KR20050006657A - 신규한 암로디핀 오로테이트 염, 그의 제조방법 및 그의약제학적 조성물 - Google Patents
신규한 암로디핀 오로테이트 염, 그의 제조방법 및 그의약제학적 조성물 Download PDFInfo
- Publication number
- KR20050006657A KR20050006657A KR1020030046548A KR20030046548A KR20050006657A KR 20050006657 A KR20050006657 A KR 20050006657A KR 1020030046548 A KR1020030046548 A KR 1020030046548A KR 20030046548 A KR20030046548 A KR 20030046548A KR 20050006657 A KR20050006657 A KR 20050006657A
- Authority
- KR
- South Korea
- Prior art keywords
- amlodipine
- salt
- formula
- orotate
- hypertension
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
- C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
구 성 성 분 | 함량 (mg/정) | 비 고 |
암로디핀 오로테이트 염 | 6.909 | 암로디핀으로서 5 mg/정 |
무구인산수소칼슘 | 63 | |
미결정질 셀룰로스 | 124.091 | Avicel PH101 |
크로스카멜로스 소디움 | 4 | Primellose |
스테아린산 마그네슘 | 2 | |
정제 중량 | 200 mg/정 |
구 성 성 분 | 함량 (mg/정) | 비 고 |
암로디핀 오로테이트 염 | 6.909 | 암로디핀으로서 5 mg/정 |
폴리소르베이트 80 | 5 | Avicel PH101 |
프로필렌카보네이트 | 3 | Primellose |
폴리에틸렌400/프로필렌글리콜 혼합액 | 6 | PEG400 : PG = 100 : 4 |
폴록사머407 | 3 | |
연질캅셀제 중량 | 23.909 mg/캅셀 |
염 | 용해도 (mg/ml) | 포화시 pH |
암로디핀 오로테이트 | 2.45 | 5.97 |
암로디핀 베실레이트 | 2.14 | 5.44 |
시험물질 | 용량(mg/kg) | 폐사율사망동물/시험동물수 | 반수치사량 (mg/kg)(95% 신뢰한계) |
암로디핀베실레이트 염 | 20 | 0/6 | 32.9(28.1 ~ 38.0) |
30 | 2/6 | ||
40 | 5/6 | ||
50 | 6/6 | ||
암로디핀오로테이트 염 | 20 | 0/6 | 34.4(29.6 ~ 39.6) |
30 | 1/6 | ||
40 | 5/6 | ||
50 | 6/6 |
약물/항목 | 암로디핀 베실레이트 염 | 암로디핀 오로테이트 염 | ||
정상 랫드 | 미주신경절단 랫드 | 정상 랫드 | 미주신경절단 랫드 | |
Cmax (ng/ml) | 40.6 | 28.1a | 39.3 | 36.1 |
Tmax(hr) | 5.6 | 8.4a | 5.2 | 6.4b |
AUC(nghr/ml) | 470 | 352a | 471 | 422 |
Claims (5)
- 하기 화학식 1의 구조를 갖는 암로디핀 오로테이트 염.[화학식 1]
- 하기 화학식 2의 암로디핀 염기와 하기 화학식 3의 오로트산을 물과 유기용매의 혼합용매하에서 반응시켜 제 1항에 따른 암로디핀 오로테이트 염을 제조하는 방법.[화학식 2][화학식 3]
- 제 1항에 기재된 화학식 1의 암로디핀 오로테이트 염을 유효성분으로 함유함을 특징으로 하는 심장질환이나 고혈압 치료용 약제학적 조성물.
- 제 3항에 있어서, 위장 운동 기능이 저하된 고혈압 환자, 위장관 절제술을 받은 고혈압 환자 또는 저산증/무산증 고혈압 환자에게 투여 시에도 일정한 용출율이 기대되는 심장질환이나 고혈압 치료용 약제학적 조성물.
- 제 3항에 있어서, 제제 형태가 정제, 경질캅셀제, 연질캅셀제, 과립제, 샤세(Sachet)의 형태인 제제 중에서 선택되는 심장질환이나 고혈압 치료용 약제학적 조성물.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR10-2003-0046548A KR100517384B1 (ko) | 2003-07-09 | 2003-07-09 | 신규한 암로디핀 오로테이트 염, 그의 제조방법 및 그의약제학적 조성물 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR10-2003-0046548A KR100517384B1 (ko) | 2003-07-09 | 2003-07-09 | 신규한 암로디핀 오로테이트 염, 그의 제조방법 및 그의약제학적 조성물 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20050006657A true KR20050006657A (ko) | 2005-01-17 |
KR100517384B1 KR100517384B1 (ko) | 2005-09-27 |
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Family Applications (1)
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KR10-2003-0046548A KR100517384B1 (ko) | 2003-07-09 | 2003-07-09 | 신규한 암로디핀 오로테이트 염, 그의 제조방법 및 그의약제학적 조성물 |
Country Status (1)
Country | Link |
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KR (1) | KR100517384B1 (ko) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1855531A2 (en) * | 2005-02-22 | 2007-11-21 | Savvipharm Inc. | Method of increasing drug oral bioavailability and compositions of less toxic orotate salts |
WO2008091085A1 (en) * | 2007-01-23 | 2008-07-31 | Cj Cheiljedang Corporation | Crystalline s-(-)-amlodipine orotate anhydrous and preparation method thereof |
-
2003
- 2003-07-09 KR KR10-2003-0046548A patent/KR100517384B1/ko active IP Right Grant
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1855531A2 (en) * | 2005-02-22 | 2007-11-21 | Savvipharm Inc. | Method of increasing drug oral bioavailability and compositions of less toxic orotate salts |
EP1855531A4 (en) * | 2005-02-22 | 2009-09-23 | Savvipharm Inc | METHOD FOR INCREASING THE ORAL BIOVERABILITY OF A MEDICAMENT AND COMPOSITIONS FROM LESS TOXIC OROTATE SALTS |
WO2008091085A1 (en) * | 2007-01-23 | 2008-07-31 | Cj Cheiljedang Corporation | Crystalline s-(-)-amlodipine orotate anhydrous and preparation method thereof |
Also Published As
Publication number | Publication date |
---|---|
KR100517384B1 (ko) | 2005-09-27 |
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