CN1599625A - H1拮抗剂和安全类固醇治疗鼻炎的用途 - Google Patents

H1拮抗剂和安全类固醇治疗鼻炎的用途 Download PDF

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CN1599625A
CN1599625A CNA028240197A CN02824019A CN1599625A CN 1599625 A CN1599625 A CN 1599625A CN A028240197 A CNA028240197 A CN A028240197A CN 02824019 A CN02824019 A CN 02824019A CN 1599625 A CN1599625 A CN 1599625A
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antagonist
compositions
rhinitis
steroid
treat
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J·M·亚妮
D·A·格玛施
S·T·米勒
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Novartis AG
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    • A61K31/435—Heterocyclic 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
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Abstract

本发明涉及用H1拮抗剂/抗过敏药和安全类固醇治疗鼻炎的组合物和方法。

Description

H1拮抗剂和安全类固醇治疗鼻炎的用途
本发明涉及H1拮抗剂/抗过敏药与安全类固醇的组合治疗鼻部病症、特别是鼻炎的用途。
发明背景
一直以来，过敏性鼻炎采用口服抗组胺药和/或口服类固醇的方案进行治疗。全身性治疗通常要求施用更高浓度的药物化合物，以便提供有效浓度，以到达必需的治疗部位。已知抗组胺化合物具有中枢神经系统(CNS)活性，其表现为嗜睡。它们还可具有抗胆碱能活性，表现为粘膜干燥。类固醇治疗无论是口服还是鼻内给药，也可以产生显著的全身性副作用，包括肾上腺功能不全、心血管紊乱和免疫抑制。在过敏小儿患者中，生长迟缓是特别重要的方面。
鼻内组合治疗是已知的。例如，WO 97/01337公开了用于治疗鼻炎的局部鼻用抗组胺药和局部鼻用类固醇的组合。它未公开本发明的安全类固醇的使用。WO 97/46243公开了含有类固醇和抗组胺药的鼻喷雾剂。该公开没有披露或提示安全类固醇的使用。对于其它活性成分，也存在同时包含类固醇和抗组胺药的鼻内用产品(例如Pharmacobel的Cortinasal；Dupa的Neovvine；Rontag的Nicorin；SmithKline Beecham的Rinosular；Cusi的Rinocusi；以及Meider的Comfonin)。
H1拮抗剂/抗过敏药与安全类固醇的组合用于治疗鼻炎的用途是未知的。
发明概述
本发明涉及治疗鼻炎的H1拮抗剂/抗过敏药与安全类固醇的组合的鼻内用组合物。对所述组合物在哺乳动物中的使用方法也进行了策划。
优选实施方案描述
本发明包括用于治疗与过敏性鼻炎相关的喷嚏和流涕的H1拮抗剂/抗过敏药的组合物。该组合物还包括安全类固醇，在此所用的术语“安全类固醇”意指可治疗伴随充血发生的嗜酸性粒细胞和嗜中性粒细胞相关性炎症但缺乏全身性生物利用度或全身性吸收后被迅速失活的类固醇。
根据本发明可用的H1拮抗剂/抗过敏药包括所有有效的化合物，包括但不限于：依美司汀、氯雷他定、5-[2-[4-二(4-氟苯基)羟甲基-1-哌啶基]乙基]-3-甲基]-2-噁唑烷酮乙二酸盐、地氯雷他定(desloratadine)、氮司丁、奥洛他定、左卡巴司汀、依匹那丁和酮替芬。
在此可使用的安全类固醇包括任何符合安全类固醇定义的糖皮质激素，包括但不限于双甲丙酰龙和氯替泼诺。
H1拮抗剂/抗过敏药和安全类固醇(化合物)可并入各种类型的用于向鼻递药的鼻内用制剂中。例如，鼻内用制剂可以含有防腐剂如苯扎氯铵、EDTA和氨丁三醇；粘度调节剂如羟丙基甲基纤维素(HPMC)和相关物质；张力调节剂例如氯化钠(NaCl)；润湿剂/表面活性剂如四丁酚醛或聚山梨酯80；pH调节剂以及水。
优选地，将化合物配制为pH约6.0至8.0的鼻内用混悬剂或溶液剂。H1拮抗剂/抗过敏药在这些制剂中的含量通常为以重量计0.01％至0.5％，但优选以重量计0.02％至0.1％。安全类固醇在那些制剂中的含量通常为以重量计0.05％至1.5％，但优选以重量计0.1％至1.0％。因此，鼻内施用时，根据熟练临床医生的常规判断，这些制剂将每天不超过2次、每次喷射1至2次施用于鼻孔。
本发明的优选组合物包括奥洛他定(0.1％)和双甲丙酰龙(0.1％)，以及依美司汀(0.05％)和双甲丙酰龙(0.1％)。
以下实施例是对本发明组合物的阐述，但绝不限制本发明。
实施例
成分     重量％
依美司汀     0.05％
双甲丙酰龙     0.1％
苯扎氯铵     0.01％
氨丁三醇     0.5％
EDTA二钠     0.01％
氯化钠(调节等张性至280mOsmols/kg)     0.6至0.8％
HPMC     0.1至0.5％
四丁酚醛     0.05％
NaOH和/或HCl     适量至pH 7.4
纯化水     适量至100％

Claims (7)

1.治疗哺乳动物的鼻炎的方法，其包括施用药学有效量的包含H1拮抗剂/抗过敏药和安全类固醇的组合物。
2.权利要求1的方法，其中所述组合物包含H1拮抗剂/抗过敏药，选自依美司汀、氯雷他定、5-[2-[4-二(4-氟苯基)羟甲基-1-哌啶基]乙基]-3-甲基]-2-噁唑烷酮乙二酸盐、地氯雷他定、氮司丁、奥洛他定、左卡巴司汀、依匹那丁和酮替芬。
3.权利要求1的方法，其中所述组合物包含选自双甲丙酰龙和氯替泼诺的安全类固醇。
4.权利要求2的方法，其中所述组合物包含选自依美司汀、奥洛他定和地氯雷他定的拮抗剂/抗过敏药。
5.治疗哺乳动物的鼻炎的方法，其包括施用药学有效量的包含依美司汀和双甲丙酰龙的组合物。
6.治疗哺乳动物的鼻炎的方法，其包括施用药学有效量的包含奥洛他定和双甲丙酰龙的组合物。
7.治疗哺乳动物的鼻炎的方法，其包括施用药学有效量的包含地氯雷他定和双甲丙酰龙的组合物。
CNA028240197A 2001-12-05 2002-11-18 H1拮抗剂和安全类固醇治疗鼻炎的用途 Pending CN1599625A (zh)

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CA2468749A1 (en) 2003-06-19
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