KR100968293B1 - 파킨슨병의 치료를 위한 개선된 경피제제 - Google Patents
파킨슨병의 치료를 위한 개선된 경피제제 Download PDFInfo
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- KR100968293B1 KR100968293B1 KR1020027018012A KR20027018012A KR100968293B1 KR 100968293 B1 KR100968293 B1 KR 100968293B1 KR 1020027018012 A KR1020027018012 A KR 1020027018012A KR 20027018012 A KR20027018012 A KR 20027018012A KR 100968293 B1 KR100968293 B1 KR 100968293B1
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- silicone
- parkinson
- disease
- rotigotine
- transdermal
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- 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
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- 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
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7069—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
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- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
Abstract
Description
패치 크기 | 로티고틴의 양 | 위약 치료와 비교한 UPDRS의 개선 | p(단측) |
10 ㎠ | 4.5 ㎎ | - 2.418 | 0.0393 |
20 ㎠ | 9.0 ㎎ | - 3.123 | 0.0063 |
30 ㎠ | 13.5 ㎎ | - 4.909 | 0.0000 |
40 ㎠ | 18.0 ㎎ | - 5.035 | 0.0000 |
조성물 성분 | 양 (㎎) |
로티고틴 염기 | 9.00 |
폴리비닐피롤리돈 | 2.00 |
실리콘 BIO-PSA™ Q7-4301 | 44.47 |
실리콘 BIO-PSA™ Q7-4201 | 44.46 |
아스코르빌 팔미테이트 | 0.02 |
DL-알파 토코페롤 | 0.05 |
메타중아황산나트륨 | 0.0006 |
매트릭스 피복중량 | 50 g/㎠ |
패치 크기 | 로티고틴의 양 | 11주일 째에 위약 치료에 대비한 평균 총 UPDRS II+III에 있어서의 개선 | p(단측) |
10 ㎠ | 4.5 ㎎ | - 2.148 | 0.0393 |
20 ㎠ | 9.0 ㎎ | - 3.123 | 0.0063 |
30 ㎠ | 13.5 ㎎ | - 4.909 | 0.0000 |
40 ㎠ | 18.0 ㎎ | - 5.035 | 0.0000 |
Claims (14)
- 하루에 한번 7주일(weeks) 또는 그 이상 동안 투여후, 단일화된 파킨슨병(Unified Parkinson's Disease) 등급 스케일(Rating Scale)(UPDRS) 파트(parts) II 및 III에 따라 측정한 것으로 위약 치료시(placebo treatment)와 비교하여 2 유니트(units) 또는 그 이상의 인간 파킨슨 환자(Human Parkinson Patient)의 상태를 개선시키는 항-파킨슨 약제(anti-parkinson medicament)의 제조를 위한,면적(area) 10 ~ 40 ㎠를 가지며 활성성분으로 로티고틴 0.1 ~ 3.15 ㎎/㎠를 함유하고, 고점착성 실리콘 압력 민감 접착제(high tack silicone pressure sensitive adhesive)인 BIO-PSA-Q7-4301(점도 500 내지 1600 mPas)과 중점착성 실리콘 압력 민감 접착제(medium tack silicone pressure sensitive adhesive)인 BIO-PSA-Q7-4201(점도 450 내지 1100 mPas)의 혼합물을 함유하는 것을 특징으로 하는 실리콘-기재 경피제제(silincone-based transdermal therapeutic system).
- 삭제
- 제 1 항에 있어서,그 실리콘-기재 경피제제는 가용화제(solubilizer)를 추가로 함유하는 것을 특징으로 하는 실리콘-기재 경피제제.
- 제 3 항에 있어서,그 가용화제(solubilizer)는 폴리비닐피롤리돈(polyvinylpyrrolidone)인 것을 특징으로 하는 실리콘-기재 경피제제.
- 제 1 항에 있어서,그 실리콘-기재 경피제제에는 무기 실리케이트(inorganic silicates) 1 wt% 미만을 함유하는 것을 특징으로 하는 실리콘-기재 경피제제.
- 제 5 항에 있어서,그 실리콘-기재 경피제제는 무기 실리케이트를 함유하지 않는 것을 특징으로 하는 실리콘-기재 경피제제.
- 제 1항에 있어서,그 실리콘-기재 경피제제는 면적(area) 10 ~ 30 ㎠를 가진 것을 특징을 하는 실리콘-기재 경피제제.
- 제 1 항에 있어서,그 실리콘-기재 경피제제에는 로티고틴(rotigotine) 0.1 ~ 1.5 ㎎/㎠을 함유하는 것을 특징으로 하는 실리콘-기재 경피제제.
- 제 1 항에 있어서,그 실리콘-기재 경피제제는 면적 10 ~ 30 ㎠와, 접착성 실리콘-기재 매트릭스(adhesive silicone-based matrix) 중에 로티고틴 함량 0.4 ~ 0.5 ㎎/㎠를 가진 하나의 패치(patch)인 것을 특징으로 하는 실리콘-기재 경피제제.
- 삭제
- 고점착성 실리콘 압력 민감 접착제(high tack silicone pressure sensitive adhesive)인 BIO-PSA-Q7-4301(점도 500 내지 1600 mPas)과 중점착성 실리콘 압력 민감 접착제(medium tack silicone pressure sensitive adhesive)인 BIO-PSA-Q7-4201(점도 450 내지 1100 mPas)의 아민-내성 실리콘 접착제의 혼합물을 함유하는 매트릭스(matrix) 중에, 활성성분으로서 로티고틴 0.4 ~ 0.5 ㎎/㎠를 함유하며, 크기(size) 10 ~ 30 ㎠를 갖는 파킨슨병 치료를 위한 경피제제(transdermal therapeutic system).
- 제 11 항에 있어서,무기 실리케이트 1 wt% 미만을 함유하는 것을 특징으로 하는 경피제제.
- 제 11 항에 있어서,추가로 하나의 가용화제(solubilizer)를 함유하는 것을 특징으로 하는 경피제제.
- 제 13 항에 있어서,그 가용화제는 폴리비닐피롤리돈인 것을 특징으로 하는 경피제제.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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DE01111110.1 | 2001-05-08 | ||
EP01111110A EP1256340B1 (en) | 2001-05-08 | 2001-05-08 | Improved transdermal therapeutic system for the treatment of Parkinson's disease |
PCT/EP2002/004975 WO2002089777A1 (en) | 2001-05-08 | 2002-05-06 | Improved transdermal therapeutic system for the treatment of parkinson's disese |
Publications (2)
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KR20030025941A KR20030025941A (ko) | 2003-03-29 |
KR100968293B1 true KR100968293B1 (ko) | 2010-07-07 |
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KR1020027018012A KR100968293B1 (ko) | 2001-05-08 | 2002-05-06 | 파킨슨병의 치료를 위한 개선된 경피제제 |
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EP (3) | EP1325742A1 (ko) |
JP (1) | JP2004528359A (ko) |
KR (1) | KR100968293B1 (ko) |
CN (1) | CN100457095C (ko) |
AT (2) | ATE246919T1 (ko) |
AU (1) | AU2002310805B8 (ko) |
CY (1) | CY1111880T1 (ko) |
DE (2) | DE60100595T2 (ko) |
DK (2) | DK1256340T3 (ko) |
ES (2) | ES2203563T3 (ko) |
HK (2) | HK1049448B (ko) |
HU (1) | HU229353B1 (ko) |
PT (2) | PT1256340E (ko) |
RU (1) | RU2273477C2 (ko) |
SI (1) | SI1256340T1 (ko) |
WO (1) | WO2002089777A1 (ko) |
ZA (1) | ZA200209980B (ko) |
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