Traditional Chinese medicine extract for resisting oxidation, moistening skin and protecting eyes as well as preparation method and application of traditional Chinese medicine extract

Abstract

The invention discloses a traditional Chinese medicine extract for resisting oxidation, moistening skin and protecting eyes as well as a preparation method and application of the traditional Chinese medicine extract. The traditional Chinese medicine extract is prepared from water extracts of radix notoginseng, radix sophorae flavescentis and cortex phellodendri bark according to the ratio of 1: 1: 1-1: 1: 10. The preparation method of the traditional Chinese medicine extract comprises the following steps: stirring and mixing aqueous extracts of radix notoginseng, radix sophorae flavescentis and cortex phellodendri according to the volume ratio of 1: 1: 1-1: 1: 10 at the temperature of 20-60 DEG C for 3-15 minutes to obtain the target traditional Chinese medicine extract. The traditional Chinese medicine extract is applied to preparation of a medicine for treating xerophthalmia. The ophthalmic preparation for treating the xerophthalmia, prepared from the traditional Chinese medicine extract provided by the invention, does not contain preservatives, and is long in shelf life, high in safety, good in treatment effect on the xerophthalmia, simple in preparation method and worthy of popularization and application.

Description

Technical Field

[0001] The invention belongs to the technical field of Chinese medicine extracts, and specifically relates to an antioxidant, skin-moistening and eye-protecting Chinese medicine extract and a preparation method and application thereof. Background Art

[0002] Dry eye refers to an eye disease caused by various factors, with dry eyes as the main symptom and tear secretion disorder. It is often accompanied by itchy eyes, foreign body sensation, burning sensation, or photophobia, blurred vision, and fluctuations in vision. Common symptoms include dry eyes, easy fatigue, itchy eyes, foreign body sensation, painful burning sensation, sticky secretions, fear of wind, photophobia, and sensitivity to external stimuli; sometimes the eyes are too dry, and the basic tears are insufficient, which stimulates reflex tear secretion and causes frequent tears; in more serious cases, the eyes will be red, swollen, congested, keratinized, and the corneal epithelium will be broken and filaments will adhere. This damage can cause corneal and conjunctival lesions over time and affect vision. At present, topical treatment drug preparations for dry eye generally add preservatives, and their safety is also uncertain. Therefore, it is extremely necessary to study a safe and effective drug for the treatment of dry eye. Summary of the invention

[0003] The first purpose of the present invention is to provide a Chinese herbal extract with antioxidant, moisturizing and eye-protecting properties. The second purpose of the present invention is to provide a preparation method and application of the Chinese herbal extract.

[0004] The first object of the present invention is achieved by providing an antioxidant, moisturizing and eye-protecting Chinese herbal extract, which is composed of water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron chinense bark in a ratio of 1:1:1-1:1:10.

[0005] The second object of the present invention is achieved in this way. The preparation method of the antioxidant, moisturizing and eye-protecting Chinese herbal extract is to stir and mix the water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron chinense in a volume ratio of 1:1:1-1:1:10 at a temperature of 20-60°C for 3-15 minutes to obtain the target Chinese herbal extract.

[0006] The application of the antioxidant, skin-moistening and eye-protecting Chinese medicinal extract is in the preparation of dry eye medicine.

[0007] The beneficial effects of the present invention are as follows: the ophthalmic preparation for treating dry eye prepared by using the Chinese medicinal extract provided by the present invention does not contain preservatives, has a long shelf life, is highly safe, has a good therapeutic effect on dry eye, and has a simple preparation method, and is worthy of popularization and application. BRIEF DESCRIPTION OF THE DRAWINGS

[0008] Figure 1 The figure is a graph showing the scavenging ability of the Chinese herbal extract of Example 1 at different concentrations on DPPH free radicals. DETAILED DESCRIPTION

[0009] The present invention is further described in detail below in conjunction with the accompanying drawings and embodiments, but the present invention is not limited in any way. Any changes or improvements made based on the teachings of the present invention fall within the protection scope of the present invention.

[0010] The invention discloses an anti-oxidation, skin-moistening and eye-protecting Chinese medicinal extract. The Chinese medicinal extract is composed of water extracts of notoginseng root, sophora flavescens root and phellodendron amurense bark in a ratio of 1:1:1-1:1:10.

[0011] The effective components in the Chinese medicine extract are as follows: berberine 0.1-5.0%, total flavonoids 0.1-5%, total sterols 0.1-7%, and caryophyllene oil 0.1-5%.

[0012] The preparation method of the water extract of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense is as follows: chop Panax notoginseng root, Sophora flavescens root or Phellodendron amurense bark into pieces of ≤5 mm, wash and sterilize, soak in pure water for 10-120 minutes, and then place in a conventional reactor or microwave reactor for extraction at 20-60° C. for 30-200 minutes to obtain the water extract of Panax notoginseng root, Sophora flavescens root or Phellodendron amurense; The mass ratio of Panax notoginseng root, Sophora flavescens root or Phellodendron amurense bark to pure water is 5-50:1000.

[0013] The present invention also provides a method for preparing the antioxidant, moisturizing and eye-protecting Chinese herbal extract, which specifically comprises stirring and mixing water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense at a volume ratio of 1:1:1-1:1:10 at a temperature of 20-60°C for 3-15 minutes to obtain the target Chinese herbal extract.

[0014] The present invention further provides the use of the antioxidant, skin-moistening and eye-protecting Chinese medicinal extract in the preparation of dry eye medicine.

[0015] The present invention further provides an ophthalmic preparation based on the Chinese herbal extract, wherein the ophthalmic preparation is eye drops, eye patches, eye ointments or eye washes.

[0016] The preparation method of the eye drops is as follows: add 1000 ml of pure water to every 100 g of the traditional Chinese medicine extract, stir evenly, filter with a 0.45 μm filter membrane, and sterilize to obtain the eye drops.

[0017] The present invention also provides the use of the Chinese medicine extract in preparing toiletries, wherein the toiletries are facial cleansing liquid, facial mask, soap, perfumed soap, shampoo or shower gel.

[0018] Example 1 10g of Panax notoginseng root, Sophora flavescens root and Phellodendron bark were chopped into pieces of ≤5mm, washed three times with alcohol for disinfection and sterilization; then washed three times with a large amount of pure water to wash away dust and residual alcohol; then added 1000g of pure water and soaked for 80 minutes, placed in a microwave reactor at 20°C and extracted at 500W for 30 minutes, respectively, to obtain water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron bark; each water extract was mixed and stirred at a ratio of 1:1:1 at 20°C to obtain the target Chinese medicine extract. After detection and analysis, the Chinese medicine extract prepared in this embodiment contains the following main components by mass ratio: berberine 0.54%, total flavonoids 0.67%, total sterols 1%, and 1.2% galangal oil.

[0019] 100 g of the Chinese herbal medicine extract was added to 1000 g of water, stirred evenly, filtered through a 0.45 μm filter membrane, and sterilized to obtain eye drops.

[0020] Example 2 5g of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark were chopped into pieces of ≤5mm, washed three times with alcohol, then washed three times with a large amount of pure water, then soaked in 1000g of pure water for 120 minutes, and then placed in a microwave reactor for extraction at 60°C and 100W for 150 minutes to obtain water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark; each water extract was mixed and stirred at a volume ratio of 1:1:8 to obtain the target Chinese medicine extract. 150g of the Chinese medicine extract was added to 1000g of water and stirred evenly, then filtered with a 0.45μm filter membrane and sterilized to obtain eye drops.

[0021] Example 3 20g of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark were chopped into pieces of ≤5mm, washed three times with alcohol, then washed three times with a large amount of pure water, then soaked in 1000g of pure water for 90 minutes, placed in a microwave reactor and extracted at 40°C and 300W for 100 minutes to obtain water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark; each water extract was mixed and stirred at a volume ratio of 1:1:5 at 20°C to obtain the target Chinese medicine extract. 80g of the Chinese medicine extract was added to 1000g of water and stirred evenly, then filtered with a 0.45μm filter membrane and sterilized to obtain eye drops.

[0022] Example 4 50g of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark were chopped into pieces of ≤5mm, washed three times with alcohol for disinfection and sterilization; then washed three times with a large amount of pure water, added into a conventional reactor, soaked in 1000g pure water for 60 minutes, and then stirred and extracted at 40°C at a speed of 100r / min for 120 minutes to obtain water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark; each water extract was stirred and mixed at 60°C in a volume ratio of 1:1:3 for 15 minutes to obtain the target Chinese medicine extract. 100g of the Chinese medicine extract was added to 1000g of water and stirred evenly, then filtered with a 0.45μm filter membrane and sterilized to obtain eye drops.

[0023] Example 5 30g of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark were chopped into pieces of ≤5mm, washed three times with alcohol, then washed three times with a large amount of pure water, and then added to a reactor, and then 1000g of pure water was added to soak for 60 minutes, and then placed in a conventional reactor at 25°C and stirred at a speed of 120r / min for 200 minutes to obtain water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark; each water extract was stirred and mixed at a volume ratio of 1:1:8 at 45°C for 3 minutes to obtain the target Chinese medicine extract. 150g of the Chinese medicine extract was added to 1000g of water and stirred evenly, and then filtered with a 0.45μm filter membrane and sterilized to obtain eye drops.

[0024] Comparative Example 1 The Chinese medicine extract of this comparative example is the water extract of Panax notoginseng root prepared according to the method of Example 1. Other operation steps are the same as those of Example 1.

[0025] Comparative Example 2 The Chinese medicine extract of this comparative example is the water extract of Sophora flavescens root prepared according to the method of Example 1. Other operation steps are the same as those of Example 1.

[0026] Comparative Example 3 The Chinese medicine extract of this comparative example is the water extract of Phellodendron amurense bark prepared according to the method of Example 1. The other operation steps are the same as those of Example 1.

[0027] Experimental Example 1: Effect of Chinese herbal extracts on dry eye rabbit model The experiment used 28 New Zealand rabbits (experimental animal production license number: SCXK (Zhejiang) 2018-0002), weighing 2.0-2.5kg, half male and half female, and was raised at a temperature of 20.2-22.6°C, a humidity of 52.7-63.4%, a 12-hour light / dark cycle, and a ventilation frequency of 8-10 times / hour; all rabbits were free to drink water. After removing the rabbit's left tear gland, Harderian gland and nictitating membrane, a cotton swab dipped in 50% trichloroacetic acid was applied to the bulbar conjunctiva 2-3mm away from the outer corneal margin for 5 seconds to make a rabbit dry eye model. The 28 New Zealand rabbits were randomly divided into 7 groups, blank group (right eye), treatment group 1 (eye drops prepared in Example 1), treatment group 2 (eye drops prepared in Example 4), comparative example group 1, comparative example group 2, comparative example group 3, and positive drug control group (sodium carboxymethyl cellulose), 4 in each group, half male and half female. The experiment was carried out after the second week after modeling.

[0028] The blank group was dripped with 50 μl of sterile saline on the left and right eyes, the treatment group 1 and the treatment group 2 were dripped with 50 μl of eye drops prepared in Example 1 and Example 2 on the left and right eyes, and the comparative example 1-3 groups were dripped with 50 μl of eye drops prepared in Comparative Example 1-3 on the left and right eyes; the positive drug group was dripped with 50 ul of 0.5% sodium carboxymethyl cellulose on the left and right eyes, once a day, for 100 consecutive days, and the right eye corneal conjunctiva Schirmer I test wetting length (mm) and bengalensis staining (grade) were examined. The results are shown in Table 1 and Table 2, respectively.

[0029] Table 1 Comparison of wetting length of right corneal conjunctiva in SchirmerⅠ test in each group (mm) Table 2 Bengal red corneal staining in each group (grade) Result analysis: The data in Table 1 and Table 2 show that the Chinese herbal extract prepared by the present invention has an excellent effect on treating dry eye in rabbit models, which is significantly better than the positive drug.

[0030] Experimental Example 2 Animal irritation test of the Chinese herbal medicine extract prepared in Example 1 1. Materials and Animals Three New Zealand rabbits weighing 2.0-2.5 kg were selected, including two males (numbered 1-2) and one female (the female was non-pregnant and had not given birth, numbered 3). They were raised at a temperature of 20.2-22.6°C, a humidity of 52.7-63.4%, a 12-hour light / dark cycle, and a ventilation frequency of 8-10 times / hour; all rabbits had free access to water.

[0031] 2. Multiple skin irritation tests Before the test, the hair on both sides of the spine of the New Zealand rabbit's back was cut off, the hair removal range was 3cm×3cm, and the coating area was 2.5cm×2.5cm. Take 0.5ml of the eye drops prepared in Example 1 and apply it on one side of the skin. The other side was used as a control. 4 hours after application, wash with water or a suitable non-irritating solvent to remove the residue. Apply once a day for 14 consecutive days. Observe the results 24 hours after each application, and score and grade according to the relevant requirements in the specification. In order to facilitate the application of eye drops and the observation of results, the hair should be cut if necessary. The treatment and preservation of the control area are the same as the test area. The test results are shown in Table 3.

[0032] As shown in Table 3, the eye drops provided by the present invention were tested for multiple intact skin irritation of rabbits and the results showed that they were non-irritating and no other toxicity was observed.

[0033] Table 3 The scores of multiple intact skin irritation reactions of the eye drops prepared in Example 1 to rabbits 3. Acute eye irritation test 1. Within 24 hours before the test, examine both eyes of the test animals to exclude animals with eye irritation symptoms, corneal defects and conjunctival damage. Gently pull open the lower eyelid of one eye of the rabbit, and drip 0.1 ml of the eye drops prepared in Example 1 into the conjunctival sac. The other eye is treated with physiological saline as a normal control. The upper and lower eyelids are passively closed for 4 seconds, and then rinsed with physiological saline after 30 seconds.

[0034] 2. Clinical examination and scoring: The eyes of the animals were examined 1h, 24h, 48h, 72h, 7d, 14d and 21d after the instillation of the eye drops prepared in Example 1, and the damage and recovery of the conjunctiva, iris and cornea of ​​the rabbits were observed with the naked eye. If no irritation reaction occurred at 72h, or the eye irritation reaction recovered at the 7th or 14th day, the experiment could be terminated in advance.

[0035] 3. Result evaluation method: 3.1 The acute irritation reactions of the cornea, iris and conjunctiva of the rabbits were scored according to the scoring criteria for eye damage, and the scores of each animal at three different observation times (the sum of the scores at 24h, 48h and 72h divided by the number of observations 3) were calculated. 3.2 The intensity of eye irritation caused by Chinese herbal medicine extracts was determined according to the average scores and recovery time of corneal, iris and conjunctival congestion and edema of the animals and the eye irritation reaction grading standard.

[0036] 4. Experimental results: No animal was poisoned. The eye irritation reaction scores are shown in Table 4.

[0037] Table 4 Rabbit eye irritation (within 3 days) reaction score Note: *The average score refers to the 24h, 48h, and 72h scores divided by the number of observation time periods 3.

[0038] The results in Table 4 show that the eye drops prepared in Example 1 of the present invention have no irritation to the acute eye irritation reaction intensity of rabbits.

[0039] Experimental Example 4 In vitro antioxidant activity test of the eye drops prepared in Example 1 The DPPH free radical scavenging ability of the eye drops prepared in Example 1 was measured.

[0040] Results: Figure 1 As shown, the eye drops prepared in Example 1 can increase the scavenging rate of DPPH free radicals by 90% at a concentration of 6.25-100% (V / V), and there is a statistical difference compared with the negative control group.

[0041] Experimental Example 5 Antiseptic performance test of the eye drops prepared in Example 1 1. The antibacterial and preservative effects of the eye drops prepared in Example 1 and the eye drops prepared in Comparative Examples 1-3 were tested with reference to the antibacterial efficacy test method of the 2020 edition of the Chinese Pharmacopoeia: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Aspergillus niger and Candida albicans were inoculated into the culture dishes to which the eye drops prepared in Example 1 were added, and cultured for 7 days. The results are shown in Table 5.

[0042] Results: As can be seen from Table 5, the eye drops with the Chinese medicine composition provided by the present invention as the main active ingredient have a good inhibitory effect on Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Aspergillus niger and Candida albicans without adding preservatives, and have a good preservative effect.

[0043] Table 5 Antibacterial efficacy of eye drops of Example 1 and Comparative Examples 1-3 2. The eye drops of Example 1 were subjected to an accelerated stability test.

[0044] The eye drops prepared in Examples 1-5 were sealed and placed under conditions of a temperature of 40°C, a relative humidity of 75%, and a light intensity of 2500LX. Samples were taken for inspection at the end of the first, second, third, and sixth months of the experiment. The inspection items were the appearance, sterility, and pH value of the eye drops.

[0045] The results of the accelerated inspection showed that there were no abnormalities in the inspection items, and the antibacterial efficacy of the eye drops prepared in Examples 1-5 still met the requirements of the pharmacopoeia.

[0046] The results of the accelerated stability study showed (Table 6) that after 24 months, the antibacterial efficacy of the eye drops of Example 1 still met the requirements of the pharmacopoeia.

[0047] Table 6 Accelerated test results Based on the above experimental examples, it can be seen that the Chinese herbal extract provided by the present invention has a better effect on dry eye syndrome, is non-irritating to the eyes, and has high safety. The accelerated investigation experiment shows that the eye drops of the present invention have stable performance within 2 years and have certain clinical value.

Claims

1. An antioxidant, moisturizing and eye-protecting Chinese herbal extract, characterized in that: The Chinese medicine extract is composed of water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense bark in a ratio of 1:1:1-1:1:

10.

2. The antioxidant, moisturizing and eye-protecting Chinese herbal extract according to claim 1, characterized in that: The effective components in the Chinese medicine extract are as follows: berberine 0.1-3.0%, total flavonoids 0.1-4%, total sterols 0.1-5%, and caryophyllene oil 0.1-5%.

3. The antioxidant, moisturizing and eye-protecting Chinese herbal extract according to claim 1, characterized in that: The preparation method of the water extract of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense is as follows: chop Panax notoginseng root, Sophora flavescens root or Phellodendron amurense bark into pieces of ≤5 mm, wash and sterilize, soak in pure water for 10-120 minutes, and then place in a conventional reactor or microwave reactor for extraction at 20-60° C. for 30-200 minutes to obtain the water extract of Panax notoginseng root, Sophora flavescens root or Phellodendron amurense; The mass ratio of Panax notoginseng root, Sophora flavescens root or Phellodendron amurense bark to pure water is 5-50:1000.

4. The method for preparing the antioxidant, moisturizing and eye-protecting Chinese herbal extract according to claim 1, characterized in that: The target Chinese medicine extract is obtained by mixing the water extracts of Panax notoginseng root, Sophora flavescens root and Phellodendron amurense in a volume ratio of 1:1:1-1:1:10 at a temperature of 20-60°C for 3-15 minutes.

5. Use of the antioxidant, moisturizing and eye-protecting Chinese medicinal extract according to claim 1 in the preparation of dry eye medicine.

6. An ophthalmic preparation based on the Chinese herbal extract according to claim 1, characterized in that: The ophthalmic preparation is eye drops, eye patches, eye ointments or eye wash solutions.

7. The ophthalmic preparation of the Chinese herbal extract according to claim 7, characterized in that: The preparation method of the eye drops is as follows: add 1000 ml of pure water to every 100 g of the traditional Chinese medicine extract, stir evenly, filter with a 0.45 μm filter membrane, and sterilize to obtain the eye drops.

8. The use of the Chinese herbal extract according to claim 1 in the preparation of toiletries, characterized in that: The toiletries are facial cleansing liquid, facial mask, soap, perfumed soap, shampoo or shower gel.

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