CN104490893A - 一种治疗失眠的药物组合物 - Google Patents

一种治疗失眠的药物组合物 Download PDF

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CN104490893A
CN104490893A CN201410722860.6A CN201410722860A CN104490893A CN 104490893 A CN104490893 A CN 104490893A CN 201410722860 A CN201410722860 A CN 201410722860A CN 104490893 A CN104490893 A CN 104490893A
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pharmaceutical composition
compound
insomnia
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diluent
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CN104490893B (zh
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李志刚
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MEIYA PHARMACEUTICAL HAIAN Co.,Ltd.
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李志刚
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep

Abstract

本发明涉及一种治疗失眠的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：

Description

一种治疗失眠的药物组合物
技术领域
本发明涉及医药领域，具体的说，本发明涉及一种治疗失眠的药物组合物。
背景技术
失眠是指睡眠不足或睡不熟的一种睡眠障碍。可分为入睡困难，时常觉醒、早醒等。主要原因有精神过度紧张或兴奋疼痛、环境嘈杂、服用兴奋性饮料或药物以及躯体性疾病等。一般多伴有疲劳、不安、全身不适、无精打采、反应迟缓、头痛、记忆力不集中等症状。它的最大影响是精神方面的，严重一点会导致精神分裂。常影响人们正常的生活、学习、工作和健康。若长期不寐，将给病人带来巨大的痛苦。
发明内容
本发明的目的在于提供一种治疗失眠的药物组合物。
为了实现本发明的目的，本发明提供一种治疗失眠的化合物，该化合物具有下列结构：
本发明还提供一种治疗失眠的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
优选地，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
优选地，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
优选地，所述稀释剂为乳糖。
优选地，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
本发明还提供化合物在制备治疗失眠的药物中的用途，该化合物具有下列结构：
本文所用的术语“药学上可接受的”指不消除本文所述的化合物的生物学活性或性质的物质，如载体或稀释剂。这类物质被施用于个体不导致不希望的生物学作用或者不以有害方式与包含它的组合物中的任何组分相互作用。
如本文所用的术语“药学上可接受的载体”包括任何和所有的溶剂、分散介质、包衣材料、表面活性剂、抗氧化剂、防腐剂(例如抗菌剂、抗真菌剂)、等渗剂、吸收延迟剂、盐、防腐剂、药物稳定剂、粘合剂、赋形剂、崩解剂、润滑剂、甜味剂、矫味剂、染料等和其组合，这是本领域技术人员所熟知的(例如参见Remington'sPharmaceutical Sciences,18th Ed.Mack PrintingCompany,1990,pp.1289-1329)。除了与活性成分不相容的载体外，在治疗或药物组合物中考虑使用任何常规载体。
经动物实验证明，本发明的化合物能够安全有效治疗失眠
具体实施方式
以下通过具体实施方式的描述对本发明作进一步说明，但这并非是对本发明的限制，本领域技术人员根据本发明的基本思想，可以做出各种修改或改进，但是只要不脱离本发明的基本思想，均在本发明的范围之内。
实验例本发明化合物对小鼠睡眠时间的影响
取NIH小鼠50只，20±2g，随机分为五组，分别为生理盐水组，安定阳性对照组、化合物高剂量组、化合物中剂量组和化合物低剂量组，每组10只。灌胃给药，40分钟后，腹腔注射戊巴比妥钠40mg/kg，记录小鼠的睡眠时间，即翻正反射消失时间。结果见下表1。数据使用SPSS 13.0进行统计。
表1
*和生理盐水组相比，P<0.05；和阳性对照组相比，P>0.05
由上表可见，本发明化合物和生理盐水组相比，具有显著性差别。本发明化合物的高剂量组和阳性安定对照组的效果相比，没有显著性差别。这说明，本发明化合物的镇静催眠效果极佳，非常适合开发出成功的临床药物。

Claims (7)

1.一种治疗失眠的化合物，其特征在于，该化合物具有下列结构：
2.一种治疗失眠的药物组合物，其特征在于，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
3.根据权利要求2所述的治疗失眠的药物组合物，其特征在于，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
4.根据权利要求3所述的治疗失眠的药物组合物，其特征在于，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
5.根据权利要求4所述的治疗失眠的药物组合物，其特征在于，所述稀释剂为乳糖。
6.根据权利要求3所述的治疗失眠的药物组合物，其特征在于，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
7.化合物在制备治疗失眠的药物中的用途，其特征在于，该化合物具有下列结构：
CN201410722860.6A 2014-12-02 2014-12-02 一种治疗失眠的药物组合物 Active CN104490893B (zh)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105218465A (zh) * 2015-11-14 2016-01-06 刘杰 一种治疗乳腺癌的药物组合物

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1546037A (zh) * 2003-12-08 2004-11-17 南昌弘益科技有限公司 地西泮滴丸及其制备方法
US20080279784A1 (en) * 2007-05-07 2008-11-13 Questcor Pharmaceuticals, Inc. Nasal administration of benzodiazepines

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1546037A (zh) * 2003-12-08 2004-11-17 南昌弘益科技有限公司 地西泮滴丸及其制备方法
US20080279784A1 (en) * 2007-05-07 2008-11-13 Questcor Pharmaceuticals, Inc. Nasal administration of benzodiazepines

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105218465A (zh) * 2015-11-14 2016-01-06 刘杰 一种治疗乳腺癌的药物组合物

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