CN112691104A - 一种用于治疗痔疮的药物及其制备方法 - Google Patents
一种用于治疗痔疮的药物及其制备方法 Download PDFInfo
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Abstract
本发明提供了一种用于治疗痔疮的药物及其制备方法。本发明的用于治疗痔疮的药物包括主药和基质，所述主药包括硝苯吡啶，且硝苯吡啶在药物中的质量含量为1‑3％；此外，该药物还可以包括其它用于治疗痔疮的化药原料和/或中药原料。本发明的药物能够良好地治疗内痔、外痔、混合痔、肛瘘、肛裂、肛门囊肿等痔疮疾病。
Description
技术领域
本发明涉及药物技术领域，尤其是涉及一种用于治疗痔疮的药物及其制备方法。
背景技术
硝苯吡啶(nifedipine)的化学名称为1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸二甲酯，又名硝苯地平，其是一种二氢吡啶类钙拮抗剂，目前主要用于预防和治疗冠心病心绞痛，特别是变异型心绞痛和冠状动脉痉挛所致心绞痛。硝苯吡啶对呼吸功能没有不良影响，因此特别适用于患有呼吸道阻塞性疾病的心绞痛患者，其疗效优于β受体拮抗剂。此外，硝苯吡啶还适用于各种类型的高血压，对顽固性、重度高血压也有较好疗效。
痔疮是肛门直肠底部及肛门粘膜的静脉丛发生曲张而形成的一个或多个柔软的静脉团的一种慢性疾病，包括内痔、外痔、混合痔。痔疮的发病原因较多，例如久坐、久站、劳累等使人体长时间处于一种固定体位会影响血液循环，从而导致盆腔内血流缓慢和腹内脏器充血，进而引起痔静脉过度充盈、曲张、隆起、静脉壁张力下降，其是引发痔疮的重要原因之一。此外，运动不足导致肠蠕动减慢，粪便下行迟缓或因习惯性便秘，从而压迫静脉，使局部充血和血液回流障碍，引起痔静脉内压升高，静脉壁抵抗力降低，也可导致痔疮的发病率增高。
痔疮的传统治疗方法包括手术疗法、超低温/超高温疗法、结扎/套扎疗法、注射疗法等。手术疗法的目的是摘除痔核或用缝扎等机械方法使之栓塞或萎陷，虽见效快，但容易复发，且可能导致大便失禁等后遗症；超低温、超高温疗法的治疗原理是利用超低温或超高温产生冷或热效应，起到使病灶组织蛋白凝固、血管栓塞封闭、电灼电凝止血、切割、组织变性、坏死脱落或硬化萎缩等治疗目的，其治疗效果一般，且同样存在易复发等问题；结扎、套扎疗法会使肛门部血液循环受阻，易产生淤血水肿、疼痛、排便困难等；注射疗法是将药物注入痔核内治疗痔疮，然而存在易引起粘膜溃烂粘膜脓肿等缺陷。
鉴于此，特提出本发明。
发明内容
本发明的目的在于提供一种用于治疗痔疮的药物及其制备方法，该药物能够良好地治疗内痔、外痔、混合痔、肛瘘、肛裂、肛门囊肿等痔疮疾病，具有疗程短、见效快、疗效好等优势。
本发明提供一种用于治疗痔疮的药物，包括主药和基质，所述主药包括硝苯吡啶，且硝苯吡啶在药物中的质量含量为1-3％，优选为2％。
硝苯吡啶(nifedipine)又称为硝苯地平，中文名称为1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸二甲酯，CAS号为21829-25-4，分子量为346.335，分子式为C17H18N2O6，结构式如下：
硝苯吡啶是现有用于预防和治疗冠心病心绞痛的药物；然而，本发明人经研究发现，其对痔疮具有良好的治疗效果。基于此，本发明特提出一种含有硝苯吡啶的用于治疗痔疮的药物。
进一步地，在本发明的用于治疗痔疮的药物中，主药还可以包括用于治疗痔疮的化药原料和/或中药原料。
在一实施方式中，化药原料为硝酸甘油，且硝酸甘油在药物中的质量含量为0.1-0.3％，优选为0.2％。研究发现，硝酸甘油与硝苯吡啶在治疗痔疮上具有良好的协同作用，能够显著提高痔疮的治愈率，同时消除硝苯吡啶在治疗痔疮时存在的副作用。
在一实施方式中，中药原料包括如下重量份的组分：地榆6-12份，槐花5-10份，蒲公英4-8份，冰片1-5份，黄柏3-6份和无花果2-4份。
优选地，中药原料包括如下重量份的组分：地榆9份、槐花8份、蒲公英6份、冰片3份、黄柏5份、无花果3份。
上述中药原料中各组分的功效如下：
地榆：为蔷薇科植物地榆Sanguisorba officinalis L.或长叶地榆Sanguisorbaofficinalis L.var.longifolia(Bert.)Yu etLi的干燥根。具有凉血止血，解毒敛疮等功效，主要用于便血，痔血，血痢，崩漏，水火烫伤，痈肿疮毒。
槐花：为豆科植物槐Sophora japonica L.的干燥花及花蕾，具有凉血止血，清肝泻火等功效，用于便血，痔血，血痢，崩漏，吐血，衄血，肝热目赤，头痛眩晕。
蒲公英：为菊科植物蒲公英、碱地蒲公英或同属数种植物的干燥全草。苦、甘，寒。主要用于疔疮肿毒，乳痈，瘰疬，目赤，咽痛，肺痈，肠痈，湿热黄疸，热淋涩痛等。
冰片：味辛、苦，微寒；归心、肝、肺经；清香宣散，具有开窍醒神，清热散毒，明目退翳的功效，主治热病高热神昏，中风痰厥惊痫，暑湿蒙蔽清窍，喉痹耳聋，口疮齿肿，疮痈疳痔，目赤肿痛，翳膜遮睛。
黄柏：为芸香科植物黄皮树Phellodendron chinense Schneid.的干燥树皮。具有有清热燥湿，泻火除蒸，解毒疗疮等功效；用于湿热泻痢，黄疸尿赤，带下阴痒，热淋涩痛，脚气痿蹙，骨蒸劳热，盗汗，遗精，疮疡肿毒，湿疹湿疮。
无花果：具有清热生津，健脾开胃，解毒消肿之功效。主治咽喉肿痛，燥咳声嘶，乳汁稀少，肠热便秘，食欲不振，消化不良，泄泻，痢疾，痈肿，癣疾。
进一步地，上述中药原料在药物中的质量含量可以为10-15％。上述中药原料与硝苯吡啶在治疗痔疮上具有良好的协同作用，能够显著提高痔疮的治愈率，同时降低硝苯吡啶的副作用。
在本发明的药物中，对基质不作严格限制，可根据剂型选择适宜的基质；例如，在药物剂型为软膏时，基质可以为凡士林、羊毛脂、聚乙二醇等。
本发明还提供上述药物的制备方法，包括：将主药与基质进行调和，调和方法为研合法、溶合法或乳化法。
具体地，研合法可以包括：将主药加少量基质研磨成糊状，再递加其余基质研匀；溶合法可以包括：将基质加热溶化后分次加入主药，不断搅拌至冷凝；乳化法可以包括：将油溶性物质加热至熔融，将水溶性物质溶于水，混合并不断搅拌至冷凝。可以根据主药性质选择适宜的调和方法。
特别是，上述中药原料可以经炒制、粉碎成粉状原料后与基质进行调合；炒制时采用小火进行炒制，炒制至中药原料达到干燥或基本干燥的状态即可进行粉碎。
本发明的药物能够有效治疗内痔、外痔、混合痔、肛瘘、肛裂、肛门囊肿等痔疮疾病，具有疗程短、见效快、疗效好、不易复发等优势。
具体实施方式
应该指出，以下详细说明都是例示性的，旨在对本申请提供进一步的说明。除非另有指明，本文使用的所有技术和科学术语具有与本申请所属技术领域的普通技术人员通常理解的相同含义。
需要注意的是，这里所使用的术语仅是为了描述具体实施方式，而非意图限制根据本申请的示例性实施方式。如在这里所使用的，除非上下文另外明确指出，否则单数形式也包括复数形式，此外，还应当理解的是，当在本说明中使用术语“包含”和/或“包括”时，其指明存在特征、步骤、操作、器件、组件和/或它们的组合。
下面将结合实施例对本发明的技术方案进行清楚、完整地描述，显然，所描述的实施例是本发明一部分实施例，而不是全部的实施例。基于本发明中的实施例，本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例，都属于本发明保护的范围。
实施例1
将0.2g硝苯吡啶与9.8g凡士林调和均匀，即制得本实施例的硝苯吡啶软膏。
实施例2
将9.8g聚乙二醇水浴加热使熔化后，加入0.18g硝苯吡啶和0.02g硝酸甘油，搅拌均匀后放冷，即制得本实施例的硝苯吡啶复方软膏。
实施例3
将地榆、槐花、蒲公英、冰片、黄柏、无花果小火炒制至干燥后粉碎，得到粉状中药原料；将粉状中药原料按照地榆9份、槐花8份、蒲公英6份、冰片3份、黄柏5份、无花果3份的配比关系混合均匀，即制得中药主料。
将0.1g硝苯吡啶、1.4g中药主料和8.5g凡士林调和均匀，即制得本实施例的硝苯吡啶中药复方软膏。
对照例1
将3g实施例3的中药主料和7g凡士林调和均匀，即制得本对照例的硝苯吡啶中药复方软膏。
试验例
采用实施例1-3的软膏和对照例1-2的软膏对痔疮进行治疗，治疗方法为：软膏涂抹在痔疮处，每天2次。
依据《痔疮疗效评定标准》，对痔疮的诊断及疗效评判标准如下：
诊断标准：内痔便血，痔核脱垂，直肠粘膜充血、溃疡，肛门不适；外痔肛门坠胀、疼痛、瘙痒、有异物感；混合痔并有内痔、外痔的双重症状。
疗效评判标准：
显效：便血、肿痛、脱垂、流脓、便秘、分泌物、痔核脱出等症状全部消失；
有效：便血、肿痛、脱垂、流脓、便秘、分泌物、痔核脱出等症状发作次数、程度、及持续时间明显减少或基本消失；
无效：内痔、外痔、混合痔症状无改变或各项症状加重。
对痔疮的治疗结果见表1。
表1各软膏对痔疮的治疗结果
结果表明：
1、采用硝苯吡啶软膏治疗痔疮时，一周左右即可见效，治疗总有效率可达73.3％，对痔疮的治疗效果较好；同时，采用硝苯吡啶软膏治疗痔疮存在27.2％的复发率，此外少数病例存在轻度头痛等副反应。
2、采用硝苯吡啶与硝酸甘油的复方软膏治疗痔疮时，治疗总有效率达到95％，治疗效果相对于硝苯吡啶软膏大大提高，且见效时间快于硝苯吡啶软膏；此外，该复方软膏的复发率低，仅5.2％，副反应也明显减少。
3、采用硝苯吡啶与中药的复方软膏治疗痔疮时，一周即可见效，总有效率达到100％，治疗效果相对于硝苯吡啶软膏及对照例1的中药软膏显著提高，无复发且无其它不良副反应。
最后应说明的是：以上各实施例仅用以说明本发明的技术方案，而非对其限制；尽管参照前述各实施例对本发明进行了详细的说明，本领域的普通技术人员应当理解：其依然可以对前述各实施例所记载的技术方案进行修改，或者对其中部分或者全部技术特征进行等同替换；而这些修改或者替换，并不使相应技术方案的本质脱离本发明各实施例技术方案的范围。
Claims (10)
1.一种用于治疗痔疮的药物，其特征在于，包括主药和基质，所述主药包括硝苯吡啶，且硝苯吡啶在药物中的质量含量为1-3％。
2.根据权利要求1所述的药物，其特征在于，主药还包括用于治疗痔疮的化药原料和/或中药原料。
3.根据权利要求2所述的药物，其特征在于，化药原料为硝酸甘油，且硝酸甘油在药物中的质量含量为0.1-0.3％。
4.根据权利要求2所述的药物，其特征在于，中药原料包括如下重量份的组分：地榆6-12份，槐花5-10份，蒲公英4-8份，冰片1-5份，黄柏3-6份和无花果2-4份。
5.根据权利要求4所述的药物，其特征在于，中药原料在药物中的质量含量为10-15％。
6.根据权利要求1所述的药物，其特征在于，基质为凡士林、羊毛脂和聚乙二醇中的至少一种。
7.权利要求1-6任一所述的药物的制备方法，其特征在于，包括：将主药与基质进行调和，调和方法为研合法、溶合法或乳化法。
8.根据权利要求7所述的制备方法，其特征在于，研合法包括：将主药加少量基质研磨成糊状，再递加其余基质研匀。
9.根据权利要求7所述的制备方法，其特征在于，溶合法包括：将基质加热溶化后分次加入主药，不断搅拌至冷凝。
10.根据权利要求7所述的制备方法，其特征在于，乳化法包括：将油溶性主药加热至熔融，将水溶性主药溶于水，混合并不断搅拌至冷凝。
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