CN103830258A - Medicine prepared by using epimedium as drug effect raw material for eyes - Google Patents
Medicine prepared by using epimedium as drug effect raw material for eyes Download PDFInfo
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- CN103830258A CN103830258A CN201410068587.XA CN201410068587A CN103830258A CN 103830258 A CN103830258 A CN 103830258A CN 201410068587 A CN201410068587 A CN 201410068587A CN 103830258 A CN103830258 A CN 103830258A
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Abstract
The invention discloses a medicine prepared by using epimedium as a drug effect raw material for eyes. The medicine is characterized in that icariin is used as the drug effect raw material and matched with pharmaceutical preparation auxiliaries acceptable to local eye parts to prepare the medicine preparation, wherein every 100 parts by weight of the medicine comprises 0.01-1.0 part by weight of icariin; the icariin is extracted from traditional Chinese medicine epimedium through alcohol. The medicine is exact in curative effect on treatment of age-related macular degeneration, and does not have remarkable side effects.
Description
Technical field
The present invention relates to medicinal preparation, relate in particular to the eye medicinal of preparing take Herba Epimedii as pharmacodynamic raw materials.
Background technology
Senile degeneration of macula (age-related macular degeneration, AMD), has become the blinding oculopathy that seriously jeopardizes old people.Because proportion of aged population constantly increases, the seriousness of AMD more merits attention.
AMD treatment is still a thorny difficult problem so far.Comprise vitrectomy excision SRNM, macula lutea transposition operation, photodynamic therapy (photodynamic therapy, PDT), laser therapy, intravitreal Glucocorticoid and VEGF (vascular endothelial growth factor, VEGF) method such as inhibitor, all uncertain therapeutic efficacy is cut, cost dearly, severe complication also may occur.
Modern Chinese medicine conducts extensive research treatment by Chinese herbs senile degeneration of macula, and by theory of Chinese medical science, macular area can belong to spleen meridian by the anatomical position at place, and ocular choroid belongs to heart channel.Therefore weakness of the spleen and stomach, transporting mistake department, insufficiency of vital energy and blood, malnutrition of eyes, blurring of vision; The wet fortune of losing of water, makes raw phlegm-damp, on turbid pathogen, violates, and order key, poor vision are closed in resistance; Heart deficiency of spleen-QI, has under one's command and haves no right, and outside blood oozing from the body openings or subcuta neous tissue arteries and veins, blocks clear key, vision rapid drawdown.The traditional Chinese medical science thinks that it is worn with age suffering from age-related macular degeneration, and deficiency of kidney-essence, due to spleen insufficiency.Deficiency of kidney-essence, insufficiency of the spleenly lose eyes losing nutrition and the weary source of God Light, and because void causes the stasis of blood, qi-blood-body fluid Shi Qichang road, causes punctum luteum hemorrhage, edema, is the more common chronic oculopathy relevant with aging of old people.Liver and kidney two void, deficiency-weakness of spleen-QI is that it is basic; Local pathology with bleeding due to blood-heat, expectorant stasis of blood water is wet relevant, thus in treatment often with nourishing the liver and kidney, invigorating the spleen and benefiting QI be; Cooling blood for hemostasis, blood stasis dispelling damp eliminating, promoting blood circulation to remove blood stasis is standard.Dialectical according to eye manifestation and whole body sign, carry out according to TCM Syndrome Type the very promising approach that determination for the treatment of based on pathogenesis obtained through differentiation of symptoms and signs is treatment in present age senile degeneration of macula.
Herba Epimedii be Berberidaceae herbaceos perennial stem and leaf, property acrid-sweet flavor, temperature, have effect of kidney invigorating and YANG supporting, expelling wind and removing dampness.Modern scientific research shows, Herba Epimedii mainly contains icariin and Flavonoid substances, and its function has: (1) anti-tissue ischemia, improve tissue blood circulation, and increase blood flow; (2) suppress thrombosis; (3) increase hemopoietic function; (4) strengthen immunologic function; (5) suppress hematoblastic aggreation.(6) stimulate optic nerve.Herba Epimedii is not found toxic and side effects.
Summary of the invention
The technical problem to be solved in the present invention is, makes eye medicinal take Herba Epimedii as effectiveness material, has definite curative effect by its treatment senile degeneration of macula disease, and non-evident effect.
A kind of eye medicinal of preparing take Herba Epimedii as pharmacodynamic raw materials of the present invention is take Herba Epimedii extract icariin as pharmacodynamic raw materials, be equipped with said pharmaceutical adjunct on the local acceptable pharmaceutics of eye and be prepared into pharmaceutical preparation, product specification is that the content of icariin in every 100 weight portion medicaments is 0.01～1.0 weight portion; Described icariin is the faint yellow acicular crystal powder with alcoholic extract by Herba Epimedii, and molecular weight is 676.65.
Herba Epimedii ophthalmic preparation prepared by application icariin and adjuvant comprises said any dosage form that is suitable for a local topical on eye drop, gel for eye use, spongaion or pharmaceutics.
The adjuvant of preparing Herba Epimedii ophthalmic preparation of the present invention comprises osmotic pressure regulator, pH adjusting agent, antibacterial, thickening agent, cosolvent.Their kind is selected and consumption is described below respectively.
1. in the time that the dosage form of made is eye drop or gel for eye use, raw material components also comprises antibacterial.Described antibacterial is the combination in any of any in thimerosal, quaternary ammonium salt, hibitane, chlorobutanol, parabens, sorbic acid or described kind; The consumption of antibacterial to be to be expressed as with the weight ratio of icariin, icariin: antibacterial=1.0:0.002～0.5.
2. in the time that the dosage form of made is eye drop, raw material components also comprises thickening agent.Described thickening agent is the combination in any of any or described kind in hypromellose, methylcellulose, hyaluronic acid sodium, polyvinyl alcohol, polyvinylpyrrolidone, polycarbophil, carboxymethyl cellulose, carbomer, chondroitin sulfate; The consumption of thickening agent to be to be expressed as with the weight ratio of icariin, Flos Chrysanthemi Indici glycosides: thickening agent=1.0:0.1～1.0.Can adopt different polymerization degree, finally make eye drop reach suitable viscosity.
3. in the time that the dosage form of made is gel for eye use, raw material components also comprises thickening agent; Described thickening agent is selected from the combination in any of a kind of or described kind in hypromellose, methylcellulose, hyaluronic acid sodium, polyvinyl alcohol, polyvinylpyrrolidone, carboxymethyl cellulose, carbomer, chondroitin sulfate, polycarbophil; The consumption of thickening agent to be to be expressed as with the weight ratio of icariin, icariin: thickening agent=1.0:0.5～5.0.
4. in the time that the dosage form of made is eye drop or gel for eye use, using pH adjusting agent to regulate the pH value of finished product medicament is 5.5～7.5; Described pH adjusting agent is the combination in any of any or described kind in sodium hydroxide, hydrochloric acid, sodium citrate, citric acid, boric acid, Borax.
5. in the time that the dosage form of made is eye drop, using osmotic pressure regulator to regulate the osmotic pressure molar density of eye drop is 250～350mOsmol/kg.Described osmotic pressure regulator is the combination in any of a kind of of sodium chloride, mannitol or two kinds.
6. in the time that the dosage form of made is eye drop or gel for eye use, use cosolvent to promote icariin to dissolve, described cosolvent is the combination in any of a kind of of Tween-80, castor oil hydrogenated or two kinds.
7. in the time that the dosage form of made is spongaion, raw material components also comprises the adjuvant of following kind and consumption: in the icariin of every 1 weight portion, and anhydrous lanolin 8～15 weight portions, liquid Paraffin 2～10 weight portions, Yellow Vaselin 75～95 weight portions.
The specific embodiment
The invention will be further described by the following examples.
embodiment 1extract icariin
Take Herba Epimedii 1000g, add 70% ethanol 10000ml, soak 24h, filter; Medicinal residues add 70% ethanol 5000ml, soak 24h, filter; Medicinal residues add 70% ethanol 5000ml again, soak 24h, filter; Above-mentioned 3 filtrate are merged, and heating is concentrated, until ethanol volatilization completely, injects water to 10000ml.
Absorption, eluting, make liquid after concentrated by activated macroporous resin column after treatment, icariin in liquid is adsorbed by resin column, and discards effluent, continue with water for injection with concentrated after flowing fluid ratio be that 1:1 ratio is taken water rinse resin post, discard flushing flow fluid, continue with 65% ethanol-eluting resin column, make absorption icariin thereon by till eluting completely, and collect eluent.
Decolouring adds active carbon by raw material 1～2:100, adds in eluent, continues both mixed liquor reflux 30 minutes, then cools the temperature to 60 ℃, and makes it to filter by clarification plate.
Recovery liquid is dry, reclaims the solvent in the filtrate that bleaching process makes, and remaining material, after the dry or drying under reduced pressure of spraying and get final product.
embodiment 2-4prepare Herba Epimedii eye drop
Embodiment 2-4 prepares the raw materials used component of Herba Epimedii eye drop and consumption as following table:
Preparation method is, by water for injection dissolving Herba Epimedii extract full dose, with water for injection by thickening agent disperse let cool, separately dissolve pH adjusting agent, osmotic pressure regulator, antibacterial with water for injection, stir evenly filtration, merge two liquid, add again the icariin having dissolved, add to the full amount of water for injection, filter, subpackage, to obtain final product.Using pH adjusting agent to regulate the pH value of finished product eye drop is 5.5～7.5.
embodiment 5-7prepare Herba Epimedii gel for eye use
Embodiment 5-7 prepares the raw materials used component of Herba Epimedii gel for eye use and consumption as following table:
Preparation method is, by water for injection dissolving Herba Epimedii extract full dose, to dissolve thickening agent its dispersion is let cool with water for injection, separately dissolve pH adjusting agent, antibacterial with water for injection, then add the thickening agent and the Herba Epimedii that have dissolved, benefit injects water to volume required, aseptic subpackaged, to obtain final product.Using pH adjusting agent to regulate the pH value of finished product gel for eye use is 5.5～7.5.
embodiment 8-10prepare Herba Epimedii spongaion
Embodiment 8-10 prepares the raw materials used component of Herba Epimedii spongaion and consumption as following table:
| Raw material variety | Embodiment 8 | Embodiment 9 | Embodiment 10 |
| Icariin | 0.1 gram | 1 gram | 10 grams |
| Anhydrous lanolin | 10 grams | 15 grams | 12 grams |
| Liquid Paraffin | 2 grams | 8 grams | 6 grams |
| Yellow Vaselin | 88 grams | 76 grams | 81 grams |
| Medicament specification | 0.1% Herba Epimedii spongaion | 1% Herba Epimedii spongaion | 10% Herba Epimedii spongaion |
Preparation method: dissolve Herba Epimedii extract full dose with water for injection, add in right amount through sterilizing, cooling liquid Paraffin, grind to form thin pasty state, cross 200 mesh sieves, then add gradually lanoline, Yellow Vaselin mixture aseptic, that filter, mix, to obtain final product.Usedly prepare utensil and packing container must sterilizing.
the observation of curative effect of experimental example Herba Epimedii eye drops in treatment senile degeneration of macula
By setting up the animal model of rat experiment retina photodamage, to observe the prevention effect of Herba Epimedii eye drop to senile degeneration of macula.
Research method:
120 of Sprague-Dawley (SD) rats are divided into 5 groups at random: Normal group, photic damage model group, the high, medium and low three dosage groups of Herba Epimedii eye drop.Adopt self-control lighting box (illuminance is 10800 ± 352 Lux) prolonged exposure 24 h, to set up retinal photic injury in rats model.Front 7 d of illumination start to wait respectively appearance normal saline and Herba Epimedii eye drop eye drip.7 d, 14 d, 28 d after modeling, observe retinal tissue and learn change under observation electroretinogram (ERG) change and optical microscope and perspective electron microscope.
Om observation:
Normal group: the each confluent monolayer cells marshalling of retina, even dyeing, form is normal.
Model group: the most obviously can observe the attenuation of the equal compared with normal group of each time point outer nuclear layer cell thickness, the intensity of variation maximum of 7d after modeling, and with the prolongation of time after modeling, outer nuclear layer thickness presents lasting attenuation trend, and the variation of other each cellular layers is not obvious in light Microscopic observation.Retinal mainly involves outer nuclear layer cell according to damage, shows as necrocytosis, apoptosis disappearance, and this is consistent with the result of observing of this experiment, illustrates that this experiment institute modeling type is successful.
The also compared with normal group obvious attenuation, particularly low dose group of each medication group outer nuclear layer thickness, outer nuclear layer thickness is in the obvious attenuation of 7d, but still is thicker than model group, and with the prolongation of time after modeling, do not occur that outer nuclear layer continues attenuation trend; High dose group and middle dosage group outer nuclear layer attenuation degree are less, and cell boundaries is clear, damage littlely, and difference is not obvious between the two, puts off in time, and each confluent monolayer cells structural change is little.
Transmission electron microscope observing:
Can be found out by om observation result, outer nuclear layer cell is to damage the most serious position, observes and takes pictures so Electronic Speculum is respectively organized rat retina outer nuclear layer to each time point.
Rats in normal control group outer nuclear layer cell arrangement is closely neat, clear border, even dyeing.1d after model group modeling, the obvious edema of outer nuclear layer cell, cellularity is still complete; 7d, cell occurs cracked, edema extinction; 14d, there is karyopycnosis in cell, dyes inhomogeneous; 21d, cell is cracked, dissolves disappearance; 28d, cytolysis.
Herba Epimedii eye drop administration group, outer nuclear layer cellular morphology is lighter compared with model group damage.After high, medium and low three dosage group moulds there is edema in 1d outer nuclear layer cell, and border is slightly fuzzy; 7d after mould, cell occurs cracked individually, low dose group is more obviously, but still little compared with model group damage; 14d after mould, cellular edema is disappeared gradually, still have part cell cracked, but overall structure is complete; 21d after mould, there is pyknosis in indivedual cells, dissolves, compared with 14d, cellular morphology changes little; 21d after mould, each dosage group outer nuclear layer cellular morphology and 21d difference are little.
From entirety, the each time point rat retina of each administration group outer nuclear layer cellular morphology is all complete compared with model group, and degree of injury is little, but still does not reach normal group level, still has the phenomenon of Cell apoptosis & necrosis.
Other each confluent monolayer cells of retina, comprise ganglionic cell, inner nuclear layer cell, the inside and outside joint of photoreceptor cell，photosensory cell, pigment epithelium cell etc., after modeling, under each time point transmission electron microscope, observe, cellularity integrated degree is descending presents following trend: normal group > medication group > model group, and put off in time, normal group metamorphosis is little, model group Cell apoptosis & necrosis increases gradually, and medication group cell also has damage in various degree, but little compared with model group.But from whole retina, the degree of injury of these several confluent monolayer cells is all obvious not as good as outer nuclear layer.
Claims (9)
1. an eye medicinal of preparing take Herba Epimedii as pharmacodynamic raw materials, it is characterized in that, it is take icariin as pharmacodynamic raw materials, be equipped with said pharmaceutical adjunct on the local acceptable pharmaceutics of eye and be prepared into pharmaceutical preparation, product specification is that the content of icariin in every 100 weight portion medicaments is 0.01～1.0 weight portion; Described icariin by Herba Epimedii through alcoholic extract.
2. eye medicinal according to claim 1, is characterized in that, Herba Epimedii ophthalmic preparation prepared by application icariin and adjuvant is said any dosage form that is suitable for a local topical on eye drop, gel for eye use, spongaion or pharmaceutics.
3. eye medicinal according to claim 2, is characterized in that, in the time that the dosage form of made is eye drop or gel for eye use, raw material components also comprises antibacterial; Described antibacterial is the combination in any of any in thimerosal, quaternary ammonium salt, hibitane, chlorobutanol, parabens, sorbic acid or described kind; The consumption of antibacterial to be to be expressed as with the weight ratio of icariin, icariin: antibacterial=1.0:0.002～0.5.
4. according to the eye medicinal described in claim 2 or 3, it is characterized in that, in the time that the dosage form of made is eye drop, raw material components also comprises thickening agent; Described thickening agent is the combination in any of any or described kind in hypromellose, methylcellulose, hyaluronic acid sodium, polyvinyl alcohol, polyvinylpyrrolidone, polycarbophil, carboxymethyl cellulose, carbomer, chondroitin sulfate; The consumption of thickening agent to be to be expressed as with the weight ratio of icariin, icariin: thickening agent=1.0:0.1～1.0.
5. according to the eye medicinal described in claim 2 or 3, it is characterized in that, in the time that the dosage form of made is gel for eye use, raw material components also comprises thickening agent; Described thickening agent is selected from the combination in any of a kind of or described kind in hypromellose, methylcellulose, hyaluronic acid sodium, polyvinyl alcohol, polyvinylpyrrolidone, carboxymethyl cellulose, carbomer, chondroitin sulfate, polycarbophil; The consumption of thickening agent to be to be expressed as with the weight ratio of icariin, icariin: thickening agent=1.0:0.5～5.0.
6. according to the eye medicinal described in claim 2 or 3, it is characterized in that, in the time that the dosage form of made is eye drop or gel for eye use, using pH adjusting agent to regulate the pH value of finished product medicament is 5.5～7.5; Described pH adjusting agent is the combination in any of any or described kind in sodium hydroxide, hydrochloric acid, sodium citrate, citric acid, boric acid, Borax.
7. according to the eye medicinal described in claim 2 or 3, it is characterized in that, in the time that the dosage form of made is eye drop, using osmotic pressure regulator to regulate the osmotic pressure molar density of eye drop is 250～350mOsmol/kg; Described osmotic pressure regulator is the combination in any of a kind of of sodium chloride, mannitol or two kinds.
8. according to the eye medicinal described in claim 2 or 3, it is characterized in that, in the time that the dosage form of made is eye drop or gel for eye use, use cosolvent to promote icariin to dissolve, described cosolvent is the combination in any of a kind of of Tween-80, castor oil hydrogenated or two kinds.
9. eye medicinal according to claim 2, it is characterized in that, in the time that the dosage form of made is spongaion, raw material components also comprises the adjuvant of following kind and consumption: in the icariin of every 1 weight portion, and anhydrous lanolin 8～15 weight portions, liquid Paraffin 2～10 weight portions, Yellow Vaselin 75～95 weight portions.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105920496A (en) * | 2016-05-27 | 2016-09-07 | 袁显兰 | Traditional Chinese medicine composition for macular holes |
| CN106389996A (en) * | 2016-05-27 | 2017-02-15 | 袁显兰 | Traditional Chinese medicinal composition for treating macular degeneration |
| CN107028999A (en) * | 2017-06-02 | 2017-08-11 | 广州和匠科技有限公司 | Eye-drops preparations containing barrenwort and preparation method thereof |
| CN107375197A (en) * | 2017-08-03 | 2017-11-24 | 广东莱恩医药研究院有限公司 | A kind of forsythin eye ointment and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103181941A (en) * | 2011-12-31 | 2013-07-03 | 北京东方百奥医药开发有限公司 | Application of icariin or icarisid II in preparation of medicine for preventing and curing diabetic retinopathy |
-
2014
- 2014-02-27 CN CN201410068587.XA patent/CN103830258A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103181941A (en) * | 2011-12-31 | 2013-07-03 | 北京东方百奥医药开发有限公司 | Application of icariin or icarisid II in preparation of medicine for preventing and curing diabetic retinopathy |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105920496A (en) * | 2016-05-27 | 2016-09-07 | 袁显兰 | Traditional Chinese medicine composition for macular holes |
| CN106389996A (en) * | 2016-05-27 | 2017-02-15 | 袁显兰 | Traditional Chinese medicinal composition for treating macular degeneration |
| CN107028999A (en) * | 2017-06-02 | 2017-08-11 | 广州和匠科技有限公司 | Eye-drops preparations containing barrenwort and preparation method thereof |
| CN107375197A (en) * | 2017-08-03 | 2017-11-24 | 广东莱恩医药研究院有限公司 | A kind of forsythin eye ointment and preparation method thereof |
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Application publication date: 20140604 |