TW201420133A - 針對嚴重頭痛之普拉克索的經皮遞送 - Google Patents
針對嚴重頭痛之普拉克索的經皮遞送 Download PDFInfo
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Abstract
本發明係關於一種使用普拉克索的經皮給藥來治療及預防叢集性頭痛和偏頭痛的方法。
Description
本發明係關於針對嚴重頭痛之普拉克索的經皮遞送。
叢集性頭痛(cluster headache)是彼等在一段時間內會復發的頭痛。患有叢集性頭痛的病人可能會經歷在叢集期間每天一到三次的急性發作,該叢集期可能在兩個星期到三個月的範圍內。偏頭痛(Migraines)是慢性神經系統疾病引起的嚴重頭痛和反胃。典型的偏頭痛影響頭部的二分之一,並且持續約2到約72小時。針對叢集性頭痛和偏頭痛的常見的初始治療包括口服藥物劑型的給藥。
普拉克索(Pramipexole)是一種用於有效治療早期巴金森氏症(Parkinson's disesase)和睡眠腳動症(restless legs syndrome)的非麥角靈類多巴胺受體致效藥。二鹽酸普拉克索(Pramipexole dihydrochloride)被廣泛地處方用藥,並且二鹽酸普拉克索口服固體片劑的每日劑量可用規格為0.125mg、0.25mg、0.5mg、0.75mg、1.0mg和1.5mg。
藥物的經皮遞送路徑往往比其他類型的藥物遞送路徑(諸如,口服給藥或者局部給藥)更佳,此是由於藥物經數小時或幾天的時間控釋入病人體內。然而,由於皮膚充當著非常有效的屏障,所以經皮遞送系統只能以足夠小和具有適當親脂性以滲透入皮膚的分子形式利用。
普拉克索遊離鹼是一種具有適當親脂性(脂水分配係數log P為2.35)的小分子,因此適合於經皮遞送。
普拉克索經皮貼劑是相當常用的,例如普拉克索經皮貼劑可用於治療巴金森氏症和其他病狀(包括精神分裂症、睡眠腳動症、遲發性運動障礙和運動失調、成癮性障礙、睡眠障礙、與腦損傷有關的神經功能缺損、抑鬱症、HIV感染癡呆癥、其他癡呆癥、肥胖症、糖尿病、失樂症、注意力缺失過動症、顫抖症、女性性慾升高、視網膜組織恢復、神經炎症、吸煙戒斷癥狀、神經退化性疾病和神經性疼痛)。
普拉克索之經皮遞送用於治療和預防先前未知的復發性偏頭痛和叢集性頭痛。
本發明提供一種使用包含普拉克索的經皮貼劑來治療或預防嚴重頭痛的方法,該等嚴重頭痛包括偏頭痛、叢集性頭痛、復發的叢集性頭痛、慢性的叢集性頭痛、不斷偏移的慢性叢集性頭痛等。此類貼劑可包括額外的輔助藥物。
現在已經發現普拉克索經皮貼劑可以用於治療和預防叢集性頭痛和偏頭痛。對於意欲以緩慢、可控釋的方式給藥並且給藥一次藥效可持續1到7天的藥物使用方式,經皮給藥優於口服遞送。此外,經皮遞送將可用於遞送較低劑量的藥物,此可以減少普拉克索副作用(包括起立性低血壓)的發生。另外,普拉克索的經皮緩慢可控釋放對於彼等已經經歷過第一次偏頭痛或第一次叢集性頭痛並且預計將會有復發性頭痛的病人將會有最大的益處。
經皮貼劑的結構/類型並不重要,只要經皮貼劑的成分與普拉克索化合物以及任何可能存在的額外的有效藥物化合物相容。考慮到此條件,可以使用任何類型的經皮貼劑,包括但不限於單層藥物基質層(single layer drug in adhesive)、多層藥物基質層(multi-layer drug in adhesive)、儲庫型貼劑(reservoir patch)、單層貼劑(monolithic patch)、吸劑貼劑(vapor patch)或者其他形式的經皮貼劑。本發明雖然部分地依賴於已知形式的經皮貼劑遞送,但是大體上與貼劑的結構態樣無關,只要所有的經皮貼劑能以所欲數量、速率和持續時間來有效地遞送藥物。
使用藥物科學領域中已知的傳統經皮貼劑技術,可以將普拉克索遊離鹼以每日0.01mg到10mg的劑量遞送。從經皮裝置遞送藥物的持續時間可以持續1到7天。對病人的給藥速率將會在每小時1到200的範圍內。
在藥物科學領域中眾所周知的是,非解離性藥物,諸如遊離酸和遊離鹼,最容易使自身經皮遞送。雖然經皮遞
送普拉克索鹽(諸如,二鹽酸鹽或者較親脂的鹽(例如,苯磺酸鹽))是可能的,但是用於經皮遞送的較佳化學形式是普拉克索遊離鹼。非解離性的遊離鹼將更可能穿過皮膚層到達下層血管,因此對病人而言是生物可利用的。
已發現普拉克索的經皮使用可用於治療叢集性頭痛和偏頭痛,以及預防叢集性頭痛、偏頭痛、復發性偏頭痛、復發的叢集性頭痛、慢性的叢集性頭痛和慢性的偏頭痛。
普拉克索可以自身單獨地經皮遞送,或者與一或多種可用於治療或預防嚴重頭痛的其他藥物一起使用。此類輔助藥物包括但不限於血清素受體致效劑(serotonin receptor agonists)、非類固醇抗炎藥(NSAIDS)、抗抑鬱藥(antidepressants)、麥角生物鹼(ergot alkaloids)、類鴉片藥物(opioids)、抗癲癇藥(antiepileptics)、鎮癲癇藥(anti-seizure drugs)、鈣離子通道阻斷劑(calcium channel blockers),以及β受體阻斷劑(beta blockers)。此類其他的藥物可以包含在經皮貼劑內或者單獨地給藥。
血清素受體致效劑的實例包括但不限於司麥普坦(sumatriptan)、依利曲坦(elitriptan)、夫羅曲坦(frovotriptan)、佐米曲坦(zolmitriptan)、那拉曲坦(naratriptan)、利紮曲普坦(rizatriptan)以及阿莫曲坦(almotriptan)。
NSAIDS的實例包括但不限於布洛芬(ibuprofen)、那普洛辛(naproxen)、阿斯匹靈(aspirin)、乙醯胺酚(acetaminophen)、吲美灑辛(indomethacin)以及凱妥普洛
芬(ketoprofen)。
抗抑鬱藥的實例包括但不限於阿米替林(amitriptyline)。
麥角生物鹼(ergotalkaloid)的實例包括但不限於麥角胺(ergotamine)。
類鴉片藥物的實例包括但不限於氧可酮(oxycodone)和氫可酮(hydrocodone)。
抗癲癇藥的實例包括但不限於佳巴本汀(gabapentin)、托比拉邁(topiramate)和左乙拉西坦(levetiracetam)。
鎮癲癇藥的實例包括但不限於戊酸鈉(sodium valerate)。
鈣離子通道阻斷劑的實例包括但不限於維拉帕米(verapamil)和安洛待平(amlodipine)。
β阻斷劑的實例包括但不限於心得安(propanolol)、美多心安(metoprolol)、卡維地洛(cavedilol)和阿替洛爾(atenolol)。
Claims (15)
- 一種普拉克索在製造一藥物上的用途,該藥物用於藉由對一病人經皮地施用普拉克索來治療或者預防該病人的叢集性頭痛及偏頭痛。
- 如請求項1所述之方法,其中該經皮遞送的形式為一貼劑。
- 如請求項2所述之方法,其中該經皮貼劑的形式是從一單層藥物基質層、一多層藥物基質層、一儲庫型貼劑、一單層貼劑及一吸劑貼劑中的至少一者中選出的一形式。
- 如請求項1所述之方法,其中該叢集性頭痛及該偏頭痛是復發性的或慢性的。
- 如請求項1所述之方法,其中該普拉克索是以每日0.01mg到10mg的劑量遞送1到7天。
- 如請求項5所述之方法,其中對病人給藥的速率在每小時1μg到200μg的範圍內。
- 如請求項1所述之方法,其中該普拉克索是以其遊離鹼的形式遞送的。
- 如請求項1所述之方法,該方法進一步包含可用於治療或者預防頭痛的一額外藥物。
- 如請求項8所述之方法,其中該額外的藥物是從一血清素受體致效劑、一非類固醇抗炎藥、一抗抑鬱劑、一麥角生物鹼、一類鴉片藥物、一抗癲癇藥、一鎮癲癇藥、一鈣離子通道阻斷劑及一β受體阻斷劑的至少一者中選出的。
- 如請求項9所述之方法,其中該血清素受體致效劑是從司麥普坦、依利曲坦、夫羅曲坦、佐米曲坦、那拉曲坦、利紮曲普坦以及阿莫曲坦中的至少一者中選出的。
- 如請求項9所述之方法,其中該非類固醇抗炎藥是從布洛芬、那普洛辛、阿斯匹靈、乙醯胺酚、吲美灑辛以及凱妥普洛芬中的至少一者中選出的。
- 如請求項9所述之方法,其中該抗抑鬱藥是阿米替林。
- 如請求項9所述之方法,其中該麥角生物鹼是麥角胺。
- 如請求項9所述之方法,其中該類鴉片藥物是從氧可酮及氫可酮的至少一者中選出的。
- 如請求項9所述之方法,其中該抗癲癇藥是視情況地從佳巴本汀、托比拉邁和左乙拉西坦的至少一者中選出的,該鎮癲癇藥視情況為戊酸鈉,該鈣離子通道阻斷劑視情況從維拉帕米和安洛待平的至少一者中選出的,以及該β受體阻斷劑視情況從心得安、美多心安、卡維地洛和阿替洛爾的至少一者中選出的。
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CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
EP2946776A1 (de) * | 2014-05-20 | 2015-11-25 | LTS LOHMANN Therapie-Systeme AG | Transdermales therapeutisches System zur Abgabe von Amitriptylin |
US9707184B2 (en) | 2014-07-17 | 2017-07-18 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
AU2015336065A1 (en) | 2014-10-20 | 2017-05-04 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
CN104523709A (zh) * | 2014-12-22 | 2015-04-22 | 青岛正大海尔制药有限公司 | 一种含有琥珀酸夫罗曲坦的复方缓释制剂 |
WO2020227646A1 (en) * | 2019-05-09 | 2020-11-12 | Apkarian Technologies Llc | Methods and compositions for treating pain |
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US7921999B1 (en) * | 2001-12-20 | 2011-04-12 | Watson Laboratories, Inc. | Peelable pouch for transdermal patch and method for packaging |
MY136318A (en) * | 2002-07-25 | 2008-09-30 | Pharmacia Corp | Sustained-release tablet composition |
DE10333393A1 (de) * | 2003-07-23 | 2005-02-24 | Lts Lohmann Therapie-Systeme Ag | Transdermales Therapeutisches System mit dem Wirkstoff Pramipexol |
US8252321B2 (en) * | 2004-09-13 | 2012-08-28 | Chrono Therapeutics, Inc. | Biosynchronous transdermal drug delivery for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and the treatment of hyperglycemia, alzheimer's disease, sleep disorders, parkinson's disease, aids, epilepsy, attention deficit disorder, nicotine addiction, cancer, headache and pain control, asthma, angina, hypertension, depression, cold, flu and the like |
TW200628175A (en) * | 2004-10-08 | 2006-08-16 | Noven Pharma | Transdermal drug delivert device including an occlusive backing |
US8524273B2 (en) * | 2006-02-28 | 2013-09-03 | Hisamitsu Pharmaceutical Co., Inc. | Transdermal absorption preparation |
WO2008001204A2 (en) * | 2006-06-29 | 2008-01-03 | Antares Pharma Ipl Ag | Transdermal compositions of pramipexole having enhanced permeation properties |
WO2008009663A1 (en) * | 2006-07-19 | 2008-01-24 | Boehringer Ingelheim International Gmbh | Treatment of pain |
JP2010521493A (ja) * | 2007-03-14 | 2010-06-24 | ノップ ニューロサイエンシーズ、インク. | (6r)−4,5,6,7−テトラヒドロ−n6−プロピル−2,6−ベンゾチアゾール−ジアミンの放出調節製剤およびそれらの使用方法 |
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WO2011046927A1 (en) * | 2009-10-13 | 2011-04-21 | Nupathe,Inc. | Transdermal methods and systems for the delivery of rizatriptan |
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JP2015524470A (ja) | 2015-08-24 |
CN104640449A (zh) | 2015-05-20 |
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AU2013299885A1 (en) | 2015-03-19 |
AU2017201316A1 (en) | 2017-03-16 |
IN2015DN00912A (zh) | 2015-06-12 |
WO2014025638A4 (en) | 2014-04-03 |
US20140045801A1 (en) | 2014-02-13 |
WO2014025638A1 (en) | 2014-02-13 |
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