KR920019336A - 소화관 점막 부착성 매트릭스, 약제제 및 코우팅 조성물 - Google Patents
소화관 점막 부착성 매트릭스, 약제제 및 코우팅 조성물 Download PDFInfo
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Abstract
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Claims (35)
- 폴리글리세롤 지방산 에스테르 또는 지질 및 약효성분을 함유하는 매트릭스 입자의 적어도 표층 근방에서 물과 접촉하여 점성을 생성할 수 있는 점성물질이 분산되어 있는, 상온에서 고체인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 점성물질이 카르복실기 또는 그의 염을 함유하는 중합체, 셀룰로스 에테르, 분자량 200,000이상의 폴리에틸렌글리콜 및 천연점성물질로 이루어진 군으로부터 선택된 적어도 하나인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 점성물질이 아크릴산 중합체/ 및 또는 그의 염인 소화관 점막 부착성 매트릭스.
- 제2항에 있어서, 카르복실기 또는 그의 염을 함유하는 중합체가 그들의 구성단량체로서 아클릴산으로부터 수득될 수 있는 아크릴산 중합체 또는 그의 염인 소화관 점막 부착성 매트릭스.
- 제4항에 있어서, 아클릴산중합체 또는 그의 염이 각각 58.0~63.0중량%의 카르복실기를 포함하며 200,000~6,00,000의 분라량을 갖는 소화관 점막 부착성 매트릭스.
- 제2항에 있어서, 상기 셀룰로스에테르가 카르복시메틸셀룰로스 나트륨, 히드록시프로필메틸셀룰로스, 메틸셀룰로스 및 결정 셀룰로스-카르복시메틸셀룰로스 나트륨인소화관 점막 부착성 매트릭스.
- 제2항에 있어서, 천연 점성 물질이 점액질, 한천, 젤라틴, 펙틴, 카라기난(carrageenan), 알긴산 나트륨, 로커스트 빔 검(locust beam gum), 크산탄 검 및 트라가칸트 검(tragacanth gum), 아라비아 검, 키토산, 풀루란(pullulan) 및 왁시스타치(waxistarch)인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 점성물질의 함유량이 상기 매트릭스 입자의 전중량에 대하여 0.005~95중량%인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 폴리글릴세롤 지방산 에스테르가 하기 식(I)로 표시되는 폴리글리세롤과 포화 또는 불포화 고급 지방산의 에스테르인 소화관 점막 부착성 매트릭스.〔식중 n은 중합도를 나타내며, 2이상의 정수이다.〕
- 제9항에 있어서, n이 2~50인 소화관 점막 부착성 매트릭스.
- 제9항에 있어서, 상기 지방산이 탄소수 8~40의 포화 또는 불포화 고급 지방산인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 폴리글리세롤 지방산 에스테르가 베헨산 헥사(테트라)글리세리드, 스테아린산 모노(테트라) 글리세리드 스테아린산 펜타(테트라)글리세리드, 스테아린산 펜타(헥사)글리세리드, 스테아린산 세스퀴(헥사)글리세리드, 스테아린산 모노(테카(글리세리드 도는 그들의 혼합물인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 폴리그릴세롤 지방산 에스테르가 1~22의 HLB(hydrophile-lipophile balance)를 갖는 점막 부착성 매트리스.
- 제1항에 있어서, 상기 폴리글리세롤 지방산 에스테르의 융점이 15-80℃인 소화관 점막 부착성 매트리스.
- 제1항에 있어서, 상기 지질의 융점이 40-120℃인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 상기 지질이 C14~22의 포화 지방산 또는 그의 염, C16~22의 고급알콜, 지방산 글리세롤 에스테르, 오일류, 왁스류, 탄화수소 또는 인지질인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 약효성분이 항궤양제 또는 위염 치료제인 소화관 점낙 부착성 매트릭스.
- 제1항에 있어서, 상기 약효성분이 하기식(Ⅱ)으로 표시되는 화합물 또는 약리학적으로 허용되는 염인 소화관 점막 부착성 매트릭스.〔식중, R1은 수소원자, 알킬기, 할로겐원자, 시아노기, 카르복시기, 알콕시, 카르보닐기, 알콕시카르보닐알킬기, 카르보모일기, 카르바모일알킬기, 히드록시기, 알콕시기, 히드록시알킬기, 트리플루오로메틸기, 아실기, 카릅바모일옥시기, 니트로기, 아실옥시기, 아릴기, 아릴옥시기, 알킬티오기, 또는 알킬술피닐기를 나타내고; R2는 수소원자, 알킬기, 아실기, 알콕시카르보닐기, 카르바모일기, 알킬카르바모일기, 디알킬카르바모일기, 알킬카르보닐메틸기, 알콕시카르보닐메틸기 또는 알킬술포닐기를 나타내고; R3및 R5는 동일 또는 상이하며, 각기 수소원자, 알킬기, 알콕시기 또는 알콕시 알콕시기를 나타내고; R4는 수소원자, 알킬기, 불소화되어 있어도 좋은 알콕시기, 알콕시 알콕시기, 불소화되어 있어도 좋은 알케닐옥시기 또는 불소화되어 있어도 좋은 알키닐옥시기를 나타내고 m은 0 내지 4의 정수를 나타낸다.〕
- 제18항에 있어서, 상기 식(Ⅱ)으로 표시되는 화합물의 R1, R2및 R5가 수소원자이고, R3이 수소원자 또는 메틸기인 소화관 점막부착성 매트릭스.
- 제18항에 있어서, 상기 식(Ⅱ)으로 표시되는 화합물의 R4가 불소화된 C1~4의 알콕시기인 소화관 점막 부착성 매트릭스.
- 제18항에 있어서, 상기 식(Ⅱ)으로 표시되는 화합물의 R1이 5위치에서 치환된 수소원자, 불소원자, 메톡시기 또는 트리플루오로메틸기이고; R2가 수소원자이고; R3이 수소원자 또는 메틸기이고; R4가 불소화되어 있어도 좋은 C1~4알콕시기, 2-프로페닐옥시기 또는 알릴기이고; R5가 수소원자 또는 메틸기이고, m=1인 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 산성 약호성분과 함께 물에 대하여 불용 또는 난용의 고체 염기를 함유하는 소화관 점막 부착성 매트리스.
- 제1항에 있어서, 염기성 약효성분과 함께 장용성 중합체를 함유하는 소화관 점막 부착성 매트릭스.
- 제1항에 있어서, 매트릭스 입자에 있어서의 폴리글리세롤 지방산 에스테르 및/또는 상기 지질의 함유량이 상기 약효성분의 1중량부에 대하여 0.001~10000중량부인 소화관 점막 부착성 매트리스.
- 제1항에 있어서, 상기 식(I)으로 표시되는 폴리글리세롤(n은 2~50)과 탄소수 8 내지 40의 포화 또는 불포화 고급 지방산의 에스테르 및/또는 상기 지질과, 상기 약효성분과, 상기 점성물질을 함유하는 매트릭스 입자중에서, 상기 폴리그릴세롤 지방산 에스테르 및/또는 지질의 함유량이 약효성 분량 1중량부에 대하여 0.001~10,0000중량부이고, 상기 점성물질이 아크릴 산 중합체 및/또는 그의 염을 소화관 점막 부착성 매트리스.
- 제1항에 있어서, 상기 매트릭스의 융점이 30~120℃인 소화관 점막 부착성 매트릭스.
- 폴리글리세롤 지방산 에스테르 또는 지질 및 약효성분을 포함하는 매트릭스 입자로, 상기 입자는 물과의 접촉으로 점성을 생성하는 점성물질을 포함하는 코우팅 조성물로부터 형성되는 피복층을 갖는, 상온에서 고체인 소화관 점막 부착성 매트리스.
- 제27항에 있어서, 상기 피복층이 폴리글리세롤 지방산 에스테르, 지질, 장용성 중합체 및 수불용성 중합체로 이루어진 군으로부터 선택된 적어도 하나의 성분을 함유하는 소화관 점막 부착성 매트릭스.
- 제27항에 있어서, 상기 피복층 중의 점성물징의 함유량이 피복층 전량을 기준으로 0.005~100중량%인 소화관 점막 매트릭스.
- 제27항에 있어서, 상기 매트릭스 입자를 기준으로 상기 코우팅 조성물의 피복량이 0.1~100중량%인 소화관 점막 부착성 매트릭스.
- (1)폴리글리세롤 지방산 에스테르 또는 지질과 약효성분을 함유하는 매트릭스 입자의 적어도 표층 근방에서 물과 접촉하여 점성을 생성시킬수 있는 점성물질이 분산되어 있는 상온에서 고체인 소화관 점막 부착성 매트릭스 또는 (2)폴리글리세롤 지방산 에스테르 또는 지질과 약효성분을 함유하는 매트릭스 입자가 물과의 접촉으로 점성을 생성시키는 점성물질을 함유하는 코우팅 조성물로 피복되어 있는 상온에서 고체인 소화관 점막 부착성 매트리스를 함유하는 고형약제.
- 제31항에 있어서, 고형 약재의 투약형태가 세립제, 과립제, 환제, 상기 세립제 또는 과립제를 압축 성형한 정제 및 상기 세립제 또는 과립제를 캡슐에 충전하여 수득될 수 있는 캡슐제로 이루어진 군으로부터 선택된 고형약제.
- 적어도 물과 접촉하여 점성을 생성시키는 점성물질로 함유하는 코우팅 조성물.
- 제33항에 있어서, 폴리글리세롤 지방산 에스테트, 지질, 장용성 중합체 및 수불용성 중합체로 이루어진 군으로부터 선택된 적어도 하나의 성분을 함유하는 코우팅 조성물.
- 제33항에 있어서, 비휘발 물질을 기준으로, 상기 점성물질을 0.005~100중량%함유하는 코우팅 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
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JP22515591 | 1991-08-09 |
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US20220361552A1 (en) * | 2019-12-10 | 2022-11-17 | Tyler White | Particles Containing a Lipid Matrix Core and Active Ingredient |
WO2024075017A1 (en) | 2022-10-04 | 2024-04-11 | Zabirnyk Arsenii | Inhibition of aortic valve calcification |
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-
1992
- 1992-04-11 TW TW081102828A patent/TW209174B/zh active
- 1992-04-14 DE DE69217711T patent/DE69217711T2/de not_active Expired - Fee Related
- 1992-04-14 EP EP92303357A patent/EP0514008B1/en not_active Expired - Lifetime
- 1992-04-14 ES ES92303357T patent/ES2098447T3/es not_active Expired - Lifetime
- 1992-04-14 SG SG1996002366A patent/SG50480A1/en unknown
- 1992-04-14 AT AT92303357T patent/ATE149348T1/de not_active IP Right Cessation
- 1992-04-14 DK DK92303357.5T patent/DK0514008T3/da active
- 1992-04-15 JP JP12268192A patent/JP3272029B2/ja not_active Expired - Fee Related
- 1992-04-16 CA CA002066384A patent/CA2066384C/en not_active Expired - Fee Related
- 1992-04-18 KR KR1019920006554A patent/KR100217165B1/ko not_active IP Right Cessation
-
1995
- 1995-03-29 US US08/412,591 patent/US5576025A/en not_active Expired - Lifetime
-
1996
- 1996-08-20 US US08/697,166 patent/US5731006A/en not_active Expired - Fee Related
-
1997
- 1997-05-09 GR GR970401036T patent/GR3023383T3/el unknown
- 1997-12-18 US US08/993,314 patent/US6368635B1/en not_active Expired - Fee Related
-
2001
- 2001-05-11 JP JP2001141179A patent/JP4084000B2/ja not_active Expired - Fee Related
- 2001-05-11 JP JP2001141178A patent/JP2001354593A/ja active Pending
-
2002
- 2002-02-20 US US10/077,896 patent/US20020142041A1/en not_active Abandoned
-
2007
- 2007-07-09 JP JP2007179258A patent/JP2007246547A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
JP2001354550A (ja) | 2001-12-25 |
GR3023383T3 (en) | 1997-08-29 |
EP0514008B1 (en) | 1997-03-05 |
DK0514008T3 (da) | 1997-05-12 |
ATE149348T1 (de) | 1997-03-15 |
TW209174B (ko) | 1993-07-11 |
DE69217711T2 (de) | 1997-07-17 |
US20020142041A1 (en) | 2002-10-03 |
CA2066384C (en) | 2007-04-03 |
JPH05132416A (ja) | 1993-05-28 |
JP3272029B2 (ja) | 2002-04-08 |
JP4084000B2 (ja) | 2008-04-30 |
CA2066384A1 (en) | 1992-10-20 |
US6368635B1 (en) | 2002-04-09 |
JP2001354593A (ja) | 2001-12-25 |
EP0514008A1 (en) | 1992-11-19 |
SG50480A1 (en) | 1998-07-20 |
US5576025A (en) | 1996-11-19 |
DE69217711D1 (de) | 1997-04-10 |
KR100217165B1 (ko) | 1999-09-01 |
ES2098447T3 (es) | 1997-05-01 |
US5731006A (en) | 1998-03-24 |
JP2007246547A (ja) | 2007-09-27 |
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