0.3-0.8mm, average 0.5mm.Observation to the 20th day after suture, it is seen that the number and total length of administration group new vessels compared with
Control group is significantly reduced, and the process of angiogenesis also slows down.Show that dextran sulfate can suppress the corneal vessels of suture caused rabbit
It is newborn.
（2）It is in progress with slit lamp observation cornea rebirth blood vessel, there are new vessels immersion, the new green blood of administration group in periphery at 1 week
Pipe number is significantly reduced compared with control group, and vascular occlusion is in wire after 2 weeks, until disappearing.There is vascular occlusion after 2 weeks in control group,
Blood vessel disappears after about 5 weeks.Show that dextran sulfate can suppress the cornea of rats angiogenesis caused by alkali burn.
Certainly, described above is not limitation of the present invention, and the present invention is also not limited to the example above, the art
Those of ordinary skill, the present invention essential scope in, the variations, modifications, additions or substitutions made, should all belong to the present invention
Protection domain.
Claims (5)
1. dextran sulfate is preparing the application in suppressing corneal vascularization medicine.
2. a kind of medicine for treating corneal vascularization, it is characterised in that active component be dextran sulfate or its pharmaceutically may be used
Salt, ester, the solvate of receiving.
3. medicine according to claim 2, it is characterised in that the valid density of active component is 2-80%.
4. medicine according to claim 3, it is characterised in that the valid density of active component is 5-30%.
5. medicine according to claim 3, it is characterised in that the valid density of active component is 10-15%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710376482.4A CN107137421A (en) | 2017-05-25 | 2017-05-25 | Dextran sulfate is preparing the application in suppressing corneal vascularization medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710376482.4A CN107137421A (en) | 2017-05-25 | 2017-05-25 | Dextran sulfate is preparing the application in suppressing corneal vascularization medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107137421A true CN107137421A (en) | 2017-09-08 |
Family
ID=59780077
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710376482.4A Pending CN107137421A (en) | 2017-05-25 | 2017-05-25 | Dextran sulfate is preparing the application in suppressing corneal vascularization medicine |
Country Status (1)
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| CN (1) | CN107137421A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11291684B2 (en) | 2017-05-17 | 2022-04-05 | Tx Medic Ab | Treatment of glaucoma |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1277554A (en) * | 1997-10-24 | 2000-12-20 | 克诺尔有限公司 | Use of glycosaminoglycans for producing pharmaceutical preparations for treating diabetes-associated diseases of the eye |
| CN1424030A (en) * | 2002-12-23 | 2003-06-18 | 南京医科大学 | Medicines for preventing and treating retina and cornea blood vessel diseases |
| CN106573012A (en) * | 2014-06-12 | 2017-04-19 | Tx医生公司 | The use of dextran sulfate having an average molecular weight below 10000 Da for inducing angiogenisis in a subject |
-
2017
- 2017-05-25 CN CN201710376482.4A patent/CN107137421A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1277554A (en) * | 1997-10-24 | 2000-12-20 | 克诺尔有限公司 | Use of glycosaminoglycans for producing pharmaceutical preparations for treating diabetes-associated diseases of the eye |
| CN1424030A (en) * | 2002-12-23 | 2003-06-18 | 南京医科大学 | Medicines for preventing and treating retina and cornea blood vessel diseases |
| CN106573012A (en) * | 2014-06-12 | 2017-04-19 | Tx医生公司 | The use of dextran sulfate having an average molecular weight below 10000 Da for inducing angiogenisis in a subject |
Non-Patent Citations (1)
| Title |
|---|
| CRYSTAL SHIN等: "Anti-Angiogenic Polymer Therapeutic for Corneal Neovascularization", 《ARVO ANNUAL MEETING ABSTRACT》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11291684B2 (en) | 2017-05-17 | 2022-04-05 | Tx Medic Ab | Treatment of glaucoma |
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