WO2018133618A1 - 绿原酸在制备防治眼部炎症的药物中的用途 - Google Patents

绿原酸在制备防治眼部炎症的药物中的用途 Download PDF

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WO2018133618A1
WO2018133618A1 PCT/CN2017/117531 CN2017117531W WO2018133618A1 WO 2018133618 A1 WO2018133618 A1 WO 2018133618A1 CN 2017117531 W CN2017117531 W CN 2017117531W WO 2018133618 A1 WO2018133618 A1 WO 2018133618A1
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chlorogenic acid
use according
drug
preparation
preventing
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张洁
宁玲
张亮
黄望
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四川九章生物科技有限公司
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Priority to US17/425,316 priority Critical patent/US20220184019A1/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids

Definitions

  • the invention relates to the use of chlorogenic acid in the preparation of a medicament for preventing and treating ocular inflammation, and belongs to the field of medicine.
  • Ocular inflammation is an inflammatory reaction of the ocular tissue under the influence of the outside and the body's own factors.
  • the clinical incidence is high, and the hazards include keratitis, scleritis, and uveitis.
  • Keratitis mainly manifests as pain, photophobia, tearing, eyelids and other irritating symptoms and ciliary congestion, corneal opacity infiltration or ulceration, etc., severe cases can cause blindness.
  • Scleritis is often caused by redness and decreased vision. It is characterized by severe eye pain. It is acute, often accompanied by cornea and uveitis, and has a poor prognosis.
  • Uveitis refers to the simultaneous or sequential inflammation of the iris, ciliary body and choroid.
  • the present invention provides the use of chlorogenic acid for the preparation of a medicament for the treatment and/or prevention of ocular inflammation.
  • the medicament is a medicament for treating and/or preventing autoimmune ocular inflammation.
  • the medicament is a medicament for treating and/or preventing uveitis, scleritis, conjunctivitis, keratitis, retinitis or vitreous inflammation.
  • the medicament is a medicament for treating and/or preventing autoimmune uveitis caused by a vitamin A-binding protein between photoreceptors.
  • the medicament is a medicament for treating and/or preventing non-microbial infectious scleritis.
  • the medicament is prepared by adding an effective amount of chlorogenic acid as an active ingredient, adding a pharmaceutically acceptable adjuvant or an auxiliary component.
  • the preparation is an oral preparation, an injection or an ophthalmic preparation.
  • the injection is an intramuscular preparation or an intravenous preparation.
  • the injection is prepared from the following raw materials in a weight ratio: 30 parts of chlorogenic acid, 2 parts of sodium hydrogen sulfite, and 80 parts of mannitol.
  • the preparation unit contains 1 to 500 mg of chlorogenic acid per preparation unit.
  • the drug contains 210 mg of chlorogenic acid per preparation unit.
  • the dosage of the chlorogenic acid for injection in the present invention is 3 mg/kg for adults, and the adult is calculated for 70 kg of body weight, so the chlorogenic acid content per unit of the preparation is 210 mg.
  • the present invention provides a pharmaceutical composition for treating and/or preventing ocular inflammation which is prepared by adding chlorogenic acid as an active ingredient, adding a pharmaceutically acceptable adjuvant or an auxiliary ingredient.
  • the present invention also provides a method of treating and/or preventing ocular inflammation, characterized in that it is administered to a subject with chlorogenic acid.
  • the subject is a patient with autoimmune ocular inflammation.
  • the subject is uveitis, scleritis, conjunctivitis, keratitis, retinitis or
  • the subject is an autoimmune Portuguese caused by a vitamin A-binding protein between photoreceptors
  • the subject is a patient with non-microbial infectious scleritis.
  • the present invention provides the use of chlorogenic acid for the preparation of a medicament for preventing and treating ocular inflammation.
  • Pharmacodynamic experiments show that chlorogenic acid can significantly alleviate the symptoms of uveitis and scleritis, and has a good therapeutic effect on ocular inflammation, providing a new choice for clinical medication.
  • Fig. 1 is a graph showing the results of ocular inflammation scores of the experimental example 1.
  • the raw materials and equipment used in the specific embodiments of the present invention are known products and are obtained by purchasing commercially available products.
  • a chlorogenic acid lyophilized powder for injection was prepared according to the method of Example 1 of Patent ZL201310366945.0.
  • Chlorogenic acid extracted from Eucommia ulmoides leaves by Sichuan Jiuzhang Biotechnology Co., Ltd., has a purity of 98.4%.
  • Photoreceptor cell vitamin A-binding protein is a macromolecular glycolipid protein that is the main soluble protein in the photoreceptor intercellular matrix (IPM). Studies have shown that IRBP can induce experimental autoimmune uveitis (EAU).
  • tuberculosis H37RA powder 1.4 ml of PBS, 2 ml of complete Freund's adjuvant (CFA), and repeated bolus injection and fully emulsified were added. , 4ml of mixed emulsion was obtained.
  • the needle was inserted subcutaneously from the middle of the rat footpad and sneaked up to the lower end of the humerus.
  • 0.2 ml of the mixed emulsion was slowly injected (the final immunization volume of each rat was 30 ug IRBP polypeptide and 250 ug of M. tuberculosis H37RA), and the needle was pressed and pressed. At the needle to prevent the emulsion from overflowing. Over the above operation, 30 rats were prepared for animal models.
  • the animals were divided into a blank control group and a chlorogenic acid administration group, and each group was administered intraperitoneally.
  • the chlorogenic acid administration group was given 20 mg/kg.
  • Drug; blank control group was intraperitoneally injected with an equal dose of normal saline.
  • Inflammation score The specific scoring criteria are as follows, 0 points: no inflammatory reaction, normal red light reflection in the fundus; 0.5 points: mild expansion of the iris blood vessels, congestion; 1 point: moderate congestion of the iris vessels, dilated pupils; 2 points: mild turbidity of the aqueous humor, Red light reflection on the fundus weakened; 3 points: turbidity in the aqueous humor, red light reflection on the fundus weakened; 4 points: anterior chamber empyema, pupillary membrane closed, red light reflection disappeared.
  • the control group showed iris vascular congestion and pupil dilation. After that, the symptoms of the eye were aggravated with the increase of the number of immunization days. On the 9th day after immunization, the symptoms were obvious. The symptoms were iris vascular congestion, empyema in the anterior chamber and posterior chamber, and the pupil area was exuded, and the red light reflection at the fundus was weakened. On the 12th day of immunization, the symptoms reached a peak, which showed turbidity and empyema in the anterior chamber, partial pupillary membrane closure, anterior chamber shallowing, iris bulging, and even anterior chamber hemorrhage.
  • the pupils were closed, most of the pupils were open, the anterior chamber was reduced, and the exudation began to be absorbed.
  • the anterior chamber was deepened and the iris vessels were congested.
  • the symptoms of the rats were further alleviated, the pupillary membrane was closed, the anterior chamber depth was basically normal, the aqueous humor was slightly turbid, the iris blood vessels were congested, and the red light reflected from the fundus was present.
  • the ocular inflammation in the chlorogenic acid treatment group was significantly reduced at the same time point compared with the control group.
  • the eye symptoms were mild, showing anterior aqueous humor, iris vascular congestion, blurred texture, and abnormal pupil dilation.
  • the vascular congestion of the iris was aggravated, and the anterior chamber was turbid in water, and the symptoms were quickly relieved.
  • the pupil was basically normal, the depth of the anterior chamber was basically normal, and the aqueous humor was clear or slightly turbid.
  • chlorogenic acid test group 20 patients with scleritis were randomly divided into two groups, namely, chlorogenic acid test group and dexamethasone sodium phosphate control group.
  • chlorogenic acid control group 1 male and 9 female, average age (30.5 ⁇ 5.1) years old, mean disease duration (5.1 ⁇ 0.3).
  • dexamethasone sodium phosphate there were 1 male and 9 female, with an average age of (31.5 ⁇ 4.7) years and an average disease duration (5.5 ⁇ 0.3).
  • P>0.05 There was no statistically significant difference in the clinical data of age, sex and duration of disease between the two groups (P>0.05), which was comparable.

Abstract

本发明提供了绿原酸在制备治疗和/或预防眼部炎症的药物中的用途，绿原酸能够明显缓解葡萄膜炎、巩膜炎症状，对眼部炎症具有良好的治疗效果。

Description

绿原酸在制备防治眼部炎症的药物中的用途 技术领域
本发明涉及绿原酸在制备防治眼部炎症的药物中的用途，属于医药领域。
背景技术
眼部炎症是眼部组织在外界和机体自身因素的作用下发生的炎性反应，临床发病率较高、危害较大的包括角膜炎、巩膜炎、葡萄膜炎等。角膜炎主要表现为疼痛、畏光、流泪、眼睑痉挛等刺激症状及睫状充血、角膜混浊浸润或溃疡等，严重者可致盲。巩膜炎多以眼红和视力下降为始发症状，以重度眼痛为主要特点，发病急，常伴发角膜及葡萄膜炎，预后不佳。葡萄膜炎是指虹膜、睫状体及脉络膜同时或先后发生炎症，若失治或误治，可引起角膜水肿、青光眼、视网膜脱离等并发症，后果非常严重。由于上述疾病对眼部健康危害极大，治疗不当可致盲，已引起世界范围内的重视。
因此，寻求合理而有效的眼部炎症的治疗药物，已成为眼科领域一个亟待解决的问题。
发明内容
本发明的目的在于提供绿原酸在制备防治眼部炎症的药物中的用途。
本发明提供了绿原酸在制备治疗和/或预防眼部炎症的药物中的用途。
进一步地，所述的药物是治疗和/或预防自身免疫性眼部炎症的药物。
进一步地，所述的药物是治疗和/或预防葡萄膜炎、巩膜炎、结膜炎、角膜炎、视网膜炎或玻璃体炎症的药物。
进一步地，所述的药物是治疗和/或预防光感受器间维生素A类结合蛋白所致自身免疫性葡萄膜炎的药物。
进一步地，所述的药物是治疗和/或预防非微生物感染性巩膜炎的药物。
进一步地，所述的药物是以有效量的绿原酸为活性成分，加入药学上可接受的辅料或者辅助性成分制备而成的制剂。
进一步地，所述的制剂为口服制剂、注射剂或眼用制剂。
进一步地，所述的注射剂为肌肉注射制剂或静脉注射制剂。
进一步地，所述的注射剂由下述重量配比的原辅料制备而成：绿原酸30份、亚硫酸氢钠2份、甘露醇80份。
进一步地，所述药物中每制剂单位含有绿原酸1～500mg。
进一步地，所述药物中每制剂单位含有绿原酸210mg。
本发明注射用绿原酸给予成人的剂量为3mg/kg，成人按体重70kg计算，因此每制剂单位绿原酸含量为210mg。
本发明提供了一种治疗和/或预防眼部炎症的药物组合物，它是以绿原酸为活性成分，加入药学上可接受的辅料或者辅助性成分制备而成的制剂。
本发明还提供了一种治疗和/或预防眼部炎症的方法，其特征在于：它是给予受试者绿原酸。
其中，所述受试者是自身免疫性眼部炎症的患者。
其中，所述受试者是葡萄膜炎、巩膜炎、结膜炎、角膜炎、视网膜炎或
玻璃体炎症的患者。
其中，所述受试者是光感受器间维生素A类结合蛋白所致自身免疫性葡
萄膜炎的患者。
其中，所述受试者是非微生物感染性巩膜炎的患者。
本发明提供了绿原酸在制备防治眼部炎症的药物中的用途。药效实验表明，绿原酸能够明显缓解葡萄膜炎、巩膜炎的症状，对眼部炎症具有良好的治疗效果，为临床用药提供了一种新的选择。
显然，根据本发明的上述内容，按照本领域的普通技术知识和惯用手段，在不脱离本发明上述基本技术思想前提下，还可以做出其它多种形式的修改、替换或变更。
以下通过实施例形式的具体实施方式，对本发明的上述内容再作进一步的详细说明。但不应将此理解为本发明上述主题的范围仅限于以下的实例。凡基于本发明上述内容所实现的技术均属于本发明的范围。
附图说明
图1为实验例1大鼠眼部炎症评分结果图。
具体实施方式
本发明具体实施方式中使用的原料、设备均为已知产品，通过购买市售产品获得。
实施例1注射用绿原酸冻干粉针的制备
本实施例根据专利ZL201310366945.0中实施例1的方法制备注射用绿原酸冻干粉针。
1.主药
绿原酸，由四川九章生物科技有限公司提取自杜仲叶，纯度为98.4％。
2.处方：
Figure PCTCN2017117531-appb-000001
按照上述处方经冻干制成1000支，规格为30mg/支的注射用绿原酸冻干粉针剂。
以下实验例中，所述绿原酸冻干粉针剂均根据实施例1制备。
以下通过实验例证明本发明的有益效果。
实验例1绿原酸对葡萄膜炎的治疗效果
感光细胞间维生素A类结合蛋白(IRBP)是一个大分子糖脂蛋白，是感光细胞间基质(IPM)中主要的可溶性蛋白。研究表明，IRBP可诱发实验性自身免疫性葡萄膜炎(EAU)。
1、造模
6-8周龄SD大鼠30只，体质量160-180g，将动物按序编号。以下操作均在超净台内进行：取光感受器间维生素A类结合蛋白(Interphotoreceptor Binding protein，IRBR)粉剂(1mg/支)1支，加入1ml PBS,混匀并待其充分溶解，配成含IRBP浓度为1000ug/ml的PBS溶液，放置备用。无菌条件下称取结核分枝杆菌H37RA(250ug*20＝5mg)10mg备用。2支5ml螺口注射器连接三通阀，依次分别加入含IRBP的PBS溶液0.6ml、结核分枝杆菌H37RA粉剂10mg、PBS 1.4ml、完全弗氏佐剂(CFA)2ml，反复推注并充分乳化，得混合乳剂4ml。自大鼠足垫中部皮下进针，向上潜行至胫骨上端皮下处，缓慢推注混合乳剂0.2ml(每只大鼠最终免疫量为30ugIRBP多肽与250ug结核分枝杆菌H37RA),出针并按压进针处，以防乳剂溢出。反复以上操作，共对30只大鼠进行动物模型制作。
2、动物的给药
自身免疫6天出现症状后采用随机数字表法蒋动物分组，分为空白对照组与绿原酸给药组，每组15只，腹腔注射给药；绿原酸给药组按20mg/kg给药；空白对照组腹腔注射等剂量的生理盐水。
3、大鼠眼部裂隙灯下观察及炎症评分
每日在裂隙灯下观察各组大鼠眼部炎症表现，并参照Caspi临床分级进 行炎症评分。具体评分标准如下，0分：无炎症反应，眼底红光反射正常；0.5分：虹膜血管轻度扩张、充血；1分：虹膜血管中度充血，瞳孔缩小；2分：房水轻度混浊，眼底红光反射减弱；3分：房水中度混浊，眼底红光反射减弱；4分：前房积脓，瞳孔膜闭，眼底红光反射消失。
4、大鼠眼部症状观察及炎症评分
炎症评分结果见表1、图1：
表1大鼠眼部炎症评分结果
Figure PCTCN2017117531-appb-000002
实验结果：对照组表现为虹膜血管充血，瞳孔缩小，此后眼部症状表现随免疫天数的增加而加重。免疫后第9天，症状明显，表现为虹膜血管充血，前房及后房积脓，瞳孔区成形渗出，眼底红光反射变弱。免疫第12天症状达到高峰，表现为前房水中度混浊及积脓，部分出现瞳孔膜闭，前房变浅，虹膜膨隆，甚至前房出血，眼底红光反射基本消失。之后症状逐渐减轻，免疫15天后除个别大鼠仍有瞳孔膜闭外，绝大部分瞳孔开放，前房积后房积脓减少，渗出开始吸收，前房加深，虹膜血管充血。免疫第20天，大鼠症状进一步减轻，瞳孔膜闭消失，前房深度基本正常，房水轻度混浊，虹膜血管充血，眼底红光反射存在。
绿原酸治疗组大鼠眼部炎症表现在相同时间点较对照组明显减轻，免疫后第9天眼部症状轻微，表现为前房房水混浊，虹膜血管充血，纹理模糊，瞳孔异常缩小。第12天虹膜血管充血加重，前房房水中度混浊，之后症状迅速减轻。免疫后第15天，瞳孔基本正常，前房深度基本正常，房水清或轻微混浊。
自免疫后第6天起，绿原酸治疗组大鼠眼部炎症评分中在相同时间点相较于对照组显著降低(P＜0.05)。
以上结果表明，绿原酸对葡萄膜炎具有显著的治疗作用。
实验例2绿原酸对巩膜炎的临床疗效与结果
随机将20例巩膜炎的患者分为绿原酸试验组10例，对照组10例。绿原酸试验组的患者给予绿原酸3mg/(kg.d)，肌肉注射。对照组的患者给地塞 米松磷酸钠5mg/d、静脉滴注，连续观察治疗5天后改为口服尼泼松(1mg/(kg.d))。两组均连续给药1个月。
1、一般临床资料
现有在首都医科大学附属北京世纪坛医院开展的注射用绿原酸治疗恶性脑胶质瘤的I期临床试验(临床批件号：2013L01855)，在本试验中，所有受试者根据其各自所在组的给药剂量，分别于每天上午肌肉注射绿原酸冻干粉针剂。
根据随机表将巩膜炎患者20例随机分为两组，即绿原酸试验组与地塞米松磷酸钠对照组，其中绿原酸对照组10例中，男1例，女9例，平均年龄(30.5±5.1)岁，平均病程(5.1±0.3)。地塞米松磷酸钠对照组中男1例，女9例，平均年龄(31.5±4.7)岁，平均病程(5.5±0.3)。两组病例在年龄、性别、病程等临床资料经统计学处理差异无统计学意义(P＞0.05)，具有可比性。
2、入选标准：
(1)详细询问病史，进行裂隙灯检查、眼底检查、超声检查、眼部影像学等详细检查，明确诊断为巩膜炎患者；(2)无糖皮质激素及绿原酸禁忌症；(3)非微生物感染性巩膜炎患者；(4)血常规，电解质、肝功能、肾功能、血压和血糖等无明显异常者。
3、排除标准：
(1)微生物感染性巩膜炎及全身有感染性疾病患者；(2)表层巩膜炎；(3)使用糖皮质激素过敏或者出现毒副作用者；(4)孕妇及哺乳期产妇与婴儿；(5)中度高血压、严重心脑血管疾病、糖尿病、肝肾功能受损者；(6)依从性差，拒绝定期复查及随访者。
4、治疗方法：
绿原酸试验组的患者给予绿原酸3mg/(kg.d)，肌肉注射。对照组的患者给地塞米松磷酸钠5mg/日、静脉滴注，连续观察治疗3天后改为口服尼泼松(1mg/(kg.d))。两组均连续给药1个月。
5、疗效评定标准：
(1)治愈：治疗后眼部症状和体征完全消失；(2)好转：治疗后眼部症状和体征改善；(3)无效：炎症未控制，或情况同治疗前。
6、视力评定标准：
(1)治疗后采用同一对数视力表(有屈光不正者测最佳矫正视力)检测 记录。明显提高：提高3行及以上；好转：提高1-2行；无效：视力未提高甚至下降。
7、结果：
表2绿原酸对巩膜炎的临床治疗效果(1个月炎症控制情况)
组别 n(例) 治愈 好转 无效 总有效率
绿原酸组 10 5(50％)* 3(30％) 2(20％) 8(80％)*
对照组 10 2(20％) 3(30％) 5(50％) 5(50％)
注，两组之间比较，*P＜0.05
表3 1个月时视力恢复情况
Figure PCTCN2017117531-appb-000003
注，两组之间比较，*P＜0.05
实验结果：绿原酸给药组在炎症控制效果与视力恢复情况方面均显著优于对照组(P＜0.05)，说明绿原酸能够有效治疗巩膜炎。

Claims (15)

  1. 绿原酸在制备治疗和/或预防眼部炎症的药物中的用途。
  2. 如权利要求1所述的用途，其特征是：所述的药物是治疗和/或预防自身免疫性眼部炎症的药物。
  3. 如权利要求1或2所述的用途，其特征是：所述的药物是治疗和/或预防葡萄膜炎、巩膜炎、结膜炎、角膜炎、视网膜炎或玻璃体炎症的药物。
  4. 如权利要求3所述的用途，其特征是：所述的药物是治疗和/或预防光感受器间维生素A类结合蛋白所致自身免疫性葡萄膜炎的药物。
  5. 如权利要求3所述的用途，其特征是：所述的药物是治疗和/或预防非微生物感染性巩膜炎的药物。
  6. 如权利要求1～5任意一项所述用途，其特征是：所述的药物是以有效量的绿原酸为活性成分，加入药学上可接受的辅料或者辅助性成分制备而成的制剂。
  7. 如权利要求6所述的用途，其特征是：所述的制剂为口服制剂、注射剂或眼用制剂。
  8. 如权利要求7所述的用途，其特征是：所述的注射剂为肌肉注射制剂或静脉注射制剂。
  9. 如权利要求7所述的用途，其特征是：所述的注射剂由下述重量配比的原辅料制备而成：绿原酸30份、亚硫酸氢钠2份、甘露醇80份。
  10. 如权利要求1所述的用途，其特征是：所述药物中每制剂单位含有绿原酸1～500mg。
  11. 一种治疗和/或预防眼部炎症的方法，其特征在于：它是给予受试者绿原酸。
  12. 如权利要求11所述的方法，其特征是：所述受试者是自身免疫性眼部炎症的患者。
  13. 如权利要求11或12所述的用途，其特征是：所述受试者是葡萄膜炎、巩膜炎、结膜炎、角膜炎、视网膜炎或玻璃体炎症的患者。
  14. 如权利要求13所述的用途，其特征是：所述受试者是光感受器间维生素A类结合蛋白所致自身免疫性葡萄膜炎的患者。
  15. 如权利要求13所述的用途，其特征是：所述受试者是非微生物感染性巩膜炎的患者。
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