CN105663902A - 一种治疗视网膜激光光凝术引起视网膜水肿的组合物 - Google Patents
一种治疗视网膜激光光凝术引起视网膜水肿的组合物 Download PDFInfo
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Abstract
本发明公开了一种治疗视网膜激光光凝术引起视网膜水肿的组合物,其特征在于:由以下原料药制成:左卡尼汀0.2-0.8g、当归20-30g、川芎20-30g、炒薏苡仁10-20g、白芍5-10g。利用左卡尼汀增强机体抗氧化应激水平,利用中药成分活血化瘀,健脾渗湿,改善人体内环境,从而改善视网膜微循环及缺氧状态,促进视网膜及黄斑部位的水肿吸收,最终共同起到治疗视网膜激光光凝术引起视网膜水肿的功效。
Description
技术领域
本发明涉及一种治疗视网膜水肿的组合物,尤其是涉及一种治疗视网膜激光光凝术引起视网膜水肿的组合物。
背景技术
随着人类生活水平的普遍提高及人均寿命的延长,目前国内外糖尿病的发病率较以往显著升高。糖尿病在我国已成为仅次于心脑血管疾病和肿瘤的第三大重要慢性疾病,严重威胁着人们的健康。糖尿病有许多并发症,其中糖尿病视网膜病变(diabeticretinopathy,DR)是糖尿病严重的并发症之一,是糖尿病患者最为常见的眼部微血管并发症,影响了患者的视力和生活质量,是目前世界上四大主要致盲病因之一。
对于DR的治疗,现阶段首先是针对原发病控制血糖,通过控制饮食和药物治疗,使血糖稳定的控制在正常范围之内。在此基础上,对于DR最常用和有效的治疗方法是激光光凝术。尤其是出现眼底视网膜无灌注和渗漏,主要采用激光光凝术具有显著的疗效。及时应用激光治疗,封闭渗漏点及微动脉瘤减少渗出,进而增加对视网膜的供血、供氧,有利于恢复和稳定,可使视力丧失减少50%-70%。
然而,激光光凝术本身是一种破坏性的治疗手段,其主要作用于视网膜色素上皮层,激光可以造成光感受细胞、色素上皮细胞、及血管的损伤,引起细胞变性坏死,细胞膜通透性增强;细胞发生增殖形成瘢痕;微血管阻塞导致血管屏障功能损伤,以上均会造成视网膜水肿。因此,在研究中,为了最大程度的减少激光光凝术带来的副作用,我们采用中西药综合治疗视网膜激光光凝术引起视网膜水肿的方法,利用左卡尼汀增强机体抗氧化应激水平,利用中药成分活血化瘀,健脾渗湿,改善人体内环境,从而改善视网膜微循环及缺氧状态,促进视网膜及黄斑部位的水肿吸收,最终共同起到治疗视网膜激光光凝术引起视网膜水肿的功效。
左卡尼汀(L-carnitine,LC)又名左旋肉碱,是哺乳类动物体内能量代谢所必须的天然物质,主要于肝脏、肾脏、心脏等组织内由三甲赖氨酸转化成γ-丁酰甜菜碱,再由肝脏、肾及脑组织将其转化成卡尼汀而合成,参与体内脂类代谢,对机体细胞能量代谢产生及转运起重要作用,是心、脑、肾等组织器官代谢所需能量的主要来源之一。同时LC还具有促进蛋白质降解、抗氧化、保护细胞膜等功能。左卡尼汀目前已广泛应用于心肌病、肝脏疾病、透析病人、糖尿病、男性不育、神经肌肉疾病、肾脏疾病等疾病的治疗。正常情况下,LC可将长链脂肪酸通过位于线粒体外膜的卡尼汀脂酰转移酶-Ⅰ及内膜的卡尼汀脂酰转移酶-Ⅱ将其转运到线粒体中,然后在线粒体酶的作用可将脂酰辅酶A(CoA)在线粒体中进行β-氧化。缺血、缺氧时脂类代谢发生障碍,可导致长链脂酰卡尼汀在线粒体中堆积及脂酰-CoA的堆积,致使游离的卡尼汀被大量消耗减少,而堆积的脂酰-CoA可导致膜结构的改变、膜相崩解致细胞死亡。如体内有足量的游离卡尼汀,则可使堆积的脂酰-CoA进入线粒体中在线粒体酶的作用下进行β-氧化,从而纠正脂类代谢障碍所致的能量失衡,防止脂质过氧化。另外有研究表明,LC除了可以促进脂肪酸通过β-氧化进行氧化利用外,它还可作为一种氧自由基清除剂有效的清除体内的氧自由基,其在增强机体抗氧化应激、防止脂质过氧化等方面具有明显保护作用。
当归(RADIXANGELICAESINENSIS),为伞形科植物当归Angelicasinensis(Oliv.)Diels的干燥根。秋末采挖,除去须根及泥沙,待水分稍蒸发后,捆成小把,上棚,用烟火慢慢熏干。甘、辛,温。归肝、心、脾经。补血活血,调经止痛,润肠通便。用于血虚萎黄,眩晕心悸,月经不调,经闭痛经,虚寒腹痛,肠燥便秘,风湿痹痛,跌扑损伤,痈疽疮疡。酒当归活血通经。用于经闭痛经,风湿痹痛,跌扑损伤。
川芎(RHIZOMACHUANXIONG),为伞形科植物川芎LigusticumchuanxiongHort.的干燥根茎。夏季当茎上的节盘显著突出,并略带紫色时采挖,除去泥沙,晒后炕干,再去须根。辛,温。归肝、胆、心包经。活血行气,祛风止痛。用于月经不调,经闭痛经,癥瘕腹痛,胸胁刺痛,跌扑肿痛,头痛,风湿痹痛。
炒薏苡仁(SEMENCOICIS),为为禾本科植物薏苡Coixlacryma-jobiL.var.ma-yuen(Roman.)Stapf的干燥成熟种仁。秋季果实成熟时采割植株,晒干,打下果实,再晒干,除去外壳、黄褐色种皮及杂质,收集种仁。甘、淡,凉。归脾、胃、肺经。健脾渗湿,除痹止泻,清热排浓。用于水肿,脚气,小便不利,湿痹拘挛,脾虚泄泻,肺痈,肠痈;扁平疣。
白芍(RADIXPAEONIAEALBA),为毛茛科植物芍药PaeonialactifloraPall.的干燥根。夏、秋二季采挖,洗净,除去头尾及细根,置沸水中煮后除去外皮或去皮后再煮,晒干。苦、酸,微寒。归肝、脾经。平肝止痛,养血调经,敛阴止汗。用于头痛眩晕,胁痛,腹痛,四肢挛痛,血虚萎黄,月经不调,自汗,盗汗。
发明内容
鉴于以上,本发明提供了一种治疗视网膜激光光凝术引起视网膜水肿的组合物,它能够增强机体抗氧化应激水平,活血化瘀,健脾渗湿,改善人体内环境,从而改善视网膜微循环及缺氧状态,促进视网膜及黄斑部位的水肿吸收,最终共同起到治疗视网膜激光光凝术引起视网膜水肿的功效。
实现以上效果的本发明组合物由以下原料药制成:左卡尼汀0.2-0.8g、当归20-30g、川芎20-30g、炒薏苡仁10-20g、白芍5-10g。
本发明组合物还可以由以下原料药制成:左卡尼汀0.3-0.6g、当归22-28g、川芎22-28g、炒薏苡仁12-18g、白芍6-9g。
本发明组合物还可以由以下原料药制成:左卡尼汀0.4-0.6g、当归23-26、川芎23-26g、炒薏苡仁13-16g、白芍7-8g。
本发明组合物还可以由以下原料药制成:左卡尼汀0.5g、当归25、川芎23g、炒薏苡仁15g、白芍8g。
本发明组合物的制备方法包括以下步骤:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混合粉碎成粉末,过40目筛,得混合粉末;
(3)将步骤(2)所得的混合粉末与左卡尼汀混合,作为活性成分制备成药学上可接受的制剂。
或:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加8-10倍量水,浸泡2-4小时,煎煮1-3次,每次1-3小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏,加乙醇静置、醇沉、过滤,滤液减压回收乙醇至无醇味,减压浓缩至60℃热测时相对密度1.00-1.05的流浸膏;
(3)将步骤(2)所得的流浸膏与左卡尼汀混合,制备成药学上可接受的制剂。
或:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加6-8倍量水,煎煮1-3次,每次2-3小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏;
(3)将步骤(2)所得的清膏与左卡尼汀混合,制备成药学上可接受的制剂。
本发明组合物中,剂型为胶囊剂、片剂、颗粒剂、散剂或口服液,为使上述剂型能够实现,可以在制备这些剂型时加入药学可接受的辅料,例如:填充剂、崩解剂、润滑剂、助悬剂、粘合剂、甜味剂、矫味剂、防腐剂等,填充剂包括:淀粉、预胶化淀粉、乳糖、甘露醇、甲壳素、微晶纤维素、蔗糖等,崩解剂包括:淀粉、预胶化淀粉、微晶纤维素、羧甲基淀粉钠、交联聚乙烯吡咯烷酮、低取代羟丙纤维素、交联羧甲基纤维素钠等,润滑剂包括:硬脂酸镁、十二烷基硫酸钠、滑石粉、二氧化硅等,助悬剂包括:聚乙烯吡咯烷酮、微晶纤维素、蔗糖、琼脂、羟丙基甲基纤维素等,粘合剂包括,淀粉浆、聚乙烯吡咯烷酮、羟丙基甲基纤维素等,甜味剂包括:糖精钠、阿斯帕坦、蔗糖、甜蜜素、甘草次酸等,矫味剂包括:甜味剂及各种香精,防腐剂包括:尼泊金类、苯甲酸、苯甲酸钠、山梨酸及其盐类、苯扎溴铵、醋酸氯乙定、桉叶油等。
具体实施方式
以下通过实施例对本发明作进一步详细的说明,但本发明的保护范围不受具体实施例的任何限制,而是由权利要求加以限定。
实施例1
按重量计,取左卡尼汀0.8g、当归30g、川芎30g、炒薏苡仁20g、白芍10g。
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混合粉碎成粉末,过40目筛,得混合粉末;
(3)将步骤(2)所得的混合粉末与左卡尼汀混合,作为活性成分,与适量淀粉混匀,过筛后充分混匀,分装入胶囊中即得。
实施例2
按重量计,取左卡尼汀0.3g、当归22g、川芎22g、炒薏苡仁12g、白芍6g。
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加8倍量水,煎煮3次,每次2小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏;
(3)将步骤(2)所得的清膏与左卡尼汀混合,作为活性成分,与适量淀粉混匀,过筛后充分混匀,分装入胶囊中即得。
实施例3
按重量计,取左卡尼汀0.5g、当归23g、川芎25g、炒薏苡仁14g、白芍7g。
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加6倍量水,煎煮2次,每次2小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏;
(3)将步骤(2)所得的清膏与左卡尼汀混合,作为活性成分,与适量淀粉混匀,过筛后充分混匀,分装入胶囊中即得。
实施例4
按重量计,取左卡尼汀0.5g、当归25、川芎23g、炒薏苡仁15g、白芍8g。
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加8倍量水,煎煮3次,每次3小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏;
(3)将步骤(2)所得的清膏与左卡尼汀混合,作为活性成分,与适量淀粉混匀,过筛后充分混匀,分装入胶囊中即得。
实施例5
1.实验方法:
ErythrosinB是一种类似于rosebengal的II型光敏染料,在激光激发下可引起血管内皮屏障的点状损伤,引起血管源性水肿及血小板血栓。目前,已有大量研究利用erythrosinB以及rosebengal的光化学特性来诱导各种组织的血管栓塞以及缺血模型,包括脑、脊髓、视神经以及视网膜缺血模型。在以上模型中,都可观察到明显的组织水肿,因而本实验利用这一光化学反应的原理,通过低强度的激光照射可能可以在诱导视网膜水肿的同时避免血管栓塞,从而建立一个单纯血管源性视网膜水肿动物模型。
激光照射系统:该激光照射系统由532nmNd:YAG激光器(RD532-50G4,陕西日成科技发展有限公司)、5倍扩束镜、反射棱镜、挡光片(带直径5mm圆孔)及电源(电压、电流可调)组成。最终输出激光波长532nm,能量0-50mw可调,光斑直径为5mm。通过M93型激光功率计(北京光电技术研究所)测量激光能量。
取体重为200-230g的雄性SD大鼠30只,按体重随机分为6组,分别为:正常对照组、本发明低剂量组、本发明中剂量组、本发明高剂量组、左卡尼汀组、模型对照组。每组5只。其中,本发明组为实施例4制备的活性成分。每天灌胃给药一次,模型对照组和正常对照组灌胃给同体积的蒸馏水,连续3天。末次给药后,将大鼠麻醉并充分散瞳:光学相干断层扫描(OCT,HeidelbergEngineeringHRA2,HeidelbergEngineeringGmbH)检查使用交叉线性扫描做水平及垂直方向扫描(扫描角度为30°,扫描长度为5.1mm),使视神经切面位于扫描线中心。每只眼选取水平及垂直方向各一张清晰的OCT图像,选取距离视盘边缘500μm处,使用图像分析软件(ImageJ1.46)测量视网膜色素上皮层(retinalpigmentepithelium,RPE)与视网膜神经纤维层(retinalnervefiberlayer,RNFL)之间的厚度,将所得的四个数据的平均值作为视网膜厚度。
其中,造模按照以下步骤进行:用1%戊巴比妥钠按40mg/kg麻醉大鼠,复方托吡卡胺滴眼液(美多丽,参天制药株式会社)滴眼散瞳。将大鼠尾静脉注射2%ErythrosinB水溶液(MPBiomedicals,LLC,20mg/kg),左氧氟沙星眼膏涂眼后置载玻片于大鼠角膜上,显微镜下调整大鼠头位,使5mm激光光斑通过瞳孔区照射眼底,视乳头位于光斑中央位置,在给予静脉注射2%的ErythrosinB溶液后,迅速开启预先调好能量的激光器,进行激光照射8分钟。
正常对照组:左右眼均不造模,每天给予生理盐水。
本发明低剂量组:左眼造模后,根据体重每天给予2.0g生药/kg的实施例4制备的活性成分。
本发明中剂量组:左眼造模后,根据体重每天给予4.0g生药/kg的实施例4制备的活性成分。
本发明高剂量组:左眼造模后,根据体重每天给予8.0g生药/kg的实施例4制备的活性成分。
左卡尼汀组:左眼造模后,根据体重每天给予4.0/kg左卡尼汀。
模型对照组:左眼造模后,每天给予生理盐水。右眼为单纯激光照射对照组,不注射ErythrosinB,扩瞳后直接激光照射8分钟。
实验前视网膜厚度各组大鼠无显著性差异(P>0.05)。实验后结果如下:
表1各组平均视网膜厚度比较
结果表明,与正常对照组相比,模型对照组左眼视网膜厚度明显增加,且模型对照组右眼给药后比给药前厚度增加幅度较小,证明给予ErythrosinB的模型对照组左眼造模成功。而与模型对照组左眼相比,本发明给药组对于视网膜水肿的消除具有极显著性差异(**P<0.01);虽然左卡尼汀组由于左卡尼汀本身的氧自由基清除作用使得小鼠的视网膜水肿有一定的消除(*P<0.05),但是与本发明药物组相比,其作用效果不明显。
实验证实本发明采用的组合物在治疗由激光引起的视网膜水肿时,中药成分和西药成分共同作用,产生了协同作用,能够明显降低视网膜水肿导致的视网膜厚度。
实施例6
根据第Ⅲ届全国眼科学术会议制定的糖尿病视网膜病变分型、分期标准,选取2011-2013年确诊的Ⅲ~Ⅳ期糖尿病视网膜病变22例(22只眼),其中男12例,女10例,年龄45-67岁。将患者随机分为本发明组和对照组,每组各11例(11只眼)。两组一般资料经统计学处理无显著性差异(P>0.05)。
诊断标准参照1984年我国制定的糖尿病视网膜病变分型、分期标准。纳入标准:①诊断为糖尿病视网膜病变的患者;②符合分期标准的Ⅲ~Ⅳ期患者;③无其他眼底疾病,屈光间质清晰,能看清眼底,不影响造影和激光治疗。排除标准:①糖尿病视网膜病变患者,但不属于Ⅲ~Ⅳ期;②有其他眼病或屈光间质混浊影响造影和激光治疗;③未按规定用药,无法判定疗效或资料不全者。
两组患者均采用同样的方法进行视网膜激光光凝术,采用美国科以人便携式激光机。能量150-400mW,光斑大小100-400μm,曝光时间0.1-0.4s。光斑反应强度为Ⅲ级(Tso’s分级):视网膜光斑呈外围两个淡灰色环的浓白色斑,其白色中心为视网膜内核层坏死,外围的淡灰色环分别为外核层和色素上皮的坏死,恢复期有脉络膜视网膜瘢痕形成。本发明组患者视网膜激光术后当天开始服实施例4制备的胶囊,1剂/d。对照组口服肌苷0.2g3次/d,维生素C0.1g3次/d。两组均严格控制血糖水平。
术后30天,对术前和术后的疗效进行评判。疗效判定:①痊愈:矫正视力明显提高,视网膜水肿或眼底出血、渗出吸收;②显效:矫正视力提高,视网膜水肿或眼底出血、渗出基本吸收;③无效:矫正视力略有提高或无改善,视网膜水肿现象未消除。
表2本发明组和对照组疗效比较
总病例数 | 痊愈 | 显效 | 无效 | 总有效率(%) | |
本发明组 | 11 | 5 | 5 | 1 | 90.9 |
对照组 | 11 | 3 | 6 | 2 | 81.8 |
该实验证实,在实际治疗时采用本发明药物与视网膜激光光凝术联用,能够大幅度降低手术给患者带来的副作用,提高患者生活质量。
Claims (10)
1.一种治疗视网膜激光光凝术引起视网膜水肿的组合物,其特征在于:由以下原料药制成:左卡尼汀0.2-0.8g。
2.一种治疗视网膜激光光凝术引起视网膜水肿的组合物,其特征在于:由以下原料药制成:左卡尼汀0.2-0.8g、当归20-30g、川芎20-30g、炒薏苡仁10-20g、白芍5-10g。
3.如权利要求2所述的组合物,其特征在于:由以下原料药制成:左卡尼汀0.3-0.6g、当归22-28g、川芎22-28g、炒薏苡仁12-18g、白芍6-9g。
4.如权利要求3所述的组合物,其特征在于:由以下原料药制成:左卡尼汀0.4-0.6g、当归23-26、川芎23-26g、炒薏苡仁13-16g、白芍7-8g。
5.如权利要求4所述的组合物,其特征在于:由以下原料药制成:左卡尼汀0.5g、当归25、川芎23g、炒薏苡仁15g、白芍8g。
6.如权利要求2-5任一项所述的组合物,其特征在于:剂型为胶囊剂、片剂或颗粒剂。
7.如权利要求2-6任一项所述的组合物的制备方法,其特征在于,包括以下步骤:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混合粉碎成粉末,过40目筛,得混合粉末;
(3)将步骤(2)所得的混合粉末与左卡尼汀混合,作为活性成分制备成药学上可接受的制剂。
8.如权利要求2-6任一项所述的组合物的制备方法,其特征在于,包括以下步骤:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加8-10倍量水,浸泡2-4小时,煎煮1-3次,每次1-3小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏,加乙醇静置、醇沉、过滤,滤液减压回收乙醇至无醇味,减压浓缩至60℃热测时相对密度1.00-1.05的流浸膏;
(3)将步骤(2)所得的流浸膏与左卡尼汀混合,制备成药学上可接受的制剂。
9.如权利要求2-6任一项所述的组合物的制备方法,其特征在于,包括以下步骤:
(1)除左卡尼汀外,按照原料药重量比例称取中药材,净选;
(2)将上述净选后药材混匀,粉碎成粗粉,加6-8倍量水,煎煮1-3次,每次2-3小时,过滤,合并滤液,减压浓缩至60℃热测时相对密度为1.20-1.30的清膏;
(3)将步骤(2)所得的清膏与左卡尼汀混合,制备成药学上可接受的制剂。
10.如权利要求2-6任一项所述的组合物在制备治疗视网膜激光光凝术引起视网膜水肿的药物中的应用。
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