WO2021195904A1 - Utilisation d'une composition contenant astragali radix, puerariae lobatae radix et erigerontis herba - Google Patents

Utilisation d'une composition contenant astragali radix, puerariae lobatae radix et erigerontis herba Download PDF

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WO2021195904A1
WO2021195904A1 PCT/CN2020/082231 CN2020082231W WO2021195904A1 WO 2021195904 A1 WO2021195904 A1 WO 2021195904A1 CN 2020082231 W CN2020082231 W CN 2020082231W WO 2021195904 A1 WO2021195904 A1 WO 2021195904A1
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glaucoma
composition
astragalus
parts
extract
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PCT/CN2020/082231
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English (en)
Chinese (zh)
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孙克宏
秦少容
白礼西
段俊国
杨巧巧
郑飞鸣
卿玉玲
黄静
彭涛
金思岑
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重庆太极实业（集团）股份有限公司
重庆太极医药研究院有限公司
成都中医药大学
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Priority to PCT/CN2020/082231 priority Critical patent/WO2021195904A1/fr
Publication of WO2021195904A1 publication Critical patent/WO2021195904A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/481—Astragalus (milkvetch)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/488—Pueraria (kudzu)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics

Definitions

  • This application relates to a composition containing astragalus, kudzu root and breviscapine and the use thereof. Specifically, the application relates to the use of a composition containing astragalus, kudzu root and breviscapine in the treatment of ophthalmic diseases.
  • Glaucoma is a group of diseases characterized by atrophy and depression of the optic papilla, visual field defects, and decreased vision. Pathological increase in intraocular pressure and insufficient blood supply to the optic nerve are the primary risk factors for its onset. The tolerance of the optic nerve to pressure damage is also similar to that of glaucoma. The occurrence is related to development. Obstruction of any link in the aqueous humor circulation can lead to increased intraocular pressure and cause pathological changes. However, some patients have normal intraocular pressure glaucoma. Glaucoma is one of the three major blindness diseases that cause blindness in humans, with an incidence of 1% in the total population and 2% after the age of 45. Clinically, glaucoma is divided into primary, secondary, congenital, and mixed types based on the cause, angle of the chamber, and intraocular pressure.
  • Intraocular pressure Pathological increase in intraocular pressure is the main risk factor for glaucoma. Increased intraocular pressure leads to optic nerve damage through two mechanisms: mechanical compression and optic nerve ischemia. The longer the increase in intraocular pressure lasts, the more severe the damage to visual function. The reason for the increased intraocular pressure in glaucoma is that the dynamic balance of aqueous humor circulation is disrupted. A few are due to excessive secretion of aqueous humor, but most of them still have obstacles to the outflow of aqueous humor, such as narrow or even closed anterior chamber angle, hardening of the trabeculae, etc.
  • Angle-closure glaucoma is divided into acute angle-closure glaucoma and chronic angle-closure glaucoma according to the rapid onset of disease. glaucoma.
  • Glaucoma is one of the main causes of blindness in my country, and the damage to visual function caused by glaucoma is irreversible and the consequences are extremely serious. Generally speaking, glaucoma cannot be prevented, but if it is detected early and treated appropriately, most patients can maintain useful visual function throughout their lives. Therefore, the prevention of blindness in glaucoma must emphasize early detection, early diagnosis and early treatment.
  • the main purpose of treatment is to reduce intraocular pressure, reduce eye tissue damage, and protect visual function.
  • the present application provides the use of a composition comprising astragalus, pueraria lobata and breviscapine in the preparation of a medicament for treating glaucoma in an individual.
  • the present application provides a method for treating glaucoma, which comprises administering to an individual a therapeutically effective amount of a composition comprising astragalus, kudzu root and breviscapine.
  • the present application provides a composition comprising astragalus, kudzu root and breviscapine, which is used for the treatment of glaucoma.
  • the present application provides a composition comprising astragalus, kudzu root and breviscapine.
  • the aforementioned glaucoma is ocular hypertension glaucoma.
  • the glaucoma is selected from primary glaucoma, secondary glaucoma, congenital glaucoma, or mixed glaucoma.
  • the glaucoma is open-angle glaucoma or closed-angle glaucoma.
  • compositions and a pharmaceutically acceptable carrier are formulated into a pharmaceutically acceptable dosage form, preferably a suspension, powder, tablet, granule, pill, syrup or eye drops, more Preferably it is a suspension.
  • the above-mentioned composition is administered by gavage, oral administration, eye drops, enema, subcutaneous, intramuscular, or intraperitoneal administration; preferably, the composition is administered by gavage.
  • the dosage of the composition is 100 to 1000 mg/kg body weight, preferably 300 to 600 mg/kg body weight per day.
  • the composition is for administration 1 to 3 times a day, for example, once a day by gavage.
  • the above composition includes the following raw materials in the following weight ratio: 10-40 parts of Astragalus, 10-30 parts of Pueraria lobata, and 10-30 parts of Erigeron breviscapus.
  • the above-mentioned composition contains the following active ingredients in the following weight ratio: 1-10 parts of Astragalus extract, 50-125 parts of Pueraria lobata extract, and 20-60 parts of Dengzhan extract.
  • the medicament of the present application is prepared from raw materials of Astragalus, Pueraria lobata and Erigeron breviscapus or water or organic solvent extracts of Astragalus, Pueraria lobata and Erigeron breviscapus as active ingredients, plus a pharmaceutically acceptable carrier.
  • the raw materials of Astragalus, Pueraria lobata and Erigeron breviscapus in a certain weight ratio are weighed to prepare extracts of Astragalus, Pueraria lobata and Erigeron breviscapus, respectively, and other active ingredients or pharmaceuticals are added according to the preparation method of conventional Chinese medicine formulations.
  • the above-acceptable carriers are made into different dosage forms, such as suspensions, powders, tablets, granules, pills, eye drops and other dosage forms.
  • the application also provides the use of a composition comprising astragalus, pueraria lobata and breviscapine in the preparation of a medicament for the treatment of ocular hypertension in an individual, as well as a method for the treatment of ocular hypertension in an individual, which comprises administering to the individual A therapeutically effective amount of a composition comprising astragalus, kudzu root and breviscapine.
  • Figure 1 shows the individual data of each group of animal eye examinations.
  • Figure 2 shows the individual data of OCT and HRT examination of the anterior segment of each group of animals.
  • Figures 3A-D show individual data of intraocular pressure measurement (mmHg) of animals in each group.
  • Figures 4A-D show individual data on the percentage reduction in intraocular pressure ( ⁇ IOP%) of each group of animals.
  • Figure 5 shows statistical data of the percentage decrease in intraocular pressure ( ⁇ IOP%) in male animals.
  • Figure 6 shows statistical data of the percentage decrease in intraocular pressure ( ⁇ IOP%) of female animals.
  • composition comprising astragalus, kudzu root and breviscapine can treat glaucoma, such as high intraocular pressure glaucoma.
  • the application provides the use of a composition comprising astragalus, kudzu root and breviscapine in the preparation of a medicament for the treatment of glaucoma.
  • the glaucoma is ocular hypertension glaucoma. In certain embodiments, the glaucoma is selected from primary glaucoma, secondary glaucoma, congenital glaucoma, or mixed glaucoma.
  • the glaucoma is open-angle glaucoma or closed-angle glaucoma.
  • Treatment includes inhibiting, curing, alleviating, alleviating or delaying glaucoma and related symptoms.
  • the composition of the present application is formulated into a pharmaceutically acceptable dosage form together with a pharmaceutically acceptable carrier, preferably a suspension, eye drops, oral liquid, capsule, tablet or granule, More preferably, it is a suspension suitable for gastric gavage.
  • a pharmaceutically acceptable carrier preferably a suspension, eye drops, oral liquid, capsule, tablet or granule, More preferably, it is a suspension suitable for gastric gavage.
  • the "pharmaceutically acceptable carrier” mentioned in this application refers to a carrier that does not interfere with the effectiveness of the biological activity of the active ingredient, including those conventionally used in the pharmaceutical field.
  • the pharmaceutically acceptable carrier of the present application can be solid or liquid, and includes pharmaceutically acceptable excipients, buffers, emulsifiers, stabilizers, preservatives, diluents, encapsulants, fillers, and the like.
  • pharmaceutically acceptable buffers include phosphate, acetate, citrate, borate, and carbonate.
  • composition of the present application can be presented in a unit dosage form, and can be prepared by any method known in the pharmaceutical art. All methods include the step of combining the active ingredient of the present application with one or more pharmaceutically acceptable carriers. Generally, the composition is prepared by combining the active ingredient with a liquid carrier, a solid carrier, or both, and then the prepared product is shaped as needed. The specific formulation method depends on the chosen route of administration. In some embodiments, the composition can be manufactured by conventional mixing, dissolving, granulating, tableting, grinding, emulsifying, encapsulating, capturing, or freeze-drying methods.
  • the composition is administered by gavage, oral, eye drops, enema, subcutaneous, parenteral, intravenous, intraarterial, intracranial, intrathecal, intraperitoneal, topical, intranasal, or intramuscular administration .
  • the combination is administered by gavage or orally.
  • the administration dose of the composition of the present application is 50 to 1000 mg/kg body weight per day, preferably 100-800 mg/kg body weight, more preferably 300-600 mg/kg body weight, such as 300, 350, 400, 450, 500, 550, 600 mg/kg body weight or a dose between any two of the above values.
  • the composition is administered 1, 2, 3, 4 or more times a day.
  • the composition may also be administered less than once a day, for example, every 2, 3, 4, 5 , 6, 7, 8, 9, 10, 11, 12, 13, or 14 days.
  • the number of daily administrations is constant (e.g., once or twice daily). In other embodiments, the number of administrations is variable. The number of administrations may vary according to the effectiveness of the composition, observed side effects, specific routes of administration, specific characteristics of the individual, individual health history and risk factors (such as age, weight, general health, etc.), or dosage form.
  • the duration of administration of the composition is 1-12 weeks, such as 1, 2, 3, 4, 6, 8, 10, 12 weeks, or the number of weeks between any two of the above values, Or about the time period.
  • the composition is continuously administered for 2 weeks, 3 weeks, 4 weeks, 5 weeks, 6 weeks, 8 weeks, or more weeks. In some embodiments, administration of the composition is continued until the individual no longer requires treatment.
  • the present application provides a method for treating glaucoma, which comprises administering to an individual a therapeutically effective amount of a composition comprising astragalus, kudzu root and breviscapine.
  • a therapeutically effective amount of a composition comprising astragalus, kudzu root and breviscapine for treating glaucoma in an individual is provided.
  • the "therapeutically effective dose” used herein can be determined according to specific conditions, and those of ordinary skill in the art can easily grasp the actual required drug dose, for example, it can be determined according to the patient's weight, age, and disease conditions.
  • the composition contains pharmaceutically acceptable carriers, they can be mixed according to conventional methods in the pharmaceutical field to prepare the desired drug.
  • the composition of the application comprising astragalus, kudzu root and breviscapine can improve the intraocular pressure of glaucoma patients.
  • the composition significantly reduces the intraocular pressure of glaucoma patients without significant side effects.
  • the composition of the present application has a dose-effect relationship in reducing intraocular pressure.
  • the composition of the present application comprising Astragalus, Pueraria lobata and Erigeron breviscapus can reduce the ocular hypertension induced by dexamethasone in SD rats.
  • the effect of reducing intraocular pressure of the above composition is independent of the sex of the affected individual, for example, it is effective for both female rats and male rats.
  • the composition of the application comprising Astragalus, Pueraria lobata and Erigeron breviscapus has no significant difference in the incidence of adverse events and adverse reactions in the glaucoma used to treat individuals compared with the negative control treatment group, indicating that this The applied drug has no obvious side effects in the treatment of glaucoma and has high safety.
  • the "individual” mentioned in this application refers to mammals, including primates and non-primates, such as humans, apes, monkeys, cows, horses, pigs, sheep, goats, dogs, cats, and such as rats And mice, rodents, etc.
  • the present application provides a composition comprising Astragalus, Pueraria lobata and Erigeron breviscapus.
  • the composition described above is used to treat or prevent glaucoma in an individual.
  • the composition of the present application is prepared from raw materials containing the following weight ratios: 10-40 parts of Astragalus, 10-30 parts of Pueraria lobata, and 10-30 parts of Erigeron breviscapus.
  • the composition of the present application is prepared from raw materials containing the following weight ratios: 20-30 parts of Astragalus, 20-40 parts of Pueraria lobata, and 20-30 parts of Erigeron breviscapus.
  • the composition of the present application is prepared from raw materials containing the following weight ratios: 20 parts of Astragalus, 30 parts of Pueraria lobata, and 20 parts of Erigeron breviscapus.
  • composition of the present application is prepared from raw materials or water or organic solvent extracts of Astragalus, Pueraria lobata, Erigeron breviscapus as active ingredients, plus pharmaceutically acceptable excipients or auxiliary ingredients.
  • the composition comprises the following components in a weight ratio: 1-10 parts of Astragalus extract, 50-125 parts of Pueraria lobata extract, and 20-60 parts of Dengzhan extract.
  • the composition comprises astragalus extract, pueraria lobata extract, breviscapine extract, wherein the pueraria lobata extract contains not less than 60% total isoflavones calculated as puerarin, and contains no less than puerarin 20%; Astragalus extract contains not less than 50% total saponins calculated as astragaloside IV, and not less than 5% astragaloside IV; Erigeron breviscapus extract contains not less than 35% total flavonoids calculated as rutin, including wild Baicalin is not less than 3%.
  • the weight ratio of the composition is: 1-10 parts of Astragalus extract, 50-125 parts of Pueraria lobata extract, and 20-60 parts of Dengzhan extract.
  • the weight ratio of the composition is: 1 part of Astragalus extract, 70 parts of Pueraria lobata extract, and 25 parts of Dengzhan extract.
  • the preparation method of the composition comprising Astragalus, Pueraria lobata and Erigeron breviscapus in this application includes the following steps:
  • Pueraria lobata pulverized into coarse powder extracted with 60-95% ethanol, filtered, combined the filtrate, recovered ethanol, concentrated, passed through a macroporous adsorption resin column, eluted with water, discarded the water eluate, and reused 10-95 % Ethanol elution, collect ethanol eluate, recover ethanol, concentrate into thick paste, dry under reduced pressure, pulverize into fine powder to obtain Pueraria lobata extract;
  • Astragalus is crushed into coarse powder, extracted with 60-95% ethanol under heating and refluxing, filtered, combined with the filtrate, recovered ethanol, concentrated, sodium hydroxide is added to the alkali content of 2-5%, and n-butanol is added for dynamic extraction 2 -5 times, combine the n-butanol solution, wash with 2-5% sodium hydroxide solution, then wash with water, discard the lotion, combine the n-butanol solution, concentrate under reduced pressure to near dryness, add acetone to grind and wash until the color is light, take The precipitate was dried under reduced pressure and pulverized into fine powder to obtain an Astragalus extract;
  • Decoction of Erigeron breviscapus with water combine the decoction, filter, concentrate and pass through a macroporous adsorption resin column, eluate with water, discard the water eluate, continue to elute with 10-95% ethanol, collect ethanol for elution Liquid, recovered ethanol, concentrated into a thick paste, dried under reduced pressure, pulverized into fine powder, to obtain Erigeron breviscapus extract;
  • the weight ratio of the raw materials may be 20-30 parts of Astragalus, 20-40 parts of Pueraria lobata, and 20-30 parts of Erigeron breviscapus.
  • Astragalus can be 20, 21, 22, 23, 24, 25, 26, 27, 28, 29 or 30, and Pueraria can be 20, 22, 24, 26, 28, 30, 32, 34, 36, 38.
  • Or 40 parts, Erigeron breviscapus can be 20, 21, 22, 23, 24, 25, 26, 27, 28, 29 or 30 parts.
  • the weight ratio of the raw materials may be 20 parts of Astragalus, 30 parts of Pueraria lobata, and 20 parts of Erigeron breviscapus.
  • the raw materials of the drug in this application can be prepared into a pharmaceutical commonly used preparation.
  • the obtained dry fine powder with the three herbs as the main component is added with auxiliary materials according to the preparation method of traditional Chinese medicine dosage forms to make different dosage forms, such as suspensions, tablets, granules, pills, capsules and eye drops. Agents and other dosage forms.
  • 30 kg of Astragalus, 40 kg of Pueraria lobata, and 30 kg of Erigeron breviscapus are weighed, and powdered directly to obtain a powder. Before use, add a suitable solvent and mix to obtain a suspension for later use.
  • 1 kg of the aforementioned astragalus extract, 50 kg of Pueraria lobata extract, and 30 kg of Erigeron breviscapus extract are taken, mixed, starch is added, granulated, granulated, magnesium stearate is added, and tablets are compressed to obtain tablets.
  • 10 kg of the above-mentioned astragalus extract, 125 kg of Pueraria lobata extract, and 60 kg of Erigeron breviscapus extract are mixed, and starch is added, granulated, sized, and directly filled into capsules to obtain capsules.
  • 2 kg of the above-mentioned astragalus extract, 80 kg of Pueraria lobata extract, and 40 kg of Erigeron breviscapus extract are mixed, and starch is added, granulated, granulated, and directly encapsulated to obtain pharmaceutical granules.
  • 30 kg of Astragalus, 40 kg of Pueraria lobata, and 30 kg of Erigeron breviscapus are extracted according to the above method, and 20 kg of Rehmannia glutinosa, 20 kg of wolfberry, 15 kg of cassia, and 20 kg of Fuwei seed are decocted and concentrated. Mixing, adding starch, granulating, granulating, adding magnesium stearate, and compressing to obtain tablets.
  • the composition containing Astragalus, Pueraria lobata, Erigeron breviscapus is first made into powder, and then a suitable solvent is added and mixed to obtain a suspension for later use.
  • composition of the present application can also refer to the method in Chinese Patent CN100594913C, the entire content of which is incorporated herein by reference in its entirety.
  • Example 1 Preparation of a composition containing Astragalus, Pueraria lobata and Erigeron breviscapus
  • Pueraria lobata was crushed into coarse powder, extracted twice with 60% ethanol at reflux for 1 hour each time, filtered, combined the filtrate, recovered ethanol, concentrated appropriately, added to the treated macroporous adsorption resin column, and eluted with water. Discard the water eluent, continue to elute with 70% ethanol, collect the ethanol eluent, concentrate under reduced pressure into a thick paste, dry under reduced pressure, and pulverize into fine powder to obtain Pueraria lobata extract;
  • Astragalus was pulverized into coarse powder, extracted with 90% ethanol under heating and refluxing for three times, 1 hour each time, filtered, combined the filtrates, recovered ethanol, concentrated appropriately, added sodium hydroxide to 5% alkali content, and dynamically extracted with n-butanol Twice, combine the n-butanol solution, wash with 5% sodium hydroxide solution once, and wash twice with water, discard the lotion, combine the n-butanol solution, concentrate under reduced pressure to near dryness, add acetone to grind and wash until the color is light, take The precipitate was dried under reduced pressure and pulverized into fine powder to obtain an Astragalus extract;
  • Decoction of Erigeron breviscapus with water for three times, 1 hour each time combine the decoction, filter, and concentrate appropriately, add to the treated macroporous adsorption resin column, elute with water, discard the water eluent, and continue to use 70 % Ethanol elution, collect the ethanol eluate, recover the ethanol, concentrate into a thick paste, dry under reduced pressure, and pulverize into fine powder to obtain the Erigeron breviscapus extract;
  • Example 2 The therapeutic effect of the composition of the present application on glaucoma
  • Sprague-Dawley (SD) rats were purchased from Beijing Weitong Lihua Laboratory Animal Technology Co., Ltd., with half males and half males.
  • the animal grade is SPF grade.
  • Qualified feed (purchased from Beijing Keao Xieli Feed Co., Ltd.) is provided every day. Animals eat and drink freely.
  • Beijing Keyao Xieli Feed Co., Ltd. and Pony tested the nutrient components (main test components: crude protein, crude fat, crude fiber, moisture, calcium, total phosphorus, crude ash) and physical and chemical indicators (mainly tested) of each batch of feed.
  • Indicators arsenic, lead, mercury, cadmium, BHC, DDT, aflatoxin B1) for testing, refer to China's national standards GB14924.2-2001 and GB14924.3-2010 and GB5749-2006 to ensure that there is no influence or interference test The resulting contaminants are present.
  • the starting age (D1) of the experimental animals was 10-12 weeks of age. Before the administration (D1 day), the weight of male animals was 298-358g, and the weight of female animals was 174-239g.
  • dexamethasone purchased from Chongqing Taiji Pharmaceutical Research Institute Co., Ltd., batch number 20180812, specification 5mL:5mg
  • dexamethasone purchased from Chongqing Taiji Pharmaceutical Research Institute Co., Ltd., batch number 20180812, specification 5mL:5mg
  • Administration method animals in the negative control group were given physiological saline, and animals in the low-dose and high-dose groups of the test article were given different concentrations of the test article.
  • the dosage of each animal needs to be adjusted according to the body weight recently measured before the administration.
  • the volume of administration should be 1 or 2 digits after the decimal point.
  • the test product is in a suspended state during the administration.
  • the animals are weighed when they are received, before grouping, and once a week after grouping. They are planned to be weighed before euthanasia, and they are also measured when they are found dead or dying.
  • Inspection time 1 time before modeling and after the last IOP measurement.
  • a slit lamp to observe the animal’s eyelids, conjunctiva, sclera, cornea, anterior chamber, iris, pupil and its posterior refractive interstitium, and use ophthalmoscope to observe the fundus.
  • a slit lamp microscope system to acquire images.
  • the intraocular pressure is measured at least 3 times a week (in the morning, once every other day), until the model is divided into groups.
  • Measurement method Put the animal in a fixed box, drop 1 to 2 drops of 4% oxybucaine hydrochloride eye drops for epithelial anaesthesia, and then use a rebound tonometer to measure the binocular intraocular pressure, and get each eye each time After taking the average of the 2 valid data, get the intraocular pressure of the eye.
  • Data collection Write down the measured and observed data results required by the test plan on an appropriate table or collect data directly through a computer.
  • the Tonovet Lab rebound tonometer of Icare was used to measure the intraocular pressure (IOP) of animals.
  • IOP intraocular pressure
  • the individual data of the intraocular pressure of each group of animals are shown in Figures 3A-D, the individual data of the intraocular pressure reduction percentage ( ⁇ IOP%) are shown in Figures 4A-D, and the statistical data are shown in Tables 1A-C and Figures 5 and 6.
  • Test product low-dose group Compared with the negative control group in the same period, ⁇ IOP% at all checkpoints decreased after administration, and the difference was statistically significant at 7, 11, 14, 18, 21, and 23 days after the first administration Significance (P values are p ⁇ 0.05, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.05, p ⁇ 0.001).
  • Test product high-dose group Compared with the negative control group in the same period, ⁇ IOP% at all checkpoints decreased after administration, among which 4, 7, 9, 11, 14, 16, 18, 21, 23 after the first administration , 25, and 28 days, the difference was statistically significant (P values were p ⁇ 0.05, p ⁇ 0.01, p ⁇ 0.05, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.05, p ⁇ 0.01, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.05, p ⁇ 0.05); Compared with the low-dose group of the test product during the same period, ⁇ IOP% at all checkpoints decreased after administration, and only 9 days after the first administration, the difference was statistically significant (p ⁇ 0.05).
  • Test product low-dose group Compared with the negative control group in the same period, ⁇ IOP% at all checkpoints decreased after administration, among which 4, 7, 11, 14, 16, 18, 21, 23, 25 after the first administration , 28 days, the difference was statistically significant (P values were p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.01, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.05).
  • Test product high-dose group Compared with the negative control group in the same period, ⁇ IOP% at all checkpoints decreased after administration, among which 4, 7, 9, 11, 14, 16, 18, 21, 23 after the first administration , 25, 28, and 30 days, the difference was statistically significant (P values were p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.001, p ⁇ 0.01, p ⁇ 0.05); Compared with the low-dose group of the test product in the same period, except for 4, 7, 14, 16 days after the first dose, the remaining days after the administration checkpoint ⁇ IOP% Both decreased, only 9 days after the first administration, the difference was statistically significant (p ⁇ 0.05).
  • n the number of animal eyes included in the statistical analysis.
  • n the number of animal eyes included in the statistical analysis.
  • n the number of animal eyes included in the statistical analysis.
  • the test product (300mg/kg, 600mg/kg) was administered once a day to SD rats with high intraocular pressure by intragastric administration for 30 consecutive days, all of which showed the effect of lowering intraocular pressure.
  • the 600mg/kg dose group The effect of lowering intraocular pressure is stronger than that of the 300mg/kg dose group.
  • composition of the present application has a good effect in treating glaucoma, can significantly reduce the intraocular pressure of model animals in a short time, and this improvement effect presents a certain dose-effect relationship.

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Abstract

L'invention concerne l'utilisation d'une composition contenant Astragali radix, Puerariae lobatae radix et Erigerontis herbadans dans la préparation d'un médicament pour le traitement du glaucome et de l'hypertension oculaire chez des individus.
PCT/CN2020/082231 2020-03-31 2020-03-31 Utilisation d'une composition contenant astragali radix, puerariae lobatae radix et erigerontis herba WO2021195904A1 (fr)

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CN115105520A (zh) * 2022-07-15 2022-09-27 中国科学技术大学 黄芩苷在制备用于治疗弱视的药物中的应用

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ZHANG YAN, HU YINGFAN;YANG QIAOQIAO;WANG LEI;MENG XIANLI;ZHANG YI: "Protective Effect and Mechanism of Qidengmingmu Capsule on Diabetic Retinopathy Rats Induced by Streptozotocin", PHARMACOLOGY AND CLINICS OF CHINESE MATERIA MEDICA, vol. 31, no. 4, 30 April 2015 (2015-04-30), pages 166 - 170, XP055854834, DOI: 10.13412/j.cnki.zyyl.2015.04.052 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115105520A (zh) * 2022-07-15 2022-09-27 中国科学技术大学 黄芩苷在制备用于治疗弱视的药物中的应用
CN115105520B (zh) * 2022-07-15 2023-10-20 中国科学技术大学 黄芩苷在制备用于治疗弱视的药物中的应用

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