KR100970528B1 - 항신생물제, 특히 테모졸로마이드의 약제학적 제형, 이의제조 및 사용 방법 - Google Patents
항신생물제, 특히 테모졸로마이드의 약제학적 제형, 이의제조 및 사용 방법 Download PDFInfo
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Abstract
Description
성분 | mg/ml | wt% |
*테모졸로마이드 | 2.50 | 8 |
L-트레오닌 | 4.00 | 13 |
폴리소르베이트 80 | 3.00 | 9 |
시트르산 나트륨 이수화물 | 5.88 | 18 |
만니톨 | 15.0 | 47 |
**염산 | 1.48 | 5 |
적량의 주입용 수 | 1.00ml |
성분 | mg/ml | wt% |
*테모졸로마이드 | 2.50 | 8% |
L-히스티딘 | 2.00 | 7% |
폴리소르베이트 80 | 3.00 | 10% |
시트르산 나트륨 이수화물 | 5.88 | 19% |
만니톨 | 15.0 | 49 |
**염산 | 2.08 | 7 |
적량의 주입용 수 | 1.00ml |
성분 | mg/ml(물 제외) | wt% |
*테모졸로마이드 | 2.50 | 8 |
L-아스파라긴 | 4.00 | 13 |
폴리소르베이트 80 | 3.00 | 9 |
시트르산 나트륨 이수화물 | 5.88 | 18 |
만니톨 | 15.0 | 47 |
**염산 | 1.48 | 5 |
적량의 주입용 수 | 1.00ml |
성분 | mg/ml | wt% |
*테모졸로마이드 | 2.50 | 8 |
우레아 | 5.00 | 17 |
시트르산 나트륨 이수화물 | 5.88 | 20 |
만니톨 | 15.0 | 50 |
**염산 | 1.48 | 5 |
적량의 주입용 수 | 1.00ml |
뱃치 번호 | 안정성 싯점/조건 |
초기 % 검정 1 |
초기 % 검정 2 |
평균 초기 % (n = 2) | 수분 (%) | pH | 재구성 시간(초) |
A | 초기 | 100.00 | 100.00 | 100.00 | 0.4 | 3.75 | 30 |
A | 1주, LTC/LTR | 100.00 | 99.63 | 99.82 | 0.4 | 3.77 | 30 |
A | 1주, LTC/LTR 대조군 | 100.11 | 99.99 | 100.05 | 0.4 | 3.77 | 30 |
A | 4주, 4 | 100.18 | 99.62 | 99.9 | 0.4 | 3.83 | 30 |
A | 4주, 25H | 100.24 | 99.13 | 99.69 | 0.3 | 3.84 | 30 |
A | 4주, 40 | 99.17 | 98.11 | 98.64 | 0.4 | 3.84 | 30 |
A | 8주, 25H | 99.43 | 98.82 | 99.125 | 0.4 | 3.81 | 30 |
A | 12주, 4 | 99.37 | 99.59 | 99.48 | 0.3 | 3.83 | 30 |
A | 12주, 25H | 99.24 | 99.22 | 99.23 | 0.4 | 3.82 | 30 |
상기 표에서, "LTC"는 25℃에서의 광안정성 시험을 의미하고, "LTR"은 4℃에서의 광안정성 시험을 의미하며, "25H"는 60% 실내 습도에서 25℃인 조건을 의미하고, "40"은 75% 실내 습도에서 40℃인 조건을 의미하며, "4"는 4℃를 의미하고, "LTC/LTR 대조군"은 광을 차폐시킨 2개의 조건하에서의 광안정성 샘플(LTC & LTR 샘플은 알루미늄 호일과 같은 불투명 물질로 덮는다)을 의미한다. |
뱃치 번호 | 안정성 싯점/조건 |
초기 % 검정 1 |
초기 % 검정 2 |
평균 초기 % (n = 2) | 습도 (%) | pH | 재구성 시간(초) |
B | 초기 | 100.00 | 100.00 | 100.00 | 1.6 | 3.96 | 30 |
B | 1주, LTC/LTR | 100.65 | 100.41 | 100.53 | 1.3 | 6.97 | 30 |
B | 1주, LTC/LTR 대조군 | 99.63 | 100.27 | 99.95 | 1.6 | 3.97 | 30 |
B | 4주, 4 | 100.45 | 100.43 | 100.44 | 2.1 | 4.00 | 30 |
B | 4주, 25H | 99.89 | 99.04 | 99.47 | 2.0 | 4.00 | 30 |
B | 4주, 40 | 99.86 | 99.66 | 99.76 | 2.0 | 4.00 | 30 |
B | 8주, 25H | 99.91 | 100.15 | 100.03 | 2.0 | 4.04 | 30 |
B | 12주, 4 | 100.16 | 100.00 | 100.08 | 2.0 | 4.01 | 30 |
B | 12주, 25H | 98.84 | 100.2 | 99.52 | 2.0 | 4.00 | 30 |
뱃치 번호 | 안정성 싯점/조건 |
초기 % 검정 1 |
초기 % 검정 2 |
평균 초기 % (n = 2) | 수분 (%) | pH | 재구성 시간(초) |
C | 초기 | 100.00 | 100.00 | 100.00 | 0.3 | 4.00 | 30 |
C | 1주, LTC/LTR | 97.59 | 103.68 | 100.635 | 0.4 | 4.04 | 30 |
C | 1주, LTC/LTR 대조군 | 98.14 | 99.55 | 98.845 | 0.5 | 4.04 | 30 |
C | 4주, 4 | 97.09 | 97.47 | 97.28 | 0.4 | 4.03 | 30 |
C | 4주, 25H | 98.49 | 97.18 | 97.835 | 0.5 | 4.03 | 30 |
C | 4주, 40 | 97.96 | 97.28 | 97.62 | 0.6 | 4.06 | 90 |
C | 8주, 25H | 98.42 | 97.56 | 97.99 | 0.6 | 4.04 | 30 |
C | 12주, 4 | 98.27 | 96.94 | 97.605 | 0.4 | 4.02 | 30 |
C | 12주, 25H | 98.67 | 97.77 | 98.22 | 0.6 | 4.02 | 30 |
뱃치 번호 | 안정성 싯점/조건 |
초기 % 검정 1 |
초기 % 검정 2 |
평균 초기 % (n = 2) | 수분 (%) | pH | 재구성 시간(초) |
D | 초기 | 100.00 | 100.00 | 100.00 | 0.4 | 4 | 30 |
D | 1주, LTC/LTR | 103.87 | 98.41 | 101.14 | 0.3 | 4.03 | 30 |
D | 1주, LTC/LTR 대조군 | 100.46 | 98.95 | 99.705 | 0.4 | 4.02 | 30 |
D | 4주, 4 | 101.06 | 99.3 | 100.18 | 0.4 | 4.02 | 30 |
D | 4주, 25H | 101.69 | 98.97 | 100.33 | 0.4 | 4.02 | 30 |
D | 4주, 40 | 101.49 | 98.95 | 100.22 | 0.7 | 4.03 | 30 |
D | 8주, 25H | 100.86 | 98.78 | 99.82 | 0.5 | 4.01 | 30 |
D | 12주, 4 | 101.3 | 99.28 | 100.29 | 0.4 | 4 | 30 |
D | 12주, 25H | 101.37 | 98.59 | 99.98 | 0.5 | 4 | 30 |
Claims (40)
- 테모졸로마이드 또는 이의 약제학적으로 허용되는 염, 하나 이상의 수성 희석액, 및 상기 테모졸로마이드를 용해시키기에 충분한 하나 이상의 용해 증진제(여기서, 용해 증진제는 우레아, L-히스티딘, L-트레오닌, L-아스파라긴, L-세린, L-글루타민 또는 이의 혼합물이다)를 포함하는 약제학적 제형.
- 제1항에 있어서, 폴리소르베이트를 추가로 포함하는 약제학적 제형.
- 제2항에 있어서, 폴리소르베이트가 폴리소르베이트 20, 폴리소르베이트 80 또는 이의 혼합물인 약제학적 제형.
- 제3항에 있어서, 폴리소르베이트가 폴리소르베이트 80인 약제학적 제형.
- 제1항에 있어서, 하나 이상의 충전제(bulking agent)를 추가로 포함하는 약제학적 제형.
- 제5항에 있어서, 충전제가 만니톨인 약제학적 제형.
- 제1항에 있어서, 하나 이상의 완충액을 추가로 포함하는 약제학적 제형.
- 제7항에 있어서, 완충액이 시트르산 나트륨 이수화물인 약제학적 제형.
- 제1항에 있어서, pH 조절제를 추가로 포함하는 약제학적 제형.
- 제9항에 있어서, pH 조절제가 염산인 약제학적 제형.
- 제10항에 있어서, pH가 3.0 내지 4.5의 범위인 약제학적 제형.
- 제10항에 있어서, pH가 3.8 내지 4.2의 범위인 약제학적 제형.
- 제1항에 있어서, 수성 희석액이 물인 약제학적 제형.
- 제1항에 있어서, 용해 증진제가 L-트레오닌인 약제학적 제형.
- 테모졸로마이드 또는 이의 약제학적으로 허용되는 염, 하나 이상의 수성 희석액, L-트레오닌, 폴리소르베이트, 충전제, 완충액 및 pH 조절제를 포함하는 약제학적 제형.
- 제15항에 있어서, 폴리소르베이트가 폴리소르베이트 80이고, pH 조절제가 염산이고, 완충액이 시트레이트 완충액이며, 충전제가 만니톨인 약제학적 제형.
- 제16항에 있어서, 테모졸로마이드가 4중량% 내지 16중량% 범위의 양으로 존재하고, 염산이 4중량% 내지 8중량% 범위의 양으로 존재하며, 시트레이트 완충액이 15중량% 내지 28중량% 범위의 양으로 존재하고, 폴리소르베이트가 4중량% 내지 16중량% 범위의 양으로 존재하며, L-트레오닌이 8중량% 내지 20중량% 범위의 양으로 존재하고, 만니톨이 40중량% 내지 56중량% 범위의 양으로 존재하는 약제학적 제형.
- 제17항에 있어서, 테모졸로마이드가 8중량%의 양으로 존재하고, 염산이 5중량%의 양으로 존재하며, 시트레이트 완충액이 18중량%의 양으로 존재하고, 폴리소르베이트가 9중량%의 양으로 존재하며, L-트레오닌이 13중량%의 양으로 존재하고, 만니톨이 47중량%의 양으로 존재하는 약제학적 제형.
- L-트레오닌을 하나 이상의 수성 희석액 속에 용해시키는 단계(i); 및하나 이상의 테모졸로마이드 또는 이의 약제학적으로 허용되는 염을 가하는 단계(ii)를 포함하는, 약제학적 제형의 제조방법.
- 제19항에 있어서, 단계(i)이a) 만니톨을 가하는 단계;b) 시트르산 완충액을 가하는 단계; 및c) 하나 이상의 pH 조절제를 가하여 용액을 형성시키는 단계를 추가로 포함하는 방법.
- 제19항 또는 제20항에 있어서, 상기 방법으로 형성된 용액을 동결건조시켜 동결건조된 분말로 형성시키는 단계를 추가로 포함하는 방법.
- 제21항에 따른 방법으로 제조된 동결건조된 분말.
- 제22항에 따른 동결건조된 분말을 함유하는 용기를 포함하는 제품.
- 제23항에 있어서, 용기가 주사기 또는 바이알(vial)인 제품.
- 제23항에 있어서, 동결건조된 분말의 재구성에 적합한 일정량의 하나 이상의 수성 희석액을 추가로 포함하는 제품.
- 제22항에 따른 동결건조된 분말을 일정량의 하나 이상의 수성 희석액 중에 재구성시킴으로써 제조된, 환자에 투여하기에 적합한 약제학적 제형.
- 제1항 내지 제18항 중의 어느 한 항에 있어서, 신경아교종을 치료하거나 예방하는데 사용되는 약제학적 제형.
- 삭제
- 삭제
- 제15항 내지 제18항 중의 어느 한 항에 있어서, 제형의 pH가 3.8 내지 4.2의 범위인 약제학적 제형.
- 삭제
- 삭제
- 삭제
- 삭제
- 삭제
- 삭제
- 삭제
- 삭제
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- 삭제
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