CN109260526A - 小檗碱洗脱球囊赋形液及其应用 - Google Patents

小檗碱洗脱球囊赋形液及其应用 Download PDF

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CN109260526A
CN109260526A CN201810954583.XA CN201810954583A CN109260526A CN 109260526 A CN109260526 A CN 109260526A CN 201810954583 A CN201810954583 A CN 201810954583A CN 109260526 A CN109260526 A CN 109260526A
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陈绍良
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Abstract

小檗碱洗脱球囊赋形液及其应用，有效成分按如下比例包括：碘普罗胺‑370:60‑90mL；苯甲酸钠：20 mg‑40 mg；聚乙二醇：5 mg‑60 mg；乙醇：5 mL‑12mL；纯化水：2 mL‑5 mL，还含有聚乳酸‑羟基乙酸共聚物（PLGA）1‑50mg/mL。利用该赋形液使得通过指引导管后球囊上保持率更高，球囊扩张后表面残留率低，同时血管组织中吸收率（%）高，病患新生血管消失，血管重构改善。

Description

小檗碱洗脱球囊赋形液及其应用
技术领域
本发明属于载药球囊技术领域，具体涉及小檗碱洗脱球囊赋形液及其应用。
背景技术
小檗碱又称黄连素。一种常见的异喹啉生物碱，分子式C20H18NO4。它存在于小檗科等四个科十个属的许多植物中。1826年M.-E.夏瓦利埃和G.佩尔坦从Xanthoxylonclava树皮中首次获得。小檗碱为一种季铵生物碱。从乙醚中可析出黄色针状晶体；熔点85-86℃；溶于水，难溶于苯、乙醚和氯仿。其盐类在水中的溶解度都比较小，例如盐酸盐为1:500，硫酸盐为1:30。小檗碱对溶血性链球菌，金黄色葡萄球菌，淋球菌和弗氏、志贺氏痢疾杆菌等均有抗菌作用，并有增强白血球吞噬作用，对结核杆菌、鼠疫菌也有不同程度的抑制作用，对大鼠的阿米巴菌也有抑制效用。小檗碱在动物身上有抗箭毒作用，并具有末梢性的降压及解热作用。小檗碱的盐酸盐(俗称盐酸黄连素)已广泛用于治疗胃肠炎、细菌性痢疾等，对肺结核、猩红热、急性扁桃腺炎和呼吸道感染也有一定疗效。小檗碱尚具有降低血脂及调节血糖的作用。小檗碱难溶于水，不溶于乙醚和氯仿，但是易溶于脂肪。因此，小檗碱极其容易被血管壁组织吸收，从而具有显著地抑制血管平滑肌细胞增殖的作用。
发明内容
解决的技术问题：本发明提供一种小檗碱洗脱球囊赋形液及其应用，利用该赋形液使得通过指引导管后球囊上保持率更高，球囊扩张后表面残留率低，同时血管组织中吸收率(％)高。
技术方案：小檗碱洗脱球囊赋形液，有效成分按如下比例包括：碘普罗胺-370:60-90mL；苯甲酸钠：20mg-40mg；聚乙二醇：5mg-60mg；乙醇：5mL-12mL；纯化水：2mL-5mL。
优选的，上述小檗碱洗脱球囊赋形液，还含有聚乳酸-羟基乙酸共聚物(PLGA)1-50mg/mL。
优选的，上述小檗碱洗脱球囊赋形液，按如下比例组成：碘普罗胺-370:60mL；苯甲酸钠：30mg；聚乙二醇：35mg；乙醇：9mL；纯化水：3mL；聚乳酸-羟基乙酸共聚物(PLGA)20mg/mL。
上述赋形液在制备小檗碱洗脱球囊中的应用。
上述应用的具体步骤为：将小檗碱及其赋形液的混合液放入药物涂层机中，将球囊直接放入涂层机的孔道中静置5分钟，取出球囊，以5m/s的风速吹干30-60s后，重复将球囊再次置入涂层机中静置5分钟，吹干；上述步骤重复5-10次，取出球囊用无水酒精擦洗、去除球囊两侧肩部金属标志以外部分的药物。
上述小檗碱在混合液中的浓度为50μmol/L-300μmol/L。
有益结果：本发明提供一种小檗碱洗脱球囊赋形液及其应用，利用该赋形液使得通过指引导管后球囊上保持率更高，球囊扩张后表面残留率低，同时血管组织中吸收率(％)高，病患新生血管消失，血管重构改善。
附图说明
图1为动物前降支小檗碱治疗前后光学相性断层扫描(OCT)图像。左图：治疗前，可见大量斑块和新生血管，伴随血管正向重构；右图：小檗碱洗脱球囊治疗3个月后，新生血管消失，血管重构改善。
具体实施方式
以下实施例进一步说明本发明的内容，但不应理解为对本发明的限制。在不背离本发明精神和实质的情况下，对本发明方法、步骤或条件所作的修改和替换，均属于本发明的范围。若未特别指明，实施例中所用的技术手段为本领域技术人员所熟知的常规手段。
实施例1
赋形液的配制：用电子天平准确称量如下配比的赋形液
表1赋形液成分
上述各种溶液混匀后，静置2小时备用；
小檗碱洗脱球囊的制作
将小檗碱及其与赋形剂的混合液放入药物涂层机中，小檗碱在混合液中的浓度为50μmol/L-300μmol/L，将成品球囊(广东东莞博迈医疗生产的PTCA球囊)直接放入涂层机(超声喷涂仪器UC-510，北京东方金荣超声电器有限公司，北京市通州区中关村科技园通州园光机电产业基地兴光五街1号)的孔道中静置5分钟，取出球囊，以5m/s的风速吹干60s后，重复将球囊再次置入涂层机中静置5分钟，吹干；上述步骤重复5-10次。取出球囊用无水酒精擦洗、去除球囊两侧肩部金属标志以外部分的药物。
模拟测试
将制作的小檗碱洗脱球囊放入人工血管内(其内充满200mL纯化水)，膨胀球囊30s-120s后，取出球囊，应用高效液相色谱仪分别测定球囊上残余的小檗碱及人工血管纯化水中的小檗碱浓度。
表2不同赋形液涂层球囊对小檗碱丢失率及吸收率的影响(涂覆10次，膨胀120s)
动物体内测试
选用医用小型猪，经皮穿刺股动脉后，将6F左冠状动脉指引导管插入左主干的开口，将外径为0.014”的指引导丝送入到左前降支的远端，沿着导丝按照经典PCI的方法将小檗碱洗脱球囊送入到前降支和第一对角支之间的位置，膨胀球囊30s-120s后，取出球囊；
收集前降支及其第一对角支血管组织，运用上述方法测定球囊上残余的小檗碱及血管组织中的小檗碱的浓度；
同时对血管组织进行病理学分析。
表1.球囊表面不同浓度小檗碱终浓度对血管平滑肌细胞增殖率的影响

Claims (6)

1.小檗碱洗脱球囊赋形液，其特征在于有效成分按如下比例包括：碘普罗胺-370: 60-90mL；苯甲酸钠：20 mg-40 mg；聚乙二醇：5 mg-60 mg；乙醇：5 mL-12mL；纯化水：2 mL-5mL。
2.根据权利要求1所述小檗碱洗脱球囊赋形液，其特征在于还含有聚乳酸-羟基乙酸共聚物（PLGA）1-50mg/mL。
3.根据权利要求2所述小檗碱洗脱球囊赋形液，其特征在于按如下比例组成：碘普罗胺-370: 60mL；苯甲酸钠：30 mg；聚乙二醇：35 mg；乙醇：9mL；纯化水：3 mL；聚乳酸-羟基乙酸共聚物（PLGA）20mg/mL。
4.权利要求1~3任一所述赋形液在制备小檗碱洗脱球囊中的应用。
5.根据权利要求4所述的应用，其特征在于将小檗碱及其赋形液的混合液放入药物涂层机中，将球囊直接放入涂层机的孔道中静置5分钟，取出球囊，以5m/s的风速吹干30-60s后，重复将球囊再次置入涂层机中静置5分钟，吹干；上述步骤重复5-10次，取出球囊用无水酒精擦洗、去除球囊两侧肩部金属标志以外部分的药物。
6.根据权利要求5所述的应用，其特征在于小檗碱在混合液中的浓度为50 μmol/L-300μmol/L。
CN201810954583.XA 2018-08-21 2018-08-21 小檗碱洗脱球囊赋形液及其应用 Pending CN109260526A (zh)

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103736154A (zh) * 2013-12-26 2014-04-23 先健科技(深圳)有限公司 药物涂层球囊导管
CN103990221A (zh) * 2013-02-19 2014-08-20 上海微创医疗器械（集团）有限公司 一种药物洗脱球囊装置
WO2014125465A2 (en) * 2013-02-13 2014-08-21 Prendergast Thomas Patrick Method for loading dilatable catherer balloons and dilatation catheters obtained therefrom
CN104353132A (zh) * 2014-11-21 2015-02-18 浙江归创医疗器械有限公司 一种植入或介入医疗器械上药物涂层的涂覆工艺
CN106237395A (zh) * 2016-09-30 2016-12-21 鼎科医疗技术（苏州）有限公司 一种药物涂层球囊及其制备方法
CN106621003A (zh) * 2016-11-10 2017-05-10 乐普（北京）医疗器械股份有限公司 一种药物球囊导管及其制备方法和应用
CN107158486A (zh) * 2017-03-24 2017-09-15 陈绍良 小檗碱洗脱支架

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014125465A2 (en) * 2013-02-13 2014-08-21 Prendergast Thomas Patrick Method for loading dilatable catherer balloons and dilatation catheters obtained therefrom
CN103990221A (zh) * 2013-02-19 2014-08-20 上海微创医疗器械（集团）有限公司 一种药物洗脱球囊装置
CN103736154A (zh) * 2013-12-26 2014-04-23 先健科技(深圳)有限公司 药物涂层球囊导管
CN104353132A (zh) * 2014-11-21 2015-02-18 浙江归创医疗器械有限公司 一种植入或介入医疗器械上药物涂层的涂覆工艺
CN106237395A (zh) * 2016-09-30 2016-12-21 鼎科医疗技术（苏州）有限公司 一种药物涂层球囊及其制备方法
CN106621003A (zh) * 2016-11-10 2017-05-10 乐普（北京）医疗器械股份有限公司 一种药物球囊导管及其制备方法和应用
CN107158486A (zh) * 2017-03-24 2017-09-15 陈绍良 小檗碱洗脱支架

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Application publication date: 20190125