CN1141098C - 盐酸苯环壬酯的新用途 - Google Patents

盐酸苯环壬酯的新用途 Download PDF

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CN1141098C
CN1141098C CNB011048905A CN01104890A CN1141098C CN 1141098 C CN1141098 C CN 1141098C CN B011048905 A CNB011048905 A CN B011048905A CN 01104890 A CN01104890 A CN 01104890A CN 1141098 C CN1141098 C CN 1141098C
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benzene ring
vertigo
hydrochloride
nonyl ester
ring nonyl
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CN1312074A (zh
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刘传缋
梁起山
崔文玉
高占国
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Institute of Pharmacology and Toxicology of AMMS
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Priority to US10/469,396 priority patent/US20040097737A1/en
Priority to PCT/CN2002/000132 priority patent/WO2002067934A1/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

本发明涉及盐酸苯环壬酯的新用途,尤其是盐酸苯环壬酯在制备用于治疗或缓解眩晕症急性发作药物中的用途。

Description

盐酸苯环壬酯的新用途
本发明涉及盐酸苯环壬酯的新用途,尤其是盐酸苯环壬酯在制备用于治疗或缓解眩晕症急性发作药物中的用途。
盐酸苯环壬酯,系统名为2-苯基-2-环戊基-2-羟基乙酸-3-甲基-3-氮杂双环(3,3,1)壬-9α-酯盐酸盐,结构式为
中国专利申请97125424.9和中国专利申请93119491.1公开了它的制备方法、药物组合物和作为抗运动病(晕车、船、机等)药物的用途。
眩晕症是前庭器官受到强烈刺激而引起的一种疾病,常以头晕目旋、恶心呕吐、不能睁眼、不能坐立等症候群为特征,是耳鼻喉科和神经内科的常见病之一。它可由耳部疾患(周围性眩晕)和脑部疾患(中枢性眩晕)等多种疾病所致,其中以梅尼埃病和位置性眩晕发病率最高。患者常因急性发作眩晕来去医院急诊。目前尚无根治眩晕症的特效药,只能采取支持疗法或用药物控制急性发作。
本发明的一个目的是提供一种能有效治疗和缓解眩晕症急性发作的药物。
本发明人经研究现发现,与目前临床上常用的治疗眩晕症药物眩晕停对比,盐酸苯环壬酯具有更好治疗或缓解眩晕症急性发作的作用。对231名急性眩晕症发作病人的观察,肯定了盐酸苯环壬酯的这种作用。
因此,本发明涉及盐酸苯环壬酯在制备用于治疗或缓解眩晕症急性发作的药物中用途。
本发明还涉及治疗或缓解眩晕症急性发作患者的方法,其包括给将盐酸苯环壬酯给予有眩晕症急性发作的患者。
本发明还涉及用于治疗或缓解眩晕症急性发作的药物组合物,其包括盐酸苯环壬酯及药用载体或赋形剂。
下面的实施例将用来详细说明,但不限制本发明。
患者来门诊/急诊求治,经检查判定为眩晕症急性发作,首次给予盐酸苯环壬酯片2片(每片2毫克),随后每天口服2-3次,每次1片。阳性对照药为眩晕停,每片25毫米。首次口服2片,随后每天口服2-3次,每次1片。观察三天疗效。服药后眩晕症状消失为显效,减轻为好转,无改变为无效。结果见表1。
表1盐酸苯环壬酯治疗急性眩晕症病人效果
              盐酸苯环壬酯                      眩晕停
       人数   显效   好转   总有效   人数   显效    好转    总有效梅尼埃病    54    38      12      50*    26    8       10       18
            (70.4)  (22.2)  (92.6)        (30.8)  (38.4)   (69.2)位置性眩晕  13    12      1       13       3     1       1        2
            (92.3)  (7.7)   (100)         (33.3)  (33.3)   (66.6)椎基底动脉  34    22      5       27       8     0       5        5供血不足眩晕    (64.7)  (14.7)  (79.4)          (0)   (62.5)   (62.5)其它眩晕症  71    42      22      64      22    13       6       19
            (59.1)  (31.0)  (90.1)        (59.0)  (27.3)   (86.3)合计        172   114     40      154     59    22      22       44
            (66.3)  (23.3)  (89.6)        (37.3)  (37.3)   (74.6)
总有效=显效+好转
盐酸苯环壬酯和眩晕停比较,*P<0.05
由表1看出,盐酸苯环壬酯治疗急性发作眩晕症172人,总有效率为89.6%,比阳性对照组眩晕停治疗59人的总有效率74.6%高,但统计学处理P>0.05尚无显著性。但对发病率最高的酶尼埃病治疗而言,盐酸苯环壬酯的总有效率为92.6%,比眩晕停的69.2高许多,统计学处理,P<0.05,差别明显。如果将发病率最高的酶尼埃病和位置性眩晕两个病种合计,则盐酸苯环壬酯的总有效率为63/67,占94.0%,比眩晕停的19/28(占67.9%)高许多,统计学处理,P<0.01,差别非常明显。因此,盐酸苯环壬酯治疗急性眩晕症发作是有效的,在发病率较高的病种上,疗效明显好于眩晕停。

Claims (1)

1.下式所示盐酸苯环壬酯在制备用于治疗或缓解眩晕症急性发作的药物中应用。
CNB011048905A 2001-02-28 2001-02-28 盐酸苯环壬酯的新用途 Expired - Fee Related CN1141098C (zh)

Priority Applications (3)

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CNB011048905A CN1141098C (zh) 2001-02-28 2001-02-28 盐酸苯环壬酯的新用途
US10/469,396 US20040097737A1 (en) 2001-02-28 2002-02-28 Use of phencynonate hydrochloride
PCT/CN2002/000132 WO2002067934A1 (fr) 2001-02-28 2002-02-28 Nouvelle utilisation de l'hydrochlorure de phencynonate

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005099697A1 (fr) * 2004-04-16 2005-10-27 Institute Of Pharmacology And Toxicology Of The Academy Of Military Medical Sciences Utilisation d'hydrochlorure de phenylcynonate dans le traitement ou l'attenuation des symptomes de l'epilepsie
CN100341850C (zh) * 2004-11-30 2007-10-10 中国人民解放军军事医学科学院毒物药物研究所 去甲基苯环壬酯光学异构体与n-对甲基苯磺酰谷氨酸光学异构体的盐及其制备方法和用途

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CN1039623C (zh) * 1993-10-22 1998-09-02 中国人民解放军军事医学科学院毒物药物研究所 一种防治运动病综合征的药物组合物及其制备方法
CN1045956C (zh) * 1997-12-09 1999-10-27 中国人民解放军军事医学科学院毒物药物研究所 盐酸苯环壬酯的制备方法

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