CN103491961A - 阿立哌唑组合物和用于其经皮给药的方法 - Google Patents

阿立哌唑组合物和用于其经皮给药的方法 Download PDF

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CN103491961A
CN103491961A CN201180052667.0A CN201180052667A CN103491961A CN 103491961 A CN103491961 A CN 103491961A CN 201180052667 A CN201180052667 A CN 201180052667A CN 103491961 A CN103491961 A CN 103491961A
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福蒂斯·M·普拉柯吉安尼斯
穆罕默德·安瓦尔·霍萨因
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Abstract

本发明公开了液体和凝胶制剂的组合物，其包含以贴片形式经皮给药的阿立哌唑。

Description

阿立哌唑组合物和用于其经皮给药的方法
发明领域
本发明涉及药物组合物的经皮给药领域，其具有可接受的体外性能和优良的生物利用度。特别地，本发明的经皮药物组合物包括贴片剂型的阿立哌唑的液体或凝胶。
发明背景
阿立哌唑（ARPZ）是第一种新型的非典型抗精神病药物（第三代）。在生化上，ARPZ是D2族多巴胺受体的部分激动剂1,2。它能有效对抗精神分裂症的阳性和阴性症状3,4。ARPZ是喹啉酮衍生物，为白色晶体粉末，几乎不溶于水，具有低熔点（135-140℃），MW448,38g/mol和4.54的分配系数。
发明内容
实施例
ARPZ几乎不溶于水并且已被配制为液体和凝胶剂型（表1）。所有被报道的值均为重量/体积百分比（W/V）。
表1：阿立哌唑的液体和凝胶制剂的组合物（5%W/V）
将实验的最佳混合料设计用于筛选制剂变量的水平。预计1%W/V-20%W/V ARPZ液体制剂的最佳组合物具有NMP40%，DMSO40%，醇15%和水5%（表1）。凝胶制剂应当包含约0.1%-5%W/V的胶凝剂并且最佳APRZ组合物应当在约1%W/V-20%W/V范围内并具有约.5%W/V的胶凝剂。因此，预测凝胶制剂具有40%的NMP，DMSO40%，（乙）醇15%，卡波普9710.5%，和水4.5%（表1）。然而，表2列出了其它的组合，其也能够成功生产根据本发明的液体和凝胶ARPZ制剂。
表2.N-甲基-2-吡咯烷酮（NMP）、二甲基亚砜（DMSO）、乙醇和水在液体阿立哌唑制剂中的浓度范围
Figure BDA00003128189100021
除了这些组分，本领域技术人员已知的适用于本发明的其它溶剂可用于制备所述液体制剂，还有它们的组合，包括但不限于，醇类（例如但不限于（甲基、乙基、丁基、丙基、异丙基、肉豆蔻酸异丙酯等））、二醇类（例如但不限于（丙二醇、聚乙二醇、甘油等））、矿物油、植物油等等。
实施例
评估了胶凝剂和它们的浓度对ARPZ通过人造膜和人类尸体皮肤的渗透的影响并且将两个特征图显示在图1&2中。ARPZ凝胶制剂的最佳的期望的组合物包含0.5%W/V卡波普971。ARPZ可通过胶凝剂凝胶化，所述胶凝剂包括但不限于天然聚合物（例如琼脂、海藻酸和衍生物、决明子、胶原蛋白、明胶、结冷胶、瓜尔豆胶、果胶、钾或钠角叉菜胶、黄蓍胶、黄原胶等）、半合成聚合物（例如甲基纤维素、羧甲基纤维素、羟丙基纤维素、羟丙基甲基纤维素等）合成聚合物（例如羧乙烯聚合物或卡波姆：卡波普940，卡波普934，卡波普971，泊洛沙姆，聚丙烯酰胺，聚乙烯醇，聚乙烯，及其共聚物等）和粘土（例如硅酸盐等）。此外，除了纤维素膜，可在其它人造膜的情况下评估ARPZ，其它人造膜包括但不限于硅橡胶膜（聚二甲基硅氧烷）、脂质体覆盖的膜、固载型液体膜、卵磷脂有机凝胶膜等等。除了ARPZ的凝胶制剂外，还可使用其它的剂型，包括但不限于，软膏、乳膏、乳剂、脂质体等。
图1：来自于0.5%卡波普971凝胶系统的药物浓度对通过纤维素膜的ARPZ通量的影响
Figure BDA00003128189100031
图2：来自于0.5%卡波普凝胶系统的通过尸体皮肤渗透的5%ARPZ的累计量
实施例
评估了增强剂对通过人类尸体皮肤的ARPZ的通量的影响并且显示在图3中。ARPZ凝胶制剂的期望的最佳的组合物包含月桂酸和肉豆蔻酸。除了月桂酸和肉豆蔻酸增强剂，所述ARPZ经皮给药可受以下增强剂影响，所述增强剂包括但不限于，水，亚砜，和类似化学药品，二甲基亚砜（DMSO）、二甲基乙酰胺（DMAC）、二甲基甲酰胺（DMF）、癸基甲基亚砜（DCMS）等，氮酮，吡咯烷酮N-甲基-2-吡咯烷酮（NMP），2-吡咯烷酮（2p）等，脂肪酸酯（乙酸丁酯，乙酸乙酯，油酸乙酯，肉豆蔻酸异丙酯，棕榈酸异丙酯，乙酸甲酯等），脂肪酸（癸酸，辛酸，月桂酸，油酸，肉豆蔻酸，亚油酸，硬脂酸，棕榈酸等），醇类，脂肪醇类和二醇类（nathanol，十二烷醇，丙二醇，甘油等），尿素，精油，萜烯和萜类（柠檬烯，麝香草酚，桉叶油素等），脂质体，囊泡，传递体，醇质体等。
图3在具有增强剂（脂肪酸）的0.5%卡波普凝胶系统中来自于5%ARPZ的通过人类尸体皮肤渗透的药物的累计量
Figure BDA00003128189100051
实施例
评估了pH对通过人类尸体皮肤的ARPZ的渗透的影响并且将特征图显示在图2中。ARPZ凝胶经皮制剂的优选的最佳的组合物具有大约6-7的pH。除了这些最佳的pH值，ARPZ经皮给药可能受所述优选范围以外的pH值的影响，但是影响程度更小。因此，依赖于使用的环境，本发明在大约6-7的优选的pH范围以外仍然可能实现。
这里发现的系统可以50mcg/ch-2.h-800mcg/ch-2.h的通量给药ARPZ，其可产生需要疗效的ARPZ血液水平。根据本发明的教导，可通过改变所述参数（例如ARPZ初始浓度、贴片的表面积、制剂的pH、载体组成、增强剂形式和组成等）改变流量。
最佳治疗结果不仅要求合适的药物选择，而且要求有效的给药。严格的定期的药物治疗时间表的治疗精神病的服药依从性非常重要。在许多例子中，由于病人不依从，精神病药物的口服施用与最佳的给药系统相比被考虑的更少5。精神病治疗药物（特别是具有长时间持续作用的药物）的经皮给药在增加的服药依从性中（特别是在老年人口中）将是有价值的。进一步地，ARPZ经皮给药的潜在优势如下：没有猪肝色的首过效应；消除超过剂量或在剂量以下的可能性；通过简单的去除贴片，允许灵活性地终止药物施用；提供了一种简化的治疗方案，因此帮助在老年人口中的服药依从性。
参考文献
1.Inoue,T.,Domae,M.,Yamada,K.,and Furukawa,T.Effects of the novelantipsychotic agent7-([4-2,3-dichlorophenylo-1-piperazinyl]b Neuroutyloxyo-3,4-dihydro2(1H)-quinolinone(OPC-14597)on prolactin release from the rat anteriorpituitary.J.Pharmacol.Exp.Ther.1996;277(1):137-143.
2.Burris,K.D.,Moiski,T.F.,Ryan,E.,Xu,C.,Tottori,K.,Kikuchi,T.,Yocca,F.D,andMolinoff,P.B.Aripiprazole is a high affinity partial agonist at human D2dopaminereceptors.Int.J.Neuropsychopharmacol.2000;3(Suppl.1),S129.
3.Petrie,J.L.,Saha,A.R.,and McEvoy,J.P.Aripiprazole,a new atypical antipsychotic:Phase II clinical trial results.Eur.Neuropsychopharm1997;7(Suppl2):S227.
4.Saha,A.R.,McQuade,R.,Carson,W.H.,Ali,M.,W.,Durbar,G.C.,and Ingenito,G.Efficacy and safety of Aripiprazole and Risperidone vs.Placebo in patients withschizophrenia and schizoaffective disorder.World J.Biol Psych2001;2(Suppl1):305S.
5.Geeta,A.,Sanju,D.,Psychotropic Drugs and Transdermal Delivery.An Overview.Int.J.of Pharma and Bio Science,2001;V1(2).

Claims (15)

1.一种药物组合物，其包含用于经皮给药剂型的阿立哌唑。
2.权利要求1的药物组合物，其中所述阿立哌唑为凝胶或液体形式。
3.权利要求1的药物组合物，其中所述阿立哌唑以1-20%w/v的量存在。
4.权利要求2的药物组合物，其中所述阿立哌唑以1-20%w/v的量存在。
5.权利要求2的药物组合物，其中所述凝胶包含约0.1%-5%w/v的胶凝剂。
6.权利要求1的药物组合物，进一步包含大约40%N-甲基-2-吡咯烷酮、40%二甲基亚砜、15%乙醇和5%水。
7.权利要求1的药物组合物，其为液体形式并且包含醇、二醇、矿物油和/或植物油。
8.权利要求2的药物组合物，其中所述组合物为凝胶形式并且进一步包含胶凝剂，所述胶凝剂选自天然聚合物、半合成聚合物、合成聚合物、羧乙烯聚合物或卡波姆、卡波普940、卡波普934、卡波普971、泊洛沙姆、聚丙烯酰胺、聚乙烯醇、聚乙烯和其共聚物。
9.权利要求1的药物组合物，其中所述剂型为用于经皮给药的贴片。
10.权利要求1的药物组合物，其为软膏、乳膏、乳剂、脂质体剂型。
11.权利要求10的药物组合物，其中所述阿立哌唑以1-20%w/v的量存在。
12.权利要求1的药物组合物，其进一步包含增强剂。
13.权利要求12的药物组合物，其中所述增强剂选自月桂酸，肉豆蔻酸，水，亚砜，二甲基亚砜、二甲基乙酰胺、二甲基甲酰胺、癸基甲基亚砜、氮酮、吡咯烷酮、脂肪酸酯、脂肪酸、醇类、脂肪醇和二醇、尿素、精油、萜烯和萜类、脂质体、囊泡、传递体和醇质体。
14.权利要求1的药物组合物，其中所述组合物的pH为大约6-7。
15.权利要求4的药物组合物，其中所述组合物的pH为大约6-7。
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US20130171237A1 (en) 2013-07-04
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EP2632463A4 (en) 2016-04-20
AU2011320758A1 (en) 2013-05-09
CN107929239B (zh) 2021-06-01
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WO2012058091A3 (en) 2013-10-17
CN103491961B (zh) 2018-01-02
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US20130209552A1 (en) 2013-08-15
AU2011320758B2 (en) 2015-09-24
WO2012058091A2 (en) 2012-05-03
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MX339196B (es) 2016-05-16
EP2632463B1 (en) 2018-04-04

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