CN103079575A - 含有聚乙二醇和电解质的泻药 - Google Patents
含有聚乙二醇和电解质的泻药 Download PDFInfo
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Abstract
本发明涉及一种含有聚乙二醇(PEG)的具有改善的依从性的泻药。根据本发明的药品适用于治疗慢性便秘,并且其特征在于包括空间上彼此分离的两种组分A和B,组分A包括聚乙二醇(PEG)并且组分B包括至少一种电解质。
Description
技术领域
本发明涉及一种含有聚乙二醇(PEG)且具有改善的依从性(compliance)的泻药。根据本发明的药品适用于治疗慢性便秘。
背景技术
“便秘”意指干硬粪便的延迟排便。其可能是归因于减慢的肠道转运,或受损的排便反射。延迟肠道转运的原因可能是饮食因素、肠壁的改变、内分泌紊乱以及神经***的功能性和器质性障碍。而且,药物例如镇静剂、精神药物或阿片样物质可能有便秘作用。受损的排便反射见于肛管疾病中、失去直肠扩张反射或者用于施加腹部压力的肌肉虚弱的情况下。
如果低粗粮饮食是延迟肠道转运的原因,通常改变生活和饮食习惯就足够。其结果经常是临时使用加速排便的泻药。大部分泻药通过增加管腔内容积来起作用,并由此通过增加肠内的内部压力来促发蠕动波。基本上,具有这种作用的泻药可以分为三组:
·膨胀剂,其在肠内膨胀,吸收水分;
·渗透性泻药,其将水引入到肠内并且/或者通过渗透压将其保持在其中;
·抑制Na+离子的吸收并由此抑制从肠腔吸收水并且/或者使水分向腔内的分泌增强的泻药。
此外,采用被认为是通过润滑作用而促进排便的润滑剂和引发排便反射的药物。
泻药的临时摄取很少引起严重的紊乱。相反,长期服用泻药引起电解质代谢的紊乱,其又可能增加便秘。仅就长期的适应症而言,例如,在阿片样物质相关的便秘中,如果电解质未充分地替换会出现这个作用。
天然出现的或合成制备的可膨胀的不可消化的多糖(其在肠内膨胀)例如亚麻籽或印度车前属(车前草)适合作为温和泻药。它们须与充足的水一起摄入,以避免肠内物质的凝胶化。
众所周知的蓖麻油通过阻断钠-钾-依赖的ATP酶来抑制钠离子和水的吸收。通便效果是可靠的。然而,由于其仅被勉强使用,因此更适用于急性便秘的治疗。
聚乙二醇(一种聚合粉末)具有渗透效应。该粉末结合与之一起吞咽的水,被运送到大肠中。此处,渗透压局部增加,并且水被释放到肠腔中。聚乙二醇既不被吸收也不被代谢(Mutschler Arzneimittelwirkungen:Lehrbuch der Pharmakologie und Toxikologie,by E.Mutschler等人,8thEdition,Stuttgart:Wissenschaftliche Verlagsgesellschaft mbH,2001,pp.647-652)。
对于长期使用,需添加电解质,例如氯化钠或氯化钾。相应的聚乙二醇电解质溶液的效力在临床研究中示出(A.Attar等人:Comparison of a lowdose polyethylene glycol electrolyte solution with lactulose for treatment ofchronic constipation(低剂量聚乙二醇电解质溶液与乳果糖在治疗慢性便秘中的比较),Gut1999;44:226-230)。
在聚乙二醇溶液中存在电解质导致该溶液的味道不宜人(咸味)。需在数月的期间内摄食PEG电解质溶液的患者因强烈的咸味而对溶液产生厌恶。这导致对于定期摄取有较差的依从性。然而,仅在慢性便秘的情况下,需要长期的定期摄取。
发明内容
因此,本发明的目的是提供具有改善的依从性的用于治疗慢性便秘的产品。
本发明的核心在于如下事实,即如果单独服用聚乙二醇和电解质则依从性可以显著改善。
在第一实施方式中,通过用于治疗慢性便秘的药品来实现本发明的目的,该药品的特征在于包括两种物理上分离的组分A和B,其中组分A包括聚乙二醇(PEG)并且组分B包括至少一种电解质。
聚乙二醇的分子量优选在2000g/mol至6000g/mol的范围内,尤其是在3000g/mol至4000g/mol的范围内,尤其是为3350g/mol。对应的聚乙二醇在肠内具有特别好的渗透效果,其是泻药活性的主要原因。例如,特定量的PEG2000(分子量为2000g/mol的聚乙二醇)产生约为相同量的PEG4000(分子量为4000g/mol的聚乙二醇)的渗透压的2倍高的渗透压。
如果PEG的分子量太低,则PEG有苦味。这导致降低的依从性。如果PEG的分子量太高,其渗透作用太低。在这种情况下,不再实现充分的通便效果。
为实现充分的通便效果,日剂量通常在每天7g至40g PEG的范围内,优选在每天13g至26g PEG的范围内。使用摄取量小于每天7g的PEG,不能确保充分的通便效果。如果PEG的摄取量显著高于每天40g,可能导致腹泻。每天摄取13g至26g的PEG已成为成人的特别优选的剂量。然而,该值取决于个体状况,例如体重或便秘原因。
在本发明的一个实施方式中,根据本发明的药品在组分A中包括13.125g的PEG作为单位剂量。这对应于成人的标准日剂量。当需求更高时,每天可以服用高达三个单位剂量。
此外,组分A可另外包括一种或多种调味剂,其额外改善依从性。本申请含义内的“调味剂”意指味料(flavor)例如橙味料,或酸化剂例如柠檬酸。此外,组分A还可包括甜味剂,例如糖精钠、糖和/或环己氨基磺酸钠等。
包含的PEG自身几乎是无味的。根据本发明添加调味剂和/或甜味剂导致药品有宜人的味道。风味和甜味的强度可以通过改变这些物质来进行调节。因宜人的味道,即使在长期使用之后也不对本发明药品产生厌恶,从而获得(甚至在长期使用中)显著改善的依从性。
这很重要,特别是在阿片类物质相关的便秘中。相应的患者在长期内经常须使用止痛药例如镇痛药,导致慢性便秘。在这种情况下,如果患者不使用或者不定期使用泻药,这可能导致一般状况的劣化。而且,就在这种情况下,电解质的平衡是至关重要的,因为破坏的电解质平衡也会引起一般状况的劣化。
在根据本发明的一个实施方式中,组分A是颗粒尤其是用于口服溶液的颗粒形式,或者作为现成溶液。
除了包括聚乙二醇的组分A,根据本发明的药品还包括至少一种电解质。后者物理分离为组分B。
例如,NaCl和/或KCl以及任选额外的碳酸氢钠可用作电解质。而且,还可以任选另外添加例如作为柠檬酸盐的Mg盐和/或Ca盐,和/或额外的菊粉。
包括电解质的组分B可以是例如包衣颗粒或粉末的形式,作为片剂、膜片剂、胶囊和/或包衣片。具体地,组分B是膜片剂的形式。
为制备根据本发明的片剂、胶囊、膜片剂和/或包衣片,可以使用常规的赋形剂。
在另一个实施方式中,通过包括至少两种分离的容器的试剂盒来实现本发明的目的:含有药品组分A的容器1,和含有药品组分B的另一容器2。
根据本发明,容器1可以是袋(sachet)。具体地,采用包覆铝袋。这种袋适用于摄取含有聚乙二醇的颗粒或现成的饮用溶液。对一种和/或数种用途,饮用溶液还可以被填充到瓶中。
含有电解质的组分B优选是固体形式。因此,相应容器2可以是袋和/或深拉片材(deep drawn sheet)。因此,根据本发明的电解质片剂可以包含在条状泡罩(blister strip)中。
根据本发明,容器1和容器2还可以可拆离地相互连接。然而,须可以以各容器1和2保持完整的方式分离这两个容器。这可以例如通过穿孔来实现。在分离过程中,组分A和B不应被混合。
分开摄取组分A和B确保了依从性的显著改善。后者在长期内也得到保持。而且,确保了所需电解质的供应。
具体实施方式
实施例
实施例1:
组分A:颗粒:
组分B:片剂:
实施例2:
组分A:铝袋中的溶液:
组分B:片剂:
Claims (10)
1.一种用于治疗慢性便秘的药品,特征在于包括两种物理上分离的组分A和B,其中组分A包括聚乙二醇(PEG),并且组分B包括至少一种电解质。
2.根据权利要求1所述的药品,特征在于所述聚乙二醇的分子量在2000g/mol至6000g/mol的范围内,尤其是在3000g/mol至4000g/mol的范围内。
3.根据权利要求1或2所述的药品,特征在于组分A还包括一种或多种调味剂。
4.根据权利要求3所述的药品,特征在于所述调味剂包括味料和/或酸化剂和/或甜味剂。
5.根据权利要求1~4中任一项所述的药品,特征在于组分A是颗粒形式尤其是用于口服溶液的颗粒形式,或者作为水溶液。
6.根据权利要求1~5中任一项所述的药品,特征在于含有作为电解质的NaCl和/或KCl,且任选额外含有碳酸氢钠,还任选含有例如柠檬酸盐的Mg盐和/或Ca盐,并且/或者任选额外含有菊糖。
7.根据权利要求1~6中一项或多项所述的药品,特征在于组分B是包衣颗粒或粉末、片剂、膜片剂、胶囊、和/或包衣片的形式。
8.一种包括至少两种分离的容器的试剂盒,一个容器含有根据前述权利要求中任一项所述的药品的组分A,并且另一容器2含有根据前述权利要求中任一项所述的药品的组分B。
9.根据权利要求8所述的试剂盒,特征在于所述容器1是袋尤其是包覆铝袋,和/或瓶。
10.根据权利要求8或9所述的试剂盒,特征在于所述容器2是袋和/或深拉片材。
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DE202010012256U DE202010012256U1 (de) | 2010-09-07 | 2010-09-07 | Abführmittel |
PCT/EP2011/065131 WO2012031978A1 (de) | 2010-09-07 | 2011-09-01 | Abführmittel enthaltend polyethylenglykol und elektrolyte |
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JP (1) | JP2013540726A (zh) |
CN (1) | CN103079575A (zh) |
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CN107028876A (zh) * | 2016-10-09 | 2017-08-11 | 舒泰神(北京)生物制药股份有限公司 | 聚乙二醇电解质口服液及其制备方法 |
CN110433174A (zh) * | 2019-07-17 | 2019-11-12 | 华南理工大学 | 一种高依从性的复方聚乙二醇电解质散剂及其制备方法与应用 |
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AU2016226380A1 (en) * | 2015-03-02 | 2017-09-21 | Colonaryconcepts Llc | Compounds and methods for PEG metabolite and PEG breakdown product assays |
FR3056109B1 (fr) * | 2016-09-21 | 2019-10-11 | Pierre Fabre Medicament | Utilisation de formulations solides de polyethylene glycol dans le traitement de la constipation |
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CN1950097A (zh) * | 2004-04-23 | 2007-04-18 | 诺金欧洲公司 | 含有聚乙二醇和电解质的压制药物组合物 |
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CN107028876A (zh) * | 2016-10-09 | 2017-08-11 | 舒泰神(北京)生物制药股份有限公司 | 聚乙二醇电解质口服液及其制备方法 |
CN110433174A (zh) * | 2019-07-17 | 2019-11-12 | 华南理工大学 | 一种高依从性的复方聚乙二醇电解质散剂及其制备方法与应用 |
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JP2013540726A (ja) | 2013-11-07 |
DE202010012256U1 (de) | 2010-11-11 |
WO2012031978A1 (de) | 2012-03-15 |
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