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CN116056704A - 吡喹酮制剂 - Google Patents

吡喹酮制剂 Download PDF

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CN116056704A
CN116056704A CN202180055408.7A CN202180055408A CN116056704A CN 116056704 A CN116056704 A CN 116056704A CN 202180055408 A CN202180055408 A CN 202180055408A CN 116056704 A CN116056704 A CN 116056704A
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praziquantel
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peg
rubusoside
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W·米勒
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Weiya Co ltd
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Abstract

可以配制吡喹酮以增强其药代动力学、毒性和适口性。它可以作为液体、粉末或片剂储存和/或分装。减少最常见的副作用可以提高患者的依从性和满意度。改变口味可以提高患者的依从性和满意度。一旦配制，它可以用于治疗人类和兽类受试者的各种血吸虫和蠕虫。

Description

吡喹酮制剂
本发明的技术领域
本发明涉及寄生虫感染的制剂和治疗领域。特别地，本发明涉及吡喹酮制剂。
发明背景
吡喹酮是一种用于治疗多种类型的寄生虫感染的药物。具体地用于血吸虫病、华支睾吸虫病、吸虫病、绦虫感染、囊虫病、包虫病和其他吸虫感染。吡喹酮的治疗通常会导致不必要的副作用，例如由于固定或杀死的寄生虫积聚而引起的胃肠道不适。报道的副作用包括：头痛，头晕，胃痛，恶心，疲倦，虚弱，关节/肌肉疼痛，食欲不振，呕吐和出汗。这些副作用可能会伤害患者，并使使用药物的经历令人不快，并可能阻碍患者对处方药的依从性。
吡喹酮((RS)-2-(环己基羰基)-1，2，3，6，7，11b-六氢-4H-吡嗪并[2，1-a]异喹啉-4-酮)(C19H24N2O2)表示为：
Figure BDA0004113242090000011
本领域一直需要在减少副作用的情况下治疗寄生虫。
发明概述
根据本发明的一个实施方案，提供了一种液体药物制剂。制剂包括:聚乙二醇(PEG)；甜茶苷；和吡喹酮。
另一个实施方案是一种治疗患者中由血吸虫或绦虫引起的感染的方法。向患者施用液体药物制剂。制剂包括:聚乙二醇(PEG)；甜茶苷；和吡喹酮。根据一个实施方案，吡喹酮和PEG分别施用，其中PEG施用在吡喹酮施用之后。
又一个实施方案是吡喹酮的粉末状制剂，其用于在水中重构并随后作为液体制剂施用于患者。粉状制剂包括:聚乙二醇(PEG)；甜茶苷；和吡喹酮。根据一个实施方案，所述吡喹酮/甜茶苷和PEG分别施用，其中PEG施用在吡喹酮/甜茶苷施用之后。
在另一个实施例中，提供了吡喹酮的粉末状制剂。粉状制剂包括：甜茶苷和吡喹酮。
对于本领域技术人员来说，在阅读说明书后将是显而易见的这些实施例和其它实施例为本领域提供了患者依从性、满意度、舒适度和整体治疗体验方面的改进。
本发明的详细描述
本发明人开发了一种配制吡喹酮的方法，使得吡喹酮易于、准确且令人愉快地施用，并减少与其使用相关的一种或多种副作用。药代动力学特性也可能带来其他好处。
目前本领域的做法是将吡喹酮作为大片剂分装，必须将其分割(有时是多个部分)以达到病人的适当剂量。通过使用粉状或液体制剂，分装适当的剂量更容易，减少错误、变化和基于药丸拆分技术的变化的浪费。
吡喹酮仅适度溶于水。根据Merck指数，其溶解度为400mg/l。然而，如本文所公开的制剂中的元素的组合能够实现更高程度的溶解度，从而允许以适口的体积进行液体给药。液体或粉末状制剂可包括:聚乙二醇(PEG)；甜茶苷；和吡喹酮。这种组合也可以改变药代动力学特性，例如吸收。
制剂中甜茶苷与吡喹酮的比例可以在约2:1至约10:1的范围内。可以对其进行调整以实现合适的溶解度水平，胃肠道吸收和令人愉快的味觉特征。
在一些情况下，所述组合可用于形成液体制剂。在其他情况下，可能希望用它来形成片剂。
在液体和粉末状制剂中使用的聚乙二醇具有足够大的平均分子量，以使聚合物用作为渗透性泻药。通常，平均分子量在200和6000道尔顿，3000和4500之间，或在3200和3700之间。市面上流行的版本是3350、4000和6000。例如，PEG的制备可以是多分散的或单分散的。如果多分散的，则分子量描述了制剂的加权平均分子量。根据粉末或液体形式的制剂，PEG与吡喹酮的比例可介于并包括5:1和10:1之间。在一个实施例中，该比例约为8:1。
对于给药，可以在制造点、在分装药房、或由患者，粉末状在液体载体中重构。液体载体可以是水、缓冲的水溶液或含水饮料，例如能量饮料或富含电解质的饮料。或者，可以将悬甜茶苷和吡喹酮的粉末状制剂制成片剂或丸剂-带有或不带有PEG。片剂或丸剂的合适成分可包括玉米淀粉、硬脂酸镁、微晶纤维素、聚维酮、月桂基硫酸钠、聚乙二醇、二氧化钛和羟丙甲纤维素中的任何一种或全部。PEG也可以在吡喹酮之后施用。PEG或另一种泻药可能会增加吡喹酮处理过的寄生蠕虫和吸虫从宿主中排出的速率。这样做的效果是，减少人类或其他动物肠道中治疗的寄生虫和吸虫有时会出现的痛苦和滞留时间。PEG或其他泻药可以在吡喹酮施用后例如2、4、6、8、12、18、24、36或48小时施用。可以使用的其他泻药包括口服渗透剂，口服散装剂，口服大便软化剂，口服兴奋剂和/或直肠栓剂。
多种寄生虫及其引起的疾病可使用本文公开的制剂进行治疗。其中包括由血吸虫引起的血吸虫病(住血吸虫、血吸虫病或蜗牛热)，由中华肝吸虫(中国或东方吸虫)、泰国肝吸虫(东南亚肝吸虫)和猫肝吸虫(猫肝吸虫病)引起的吸虫感染，由牛带绦虫(牛肉绦虫)、猪带绦虫(猪肉绦虫)和亚洲带绦虫(亚洲绦虫)引起的绦虫病或囊尾蚴病，这些绦虫属的微小绦虫可引起囊性棘球蚴病(包虫病)或肺泡棘球蚴病。
可以治疗的患者可以是人类或兽类。通常感染的兽类动物包括马、狗、猫、家禽、牛、猪和反刍动物。这些中的任何一种都可以使用本文公开的制剂进行处理。
任何用于治疗寄生虫的组分都可以包装在试剂盒中，或者单独包装在单独的容器中，或者彼此混合。最终使用者可以用所包含的稀释剂或她自己选择和/或供应的稀释剂来重构组分。除了组分之外，试剂盒可以单独地或以混合物的形式包含使用说明、混合和/或给药的工具、储存容器等。
上述公开内容大致描述了本发明。本文公开的所有参考文献均通过引用明确并入。通过参考以下具体实施例可以获得更完整的理解，这些实施例仅用于说明的目的，而不旨在限制本发明的范围。
示例1
吡喹酮与甜茶苷的复配
通常，将成分与乙醇一起沉积到密封的容器中，并涡旋混合以形成溶液。对溶液进行离心。乙醇蒸发掉，干燥的混合物溶解在水中。该混合物再次被离心，上清液通过一个膜过滤。流动的液体被干燥，形成复方吡喹酮。
在制造液体吡喹酮的一个具体示例中，将其与甜茶苷混合以产生水溶性化学品。配制比例(10/1)为100毫克的甜茶苷与10毫克的吡喹酮。将成分沉积到装有1毫升乙醇的密封容器中，并涡旋15分钟以形成溶液。然后将混合物在12,000rpm下离心10分钟。接着，蒸发掉乙醇，然后将混合物溶于1毫升水。将该混合物再次以12,000rpm离心10分钟，并通过0.20μm膜过滤并干燥。当在水中重构时，所得混合物可用于制备吡喹酮的液体制剂。这使得制剂中的固体含量为110毫克，比例为10/1。
为了调节甜度和溶解度，该制剂可以根据条件从2/1比例-10/1比例变化。
示例2
在液体中配制复配吡喹酮/甜茶苷
吡喹酮(液体配方10/1) 7,333.37毫克
乙二醇3350 5,666.67毫克
交联羧甲基纤维素钠 43.17毫克
聚维酮 43.17毫克
月桂硫酸钠 43.17毫克
硬脂酸镁 43.17毫克
亮蓝FCF(蓝色1) 43.17
总计 13,216.22毫克
将非活性成分和活性成分(吡喹酮液体配方10/1和乙二醇3350；参见实施例1)混合均匀。然后用2.667盎司纯化水和风味增强剂如FLAVORx重构混合物。成人的剂量是每公斤20毫克吡喹酮，每天3次，例如，在清醒时每5小时一次。

Claims (32)

1.一种液体药物制剂，其特征在于，包括：
聚乙二醇(PEG)；
甜茶苷：和
吡喹酮。
2.根据权利要求1所述的液体药物制剂，其中所述PEG是多分散的。
3.根据权利要求1的液体药物制剂，其中PEG的平均分子量为2000-6000。
4.根据权利要求1所述的液体药物制剂，其中PEG是PEG3350。
5.根据权利要求1所述的液体药物制剂，其中PEG与吡喹酮的重量比在5:1与10:1之间。
6.根据权利要求1所述的液体药物制剂，其中在所述液体药物制剂中甜茶苷与吡喹酮的重量比为2:1至10:1。
7.一种治疗患者的血吸虫或绦虫感染的方法，其特征在于，包括:
将权利要求1的液体药物制剂施用于患者。
8.根据权利要求7所述的方法，其中所述患者是人。
9.根据权利要求7所述的方法，其中所述患者是兽类患者。
10.根据权利要求7所述的方法，其中所述感染是血吸虫病。
11.根据权利要求7所述的方法，其中所述血吸虫是华支睾吸虫。
12.根据权利要求7所述的方法，其中所述血吸虫是泰国肝吸虫。
13.根据权利要求7所述的方法，其中所述血吸虫是猫后皋吸虫。
14.根据权利要求7所述的方法，其中所述绦虫是牛带绦虫。
15.根据权利要求7所述的方法，其中所述绦虫是猪肉绦虫。
16.根据权利要求7所述的方法，其中所述绦虫是亚洲带绦虫。
17.根据权利要求7所述的方法，其中所述感染是棘球蚴病。
18.根据权利要求7所述的方法，其中所述患者选自下组：马、狗、猫、家禽和反刍动物。
19.根据权利要求7所述的方法，其中吡喹酮的剂量为10-40mg/kg患者体重。
20.根据权利要求7所述的方法，其中所述患者是人，并且每天被给予3剂，10-40mg/kg患者体重。
21.根据权利要求7所述的方法，其中吡喹酮的剂量为10-40mg/kg患者体重。
22.根据权利要求7所述的方法，其中所述患者是人，并且每天被给予3剂，10-40mg/kg患者体重。
23.一种吡喹酮的粉末状制剂，其适于在水中重构并随后以液体制剂形式向患者施用，所述粉末状制剂包括:
聚乙二醇(PEG)；
甜茶苷；和
吡喹酮。
24.根据权利要求23所述的粉状制剂，其中所述PEG是多分散的。
25.根据权利要求23所述的粉状制剂，其中PEG的平均分子量为2000-6000。
26.根据权利要求23所述的粉状制剂，其中所述PEG是PEG3350。
27.根据权利要求23所述的粉状制剂，其中PEG与吡喹酮的重量比在5:1与10:1之间。
28.根据权利要求23所述的粉末状制剂，其中在所述粉末状制剂中甜茶苷与吡喹酮的重量比在2:1和10:1之间。
29.一种吡喹酮的粉末状制剂，其特征在于，所述粉末状制剂包括:
甜茶苷；和
吡喹酮。
30.根据权利要求29所述的粉末状制剂，其中在所述粉末状制剂中甜茶苷与吡喹酮的重量比在2:1和10:1之间。
31.一种试剂盒，包括在单独的容器中:
聚乙二醇(PEG)；
甜茶苷；和
吡喹酮。
32.一种治疗患者的血吸虫或绦虫感染的方法，其特征在于，包括：
对患者施用吡喹酮；以及
随后向患者施用聚乙二醇(PEG)。
CN202180055408.7A 2020-08-12 2021-08-05 吡喹酮制剂 Pending CN116056704A (zh)

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Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000078149A1 (en) * 1999-06-18 2000-12-28 Bayer Aktiengesellschaft Anthelmintic compositions
WO2009126950A2 (en) * 2008-04-11 2009-10-15 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Diterpene glycosides as natural solubilizers
WO2011047227A2 (en) * 2009-10-15 2011-04-21 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Water soluble drug-solubilizer powders and their uses

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR045142A1 (es) * 2003-07-30 2005-10-19 Novartis Ag Composicion veterinaria masticable ductil de buen sabor
US8889687B2 (en) * 2011-03-04 2014-11-18 Concert Pharmaceuticals, Inc. Deuterated pyrazinoisoquinoline compounds
US9657017B2 (en) * 2013-10-17 2017-05-23 Tongli Biomedical Co., Ltd. Crystal form of (R)-praziquantel and preparation method and application thereof
IN2013MU03583A (zh) * 2013-11-14 2015-07-31 Cipla Ltd
WO2016143939A1 (ko) * 2015-03-09 2016-09-15 서울대학교산학협력단 용해도가 개선된 난용성 소재와 스테비올 배당체의 복합체 제조 방법 및 이에 의하여 제조된 용해도가 개선된 난용성 소재와 스테비올배당체의 복합체
CA3078545A1 (en) * 2017-10-06 2019-04-11 Cargill, Incorporated Stabilized steviol glycoside compositions and uses thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000078149A1 (en) * 1999-06-18 2000-12-28 Bayer Aktiengesellschaft Anthelmintic compositions
WO2009126950A2 (en) * 2008-04-11 2009-10-15 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Diterpene glycosides as natural solubilizers
WO2011047227A2 (en) * 2009-10-15 2011-04-21 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Water soluble drug-solubilizer powders and their uses

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
FANG ZHANG等: ""Reformulation of etoposide with solubility-enhancing rubusoside"", 《INTERNATIONAL JOURNAL OF PHARMACEUTICS》, vol. 434, 12 June 2012 (2012-06-12), pages 453 - 459, XP028428082, DOI: 10.1016/j.ijpharm.2012.06.013 *
LIU YANYAN 等: ""Dissolution and oral bioavailability enhancement of praziquantel by solid dispersions"", 《DRUG DELIVERY AND TRANSLATIONAL RESEARCH》, vol. 8, no. 3, 15 February 2018 (2018-02-15), pages 580 - 590 *

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