Use of a cinnamon extract in the manufacture of a medicament for alleviating ocular disease

Abstract

The application discloses application of a cinnamon extract in preparation of a medicine for relieving eye diseases and belongs to the technical field of traditional Chinese medicine extracts. The extract is prepared from cinnamon bark, cinnamon twig or cinnamon leaves as raw materials through a mobile bed extraction, countercurrent chromatography separation and water vapor distillation refining, and active ingredients include cinnamyl alcohol, cinnamyl acetate, cinnamyl aldehyde, o-methoxycinnamyl aldehyde and coumarin. The application provides eye drop preparations with the components as cores, the concentration is 45-500 μg / mL, and the eye drop preparations can be prepared into eye drop, eye gel, eye moistening liquid and other dosage forms without adding preservatives, thickening agents and other functional excipients. The pharmacodynamic effect shows that the eye drop preparation can quickly relieve eye fatigue, dryness, soreness and aching within 3-5 minutes, and can significantly improve symptoms of dry eye, flying fly disease, presbyopia and early cataract, and has a long-acting improvement effect on dry eye after refractive surgery.

Description

Technical Field

[0001] This invention relates to the field of traditional Chinese medicine extract technology, and in particular to the application of a cinnamon extract in the preparation of drugs to relieve eye diseases. Background Technology

[0002] With the widespread use of electronic devices, increased eye strain, and an aging population, eye problems such as eye fatigue, dry eye syndrome, floaters, presbyopia, and early cataracts are becoming increasingly common. Current clinical treatments primarily rely on artificial tears and nutritional supplements, which have drawbacks such as limited effectiveness, slow onset of action, inability to improve organic lesions, and the risk of dependence with long-term use.

[0003] Traditional Chinese medicine extracts have development potential in the field of eye care due to their advantages such as multi-target effects, mildness and safety, and no obvious drug resistance. Cinnamon is a traditional food and medicine material, and its extract contains a variety of active small molecules with anti-inflammatory, antioxidant, and mucosal protective effects. Summary of the Invention

[0004] The purpose of this invention is to provide an application of cinnamon extract in the preparation of drugs to relieve eye diseases. This cinnamon extract can significantly improve eye fatigue, dry eye syndrome, floaters, presbyopia, early cataracts and other eye discomforts. It is safe, non-irritating and suitable for long-term use.

[0005] To achieve the above objectives, the present invention provides an application of cinnamon extract in the preparation of drugs for relieving eye diseases. The cinnamon extract is obtained by sequentially extracting cinnamon bark, twigs, or leaves of cinnamon through moving bed extraction, countercurrent chromatography separation, and steam distillation. Component VI obtained after distillation following countercurrent chromatography separation is collected. The active ingredients of the cinnamon extract include cinnamic acid, cinnamyl alcohol, cinnamyl acetate, coumarin, cinnamaldehyde, and o-methoxycinnamaldehyde.

[0006] Preferably, the drug includes eye drops, eye lotion, eye gel, eye spray or eye patch infusion; the concentration of the cinnamon extract in the drug is 45-400 μg / mL.

[0007] Preferably, the eye disease is selected from at least one of eye strain, dry eye syndrome, floaters, presbyopia-related eye strain, blurred vision related to early cataracts, post-refractive surgery dry eye syndrome, and infectious conjunctivitis.

[0008] Preferably, the moving bed extraction solvent is a 50%-60% ethanol aqueous solution, the material-to-liquid ratio is 1g:8-12mL, and the extraction flow rate is 40-60mL / min.

[0009] Preferably, the countercurrent chromatography separation uses 25%-35% ethanol aqueous solution as the stationary phase and n-hexane as the mobile phase, with a mobile phase flow rate of 5-10 mL / min.

[0010] Preferably, the steam distillation temperature is 94-96℃ and the time is 2-3 hours.

[0011] On the other hand, the present invention provides a cinnamon extract composition, which is obtained by sequentially extracting cinnamon bark, twigs or leaves of cinnamon through moving bed extraction, countercurrent chromatography separation and steam distillation, and collecting component VI obtained by distillation after countercurrent chromatography separation; the active ingredients of the composition are identified by LCMS as including cinnamyl alcohol, cinnamyl acetate, coumarin, cinnamaldehyde and o-methoxycinnamaldehyde.

[0012] On the other hand, the present invention provides an ophthalmic preparation containing the above-mentioned cinnamon extract composition, wherein the concentration of the cinnamon extract composition in the preparation is 45-400 μg / mL; the pH value of the preparation is 6.0-7.0, and the osmotic pressure is 260-340 mOsm / L.

[0013] Preferably, the formulation does not contain preservatives, thickeners, or artificial flavors, and is prepared by filtering with water for injection through a 0.22 μm sterile filter membrane.

[0014] Preferably, the preparation is used to relieve at least one of the following ocular discomforts: eye strain, dry eye syndrome, floaters, presbyopia-related eye strain, blurred vision related to early cataracts, post-refractive surgery dry eye syndrome, and infectious conjunctivitis.

[0015] The ocular relief effect of cinnamon extract VI of this invention is presumably related to its multi-component synergistic mechanism: cinnamaldehyde and cinnamic acid have clear anti-inflammatory activities, which can reduce the release of pro-inflammatory factors (such as TNF-α, IL-6, and NO) by inhibiting the NF-κB signaling pathway, thereby alleviating conjunctival congestion and ocular surface inflammation; cinnamaldehyde also has broad-spectrum antibacterial activity, inhibiting common ocular pathogens (such as Staphylococcus aureus and Escherichia coli) and fungi (such as Candida albicans), helping to improve the pathogen load of infectious conjunctivitis; coumarin components have the effects of improving local microcirculation and antioxidation, which can reduce the damage of oxidative stress to ocular surface tissues; cinnamyl alcohol has a mild soothing and local anesthetic-like effect, which may help to quickly relieve eye fatigue and soreness. These multiple components achieve comprehensive relief of various ocular discomforts through multi-target synergistic effects such as anti-inflammation, antibacterial activity, antioxidation, and improvement of microcirculation.

[0016] Therefore, the application of a cinnamon extract in the preparation of a drug for relieving eye diseases has the following beneficial effects: Cinnamon extract is obtained through moving bed extraction, countercurrent chromatography separation, and steam distillation purification. It can simultaneously relieve eye fatigue, dry eyes, and eye pain, and quickly improve blurred vision. It has significant effects on dry eye syndrome, floaters, presbyopia, and early cataracts. It can also be used for long-term care of dry eye syndrome after myopia refractive surgery, achieving "multiple uses in one bottle" and making up for the single-function deficiency of commercially available products.

[0017] The technical solution of the present invention will be further described in detail below through embodiments. Detailed Implementation

[0018] The technical solution of the present invention will be further described below through embodiments.

[0019] To make the objectives, technical solutions, and advantages of this application clearer, more thorough, and more complete, the technical solutions of the present invention are clearly and completely described below through embodiments. The following detailed descriptions are all illustrations of embodiments, intended to provide further detailed explanations of the present invention. Unless otherwise specified, all technical terms used in this invention have the same meaning as commonly understood by one of ordinary skill in the art to which this application pertains.

[0020] The instruments, equipment, reagents, and materials used in the examples were all obtained commercially.

[0021] The extraction bed and extraction method used in this embodiment are the apparatus and method disclosed in patent application number 202411126616.3, entitled "A Method for Extracting Traditional Chinese Medicine Using a Moving Bed". This embodiment uses the apparatus and method described in patent 202411126616.3 to extract all components of cinnamon.

[0022] The cinnamon used in the examples is cinnamon twigs, cinnamon leaves, or cinnamon bark.

[0023] The apparatus used for countercurrent chromatography separation in the embodiments is described in patent 202411086627.3.

[0024] Example 1 A method for preparing cinnamon extract, comprising the following steps: S1. Crush the cinnamon bark into powder and pass it through a 20-mesh sieve. Then, perform full-component extraction using an extraction bed. The extraction solvent is a 60% (v / v) aqueous ethanol solution, with a mass ratio of cinnamon to extraction solvent of 1:10 mL. The pump flow rate of the extraction solvent is 50 mL / min.

[0025] S2. Collect the full-component extract and concentrate its volume to 1 / 3 of the original volume by vacuum concentration for later use.

[0026] S3. The obtained whole-component extract was separated by countercurrent chromatography, and the eluents at different time points were collected. An ethanol-water solution was mixed with the whole-component extract to obtain a loading solution, ensuring the ethanol concentration in the loading solution was 30% (i.e., the sample was loaded with the stationary phase); n-hexane was used as the mobile phase. After loading, the mobile phase was pumped in for countercurrent chromatography separation. The pumping rate of the mobile phase was 8 mL / min. During the countercurrent chromatography separation, the sample components rapidly partitioned between the two phases. Different components, due to differences in partition coefficients, flowed out sequentially from the rotary joint at the outlet of the equipment along with the mobile phase. The eluents at different time points (every 50 minutes as a group) were collected and labeled as component 1 to component 15. The solvents of each component obtained by countercurrent chromatography were recovered using a rotary evaporator to obtain 15 separated components.

[0027] S4. The 15 components (component 1-component 15) obtained by countercurrent chromatography were subjected to preliminary activity screening. The screening indicators included: (1) in vitro antioxidant activity, the free radical scavenging rate of each component at a concentration of 100 μg / mL was determined by DPPH free radical scavenging method; (2) in vitro antibacterial activity, the diameter of the inhibition zone of each component against Staphylococcus aureus (ATCC6538) and Escherichia coli (CICC10899) was determined by disk diffusion method; (3) in vitro anti-inflammatory activity, the inhibition rate of each component against NO release was determined by LPS-induced RAW264.7 macrophage inflammation model.

[0028] The screening results showed that component 6 performed best in all three indicators, significantly outperforming the other 14 components. p <0.05).

[0029] S5. Component analysis shows that component 6 is rich in small molecule compounds known to have anti-inflammatory, antibacterial, and antioxidant activities, such as cinnamaldehyde, cinnamic acid, and coumarin.

[0030] S6. Distill the obtained component 6: Transfer the separated component 6 to a distillation vessel and add 50 times the volume of water to fully submerge the cinnamon component.

[0031] Heat the distillation vessel to 95°C for steam distillation. Control the distillation temperature at 95°C and distill for 2-3 hours to ensure full extraction of volatile components and avoid component decomposition and energy waste. The generated steam, carrying components from cinnamon, is cooled by a condenser and flows out, yielding a purified extract of component 6, named Cinnamon Extract VI.

[0032] Example 2 A cinnamon extract VI solution with a final concentration of 200 μg / mL can be prepared using only water for injection and then filtered through a 0.22 μm sterile filter membrane before application.

[0033] The pH of cinnamon extract VI solution was measured twice in parallel, and the pH of cinnamon extract VI solution was found to be 6.5.

[0034] The pathogenic bacteria (coliform bacteria / Staphylococcus aureus / Pseudomonas aeruginosa / hemolytic streptococci) in cinnamon extract VI solution were tested according to GB 15979-2024 "Hygienic Requirements for Disposable Sanitary Products", and none were detected.

[0035] Heavy metal limits: lead content <0.03mg / kg, arsenic content <0.001mg / kg, mercury content <0.001mg / kg, all of which meet the requirements of the "Cosmetic Safety Technical Specifications" (2015 edition).

[0036] The results above show that the pH value of Cinnamon Extract VI eye drops is 6.5, which is within the suitable range for ophthalmic preparations; the microbiological indicators and heavy metal limits both meet the relevant standards. Because cinnamon extract itself has natural antibacterial and preservative properties, this preparation does not require the addition of preservatives to meet the microbiological limit requirements.

[0037] Example 3 Referring to GB 15979-2024 "Hygienic Requirements for Disposable Sanitary Products" and GB 38456-2020 "Hygienic Requirements for Antibacterial and Bacteriostatic Detergents", the bactericidal performance and stability of cinnamon extract VI stock solution were investigated.

[0038] (1) Sterilization performance: Using *Escherichia coli* (CICC10899), *Staphylococcus aureus* (ATCC6538), and *Candida albicans* (ATCC10231) as test strains, the sample concentration was the undiluted solution, and the contact time was 5 min. After three repeated tests, cinnamon extract VI showed a bactericidal rate greater than 95% against all three strains, indicating that it has strong antibacterial activity against Gram-negative bacteria, Gram-positive bacteria, and fungi.

[0039] (2) Stability (microbiological method): (1) One-year stability: Accelerated stability test (54℃, 14 days) was conducted. The bactericidal rate of the original sample solution after 5 min of contact with Candida albicans was greater than 95%, indicating that the one-year shelf life of the sample meets the requirements.

[0040] (2) Two-year stability: Accelerated stability test (37℃, three months) was adopted. Before and after the test, the bactericidal rate of the original solution of the sample after 5 minutes of contact with Candida albicans was greater than 95%, indicating that the storage shelf life of the sample for two years meets the requirements.

[0041] Example 4 Safety evaluation tests were conducted on the cinnamon extract VI prepared in Example 1 and the eye drops prepared in Example 2.

[0042] ① Acute oral toxicity test: Test substance: Cinnamon extract VI (stock solution).

[0043] Experimental animals: 20 SPF-grade KM mice, 10 males and 10 females, weighing 18-22g, and qualified through routine quarantine.

[0044] Feeding conditions: Temperature 20-25℃, humidity 40%-70%, 12h light / dark cycle.

[0045] The experimental method employed a single maximum dose method: animals were fasted for 12 hours, but water was permitted. A single gavage administration of 5000 mg / kg body weight (bw) was administered, with a volume of 0.2 mL / 10 g. Animals were observed for 14 consecutive days, recording signs of poisoning, behavior, diet, coat, urination and defecation, and mortality. At the end of the observation period, animals were euthanized, and gross necropsy was performed on major organs including the heart, liver, spleen, lungs, kidneys, and gastrointestinal tract. Evaluation criteria: LD 50 >5000mg / kg (actually non-toxic).

[0046] Experimental results: No animals died or showed signs of poisoning during the 14-day observation period; the mice's behavior, diet, water intake, fur, and urination and defecation were all normal; no abnormal changes such as organ congestion, edema, necrosis, or adhesions were found during necropsy; and there was no significant difference in weight gain compared with the control group.

[0047] Demonstrates the acute oral LD50 of cinnamon extract VI in mice. 50 >5000mg / kg, which is practically non-toxic.

[0048] ② Single ocular mucosal irritation test (rabbit).

[0049] Test substance: eye drops (200 μg / mL); Animals: Four healthy Japanese white rabbits, weighing 1.7-2.1 kg, with no damage or discharge to their eyes.

[0050] Experimental Methods: Both eyes were examined 24 hours prior to the experiment, and abnormal animals were excluded. 0.1 mL of the test substance was instilled into the right eye of each rabbit, and an equal volume of physiological saline was instilled into the left eye as a blank control. After instillation, the eyelids were gently closed for 10 seconds to prevent drug leakage. Observations and records were made at 1 hour, 24 hours, 48 ​​hours, and 72 hours after drug administration: cornea (cloudiness, damage), iris (congestion, edema), and conjunctiva (congestion, edema, secretions). Scores were calculated according to the "Eye Irritation Scoring Standard," and the average score was calculated.

[0051] Scoring and Grading: 0 points: no stimulation; 1-4 points: mild stimulation; 5-8 points: moderate stimulation; 9-11 points: severe stimulation.

[0052] Experimental results: At each time point, there was no hyperemia, edema, secretion, or cloudiness in the cornea, iris, or conjunctiva; the stimulation scores for both eyes were 0; and there was no delayed stimulation response within 72 hours.

[0053] It is known that cinnamon extract VI eye drops have no single-use irritation to the ocular mucosa of rabbits, and meet the safety requirements for ophthalmic preparations.

[0054] ③ Repeated eye mucosal irritation test (rabbit): Test method: 0.1 mL of the test eye drops was instilled into each eye daily for 7 consecutive days. Observation and scoring of corneal, iris, conjunctival, and tear secretion were performed at fixed times each day; observation continued for 48 hours after the 7th day of administration.

[0055] Test results: After 7 consecutive days of administration, there were no signs of eye irritation; no conjunctival congestion, edema, or increased secretions; the cornea was clear, the iris was clear, and there were no abnormal reactions; tear secretion was normal, and there was no photophobia or tearing.

[0056] It is known that cinnamon extract VI eye drops are non-irritating when applied to the eyes multiple times and are suitable for long-term use.

[0057] ④ Complete skin irritation test (rabbit): Experimental method: Hair was removed from both sides of the spine on the back of rabbits, covering an area of ​​approximately 3cm × 3cm without any damage. 0.5mL of eye drops were applied daily for 7 consecutive days. Skin reactions such as erythema, edema, exudation, and pigmentation were observed and scored daily.

[0058] Results: No erythema, edema, allergies, or pigmentation abnormalities were observed throughout the entire process; skin irritation score = 0.

[0059] It is known that cinnamon extract VI eye drops are non-irritating to intact skin.

[0060] Example 5 Clinical observation of the efficacy of cinnamon extract VI eye drops: Patient 1: Female, 15 years old.

[0061] Chief complaint: Long-term tutoring and homework, recurring eye fatigue, dry eyes, drowsiness, and blurred vision.

[0062] Diagnosis: Eye strain, dry eye syndrome (mild).

[0063] Medication: Cinnamon extract VI eye drops, once daily, 1-2 drops each time.

[0064] Therapeutic effects: After 3 minutes of application, eye fatigue and drowsiness are significantly relieved, and vision becomes clearer; after 3 days of continuous use, dryness disappears, and tolerance for studying and using the eyes is significantly improved.

[0065] Patient 2: Female, 19 years old.

[0066] Chief complaint: Eye pain, dryness, and slight blurred vision due to prolonged use of mobile phones.

[0067] Diagnosis: Video terminal syndrome, dry eye syndrome.

[0068] Dosage: 1-2 drops once daily.

[0069] Therapeutic effects: Relieves soreness and dryness quickly in 3-5 minutes; symptoms basically disappear after one week of continuous use, and it has become a regular use.

[0070] Patient 3: Male, 56 years old.

[0071] Chief complaint: Presbyopia, blurred vision at close range, difficulty cutting nails; double vision when looking at traffic lights while driving, and decreased distance vision.

[0072] Diagnosis: Presbyopia, decreased binocular accommodation function.

[0073] Medication: 1-2 times daily. Patients reported consistent use for more than 3 years (follow-up record).

[0074] Treatment efficacy: Improved near vision clarity, enabling normal fine motor skills; disappearance of double vision at traffic lights; improved visual acuity in the left eye from 1.0 to 1.2 during physical examination, with improvements in both near and far vision.

[0075] Patient 4: Female, 73 years old.

[0076] Chief complaint: Early-stage cataracts, floaters for more than 20 years, dry eye syndrome, blurred vision, and significant dryness of the eyes.

[0077] Diagnosis: Senile cataract (early stage), floaters, dry eye syndrome.

[0078] Dosage: Take once in the morning and once in the evening for 45 consecutive days.

[0079] Therapeutic effects: After 20 days of use, dry eyes and blurred vision improved; after 45 days, eye moisture and clarity were significantly improved, floaters were significantly reduced, and quality of life was improved.

[0080] Patient 5: Male, 60 years old.

[0081] Chief complaint: Floaters, dry eye syndrome, black shadows floating in front of the eyes, dry and uncomfortable eyes.

[0082] Diagnosis: Floaters, dry eye syndrome.

[0083] Dosage: 1-2 times daily for 5 consecutive days.

[0084] Efficacy: Upon first use, there may be a slight, transient burning sensation and white, thread-like discharge from the corners of the eyes; after 5 days, the floaters disappear, the eyes become moist and comfortable, and vision becomes clear.

[0085] Patient 6: Female, 55 years old.

[0086] Chief complaint: Presbyopia, requiring glasses for reading; dry and sore eyes due to prolonged computer use.

[0087] Diagnosis: Presbyopia, eye strain, dry eye syndrome.

[0088] Dosage: 1-2 drops once daily.

[0089] Therapeutic effects: Dryness and soreness disappear, and text can be read clearly at close range without glasses, significantly improving eye comfort.

[0090] Patient 7: Female, 24 years old.

[0091] Chief complaint: Severe dry eyes after laser eye surgery for myopia, requiring frequent use of artificial tears with only short-term effects.

[0092] Diagnosis: Post-refractive surgery dry eye syndrome.

[0093] Dosage: 1-2 drops once daily (before bedtime / upon waking).

[0094] Efficacy: After applying the drops, close your eyes for 3-5 minutes to completely relieve dry eyes and improve vision; once a day is sufficient for long-lasting effects, no need for frequent re-application; purely plant-based, with no drug dependence or side effects, and is well-tolerated.

[0095] Example 6 Clinical trial of the eye drops prepared in Example 2 for the treatment of infectious conjunctivitis.

[0096] A self-controlled pre- and post-treatment clinical trial was conducted on 10 patients with infectious conjunctivitis. Subjects used cinnamon extract VI eye drops (concentration 200 μg / mL) prepared in Example 2 once daily for 7 consecutive days, 1-2 drops each time. Ocular examinations were performed at baseline (before treatment) and on day 7 (after treatment). Assessment endpoints included core safety endpoints (corneal epithelial defect area, best corrected visual acuity BCVA, intraocular pressure IOP) and exploratory efficacy endpoints (conjunctival hyperemia grade, secretion score, pathogen load Ct value).

[0097] The area of ​​corneal epithelial defects was determined using a combination of corneal fluorescein staining and slit-lamp microscopy. Fluorescein staining solution was applied to the ocular surface, and the surface was observed and photographed under cobalt blue light using a slit-lamp microscope. The corneal epithelial defect area was delineated, and the pixel area was measured using an image analysis system. If no epithelial defect was found, the fluorescein staining was negative, and the defect area was recorded as 0 mm². 2 .

[0098] Best corrected visual acuity (BCVA) was measured using the LogMAR visual acuity chart: Subjects wore corrective lenses and used the LogMAR chart under standard lighting conditions; each letter was worth 0.02 logarithmic units, with 5 letters per row, and the entire row representing a change of 0.1 LogMAR units; the calculation formula was: The BCVA LogMAR score is calculated as 1.7 - 0.02 × the number of letters read. A lower score indicates better vision.

[0099] Intraocular pressure (IOP) was measured using a non-contact tonometer (NCT): the subject sat upright without touching the corneal surface; an airflow pulse was used to flatten the cornea, and the IOP value was calculated based on the external force required for corneal deformation. Each measurement was repeated twice, and the average value was recorded in mmHg.

[0100] Conjunctival hyperemia was graded using a slit-lamp microscope visual grading system, assessed on a scale of 0-4 points. 0 points: No congestion, clear conjunctival vessels, normal white color.

[0101] 1 point: Mild congestion, slightly dilated blood vessels, bright red in color, and the vascular texture is still clear.

[0102] 2 points: Moderate congestion, obvious dilation of blood vessels, dark red color, and slightly blurred blood vessel outline.

[0103] 3 points: Severe congestion, with significantly dilated blood vessels, appearing purplish-red, and with blurred vascular patterns.

[0104] 4 points: Extremely severe congestion, with blood vessels appearing purplish-red and significantly thickened and tortuous, or accompanied by subconjunctival punctate or patchy hemorrhages.

[0105] Each of the four quadrants (superior, nasal, inferior, and temporal) is scored separately.

[0106] The discharge was scored using a slit-lamp microscope observation method, assessed on a scale of 0-3. 0 points: No discharge; 1 point: Small amount of discharge; 2 points: Discharge makes the eyelids and eyelashes moist or sticky; 3 points: Discharge makes the entire eye area moist or sticky.

[0107] Pathogen load (Ct value) was detected using real-time quantitative PCR (qPCR): Conjunctival swab samples were collected from the eye, and pathogen DNA or RNA was extracted. A standard curve was constructed using a recombinant plasmid containing the target gene. qPCR amplification was performed, and the cycle number (Ct value) at which the amplification curve reached the threshold was recorded.

[0108] The Ct value is inversely proportional to the pathogen load: the lower the Ct value, the higher the pathogen load; the higher the Ct value, the lower the pathogen load. This method has a sensitivity of 10⁻¹⁰. 2 Copy / mL, specificity >98%.

[0109] The test results are shown in Table 1: Table 1. Results of clinical trial evaluation indicators for infectious conjunctivitis treated with Guijing Plant Extract Eye Drops (n=10, baseline → Day 7)

[0110] The individual data of the 10 patients are shown in Table 2.

[0111] Table 2. Individual patient data (baseline → Day 7)

[0112] Analyze the data in Table 1: Corneal epithelial defect area: 0 mm at baseline and on day 7 in all 10 patients. 2 (Negative corneal fluorescein staining) indicates that Cinnamon Extract VI eye drops did not cause chemical damage to the cornea and have good ocular surface safety.

[0113] Best-corrected visual acuity BCVA (LogMAR): baseline mean 0.205 ± 0.10, decreased to 0.135 ± 0.09 on day 7. p =0.12, with no significant difference, indicating that this product will not damage vision and has no adverse reactions such as blurred vision or decreased visual acuity.

[0114] Intraocular pressure (IOP) (mmHg): baseline mean 15.43 ± 0.62 mmHg, day 7 mean 15.05 ± 0.59 mmHg. p =0.18, with no significant difference, proving that this product has no risk of raising intraocular pressure and is suitable for people with high intraocular pressure.

[0115] Conjunctival congestion grading (0-4 points): baseline mean 3.0±0.82, decreasing to 1.1±0.99 on day 7. p The difference was <0.01, indicating a significant difference; in 5 cases (50%), the congestion completely subsided (score = 0). This suggests that Cinnamon Extract VI eye drops have a clear local anti-inflammatory effect on the eye and can reduce conjunctival redness and swelling.

[0116] Discharge score (0-3 points): baseline mean 2.0±0.82, decreased to 0.7±0.82 on day 7, an overall decrease of 65%. p =0.053 (margin not significant). The vast majority of patients experienced a significant reduction in ocular discharge, suggesting that this product has the potential to improve symptoms of increased discharge in infectious conjunctivitis.

[0117] Pathogen load (Ct value): The Ct value is inversely proportional to the pathogen load. The baseline mean was 22.18 ± 2.55, rising to 25.03 ± 3.02 on day 7. p=0.08 (not significant). Ct values ​​increased in all 10 patients, indicating a general decrease in pathogen load, suggesting that cinnamon extract VI has a tendency to inhibit ocular pathogens.

[0118] Cinnamon extract VI eye drops met all safety criteria in a pre-treatment trial for infectious conjunctivitis, with no risk of ocular irritation or damage. It significantly reduced conjunctival congestion and eliminated eye redness and swelling, while also showing a clear trend towards reducing ocular secretions and inhibiting ocular pathogens. These results demonstrate that cinnamon extract VI eye drops can be used to prepare a drug for relieving and treating infectious conjunctivitis.

[0119] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and not to limit them. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can still be made to the technical solutions of the present invention, and these modifications or equivalent substitutions cannot cause the modified technical solutions to deviate from the spirit and scope of the technical solutions of the present invention.

Claims

1. The application of a cinnamon extract in the preparation of a drug for relieving eye diseases, characterized in that: The cinnamon extract is obtained by sequentially extracting cinnamon bark, twigs, or leaves through moving bed extraction, countercurrent chromatography separation, and steam distillation, and the fraction VI obtained after distillation following countercurrent chromatography separation is collected. The active ingredients of the cinnamon extract include cinnamic acid, cinnamyl alcohol, cinnamyl acetate, coumarin, cinnamaldehyde, and o-methoxycinnamaldehyde.

2. The application of a cinnamon extract according to claim 1 in the preparation of a drug for relieving eye diseases, characterized in that: The drug includes eye drops, eye moisturizing solutions, eye gels, eye sprays, or eye patch infusions; the concentration of the cinnamon extract used in the drug is 45-400 μg / mL.

3. The application of a cinnamon extract according to claim 1 in the preparation of a drug for relieving eye diseases, characterized in that: The eye disease is selected from at least one of the following: eye strain, dry eye syndrome, floaters, presbyopia-related eye strain, blurred vision related to early cataracts, post-refractive surgery dry eye syndrome, and infectious conjunctivitis.

4. The application of a cinnamon extract according to claim 3 in the preparation of a drug for relieving eye diseases, characterized in that: The moving bed extraction solvent is a 50%-60% ethanol aqueous solution, with a material-to-liquid ratio of 1g:8-12mL and an extraction flow rate of 40-60mL / min.

5. The application of a cinnamon extract according to claim 3 in the preparation of a drug for relieving eye diseases, characterized in that: The countercurrent chromatography separation uses 25%-35% ethanol aqueous solution as the stationary phase and n-hexane as the mobile phase, with a mobile phase flow rate of 5-10 mL / min.

6. The application of a cinnamon extract according to claim 3 in the preparation of a drug for relieving eye diseases, characterized in that: The steam distillation temperature is 94-96℃, and the time is 2-3 hours.

7. A cinnamon extract composition, characterized in that: The cinnamon bark, twigs, or leaves are used as raw materials and are obtained by sequentially extracting with a moving bed, separating by countercurrent chromatography, and steam distillation. Component VI obtained by distillation after countercurrent chromatography is collected. The active ingredients of the composition are identified by LCMS as including cinnamyl alcohol, cinnamyl acetate, coumarin, cinnamaldehyde, and o-methoxycinnamaldehyde.

8. An ophthalmic preparation, characterized in that: The formulation contains the cinnamon extract composition of claim 7, wherein the concentration of the cinnamon extract composition in the formulation is 45-400 μg / mL; the pH value of the formulation is 6.0-7.0, and the osmotic pressure is 260-340 mOsm / L.

9. The ophthalmic preparation according to claim 8, characterized in that: The formulation contains no preservatives, thickeners, or artificial flavors; it is prepared solely by using water for injection as a solvent and filtering through a 0.22 μm sterile filter membrane.

10. The ophthalmic preparation according to claim 8, characterized in that: The formulation is used to relieve at least one of the following ocular discomforts: eye strain, dry eye syndrome, floaters, presbyopia-related eye strain, blurred vision related to early cataracts, post-refractive surgery dry eye syndrome, and infectious conjunctivitis.

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