CN1812802A - 用于治疗关节炎病症的制剂 - Google Patents

用于治疗关节炎病症的制剂 Download PDF

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CN1812802A
CN1812802A CNA2004800177557A CN200480017755A CN1812802A CN 1812802 A CN1812802 A CN 1812802A CN A2004800177557 A CNA2004800177557 A CN A2004800177557A CN 200480017755 A CN200480017755 A CN 200480017755A CN 1812802 A CN1812802 A CN 1812802A
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E·邦巴尔代利
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Abstract

本发明涉及用于治疗类风湿性关节炎和更通常而言的关节炎病症的制剂，其包括止痛剂/抗炎剂、免疫调节剂和软骨重构剂的组合，特别是包括水杨醇、乳香酸、原花青色素、N－乙酰基－葡糖胺、葡糖醛酸或葡糖醛酸内酯的组合。

Description

用于治疗关节炎病症的制剂
发明领域
本发明涉及用于治疗类风湿性关节炎和更通常而言的关节炎病症的制剂，其包括止痛剂/抗炎剂、免疫调节剂和软骨重构剂的组合。
这些通过不同作用机制起作用的药物的组合可减轻疼痛和阻止关节损伤的发展。
技术背景
类风湿性关节炎是一种慢性退化性疾病，它对很大一部分老年人造成影响，并给患者带来严重问题。类风湿性关节炎和关节炎病症的发病机理首先归因于免疫系统，接着归因于炎性病症，所述的炎性病症侵蚀关节内表面，引起变形性损伤，这种损伤是不可逆转的并且是疼痛的。
发明内容
本发明涉及包含能引起特别有效的治疗效果且在长期治疗后没有重要副作用的活性成分的组合。
本发明的药物制剂包含：
-纯的水杨醇或其衍生物或者包含它们的提取物，所述提取物选自富含水杨醇的Salix rubra提取物；
-基本上纯的乳香酸或其半合成衍生物或者富含乳香酸的印乳香(Boswelliaserrata)提取物；
-来自葡萄(Vitis vinifera)或大叶茶(Camellia sinensis)的原花青色素(procyanindins)或者大黄酸或其脂类衍生物；
-N-乙酰基-葡糖胺；
-葡糖醛酸或葡糖醛酸内酯。
水杨醇衍生物的实例包括乙酸或丁酸酯，而乳香酸衍生物的实例包括可药用的盐或酯。
本发明的制剂优先包含：
-含有25％重量水杨醇的Salix rubra提取物；
-含有20％重量乳香酸的印乳香提取物；
-任选与磷脂复合的来自葡萄或大叶茶的原花青色素或者大黄酸或其脂类衍生物；
-N-乙酰基-葡糖胺；
-葡糖醛酸或葡糖醛酸内酯。
Salix rubra提取物、印乳香提取物、原花青色素、N-乙酰基-葡糖胺、葡糖醛酸或葡糖醛酸内酯在制剂中的重量比优选分别为2∶1∶1∶1∶1。
制剂通常含有100至500mg 25％Salix提取物、50至150mg任选为磷脂复合物形式的原花青色素、20至200mg印乳香提取物以及各为10至500mg的葡糖胺和葡糖醛酸或葡糖醛酸内酯。
来自葡萄的原花色素可按照GB-A-1541469或FR-A-2092743或EP348781中所公开的方法得到，相应的磷脂复合物在US 4.963.527中有记载；大叶茶提取物在例如EP 814823中有公开。
乳香和乳香酸提取物及富含水杨醇的Salix rubra提取物可通过已知方法制备，并且可自商业途径获得。
本制剂可以是软或硬明胶胶囊剂、片剂或其它适于口服施用的形式。优选含有月见草(Enothera biennis)油为载体的胶囊剂。
来自葡萄和大叶茶的原花青色素具有抗自由基作用并抑制水解蛋白聚糖的金属蛋白酶；它们还可与Salix和乳香提取物中的环氧合酶2(COX-2)抑制成分相互协同作用。
作为原花色素的可选替换物，可以使用某些蒽醌类，主要是大黄酸或其脂类衍生物，例如二乙酰大黄酸，它们可减少细胞增殖并刺激蛋白聚糖的合成。
N-乙酰基-葡糖胺、葡糖醛酸或葡糖醛酸内酯被认为是结缔组织的结构单元，它们使本发明的制剂的疗效性质得到完善，因为它们促进关节中蛋白聚糖的重合成，这是一种重要的修复过程，它与前文提到的因素一起使症状改善。
本发明的组合物可以以单次或重复日常给药的形式长期施用，直到康复或缓解症状。
下述实施例进一步解释本发明。
实施例I-纤维素胶囊的制备
每粒胶囊含有：
Salix rubra提取物(含25％水杨醇)                  200mg
印乳香提取物(含20％乳香酸)                       100mg
绿茶提取物(含70％原花青色素)                     100mg
N-乙酰基-葡糖胺                                  100mg
葡糖醛酸内酯                                     100mg
月见草油                                   适量至700mg
实施例II-纤维素胶囊的制备
每粒胶囊含有：
Salix提取物(含25％水杨醇)                        200mg
印乳香提取物(含20％乳香酸)                       100mg
二乙酰大黄酸                                     100mg
N-乙酰基-葡糖胺                                  100mg
葡糖醛酸内酯                                     100mg
月见草油                                   适量至700mg
当施用于患有类风湿性关节炎或关节炎病症的患者时，实施例I的制剂在减轻疼痛、提高受累肢体的灵活性、关节的活组织检验和感觉舒适方面显示出稳定的临床效果。

Claims (6)

1.制剂，包含：
-纯的水杨醇或其衍生物或者包含它们的提取物，所述提取物选自富含水杨醇的Salix rubra提取物；
-基本上纯的乳香酸或其半合成衍生物或者富含乳香酸的印乳香提取物；
-来自葡萄或大叶茶的原花青色素或者大黄酸或其脂类衍生物；
-N-乙酰基-葡糖胺；
-葡糖醛酸或葡糖醛酸内酯。
2.如权利要求1所要求的制剂，包括：
-含有25％重量水杨醇的Salix rubra提取物；
-含有20％乳香酸的印乳香提取物；
-任选与磷脂复合的来自葡萄或大叶茶的原花青色素或者大黄酸或其脂类衍生物；
-N-乙酰基-葡糖胺；
-葡糖醛酸或葡糖醛酸内酯。
3.如权利要求1所要求的制剂，其中Salix rubra提取物、印乳香提取物、原花青色素、N-乙酰基-葡糖胺、葡糖醛酸或葡糖醛酸内酯在制剂中的重量比分别为2∶1∶1∶1∶1。
4.如权利要求2所要求制剂，其含有100至500mg 25％ Salix rubra提取物、50至150mg任选为磷脂复合物形式的原花青色素、20至200mg印乳香提取物以及各为10至500mg的葡糖胺、葡糖醛酸或葡糖醛酸内酯。
5.如权利要求1-3中任一项所要求的制剂，其为含有月见草油作为载体的胶囊剂。
6.下列成分的组合在制备用于治疗类风湿性关节炎和关节炎病症的药物、营养或饮食组合物的用途：
-纯的水杨醇或其衍生物或者包含它们的提取物，所述提取物选自富含水杨醇的Salix rubra提取物；
-基本上纯的乳香酸或其半合成衍生物或者富含乳香酸的印乳香提取物；
-来自葡萄或大叶茶的原花青色素或者大黄酸或其脂类衍生物；
-N-乙酰基-葡糖胺；
-葡糖醛酸或葡糖醛酸内酯。
CNA2004800177557A 2003-06-27 2004-06-01 用于治疗关节炎病症的制剂 Pending CN1812802A (zh)

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EP (1) EP1648484B1 (zh)
JP (1) JP2007513051A (zh)
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CN101500654A (zh) * 2006-08-08 2009-08-05 因德纳有限公司 用于慢性退行性炎性病症治疗的组合物
CN101371823B (zh) * 2007-03-19 2010-09-15 上海慈瑞医药科技有限公司 二乙酰大黄酸缓释胶囊的制备工艺
CN111110863A (zh) * 2020-01-21 2020-05-08 郑州大学 大黄酸磷脂复合物及其制备方法和应用、大黄酸磷脂复合物长循环脂质体及其制备方法

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ITMI20051349A1 (it) * 2005-07-14 2007-01-15 Indena Spa Estratto di salice uso e formulazioni che lo contengono
CN100417415C (zh) * 2006-06-28 2008-09-10 文彦春 浸润治疗关节炎的药物
FR2907339B1 (fr) * 2006-10-20 2009-04-24 Inneov Lab Composition comprenant de la glucosamine et au moins un polyphenol.
FR2918376B1 (fr) 2007-07-04 2011-10-28 Mathieu Borge Compositions liquides ou pateuses destinees a l'apport en elements essentiels a la synthese et a la constitution des proteoglycanes, notamment pour le traitement de la degradation du cartilage
EP2182967A1 (en) * 2007-09-04 2010-05-12 Catholic University Industry Academic Cooperation Foundation Process for preparing vitis vinifera pip extract and pharmaceutical composition for preventing or treating rheumatoid arthritis comprising the same
BRPI0913499B1 (pt) 2008-09-15 2020-03-17 Laila Nutraceuticals Composições anti-inflamatórias sinergísticas compreendendo extratos de boswellia serrata
KR101096574B1 (ko) * 2008-12-12 2011-12-20 에이치 엘 지노믹스(주) 유럽종 포도의 씨 추출물을 함유하는 골다공증 예방 또는 치료용 약학 조성물
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