CN117547550A - 一种预防和治疗白内障的药物及其制备方法 - Google Patents
一种预防和治疗白内障的药物及其制备方法 Download PDFInfo
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- CN117547550A CN117547550A CN202210924263.6A CN202210924263A CN117547550A CN 117547550 A CN117547550 A CN 117547550A CN 202210924263 A CN202210924263 A CN 202210924263A CN 117547550 A CN117547550 A CN 117547550A
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- vitamin
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- arginine
- trimethylglycine
- glycine
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Abstract
一种预防和治疗白内障的药物及其制备方法,由类胡罗卜素、维生素E、维生素C、肌醇、甘氨酸、精氨酸、三甲基甘氨酸、氯化锌抗菌剂、保湿剂去离子水配制而成。用此法制备的眼药水无任何副作用,具有抗炎、抗氧化、澄清晶状体功效,实际应用证明所得眼药水,在治疗白内障、飞蚊症及视力模糊、视力疲劳、青光眼,具有良好的效果。
Description
技术领域
本发明涉及一种眼药水,具体涉及一种预防和治疗白内障的药物及其制备方法。
背景技术
凡是各种原因如老化,遗传、局部营养障碍、免疫与代谢异常,外伤、中毒、辐射等,都能引起晶状体代谢紊乱,导致晶状体蛋白质变性而发生混浊,称为白内障,此时光线被混浊晶状体阻扰无法投射在视网膜上,导致视物模糊。多见于40岁以上,且随年龄增长而发病率增多。目前我国采用的白内障调查标准主要参考的是:1982年WHO提出,视力<0.7,晶体混浊,无其他导致视力下降的眼病为白内障的诊断标准;2001年WHO白内障的简易分级标准。这是裂隙灯检查的国内主流标准。免散瞳数码眼底照相和阅片的诊断标准有所不同。其诊断标准为:眼底像不能看清视网膜小血管,眼前节照片除外角膜疾病引起的眼底像模糊,证实存在白内障者。其手术判断标准为:眼底像不能够看清视盘和视网膜大血管,眼前节照片除外角膜疾病引起的眼底像模糊,证实存在白内障者。
众多医学研究及临床试验证明,人体细胞自由基损害是万病之源。自由基是一种缺乏电子的物质(不饱和电子物质)。自由基在人体内到处争夺人体细胞电子,如果夺去细胞蛋白分子的电子,使蛋白质接上支链发生烷基化,形成畸形的分子而使人体各种疾病的发生。
现有治疗白内障等眼疾的常用方法有药物治疗和手术治疗等方式,其中手术治疗对人体具有损害或有后遗症,还存在一定的风险;而目前的药物治疗多采用延缓白内障发展的方式,但效果不明显,且制作工艺不稳定,难以消除眼球及周边的微血管和神经等富集大量的自由基。为了消除用眼过度和环境因素产生的大量自由基,据相关资料记载,食用蓝莓、黑枸杞、桑椹、维生素E、维生素C或含硒等抗击自由基的高效物质等,对近视和白内障都有一定的效果,但效果并不明显。目前治疗白内障的方式主要是手术,或者使用滴眼液进行延缓白内障的继续发展。药物治疗方面也有文献公开。
由此,本发明人认为现代人用眼过度和环境因素以及机能老化经络不通是导致引起睫状肌、晶状体、眼球及周边的微血管和神经等自由基大量富集的根本原因。进一步说,正是由于自由基的大量富集,引起眼睛睫状肌不能灵活伸缩,引起眼睛及周边肌肉痉挛,血管堵塞,晶状体得不到营养,产生的代谢废物也得不到顺利排出,因此自由基过量才引起白内障、飞蚊症、青光眼、老花眼的根本原因。治疗药物要中西结合。本发明涉及一种复方眼药组合物,特别是涉及一种治疗白内障的复方眼药组合物。因此进行了本发明创造。
本发明的目的是,为了解决现有眼药水存在有上述的缺陷,提供一种预防和治疗白内障的药物及其制备方法。类胡罗卜素都具有羰基、羟基、甲氧基或者环氧基的化合物,这种结构是可以到达白内障等过氧化物富集的地方后,其羰基、羟基、甲氧基、环氧基会和过氧化物的一个不稳定氧进行结合形成一个或多个稳定的新的化合物,这个新的化合物会变得更容易溶解,从而达到让视力恢复。由于类胡罗卜素、维生素E、维生素C、精氨酸、肌醇、甘氨酸、精氨酸、三甲基甘氨酸、氯化锌这九个药物的抗氧化药理机制不同,将其组成复方制剂是一个非常理想的抗氧化机制,保护视神经营养眼底黄斑的配方。
发明内容
一种预防和治疗白内障的药物及其制备方法,本发明目的在于提供一种由类胡罗卜素、维生素E、维生素C、肌醇、甘氨酸、精氨酸、三甲基甘氨酸、氯化锌等活性成分组成的复方眼药组合物;本发明目的还在于提供该复方眼药组合物的配制方法。
本发明目的是通过如下技术方案实现的。
本发明复方眼药组合物由如下重量份的活性成分制成:
类胡罗卜素0.1~10.0重量份、维生素E 0.2~20.0重量份、维生素C 0.2~20.0重量份、肌醇0.1~10.0重量份、甘氨酸0.3~10.0重量份、精氨酸0.03~3.0重量份、三甲基甘氨酸0.3~30.0重量份、氯化锌0.01~0.1重量份;
上述九种成分的优选比例为:类胡罗卜素1∶维生素E 2∶维生素C 2∶肌醇1∶甘氨酸3∶精氨酸0.3∶三甲基甘氨酸3∶氯化锌0.01
上述九种活性成分:类胡罗卜素的同型异构体;维生素E、维生素C的同型异构体;肌醇、甘氨酸、精氨酸、三甲基甘氨酸、的可以是任何其化学上可接受形式的盐,如:肌醇磷酸盐、甘氨酸盐酸盐、精氨酸盐酸盐、三甲基甘氨酸盐酸盐等。
本发明组合物中类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌的浓度按重量比分别是1%~300%;复方制剂中九种混合物的浓度总和按重量比是12.31%。
本发明组合物中类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌的最佳浓度按重量比分别是1%、2%、2%、1%、3%、0.3%、3%、0.01%;复方制剂中类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌浓度总和按重量比是12.31%。
将本发明复方眼药组合物与药学上可接受的载体混合,可配制成临床可接受的各种剂型如溶液、混悬液或乳剂等。复方制剂溶液和混悬液的酸碱度范围在pH5至pH8之间。
上述制备方法中所述的药学上可接受的载体可以是适用于眼科制剂所要求的试剂,包括抗菌防腐剂,共同溶剂和粘滞剂等。
所述抗菌防腐剂可以是氯化锌、氯化苯甲烃铵,西么柔斯,氯丁醇,羟苯甲酸甲酯,羟苯甲酸丙酯,苯乙基乙醇,依地酸二钠,2,4-己二烯酸,欧内么M或其他已知的试剂。所使用的浓度范围按重量比是0.001%至1.0%。
所述共同溶剂可以是聚氧乙烯山梨醇脂肪酸酯20,60和80,聚丙二醇与环氧乙烷的加聚物 F-68,F-84和P-103,环式糊精或其他可用试剂。所使用的浓度范围按重量比是从0.01%到2%。
所述粘滞剂可以是聚乙烯醇,聚乙烯砒咯烷,甲基纤维素,羟丙基甲基纤维素,羟乙基纤维素,羟甲基纤维素,羟丙基纤维素或其他可用试剂。所使用的浓度范围按重量比是从0.01%到2%。
本发明组合物以及本发明复方制剂均可通过不同药理增强药效,起到协同增效的作用,既能抑制眼中水液的产生从而大幅度地抵抗眼睛的自由基治疗白内障,又对晶状体视神经具有保护作用,用于白内障局部药物治疗。
复方药物给药的剂量总和是每只眼睛0.001毫克至10毫克。经过实验研究,本发明组合物的所有剂量配比均具有治疗白内障、保护晶状体视神经及营养眼底黄斑的作用。
下述实验例和实施例用于进一步说明但不限于本发明。
实验例谷胱甘肽滴眼液,吡诺克辛纳滴眼液单独使用和复方新药物(复方胡罗卜素滴眼液) 使用对白内障作用一个月临床观察比较
一、患者资料
30例患者(共60只眼)均系门诊病人。其中男20例,女10例;平均年龄60岁(42-88岁),平均病程12年(2-23年)。
二、诊断标准
1、临床上以每眼裂隙镜显示毛细血管是否清晰为依据,为标准来选择病人。
2、排除已行晶体替换手术治疗的病人。
三、治疗方法
10位病人(20只眼)使用谷胱甘肽滴眼液,每日2次每次1滴;10位病人(20只眼)使用吡诺克辛纳滴眼液,每日2次每次1滴;10位病人(20只眼)复方新药物(复方胡罗卜素滴眼液);共30例患者(60只眼),28日为1个疗程。在用药前及用药后一天,一周,两周,三周,四周的随诊中,记录患者的视力,结膜,角膜,虹膜,睫毛颜色,瞳孔,晶体,眼底及压平眼压。用药前检查房角视野。
四、治疗结果
(1)药效:
平均视力
平均提高幅度(%)
(2)副作用:
用药后,仅个别病人出现异物感,眼部刺激作用,不影响继续用药。眼部检查,视力,眼前节,眼底,视野未见明显改变,虹膜颜色均未出现明显异常。全身亦未见明显副作用。三组 (谷胱甘肽滴眼液、吡诺克辛纳滴眼液、复方胡罗卜素滴眼液)病人无明显区别。
五、结论
白内障患者短期内使用谷胱甘肽滴眼液、吡诺克辛纳滴眼液视力无明显提高。复方胡罗卜素滴眼液使用可显著提高患者视力,并在统计学上明显优于谷胱甘肽滴眼液或吡诺克辛纳滴眼液单独使用。
下述实施例均能达到上述实验例的效果。
实施例1(溶液制剂)
A.把聚乙烯醇放至0.3毫升纯净水中搅匀,高压灭菌消毒,灭菌过的溶液冷却至室温;
B.将氯化苯甲烃铵,依地酸二钠,氯化钠,硫化钠,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌在室温下溶于0.7毫升纯净水中,过滤消毒;
C.将A和B步骤制作的溶液混合直至均匀成一相,加入硫酸或盐酸或氢氧化钠以调节酸碱度至6.8,然后将溶液装入眼药水瓶中。
眼局部给药,每天两次,每次一至二滴。
上述制剂中10.0mg的类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌,药物起到高于谷胱甘肽滴眼液的效果。
实施例2溶液制剂)
(类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌),
A.把聚乙烯醇放至1.5升纯净水中搅匀,高压灭菌消毒,灭菌过的溶液冷却至室温;
B.将氯化苯甲烃铵,依地酸二钠,氯化钠,硫化钠,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌在室温下溶于3.5升纯净水中,过滤消毒;
C.将A和B步骤制作的溶液混合直至均匀成一相,加入硫酸或盐酸或氢氧化钠以调节酸碱度至6.8,然后将溶液装入眼药水瓶中。
眼局部给药,每天两次,每次一至二滴。
实施例3(混悬液制剂)
(类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌),
A.粉浆的制备
向20克50至70度的纯净热水中,加入它罗索普,搅拌均匀;另加入50至70度的纯净热水到30克,得它罗索普溶液,过滤;在快速冷却循环中高压灭菌,完成循环后,在50至55RPM下经球型制粉18至19小时,得粉浆。
B.2%卡博模(Carbomer)浆的制备
向400克50至70度的纯净热水中,加入卡博模974P,搅动均匀;加入纯净水至500克,搅拌均匀,过滤,得卡博模974P浆100克。
C.制剂浓缩物的制备
向100克50至70度的纯净热水中,依次加入下列成分甘露醇,聚乙烯醇,氯化钠,依他酸二钠和氯化苯甲烃铵,过滤;加入卡博模974P浆(见B步骤);再加入纯净水至得275克制剂浓缩物。
将(类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌)微粉化溶入100克纯净水,制成溶液。
D.无菌混合
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化溶液(见C步骤)无菌过滤后,加入制剂浓缩物(见C步骤);用氢氧化钠或者盐酸调酸碱度至6.8+/-0.2;加入粉浆(见A步骤),尽可能的转移完所有的粉浆;加入纯净水至500克并充分搅拌均匀,即得混悬液制剂。
眼局部给药,每天两次,每次一至二滴。
实施例4(乳剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌,
按照下列方法来制备水性乳剂:
A.将硼酸,硼酸钠,依地酸二钠,氯化苯甲烃铵,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化以及氯化钠依次加入400克纯净水中,溶解及搅拌均匀至清澈;溶液过滤,无菌消毒。
B.将1600克纯净水加热至90度,加入聚乙烯醇,搅拌至均匀;搅拌的同时,加热至121度无菌消毒30至45分钟;冷却到50至55度,加入A步骤制备的溶液;继续搅拌至室温,得水性乳剂;将水性乳剂装入眼药水瓶。
眼局部给药,每天两次,每次一至二滴。
实施例5(混悬液制剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌,
A.粉浆的制备
向200克50至70度的纯净热水,加入它罗索普,搅拌均匀;另加入50至70度的纯净热水到300克,得它罗索普溶液,过滤;在快速冷却循环中高压灭菌,完成循环后,在50至55RPM 下经球型制粉18至19小时,得粉浆。
B.2%卡博模(Carbomer)浆的制备
向4000克50至70度的纯净热水中,加入卡博模974P,搅动均匀;加入纯净水至5000克,搅拌均匀,过滤,得卡博模974P浆1250克。
C.制剂浓缩物的制备
向1000克50至70度的纯净热水中,依次加入下列成分甘露醇,聚乙烯醇,氯化钠,依他酸二钠和氯化苯甲烃铵,过滤;加入卡博模974P浆(见B步骤);再加入纯净水至得1750克制剂浓缩物。
将类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化溶入1000克纯净水,制成溶液。
D.无菌混合
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化溶液(见C步骤)无菌过滤后,加入制剂浓缩物(见C步骤);用氢氧化钠或者盐酸调酸碱度至6.8+/-0.2;加入粉浆(见A步骤),尽可能的转移完所有的粉浆;加入纯净水至3000克并充分搅拌均匀,即得混悬液制剂。
眼局部给药,每天两次,每次一至二滴。
实施例6(溶液制剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌,
A.把聚乙烯醇放至1.5升纯净水中搅匀,高压灭菌消毒,灭菌过的溶液冷却至室温;
B.将氯化苯甲烃铵,依地酸二钠,氯化钠,硫化钠,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化在室温下溶于3.5升纯净水中,过滤消毒;
C.将A和B步骤制作的溶液混合直至均匀成一相,加入硫酸或盐酸或氢氧化钠以调节酸碱度至6.8,然后将溶液装入眼药水瓶中。
眼局部给药,每天两次,每次一至二滴。
实施例7(溶液制剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微
A.把聚乙烯醇放至0.6升纯净水中搅匀,高压灭菌消毒,灭菌过的溶液冷却至室温;
B.将氯化苯甲烃铵,依地酸二钠,氯化钠,硫化钠,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化在室温下溶于1.4升纯净水中,过滤消毒;
C.将A和B步骤制作的溶液混合直至均匀成一相,加入硫酸或盐酸或氢氧化钠以调节酸碱度至6.8,然后将溶液装入眼药水瓶中。
眼局部给药,每天两次,每次一至二滴。
实施例8(溶液制剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微
A.把聚乙烯醇放至0.75升纯净水中搅匀,高压灭菌消毒,灭菌过的溶液冷却至室温;
B.将氯化苯甲烃铵,依地酸二钠,氯化钠,硫化钠,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化在室温下溶于1.75升纯净水中,过滤消毒;
C.将A和B步骤制作的溶液混合直至均匀成一相,加入硫酸或盐酸或氢氧化钠以调节酸碱度至6.8,然后将溶液装入眼药水瓶中。
眼局部给药,每天两次,每次一至二滴。
实施例9(乳剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微
A.将硼酸,硼酸钠,依地酸二钠,氯化苯甲烃铵,类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化以及氯化钠依次加入40克纯净水中,溶解及搅拌均匀至清澈;溶液过滤,无菌消毒。
B.将160克纯净水加热至90度,加入聚乙烯醇,搅拌至均匀;搅拌的同时,加热至121度无菌消毒30至45分钟;冷却到50至55度,加入A步骤制备的溶液;继续搅拌至室温,得水性乳剂;将水性乳剂装入眼药水瓶。
眼局部给药,每天两次,每次一至二滴。
实施例10(溶液制剂)
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌微粉化的混合物1000克,按药剂学常规配制方法,加入适用于眼科制剂所要求的试剂,配制成溶液。
眼局部给药,每天两次,每次一至二滴。
Claims (6)
1.一种复方眼药组合物,其特征在于该组合物是由如下重量配比的活性成分制成:
类胡罗卜素0.1~10.0重量份、维生素E 0.2~20.0重量份、维生素C 0.2~20.0重量份、肌醇0.1~10.0重量份、甘氨酸0.3~10.0重量份、精氨酸0.03~3.0重量份、三甲基甘氨酸0.3~30.0重量份、氯化锌0.01~0.1重量份;
上述九种成分的优选比例为:类胡罗卜素1∶维生素E2∶维生素C2∶肌醇1∶甘氨酸3∶精氨酸0.3∶三甲基甘氨酸3∶氯化锌0.01。
类胡罗卜素∶维生素E∶维生素C∶肌醇∶甘氨酸∶精氨酸∶三甲基甘氨酸∶氯化锌的浓度按重量比分别是1%~300%;复方制剂中九种混合物的浓度总和按重量比是12.31%。
2.如权利要求1所述的复方眼药组合物,其特征在于上述九种活性成分:类胡罗卜素或者类胡罗卜素的同型异构体;维生素E、维生素C或者其同型异构体;肌醇、甘氨酸、精氨酸、三甲基甘氨酸的可以是任何其化学上可接受形式的盐,如:肌醇磷酸盐、甘氨酸盐酸盐、精氨酸盐酸盐、三甲基甘氨酸盐酸盐等。
3.如权利要求1或2所述的复方眼药组合物,其特征在于该组合物与药学上接受的载体混合,配制成混悬液制剂、乳剂或溶液制剂。
4.如权利要求3所述的复方眼药组合物,其特征在于所述的溶液剂型或混悬液制剂的酸碱度范围在pH5至pH8之间。
5.如权利要求1、2或4所述的复方眼药组合物在制备治疗白内障药物中的应用。
6.如权利要求3所述的复方眼药组合物在制备治疗白内障药物中的应用。
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