KR960704579A - 옥시부티닌용 모노글리세리드/락테이트 에스테르 투과 촉진제(Monoglyceride/lactate Ester Permeation Enhancer for Oxybutynin) - Google Patents

옥시부티닌용 모노글리세리드/락테이트 에스테르 투과 촉진제(Monoglyceride/lactate Ester Permeation Enhancer for Oxybutynin)

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KR960704579A
KR960704579A KR1019960701611A KR19960701611A KR960704579A KR 960704579 A KR960704579 A KR 960704579A KR 1019960701611 A KR1019960701611 A KR 1019960701611A KR 19960701611 A KR19960701611 A KR 19960701611A KR 960704579 A KR960704579 A KR 960704579A
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lactate
reservoir
mixture
skin
oxybutynin
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은 수 이
타일러 와따나베
로버트 엠. 게일
테리 엘. 불코쓰
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에드워드 엘. 만델
앨자 코포레이션
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Abstract

특정 농도로 존재하는 투여될 옥시부티닌의 치료 유효량; 및 모노글리세리드 또는 모노글리세리드의 혼합물, 및 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 투과-촉진 혼합물의 조합으로 이루어지는, 체표면이나 막을 통한 투과에 의해 옥시부티닌을 투여하기 위한 체표면 또는 막에 사용되는 물질의 조성물.

Description

옥시부티닌용 모노글리세리드/락테이트 에스테르 투과 촉진제(Monoglyceride/Lactate Ester Permeation Enhancer for Oxybutynin)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (47)

  1. (a) 투여될 옥시부티닌의 치료 유효량 및 (b) (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 투과-촉진 혼합물의 조합으로 이루어지는 체표면이나 막을 통한 투과에 의해 옥시부티닌을 투여하기 위한 체표면 또는 막에 작용하는 물질의 조성물.
  2. 제1항에 있어서, 모노글리세리드 또는 모노글리세리드의 혼합물이 조성물의 20중량%를 이루며, 락테이트 에스테르 12중량%를 이루는 것인 조성물.
  3. 제1항에 있어서, 락테이트 에스테르가 라우릴 락테이트인 조성물.
  4. 제1항에 있어서, 락테이트 에스테르가 에틸 락테이트인 조성물.
  5. 제1항에 있어서, 락테이트 에스테르가 미리스틸 락테이트인 조성물.
  6. 제1항에 있어서, 락테이트 에스테르가 세틸 락테이트인 조성물.
  7. 제1항에 있어서, 락테이트 에스테르의 혼합물이 에틸 락테이트 및 라우릴 락테이트인 조성물.
  8. 제3 내지 7항 중 어느 한 항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트인 조성물.
  9. 제8항에 있어서, 글리세롤 모노라우레이트 및 락테이트 에스테르가 각각 조성물의 20중량% 및 12중량%를 이루는 것인 조성물.
  10. (a) 치료 유효량의 옥시부티닌 및 (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 피부 투과-촉진량의 투과 혼합물로 이루어지는 저장고; (b) 저장고의 피부 반대편 상의 배면; 및 (c) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는, 치료 유효 속도에서의 옥시부티닌의 경피 투여용 장치.
  11. (a) 치료 유효량의 옥시부티닌 및 (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 피부 투과-촉진량의 투과 혼합물로 이루어지는 제1저장고; (b) 과량의 투과 촉진 혼합물 및 포화 이하의 옥시부티닌으로 이루어지는 제2저장고; (c) 제1저장고 및 제2저장고 사이의 속도-조절막; (d) 저장고의 피부 반대편 상의 배면; 및 (e) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는, 치료 유효 속도에서의 옥시부티닌의 경피 투여용 장치.
  12. 제10 또는 11항에 있어서, 추가로 유지 수단의 피부 반대편 상의 미세다공성 막으로 이루어지는 것인 장치.
  13. 제10 또는 11항에 있어서, 모노글리세리드 또는 모노글리세리드의 혼합물 20중량% 및 락테이트 에스테르 12중량%로 이루어지는 것인 장치.
  14. 제10 또는 11항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트인 장치.
  15. 제10 또는 11항에 있어서, 락테이트 에스테르가 라우릴 락테이트인 장치.
  16. 제10 또는 11항에 있어서, 락테이트 에스테르가 에틸 락테이트인 장치.
  17. 제10 또는 11항에 있어서, 락테이트 에스테르가 세틸 또는 미리스틸 락테이트인 장치.
  18. 제10 또는 11항에 있어서, 락테이트 에스테르의 혼합물이 에틸 및 라우릴 락테이트인 장치.
  19. 제10 또는 11항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트이며, 락테이트 에스테르가 에틸 락테이트 또는 라우릴 락테이트 또는 그의 혼합물인 장치.
  20. 제10 또는 11항에 있어서, 약물이 R-옥시부티닌인 장치.
  21. 제10항에 있어서, 저장고와 피부 사이의 관계를 유지시켜주는 수단이 저장고의 피부 인접면 상의 인-라인(in-line) 접착층으로 이루어지는 것인 장치.
  22. 제11항에 있어서, 저장고와 피부 사이의 관계를 유지시켜주는 수단이 제1저장고의 피부 인접면 상의 인-라인(in-line) 접착층으로 이루어지는 것인 장치.
  23. 제11항에 있어서, 제1저장고 또한 저장고와 피부 사이의 관계를 유지시켜주는 수단으로서 기능하는 접착층인 장치.
  24. 제15 내지 18항 중 어느 한 항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트인 장치.
  25. 제24항에 있어서, 글리세롤 모노라우레이트 및 락테이트 에스테르가 약물 함유 저장고의 각각 20중량% 및 12중량%로 이루어지는 것인 장치.
  26. (a) (ⅰ) 옥시부티닌 15 내지 30중량%, (ⅱ) 글리세롤 모노라우레이트 15 내지 25중량%, (ⅲ) 라우릴 락테이트 8 내지 25중량%, 및 (ⅳ) 에틸렌 비닐 아세테이트 공중합체 20 내지 62중량%로 이루어지는 저장고; (b) 저장고의 피부 반대편 상의 배면; 및 (c) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는, 치료 유효 속도에서의 옥시부티닌의 경피 투여용 장치.
  27. 제26항에 있어서, 저장고가 추가로 2 내지 30중량%의 가교된 폴리-N-비닐피롤리돈으로 이루어지는 것인 장치.
  28. 제26항에 있어서, 추가로 유지 수단의 피부 반대쪽 표면 상의 미세다공성 막으로 이루어지는 것인 장치.
  29. 제26 내지 28항 중 어느 한 항에 있어서, 저장고가 20중량%의 글리세롤 모노라우레이트 및 12중량%의 라우릴 락테이트로 이루어지는 것인 장치.
  30. (a) 옥시부티닌을 치료 유효 속도로 피부 면적에 투여하고, (b (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 투과-촉진 혼합물을 약물에 대한 침투성을 실질적으로 증가시키기에 충분한 속도로 피부 면적에 동시 투여하는 것으로 이루어지는, 옥시부티닌의 경피 투여 방법.
  31. (a) 치료 유효량의 옥시부티닌 및 (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 피부 투과-촉진량의 투과 혼합물로 이루어지는 저장고; (b) 저장고의 피부 반대편 상의 배면; 및 (c) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는 경피 약물 전달 장치를 환자의 피부 상에 올려 놓는 단계로 이루어지는 옥시부티닌의 경피 투여 방법.
  32. (a) 치료 유효량의 옥시부티닌 및 (ⅰ) 15 내지 25중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 (ⅱ) 8 내지 25중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 피부 투과-촉진량의 투과 혼합물로 이루어지는 제1저장고; (b) 과량의 투과 촉진 혼합물 및 포화 이하의 옥시부티닌으로 이루어지는 제2저장고; (c) 제1저장고 및 제2저장고 사이의 속도-조절막; (d) 저장고의 피부 반대편 상의 배면; 및 (e) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는 경피 약물 전달 장치를 환자의 피부 상에 올려 놓는 단계로 이루어지는 옥시부티닌의 경피 투여 방법.
  33. 제30 내지 32항 중 어느 한 항에 있어서, 장치가 추가로 유지 수단의 피부 반대쪽 표면 상의 미세다공성 막으로 이루어지는 것인 방법.
  34. 제30 내지 32항 중 어느 한 항에 있어서, 20중량%의 모노글리세리드 또는 모노글리세리드의 혼합물 및 12중량%의 락테이트 에스테르 또는 락테이트 에스테르의 혼합물로 이루어지는 것인 방법.
  35. 제30 내지 32항 중 어느 한 항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트인 방법.
  36. 제30 내지 32항 중 어느 한 항에 있어서, 락테이트 에스테르가 라우릴 락테이트인 방법.
  37. 제30 내지 32항 중 어느 한 항에 있어서, 락테이트 에스테르가 에틸 락테이트인 방법.
  38. 제30 내지 32항 중 어느 한 항에 있어서, 락테이트 에스테르가 세틸 또는 미리스틸 락테이트인 방법.
  39. 제30 내지 32항 중 어느 한 항에 있어서, 락테이트 에스테르의 에틸 및 라우릴 락테이트인 방법.
  40. 제30 내지 32항 중 어느 한 항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트이며, 락테이트 에스테르가 에틸 락테이트 또는 라우릴 락테이트 또는 그의 혼합물인 방법.
  41. 제36 내지 39항 중 어느 한 항에 있어서, 모노글리세리드가 글리세롤 모노라우레이트이며, 글리세롤 모노라우레이트가 20중량%를 이루고 락테이트 에스테르가 12중량%를 이루어지는 것인 방법.
  42. (a) (ⅰ) 옥시부티닌 15 내지 30중량%, (ⅱ) 글리세롤 모노라우레이트 15 내지 25중량%, (ⅲ) 라우릴 락테이트 8 내지 25중량%, 및 (ⅳ) 에틸렌 비닐 아세테이트 공중합체 20 내지 62중량%로 이루어지는 저장고; (b) 저장고의 피부 반대편 상의 배면; 및 (c) 저장고를 피부와의 약물- 및 투과 촉진 혼합물-이동 관계로 유지시켜 주는 수단으로 이루어지는 경피 약물 전달 장치를 환자의 피부 상에 올려 놓는 단계로 이루어지는 옥시부티닌의 경피 투여 방법.
  43. 제42항에 있어서, 장치가 추가로 유지 수단의 피부 반대쪽 표면 상의 미세다공성 막으로 이루어지는 것인 방법.
  44. 제42 또는 43항에 있어서, 저장고가 (ⅰ) 옥시부티닌 25중량%, (ⅱ) 글리세롤 모노라우레이트 20중량%, (ⅲ) 라우릴 락테이트 12%, 및 (ⅳ) 에틸렌 비닐 아세테이트 공중합체 43중량%로 이루어지는 것인 방법.
  45. 제42 또는 43항에 있어서, 저장고가 추가로 2 내지 30중량%의 가교된 폴리-N-비닐 피롤리돈으로 이루어지는 것인 방법.
  46. 제42 내지 44항 중 어느 한 항에 있어서, 옥시부티닌이 R-옥시부티닌인 방법.
  47. 제42 내지 44항 중 어느 한 항에 있어서, 옥시부티닌이 S-옥시부티닌인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960701611A 1993-09-29 1994-09-29 옥시부티닌용 모노글리세리드/락테이트 에스테르 투과 촉진제(Monoglyceride/lactate Ester Permeation Enhancer for Oxybutynin) KR960704579A (ko)

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US12949493A 1993-09-29 1993-09-29
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PCT/US1994/011226 WO1995009007A1 (en) 1993-09-29 1994-09-29 Monoglyceride/lactate ester permeation enhancer for oxybutynin

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KR1019960701611A KR960704579A (ko) 1993-09-29 1994-09-29 옥시부티닌용 모노글리세리드/락테이트 에스테르 투과 촉진제(Monoglyceride/lactate Ester Permeation Enhancer for Oxybutynin)

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EP0721348A1 (en) 1996-07-17
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ATE183926T1 (de) 1999-09-15
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US5686097A (en) 1997-11-11
AU7924994A (en) 1995-04-18
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WO1995009007A1 (en) 1995-04-06
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