CN104640449A - 用于剧烈头痛的普拉克索经皮递送 - Google Patents
用于剧烈头痛的普拉克索经皮递送 Download PDFInfo
- Publication number
- CN104640449A CN104640449A CN201380048419.8A CN201380048419A CN104640449A CN 104640449 A CN104640449 A CN 104640449A CN 201380048419 A CN201380048419 A CN 201380048419A CN 104640449 A CN104640449 A CN 104640449A
- Authority
- CN
- China
- Prior art keywords
- pramipexole
- alternatively
- patch
- methods according
- blocker
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/275—Nitriles; Isonitriles
- A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/4015—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/48—Ergoline derivatives, e.g. lysergic acid, ergotamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs 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
本发明涉及采用经皮施用普拉克索治疗或预防丛集性头痛和偏头痛的方法。
Description
背景技术
丛集性头痛是那些经过一段时间内复发的头痛。遭受丛集性头痛的患者在可能两周至三个月范围的丛集期间可能经历每天一至三次的阵发。偏头痛是引起剧烈头痛和恶心的慢性神经系统疾病。典型偏头痛影响一半头部并持续约2至约72小时。丛集性头痛和偏头痛常见的初始治疗由施用口服药物剂型构成。
普拉克索是指示用于治疗早期帕金森氏病以及不宁腿综合征的非麦角灵多巴胺激动剂。普拉克索二盐酸盐被广泛开处方而用作以0.125、0.25、0.5、0.75、1.0和1.5mg的强度可获得的日剂量固体口服片剂。
经皮药物递送途径通常由于药物在几个小时或数天内向患者的控释而优于其它类型的药物递送,如口服或局部施用。然而,由于皮肤充当了非常有效的屏障,经皮递送系统可能仅仅适用于足够小并具有渗透皮肤的合适亲脂性的分子。
普拉克索的游离碱是一种具有适当亲脂性(2.35的log P)的小分子,因此适于经皮递送。
经皮普拉克索贴剂相当普遍,因为它们用于帕金森氏病的治疗,以及其它疾病状态,包括精神分裂症、不宁腿综合征、迟发性运动障碍和运动障碍、成瘾性障碍、睡眠障碍、与脑损伤有关的神经功能受损、抑郁症、HIV痴呆、其它痴呆、肥胖、糖尿病、快感缺乏、注意力缺陷-多动障碍、震颤、女性欲望增强、视网膜组织修复、神经炎性障碍症、戒烟、神经变性疾病和神经性疼痛。
普拉克索用于治疗和预防复发偏头痛和丛集性头痛的经皮递送用途是前所未知的。
发明内容
本发明提供了一种使用包含普拉克索的经皮贴剂治疗或预防剧烈头痛,包括偏头痛、丛集性头痛、复发丛集性头痛、慢性丛集性头痛、从开始持续不断的慢性丛集性头痛等的方法。这样的贴剂可以包含另外的伴随药物。
具体实施方式
现据发现,普拉克索经皮贴剂可用于丛集性头痛和偏头痛的治疗和预防。药物的经皮施用优于预期用途的口服递送,因为药物能够以缓慢控释的方式提供并且能够一次施用而持续1~7天。此外,经皮递送将适用于递送低剂量的药物而能够降低普拉克索副作用包括直立性低血压的发作。此外,经皮普拉克索的缓慢控释对经历过其第一次偏头痛或丛集性头痛并预期会患有复发性头痛的那些患者将会具有最大的受益。
经皮贴剂的结构/类型并非关键之处,只要其组分与普拉克索化合物以及任何可能存在的另外的活性药物化合物相容。以此条件牢记于心,则可以使用任何类型的经皮贴剂,包括但不限于,单层粘合剂中的药物(single layer drug in adhesive)、多层粘合剂中的药物(multi-layer drug inadhesive)、储库型贴剂、单片贴剂、吸收型贴剂(吸剂型贴片,汽化贴剂,vapor patch)或其它形式的经皮贴剂。本发明尽管部分依靠经皮贴剂递送的已知形式,但是通常独立于贴剂的结构方面,其原因在于所有经皮贴剂能够以预期的量、速率和持续时间有效地递送药物。
采用药物科学领域中已知的常规经皮贴剂技术,普拉克索游离碱能够以0.01mg/天至10mg/天的剂量递送。经皮递送装置的药物递送持续时间可以持续1至7天。向患者施用药物的速率将处于1μg/h至200μg/h的范围。
在药物科学中众所周知的是,非离子化药物,如游离酸和游离碱,最容易适用于经皮递送。虽然有可能经皮递送普拉克索盐,如二盐酸盐或更亲脂的盐如苯磺酸盐,但是经皮递送的优选化学形式将是游离碱普拉克索。非离子化游离碱将更有可能穿过皮肤各层而到达下层血管而因此对患者是可生物利用的。
普拉克索的经皮用途据发现适用于治疗丛集性头痛和偏头痛,以及预防丛集性头痛、偏头痛、复发性偏头痛、复发性丛集性头痛、慢性丛集性头痛和慢性偏头痛。
普拉克索可以本身或组合一种或多种其它适用于治疗或预防剧烈头痛的药物进行经皮递送。这种伴随药物包括,但不限于血清素受体激动剂、NSAIDS、抗抑郁药、麦角生物碱、阿片、抗癫痫药、抗惊厥药、钙通道阻滞剂和β-阻滞剂。这类一种或多种其他药物可以包含于经皮贴剂中或分开施用。
血清素受体激动剂的实例包括,但不限于舒马普坦、依来曲普坦、夫罗曲坦、佐米曲坦、那拉曲坦、利扎曲坦和阿莫曲坦。
NSAIDS的实例包括,但不限于布洛芬萘普生阿司匹林对乙酰氨基酚吲哚美辛和酮洛芬。
抗抑郁药的实例包括,但不限于阿米替林。
麦角生物碱的实例包括,但不限于麦角胺。
阿片类药物的实例包括,但不限于羟考酮和氢可酮。
抗癫痫药的实例包括,但不限于,加巴喷丁托吡酯和左乙拉西坦。
抗惊厥药的实例包括,但不限于戊酸钠。
钙通道阻滞剂的实例包括,但不限于维拉帕米和氨氯地平。
β-受体阻滞剂的实例包括,但不限于普萘洛尔、美托洛尔、卡维地洛和阿替洛尔。
权利要求书(按照条约第19条的修改)
1.一种治疗或预防人类患者的丛集性头痛和偏头痛的方法,包括将普拉克索经皮施用至所述人类患者,
其中,所述经皮递送是以经皮贴剂的形式,所述经皮贴剂选自单层粘合剂中的药物、多层粘合剂中的药物、单片贴剂和吸收型贴剂中的至少一种。
4.根据权利要求1所述的方法,其中,所述丛集性头痛和偏头痛是复发性或慢性的。
5.根据权利要求1所述的方法,其中,所述普拉克索以0.01mg/天至10mg/天的剂量递送1至7天。
6.根据权利要求5所述的方法,其中,向患者施用药物的速率在1μg/h至200μg/h的范围。
7.根据权利要求1所述的方法,其中,所述普拉克索以它的游离碱形式递送。
8.根据权利要求1所述的方法,进一步包括适用于治疗或预防头痛的附加药物。
9.根据权利要求8所述的方法,其中,所述附加药物选自血清素受体激动剂、NSAID、抗抑郁药、麦角生物碱、阿片、抗癫痫药、抗惊厥药、钙通道阻滞剂和β阻滞剂中的至少一种。
10.根据权利要求9所述的方法,其中,所述血清素受体激动剂选自舒马曲坦、依来曲普坦、夫罗曲坦、佐米曲坦、那拉曲坦、利扎曲坦和阿莫曲坦中的至少一种。
11.根据权利要求9所述的方法,其中,所述NSAID选自布洛芬、萘普生、阿司匹林、对乙酰氨基酚、吲哚美辛和酮洛芬中的至少一种。
12.根据权利要求9所述的方法,其中,所述抗抑郁药是阿米替林。
13.根据权利要求9所述的方法,其中,所述麦角生物碱是麦角胺。
14.根据权利要求9所述的方法,其中,所述阿片选自羟考酮和氢可酮中的至少一种。
15.根据权利要求9所述的方法,其中,所述抗癫痫药可选地选自加巴喷丁、托吡酯和左乙拉西坦中的至少一种,所述抗惊厥药可选地是戊酸钠,所述钙通道阻滞剂可选地选自维拉帕米和氨氯地平中的至少一种,并且所述β阻滞剂可选地选自普萘洛尔、美托洛尔、卡维地洛和阿替洛尔中的至少一种。
Claims (15)
1.一种治疗或预防人类患者的丛集性头痛和偏头痛的方法,包括将普拉克索经皮施用至所述人类患者。
2.根据权利要求1所述的方法,其中,所述经皮递送是以贴剂的形式。
3.根据权利要求2所述的方法,其中,经皮贴剂是选自单层粘合剂中的药物、多层粘合剂中的药物、储库型贴剂、单片贴剂和吸收型贴剂中的至少一种的形式。
4.根据权利要求1所述的方法,其中,所述丛集性头痛和偏头痛是复发性或慢性的。
5.根据权利要求1所述的方法,其中,所述普拉克索以0.01mg/天至10mg/天的剂量递送1至7天。
6.根据权利要求5所述的方法,其中,向患者施用药物的速率在1μg/h至200μg/h的范围。
7.根据权利要求1所述的方法,其中,所述普拉克索以它的游离碱形式递送。
8.根据权利要求1所述的方法,进一步包括适用于治疗或预防头痛的附加药物。
9.根据权利要求8所述的方法,其中,所述附加药物选自血清素受体激动剂、NSAID、抗抑郁药、麦角生物碱、阿片、抗癫痫药、抗惊厥药、钙通道阻滞剂和β阻滞剂中的至少一种。
10.根据权利要求9所述的方法,其中,所述血清素受体激动剂选自舒马曲坦、依来曲普坦、夫罗曲坦、佐米曲坦、那拉曲坦、利扎曲坦和阿莫曲坦中的至少一种。
11.根据权利要求9所述的方法,其中,所述NSAID选自布洛芬、萘普生、阿司匹林、对乙酰氨基酚、吲哚美辛和酮洛芬中的至少一种。
12.根据权利要求9所述的方法,其中,所述抗抑郁药是阿米替林。
13.根据权利要求9所述的方法,其中,所述麦角生物碱是麦角胺。
14.根据权利要求9所述的方法,其中,所述阿片选自羟考酮和氢可酮中的至少一种。
15.根据权利要求9所述的方法,其中,所述抗癫痫药可选地选自加巴喷丁、托吡酯和左乙拉西坦中的至少一种,所述抗惊厥药可选地是戊酸钠,所述钙通道阻滞剂可选地选自维拉帕米和氨氯地平中的至少一种,并且所述β阻滞剂可选地选自普萘洛尔、美托洛尔、卡维地洛和阿替洛尔中的至少一种。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13/570,593 US20140045801A1 (en) | 2012-08-09 | 2012-08-09 | Pramipexole transdermal delivery for severe headaches |
US13/570,593 | 2012-08-09 | ||
PCT/US2013/053400 WO2014025638A1 (en) | 2012-08-09 | 2013-08-02 | Pramipexole transdermal delivery for severe headaches |
Publications (1)
Publication Number | Publication Date |
---|---|
CN104640449A true CN104640449A (zh) | 2015-05-20 |
Family
ID=50066647
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201380048419.8A Pending CN104640449A (zh) | 2012-08-09 | 2013-08-02 | 用于剧烈头痛的普拉克索经皮递送 |
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) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2022242766A1 (zh) * | 2021-05-21 | 2022-11-24 | 成都文鼎科技发展有限公司 | 一种调节神经病变的方法 |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2919892C (en) | 2013-08-12 | 2019-06-18 | 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 |
WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | 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 |
EP3169315B1 (en) | 2014-07-17 | 2020-06-24 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
WO2016064873A1 (en) | 2014-10-20 | 2016-04-28 | 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 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1826113A (zh) * | 2003-07-23 | 2006-08-30 | Lts勒曼治疗系统股份公司 | 含有普拉克索活性剂的透皮治疗系统 |
CN101125128A (zh) * | 2002-07-25 | 2008-02-20 | 法玛西雅公司 | 含普拉克索的缓释片剂 |
US20080176913A1 (en) * | 2006-06-29 | 2008-07-24 | Arnaud Grenier | Transdermal compositions of pramipexole having enhanced permeation properties |
CN101677564A (zh) * | 2007-03-14 | 2010-03-24 | 诺普神经科学股份有限公司 | (6r)-4,5,6,7-四氢-n6-丙基-2,6-苯并噻唑-二胺的改良释放制剂及其使用方法 |
US20110178114A1 (en) * | 2008-06-30 | 2011-07-21 | Afgin Phara Llc | Topical regional neuro-affective therapy |
Family Cites Families (8)
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 |
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 |
EP1807033B1 (en) * | 2004-10-08 | 2016-07-20 | Noven Pharmaceuticals, Inc. | Transdermal drug delivery device including an occlusive backing |
JP5190358B2 (ja) * | 2006-02-28 | 2013-04-24 | 久光製薬株式会社 | 経皮吸収型製剤 |
WO2008009663A1 (en) * | 2006-07-19 | 2008-01-24 | Boehringer Ingelheim International Gmbh | Treatment of pain |
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 |
-
2012
- 2012-08-09 US US13/570,593 patent/US20140045801A1/en not_active Abandoned
-
2013
- 2013-08-02 AU AU2013299885A patent/AU2013299885A1/en not_active Abandoned
- 2013-08-02 JP JP2015526593A patent/JP2015524470A/ja active Pending
- 2013-08-02 CN CN201380048419.8A patent/CN104640449A/zh active Pending
- 2013-08-02 WO PCT/US2013/053400 patent/WO2014025638A1/en active Application Filing
- 2013-08-02 CA CA2881355A patent/CA2881355A1/en not_active Abandoned
- 2013-08-02 EP EP13828337.9A patent/EP2884843A4/en not_active Withdrawn
- 2013-08-07 TW TW102128319A patent/TW201420133A/zh unknown
-
2015
- 2015-02-04 IN IN912DEN2015 patent/IN2015DN00912A/en unknown
-
2017
- 2017-02-27 AU AU2017201316A patent/AU2017201316A1/en not_active Abandoned
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101125128A (zh) * | 2002-07-25 | 2008-02-20 | 法玛西雅公司 | 含普拉克索的缓释片剂 |
CN1826113A (zh) * | 2003-07-23 | 2006-08-30 | Lts勒曼治疗系统股份公司 | 含有普拉克索活性剂的透皮治疗系统 |
US20080176913A1 (en) * | 2006-06-29 | 2008-07-24 | Arnaud Grenier | Transdermal compositions of pramipexole having enhanced permeation properties |
CN101677564A (zh) * | 2007-03-14 | 2010-03-24 | 诺普神经科学股份有限公司 | (6r)-4,5,6,7-四氢-n6-丙基-2,6-苯并噻唑-二胺的改良释放制剂及其使用方法 |
US20110178114A1 (en) * | 2008-06-30 | 2011-07-21 | Afgin Phara Llc | Topical regional neuro-affective therapy |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2022242766A1 (zh) * | 2021-05-21 | 2022-11-24 | 成都文鼎科技发展有限公司 | 一种调节神经病变的方法 |
Also Published As
Publication number | Publication date |
---|---|
IN2015DN00912A (zh) | 2015-06-12 |
JP2015524470A (ja) | 2015-08-24 |
WO2014025638A1 (en) | 2014-02-13 |
AU2017201316A1 (en) | 2017-03-16 |
US20140045801A1 (en) | 2014-02-13 |
AU2013299885A1 (en) | 2015-03-19 |
TW201420133A (zh) | 2014-06-01 |
EP2884843A1 (en) | 2015-06-24 |
EP2884843A4 (en) | 2016-05-11 |
WO2014025638A4 (en) | 2014-04-03 |
CA2881355A1 (en) | 2014-02-13 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN104640449A (zh) | 用于剧烈头痛的普拉克索经皮递送 | |
RU2470642C2 (ru) | Аналоги птерина для лечения состояния, чувствительного к вн4 | |
JP2019517542A5 (zh) | ||
US10533012B2 (en) | (R)-pirlindole and its pharmaceutically acceptable salts for use in medicine | |
JP2015524470A5 (zh) | ||
WO2007149283B1 (en) | Use of kw-3902 for achieving diuresis in patients with congestive heart failure and acute fluid overload | |
ES2649492T3 (es) | (S)-pirlindol o sus sales farmacéuticamente aceptables para uso en medicina | |
NO20054646L (no) | Doseringskur for ikke-steroidalt anti-inflammatorisk legemiddel | |
MX2014013179A (es) | Composicion farmaceutica que comprende (1r,4r)-6´-fluoro-n,n-dimet il-4-fenil-4´,9´-dihidro-3´h-espiro[ciclohexan-1,1´-pirano[3,4,b] indol]-4-amina y un anticonvulsivante. | |
Miranda et al. | Synergism between fentanyl and tramadol in tonic inflammatory pain: the orofacial formalin test | |
Oldfield et al. | Oxycodone/Ibuprofen combination tablet: a review of its use in the management of acute pain | |
O’Brien et al. | The use of ketamine in neuropathic pain | |
US20160263088A1 (en) | Methods and Compositions for Treating Chronic Pain | |
DE602007004018D1 (de) | Imidazolcarbonsäurealkylester-haltiges Medikament zur Behandlung neurodegenerativer Erkrankungen | |
RU2016145411A (ru) | Комбинация брекспипразола и налмефена, и ее применение для лечения синдрома химической зависимости | |
TW200427452A (en) | Active substance combinations and therapies for treating abuse of alcohol | |
RU2019120527A (ru) | Замещенное производное бензимидазола в качестве модулятора активности tnf | |
Hong | Transdermal scopolamine | |
WO2018231176A3 (en) | COMBINATIONS OF DICLOFENAC AND H2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN AND INFLAMMATION | |
Grogan | Pain in Respiratory Disease | |
UA77792U (uk) | Застосування комбінованого лікарського препарату як знеболюючого засобу | |
UA77794U (uk) | Комбінований лікарський препарат | |
TH54363A (th) | วิธีและสารผสมที่ใช้ (-) นอร์ซิสแอไพรด์ร่วมกับตัวยับยั้งบั๊มพ์ของโปรตอนหรือแอนทากอนิสท์ของตัวรับ h2 | |
RU2010107462A (ru) | ЛЕЧЕНИЕ α7-СЕЛЕКТИВНЫМИ ЛИГАНДАМИ | |
TH54362A (th) | วิธีและสารผสมที่ใช้ (+) นอร์ซิสแอไพรด์ร่วมกับตัวยับยั้งปั๊มพ์ของโปรตอนหรือแอนทากอนิสท์ของตัวรับ h2 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
EXSB | Decision made by sipo to initiate substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
RJ01 | Rejection of invention patent application after publication | ||
RJ01 | Rejection of invention patent application after publication |
Application publication date: 20150520 |