CN116672421A

CN116672421A - A topical composition for preventing and treating myopia, and its preparation method

Info

Publication number: CN116672421A
Application number: CN202310435664.XA
Authority: CN
Inventors: 朱样根
Original assignee: Individual
Current assignee: Individual
Priority date: 2023-04-21
Filing date: 2023-04-21
Publication date: 2023-09-01

Abstract

The invention discloses an external composition for preventing and treating myopia and a preparation method thereof, which is characterized in that the external composition is prepared from common selfheal fruit-spike, kelp, radix trichosanthis, airpotato yam, fritillaria cirrhosa, inula flower, mirabilitum, bitter orange, common burreed rhizome, zedoary, peach kernel, leech, puerarin, ginkgo leaf, chinese angelica, safflower, szechuan lovage rhizome, pseudo-ginseng, motherwort fruit, suberect spatholobus stem, frankincense, myrrh and red sage root, and pipewort herb, chamomile, fructus broussonetiae, tribulus terrestris, cassia seed, pearl, mother-of-pearl, concha haliotidis, mulberry leaf, gentian, peppermint and fineleaf schizonepeta herb, as well as ginseng, pilose asiabell root, astragalus root, largehead atractylodes rhizome, dried rehmannia root, radix asparagi, dwarf lilyturf root, glossy privet fruit, root, epimedium herb, medicinal indian mulberry root, rhizoma polygonati, chinese magnoliavine fruit, fructus psoraleae, white paeony root, chinese wolfberry fruit and the like which have the functions of dispelling wind and clearing heat, improving eyesight and removing nebula, and the external eye paste, cream, preparation, and the product of the external composition for preventing and treating myopia are prepared.

Description

A topical composition for preventing and treating myopia, and its preparation method

Technical Field

The invention belongs to the technical field of ophthalmic medicines of pharmaceutical preparations, and in particular relates to an external composition for preventing and treating myopia and a preparation method thereof.

Background

The incidence rate of myopia in China is very high, the incidence rate of myopia of pupil reaches 35.6%, the incidence rate of myopia of junior middle school students reaches 71.1%, the incidence rate of myopia of senior middle school students reaches 80.3%, and the incidence rate of myopia of college students reaches 87%, so that the pupil is in the trend of high-incidence, low-age and rapid progress. It seriously affects study, work and life of people, and has high risk of diseases such as retinal detachment, cataract, glaucoma, macular degeneration and the like for highly myopic people. Previously, people recognize myopia, which is mostly thought to be caused by poor accommodation of eyes with long-term close distance, i.e., by excessive ciliary muscle accommodation. Therefore, most of the treatments from drug research are drug development and treatment based on the theory, and the effect is of course not ideal. Song Xinjiang et al in the book "cause and prevention and progression of myopia" indicate that "the immediate cause of myopia formation is higher ocular pressure, which results from a regulated pupil block and ciliary muscle longitudinal fiber relaxation, scleral spur drop, small Liang Wangyan, and increased resistance to aqueous humor excretion. It is caused by the fact that ocular hypertension expansion pressure acts on the eyeball wall to gradually enlarge the eyeball and prolong the ocular axis, and is never caused by the fact that pseudomyopia continues to develop and finally true myopia is formed. "New forum". According to the new theory, the inventor combines the traditional Chinese medicine theory of China, and the invention is obtained through technical innovation in the research of long-term focus on ophthalmic medicines and eye health care products.

Disclosure of Invention

The invention aims to provide an external composition for preventing and treating myopia, fundus disease and eye fatigue, and the medicine composition of the invention has the following principle: because the long-term ocular hypertension causes the expansion of the eyeballs as the main cause, the intraocular pressure must be reduced, the expansion of the eyeballs can be reduced, the expansion of the eyeballs and the extension of the ocular axes can be reduced, according to the traditional Chinese medicine theory of China, the functions of resolving hard mass, detumescence, purging pathogenic fire, reducing qi, reducing the like traditional Chinese medicines including selfheal, kelp, radix trichosanthis, airpotato yam, fritillaria, inula flower, mirabilite, fructus aurantii, blood breaking, stasis dispelling, qi-promoting and pain relieving like traditional Chinese medicines including rhizoma sparganii, rhizoma curcumae, peach kernel, leech, puerarin, ginkgo leaf, angelica, safflower, hemlock parsley, pseudo-ginseng, motherwort fruit, suberect spatholobus stem, frankincense, myrrh and radix salviae miltiorrhizae are achieved, the effects of reducing intraocular pressure, preventing abnormal expansion of the eyeballs, reducing the expansion of the eyeballs and the extension of the ocular axes are achieved, accelerating the blood circulation of the eyes and accelerating the metabolism of the eyes are achieved, the Chinese medicinal materials such as pipewort, chamomile, fructus broussonetiae, caltrop, cassia seed, pearl, mother of pearl (layer powder), concha haliotidis, mulberry leaf, gentian, peppermint and herba schizonepetae are matched to serve as ministerial medicaments, cooperate with monarch medicaments to play roles in improving eyesight and removing nebula, dispelling wind and clearing heat, supplementing eye nutrition, and are matched with deficiency-tonifying Chinese medicaments such as ginseng, codonopsis pilosula, astragalus root, bighead atractylodes rhizome, radix rehmanniae, radix asparagi, dwarf lilyturf tuber, glossy privet fruit, adenophora root, epimedium herb, morinda root, rhizoma cibotii, fructus psoraleae, medlar, rhizoma polygonati, shizandra berry, white poria, grassleaf sweetflag rhizome and the like to supplement vital energy and blood of human body caused by overuse of eyes and consumption of essence and blood of eyes; liver and kidney are homologous, and liver and kidney are unbalanced, so that kidney essence deficiency is caused; the traditional Chinese medicine prevents myopia, protects vision, and achieves balance of yin and yang, and balance of qi and blood, by virtue of the fact that essence and blood are generated mutually and yin and yang are mutually balanced, and simultaneously the effect of simultaneously decreasing the blood and the yang is achieved from the same time of tonifying liver and kidney; the liver and kidney are full of essence and blood, so that eyes are nourished, namely various physiological functions of eyes are improved, the capability of the eyes to resist the influence of external adverse factors is improved, abnormal functions are corrected, and a visual system plays a normal role; in addition, the transdermal absorption promoter used in the preparation, such as borneol, natural borneol (d-borneol), menthol, azone and the like, promotes the absorption of the medicine, and enables the medicine to directly reach the action part, thus being a good medicine for preventing and treating myopia, preventing and slowing down fundus lesions and preventing eyestrain.

In summary, the invention is characterized in that the Chinese medicines of common selfheal fruit-spike, kelp, radix trichosanthis, airpotato yam rhizome, fritillaria cirrhosa, inula flower, mirabilite, bitter orange, common burreed rhizome, zedoary, peach seed, leech, puerarin, ginkgo leaf, chinese angelica, safflower, szechuan lovage rhizome, sanchi, motherwort fruit, suberect spatholobus stem, frankincense, myrrh and red sage root are used for resolving hard mass and detumescence, eyesight improving and nebula removing, chinese medicines of pipewort, chamomile, fructus broussonetiae, tribulus terrestris, cassia seed, pearl, nacre (layer powder), concha haliotidis, mulberry leaf, gentian, peppermint and fineleaf schizonepeta herb are matched, and then is matched with deficiency-tonifying traditional Chinese medicines such as ginseng, pilose asiabell root, astragalus root, largehead atractylodes rhizome, dried rehmannia root, cochinchnese asparagus root, dwarf lilyturf tuber, glossy privet fruit, straight ladybell root, epimedium herb, medicinal indianmulberry root, east Asian tree fern rhizome, malaytea scurfpea fruit, barbary wolfberry fruit, manyflower solomonseal rhizome, chinese magnoliavine fruit, white poria, grassleaf sweetflag rhizome and the like, and finally is added with transdermal absorption promoters such as borneol and/or natural borneol (right-handed borneol), menthol, azone and the like, and the transdermal absorption promoters are prepared into products such as external eye patches, ointments, creams, emulsions, emplastrum and the like for preventing and treating myopia, preventing and relieving eyestrain and preventing eyestrain.

The traditional Chinese medicine composition is prepared from common selfheal fruit-spike, kelp, radix trichosanthis, inula flower, mirabilite, fructus aurantii, traditional Chinese medicines of removing blood stasis, promoting circulation of qi and relieving pain, rhizoma sparganii, rhizoma curcumae, leech, puerarin, ginkgo leaf, chinese angelica, safflower, pseudo-ginseng, motherwort fruit and root of red-rooted salvia, traditional Chinese medicines of dispelling wind and clearing heat, improving eyesight and removing nebula, such as pipewort, chamomile, fructus Broussonetiae, caltrop, nacre (layer powder), concha haliotidis, gentian and schizonepeta, and traditional Chinese medicines of tonifying qi and nourishing blood, tranquillizing and improving intelligence, nourishing yin and strengthening yang, such as ginseng, astragalus mongholicus, radix rehmanniae, radix asparagi, glossy privet fruit, epimedium, fructus psoraleae, medlar, schisandra chinensis, poria cocos, rhizoma acori graminei and the like.

The traditional Chinese medicine is prepared from common selfheal fruit-spike, kelp, inula flower, mirabilite, common burreed rhizome, puerarin, chinese angelica, safflower, motherwort fruit, chinese angelica root, common burreed rhizome, kudzuvine root, chinese angelica, common burreed rhizome, fructus Broussonetiae, caltrop, mother-of-pearl (layer powder) and gentian, and further comprises the traditional Chinese medicines of replenishing qi and nourishing blood, tranquillizing and developing intelligence, nourishing yin and strengthening yang, ginseng, astragalus root, dried rehmannia root, radix asparagi, epimedium, chinese magnoliavine fruit, white poria, grassleaf sweelflag rhizome and the like.

The optimal carefully chosen formula comprises the following components in parts by weight: 3-12 parts of selfheal, 3-12 parts of kelp, 4-18 parts of inula flower, 1-9 parts of mirabilite, 2-10 parts of rhizoma sparganii, 0.2-2 parts of puerarin, 5-15 parts of angelica, 2-10 parts of safflower, 3-12 parts of motherwort fruit, 3-18 parts of pipewort, 2-10 parts of fructus Broussonetiae, 1-8 parts of fructus tribuli, 10-50 parts of pearl powder, 0.5-5 parts of gentian, 2-10 parts of ginseng, 3-12 parts of astragalus mongholicus, 3-15 parts of radix rehmanniae, 3-15 parts of radix asparagi, 5-20 parts of epimedium, 1-6 parts of schisandra chinensis, 3-12 parts of poria cocos and 1-6 parts of rhizoma acori graminei. The above Chinese medicinal materials are used for extracting effective components according to their characteristics and medicinal requirements, and adding pharmaceutically acceptable adjuvants into the extracts to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

The optimal carefully chosen formula is optimized according to parts by weight: 5-10 parts of selfheal, 5-10 parts of kelp, 6-15 parts of inula flower, 2-8 parts of mirabilite, 3-9 parts of rhizoma sparganii, 0.3-1.5 parts of puerarin, 6-12 parts of angelica, 3-8 parts of safflower, 5-10 parts of motherwort fruit, 20-40 parts of pearl powder, 6-15 parts of pipewort, 3-8 parts of fructus Broussonetiae, 2-7 parts of fructus tribuli, 0.8-4 parts of gentian, 2-8 parts of ginseng, 4-10 parts of radix astragali, 5-12 parts of radix rehmanniae, 5-12 parts of radix asparagi, 6-16 parts of epimedium, 2-6 parts of schisandra chinensis, 5-10 parts of white poria and 2-6 parts of rhizoma acori graminei. The above Chinese medicinal materials are used for extracting effective components according to their characteristics and administration requirements, and adding various extracts into pharmaceutically acceptable adjuvants to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

The optimal further carefully selected formula is further optimized according to parts by weight: 6-9 parts of selfheal, 6-9 parts of kelp, 8-14 parts of inula flower, 3-8 parts of mirabilite, 4-9 parts of rhizoma sparganii, 0.5-1.2 parts of puerarin, 8-10 parts of angelica, 4-6 parts of safflower, 6-9 parts of motherwort fruit, 22-36 parts of pearl powder, 8-12 parts of pipewort, 4-6 parts of fructus Broussonetiae, 2-6 parts of fructus tribuli, 1-3 parts of gentian, 2-6 parts of ginseng, 4-8 parts of astragalus mongholicus, 6-12 parts of radix rehmanniae, 8-12 parts of radix asparagi, 8-15 parts of epimedium, 2-5 parts of schisandra chinensis, 5-9 parts of poria cocos and 2-5 parts of rhizoma acori graminei. The above Chinese medicinal materials are extracted according to their respective characteristics and requirements, and various extracts are added into pharmaceutically acceptable adjuvants to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

The composition is characterized by further comprising a percutaneous absorption promoter, a humectant and auxiliary materials acceptable by pharmaceutical preparations.

The transdermal absorption enhancer comprises one or more of borneol, natural borneol (d-borneol), menthol, camphor, eucalyptus oil, oleic acid, azone, dimethyl sulfoxide and the like.

The humectant includes, but is not limited to, one or more of trehalose, oat beta-glucan, polyethylene glycol, glycerol, propylene glycol, butylene glycol, hexylene glycol, xylitol, sorbitol, PVP-K30, sodium hyaluronate, panthenol, ceramides, sodium Pyrrolidone Carboxylate (PCA).

The external composition for preventing and treating myopia and the preparation method thereof are characterized by comprising the following steps:

(1) Pulverizing Inulae flos, rhizoma Sparganii, radix Angelicae sinensis, fructus Leonuri, flos Eriocauli, fructus Tribuli, and rhizoma Acori Graminei into coarse powder, distilling with steam, extracting volatile oil, and storing in a container;

(2) Adding Prunellae Spica, thallus laminariae, carthami flos, fructus Broussonetiae, ginseng radix, radix astragali, radix rehmanniae, radix asparagi, and Poria into the medicinal liquid and residue after extracting volatile oil; decocting herba Epimedii, fructus Schisandrae chinensis, and radix Gentianae with water twice, adding 10 times of water for the first time, boiling for 3 hr, adding 8 times of water for the second time, boiling for 2 hr, filtering, concentrating the extractive solution, adding ethanol to precipitate for two times until ethanol content is 50-80%, and recovering ethanol to obtain Chinese medicinal extract;

(3) Adding 3-8% water into nacreous layer powder, boiling, maintaining the temperature for 6-60 hr, filtering, and concentrating to obtain nacreous layer powder extractive solution.

(4) Adding nacreous layer powder extract into the Chinese medicinal extract, stirring, adding borax, mirabilitum, PVP-K30 and puerarin, stirring for dissolving;

(5) And (3) adding the solubilizing agent Tween-80 into the extracted volatile oil, uniformly mixing, adding the volatile oil into the liquid medicine prepared in the step (4), uniformly mixing, and adding glycerol, propylene glycol, phenoxyethanol and ethylparaben, and stirring to dissolve. And finally, slowly adding the natural borneol and menthol ethanol solution under stirring, regulating the pH value to be between 6.4 and 7.8 by using disodium hydrogen phosphate solution or sodium dihydrogen phosphate solution, adding water to the whole amount, uniformly mixing, filtering, filling into an eye-protecting adhesive carrier such as pure cotton cloth, natural silk cloth aluminum-plastic composite film bag or other containers which are cut into a certain shape, and sealing.

A. pulverizing Inulae flos, rhizoma Sparganii, radix Angelicae sinensis, fructus Leonuri, flos Eriocauli, fructus Tribuli, herba Epimedii, fructus Schisandrae chinensis, radix Gentianae, and rhizoma Acori Graminei into coarse powder, adding 60-85% ethanol solution of 6-8 times of the powder, ultrasonic extracting the ethanol soaked material for 1.5 hr, filtering, adding 3-4 times 60-85% ethanol solution into the residue, ultrasonic extracting for 1.0 hr, and filtering. Combining the two filtrates, and recovering ethanol. Obtaining ethanol extract.

B. Decocting Prunellae Spica, thallus laminariae, carthami flos, fructus Broussonetiae, ginseng radix, radix astragali, radix rehmanniae, radix asparagi, and Poria with water twice, adding 10 times of water in the first time, boiling for 3 hr, adding 8 times of water in the second time, boiling for 2 hr, filtering, mixing filtrates, and concentrating to obtain Chinese medicinal extract;

C. adding 3-8% water into nacreous layer powder, boiling, maintaining the temperature for 6-60 hr, filtering, and concentrating to obtain nacreous layer powder extractive solution.

D. Adding nacreous layer powder extract and ethanol extract into the Chinese medicinal extract, stirring, mixing, adding borax, mirabilitum, and Tween-80 as solubilizer, PVP-K30 and puerarin, natural Borneolum Syntheticum, mentholum, glycerol, propylene glycol, phenoxyethanol, and ethylparaben, stirring, mixing, adding adjuvant, and adjusting pH to 6.4-7.8 with disodium hydrogen phosphate solution or sodium dihydrogen phosphate solution to obtain eye massage cream; or adding emulsion matrix, etc., and making into cream, lotion, patch, etc.

Description of the embodiments

In accordance with the present disclosure, the following detailed procedure is presented.

1. Example 1

One of the eye protection patches is made, and the eye protection patch comprises the following components in parts by weight: 6 parts of selfheal, 6 parts of kelp, 10 parts of inula flower, 3 parts of mirabilite, 6 parts of rhizoma sparganii, 1 part of puerarin, 8 parts of Chinese angelica, 4 parts of safflower, 6 parts of motherwort fruit, 30 parts of pearl powder, 9 parts of pipewort, 4 parts of fructus Broussonetiae, 3 parts of fructus tribuli, 1 part of gentian, 3 parts of ginseng, 4 parts of astragalus mongholicus, 7 parts of radix rehmanniae, 9 parts of radix asparagi, 10 parts of epimedium, 3 parts of shizandra berry, 6 parts of white poria cocos, and 3 parts of rhizoma acori graminei.

The preparation method comprises the following steps:

(1) Pulverizing Inulae flos, rhizoma Sparganii, radix Angelicae sinensis, fructus Leonuri, fructus Tribuli, flos Eriocauli, and rhizoma Acori Graminei into coarse powder, distilling with steam, extracting volatile oil, and storing in a container;

(2) Adding Prunellae Spica, thallus laminariae, carthami flos, fructus Broussonetiae, ginseng radix, radix astragali, radix rehmanniae, radix asparagi, poria, herba Epimedii, fructus Schisandrae chinensis, and radix Gentianae into the medicinal liquid and residue after extracting volatile oil, decocting with water twice, adding 10 times of water for the first time, boiling for 3 hr, adding 8 times of water for the second time, boiling for 2 hr, concentrating the extractive solution, adding ethanol until ethanol content is 50-75%, precipitating twice, and recovering ethanol to obtain the final medicinal extract;

(3) Adding 3-8% water into nacreous layer powder, boiling, maintaining for 12-60 hr, filtering, and concentrating to obtain nacreous layer powder extractive solution.

(4) Adding nacreous layer powder extract into the Chinese medicinal extract, stirring, mixing, adding Mirabilitum, borax, PVP-K30 and puerarin, stirring to dissolve;

(5) And (3) adding the extracted volatile oil into the solubilizing agent Tween-80, uniformly mixing, adding the volatile oil into the liquid medicine prepared in the step (4), uniformly mixing, and adding glycerol, propylene glycol, phenoxyethanol and ethylparaben, and stirring for dissolving. And finally, slowly adding the natural borneol and menthol ethanol solution under stirring, regulating the pH value to be between 6.4 and 7.8 by using disodium hydrogen phosphate solution or sodium dihydrogen phosphate solution, adding water to the whole amount, uniformly mixing, filtering, filling into an eye-protecting adhesive carrier such as pure cotton cloth, natural silk cloth aluminum-plastic composite film bag or other containers which are cut into a certain shape, and sealing.

2. Example two

The second eye-protecting patch is prepared from the following components in parts by weight: 9 parts of selfheal, 9 parts of kelp, 12 parts of inula flower, 6 parts of mirabilite, 9 parts of rhizoma sparganii, 0.75 part of puerarin, 10 parts of angelica, 5 parts of safflower, 9 parts of motherwort fruit, 33 parts of pearl powder, 12 parts of pipewort, 5 parts of fructus Broussonetiae, 4 parts of fructus tribuli, 2 parts of gentian, 4 parts of ginseng, 6 parts of astragalus membranaceus, 10 parts of radix rehmanniae, 12 parts of radix asparagi, 12 parts of epimedium, 3 parts of shizandra berry, 6 parts of white poria cocos, and 3 parts of rhizoma acori graminei.

The preparation method is the same as in example one.

3. Example III

The eye massage cream is prepared from the following components in parts by weight: 9 parts of selfheal, 9 parts of kelp, 9 parts of inula flower, 6 parts of mirabilite, 8 parts of rhizoma sparganii, 1 part of puerarin, 9 parts of Chinese angelica, 5 parts of safflower, 9 parts of motherwort fruit, 32 parts of pearl powder, 12 parts of pipewort, 6 parts of fructus Broussonetiae, 6 parts of fructus tribuli, 2 parts of gentian, 4 parts of ginseng, 6 parts of astragalus membranaceus, 10 parts of radix rehmanniae, 12 parts of radix asparagi, 12 parts of epimedium, 3 parts of shizandra berry, 6 parts of white poria cocos, and 3 parts of rhizoma acori graminei.

The preparation method comprises the following steps:

A. pulverizing Inulae flos, rhizoma Sparganii, radix Angelicae sinensis, fructus Leonuri, flos Eriocauli, fructus Tribuli, herba Epimedii, fructus Schisandrae chinensis, radix Gentianae, and rhizoma Acori Graminei into coarse powder, adding 60-85% ethanol solution with the amount of 6-8 times of the powder, ultrasonic extracting the ethanol soaked material for 2 hr, filtering, and recovering ethanol from the filtrate. Obtaining ethanol extract.

B. Adding 6-10 times of water into Prunellae Spica, thallus laminariae, carthami flos, fructus Broussonetiae, ginseng radix, radix astragali, radix rehmanniae, radix asparagi and Poria, decocting with water twice, adding 10 times of water in the first time, boiling for 2 hr, adding 8 times of water in the second time, boiling for 1.5 hr, concentrating the extractive solution, adding ethanol until ethanol content is 50-75%, precipitating twice, and recovering ethanol to obtain Chinese medicinal extract;

C. adding 3-8% water into nacreous layer powder, boiling, maintaining for 12-60 hr, filtering, and concentrating to obtain nacreous layer powder extractive solution.

D. Adding nacreous layer powder extract into the Chinese medicinal extract, stirring, adding borax, mirabilitum, and solubilizing agent Tween-80 and ethanol extract, PVP-K30 and puerarin, natural Borneolum Syntheticum, mentholum, glycerol, propylene glycol, phenoxyethanol, and ethylparaben, stirring, adding adjuvant, and making into eye massage cream;

3. example IV

The eye emulsion is prepared from the following components in parts by weight: 8 parts of selfheal, 8 parts of kelp, 10 parts of inula flower, 6 parts of mirabilite, 9 parts of rhizoma sparganii, 1 part of puerarin, 10 parts of Chinese angelica, 5 parts of safflower, 9 parts of motherwort fruit, 28 parts of pearl powder, 12 parts of pipewort, 6 parts of fructus Broussonetiae, 6 parts of fructus tribuli, 2 parts of gentian, 4 parts of ginseng, 6 parts of astragalus membranaceus, 12 parts of radix rehmanniae, 12 parts of radix asparagi, 12 parts of epimedium, 3 parts of shizandra berry, 6 parts of white poria cocos, and 3 parts of rhizoma acori graminei.

The preparation method is basically the same as that of the third embodiment, and the eye massage emulsion is prepared by adding the emulsion auxiliary materials after all materials are added.

5. Example five

Local skin irritation test

12 adult New Zealand rabbits are taken, the common level is not limited, the weight of the rabbits is 2.0 to 3. okg, the rabbits are divided into two groups, one group is an eye patch group, and the other group is eye massage cream. The hairs on both sides of the back spine of the experimental animal are cut off (the epidermis can not be damaged) 24 hours before the experiment, and the hair removing range is about 5cm multiplied by 8cm on the left and right sides. By adopting a self-contrast method, the left side of each rabbit in the first group is applied with 4.5 cm multiplied by 7.5 cm eye protection patches (experiments) prepared in the second embodiment of the invention, the right side is applied with 4.5 cm multiplied by 7.5 cm physiological saline patches (contrast), and the two patches are continuously applied for 7d three times a day for 30 minutes each time. The eye massage cream prepared in the third embodiment of the present invention was applied to the left side of each rabbit in the second group (test), and physiological saline was applied to the right side (control), three times a day, followed by administration for 7d. Skin changes were observed immediately after each dose and about 2 hours after the dose and 1, 6, 12, 24, h after the last dose on day 7. Scoring was performed according to the skin irritation assay scoring criteria of table 1.

TABLE 1 skin irritation test scoring criteria

Test results: see table 2.

TABLE 2 skin irritation response score table

Conclusion: the test result shows that the eye protection plaster and the eye massage cream prepared by the composition have no skin irritation.

6. Example six eye stimulatory experiments were performed on 12 adult New Zealand rabbits, normal grade, with no limitation on male and female, and a body weight of 2.0-3. okg. Prior to the test, visual inspection: the cornea is free from turbidity, conjunctiva congestion, edema and secretion, pupil is round, two sides are equal, and the light reflection is good. Slit lamp inspection: the cornea is transparent and has no pannus and pannus; clear iris texture and no congestion and edema. 1% sodium fluorescein is used as an eye drop, each rabbit is washed clean by normal saline after dropping one drop, and then observed by a slit lamp, and the cornea is normal when the cornea is not stained. The eye mask is divided into two groups, wherein the first group is an eye mask liquid medicine group prepared according to the second embodiment of the invention, and the second group is an eye massage cream group prepared according to the third embodiment of the invention, and a left eye self-comparison method and a right eye self-comparison method are respectively adopted. The eye protection patch medicine liquid (test) prepared in the second embodiment of the invention is dropped into the left eye of each rabbit in the first group, physiological saline is dropped into the right eye (control), and then the eyelid is gently closed for about 10 seconds each time, and the medicine liquid is continuously administrated for 7d three times a day. In the second group, the right eye of each rabbit was coated with an appropriate amount of the eye massage cream prepared in the third embodiment of the present invention (test), and the right eye was dropped with physiological saline (control), one drop at a time, and then the eyelid was gently closed for about 10 seconds, three times a day, followed by administration for 7d. Eye changes were observed before and after daily dosing, and 1, 24, 48, 72h and 7d after the last dosing, eye drops were rinsed with 1% sodium fluorescein and the rabbit eyes were examined with a slit lamp for conjunctiva, cornea, iris and other observed lesions and scored according to the eye irritation scoring criteria of table 3.

TABLE 3 eye irritation scoring criteria

Killing experimental animals and taking materials

At the end of the 3 month observation period following dosing, animals were sacrificed using air embolism. Meanwhile, the eyeballs are taken for pathological preparation.

Evaluation of results

According to SOP/LOC-008-1-1 standard operation procedure for eye irritation test, according to the requirements of Table 3, the irritation response scores of cornea, iris and conjunctiva of each animal at each observation time are added to obtain total integral, and the integral sum of one group is divided by the animal number to obtain final score. The degree of irritation was judged according to the eye irritation evaluation criteria, as shown in Table 4. Meanwhile, pathological changes of tissues such as anterior segments (including cornea, iris and conjunctiva) and posterior segments (crystalline lens, retina and choroid) of eyes are observed and evaluated by reading pathological sections of eyeballs.

TABLE 4 evaluation criteria for eye irritation

TABLE 5 eye irritation response score table

When eye irritation was observed, no irritation was observed in the conjunctiva, cornea, and iris of eyes of both groups of 6 rabbits, and no other damage was observed. Pathological changes are not seen in the pathological section of eyeball, and tissues such as anterior segment (including cornea, iris and conjunctiva) and posterior segment (lens, retina and choroid) of eye are observed.

The test results showed that neither the test group nor the control group had ocular irritation.

7. Example seven human trial experiments selected volunteers, male and female were not limited, aged 6-18 years, were healthy, had no eye disease, and were 30 total people. The method adopts a blind test and a left-right eye comparison method, namely, one eye is applied to the eye protection patch (test) prepared in the second embodiment of the invention, and the other eye is applied to the normal saline eye protection patch (comparison), and the left eye and the right eye are alternately tested in a random double-blind way each time, namely, a subject does not know whether the eye is applied to a test product or a comparison product; the adhesive is continuously applied for 7d twice a day for 15-20 minutes each time. Before and after each application, eyes of a tester are checked, subjective feeling and using effect are inquired, and records are made in time.

Test results the test drug showed 1 case of slight discomfort, mainly slight fever and itching; the control drug was 0.

Other people have no uncomfortable feeling, most people show that the cool comfort level and the moisturizing and anti-dry eye effect of the test medicine are better than those of the reference medicine, and the test medicine has a clear and bright feeling after the test medicine is moistened.

8. Example eight

In the using process of the external composition for preventing and delaying myopia, the human body trial effect test is carried out through the second eye patch of the embodiment and the third massage cream of the embodiment.

90 volunteers meeting the conditions are selected, myopic patients aged 7-12 years old are unlimited for men and women, binocular myopia is selected in < -0.5D < -3D and no other eye disease patients are selected, and the volunteers are randomly divided into 3 groups of 30 people. Under the coordination and supervision of parents, the eye protection plaster prepared by the embodiment II of the invention is applied to eyes in the test 1 group, the eyes are tightly closed in the test 2 group, the massage cream prepared by the embodiment III of the invention is used for massaging acupoints such as Zanzhu, yangbai, yuyao, sun, sibai, qiuzhu, jingming and the like for about 30 minutes around eyes, and the eye protection plaster prepared by the embodiment III of the invention is applied to eyes in the test 3 group which is a comparison group. 2 times per day for 6 months. The vision inspection is carried out before each group of medicines is used, and the vision inspection is carried out after the medicines are used for 3 and 6 months respectively.

Curative effect judgment standard:

the effect is shown: vision improvement-1D and above;

the method is effective: slightly improving vision or maintaining the vision without reduction;

invalidation: vision continues to decline.

The test results are shown in the following table:

the trial result shows that the eye plaster and the eye massage cream of the composition have obvious effects of preventing and delaying myopia.

The external eye medicament prepared by the invention has no adverse reaction and toxic or side effect in human body trial, and the safety of the medicament is proved.

Claims

1. A topical composition for preventing and treating myopia and its preparation method, characterized by, by resolving hard mass detumescence, pathogenic fire purging and qi lowering traditional Chinese medicine Prunellae Spica, thallus laminariae, radix Trichosanthis, rhizoma Dioscoreae Bulbiferae, bulbus Fritillariae Cirrhosae, inulae flos, mirabilitum, fructus Aurantii and blood breaking and stasis expelling, qi promoting and pain relieving traditional Chinese medicine rhizoma Sparganii, curcumae rhizoma, semen Persicae, hirudo, puerarin, folium Ginkgo, radix Angelicae sinensis, carthami flos, rhizoma Ligustici Chuanxiong, notoginseng radix, fructus Leonuri, caulis Spatholobi, olibanum, myrrha, saviae Miltiorrhizae radix, wind dispelling and heat clearing away, eyesight improving and nebula removing traditional Chinese medicine flos Eriocauli, flos Chrysanthemi, fructus Broussonetiae, fructus Tribuli, semen Cassiae, margarita, concha Margaritifera (layer powder), concha Haliotidis, folium Mori, radix Gentianae, herba Menthae, herba Schizonepetae, and other deficiency tonifying traditional Chinese medicine such as radix Ginseng, radix Codonopsis, radix astragali, atractylodis rhizoma, radix asparagi, radix Ophiopogonis, fructus Ligustri Lucidi, radix Adenophorae, radix Glehniae, radix Morindae officinalis, rhizoma Polygonati, fructus Schisandrae chinensis, poria, rhizoma Acori Graminei, and the like, and it is prepared into topical patch for preventing and treating myopia, eye diseases, and its preparation, such as eye drop, and eye drop, and eye drop.

2. The external composition for preventing and treating myopia and the preparation method thereof according to claim 1, wherein the external composition is characterized by comprising the traditional Chinese medicines of selfheal, kelp, radix trichosanthis, inula flower, mirabilitum, fructus aurantii, blood breaking, stasis removing, qi circulation promoting and pain relieving traditional Chinese medicines of rhizoma sparganii, rhizoma curcumae, leech, puerarin, ginkgo leaf, angelica sinensis, safflower, pseudo-ginseng, motherwort fruit and root of red-rooted salvia, the traditional Chinese medicines of pipewort, chamomile, fructus Broussonetiae, caltrop, mother-of-pearl (layer powder), concha haliotidis, gentian and herba schizonepetae, the traditional Chinese medicines of tonifying qi, nourishing blood, soothing the nerves, promoting intelligence, nourishing yin, tonifying yang and the like, the traditional Chinese medicines of ginseng, astragalus, radix rehmanniae, radix asparagi, glossy privet fruit, epimedium, fructus psoraleae, medlar, shizandra, rhizoma acori graminei, and the like.

3. The composition for external use for preventing and treating myopia and its preparation method according to claim 1 and 2, wherein: the traditional Chinese medicine is prepared from common selfheal fruit-spike, kelp, inula flower, mirabilite, common burreed rhizome, puerarin, chinese angelica, safflower, motherwort fruit, chinese angelica root, common burreed rhizome, auxiliary materials of wind dispelling, heat clearing, eyesight improving and nebula removing, chinese medicinal pipewort, fructus Broussonetiae, caltrop, mother-of-pearl (layer powder) and gentian, auxiliary materials of qi supplementing, blood nourishing, nerve soothing, intelligence improving, yin nourishing, yang strengthening and other deficiency tonifying traditional Chinese medicines of ginseng, astragalus mongholicus, radix rehmanniae, radix asparagi, epimedium, schisandra chinensis, poria cocos, rhizoma acori graminei and the like.

4. A topical composition for preventing and treating myopia and its preparation method according to claims 1, 2 and 3, wherein the best choice formulation comprises by weight: 3-12 parts of selfheal, 3-12 parts of kelp, 4-18 parts of inula flower, 1-9 parts of mirabilite, 2-10 parts of rhizoma sparganii, 0.2-2 parts of puerarin, 5-15 parts of angelica, 2-10 parts of safflower, 3-12 parts of motherwort fruit, 3-18 parts of pipewort, 2-10 parts of fructus Broussonetiae, 1-8 parts of fructus tribuli, 10-50 parts of pearl powder, 0.5-5 parts of gentian, 2-10 parts of ginseng, 3-12 parts of astragalus mongholicus, 3-15 parts of radix rehmanniae, 3-15 parts of radix asparagi, 5-20 parts of epimedium, 1-6 parts of schisandra chinensis, 3-12 parts of poria cocos and 1-6 parts of rhizoma acori graminei. The above Chinese medicinal materials are used for extracting effective components according to their characteristics and medicinal requirements, and adding pharmaceutically acceptable adjuvants into the extracts to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

5. The composition for external use for preventing and treating myopia and its preparation method according to claims 1, 2, 3 and 4, wherein the best choice formulation is optimized by weight: 5-10 parts of selfheal, 5-10 parts of kelp, 6-15 parts of inula flower, 2-8 parts of mirabilite, 3-9 parts of rhizoma sparganii, 0.3-1.5 parts of puerarin, 6-12 parts of angelica, 3-8 parts of safflower, 5-10 parts of motherwort fruit, 20-40 parts of pearl powder, 6-15 parts of pipewort, 3-8 parts of fructus Broussonetiae, 2-7 parts of fructus tribuli, 0.8-4 parts of gentian, 2-8 parts of ginseng, 4-10 parts of radix astragali, 5-12 parts of radix rehmanniae, 5-12 parts of radix asparagi, 6-16 parts of epimedium, 2-6 parts of schisandra chinensis, 5-10 parts of white poria and 2-6 parts of rhizoma acori graminei. The above Chinese medicinal materials are used for extracting effective components according to their characteristics and administration requirements, and adding various extracts into pharmaceutically acceptable adjuvants to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

6. A topical composition for preventing and treating myopia and its preparation according to claims 1, 2, 3, 4, 5, wherein the best further choice formulation is further optimized in parts by weight: 6-9 parts of selfheal, 6-9 parts of kelp, 8-14 parts of inula flower, 3-8 parts of mirabilite, 4-9 parts of rhizoma sparganii, 0.5-1.2 parts of puerarin, 8-10 parts of angelica, 4-6 parts of safflower, 6-9 parts of motherwort fruit, 22-36 parts of pearl powder, 8-12 parts of pipewort, 4-6 parts of fructus Broussonetiae, 2-6 parts of fructus tribuli, 1-3 parts of gentian, 2-6 parts of ginseng, 4-8 parts of astragalus mongholicus, 6-12 parts of radix rehmanniae, 8-12 parts of radix asparagi, 8-15 parts of epimedium, 2-5 parts of schisandra chinensis, 5-9 parts of poria cocos and 2-5 parts of rhizoma acori graminei. The above Chinese medicinal materials are extracted according to their respective characteristics and requirements, and various extracts are added into pharmaceutically acceptable adjuvants to make into topical preparations for eye such as patch, unguent, cream, emulsion, patch, etc.

7. The external composition for preventing and treating myopia and its preparation method according to claim 1, 2, 3, 4, 5 and 6, further comprising transdermal absorption enhancer, humectant and pharmaceutically acceptable adjuvants.

8. The composition for external use for preventing and treating myopia and its preparation method according to claim 7, wherein the percutaneous absorption enhancer comprises one or more of Borneolum Syntheticum, natural borneol (D-borneol), menthol, camphor, eucalyptus oil, oleic acid, azone, dimethyl sulfoxide, etc. The humectant includes, but is not limited to, one or more of trehalose, oat beta-glucan, polyethylene glycol, glycerol, propylene glycol, butylene glycol, hexylene glycol, xylitol, sorbitol, PVP-K30, sodium hyaluronate, panthenol, ceramides, sodium Pyrrolidone Carboxylate (PCA).

9. The external composition for preventing and treating myopia and its preparation method according to claim 1, 2, 3, 4, 5, 6, 7, 8, wherein the preparation method is as follows:

(3) Adding 3-8 amount of water into the nacreous layer powder, boiling, maintaining the temperature for 6-60 hours, filtering, and concentrating to obtain nacreous layer powder extract;

10. The external composition for preventing and treating myopia and its preparation method according to claim 1, 2, 3, 4, 5, 6, 7, 8, wherein the preparation method is as follows:

A. pulverizing Inulae flos, rhizoma Sparganii, radix Angelicae sinensis, fructus Leonuri, flos Eriocauli, fructus Tribuli, herba Epimedii, fructus Schisandrae chinensis, radix Gentianae, and rhizoma Acori Graminei into coarse powder, adding 60-85% ethanol solution of 6-8 times of the powder, ultrasonic extracting the ethanol soaked material for 1.5 hr, filtering, adding 3-4 times 60-85% ethanol solution into the residue, ultrasonic extracting for 1.0 hr, and filtering. Combining the two filtrates, and recovering ethanol. Obtaining ethanol extract;

B. decocting Prunellae Spica, thallus laminariae, carthami flos, fructus Broussonetiae, ginseng radix, radix astragali, radix rehmanniae, radix asparagi, and Poria with water twice, adding 10 times of water in the first time, boiling for 3 hr, adding 8 times of water in the second time, boiling for 2 hr, filtering, mixing extractive solutions, and concentrating to obtain Chinese medicinal extract;

C. adding 3-8 amount of water into the nacreous layer powder, boiling, maintaining the temperature for 6-60 hours, filtering, and concentrating to obtain nacreous layer powder extract;