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 PDF

Info

Publication number
TW201420133A
TW201420133A TW102128319A TW102128319A TW201420133A TW 201420133 A TW201420133 A TW 201420133A TW 102128319 A TW102128319 A TW 102128319A TW 102128319 A TW102128319 A TW 102128319A TW 201420133 A TW201420133 A TW 201420133A
Authority
TW
Taiwan
Prior art keywords
drug
pramipexole
patch
patient
transdermal
Prior art date
Application number
TW102128319A
Other languages
English (en)
Inventor
David Thomas Rossi
Original Assignee
Mylan Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mylan Inc filed Critical Mylan Inc
Publication of TW201420133A publication Critical patent/TW201420133A/zh

Links

Classifications

    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/48Ergoline derivatives, e.g. lysergic acid, ergotamine
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; Derivatives thereof
    • A61K31/612Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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

針對嚴重頭痛之普拉克索的經皮遞送
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)

  1. 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。
  2. 如請求項1所述之方法,其中該經皮遞送的形式為一貼劑。
  3. 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。
  4. 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。
  5. 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。
  6. 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。
  7. 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。
  8. 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。
  9. 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。
  10. 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。
  11. 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。
  12. 如請求項9所述之方法,其中該抗抑鬱藥是阿米替林。
  13. 如請求項9所述之方法,其中該麥角生物鹼是麥角胺。
  14. 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。
  15. 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。
TW102128319A 2012-08-09 2013-08-07 針對嚴重頭痛之普拉克索的經皮遞送 TW201420133A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13/570,593 US20140045801A1 (en) 2012-08-09 2012-08-09 Pramipexole transdermal delivery for severe headaches
PCT/US2013/053400 WO2014025638A1 (en) 2012-08-09 2013-08-02 Pramipexole transdermal delivery for severe headaches

Publications (1)

Publication Number Publication Date
TW201420133A true TW201420133A (zh) 2014-06-01

Family

ID=50066647

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102128319A TW201420133A (zh) 2012-08-09 2013-08-07 針對嚴重頭痛之普拉克索的經皮遞送

Country Status (9)

Country Link
US (1) US20140045801A1 (zh)
EP (1) EP2884843A4 (zh)
JP (1) JP2015524470A (zh)
CN (1) CN104640449A (zh)
AU (2) AU2013299885A1 (zh)
CA (1) CA2881355A1 (zh)
IN (1) IN2015DN00912A (zh)
TW (1) TW201420133A (zh)
WO (1) WO2014025638A1 (zh)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA3219716A1 (en) * 2021-05-21 2022-11-24 Wen Zeng Method for modulating neuropathies

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070243240A9 (en) * 2000-08-24 2007-10-18 Fred Windt-Hanke Transdermal therapeutic system
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
JP2011526889A (ja) * 2008-06-30 2011-10-20 アフギン ファーマ,エルエルシー 局所局部的神経作用療法
WO2010010141A1 (en) * 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Pramipexole for treating cardiomyopathy
WO2011046927A1 (en) * 2009-10-13 2011-04-21 Nupathe,Inc. Transdermal methods and systems for the delivery of rizatriptan

Also Published As

Publication number Publication date
CA2881355A1 (en) 2014-02-13
JP2015524470A (ja) 2015-08-24
CN104640449A (zh) 2015-05-20
EP2884843A4 (en) 2016-05-11
EP2884843A1 (en) 2015-06-24
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

Similar Documents

Publication Publication Date Title
TW201420133A (zh) 針對嚴重頭痛之普拉克索的經皮遞送
Chen et al. Pharmacotherapy for Parkinson's disease
JP2015524470A5 (zh)
JP2013523764A (ja) 体性感覚障害治療用の組成物と方法
RU2010143864A (ru) Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов
TWI457331B (zh) 以飢餓激素仿劑為主之增強的偏頭痛治療
US20130150346A1 (en) Use of FAAH Inhibitors for Treating Parkinson's Disease and Restless Legs Syndrome
ES2649492T3 (es) (S)-pirlindol o sus sales farmacéuticamente aceptables para uso en medicina
US8642639B2 (en) Formulation for L-tryptophane comprising carbidopa/benserazide
ES2649491T3 (es) (R)-pirlindol y sus sales farmacéuticamente aceptables para uso en medicina
Marinangeli et al. Improved cancer pain treatment using combined fentanyl‐TTS and tramadol
JP2021138703A (ja) オピオイドとn−アシルエタノールアミンの組み合わせ
JP2018522020A (ja) 鎮咳組成物及び方法
WO2020229388A1 (en) Mirtazapine for use in medication overuse headache based on tension-type headache
JP3394257B2 (ja) パーキンソン病の治療を目的とする医薬品の製造のためのエファロキサンおよびその誘導体の使用
O’Brien et al. The use of ketamine in neuropathic pain
US20160263088A1 (en) Methods and Compositions for Treating Chronic Pain
JP6027916B2 (ja) ロキソプロフェン含有医薬組成物
DE602007004018D1 (de) Imidazolcarbonsäurealkylester-haltiges Medikament zur Behandlung neurodegenerativer Erkrankungen
WO2018159716A1 (ja) アルコール使用障害の治療薬
JP2008524176A (ja) ジヒドロイミダゾピラジン誘導体を含む鎮痛性組合せ物
JP2021535216A (ja) セバコイルジナルブフィンとアセトアミノフェンの医薬品製剤及び疼痛を治療する方法
US20050101655A1 (en) Migraine treatments including isovaleramide compounds and serotonin agonists
TW200427452A (en) Active substance combinations and therapies for treating abuse of alcohol
JP2017137306A (ja) トリプタンとアスコルビン酸を含有する医薬組成物