CN105920280A - Compound preparation for treating retinopathy and amblyopia and preparation method of compound preparation - Google Patents
Compound preparation for treating retinopathy and amblyopia and preparation method of compound preparation Download PDFInfo
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Abstract
The invention relates to a compound preparation for treating retinopathy and amblyopia and a preparation method of the compound preparation. The compound preparation comprises medicinal raw materials and medical common auxiliary materials, the raw materials include fennel, aloe, caltrop, roseleaf, fructus chebulae, mastich, operculina turpethum roots, the auxiliary materials include beta-cyclodextrin, hydroxy propyl cellulose, polyvinylpolypyrrolidone, starch, magnesium stearate and honey, and the medicinal raw materials and the medical common auxiliary materials are prepared into tablets, pills and capsules by extracting solvent, removing impurities, concentrating and drying. The compound preparation has functions of removing abnormal balgam, exhausting qi, clearing brain, improving eyesight, removing stagnancy and stopping pain, and the compound preparation is used for nyctalopia, visual deterioration, dry eye hyperdacryosis and headache. Pharmacological experiment indicates that the compound preparation can improve survival ability of oxidative stress damage model ARPE-19 (acute retinal pigment epithelitis-19) cells to different extents, relieve oxidative stress damage of the ARPE-19 cells and protect the ARPE-19 cells, and the compound preparation can protect retinopathy and amblyopia.
Description
Technical field
The present invention relates to a kind of compound preparation treating PVR and amblyopia and preparation method thereof, belong to uighur medicine and the people
Race's pharmaceutical technology field.
Background technology
Retinal pigment degeneration be receptor cell and pigment epithelial cell afunction is principal character one group chronic, carry out
Property, hereditary retinal dystrophy disease.Belong to one of internationally recognized ophthalmology difficult disease, involve eyes more.Current domestic patient
About 300,000, the whole world about 3,000,000 people, is one of the most modal blinding illness in eye.The morbidity of retinal pigment degeneration
Rate is 1/3500~1/5000, and the domestic incidence of disease is 1/4016~1/3467, and retinal pigment degeneration is the cause that developed country is main
One of blind property illness in eye.It is reported, in the crowd in 21-60 year, vision impairment that retinal pigment degeneration causes or blind be
25%-28%.The retinal pigment degeneration incidence of disease in single-gene blinding Genetic eye diseases holds pride of place.Retinal pigment degeneration
Typical case's retinal pigment degeneration and atypical retinitis pigmentosa can be divided into.The case feature that typical case's retinal pigment degeneration is clinical
For yctalopia, Progressive symmetric erythrokeratodermia visual field damage, visual impairment, electroretinogram is abnormal or calm, atypical retinitis pigmentosa
Pathological characters be progressivity yctalopia, the tiny yellow-white crystalline of retina Posterior pole, choroidal sclerosis, cornea periphery crystallization calmness.
The overwhelming majority is typical case's retinal pigment degeneration clinically.Its eyeground figure is presented with typical three and levies: osteocyte sample pigmentation,
Retinal vessel is narrower, depending on nipple color wax.Atypical retinitis pigmentosa can be divided into: retinitis pigmentosa sine pigment,
Centrality retinal pigment degeneration, fluorescent angiography in patients with crystalline retinitis pigmentosa, white point shape retinal pigment degeneration, fan-shaped retinal pigment
Sex change etc..Retinal pigment degeneration also can be divided into eyes primary pigmentary degeneration of retina, simple eye retinal pigment degeneration.Further,
Many patients with retinitis pigmentosa are associated with eye other diseases or with the other diseases outside eye disease.Belong to concurrency
Retinal pigment degeneration.Such as nerve deafness companion typical case retinal pigment degeneration Usher ' s syndrome, retinal pigment becomes
Sexual partner has cataract, and retinal pigment degeneration is with glaucoma etc..
Therefore, find anti-PVR and the effective ways of amblyopia and active drug, be current an urgent demand, have far-reaching
Meaning and great social value.At present, the medicine developed for multiple approach and link, clinically achieved with
Certain curative effect.As having a mono-interferon, p mono-interferon, potenxin, urso and virus for the medicine of chronic hepatitis
Etc.;Corticosteroid, TNF Q, Y mono-interferon, interleukin 8 quality is then had for the medicine of liver fibrosis
One 2, colchicin etc..But, although existing medicine is widely used the most clinically, but its effect still fails to reach reason
Think, and its toxic and side effect is the biggest, therefore being extremely restricted in clinical practice.
Uighur medicine has the history of thousand of years to the understanding of illness in eye, therefore, utilizes dimension doctor's dimension medicine preventing and treating PVR, weak
Depending on research the most constantly carry out in the middle of.At present, no matter at simple, or the research aspect of compound medicine and active ingredient is the most
Obtain the achievement attracted people's attention.Its mechanism of action is unlike Western medicine, the most single, unilateral, but by Mutiple Targets, too many levels,
Multipath regulation realizes, and has compound and comprehensive Therapy characteristics.Novel because of exploitation " safely, effectively, inexpensive " resists
PVR and the medicine of amblyopia, have extremely important social effect and economic valency to the control of disease and the deterioration of disease
Value, it has also become China's PVR and the inexorable trend of amblyopia Chinese medicine development.
Retinal pigment epithelium (retinal pigment epitheliu, RPE) is in retinal neuronal cell and arteries and veins
The epithelium layer of pigment is contained between network film.Major function is: controls liquid and the nutrition of subretinal space, maintains light sensation
The nutrition of receiver cell, updates, and regeneration swallows and digests the secretion of photoreceptor cell, plays blood-retina barrier
Function, maintains amphiblestroid attachment, the regeneration after damage and reparation.RPE is the vital tissue maintaining photoreceptor function.Depending on
Retinal pigment epithelial cell participates in retinal pigment degeneration, diabetic retinopathy, the disease such as age-related macular deformation
Occur and development.
ARPE-19 cell is derived from one group of cell of spontaneous immortalization in people's primary retinal pigment epithelium incubation.
Study the pattern cell being most widely used of PVR at present.There is Main Morphology and the attributive character of RPE, be to grind
Study carefully the standard cell lines system of RPE.Give external source H2O2Process the simple and easy cell membrane that cell is then research RPE oxidative damage
Type method for building up, can effectively simulate the oxidative damage process of RPE, and this part research is by giving variable concentrations H2O2Induce
The oxidative stress of ARPE-19 cell, causes cell viability to decline, and gives compound medicine process and then can improve, alleviate H2O2Right
The oxidative damage of ARPE-19 cell, inquires into a kind of compound dimension full extract of medicine to H2O2The protection of induction ARPE-19 oxidative stress
Effect and mechanism, detect intracellular MDA (malondialdehyde, MDA), superoxide dismutase (super oxide
Dismutase, SOD), GSH-Px (glutathione peroxidase, GSH-Px), compound dimension medicine complete
Extract patients before and after intervention H2O2The change of level in induction ARPE-19, and with the apoptosis-related Bax of the methodology of western,
The albumen such as Bcl-2, Caspase-3 change in this Antioxidation Mechanism.From anti-oxidant angle, compound is tieed up medicine full extract effect
And protection mechanism is illustrated, for retinal pigment degeneration treatment new idea is provided.
Summary of the invention
Present invention aim at, it is provided that a kind of compound preparation treating PVR and amblyopia and preparation method thereof, this compound medicine
Thing is by fennel seeds, aloe, puncture vine, roseleaf, terminalia flesh, smokes Lu Xiang, turpeth 7 taste medicinal material is raw material and medical science
Upper conventional auxiliary material beta cyclodextrin, hydroxypropyl cellulose, PVPP, starch, magnesium stearate and honey, use solvent to carry
Take, removal of impurities, concentrate, be dried make tablet, pill, capsule.This compound preparation has removes abnormal lymphatic temperament, scattered gas,
Brain refreshing and eyesight improving, logical stagnant, pain relieving.For yctalopia, hypopsia, the puckery many tears of mesh, headache.This compound preparation is according to Uygur
Medicine is theoretical, in conjunction with national medicine Medicinal Trait, according to the Uygur nationality in long-term clinical practice among the people, uses reasonable drawing side
Active ingredient in method dissolution preparation, strengthens drug effect, improves bioavilability.Prove through cell experiment: this compound preparation is protected
Eyesight protecting net membranochromic pigments epithelial cell, has protective effect to PVR and amblyopia.
A kind of compound preparation treating PVR and amblyopia of the present invention, said preparation is by bulk drug fennel seeds 3-30
Part, aloe 9-90 part, puncture vine 5-45 part, roseleaf 7-60 part, terminalia flesh 6-50 part, smoke Lu Xiang 3-30 part, box
Really rattan root 3-30 part, auxiliary material is beta cyclodextrin 4-10 part, hydroxypropyl cellulose 26 parts, PVPP 6 parts, starch 5
Part, magnesium stearate 1 part and honey 10-50 part are made.
Described treatment PVR and the compound preparation of amblyopia, said preparation is by bulk drug fennel seeds 3-20 part, aloe 9-60
Part, puncture vine 5-30 part, roseleaf 7-40 part, terminalia flesh 6-35 part, smoke Lu Xiang 3-20 part, turpeth 3-20 part,
Auxiliary material is beta cyclodextrin 4-10 part, hydroxypropyl cellulose 26 parts, PVPP 6 parts, starch 5 parts, magnesium stearate 1 part
Make with honey 10-40 part.
The preparation method of the compound preparation of described treatment PVR and amblyopia, follows these steps to carry out:
A, by taking aloe, turpeth through screened, smoke Lu Xiang tri-taste mixed powder and be broken into 40-200 mesh, obtain crude drug powder,
Standby;
B, fennel seeds add 6-12 times amount water, soak 5-24 hour, and the way of distillation extracts volatile oil, 5-10 hour time, distillation
After the another device of the aqueous solution collect, by every 4 parts of-10 parts of inclusions of 0.6ml-2ml volatile oil beta cyclodextrin, temperature 30 DEG C-60 DEG C,
Mixing time 30min, temperature 4 DEG C refrigerates 10 hours, filters, and temperature 40 DEG C-60 DEG C is dried, and crosses 40-100 mesh sieve,
To volatile oil clathrate compound, standby;
C, the fennel seeds dregs of a decoction and puncture vine, roseleaf, the terminalia flesh water of 6-20 times amount are extracted 1-4 time, when extracting every time
Between be 1-4 hour, obtain extract;
D, extract is filtered separate the dregs of a decoction and liquid, liquid reduced pressure concentration is become the medicinal extract of relative density 1.10-1.40, filter
Cross, obtain medicinal extract, standby;
E, medicinal extract step d obtained, be vacuum dried by temperature 30-80 DEG C, time 24-48h, obtains dry extract, then will
With the crude drug powder in step a, the volatile oil clathrate compound in step b after medicinal extract pulverizing, then it is viscous by PVPP ethanol solution
Mixture, fully mixes with auxiliary material hydroxypropyl cellulose, starch, magnesium stearate, and pharmaceutical methods is pressed into tablet routinely;
Or by the medicinal extract in step d, be vacuum dried by temperature 30-80 DEG C, time 24-48h, obtain dry extract, then by medicinal extract
With the crude drug powder in step a, the volatile oil clathrate compound in step b after pulverizing, then it is adhesive by PVPP ethanol solution,
Fully mixing with auxiliary material hydroxypropyl cellulose, starch, magnesium stearate, pharmaceutical methods makes capsule routinely;
Or by the medicinal extract in step d, be vacuum dried by temperature 30-80 DEG C, time 24-48h, obtain dry extract, then by medicinal extract
With the crude drug powder in step a, the volatile oil clathrate compound in step b after pulverizing, then it is adhesive by water or honey, fully mixes,
Pharmaceutical methods makes pill routinely.
Treatment PVR of the present invention and amblyopia compound preparation have the abnormal lymphatic temperament of removing, dissipate gas, brain refreshing and eyesight improving,
Pain relieving, logical stagnant;For yctalopia, hypopsia, the puckery many tears of mesh, purposes in the medicine such as headache.
Of the present invention a kind of treat the pharmacological property of each component in PVR and amblyopia compound preparation and be:
Aloe is that element aloe Aloe barbadensis Miller. Aloe ferox Miller Aloe ferox is drawn in liliaceous plant storehouse
Miller or other belong to the dry product of concentrated juice of kindred plant leaf together.The former practises title " old aloe " the latter and practises title " new aloe ".
Uygur medicine has raw dry heat, and soft stool rushes down clearly, anti-inflammatory detumescence, clear sore of dispeling the wind, cold-dispelling pain-relieving, and diuresis is stimulated the menstrual flow, and nourishes the liver to improve visual acuity,
Desinsection.Curing mainly raw property or lymphatic temperament disease such as, stomach is weak, constipation, and various sores are hindered, and arthralgia, yctalopia regards
Weak, irregular menstruation, difficult urination, enterozoon, 2-6g for oral administration.
Puncture vine is the dry mature fruit of zygophyllaceae plant puncture vine Tribulus terrestris L..Adopt during fruit maturation in autumn
Cut plant, dry, lay fruit, remove impurity.Uygur medicine has raw dry heat, and diuresis is stimulated the menstrual flow, improving eyesight, stone decomposing and discharging,
Relieving cough and asthma, strengthen pigment.Cure mainly raw property or lymphatic temperament disease, such as urinary obstruction, irregular menstruation, kidney stone, wing
Light calculus, gonorrhoea, cough, asthma, leucoderma, dizziness of having a headache, cataract (barrier) etc..Modern study shows,
Its main active is saponin(e and flavones ingredient, and wherein saponin component has good effect, and its to cardiovascular system
Flavones ingredient has the effect of the Rat retina Neuronal Survival promoting mixed culture, therefore puncture vine is likely developed to as protection
Eyesight, a kind of new drug for the treatment of glaucoma, 5-7g for oral administration.
Roseleaf is rosaceous plant Tujue rose Rosa damascena Mill. or rose Rosa rugusa Thunb.
It is dried petal.Spring, season initial bloom stage are gathered, and dry in the shade, and remove the impurity such as holder, calyx, dry and decayed petal.Uygur medicine has taste
Mending stomach, improve digestion, resuscitation with aromatics, ataralgesia, dissipate wind anti-inflammatory, soft intestines defaecation, moisturizing blazes.Cure mainly stomach to receive not
Good, indigestion, various tuberculosis cause deeline, neurasthenia, palpitaition, have a sleepless night, dizzy, rheumatalgia pain,
Myocarditis, hepatitis, constipation, appearance is pale.Containing multiple chemical compositions such as volatile oil, Polyphenols, flavonoids in rose,
There is minimizing and eliminate free radical, antioxidation activity, antithrombotic, anticancer, anti-inflammatory, antibacterial, immunoregulation effect, reducing blood lipid
With the prevention multiple physiologically active such as heart disease.Document report rose wate decoction is to staphylococcus aureus, typhoid bacillus and tuberculosis
Bacillus all has inhibitory action, 5-7g for oral administration.
Terminalia flesh is combretaceae plant myrobalan Terminalia chebula Retz. or what sub-Terminalia of fine hair
The dry mature fruit of chebula Retz.var.tomentella Kurt..Gather when autumn, winter two season fruit maturation, remove
Decontamination, dries.Uygur medicine has raw dry raw cold, removes abnormal bile matter and dysregulation blood matter, and brain, benefit are mended in heat-clearing
Stomach, strengthens memory, improves eyesight, and the heat that disappears is except strongly fragrant, and eliminating dampness nourishing the muscle and tendon, cool blood crow sends out.Cure mainly hot and courage matter or blood matter
Disease, as empty in hot brain, stomach void, failure of memory, eyesight reduces, hot melancholia, moist facial paralysis, blood-head white hair.Really
Real ingredient is chebulinic acid, Chebulagic acid, gallic acid, 1,3,6-trigalloylglucose, 1,2,3,4,6-five no food
Sub-acyl glucose, corilagin, terchebin, glucogallin, benzoaric acid etc., 5-7g for oral administration.
Smoke the resin that Lu Xiang is Anacardiaceae mucilaginous gum Boswellia carterii Pistacia lentiscus L., bark lengthwise is hurt, tree
Fat flows out solidification, collects, Ex-all magazine.Uygur medicine has raw dry heat, dispelling cold and eliminating dampness, nourishes dominating organs, mends stomach and disappears
Food, dissipates gas de-swelling, strengthens digestion, fragrance deodorizing etc..Curing mainly raw property or lymphatic temperament disease, void as cold in gastral cavilty, digestion are not
Good, diarrhoea abdominal distension, odontopathy halitosis etc., 5-7g for oral administration.
Turpeth is that convolvulaceous plant box fruit rattan Operculina turpethum (L.) S.Manso is dried root.Uygur medicine
Having life and do heat, remove abnormal lymphatic temperament, eliminating dampness detumescence, cold-dispelling pain-relieving, nourishing the muscle and tendon of dispeling the wind, relieving cough and asthma, except trembling with fear, solution is strongly fragrant,
Soft heavily fortified point disappears hemorrhoid, opens ear skilful etc..Cure mainly raw property or lymphatic temperament disease, such as oedema, arthralgia, Minor articulus pain, seat
Osteoneuralgia, facial paralysis, cough, asthma, melancholia, hemorrhoid, tinnitus, deaf etc..Its chemical constitution study has no report,
Character be two grades xeothermic, there is dehumidifying, drive bile effect, for oedema, hemorrhoid, arthritis, sciatica, urine not
The diseases such as profit, use warm boiled water, 5-7g for oral administration after being used for beating powder.
Accompanying drawing explanation
Fig. 1 be variable concentrations cell growth of the present invention affect figure;
Fig. 2 is the variable concentrations of the present invention impact (p < 0.01vs control) figure on cell viability;
Fig. 3 is that variable concentrations of the present invention is to H2O2(p < 0.01vs control schemes, wherein a in the impact of inducing cell viability
For without H2O2Normal group cell b is with 100 μm ol/L H2O2Inducing cell;
Fig. 4 is that the present invention is to H2O2That induces ARPE-19 cellular anti-oxidant level affects figure;
Fig. 5 is caspase-3 of the present invention, and (P < 0.05=schemes in the expression of Bcl-2, Bcl-xL albumen.
Detailed description of the invention
Embodiment 1 (with prepare 1000 as radix, prepare tablet)
A, by taking aloe, turpeth through screened, smoke Lu Xiang 3 taste mixed powder and be broken into 100 mesh, standby;
B, fennel seeds adding 12 times amount water, soak 24 hours, the way of distillation extracts volatile oil 10 hours, water-soluble after distillation
The another device of liquid is collected;Every 0.6ml volatile oil 4 parts of inclusions of betadex, temperature 30 DEG C, mixing time 30min, temperature 4
DEG C refrigeration 10 hours, filter, temperature 40 DEG C be dried, cross 80 mesh sieves, standby;
C, by the fennel seeds dregs of a decoction and puncture vine, roseleaf, the terminalia flesh water extraction 2 times of 20 times amount, each extraction time
It is 2 hours, obtains extract;
D, by extract, filter and separate the dregs of a decoction and liquid, liquid reduced pressure concentration is become the medicinal extract of relative density 1.30, filter,
Obtain medicinal extract, standby;
E, by medicinal extract, be vacuum dried with temperature 60 C, time 24-48h, obtain dry extract, then after medicinal extract is pulverized with step
Crude drug powder in rapid a, the volatile oil clathrate compound in step b, then be adhesive by PVPP ethanol solution, with auxiliary material hydroxyl
Propyl cellulose, starch, magnesium stearate fully mix, routinely pharmaceutical methods make every 0.3g, 0.4g, 0.45g or
The tablet (table 1) of 0.5g.
Table 1
Embodiment 2 (preparing 1000 is radix, prepares capsule)
A, by taking aloe, turpeth through screened, smoke Lu Xiang tri-taste mixed powder and be broken into 120 mesh, standby;
B, fennel seeds adding 10 times amount water, soak 6 hours, the way of distillation extracts volatile oil 6 hours, the aqueous solution after distillation
Another device is collected;Every 0.6ml volatile oil 5 parts of inclusions of betadex, temperature 40 DEG C, mixing time 20min, refrigerate 4 DEG C
12 hours, filtering, 50 DEG C are dried, and cross 100 mesh sieves, standby;
C, the fennel seeds dregs of a decoction and puncture vine, roseleaf, the terminalia flesh water extraction 3 times of 16 times amount, each extraction time is
1.5 hours, obtain extract;
D, by Aqueous extracts, filter and separate the dregs of a decoction and liquid, liquid reduced pressure concentration is become the medicinal extract of relative density 1.35, filter,
Obtain medicinal extract, standby;
E, by medicinal extract, with temperature 55 DEG C vacuum drying, time 24-48h, obtain dry extract, then after medicinal extract is pulverized with step
Crude drug powder in rapid a, the volatile oil clathrate compound in step b, then be adhesive by PVPP ethanol solution, with auxiliary material hydroxyl
Propyl cellulose, starch, magnesium stearate fully mix, routinely pharmaceutical methods make every 0.25g, 0.3g, 0.35g or
The hard shell capsules (table 2) of 0.4g.
Table 2
Embodiment 3 (to prepare 1000 as radix, prepare pill)
A, by above seven tastes through having screened, take aloe, turpeth, smoke Lu Xiang tri-taste mixed powder and be broken into 80 mesh, standby;
B, fennel seeds adding 8 times amount water, soak 4 hours, the way of distillation extracts volatile oil 4 hours, the aqueous solution after distillation
Another device is collected, every 6 parts of inclusions of 0.6ml volatile oil betadex, temperature 40 DEG C, mixing time 40min, temperature 4
DEG C refrigeration 8 hours, filter, temperature 45 C is dried, cross 80 mesh sieves, standby;
C, by the fennel seeds dregs of a decoction and puncture vine, roseleaf, the terminalia flesh water extraction 2 times of 18 times amount, each extraction time
It is 2 hours, obtains extract;
D, by Aqueous extracts, filter and separate the dregs of a decoction and liquid, liquid reduced pressure concentration is become the medicinal extract of relative density 1.25, filter,
Obtain medicinal extract, standby;
E, by medicinal extract, with temperature 54 DEG C vacuum drying, time 24-48h, obtain dry extract, then after medicinal extract is pulverized with step
Crude drug powder in rapid a, the volatile oil clathrate compound in step b, then honey is fully mixed, pharmaceutical methods makes every routinely
The pill (table 3) of 0.1g, 0.15g, 0.2g, 0.3g or 2g.
Table 3
Embodiment 4 (impact of compound preparation cell viability)
By ARPE-19 cell with 2 × 106/ well is inoculated in 6 orifice plates, temperature 37 DEG C, 5%CO2Incubator cultivates 6h extremely
Nearly Fusion Strain, addition ultimate density is 0 μ g/mL, 10 μ g/mL, 20 μ g/mL, 40 μ g/mL, 80 μ g/mL
The amino acid of compound preparation and culture medium (the DMEM)/F12 culture medium of glucose, temperature 37 DEG C, 5% CO2gas incubator
Cultivate 6h, discard culture medium, then with 100 μm ol/L H2O2Induction ARPE-19 cell 18h, collects each hole ARPE-19
Cell, adds cell pyrolysis liquid, and 4 DEG C of refrigerated centrifuge 12000rpm are centrifuged 5 minutes, is transferred to by supernatant clean centrifugal
Guan Zhong, temperature-80 DEG C preservation, carry out MDA (MDA), superoxide dismutase (SOD), glutathione peroxidase
The concentration of enzyme (GSH-Px) measures, and every kind for the treatment of conditions are all provided with 3 multiple holes, and each measurement is all repeated 3 times, Western-blot
Method measure Bcl-2, Bcl-xL Caspase-3 albumen situation of change.
Embodiment 5
The curative effect of this compound preparation is observed from the level of cell:
The impact on ARPE-19 cell viability of the variable concentrations medicine:
By ARPE-19 cell with 2 × 104/ well is inoculated in 96 orifice plates, temperature 37 DEG C, and 6h cultivated by 5% carbon dioxide training case
To nearly Fusion Strain, be separately added into ultimate density be 0 μ g/mL, 10 μ g/mL, 20 μ g/mL, 40 μ g/mL, 80 μ g/mL
The DMEM/F12 culture medium of dimension compound medicine thing, cultivates at 37 DEG C of 5% CO2gas incubator.18 as a child, with MTT
Colorimetric method surveys OD490, comparing with control group, result is shown in Fig. 1.
OD is measured with mtt assay490Calculate cell viability:
Compared with control group A RPE-19: the cell viability of the ARPE-19 that 40 μ g/mL concentration medicines process is relatively big, than comparison
Group has rised in value 2.38 times, has significant difference (P < 0.01VS control) to see Fig. 2.
Compound preparation is to H2O2The impact of induction ARPE-19 cell viability:
The ARPE-19 giving variable concentrations medicine preculture 6h is again exposed to 100 μm ol/L H2O2Rear cell viability is more not
Through medicine, pretreatment person is obviously improved, and without medicine process ARPE19 at 100 μm ol/L H2O2Under induction, cell viability
More both without medicine also without H2O2Induced oxidation person stress be decreased obviously (P < 0.001).See Fig. 3:
Result: pre-process 6h with the compound preparation of 20 μ g/mL, 40 μ g/mL, 80 μ g/mL and then can alleviate exogenous
H2O2The oxidativestress damage of the ARPE-19 cell of induction, improves external source H2O2MDA, SOD, GSh-Px of causing and cell
The change of viability.Therefore, Sha Biya has alleviation H2O2The effect of induction ARPE-19 oxidativestress damage, is shown in Fig. 4.
Western blot result display Bcl-2, Bcl-xL protein expression level H2O2Modeling group ties up medicine less than Normal group
Compound medicine protection group is higher than H2O2Modeling group (P < 0.05, Caspase-3 protein expression level H2O2Modeling group is higher than the most right
Compound medicine thing protection group is tieed up less than H according to group2O2Modeling group P < 0.05;H is described2O2Bcl-2, Bcl-xL egg can be lowered
White expression, raises the expression of Caspase-3 albumen;And tie up the ARPE-19 people of compound medicine thing protection hydrogen peroxide-induced
Raise the expression of Bcl-2, Bcl-xL albumen during the oxidativestress damage of retinal pigment epithelium, lower Caspase-3
The expression of albumen, is shown in Fig. 5.
Sum up: also can alleviate external source 100 μm ol/L H with compound preparation pretreatment cell 6h2O2Cultivate what 18h was induced
The rising of the intracellular MDA of ARPE-19 and the decline of SOD, GSH-Px vigor.
The Sha Biya of low middle concentration is to H2O2Induction ARPE-19 oxidativestress damage has protective effect, and it may pass through mitochondria
Approach, through controlling the release of cromoci, suppression Caspase-3 albumen strengthens and Bcl-2, Bcl-xL protein decreased,
To ARPE-19 cells play protective effect.
Variable concentrations compound preparation affects in the experiment of cell viability and shows, along with drug concentration improves, cell viability is gradually
Improving, the cell viability of the ARPE-19 that 40 μ g/mL concentration medicines process is best.The ARPE-19 of variable concentrations pharmaceutical intervention 6h
Cell is again exposed to 100 μm ol/L H2O2Rear cell viability is relatively obviously improved without medicine pretreatment person.The dimension of variable concentrations
Medicine compound pretreatment ARPE-19 cell 6h then can alleviate exogenous H2O2The oxidative stress of the ARPE-19 cell of induction damages
Wound, improves external source H2O2MDA, SOD, the GSh-Px caused changes.Western-blot experiment shows, by mitochondria way
Footpath, through controlling the release of cromoci, suppression Caspase-3 albumen strengthens and Bcl-2, Bcl-xl protein decreased, right
ARPE-19 cells play protective effect.
Claims (3)
1. the compound preparation treating PVR and amblyopia, it is characterized in that said preparation is by bulk drug fennel seeds 3-30 part, aloe 9-90 part, puncture vine 5-45 part, roseleaf 7-60 part, terminalia flesh 6-50 part, smokes Lu Xiang 3-30 part, turpeth 3-30 part, and auxiliary material is that beta cyclodextrin 4-10 part, hydroxypropyl cellulose 26 parts, PVPP 6 parts, starch 5 parts, magnesium stearate 1 part and honey 10-50 part are made.
Treatment PVR the most according to claim 1 and the compound preparation of amblyopia, it is characterized in that said preparation is by bulk drug fennel seeds 3-20 part, aloe 9-60 part, puncture vine 5-30 part, roseleaf 7-40 part, terminalia flesh 6-35 part, smokes Lu Xiang 3-20 part, turpeth 3-20 part, and auxiliary material is that beta cyclodextrin 4-10 part, hydroxypropyl cellulose 26 parts, PVPP 6 parts, starch 5 parts, magnesium stearate 1 part and honey 10-40 part are made.
The preparation method of the compound preparation for the treatment of PVR the most according to claim 1 and 2 and amblyopia, it is characterised in that follow these steps to carry out:
A, by taking aloe, turpeth through screened, smoke Lu Xiang tri-taste mixed powder and be broken into 40-200 mesh, obtain crude drug powder, standby;
B, fennel seeds add 6-12 times amount water, soak 5-24 hour, and the way of distillation extracts volatile oil, 5-10 hour time, the another device of the aqueous solution after distillation is collected, by every 4 parts of-10 parts of inclusions of 0.6ml-2ml volatile oil beta cyclodextrin, temperature 30 DEG C-60 DEG C, mixing time 30min, temperature 4 DEG C refrigerates 10 hours, filters, temperature 40 DEG C-60 DEG C is dried, cross 40-100 mesh sieve, obtain volatile oil clathrate compound, standby;
C, the fennel seeds dregs of a decoction and puncture vine, roseleaf, the terminalia flesh water of 6-20 times amount being extracted 1-4 time, each extraction time is 1-4 hour, obtains extract;
D, extract is filtered separate the dregs of a decoction and liquid, liquid reduced pressure concentration is become the medicinal extract of relative density 1.10-1.40, filters, obtain medicinal extract, standby;
E, the medicinal extract that step d is obtained, it is vacuum dried by temperature 30-80 DEG C, time 24-48h, obtain dry extract, with the crude drug powder in step a, the volatile oil clathrate compound in step b after again medicinal extract being pulverized, being adhesive by PVPP ethanol solution again, fully mix with auxiliary material hydroxypropyl cellulose, starch, magnesium stearate, pharmaceutical methods is pressed into tablet routinely;
Or by the medicinal extract in step d, it is vacuum dried by temperature 30-80 DEG C, time 24-48h, obtain dry extract, with the crude drug powder in step a, the volatile oil clathrate compound in step b after again medicinal extract being pulverized, being adhesive by PVPP ethanol solution again, fully mix with auxiliary material hydroxypropyl cellulose, starch, magnesium stearate, pharmaceutical methods makes capsule routinely;
Or by the medicinal extract in step d, be vacuum dried by temperature 30-80 DEG C, time 24-48h, obtain dry extract, then after medicinal extract is pulverized with the crude drug powder in step a, the volatile oil clathrate compound in step b, then be adhesive by water or honey, fully mixing, pharmaceutical methods makes pill routinely.
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CN108938687A (en) * | 2018-09-03 | 2018-12-07 | 辽宁何氏医学院 | Puncture vine prevents and treats the application in retinal damage disease medicament in preparation |
CN110721259A (en) * | 2019-12-04 | 2020-01-24 | 中国科学院新疆理化技术研究所 | Preparation method and application of compound preparation with human aldose reductase inhibitor effect |
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CN1899448A (en) * | 2006-07-06 | 2007-01-24 | 浙江大学 | Chinese medicine compound preparation for treating amblyopia and its preparing method |
CN102293276A (en) * | 2011-09-22 | 2011-12-28 | 王璐 | Liver-clearing vision-improving health-care tea |
CN102579840A (en) * | 2012-03-26 | 2012-07-18 | 许梅 | Chinese medicinal composition with effects of reducing intraocular pressure and protecting optic nerves and preparation method thereof |
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CN1899448A (en) * | 2006-07-06 | 2007-01-24 | 浙江大学 | Chinese medicine compound preparation for treating amblyopia and its preparing method |
CN102293276A (en) * | 2011-09-22 | 2011-12-28 | 王璐 | Liver-clearing vision-improving health-care tea |
CN102579840A (en) * | 2012-03-26 | 2012-07-18 | 许梅 | Chinese medicinal composition with effects of reducing intraocular pressure and protecting optic nerves and preparation method thereof |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108938687A (en) * | 2018-09-03 | 2018-12-07 | 辽宁何氏医学院 | Puncture vine prevents and treats the application in retinal damage disease medicament in preparation |
CN108938687B (en) * | 2018-09-03 | 2021-06-25 | 辽宁何氏医学院 | Application of tribulus in preparation of medicine for preventing and treating retinal injury diseases |
CN110721259A (en) * | 2019-12-04 | 2020-01-24 | 中国科学院新疆理化技术研究所 | Preparation method and application of compound preparation with human aldose reductase inhibitor effect |
CN110721259B (en) * | 2019-12-04 | 2021-12-07 | 中国科学院新疆理化技术研究所 | Preparation method and application of compound preparation with human aldose reductase inhibitor effect |
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