CN1493317A - Balsam pear frost eye medicament for preventing and treating eataract, vision fatigue - Google Patents
Balsam pear frost eye medicament for preventing and treating eataract, vision fatigue Download PDFInfo
- Publication number
- CN1493317A CN1493317A CNA02145017XA CN02145017A CN1493317A CN 1493317 A CN1493317 A CN 1493317A CN A02145017X A CNA02145017X A CN A02145017XA CN 02145017 A CN02145017 A CN 02145017A CN 1493317 A CN1493317 A CN 1493317A
- Authority
- CN
- China
- Prior art keywords
- fructus momordicae
- momordicae charantiae
- preparation
- injection
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
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Landscapes
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Abstract
A Chinese medicine 'balsam pear cream' in the form of eye drops for preventing and treating cataract and asthenopia is prepared from balsam pear, chrysanthemum flower, pale butterflybush flower and borneol through proportionally preparing, filtering and loading in bottle. Its advantage is high curative effect.
Description
Technical field
The present invention relates to be used for prevention and treat various types of cataract, alleviate excess eye-using and cause the asthenopic Fructus Momordicae charantiae cremor ophthalmic preparation that contains, also relate to the production method of this Fructus Momordicae charantiae cremor ophthalmic preparation.
Prior art
Cataract, Chinese medicine are referred to as " cataract ", be with brilliant pearl muddiness, vision slowly fall, gradually to blind be the chronic common oculopathy of cardinal symptom, be more common in old age and presenium person more than 50 years old.The treatment cataract has operative treatment and two kinds of methods of Drug therapy both at home and abroad at present, operative therapy is at present effective method, but the posterior capsule opacification of postoperative generation in late period is its topmost complication, the posterior capsule opacification incidence rate is approximately still 30%～50% in 5 years after surgery, and most senile patient has surgical contraindications such as hypertension, heart disease, cerebrovascular, and there is certain risk in operative treatment; In, adopt Drug therapy in early days, as Zhejiang College Of Traditional Chinese Medicine [journal of shanghai Chinese medicine 2001,35 (11): 26～28] (hiding from view diffusing is the diffusing accent of being made by tens of flavor Chinese medicines such as Moschus, Margarita, MEIHUA BINGPIAN, Concha Haliotidis, Calamina, Radix Salviae Miltiorrhizae, succinums to have developed the diffusing eye drop of hiding from view, every bottle of powder is joined one bottle of eye drip solvent, during use medicated powder is poured in the solvent, is shaken up the back eye drip), the immature phase senile cataract is carried out observation of curative effect, its obvious effective rate 33.3%, effective percentage 72.7%; The Sha Puaisi eye drop (containing 5% bendazac lysine) that Pinghu, Zhejiang Province pharmaceutical factory [pharmacy progress 2001,25 (3): 176～178] produces has certain curative effect to senile cataract; Hangzhou first biochemical pharmaceutical factory [the biochemical drug magazine 1990, (3): 23～27] the ammonia peptide iodine eye drop (health pig whole eyeball hydrolyzed solution and thyroid hydrolyzed solution mix by series of process process proportioning) of Sheng Chaning, the vitreous opacity total effective rate that a variety of causes is caused reaches 72.96%, to all kinds cataract (especially senile cataract), obvious effective rate reaches 12.65%, and the conservative estimation total effective rate reaches 60.67%.
The method of alleviating asthenopia mainly adopts medicine, as Runshu eye drops, ZHENSHIMING DIYANYE, the honest collyrium of Xinle etc., dominant mechanism is: contain penetrating dose of various effective ingredient such as various natural activity aminoacid, alkaloid, various trace elements and ion etc. in the eye drop, they not only can regulate eyeball ciliary muscle and iris circular muscle physiological function, and can also increase visual organization nutrition, improve the eyeball blood circulation.
From Cucurbitaceae Fructus Momordicae charantiae (Momordica charantia L.) fruit, extract the Fructus Momordicae charantiae cremor that makes, the known active component that can be used as blood sugar lowering, antineoplastic agent, antimicrobial drug etc., for Fructus Momordicae charantiae chemical constituent, pharmacology and toxicity research, domestic more existing pertinent literature reports.As: (1) Beijing pharmaceutical chemistry institute Zheng Shuo etc. has studied the separation and purification and the character [journal of biological chemistry 1992 thereof of Charantin analog, 8 (4): 429～433], the author adopts ammonium sulfate precipitation, affinity chromatograph, methods such as gel filtration, make momordicine I from the Fructus Momordicae charantiae kernel, II, they all present single district band on SDS-polyacrylamide gel electrophoresis and isoelectric focusing electrophoresis, its molecular weight is respectively 26000 and 28000, isoelectric point, IP 8.3, sugar content 1.6% and 2.05%, momordicine I is 2.54mg/kg to mouse peritoneal administration LD50 value, and the fatal dose scope of momordicine I I is 9mg/kg～14mg/kg.(2) Xie Huiyuan of united family hospital, Shenzhen Guangdong Pharmaceutical University etc. has studied Chinese medicine Fructus Momordicae charantiae chemical constituent [Chinese crude drug 1998,21 (9): 458～459], obtain two parts by precipitate with ethanol: water-soluble portion and have a precipitate with ethanol part of polysaccharide, further decompose, obtain four chemical compounds, identify through structure to be respectively vicine, trehalose, Charantin A and Charantin B.(3) CN 1167632, CN 1244531 disclose Charantin glycosides and Charantin extraction process, wherein CN1167632 under field conditions (factors), utilize chemical pure sodium sulfate from Fructus Momordicae charantiae, to extract the Charantin glycosides, with this Charantin glycosides and other drug matching make treatment acute cigarette inflammation, laryngitis, tonsillitis, cure rate reaches more than 90%; CN1244531 adopts homogenate, stirring, sucking filtration, adjust pH, cold preservation, precipitate, leave standstill, separate out step makes colourless acicular crystal, the reuse silica gel G is carried out thin layer chromatography, eluting, filtration, vacuum drying, gets colourless crystallization, is carried out reflux, filtration drying again, carrying out ply of paper at last analyses and promptly gets pure Charantin, purity can reach 7%, the effective percentage that is used for the treatment of diabetes reaches 82%, cure rate is 40%, and has no side effect, and can reach the effect of the blood sugar lowering of lasting stability.
The Fructus Momordicae charantiae cremor active component that extracts from Fructus Momordicae charantiae is used for prevention or treatment ophthalmic such as cataract, asthenopia, xerophthalmia etc. and does not see document or patent report.Fructus Momordicae charantiae cremor has to relieve summer heat washs heat, and the effect of the detoxifcation that makes eye bright also has the invigorating the liver and kidney function.And in, how weak with age old cataract oculopathy is, the hepatic and renal YIN deficiency, due to the asthenia of essence and blood, eyes losing nutrition, Fructus Momordicae charantiae cremor can suppress and treat cataractous generation and development from aspects such as the heat that uncharms, eliminates the asthenopia that causes with a transition.
Summary of the invention
The object of the present invention is to provide the Fructus Momordicae charantiae cremor ophthalmic preparation, said preparation is used for prevention and treats various types of cataract of eyes or alleviate excess eye-using and cause asthenopia.
The preparation that the present invention relates to contains Fructus Momordicae charantiae cremor, Borneolum Syntheticum, sodium chloride and water for injection, 100 parts of weight meters, and proportioning is (as follows): Fructus Momordicae charantiae cremor 1～5, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
The preparation that the present invention relates to contains Fructus Momordicae charantiae cremor, Flos Chrysanthemi extract, Borneolum Syntheticum, sodium chloride and water for injection, and the weight proportion of raw material is: Fructus Momordicae charantiae cremor 1～5, Flos Chrysanthemi extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
The preparation that the present invention relates to contains Fructus Momordicae charantiae cremor, Flos Buddlejae extract, Borneolum Syntheticum, sodium chloride and water for injection, the weight proportion of raw material is: Fructus Momordicae charantiae cremor 1～5, Flos Buddlejae extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
The preparation that the present invention relates to contains Fructus Momordicae charantiae cremor, Flos Chrysanthemi extract, Flos Buddlejae extract, Borneolum Syntheticum, sodium chloride and water for injection, the weight proportion of raw material is: Fructus Momordicae charantiae cremor 1～5, Flos Chrysanthemi extract 0.5～4, Flos Buddlejae extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
The optimum weight proportioning of preparation preparation of the present invention is: Fructus Momordicae charantiae cremor 5, Flos Chrysanthemi extract 4, Flos Buddlejae extract 4, Borneolum Syntheticum 0.015 and sodium chloride 1.8, all the other are water for injection.
The producer of preparation preparation of the present invention is:
(1) gets clean ripe bright Fructus Momordicae charantiae, draw out seed core, the Natrii Sulfas of packing in abdomen is collected white crystalline powder, with the white crystalline powder of collecting, with the dissolving of 3.3 times of amount water for injection, cooling, filtrate filtered is evaporated to nearly saturation, and institute's concentrated solution Boping is laid in the stainless steel disc, crystal is separated out, and does promptly getting Fructus Momordicae charantiae cremor with wind;
(2) get Flos Chrysanthemi, add the water of 8 times～10 times of amounts, soak 30min, decoct secondary, each 1h merges filtrate twice, being concentrated into relative density is 1.17 ± 2 (70 ℃), fully stir, leave standstill 12h, the leaching supernatant, reclaim ethanol in there not being the alcohol flavor, add the water of 4 times of amounts, leave standstill 12h, the leaching supernatant, being concentrated into relative density is the extractum of 1.10～1.15 (80 ℃), be cooled to 40 ℃, add ethanol, make to contain the alcohol amount and reach 85%, leave standstill 12h, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, obtains Flos Chrysanthemi extract;
(3) get Flos Buddlejae, add the water of 8 times～10 times of amounts, soak 30min, decoct secondary, each 1h merges filtrate twice, being concentrated into relative density is 1.17 ± 2 (70 ℃), fully stir, leave standstill 12h, the leaching supernatant, reclaim ethanol in there not being the alcohol flavor, add the water of 4 times of amounts, leave standstill 12h, the leaching supernatant, being concentrated into relative density is the extractum of 1.10～1.15 (80 ℃), be cooled to 40 ℃, add ethanol, make to contain the alcohol amount and reach 85%, leave standstill 12h, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, obtains Flos Buddlejae extract;
(4) Fructus Momordicae charantiae cremor, sodium chloride of getting proportional quantity is with 75% water for injection dissolving of full dose, or the Flos Chrysanthemi extract and/or the Flos Buddlejae extract that add proportional quantity stir, add 0.5% activated carbon decolorizing then, add to the full amount of water for injection, stir, filter, add Borneolum Syntheticum in the elimination active carbon, filtrate, filter through sintered glass funnel, the eye drop preparation of certain loading amount is made in the filtrate fill.
Good effect of the present invention is:
The present invention is an ophthalmic preparation, adopt the scientific and reasonable compatibility of Fructus Momordicae charantiae cremor and Borneolum Syntheticum, Flos Chrysanthemi extract, Flos Buddlejae extract, can effectively prevent and treat various types of cataract, alleviate the asthenopia that excess eye-using causes effectively, xerophthalmia, keratitis, viral inflammation are also had better therapeutic effect.
Usage: the eye drop of the present invention as fill becomes 1ml/ to prop up, splash in the eyelid, 1 time 1,3 times～4 times on the one.
The Fructus Momordicae charantiae cremor eye drop that the present invention makes, the LD of mouse peritoneal injection
50＞0.6g/kg, the LD of mouse mainline administration
50＞5.0g/kg, 3529 times and 2941 times of quite clinical human eye drip daily dose respectively, show clinical drug safety, indicating well prospect in medicine.
Raw material sources such as Fructus Momordicae charantiae, Flos Chrysanthemi, Flos Buddlejae are abundant, inexpensive, toxic and side effects is low, and preparation technology is simple, can be made into eye drop dosage form commonly used, and is easy to use.
The Fructus Momordicae charantiae cremor eye drop pharmacological action that the present invention makes: rat D-galactose cataract is had tangible prevention, therapeutical effect; Cavia porcellus D-galactose cataract also there is the obvious suppression effect; Rat cataract due to the sodium selenite there is the obvious treatment effect; Eyelash shape muscular tension is reduced, tired eyes are played regulating action; The ciliary machine is in spasticity has regulating action.
The detailed description of the invention
Cataract of eyes is more common in old age and the presenium person more than 50 years old, and is weak with age, and the hepatic and renal YIN deficiency is due to the asthenia of essence and blood, eyes losing nutrition; Or deficiency of spleen-YANG and kidneyYANG, insufficiency of the spleen mistake fortune, the five internal organs honor is in order; Or cloudy smart weak, internal injury caused by excess of seven emotions can not be joined sun, due to asthenic fire is superior; Or stagnation of QI due to depression of the liver, strongly fragrant fire-transformation of a specified duration; Working with one's mind exhausts think of, contains in the heart-fire, and the conscience fire is scorching, and brilliant pearl is lost and supports, and becomes muddiness.In simple terms, exactly owing to empty, fire cause cataractous generation and development.Modern study shows that cataractous generation mainly because heat radiation causes, is shone the life of working under the hot environment, often the easiest trouble cataract as sunburst.Therefore, the heat that uncharms is to suppress cataractous generation and the effective means of controlling cataractous development.And asthenopia often appear at excessive with occur looking after the eye or after the lasting near work fuzzy, ophthalmic bloated, dry and astringent, shed tears, general malaises such as eye symptom such as eye socket is ached and headache, dizzy, nauseating, irritated, weak, hypomnesis.Mainly be from aspects such as clearing away heat to improve acuity of vision, invigorating the liver and kidney prevention asthenopia.
Fructus Momordicae charantiae cremor is by the preparation of Fructus Momordicae charantiae and Natrii Sulfas and get, and collects the nature and flavor of the two, has that bitter cold is purged heat, intestinal stasis relieving is moisturized, hard masses softening and resolving, the effect that clears away heart-fire and make eye bright.Fructus Momordicae charantiae cremor is soluble in water, and the desirable medicine mother for the preparation eye drop allocates heat and toxic materials clearing away medicine into, can be used for an outer various infection, adds the removing nebula to improve visual acuity medicine, can be used for treating various hot nebula films.
Flos Chrysanthemi has wind and heat dispersing, the tonifying YIN suppressing the hyperactive liver, and the effect of improving acuity of vision and removing nebula, the blurred vision cataract that the treatment deficiency of the liver and kindey causes, modern study shows that Flos Chrysanthemi also has vision protection, the effect of alleviating asthenopia.The Flos Buddlejae removing heat from the liver, improving acuity of vision and removing nebula cures mainly the optic atrohic blindness cataracta, blood vessel in the clear order.
Borneolum Syntheticum leads to all keys, the stagnated fire of loosing, removing nebula to improve visual acuity, reducing swelling and alleviating pain.Can anneal, moisten puckery, pain relieving.Its armaticity can be led to all keys dirty evil of loosing, and goes to be detained, and with other drug mutually 5, its application is more extensive, is usually used in treating in the asthenopic eye drop.
The ophthalmic preparation Main Ingredients and Appearance of the present invention's design is a Fructus Momordicae charantiae cremor, be aided with Borneolum Syntheticum, or Flos Chrysanthemi extract and/or Flos Buddlejae extract, be exactly according to the cataractous cause of disease, reasonable scientific composition, purge heat to reach bitter cold, the effect of removing nebula to improve visual acuity, in, the cataractous treatment of early-stage senile and prevention, alleviating asthenopia provide new effective way.
The materia medica test of preparation of the present invention:
1. the Fructus Momordicae charantiae cremor eye drop is to the preventive effect test of rat D-galactose cataract
Get 40 of wistar kind rats, body weight 35g～50g, male and female half and half are divided into 5 groups at random, that is: blank group, model group, Moschus moschiferous pearl eye drops for improving eyesight group (6%) and the large and small dosage group of Fructus Momordicae charantiae cremor eye drop (20% and 10%).Blank group lumbar injection every day is with volume normal saline and drinking public water supply, and other is respectively organized rat and drinks 10%D-galactose and lumbar injection 50%D-galactose aqueous solution every day, and injected dose is 5g/kg.The large and small dosage group of Moschus moschiferous pearl eye drops for improving eyesight group and Fructus Momordicae charantiae cremor eye drop.Animal is put drops in one's eyes 4 times every day when injecting and drinking with the dosage galactose, each 1 eye, 2h at interval, successive administration and gave galactose 30 days, behind medicine the 7th, 14,21 and 30 day, with slit lamp examination lenticular opacity intensity, mark by table 1 standards of grading, the results are shown in Table 2.
Table 1 rat D-galactose cataract lenticular opacity degree standards of grading
Score value lenticular opacity degree
1 does not have muddiness, crystalline lens transparent clear
2 is slight muddy, and only there is cavity in portion under the line
3 is highly muddy, and the cavity degree of expansion is to central authorities
4 nuclears are muddy, and crystalline lens only presents the nuclear cataract in central authorities
5 is muddy fully, and whole crystalline lens is total cataract
15 total marks
The preventive effect of table 2 pair rat D-galactose cataract
Dosage eye number is crystalline body fluid degree score value (X ± SD)
Group
(％) (n) 0 7 14 21 30
Blank-16 00000
1.625 2.688 3.063 3.438
Model-16 0
±0.719 ±1.014 ±0.929 ±0.727
1.563 2.000 2.313 2.688
The Moschus moschiferous pearl makes eye bright 6.0 16 0
±0.629 ±0.632
*?±0.793
*?±0.873
*
1.438 2.125 2.375 2.438
Fructus Momordicae charantiae cremor eye drop 20.0 16 0
±0.727 ±0.719
*?±0.885
*?±0.629
**
1.625 2.438 2.875 2.813
10.0 16 0
±0.957 ±0.892 ±0.806 ±0.834
*
Compare with model group
*P＜0.05
*P＜0.01
The result shows, the large and small dosage group of Fructus Momordicae charantiae cremor eye drop lenticular opacity degree score value is significantly less than model group (p＜0.05,0.01), illustrating that the Fructus Momordicae charantiae cremor eye drop has tangible preventive effect to the galactose cataract rat, its effect is suitable with Moschus moschiferous pearl eye drops for improving eyesight.
2. the Fructus Momordicae charantiae cremor eye drop is to the cataractous therapeutical effect test of rat galactose
Get 50 of Wistar kind rats, body weight 35g～50g, male and female half and half, lumbar injection 50% galactose (5g/kg) and drank 10% galactose aqueous solution to the 15 days, stop injection and drink galactose, with slit lamp examination animal lenticular opacity degree, select the similar rat of lenticular opacity degree, be divided into 4 groups at random, 8 every group, began to treat (method and dosage are with test one) in the 16th day with being subjected to the reagent thing to carry out smelting, successive administration 30 days is behind medicine first the 10th, 20 and 30 days, use slit lamp examination lenticular opacity degree respectively, mark by table 1 standards of grading, the results are shown in Table 3.
The therapeutical effect of table 3 pair rat D-galactose cataract
The dosage eye is counted lenticular opacity degree score value (X ± SD divides)
Group
(%) before (n) administration after the administration 10 20 30 (my god)
3.000 3.438 3.563 3.750
Model-16
±0.816 ±0.512 ±0.512 ±0.447
3.063 3.375 2.438 1.938
The Moschus moschiferous pearl makes eye bright 6.0 16
±0.772 ±0.619 ±0.512
** ±0.772
**
Fructus Momordicae charantiae cremor
3.000 3.313 2.750 1.813
20.0 16
Eye drop
±0.966 ±0.602 ±0.517
* ±0.834
**
3.125 3.563 3.375 3.000
10.0 16
±0.719 ±0.512 ±0.500 ±0.730
*
Compare with model group
*P＜0.05
*P＜0.01
The result shows, big small dose group of Fructus Momordicae charantiae cremor eye drop and model group compare, lenticular opacity degree score value significant difference (p＜0.05,0.01), illustrate that product of the present invention has the obvious treatment effect to rat galactose-cataract, its effect is close with Moschus moschiferous pearl eye drops for improving eyesight.
3. the Fructus Momordicae charantiae cremor eye drop is to the influence test of Cavia porcellus D-galactose cataract
Get 40 of Cavia porcelluss, body weight 240-310g, male and female half and half are divided into 5 groups at random, and 8 every group, that is: blank group, model group, Moschus moschiferous pearl eye drops for improving eyesight group and the large and small dosage group of Fructus Momordicae charantiae cremor eye drop.Remove matched group retrobulbar injection every days two with the volume normal saline, other each treated animal retrobulbar injection every day 0.2ml 0.4%D-galactose normal saline once, the large and small dosage group of Moschus moschiferous pearl eye drops for improving eyesight group (6.0%) and Fructus Momordicae charantiae cremor eye drop (concentration is respectively 20% and 10%) medication every day 4 times in injection of d-galactose, each 1 droplet/eye, interval 2h, continuous eye drip and gave galactose 10 days, each treated animal was checked under slit lamp respectively in the 11st day, observe an animal per lens opacities degree and press the scoring of table 4 standards of grading, the results are shown in Table 5.
The muddy degree standards of grading of table 4 Cavia porcellus D-galactose cataractous lens
Score value lenticular opacity degree
0 crystalline lens is transparent
1 strip muddiness
The muddiness of strip more than 2
3 ring-type muddinesses
The table 5 pair cataractous influence of Cavia porcellus D-galactose
Group dosage (%) eye number (n) lenticular opacity degree (X ± SD divides)
Blank-16 0
Model-16 2.438 ± 0.629
The Moschus moschiferous pearl makes eye bright 6.0 16 1.000 ± 0.730
*
Fructus Momordicae charantiae cremor eye drop 20.0 16 1.063 ± 0.574
*
10.0 16 2.313±0.602
Compare with model group
*P＜0.01
The result shows that the heavy dose of group of Fructus Momordicae charantiae cremor eye drop compares with model group, and (p＜0.01=illustrates that product of the present invention has the obvious suppression effect to Cavia porcellus D-galactose cataract to significant difference.
4. the Fructus Momordicae charantiae cremor eye drop is to the therapeutical effect of the sour sodium cataract in Asia
The sodium selenite solution (3.46mg/kg body weight) of subcutaneous injection 1ml next day that the rat that was born 14 days being distinguished, inject altogether 3 times, the lenticular muddy degree of inferior daily slit lamp examination is selected 32 of the similar rats of lenticular opacity degree (lenticular opacity degree standards of grading see Table 6), is divided into 4 groups at random, every group 8, dosage and method were treated the reuse slit lamp examination one month continuously with test 2, respectively organize the lenticular opacity degree, the results are shown in Table 7.
Table 6 rat sodium selenite cataract lenticular opacity degree standards of grading
Score value lenticular opacity degree
0 crystalline lens transparent clear does not have muddy
In 1 nuclear little cloud temperature, bar are arranged
2 fritter flocculent turbidities
3＜1/3 Lycoperdon polymorphum Vitt muddinesses
4≤1/3 white casses
5＞1/3 white casses
The smelting treatment effect of table 7 pair rat sodium selenite cataract
The dosage eye is counted lenticular opacity degree score value (X ± SD divides)
Group
(%) behind (n) administration prodrug 30 days
3.94 4.00
Model-16 ± 0.57 ± 0.52
3.94 3.06
The Moschus moschiferous pearl makes eye bright 6.0 16 ± 0.68 ± 0.77
*
4.00 3.12
Fructus Momordicae charantiae cremor eye drop 20.0 16 ± 0.73 ± 0.72
*
4.06 3.88
10.0 16 ±0.77 ±0.72
Compare with model group
*P＜0.05
The result shows that the Fructus Momordicae charantiae cremor eye drop is heavy dose of all can obviously treat rat sodium selenite cataract (p＜0.05) with Moschus moschiferous pearl eye drops for improving eyesight.
Experimental result shows that the Fructus Momordicae charantiae cremor eye drop has tangible prevention, therapeutical effect to rat D-galactose cataract; Cavia porcellus D-galactose cataract also there is the obvious suppression effect; Rat cataract due to the sodium selenite there is the obvious treatment effect.
5. the Fructus Momordicae charantiae cremor eye drop is to the influence of rabbit eyelash shape muscular tension
Get healthy rabbits, the extraction eyeball is put in the K-H liquid, remove cornea, crystalline lens and vitreous body, in between sclera and ciliary muscle, peel off, free ciliary muscle, but the flesh ligament links to each other with sclera, and ciliary muscle vertically is cut into the wide flesh bar of about 4mm together with sclera, sclera at about 3mm place, distance ciliary muscle lower end is cut off, and removes unnecessary sclera.Two ciliary muscle bars are contacted with silk thread, and the two ends threading is fixed in the maxwell bath pipe bottom that fills K-H liquid down up and down, on be connected on the transducer lever, application of load 100mg, 30 ℃ of constant temperature, logical hydroperoxy-, the ciliary muscle contraction activity inventory is on monitor, about 1 hour of incubation, treat that muscular tension is stable after, put 19ml K-H nutritional solution in the maxwell bath pipe, add Fructus Momordicae charantiae cremor eye drop and ZHENSHIMING DIYANYE 1ml, final concentration is the diluted 20 times concentration of former collyrium.Observation is under drug effect, and the tensile variation of corpus ciliare serves as zero with muscular tension before the administration, and 8 minutes internal tension minimums are the administration backward pull after the record administration.
The result shows that to behind the Fructus Momordicae charantiae cremor eye drop, ciliary muscle tension force reduces gradually, maximum decline 12.39mm (seeing Table 8) in 8 minutes, and obvious this medicine can obviously reduce rabbit ciliary muscle tension force, and its effect is better than ZHENSHIMING DIYANYE (P＜0.05).Show that this medicine can make eyelash shape muscular tension reduce, and plays regulating action to tired eyes.
Table 8 Fructus Momordicae charantiae cremor eye drop is to the influence of rabbit eyelash shape muscular tension
The medicine final concentration
The tension force drop-out value
Group
The experimental example number
(medicament for the eyes extension rate)
(X±SD，mm
ZHENSHIMING DIYANYE 20 9 8.28 ± 3.00
Fructus Momordicae charantiae cremor eye drop 20 9 12.39 ± 3.14
*
*Compare P＜0.05 with ZHENSHIMING DIYANYE
6. the Fructus Momordicae charantiae cremor eye drop is to the spasmolysis of rabbit eye ciliary muscle
Method is the same, and adding the acetylcholine final concentration in the maxwell bath pipe is 5 * 10
-5, ciliary muscle is stable spasticity, waits to cause the stable back of convulsion effect and adds medicament for the eyes, observes the convulsion effect that causes to anti-acetylcholine.That measures acetylcholine causes the convulsion height, measures acetylcholine and causes and add medicine after the convulsion you are the spasmolytic degree with its difference of minimum altitude in 8 minutes, carries out statistical with this difference.
The result shows that the lagophthalmos ciliary muscle causes under the convulsion state at acetylcholine, and two medicines all have spasmolysis (seeing Table 9), and Fructus Momordicae charantiae cremor eye drop spasmolysis slightly is better than ZHENSHIMING DIYANYE, shows that this medicine is in spasticity to the ciliary machine and has regulating action.
Table 9 Fructus Momordicae charantiae cremor eye drop is to the spasmolysis of rabbit eye ciliary muscle
Medicine final concentration acetylcholine causes height suppression ratio under the convulsion drug effect
Group
(medicament for the eyes extension rate) highly (mm) reduction value (mm) is (%)
ZHENSHIMING DIYANYE 20 18.13 ± 6.06 7.50 ± 4.12 41.36
Fructus Momordicae charantiae cremor eye drop 20 18.38 ± 4.44 10.25 ± 3.80 55.77
(n＝8，X±SD)
Experimental result shows that the Fructus Momordicae charantiae cremor eye drop can make eyelash shape muscular tension reduce, and tired eyes are played regulating action; The ciliary machine is in spasticity has regulating action.
The acute toxicity test of Fructus Momordicae charantiae cremor eye drop
The LD of Fructus Momordicae charantiae cremor eye drop mouse peritoneal drug administration by injection
50＞6.0g/kg, the LD of mouse mainline administration
50＞5.0g/kg, illustrates product clinical drug safety of the present invention by 3529 times and 2941 times of quite clinical human eye drip daily dose respectively.
Fructus Momordicae charantiae cremor eye drop long term toxicity test
Rabbit was dripped Fructus Momordicae charantiae cremor eye drop (20% and 10%) in continuous 3 months, was respectively 35 and 17.5 times of clinical adult's one consumption per day.The general situation of animal compares no significant difference as behavior performance, fur gloss, diet drinking-water and body weight change and matched group as a result.Administration was taken a blood sample after 3 months, surveyed its hemogram and blood parameters, as a result no abnormality seen.Main substantial viscera weight also no abnormality seen changes important organ histopathological examination no abnormality seen.Above results suggest, product long-term prescription safety of the present invention.
Fructus Momordicae charantiae cremor eye drop eye irritation, anaphylaxis and hemolytic test
Experimental rabbits, the big ear white race of Japan, body weight 1.8kg～2.3kg; Albino guinea-pig, body weight are 240g～260g, and male and female half and half provide by the second clinical experiment animal housing of Chinese Medical Sciences University, the quality certification number: No. the 021st, distant real kinoplaszm word.
Administration in the Fructus Momordicae charantiae cremor eye drop rabbit conjunctival, no matter single administration, multiple dosing and damaged conjunctiva administration all do not present the local excitation reaction.Prove that through Cavia porcellus vivo medicine-feeding allergic experiment product of the present invention does not produce anaphylaxis.Hemolytic test shows that product of the present invention does not have hemolytic.
Embodiment 1:
The production method for preparing Fructus Momordicae charantiae cremor eye drip liquor of the present invention is:
(1) Fructus Momordicae charantiae cremor: get fresh Fructus Momordicae charantiae, remove melon pulp, clean chopping, put into the sand jar, add Natrii Sulfas, cover FE Tiler, place the outdoor ventilation of taking shelter from rain, after a few days, jar white white sample thing of outer appearance is brushed down, with bottled good every day, wait to exhaust, put in the beaker, boil 30 fens kinds, put coldly, filter; With the moisture evaporate to dryness, crystallization had both got the crude product Fructus Momordicae charantiae cremor in the ventilation air slaking to filtrate in water-bath.The Fructus Momordicae charantiae cremor semifinished product cools off with the dissolving of 3.3 times of amounts (weight) water for injection, and filtrate filtered is evaporated to nearly saturation, and institute's concentrated solution Boping is laid in the stainless steel disc, and crystal is separated out, and does promptly getting Fructus Momordicae charantiae cremor with wind.
(2) Flos Chrysanthemi extract: get Flos Chrysanthemi, add the water of 8 times～10 times of amounts, soak 30min, decoct secondary, each 1h merges filtrate twice, being concentrated into relative density is 1.17 ± 2 (70 ℃), fully stir, leave standstill 12h, the leaching supernatant, reclaim ethanol in there not being the alcohol flavor, add the water of 4 times of amounts, leave standstill 12h, the leaching supernatant, being concentrated into relative density is the extractum of 1.10～1.15 (80 ℃), be cooled to 40 ℃, add ethanol, make to contain the alcohol amount and reach 85%, leave standstill 12h, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, obtains Flos Chrysanthemi extract;
(3) get Flos Buddlejae, add the water of 8 times～10 times of amounts, soak 30min, decoct secondary, each 1h merges filtrate twice, being concentrated into relative density is 1.17 ± 2 (70 ℃), fully stir, leave standstill 12h, the leaching supernatant, reclaim ethanol in there not being the alcohol flavor, add the water of 4 times of amounts, leave standstill 12h, the leaching supernatant, being concentrated into relative density is the extractum of 1.10～1.15 (80 ℃), be cooled to 40 ℃, add ethanol, make to contain the alcohol amount and reach 85%, leave standstill 12h, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, obtains Flos Buddlejae extract;
(4) Fructus Momordicae charantiae cremor, sodium chloride of getting proportional quantity is with 75% water for injection dissolving of full dose, or the Flos Chrysanthemi extract and/or the Flos Buddlejae extract that add proportional quantity stir, add 0.5% active carbon (decolouring) then, add to the full amount of water for injection, stir, filter, the elimination active carbon adds Borneolum Syntheticum, filters through sintered glass funnel, the eye drop preparation of certain loading amount is made in the filtrate fill.
Embodiment 2:
The production method for preparing Fructus Momordicae charantiae cremor gel 1000g of the present invention is:
(1)～(3) step is the same;
(4) get the Fructus Momordicae charantiae cremor of proportional quantity, and/or Flos Chrysanthemi extract and/or Flos Buddlejae extract, with about 75% water for injection dissolving, 4g carbomer gel base material is soaked wherein 12 hours then, get an amount of Borax, boric acid adds wherein, to be adjusted to pH5.0～7.0, stir, moisturizing is fully stirred to full dose, filter with 220 mesh sieve cloth, get clear gel, pressure sterilizing, cooling, packing had both got the Fructus Momordicae charantiae cremor gel.
Embodiment 3
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 20 grams, Flos Chrysanthemi extract 15 grams, Flos Buddlejae extract 15 grams, Borneolum Syntheticum 0.06 gram, sodium chloride 5 gram waters for injection add to 1000ml.
Embodiment 4:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 50 grams, Flos Chrysanthemi extract 40 grams, Flos Buddlejae extract 40 grams, Borneolum Syntheticum 1.5 grams, sodium chloride 18 grams, water for injection adds to 1000ml.
Embodiment 5:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 30 grams, Flos Chrysanthemi extract 25 grams, Flos Buddlejae extract 25 grams, Borneolum Syntheticum 0.1 gram, sodium chloride 9 grams, water for injection adds to 1000ml.
Embodiment 6:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 20 grams, Flos Chrysanthemi extract 15 grams, Borneolum Syntheticum 0.06 gram, sodium chloride 5 grams, water for injection adds to 1000ml.
Embodiment 7:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 50 grams, Flos Chrysanthemi extract 40 grams, Borneolum Syntheticum 1.5 grams, sodium chloride 18 grams, water for injection adds to 1000ml.
Embodiment 8:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 30 grams, Flos Chrysanthemi extract 25 grams, Borneolum Syntheticum 0.1 gram, sodium chloride 9 grams, water for injection adds to 1000ml.
Embodiment 9:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 20 grams, Flos Buddlejae extract 15 grams, Borneolum Syntheticum 0.06 gram, sodium chloride 5 grams, water for injection adds to 1000ml.
Embodiment 10:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 50 grams, Flos Buddlejae extract 40 grams, Borneolum Syntheticum 1.5 grams, sodium chloride 18 grams, water for injection adds to 1000ml.
Embodiment 11:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 30 grams, Flos Buddlejae extract 25 grams, Borneolum Syntheticum 0.1 gram, sodium chloride 9 grams, water for injection adds to 1000ml.
Embodiment 12:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 20 grams, Borneolum Syntheticum 0.06 gram, sodium chloride 5 grams, water for injection adds to 1000ml.
Embodiment 13:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 50 grams, Borneolum Syntheticum 1.5 grams, sodium chloride 18 grams, water for injection adds to 1000ml.
Embodiment 14:
The prescription of preparation preparation of the present invention: Fructus Momordicae charantiae cremor 30 grams, Borneolum Syntheticum 0.1 gram, sodium chloride 9 grams, water for injection adds to 1000ml.
Claims (9)
1, a kind of prevention and treatment cataract, asthenopic Fructus Momordicae charantiae cremor ophthalmic preparation, described preparation contains Fructus Momordicae charantiae cremor, Borneolum Syntheticum, sodium chloride and water for injection, 100 parts of weight meters, proportioning is: Fructus Momordicae charantiae cremor 1～5, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
2, preparation according to claim 1 is characterized in that described preparation contains Flos Chrysanthemi extract, and weight proportion is: Fructus Momordicae charantiae cremor 1～5, Flos Chrysanthemi extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
3, according to the described preparation of claim 1, it is characterized in that described preparation contains Flos Buddlejae extract, weight proportion is: Fructus Momordicae charantiae cremor 1～5, Flos Buddlejae extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
4, preparation according to claim 2, it is characterized in that described preparation contains Flos Buddlejae extract, weight proportion is: Fructus Momordicae charantiae cremor 1～5, Flos Chrysanthemi extract 0.5～4, Flos Buddlejae extract 0.5～4, Borneolum Syntheticum 0.005～0.02 and sodium chloride 0.45～1.8, all the other are water for injection.
5, preparation according to claim 4 is characterized in that weight proportion is: Fructus Momordicae charantiae cremor 5, Flos Chrysanthemi extract 4, Flos Buddlejae extract 4, Borneolum Syntheticum 0.015 and sodium chloride 1.8, all the other are water for injection.
6,, it is characterized in that said preparation is the above a dosage form of any pharmaceutics according to the described preparation of claim 1～5.
7, preparation according to claim 6 is characterized in that said preparation is eye drip liquor or gel.
8, according to claim 1, the production method of 7 described preparations, it is characterized in that 75% the water for injection dissolving with full dose of the Fructus Momordicae charantiae cremor of effective dose, sodium chloride is added 0.5% activated carbon decolorizing, add to the full amount of water for injection, stir, the elimination active carbon adds Borneolum Syntheticum then, filters through sintered glass funnel, the eye drop preparation of certain loading amount is made in the filtrate fill.
9, according to claim 2～5, the production method of 7 described preparations is characterized in that the Flos Chrysanthemi extract and/or the Flos Buddlejae extract that add described proportioning stir with 75% the water for injection dissolving with full dose of the Fructus Momordicae charantiae cremor of effective dose, sodium chloride, the activated carbon decolorizing of adding 0.5%, add to the full amount of water for injection, stir, the elimination active carbon, add Borneolum Syntheticum then, filter through sintered glass funnel, the eye drop preparation of certain loading amount is made in fill.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02145017 CN1265803C (en) | 2002-10-31 | 2002-10-31 | Balsam pear frost eye medicament for preventing and treating eataract, vision fatigue |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02145017 CN1265803C (en) | 2002-10-31 | 2002-10-31 | Balsam pear frost eye medicament for preventing and treating eataract, vision fatigue |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1493317A true CN1493317A (en) | 2004-05-05 |
| CN1265803C CN1265803C (en) | 2006-07-26 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02145017 Expired - Fee Related CN1265803C (en) | 2002-10-31 | 2002-10-31 | Balsam pear frost eye medicament for preventing and treating eataract, vision fatigue |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103860736A (en) * | 2014-04-05 | 2014-06-18 | 赵凤娥 | Chinese herba preparation for treating cataract and preparation method thereof |
-
2002
- 2002-10-31 CN CN 02145017 patent/CN1265803C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103860736A (en) * | 2014-04-05 | 2014-06-18 | 赵凤娥 | Chinese herba preparation for treating cataract and preparation method thereof |
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| Publication number | Publication date |
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| CN1265803C (en) | 2006-07-26 |
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