CN106668348A - Pharmaceutical composition for treating diabetic retinopathy - Google Patents

Pharmaceutical composition for treating diabetic retinopathy Download PDF

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Publication number
CN106668348A
CN106668348A CN201611133149.2A CN201611133149A CN106668348A CN 106668348 A CN106668348 A CN 106668348A CN 201611133149 A CN201611133149 A CN 201611133149A CN 106668348 A CN106668348 A CN 106668348A
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ethanol
weight portion
pharmaceutical composition
weight
diabetic retinopathy
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不公告发明人
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Jinan Haoyu Qingtian Medicine Technology Co ltd
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Jinan Haoyu Qingtian Medicine Technology Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/27Asclepiadaceae (Milkweed family), e.g. hoya
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/87Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/39Complex extraction schemes, e.g. fractionation or repeated extraction steps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/51Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/55Liquid-liquid separation; Phase separation

Abstract

The invention discloses a pharmaceutical composition for treating diabetic retinopathy, and a preparation method thereof. The pharmaceutical composition is prepared by compounding the following bulk pharmaceutical chemicals: parthenocissus himalayana (royle) planch, prolactin, polygalic acid, hydroxyevodiamine and jujubaside B, can be prepared into various dosage forms according to a conventional preparation process, and has a significant curative effect on treating the diabetic retinopathy.

Description

For treating the pharmaceutical composition of diabetic retinopathy
Technical field
The invention belongs to technical field of Chinese medicines, more particularly to a kind of pharmaceutical composition for treating diabetic retinopathy and Its preparation method.
Background technology
Diabetic retinopathy (diabetic retinopathy, DR) be the big diseases causing blindness of universally acknowledged four it One, with retinal vascular occlusion circulatory disturbance as major pathologic features.At present doctor trained in Western medicine is removed more to taking routine observation simple type Outside control blood glucose, special Therapeutic Method is there is no.
DR is one of common microvascular complication of diabetes, such as effectively treatment not in time, can cause blindness.Insulin Though DR can be prevented to occur, to established DR without obvious effect.Blood glucose, the blood of actively control patient are needed in treatment Pressure, blood fat situation, to avoiding increasing for clinical symptoms, prevent more complication to occur.If NO releases are reduced, ET increases Plus, then can accelerate or promote the development of DR.Primary disease belongs to the categories such as Chinese medicine " blurring of vission " " vitreous opacity ".Because it is in sugar Develop on the basis of urine disease, based on the theory of " many stasis of bloods of prolonged illness " " pathogen usually intruding into collateral in protracted disease ", because blood stasis are hindered in eyeball key, eyeball key loses supports, And cause optical fundus hypoxic-ischemic and bleeding, and it is bleeding into vitreous body and into the blood stasis from Jing, vicious cycle is formed, therefore it is clinical It was observed that mostly being recurrent exerbation the characteristics of primary disease retinal hemorrhage.
Three-jaw gold dragon:For Vitaceae Parthenocissuses plant parthenocissus himalayana Plancs Parthenocissus himalayana (Royle)Planch. the Herb of [ Ampelopsis himalayana Royle ].Autumn, winter harvesting root and stem, cut after cleaning Piece or cutting, dry.Summer, autumn picking leaves, dry.【Nature and flavor】It is pungent;Temperature.【Indication】Expelling wind and removing dampness;Dissipate blood stasis and smoothing collaterals.Main wind Pain of dampness syndrome;Traumatic injury;Fracture.【Former phytomorph】Parthenocissus himalayana Plancs fallen leaves woody climber.Multi-branched, branch is sturdy, drabon Color;Tendril is short and branch, and there is sucker on top.The lobule alternate of palmate 3;The long 5-12cm of common petiole, without hair or hairiness;Blade papery, Middle lobule is avette or width drape over one's shoulders needle-like avette, long 6-12cm, wide 2-7cm, and tip is tapering or nearly shape of tail, and base portion wedge shape, side life is little Leaf is asymmetric, tiltedly avette, and lobule is smaller compared with the middle of, and edge has substantially and the sawtooth with tip, above without hair, below or along vein There is thin pubescence;The long 5-6mm of petiolule.Flower both sexes, cyme be often born in the top of brachyplast or with leaf opposite;Bennet is compared with petiole It is short;Flower light green, 5 numbers 4 are counted sometimes;Calyx shallow disc shape, full edge;Petal Long Circle;Stamen and petal opposite;Floral disc is not obvious; Style short cylindrical shape, tip often expands discoid after petal comes off.Berry is spherical, ripe time-varying pitchy, has white lead, seed 1-2 .Record in dictionary of medicinal plant.
Hetrostemma oblongifolium Cost.:This product is dicotyledon medicine asclepiadaceae Heterostemma alatum Witht. platymiscium Hetrostemma oblongifolium Cost. Hetrostemma The Herb of oblongifolium Cost..Autumn harvests, and dries.【Nature and flavor】It is slight bitter, sweet;It is flat.【Return through】Liver Channel.【Function master Control】Lactogenic.QI and blood stasis after main product;Agalactia.【Former phytomorph】Weak winding liana.Herb has milk, and stem is by 2 row Pubescence.Leaf opposite;The long 2-4cm of petiole;Blade Long Circle, dilute ovate Long Circle, long 7.5-11cm, wide 3.5-4.5cm, tip is sharp Point, basal circular;Per side 5-7 bars, arc rises lateral vein.Umbrella shape shape cyme axil is given birth to, and long 2-3cm is blossomed 4-5;Calyx 5 Drastic crack, inner face base portion has body of gland about 10;Corolla outside light green, inner face yellow, spoke shape, diameter 1-1.5cm;Corolla splits levies 5, Cover to the right;Paracorolla five-pointed star aristiform, the every room 1 of massula, square circular, uprightly.Follicle radish fruit wire lanceolar, is up to 12cm, diameter about 1cm, it is tapering to tip.Seed is up to 2cm, wide about 3mm, white thin,tough silk matter kind hair of the seed tool up to 3cm.Flower Month phase 8-10, the fruiting period 9-12 month.Record in dictionary of medicinal plant.
Hydroxyevodiamine(Hydroxyevodiamine):CAS 1238-43-3, molecular formula C19H17N3O2, molecular weight 319.36.【Ingredient origin】Fructus Evodiae Evodia rutaecarpa..
Spine Date Seed jujubosideB(Jujuboside B):CAS 55466-05-2, molecular formula C52H84O21, molecular weight 1045.21.【Biological activity】It is anti-sweet to hide agent (1mmol/L suppresses the sweet taste of 0.2M sucrose).【Ingredient origin】Fructus Jujubae Ziziphus jujuba, Semen Ziziphi Spinosae Ziziphus jujuba var.spinosa.
Polygalacic acid(Polygalacic acid):CAS 22338-71-2, molecular formula C30H48O6, molecular weight 504.70. 【Ingredient origin】Radix Platycodoniss Platycodon grandiflorum.
3 crude drug chemical constitutions:
Spine Date Seed jujubosideB(Phytolaccasaponin B)
Hydroxyevodiamine(Hydroxyevodiamine)Polygalacic acid(Polygalacic acid).
The content of the invention
The purpose of the present invention is to overcome the shortcomings of background technology, there is provided a kind of medicine of effectively treatment diabetic retinopathy Compositions and preparation method thereof.
The present invention adopts the following technical scheme that realization:
The composition and weight portion for making the crude drug of the pharmaceutical composition of the treatment diabetic retinopathy be:
Three-jaw gold dragon 4780-4790 weight portion Hetrostemma oblongifolium Cost. 2650-2670 weight portion Polygalacic acid 30-36 weight portion hydroxyl Wus Fructus Evodiae alkali 22-26 weight portion Spine Date Seed jujubosideB 17-19 weight portions.
The pharmaceutical composition for the treatment of diabetic retinopathy is preferably used in, is by the crude drug group of following weight portion Into:
The weight of 33 weight portion Hydroxyevodiamine of three-jaw gold 2660 weight portion Polygalacic acid of imperial 4785 weight portion Hetrostemma oblongifolium Cost. 24 Part weight portion of Spine Date Seed jujubosideB 18.
A kind of pharmaceutical composition for treating diabetic retinopathy, it is characterised in that pharmaceutical composition can adopt preparation Conventional method prepares piece agent or capsule or drop pill.
A kind of pharmaceutical composition for treating diabetic retinopathy, it is characterised in that pharmaceutical composition and chemical drugs or in The treatment diabetic retinopathy medicine of medicine composition.
A kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy, it is characterised in that make as follows It is standby:
The composition and weight portion of crude drug be:Three-jaw gold dragon 4780-4790 weight portion Hetrostemma oblongifolium Cost. 2650-2670 weight portions are remote Will acid 30-36 weight portion Hydroxyevodiamine 22-26 weight portion Spine Date Seed jujubosideB 17-19 weight portions;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
Preferred a kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy, it is characterised in that by as follows It is prepared by step:
The composition and weight portion of crude drug be:The weight of 2660 weight portion Polygalacic acid of the three-jaw imperial 4785 weight portion Hetrostemma oblongifolium Cost. of gold 33 The weight portion of 24 weight portion Spine Date Seed jujubosideB of part Hydroxyevodiamine 18;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
A kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy, it is characterised in that pharmaceutical composition can To prepare piece agent or capsule or drop pill using the conventional method of galenic pharmacy.
A kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy, it is characterised in that pharmaceutical composition with Chemical drugs or Chinese medicine composition treatment diabetic retinopathy medicine.
Medicine composite for curing diabetic retinopathy is evident in efficacy.
Specific embodiment
Embodiment 1:Pharmaceutical composition for the treatment of diabetic retinopathy and preparation method thereof
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:Three-jaw gold dragon 4785g Hetrostemma oblongifolium Cost. 2660g Polygalacic acid 33g Hydroxyevodiamine 24g Spine Date Seed jujubosideB 18g;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
Embodiment 2:Pharmaceutical composition for the treatment of diabetic retinopathy and preparation method thereof
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:Three-jaw gold dragon 4780g Hetrostemma oblongifolium Cost. 2670g Polygalacic acid 30g Hydroxyevodiamine 26g Spine Date Seed jujubosideB 17g;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
Embodiment 3:Pharmaceutical composition for the treatment of diabetic retinopathy and preparation method thereof
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:Three-jaw gold dragon 4790g Hetrostemma oblongifolium Cost. 2650g Polygalacic acid 36g Hydroxyevodiamine 22g Spine Date Seed jujubosideB 19g;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
Embodiment 4:The preparation of tablet
The pharmaceutical composition 724g of Example 1, adds starch 828g, mixes, and granulation is dried, plus Microcrystalline Cellulose 250g, Hard Fat Sour magnesium 10g, mixes, and is pressed into 5000, obtains final product medicinal composition tablets.
Embodiment 5:The preparation of capsule
The pharmaceutical composition 60g of Example 2, adds starch 70g, mixes, and granulation is dried, granulate, adds appropriate magnesium stearate, Mix, encapsulated 500, obtain final product medicament composition capsule.
Embodiment 6:The preparation of drop pill
Weigh (80 DEG C) heating of polyethylene glycol 6000 213g water-baths and boil molten, add the g of 3 pharmaceutical composition of embodiment 14, fully stir Mix uniform, with liquid paraffin as coolant, put glass tubing(4*80cm)In, chilling temperature is -6 DEG C, and drip internal-and external diameter is 7.0/ 2.0 (mm/mm), drip is 2.5cm away from liquid level, and drop speed, as optimum condition, with cotton the cold of drop pill surface is blotted with per point 63 drops Solidifying agent, obtains final product medicament composition dropping pills.
Embodiment 7:The pharmaceutical composition for the treatment of diabetic retinopathy
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:
The weight portion of 30 weight portion Hydroxyevodiamine of Polygalacic acid, 20 weight portion Spine Date Seed jujubosideB 45.
Embodiment 8:The pharmaceutical composition for the treatment of diabetic retinopathy
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:
The weight portion of 20 weight portion Hydroxyevodiamine of Polygalacic acid, 20 weight portion Spine Date Seed jujubosideB 20.
Embodiment 9:The pharmaceutical composition for the treatment of diabetic retinopathy
Treatment diabetic retinopathy pharmaceutical composition crude drug composition and weight portion be:
The weight portion of 40 weight portion Hydroxyevodiamine of Polygalacic acid, 20 weight portion Spine Date Seed jujubosideB 35.
Experimental example 1:The experimental study for the treatment of diabetic retinopathy
1 clinical data
1.1 case selection
1. age 18~70 years old;2. meet the diagnosis of 2 patients with type Ⅰ DM, and meet diagnosis and the parting standard of simple type DR.
1.2 exclusion standard
1. proliferous type DR patient;2. serious refractive media muddiness person;3. systemic infection disease and malignant tumor person are merged;4. ketone Disease acidosis, hyperosmolality syndrome person;5. severe cardiac hepatic and kidney function obstacle person;6. trimester of pregnancy and women breast-feeding their children;7. once row optical fundus Laser therapy or to this class ingredient allergy sufferers;8. psychiatric patient and without independent behavior ability person;9. mismatch treatment, Person lost to follow-up before treatment end.
1.3 physical data
20 patients are pressed into into a group sequencing and are equally divided into two groups.Observation group 10, man 5, female 5;Age 50~ 68 years old, average (54.85 ± 8.14) year;The course of disease 1~5 year, average (4.12 ± 1.23) year.Matched group 10, man 5, Female 5;51~67 years old age, average (54.94 ± 8.05) year;The course of disease 1~5 year, average (4.25 ± 1.34) year.Two groups Physical data no significant difference (P > 0.05), can be contrasted.
2 methods
2.1 matched group
Carry out health education in diabetes, to nurse one's health diet and suitable exercise based on, keep it is happy, strictly give up alcohol.According to Patient's concrete condition carries out glucose-lowering treatment using oral antidiabetic drug or insulin, and the symptomatic treatment such as hypertension and hyperlipemia.
2.2 observation group
Add pharmaceutical composition on the basis of matched group(The pharmaceutical composition of embodiment 1)Treatment, orally, each 1.2g, daily 3 It is secondary.
2.3 observation item
Situation is changed using fluoroscopic visualization inspection observation patient's retinal hemorrhage, microangioma, fluorescence leakage scope.Lab testing Index is mainly monitored in fasting glucose (FPG), 2h-plasma glucose (2 hPG), T-CHOL (TC), triglyceride (TG), blood plasma Pi Su (ET-1), nitric oxide (NO) and DDi content change situation.Two groups of patients unite after continuously treating 3 months Meter curative effect.
2.4 statistical method
Data analysiss are carried out using the statistical softwares of SPSS 15. 0.Ranked data adopt rank test, measurement data to adopt t Inspection.
3 criterions of therapeutical effect and therapeutic outcome
3.1 criterion of therapeutical effect
It is effective:Retinal hemorrhage, microangioma etc. are significantly reduced, and fluorescence leakage disappears, and vision is improved earlier above more than 2 rows;
Effectively:Retinal hemorrhage, microangioma are reduced, and fluorescence leakage scope diminishes, and before vision stability or relatively treatment 1 row is improved More than;
It is invalid:Not up to above standard even adds severe one.
3. 2 Clinical efficacy comparison
As shown in table 1.Observation group and matched group total effective rate are respectively 100%, 60.00%, statistically significant (the P < of difference 0.05) 。
1 two groups of Clinical efficacy comparisons of table [ example (%) ]
Group Number of cases It is effective Effectively It is invalid Total effective rate
Observation group 10 7 3 0 100*
Matched group 10 3 3 4 60.00
Note:Compare with matched group, * P < 0.05.
3.3 blood glucose and Blood Lipid situation compare
FPG, 2hPG, TC and TG level is reduced after two groups of treatments, and with this group before treatment, difference has statistics to anticipate Adopted (P < 0.01);Compare between group, difference not statistically significant (P > 0.05).
3.4 endothelin level, nitric oxide and DDi situation of change compare
ET-1 and DDi decline after two groups of treatments, are declined with observation group and are become apparent from, and compare between group, and difference has statistics Learn meaning (P < 0.05).Two groups of NO levels are raised, and are raised with observation group and are become apparent from, and are compared between group, and difference is statistically significant (P < 0.05).

Claims (8)

1. a kind of pharmaceutical composition for treating diabetic retinopathy, it is characterised in that make the crude drug of the pharmaceutical composition Composition and weight portion be:
Three-jaw gold dragon 4780-4790 weight portion Hetrostemma oblongifolium Cost. 2650-2670 weight portion Polygalacic acid 30-36 weight portion hydroxyl Wus Fructus Evodiae alkali 22-26 weight portion Spine Date Seed jujubosideB 17-19 weight portions.
2. a kind of pharmaceutical composition for treating diabetic retinopathy according to claim 1, it is characterised in that make this The composition and weight portion of the crude drug of pharmaceutical composition be:
The weight portion of 33 weight portion Hydroxyevodiamine of three-jaw gold 2660 weight portion Polygalacic acid of imperial 4785 weight portion Hetrostemma oblongifolium Cost. 24 The weight portion of Spine Date Seed jujubosideB 18.
3. a kind of pharmaceutical composition for treating diabetic retinopathy according to claim 1, it is characterised in that medicine group Compound can adopt the conventional method of galenic pharmacy to prepare piece agent or capsule or drop pill.
4. a kind of pharmaceutical composition for treating diabetic retinopathy according to claim 1, it is characterised in that medicine group The treatment diabetic retinopathy medicine that compound is constituted with chemical drugs or Chinese medicine.
5. a kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy, it is characterised in that make as follows It is standby:
The composition and weight portion of crude drug be:Three-jaw gold dragon 4780-4790 weight portion Hetrostemma oblongifolium Cost. 2650-2670 weight portions are remote Will acid 30-36 weight portion Hydroxyevodiamine 22-26 weight portion Spine Date Seed jujubosideB 17-19 weight portions;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
6. a kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy according to claim 5, its feature It is to prepare as follows:
The composition and weight portion of crude drug be:The weight of 2660 weight portion Polygalacic acid of the three-jaw imperial 4785 weight portion Hetrostemma oblongifolium Cost. of gold 33 The weight portion of 24 weight portion Spine Date Seed jujubosideB of part Hydroxyevodiamine 18;
Preparation method:
(1)Three-jaw gold dragon, Hetrostemma oblongifolium Cost., Polygalacic acid, Hydroxyevodiamine, Spine Date Seed jujubosideB are taken by crude drug proportioning, is mixed, used Used as solvent, 32 DEG C of warm macerating are extracted the ethanol of weight percent concentration 45%, and extraction time is 8 times, and each extraction time is 48 little When, each solvent load is 39 times of crude drug gross weight, filters, and obtains medicinal residues A and extracting solution A, and extracting solution A reclaims ethanol, dense Relative density 1.05 is reduced to, is filtered, medicinal liquid is first washed with water by HP50 macroporous adsorptive resins, then dense with percentage by weight 17% ethanol solution eluting HP50 macroporous adsorptive resins are spent, the ethanol elution of weight percent concentration 17% is collected, ethanol is reclaimed, Concentrate drying, obtains final product extract A;
(2)Take step(1)Medicinal residues A, with the ethanol of weight percent concentration 71% as solvent, heating and refluxing extraction 14 times, carries every time The time is taken for 0.4 hour, each solvent load is 17 times of medicinal residues A weight, filters, obtain medicinal residues B and extracting solution B, extracting solution B is returned Ethanol is received, relative density 1.16 is concentrated into, is filtered, medicinal liquid is first washed with water by LSD632 macroporous adsorptive resins, then with again The amount ethanol solution eluting LSD632 macroporous adsorptive resins of percent concentration 86%, collect the ethanol elution of weight percent concentration 86% Liquid, reclaims ethanol, and concentrate drying obtains final product extract B;
(3)Extract A and extract B are mixed, pharmaceutical composition is obtained final product.
7. a kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy according to claim 5, its feature It is that pharmaceutical composition can adopt the conventional method of galenic pharmacy to prepare piece agent or capsule or drop pill.
8. a kind of preparation method of the pharmaceutical composition for treating diabetic retinopathy according to claim 5, its feature It is pharmaceutical composition and chemical drugs or Chinese medicine composition treatment diabetic retinopathy medicine.
CN201611133149.2A 2016-12-10 2016-12-10 Pharmaceutical composition for treating diabetic retinopathy Withdrawn CN106668348A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108186890A (en) * 2018-03-28 2018-06-22 山东中医药大学附属医院 A kind of pharmaceutical composition for treating diabetes
WO2021194110A1 (en) * 2020-03-27 2021-09-30 경희대학교 산학협력단 Composition for preventing or treating metabolic diseases, containing jujuboside a as active ingredient
CN115006421A (en) * 2022-07-01 2022-09-06 上海健康医学院 Application of jujuboside B in preparation of angiogenesis inhibiting medicine

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108186890A (en) * 2018-03-28 2018-06-22 山东中医药大学附属医院 A kind of pharmaceutical composition for treating diabetes
WO2021194110A1 (en) * 2020-03-27 2021-09-30 경희대학교 산학협력단 Composition for preventing or treating metabolic diseases, containing jujuboside a as active ingredient
CN115006421A (en) * 2022-07-01 2022-09-06 上海健康医学院 Application of jujuboside B in preparation of angiogenesis inhibiting medicine

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