KR950702436A - 가교 결합 양이온성 중합체 및 알콜실화 에테르를 함유하는 국소용 약학 조성물(pharmaceutical composition for topical use containing a crosslinked cationic polymer and an alkoxylated ether) - Google Patents

가교 결합 양이온성 중합체 및 알콜실화 에테르를 함유하는 국소용 약학 조성물(pharmaceutical composition for topical use containing a crosslinked cationic polymer and an alkoxylated ether) Download PDF

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KR950702436A
KR950702436A KR1019950700366A KR19950700366A KR950702436A KR 950702436 A KR950702436 A KR 950702436A KR 1019950700366 A KR1019950700366 A KR 1019950700366A KR 19950700366 A KR19950700366 A KR 19950700366A KR 950702436 A KR950702436 A KR 950702436A
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acid
agent
hydrochloride
mixtures
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크리스틴 볼륨 로버타
엔델 덱크너 죠지
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자코부스 코르넬리스 라세르
더 프록터 앤 갬블 캄파니
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    • A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
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Abstract

본 발명은 안전하고 유효한 양의 약학 활성물질, 약 0.1% 내지 약 10.0%의 고분자량 양이온성 중합체, 약 0.05% 내지 약 5%의 고 HLB 비이온성 계면활성제 및 약 0.1% 내지 약 25%의 알콕실화 에테르를 포함하는 국소 치료용 약학 조성물에 관한 것이다. 보다 바람직한 구현 예에 의하면, 본 조성물은 약 0.01% 내지 약 5%의 저 HLB 비독성 계면활성제를 포함한다.

Description

가교 결합 양이온성 중합체 및 알콜실화 에테르를 함유하는 국소용 약학 조성물(PHARMACEUTICAL COMPOSITION FOR TOPICAL USE CONTAINING A CROSSLINKED CATIONIC POLYMER AND AN ALKOXYLATED ETHER)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. 하기 성분을 호함하는 피부 투과성이 향상된 국소 치료용 약학 조성물: (a) 안전하고 유효한 양의 약학적 활성물질; (b) 가교 결합체를 함유하는 고분자량의, 하기 식의 가교 결합된 양이온성 중합체 0.1% 내지 10.0%;
    (A)l(B)m(C)c
    [여기에서, (A)는 디알킬아미노알킬 아크릴레이트 단량체 또는 이의 4급 암모늄 또는 산부가염이고, (B)는 디알킬아미노알킬 메타크릴레이트 단량체 또는 이의 4급 암모늄 또는 산부가염이고, (C)는 아크릴 아미드이고, l은 0이상의 정수이며, m은 1 이상의 정수이며, n은 0이상의 정수이다]; (c) 고 HLB 비이온성 계면 활성제 0.05% 내지 5% 및 (d) 하기식의 알콕실화 에테로 0.1% 내지 25%
    [여기에서, R은 C1~C18, 바람직하게는 C1~C10, 가장 바람직하게는 C1~C5의 직쇄 또는 축쇄이고, X는 메틸 또는 에틸이며, n은 약 5~약 20의 평균이다].
  2. 제1항에 있어서, 가교제가 메틸렌 비스 아크릴아미드, 에틸렌 글리콜 디-(메트) 아크릴레이트, 디-(메트)아크릴아미드, 시아노 메틸아크릴레이트, 비닐옥시에틸아크릴레이트, 비닐옥시에틸메타크릴레이트, 알릴펜타에리트리톨, 트리메티롤프로판 디알릴에테르, 알릴수크로스, 부타디엔, 이소프렌, 디비닐벤젠, 디비닐나프탈렌 및 알릴아크릴레이트 및 이의 혼합물로 이루어진 군으로 부터 선택되고, 바람직하게는 비스아크릴 아미드인 조성물.
  3. 제2항에 있어서, 8 내지 22개의 탄소를 지니고, 6 내지 30개의 에틸렌 옥시드기를 지닌 에톡실화 알콜로 부터 비이온성 계면활성제를 선택하고, 바람직하게는, 세테쓰-10, 스테아레쓰-21 및 이의 혼합물로 부터 고 HLB 비이온성 계면활성제를 선택하며, PPG-14 부틸 에테르, PPG-15 스테아릴 에테르 및 이의 혼합물로 구성된 군에서 알콕실화에테르를 선택함을 특징으로 하는 조성물.
  4. 제3항에 있어서, 항좌창제, 주름방지제, 피부 위축 방지제, 비스테로이드계 항염증제, 스테로이드께 항염증제, 태양없는 선탠제, 햇빛 차단제, 상처 치료제, 피부 표백제 또는 광택제, 항히스타민제, 진해제, 진양제, 항콜린 작용제, 진토제 및 진구토제, 식욕억제제, 중추신경 자극제, 항부정맥제, β-아드레날린 작동 차단제, 강심제, 항고혈압제, 이뇨제, 혈관확장제, 혈관수축제, 항궤양제, 마취제, 항우울증제, 신경안정제 및 진정제, 항정신병제, 항생제, 항종양제, 항말라리아제, 근이완제, 항경련제, 지사제 및 골 화성제 및 이의 혼합물로 구성된 군에서 약학적 활성물질을 선택하고, 바람직하게는, 항히스타민제가 말레산 클로르페니르아민, 탄닌산 클로르페니르아민, 염산 트리프롤리딘, 옥살산 트리프롤리딘, 염산 디페니르아민, 아스코르브산 디페니르아민, 시트르산 디페니르아민, 숙신산 독실아민, 말레산 피릴아민, 염산 피릴아민, 탄닌산 피릴아민, 타르타르산 페닌다민, 염산 프로메타진, 염산 시프로헵타딘, 말레산 아자타딘, 푸마르산 클레마스틴, 말레산 카르비녹사민, 염산 카르비녹사민, 염산 트리펠렌아민, 시트르산 트리펠렌아민, 말레산 데스클로르레니르아민, 말레산 브롬 페니르아민 및 염산 클로르시클리진 및 이의 혼합물로 구성된 군에서 선택되고; 진해제가 브롬화수소산 덱스트 로메토르판, 시트르산 카르베타펜탄, 인산 코데인 및 염산 N-옥시드 및 이의 혼합물로 구성된 군에서 선택되고; 항콜린 작용제가 브롬화수소산스코플라민, 염산 스코플라민, 황산 아트로핀, 무카트산 아트로핀, 브롬화수소산 호마트로핀 및 염산 호마트로핀 및 이의 혼합물로 구성된 군에서 선택되고; 진토제 및 진구토제가 염산시클리진, 염산 메클리진, 염산 클로르프로마진 및 말레산 클로르프로마진 및 이의 혼합물로 구성된 군에서 선택되고; 식욕 억제제가 염산 벤즈페타민, 염산 페테르민, 염산 클로르펜테르민 및 염산 펜플루라민 및 이의 혼합물로 구성된 군에서 선택되고; 항생제가 β-락탐 약제, 퀴놀론 약제, 시프로플록사신, 노르프록사신, 테트라사이클린, 에리트로마이신, 헥사미딘 이세티오네이트, 트리클로산, 독시사이클린, 카프레오마이신, 클로르헥시딘, 크로르 테트라사이클린, 옥시테트라사이클린, 클린다마이신, 에탐부톨, 메트로니다졸, 펜타미딘, 젠타디신, 카나마이신, 리네오마이신, 메타사이클린, 메테나민, 미노사이클린, 네오마이신, 네틸미신, 파로모마이신, 스트렙토마이신, 토부라마이신, 미토나졸 및 아만파딘의 약학적으로 허용 가능한 염 및 이의 혼합물로 구성된 군에서 선택되고; 항부정맥제가 염산 프로프라눌롤, 염산 프로카인아미드, 황산 퀴니딘 및 글루콘산 퀴니딘 및 이의 혼합물로 이루어진 군에서 선택되고; 항고혈압제가 말레산 에날라프릴, 염산 클로니딘, 염산 히드라라진 및 황산 히드라라진 및 이의 혼합물로 구성된 군에서 선택되고; 마취제 또는 진양제가 염산 리도카인, 염산 부피바카인, 염산 클로르프로카인, 염산 디부카인, 염산 에티도카인, 염산 메피바카인, 염산 테트라카인, 염산 디클로닌 및 염산 헥실카인 및 이의 혼합물로 구성된 군에서 선택되고; 골활성제가 6-아미노-1-히드록시헥산-1, 1-디포스폰산, 3-아미노-1-히드록시-프로판-1, 1-디포스폰산, 옥타히드로-1-피리딘-6, 6-디포스폰산, 2-(2′-피페리디닐) 에탄-1, 1-디포스폰산; 2-(3′-피페리디닐)-에탄-1, 1-디포스폰산; 2-(2′-피페리디닐)-1-히드록시-에탄-1, 1-디포스폰산; 2-(3′-피vp디닐-1-히드록시-에탄-1, 1-디포스폰산; N-(2′-(3′-메틸)-피페리디닐리덴)-아미노메탄 디포스폰산; N-(2′-(1′, 3′-디아지닐리덴)) 아미노메탄 디포스폰산; 및 N-(2-(3-메틸피페리디닐리덴))-아미노메탄포스포노메틸 메스핀산 또는 이의 에스테르 및 이의 혼합물로 구성된 군에서 선택되고; 비스테로이드계 항염증제가 프로피온산 유도체, 아세트산 유도체, 펜암산 유도체, 비페닐 카르복실산 유도체 및 옥시캄 및 이의 혼합물로 구성된 군에서 선택되고; 비스테로이드계 항염증제가 아스피린, 아세트아미노펜, 이부프로펜, 나프록센, 벤옥사프로펜, 플루르비프로펜, 페노프로펜, 펜부펜, 케토프로펜, 인도프로펜, 피르프로펜, 카프로펜, 옥사프로진, 프라토프로펜, 미로프로펜, 티옥사프로펜, 스프로펜, 알미노프로펜, 티아프로펜산, 플루프로펜 및 불클록시산 및 이의 혼합물로 구성된 군에서 선택됨을 특징으로 하는 조성물.
  5. 제3항에 있어서, 항좌창제가 살리실산, 황, 레소르시놀, N-아세틸시스테인, 옥토피록스, 레티노산 및 이의 유도체, 벤조일 퍼옥시드, 에리트로마이신, 아연, 테트라사이클린, 아젤라산 및 이의 유도체, 페녹시 에탄올 및 페녹시 프로포놀, 에틸아세테이트, 클린다마이신 및 메클로사이클린, 플라비노이드, 락트산, 글리콜산, 피루브산, 요소, 황산심놀 및 이의 유도체, 데옥시콜레이트 및 콜레이트 및 이의 혼합물로 구성된 군에서 선택되고, 항 주름제 또는 피부 위축 방지제는 글리콜산, 락트산, 살리실산 및 이의 혼합물로 구성된 군에서 선택됨을 특징으로 하는 조성물.
  6. 제3항에 있어서, 약학 활성제가 살리실산, 글리콜산, 락트산 및 이의 혼합물로 구성된 군에서 선택됨을 특징으로 하는 조성물.
  7. 제5항에 있어서, 양이온성 중합체 중의 (C)의 양이 50몰% 내지 90몰%이고; 바람직하게는 양이온성 중합체의 l이 0이며 (B) : (C)의 비가 45:55 내지 55:45이고, 보다 바람직하게는, 양이온성 중합체에서 1 및 n이 모두 0인 조성물.
  8. 제7항에 있어서, 휘발성 실리콘 오일, 비휘발성 실리콘 오일, 다측쇄 탄화수소 및 이의 혼합물로 구성된 군에서 선택된 피부연화제 1% 내지 10% 및 글리세린 3% 내지 5%를 추가로 포함하는 조성물.
  9. 제3항에 있어서, 활성 약물이 디히드록시아세톤, 인돌 유도체 및 이의 혼합물로 구성된 군에서 선택된 태양없는 선탠제이고, 바람직하게는 조성물이 2-에틸헥실 p-메톡시신나메이트, 2-에틸헥실 N, N-디메틸-p-아미노벤조에이트, p-아미노벤조산, 2-페닐벤즈이미다졸-5-술폰산, 옥토크릴렌, 옥시벤존, 살리실산 호모멘틸, 살리실산 옥틸, 4,4′-메톡시-t-부틸디벤조일메탄, 4-이소프로필 디벤조일메탄, 3-벤질리덴 캄포, 3-(4-메틸벤질리덴) 캄포, 이산화티타늄, 산화아연, 실리카, 산화철 및 이의 혼합물로 구성된 군에서 선택된 햇빛 차단제를 추가로 포함하는 조성물.
  10. 하기 성분을 호함하는 피부 투과성이 향상된 국소 치료용 약학 조성물; (a) 안전하고 유효한 양의 약학적 활성물질; (b) 가교 결합체를 함유하는 고분자량의, 하기 식의 가교 결합된 양이온성 중합체 0.1% 내지 10.0%;
    (A)l(B)m(C)c
    [여기에서, (A)는 디알킬아미노알킬 아크릴레이트 단량체 또는 이의 4급 암모늄 또는 산부가염이고, (B)는 디알킬아미노알킬 메타크릴레이트 단량체 또는 이의 4급 암모늄 또는 산부가염이고, (C)는 아크릴 아미드이고, l은 0이상의 정수이며, m은 1 이상의 정수이며, n은 0이상의 정수이다]; (c) 고 HLB 비이온성 계면 활성제 0.05% 내지 5%, (d) 저 HLB 비이온성 계면활성제 0.01% 내지 5%; 및 (e) 하기식의 알콕실화 에테로 0.1% 내지 25%
    [여기에서, R은 C1~C18, 바람직하게는 C1~C10, 가장 바람직하게는 C1~C5의 직쇄 또는 축쇄이고, X는 메틸 또는 에틸이며, n은 약 5~약 20의 평균이다].
  11. 제10항에 있어서, 가교제가 메틸렌 비스 아크릴아미드, 에틸렌 글리콜 디-(메트) 아크릴레이트, 디-(메트) 아크릴아미드, 시아노 메틸아크릴레이트, 비닐옥시에틸아크릴레이트, 비닐옥시에틸메타크릴레이트, 알릴펜타에리트리톨, 트리메티롤프로판 디알릴에테르, 알릴수크로스, 부타디엔, 이소프렌, 디비닐벤젠, 디비닐나프탈렌 및 알릴아크릴레이트 및 이의 혼합물로 이루어진 군으로 부터 선택되고, 바람직하게는 가교제가 비스아크릴아미드인 조성물.
  12. 제11항에 있어서, 8 내지 22개의 탄소를 지니고, 6 내지 30개의 에틸렌 옥시드기를 지닌 에톡실화 알콜로 부터 비이온성 계면활성제를 선택하고, 바람직하게는, 세테쓰-10, 스테아레쓰-21 및 이의 혼합물로 부터 고 HLB 비이온성 계면활성제를 선택하며, PPG-14 부틸 에테르, PPG-15 스테아릴 에테르 및 이의 혼합물로 구성된 군에서 알콕실화 에테르를 선택함을 특징으로 하는 조성물.
  13. 제12항에 있어서, 8 내지 22개의 탄소를 지니고, 1 내지 5개의 에틸렌 옥시드기를 지닌 에톡실화 알콜로 부터 저 HLB 비이온성 계면활성제를 선택하고, 바람직하게는, 스테아레쓰-2, 세테쓰-2, 라우레쓰-2, 올레쓰-2 및 이의 혼합물로 구성된 군에서 저 HLB 비이온성 계면활성제를 선택하고; 바람직하게는 저 HLB 비이온성 계면활성제 스테아레쓰-2임을 특징으로 하는 조성물.
  14. 제13항에 있어서, 항좌창제, 주름방지제, 피부 위축 방지제, 비스테로이드계 항염증제 스테로이드께 항염증제, 태양없는 선탠제, 햇빛 차단제, 상처 치료제, 피부 표백제 또는 광택제, 항히스타민제, 진해제, 진양제, 항콜린 작용제, 진토제 및 진구토제, 식욕억제제, 중추신경 자극제, 항부정맥제, β-아드레날린 작동 차단제, 강심제, 항고혈압제, 이뇨제, 혈관확장제, 혈관수축제, 항궤양제, 마취제, 항우울증제, 신경안정제 및 진정제, 항정신병제, 항생제, 항종양제, 항말라리아제, 근이완제, 항경련제, 지사제 및 골 화성제 및 이의 혼합물로 구성된 군에서 약학적 활성물질을 선택함을 특징으로 하는 조성물.
  15. 제13항에 있어서, 항좌창제가 살리실산, 황, 레소르시놀, N-아세틸시스테인, 옥토피록스, 레티노산 및 이의 유도체, 벤조일 퍼옥시드, 에리트로마이신, 아연, 테트라사이클린, 아젤라산 및 이의 유도체, 페녹시 에탄올 및 페녹시 프로포놀, 에틸아세테이트, 클린다마이신 및 메클로사이클린, 플라비노이드, 락트산, 글리콜산, 피루브산, 요소, 황산심놀 및 이의 유도체, 데옥시콜레이트 및 콜레이트 및 이의 혼합물로 구성된 군에서 선택되고, 항 주름제 또는 피부 위축 방지제가 글리콜산, 락트산, 살리실산 및 이의 혼합물로 구성된 군에서 선택됨을 특징으로 하는 조성물.
  16. 제13항에 있어서, 약학 활성제가 살리실산, 글리콜산, 락트산 및 이의 혼합물로 구성된 군에서 선택됨을 특징으로 하는 조성물.
  17. 제13항에 있어서, 양이온성 중합체 중의 (C)의 양이 50몰% 내지 90몰%이고; 바람직하게는 양이온성 중합체의 l이 0이며 (B) : (C)의 비가 45:55 내지 55:45이고, 보다 바람직하게는, 양이온성 중합체에서 1 및 n이 모두 0인 조성물.
  18. 제17항에 있어서, 휘발성 실리콘 오일, 비휘발성 실리콘 오일, 다측쇄 탄화수소 및 이의 혼합물로 구성된 군에서 선택된 피부연화제 1% 내지 10% 및 글리세린 3% 내지 5%를 추가로 포함하는 조성물.
  19. 제13항에 있어서, 활성 약물이 디히드록시아세톤, 인돌 유도체 및 이의 혼합물로 구성된 군에서 선택된 태양없는 선탠제이고, 바람직하게는 조성물이 2-에틸헥실 p-메톡시신나메이트, 2-에틸헥실 N, N-디메틸-p-아미노벤조에이트, p-아미노벤조산, 2-페닐벤즈이미다졸-5-술폰산, 옥토크릴렌, 옥시벤존, 살리실산 호모멘틸, 살리실산 옥틸, 4,4′-메톡시-t-부티디벤조일메탄, 4-이소프로필 디벤조일메탄, 3-벤질리덴 캄포, 3-(4-메틸벤질리덴) 캄포, 이산화티타늄, 산화아연, 실리카, 산화철 및 이의 혼합물로 구성된 군에서 선택된 햇빛 차단제를 추가로 포함하는 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950700366A 1992-07-28 1993-07-12 가교 결합 양이온성 중합체 및 알콜실화 에테르를 함유하는 국소용 약학 조성물(pharmaceutical composition for topical use containing a crosslinked cationic polymer and an alkoxylated ether) KR950702436A (ko)

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US92093792A 1992-07-28 1992-07-28
US07/920937 1992-07-28
US95052792A 1992-09-25 1992-09-25
US07/950527 1992-09-25
US3321193A 1993-03-18 1993-03-18
US08/033211 1993-03-18
US7997793A 1993-06-25 1993-06-25
US08/079977 1993-06-25
PCT/US1993/006542 WO1994002176A1 (en) 1992-07-28 1993-07-12 Pharmaceutical composition for topical use containing a crosslinked cationic polymer and an alkoxylated ether

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BR9306816A (pt) 1998-12-08
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AU4673993A (en) 1994-02-14
JP3567990B2 (ja) 2004-09-22
FI950368A0 (fi) 1995-01-27
US5614178A (en) 1997-03-25
WO1994002176A1 (en) 1994-02-03
DE69310518D1 (de) 1997-06-12
DE69310518T2 (de) 1997-10-02
NO950291D0 (no) 1995-01-26
FI950368A (fi) 1995-03-10
NO950291L (no) 1995-03-27
ES2101330T3 (es) 1997-07-01
CA2141192A1 (en) 1994-02-03
CA2141192C (en) 1999-02-02
JPH07509243A (ja) 1995-10-12
CN1072965C (zh) 2001-10-17
ATE152630T1 (de) 1997-05-15
CN1091317A (zh) 1994-08-31

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