KR100648536B1 - 침투 보강 및 자극 감소를 위한 계 - Google Patents
침투 보강 및 자극 감소를 위한 계 Download PDFInfo
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Abstract
Description
제제 | 제제 성분 | 평균 테스토스테론 플럭스 ±표준 편차 | 120 시간 경과후의 총 홍반 등급 ±표준 편차 |
A | T2, PG37, ET15, IPA15, KH1, O Acd 1.0 | 21.21±1.87 | 4.0±0.3 |
B | T2, PG37, ET15, IPA15, KH1, O Alc 1.0 | 15.08±3.96 | 8.7±0.3 |
제제 | 활성 성분 | 글리콜 | 알콜 #1 | 알콜 #2 | 막 유동화제 | 겔화제 | 가교제 | 물 |
545 | T 2.0 | PG 36.6 | ET 15.0 | IPA 15.0 | O Acd 1.0 | C1 0.6 | TEA 0.4 | 29.4 |
546 | T 2.0 | PG 36.6 | ET 15.0 | IPA 15.0 | O Alc 1.0 | C1 0.6 | TEA 0.4 | 29.4 |
번호 | ET | IPA | PG | O Acd | T | IR | IR | Carb | TEA | 물 |
J | 15.0 | 15.0 | 35.6 | 1.0 | 2.0 | 1.0 | -- | 0.6 | 0.4 | 29.4 |
K | 15.0 | 15.0 | 35.1 | 2.5 | 2.0 | -- | -- | 0.6 | 0.4 | 29.4 |
L | 15.0 | 15.0 | 34.6 | 1.0 | 2.0 | 1.0 | 1.0 | 0.6 | 0.4 | 29.4 |
제제 번호 | DAA-97-602 | DAA-97-601 | DAA-97-600 |
에탄올 | 15.0 | 15.0 | 15.0 |
이소프로필 알콜 | 15.0 | 15.0 | 15.0 |
프로필렌 글리콜 | 35.6 | 35.1 | 34.6 |
올레산 | 1.0 | 2.5 | 2.0 |
테스토스테론 | 2.0 | 2.0 | 2.0 |
자극 감소제 No 1 | 1.0 | - | 1.0 |
자극 감소제 No 2 | - | - | 1.0 |
Carbopol 1342 | 0.6 | 0.6 | 0.6 |
트리에탄올아민 | 0.4 | 0.4 | 0.4 |
물 | 29.4 | 29.4 | 29.4 |
제제의 조성 | |||||
성분 | 0.50% | 1.00% | 1.25% | 1.50% | 2.00% |
제제 1: 6.0 제제 2: 4.5 제제 6: 3.0 | 제제 11: 5.0 제제 8: 3.0 제제 14: 6.0 제제 15: 7.0 제제 16: 8.0 | 제제 3: 6.0 | 제제 7: 3.0 | 제제 4: 6.0 제제 5: 3.0 제제 9: 4.0 제제 10: 5.0 제제 12: 7.0 제제 13: 8.0 | |
테스토스테론 USP/NF | 0.50 | 1.00 | 1.25 | 1.50 | 2.00 |
Carbomer 1342 USP | 0.60 | 0.60 | 0.60 | 0.60 | 0.60 |
프로필렌 글리콜 USP | 35.61 | 35.44 | 35.33 | 35.23 | 35.05 |
이소프로필 알콜 USP | 15.24 | 15.16 | 15.12 | 15.08 | 15.00 |
무수 알콜 USP | 15.24 | 15.16 | 15.12 | 15.08 | 15.00 |
올레산 USP | 2.50 | 2.50 | 2.50 | 2.50 | 2.50 |
트리에탄올아민 99% NF 또는 HCl 1N | pH에 대해 충분량 | pH에 대해 충분량 | pH에 대해 충분량 | pH에 대해 충분량 | pH에 대해 충분량 |
부틸화된 히드록시톨루엔, NF | 0.050 | 0.050 | 0.050 | 0.050 | 0.050 |
정제수, USP | 29.87 | 29.72 | 29.64 | 29.54 | 29.40 |
제제 | 실험 | 24 시간 동안 침투된 테스토스테론 함량 (㎍/㎠) | 피부상의 잔류물 알콜 면봉 (㎍/㎠) | 피부상의 잔류물 테이프 스트립 (㎍/㎠) | 피부내에서의 함량 (㎍/g 조직) | |||||
코드 | 조성 및 pH | 평균 | 표준 편차 | 평균 | 표준 편차 | 평균 | 표준 편차 | 평균 | 표준 편차 | |
#4 (601) | 2.00% 테스토스테론 pH 6.0 | 1 | 24.31 | 3.98 | 55.4 | 15.9 | 18.7 | 11.2 | 409.3 | 112.5 |
2 | 31.36 | 6.09 | 59.8 | 22.3 | 19.6 | 6.6 | 257.3 | 71.4 | ||
3 | 22.76 | 4.02 | 57.2 | 20.2 | 15.0 | 7.2 | 267.1 | 63.7 | ||
4 | 46.96 | 14.19 | 79.3 | 5.8 | 21.4 | 7.0 | 726.8 | 111.5 | ||
5 | 35.45 | 5.63 | 51.2* | 13.4* | 29.9 | 6.3 | 439.0 | 159.4 | ||
* 알콜 면봉은 건조한 면봉으로부터 얻음 |
24 시간 동안 침투된 시험관내 축적량 (㎍/㎠. 평균±표준 편차, n=5-6) | 1일 5 ㎎의 전달에 필요한 면적 | 투여된 테스토스테론 총량 (100 ㎠당 겔 1 g) | 24 시간 경과후 피부상에 잔존하는 잔류물 (면봉+테이프 스트립) | 24 시간 경과후 피부내에 잔존하는 테스토스테론 | |
2.0% 겔 pH 6.0 (제제 4) | 47.0±14.2 | 106 ㎠ | 21.2 ㎎ (100%) | 10.7 ㎎ (49±5%) | 2.8 ㎎ (13±4%) |
1.0% 겔 pH 6.0 (제제 14) | 28.0±4.8 | 178 ㎠ | 17.8 ㎎ (100%) | 5.7 ㎎ (32±4%) | 2.5 ㎎ (14±2%) |
국소용 테스토스테론 겔의 임상적 제제 | ||
성분 | % w/w | |
1.0% | 2.0% | |
테스토스테론, USP/NF | 1.00 | 2.00 |
무수 에탄올, USP | 15.00 | 15.00 |
2-프로판올, USP | 15.00 | 15.00 |
프로필렌 글리콜, USP | 35.05 | 35.05 |
올레산, NF | 2.50 | 2.50 |
부틸화된 히드록시톨루엔, NF | 0.05 | 0.05 |
Carbomer, USP | 0.60 | 0.60 |
트리에탄올아민, NF, pH 6.0까지의 충분량 | 0.30-0.40 | 0.30-0.40 |
정제수, USP 충분량 | 30.00-29.90 | 29.00-28.90 |
총량 | 100.00 | 100.0 |
성분 | g/20 ㎏ 회분 | |
1.0% | 2.0% | |
테스토스테론, USP/NF | 200.00 | 400.00 |
무수 에탄올3 USP/NF | 3,000.00 | 3,000.00 |
2-프로판올, USP | 3,000.00 | 3,000.00 |
프로필렌 글리콜, USP | 7,010.00 | 7,010.00 |
올레산, NF | 500.00 | 500.00 |
부틸화된 히드록시톨루엔, NF | 10.00 | 10.00 |
Carbomer4 USP | 120.00 | 120.00 |
트리에탄올아민5, NF 충분량 | 60.00-80.00 | 60.00-80.00 |
정제수6 USP 충분량 | 6,000.00-5,980.00 | 5,800.00-5,780.00 |
총량 | 20,000.00 | 20,000.00 |
Claims (45)
- a) 테스토스테론 또는 테스토스테론 프로피오네이트인 활성제 0.1 내지 2 중량%;b) (i) 올레산을 포함하는 막 유동화제, (ii) C1-C4 알콜과 (iii) 글리콜로 구성되는 침투 보강계; 및c) 겔화제로 구성되며, 5 내지 8의 pH 값을 갖는 침투 보강특성을 갖는 국소 도포용 조성물
- 삭제
- 삭제
- 삭제
- 삭제
- 삭제
- 제1항에 있어서, 상기 활성제는 상기 조성물의 중량을 기준으로 하여 1∼2 중량%로 존재하는 것인 국소 도포용 조성물.
- 삭제
- 삭제
- 제1항에 있어서, 상기 올레산은 상기 조성물의 중량을 기준으로 하여 0.1∼10 중량%로 존재하는 것인 국소 도포용 조성물.
- 제10항에 있어서, 상기 올레산은 상기 조성물의 중량을 기준으로 하여 0.1∼5 중량%로 존재하는 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 C1-C4 알콜은 에탄올, 프로판올, 이소프로판올 및 이의 혼합물로 구성된 군에서 선택된 것인 국소 도포용 조성물.
- 제12항에 있어서, 상기 C1-C4 알콜은 에탄올인 것인 국소 도포용 조성물.
- 제12항에 있어서, 상기 C1-C4 알콜은 프로판올인 것인 국소 도포용 조성물.
- 제12항에 있어서, 상기 C1-C4 알콜은 이소프로판올인 것인 국소 도포용 조성물.
- 제12항에 있어서, 상기 C1-C4 알콜은 에탄올 및 이소프로판올의 혼합물인 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 C1-C4 알콜은 상기 조성물의 중량을 기준으로 하여 5∼65 중량%로 존재하는 것인 국소 도포용 조성물.
- 제17항에 있어서, 상기 C1-C4 알콜은 상기 조성물의 중량을 기준으로 하여 10∼40 중량%로 존재하는 것인 국소 도포용 조성물.
- 제17항에 있어서, 상기 C1-C4 알콜은 상기 조성물의 중량을 기준으로 하여 25∼35 중량%로 존재하는 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 글리콜은 에틸렌 글리콜, 프로필렌 글리콜, 부틸렌 글리콜 및 이의 혼합물로 구성된 군에서 선택되는 것인 국소 도포용 조성물.
- 제20항에 있어서, 상기 글리콜은 에틸렌 글리콜인 것인 국소 도포용 조성물.
- 제20항에 있어서, 상기 글리콜은 부틸렌 글리콜인 것인 국소 도포용 조성물.
- 제20항에 있어서, 상기 글리콜은 프로필렌 글리콜인 것인 국소 도포용 조성물.
- 제20항에 있어서, 상기 글리콜은 에틸렌 글리콜 및 부틸렌 글리콜의 혼합물인 것인 국소 도포용 조성물.
- 제20항에 있어서, 상기 글리콜은 프로필렌 글리콜 및 부틸렌 글리콜의 혼합물인 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 글리콜은 상기 조성물의 중량을 기준으로 하여 25∼55 중량%로 존재하는 것인 국소 도포용 조성물.
- 제26항에 있어서, 상기 글리콜은 상기 조성물의 중량을 기준으로 하여 30∼40 중량%로 존재하는 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 겔화제는 Carbopol 1342, Carbopol 940, Klucel 및 Klucel HF로 구성된 군에서 선택된 것인 국소 도포용 조성물.
- 제28항에 있어서, 상기 겔화제는 Carbopol 1342인 것인 국소 도포용 조성물.
- 제1항에 있어서, 상기 겔화제는 상기 조성물의 중량을 기준으로 하여 0.1∼10 중량%로 존재하는 것인 국소 도포용 조성물.
- 제30항에 있어서, 상기 겔화제는 상기 조성물의 중량을 기준으로 하여 0.1∼5 중량%로 존재하는 것인 국소 도포용 조성물.
- 제30항에 있어서, 상기 겔화제는 상기 조성물의 중량을 기준으로 하여 1∼3 중량%로 존재하는 것인 국소 도포용 조성물.
- a) 테스토스테론 또는 테스토스테론 프로피오네이트인 활성제 0.1 내지 2 중량%;b) (i) 올레산을 포함하는 막 유동화제, (ii) C1-C4 알콜과 (iii) 글리콜로 구성되는 침투 보강계;c) 겔화제; 및d) 불활성 담체로 구성되며, 5 내지 8의 pH 값을 갖는 침투 보강 특성을 갖는 국소 도포용 조성물.
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US6498097P | 1997-11-10 | 1997-11-10 | |
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-
1998
- 1998-11-09 PT PT04028426T patent/PT1510213E/pt unknown
- 1998-11-09 EP EP98956663A patent/EP1030668A4/en not_active Withdrawn
- 1998-11-09 KR KR1020007005094A patent/KR100648536B1/ko active IP Right Grant
- 1998-11-09 US US09/189,090 patent/US6319913B1/en not_active Expired - Lifetime
- 1998-11-09 AT AT04028426T patent/ATE418988T1/de active
- 1998-11-09 ES ES04028426T patent/ES2318233T3/es not_active Expired - Lifetime
- 1998-11-09 EP EP04028426A patent/EP1510213B1/en not_active Revoked
- 1998-11-09 JP JP2000520133A patent/JP4139860B2/ja not_active Expired - Fee Related
- 1998-11-09 CA CA002309688A patent/CA2309688C/en not_active Expired - Fee Related
- 1998-11-09 NZ NZ504423A patent/NZ504423A/xx not_active IP Right Cessation
- 1998-11-09 CN CNB988130491A patent/CN1172674C/zh not_active Expired - Fee Related
- 1998-11-09 WO PCT/US1998/023750 patent/WO1999024041A1/en active IP Right Grant
- 1998-11-09 IL IL13604298A patent/IL136042A/xx not_active IP Right Cessation
- 1998-11-09 AU AU13132/99A patent/AU747041B2/en not_active Ceased
- 1998-11-09 BR BRPI9814014-0A patent/BR9814014B1/pt not_active IP Right Cessation
- 1998-11-09 DE DE69840426T patent/DE69840426D1/de not_active Expired - Lifetime
- 1998-11-09 DK DK04028426T patent/DK1510213T3/da active
-
2000
- 2000-05-10 NO NO20002422A patent/NO20002422L/no not_active Application Discontinuation
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2001
- 2001-09-24 US US09/963,287 patent/US6579865B2/en not_active Expired - Lifetime
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2003
- 2003-03-12 US US10/389,715 patent/US7157097B2/en not_active Expired - Lifetime
-
2004
- 2004-10-28 JP JP2004313201A patent/JP2005047932A/ja not_active Withdrawn
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Also Published As
Publication number | Publication date |
---|---|
US7157097B2 (en) | 2007-01-02 |
KR20010031984A (ko) | 2001-04-16 |
NZ504423A (en) | 2003-04-29 |
NO20002422L (no) | 2000-06-21 |
US20020058650A1 (en) | 2002-05-16 |
AU1313299A (en) | 1999-05-31 |
DK1510213T3 (da) | 2009-03-23 |
US6319913B1 (en) | 2001-11-20 |
EP1030668A4 (en) | 2002-09-25 |
NO20002422D0 (no) | 2000-05-10 |
WO1999024041A1 (en) | 1999-05-20 |
US6579865B2 (en) | 2003-06-17 |
AU747041B2 (en) | 2002-05-09 |
EP1510213A3 (en) | 2005-03-23 |
IL136042A0 (en) | 2001-05-20 |
CA2309688A1 (en) | 1999-05-20 |
JP2005047932A (ja) | 2005-02-24 |
EP1030668A1 (en) | 2000-08-30 |
DE69840426D1 (de) | 2009-02-12 |
US20030166625A1 (en) | 2003-09-04 |
BR9814014A (pt) | 2000-09-26 |
EP1510213B1 (en) | 2008-12-31 |
CN1172674C (zh) | 2004-10-27 |
ES2318233T3 (es) | 2009-05-01 |
AU747041C (en) | 1999-05-31 |
JP4139860B2 (ja) | 2008-08-27 |
ATE418988T1 (de) | 2009-01-15 |
EP1510213A2 (en) | 2005-03-02 |
PT1510213E (pt) | 2009-02-12 |
CA2309688C (en) | 2007-04-24 |
JP2001522804A (ja) | 2001-11-20 |
CN1285749A (zh) | 2001-02-28 |
IL136042A (en) | 2005-12-18 |
BR9814014B1 (pt) | 2014-10-07 |
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