KR100802625B1 - 생물학적으로 활성인 친수성 화합물의 비경구적 투여를위한 서방성 약제학적 조성물 - Google Patents
생물학적으로 활성인 친수성 화합물의 비경구적 투여를위한 서방성 약제학적 조성물 Download PDFInfo
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- KR100802625B1 KR100802625B1 KR1020027015828A KR20027015828A KR100802625B1 KR 100802625 B1 KR100802625 B1 KR 100802625B1 KR 1020027015828 A KR1020027015828 A KR 1020027015828A KR 20027015828 A KR20027015828 A KR 20027015828A KR 100802625 B1 KR100802625 B1 KR 100802625B1
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- microemulsion
- biologically active
- active compound
- microemulsions
- acetate
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Abstract
Description
화합물 | 양 (mg) | 부종의 존재 (평균 등급*) | 궤양의 존재 | ||||
48시간 | 7일 | 14일 | 48시간 | 7일 | 14일 | ||
마이크로에멀젼 A(1) | 125㎕ | 2 | 2 | 1 | 무 | 무 | 무 |
마이크로에멀젼 A(1) | 500㎕ | 3 | 3 | 2.5 | 무 | 무 | 무 |
마이크로에멀젼 A(2) | 125㎕ | 3 | 3 | 3 | 유 | 유 | 유 |
샘플채취 시간 | 0.5시간 | 24시간 | 4일 | 6일 | 8일 |
옥트레오타이드 (ng/ml) | 539 | 40.2 | 62.5 | 4.5 | 7.6 |
56일째에 체중 및 생식기 무게(g) | ||||
체중 | 고환 | 전립선 | 정낭 | |
대조군 | 645±34 | 3.73±0.16 | 0.82±0.04 | 1.96±0.09 |
실험군 | 608±35 | 1.94±0.42 | 0.35±0.14 | 0.55±0.16 |
(p<0.01) | (p<0.5) | (p<0.05) |
Claims (20)
- a) 치료학적으로 활성이 있는 친수성 화합물을 함유하는 20 w/w% 이하의 친수성 수성(aqueous) 내상;b) C8-C20 포화 또는 불포화 카르복실산과 C2-C8 선형 또는 분지형 알콜 잔기의 에스테르, 또는 C8-C20 지방산의 모노, 디- 및 트리글리세라이드로부터 선택된 30 내지 98 w/w%의 소수성 외상; 및c) C4-C20의 포화 또는 불포화 카르복실산 잔기를 함유하고 포스포에스테르 모이어티로서 콜린, 에탄올아민, 세린, 글레세롤 잔기를 갖는 천연 또는 합성 글리세로인지질로부터 선택된 계면활성제와 C8-C20 지방산 또는 C2-C12 알콜로부터 선택된 공계면활성제의 혼합물로서 계면활성제/공계면활성제의 중량 비율이 2 이상인 혼합물 50 w/w% 이하로 구성되고,친수성 또는 적절한 유도체화 반응에 의해 친수성화된 생물학적 활성 화합물의 비경구 투여에 적절하고, 함유된 활성 화합물의 지속적 방출을 제공하는, 안정하고, 생물학적으로 적합하며 우수한 내성(well tolerated)의 w/o 마이크로에멀젼.
- 삭제
- 제 1 항에 있어서, 상기 친수성, 생물학적 활성 화합물이 펩티드, 단백질, 올리고- 또는 폴리사카라이드인 것을 특징으로 하는 마이크로에멀젼.
- 제 3 항에 있어서, 상기 생물학적 활성 화합물이 펩티드인 것을 특징으로 하는 마이크로에멀젼.
- 제 4 항에 있어서, 상기 생물학적 활성 화합물이 LHRH 호르몬 펩티드 유사체인 것을 특징으로 하는 마이크로에멀젼.
- 제 5 항에 있어서, 상기 생물학적으로 활성인 화합물이 류프롤라이드(Leuprolide) 아세테이트, 고세렐린(Goserelin), 트립토렐린(Triptorelin), 나파렐린(Nafarelin), 히스트렐린(Histrelin), 세트로렐릭스(Cetrorelix), 또는 그들의 아세테이트염인 것을 특징으로 하는 마이크로에멀젼.
- 삭제
- 제 5 항에 있어서, 상기 생물학적 활성 화합물은 소마토스타틴, 옥트레오타이드(Octreotide), 또는 란레오타이드(Lanreotide)인 것을 특징으로 하는 마이크로에멀젼.
- 제 3 항에 있어서, 상기 생물학적 활성 화합물은 올리고- 또는 폴리사카라이드인 것을 특징으로 하는 마이크로에멀젼.
- 제 9 항에 있어서, 상기 생물학적 활성 화합물이 비분획 헤파린 또는 저분자량 헤파린인 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 생물학적 활성화합물을 함유하는 수상은 pH 4.5 내지 7.5인 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 생물학적 활성화합물을 함유하는 수상은 pH 5 내지 7인 것을 특징으로 하는 마이크로에멀젼.
- 제 11 항에 있어서, 상기 pH는 천연 아미노산의 첨가에 의해 조정되는 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 계면활성제/공계면활성제의 중량 비율이 3.5 이상인 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 계면활성제 및 공계면활성제의 함량은 35 w/w% 미만인 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 마이크로에멀젼은 1 회 투여 후 30 일 이상 테스토스테론의 생성을 억제하며 테스토스테론의 농도를 투여 후 48시간 후에 감소시키는 약제를 제조하기 위해, 류프롤라이드, 고세렐린, 트립토렐린, 나파렐린 아세테이트, 히스트렐린, 세트로렐릭스, 또는 그의 아세테이트염, 또는 다른 LHRH 유사체를 포함하는 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 마이크로에멀젼은 8 일 이상 성장 호르몬 생성을 억제하기 위한 약제를 제조하기 위해, 옥트레오타이드 또는 그의 유사체를 포함하는 것을 특징으로 하는 마이크로에멀젼.
- 제 1 항에 있어서, 상기 마이크로에멀젼은 1 회 투여 후 지속적 방출을 갖는 약제를 제조하기 위해, 비분획 헤파린 또는 저분자량 헤파린을 함유하는 것을 특징으로 하는 마이크로에멀젼.
- 삭제
- 삭제
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Application Number | Priority Date | Filing Date | Title |
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IT2000MI001173A IT1318539B1 (it) | 2000-05-26 | 2000-05-26 | Composizioni farmaceutiche a rilascio prolungato per lasomministrazione parenterale di sostanze idrofile biologicamente |
ITMI2000A001173 | 2000-05-26 | ||
PCT/EP2001/005949 WO2001089479A2 (en) | 2000-05-26 | 2001-05-23 | Sustained release pharmaceutical compositions for parenteral administration of hydrophilic compounds |
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KR20030011856A KR20030011856A (ko) | 2003-02-11 |
KR100802625B1 true KR100802625B1 (ko) | 2008-02-13 |
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KR1020027015828A KR100802625B1 (ko) | 2000-05-26 | 2001-05-23 | 생물학적으로 활성인 친수성 화합물의 비경구적 투여를위한 서방성 약제학적 조성물 |
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US (1) | US7157099B2 (ko) |
EP (1) | EP1283700B1 (ko) |
JP (1) | JP4954423B2 (ko) |
KR (1) | KR100802625B1 (ko) |
CN (1) | CN100479856C (ko) |
AT (1) | ATE321533T1 (ko) |
AU (2) | AU8178601A (ko) |
BR (1) | BRPI0111016B8 (ko) |
CA (1) | CA2409854C (ko) |
CY (1) | CY1105262T1 (ko) |
CZ (1) | CZ302059B6 (ko) |
DE (1) | DE60118395T2 (ko) |
DK (1) | DK1283700T3 (ko) |
ES (1) | ES2257428T3 (ko) |
HR (1) | HRP20020929A2 (ko) |
HU (1) | HU228926B1 (ko) |
IL (1) | IL153011A0 (ko) |
IT (1) | IT1318539B1 (ko) |
MX (1) | MXPA02011539A (ko) |
NO (1) | NO334880B1 (ko) |
PL (1) | PL203354B1 (ko) |
PT (1) | PT1283700E (ko) |
RU (1) | RU2272615C2 (ko) |
SI (1) | SI1283700T1 (ko) |
SK (1) | SK16552002A3 (ko) |
WO (1) | WO2001089479A2 (ko) |
YU (1) | YU88202A (ko) |
ZA (1) | ZA200209520B (ko) |
Cited By (1)
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US10478470B2 (en) | 2014-07-28 | 2019-11-19 | Sk Chemicals Co., Ltd. | Pharmaceutical composition containing leuprolide and having both immediate and sustained release properties |
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US7658938B2 (en) | 1999-02-22 | 2010-02-09 | Merrion Reasearch III Limited | Solid oral dosage form containing an enhancer |
US8119159B2 (en) | 1999-02-22 | 2012-02-21 | Merrion Research Iii Limited | Solid oral dosage form containing an enhancer |
DK1787658T3 (da) | 2005-11-10 | 2012-06-25 | Chemi Spa | Formuleringer med forsinket frigørelse og indeholdende somatostatin-analoge væksthormoninhibitorer |
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