CN106265661A - 一种治疗腰椎间盘突出症的药物 - Google Patents
一种治疗腰椎间盘突出症的药物 Download PDFInfo
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Abstract
本发明涉及一种治疗腰椎间盘突出症的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
Description
技术领域
本发明涉及医药领域，具体的说，本发明涉及一种治疗腰椎间盘突出症的药物。
背景技术
腰椎间盘突出症是一种常见病，多发病，由于坐势或睡势的不注意，过度劳损，或体位长期固定后的突然改变，动作猛力等因素，使腰椎纤维环向外膨出，从而髓核向外突出，从而形成腰椎间盘突出症状。
调查发现，随着社会的进步、现代化信息产业的突飞迅猛发展，一些年青人长时间伏在电脑上；热衷于玩弄手机；长时间躬着腰背盯着屏幕，长期保持一种不良习惯的身体姿态，使患腰椎间盘突出症的，呈越来越年青化趋势。
一般西医在治疗椎间盘突出时，主要采用理疗的方法，还有的采用红外线、超短波或短波透热疗法等增加局部血循环、促使炎症及肿胀消退、疼痛减轻、并以增强药物对局部的作用。西医所采用的另一种方法就是通过内服药物来治疗，一般首选药物为阿斯匹林，它具有退热、镇痛和抗炎作用，但长期服用易发生恶心、呕吐、胃痛及食欲减退等消化道症状，严重者可发生胃粘膜糜烂、溃疡和出血、大剂量服用可引起肾损害。
发明内容
本发明的目的在于提供一种治疗腰椎间盘突出症的药物组合物。
为了实现本发明的目的，本发明提供一种治疗腰椎间盘突出症的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
优选地，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
优选地，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
优选地，所述稀释剂为乳糖。
优选地，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
本发明还提供化合物在制备治疗腰椎间盘突出症的药物中的用途，该化合物具有下列结构：
本文所用的术语“药学上可接受的”指不消除本文所述的化合物的生物学活性或性质的物质，如载体或稀释剂。这类物质被施用于个体不导致不希望的生物学作用或者不以有害方式与包含它的组合物中的任何组分相互作用。
如本文所用的术语“药学上可接受的载体”包括任何和所有的溶剂、分散介质、包衣材料、表面活性剂、抗氧化剂、防腐剂(例如抗菌剂、抗真菌剂)、等渗剂、吸收延迟剂、盐、防腐剂、药物稳定剂、粘合剂、赋形剂、崩解剂、润滑剂、甜味剂、矫味剂、染料等和其组合，这是本领域技术人员所熟知的(例如参见Remington's Pharmaceutical Sciences,18thEd.Mack Printing Company,1990,pp.1289-1329)。除了与活性成分不相容的载体外，在治疗或药物组合物中考虑使用任何常规载体。
本发明的药物组合物包括上述化合物或其药学上可接受的盐、溶剂化物、异构体、基于上述化合物基础上的药物前体或以上所述形式的任意混合物。这些化合物可用于制备预防和/或治疗腰椎间盘突出症的药物。
附图简要说明
图1各组椎间盘组织的病理变化(HE×100)。
具体实施方式
以下通过具体实施方式的描述对本发明作进一步说明，但这并非是对本发明的限制，本领域技术人员根据本发明的基本思想，可以做出各种修改或改进，但是只要不脱离本发明的基本思想，均在本发明的范围之内。
实验例 本发明药物对腰椎间盘突出症大鼠椎间盘组织的病理变化的影响
目标化合物：
实验动物
健康、雄性SD大鼠50只，清洁级，体质量250g左右。
实验药物
10％水合氯醛(南京军区南京总医院提供)；红霉素软膏(上海第九制药厂)；硫唑嘌呤(上海信谊药厂有限公司)。
主要仪器
高速冷冻离心机(Thermo SCIENTIFIC,Mi-croCl 21R)隔水式电热恒温培养箱(上海跃进医疗器械一厂，PYX-DHS-40X50-S-II)，自动脱水机(德国LEICA公司，TP1020)，石蜡切片机(德国LEI-CA公司，RM2235)，摊片烤片机(湖北孝感宏业医用仪器有限公司，CS-VI)，组织包埋中心(日本SAKURA公司，Tissue-Tek TEL)，光学显微镜(德国LEICA公司，DM1000)，图像分析软件(德国LEICA公司，Qwin V3)。
动物分组
适应性喂养5d后，进行标记、称质量，用随机数字表法将大鼠分为5组：空白组、假手术组、模型组、目标化合物组、对照组，每组10只，分笼饲养。
造模方法(刘锦涛，姜宏，王拥军，等.大鼠破裂型椎间盘突出模型的建立及突出物重吸收机制的研究[J].中国骨伤,201023(5):370-372.Liu JT，Jiang H，Wang YJ，et a1.Astudy of a rat lumbar discherniation model and the mechanism spontaneous ofresorption[J].China J Orthop Traumatol，2010，23(5):370-372.)
经10％的水合氯醛(40g/kg)腹腔注射麻醉成功后，剃去背部体毛，固定，外科常规消毒。无菌条件下，每只切取尾椎椎间盘2个，包含上下软骨终板。用无菌10ml二注射器针头刺破上下终板，使髓核暴露，造成游离或破裂状态。用7号手术线“米”形包绕椎间盘，放入生理盐水器皿中备用。然后无菌条件下后正中线后路依次切开皮肤、皮下组织、筋膜、肌肉，将取出尾椎间盘放入L4～L5处左侧肌肉层中，逐层缝合。伤口处涂以红霉素软膏，连续换药3d。假手术组仅切开背部和尾巴相应部位，不作尾椎椎间盘移植，余同造模。空白组不做任何处理。完成造模。
造模后第5天开始干预。目标化合物组将化合物溶于生理盐水，按5mg/kg·d的剂量灌胃给药。对照组用硫唑嘌呤溶于生理盐水，按5mg/kg·d的剂量灌胃给药。疗程：每日1次，连续治疗10天。空白组和假手术组正常饲养，不做任何处理。模型组给予等剂量的生理盐水。
处死大鼠，空白组、假手术组切取相应尾椎椎间盘，模型组、化合物组、对照组切开原手术部位，找到手术线，取出移植尾椎椎间盘，10％甲醛固定，4℃保存。将固定后的椎间盘组织行石蜡切片，HE染色，光镜下进行病理组织形态学观察，结果照相保存。
各组椎间盘组织的病理变化见图1。
空白组和假手术组椎间盘组织中可见髓核、纤维软骨及胶原纤维，周围骨组织形态正常，胶原纤维排列整齐，结构清楚，未见炎性细胞浸润。模型组椎间盘组织中纤维组织显著增生，排列紊乱，间质可见大量炎细胞浸润，并见较多异物巨细胞，显示造模成功。化合物组纤维组织轻度增生，排列不整齐，间质可见少量炎细胞浸润。对照组纤维组织中度增生，间质可见少量炎细胞浸润。说明本发明化合物和对照药物对于腰椎间盘突出症具有治疗效果。
Claims (6)
1.一种治疗腰椎间盘突出症的药物组合物，其特征在于，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
2.根据权利要求1所述的治疗腰椎间盘突出症的药物组合物，其特征在于，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
3.根据权利要求2所述的治疗腰椎间盘突出症的药物组合物，其特征在于，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
4.根据权利要求3所述的治疗腰椎间盘突出症的药物组合物，其特征在于，所述稀释剂为乳糖。
5.根据权利要求2所述的治疗腰椎间盘突出症的药物组合物，其特征在于，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
6.化合物在制备治疗腰椎间盘突出症的药物中的用途，其特征在于，该化合物具有下列结构：
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