KR20130081013A - 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 - Google Patents
레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 Download PDFInfo
- Publication number
- KR20130081013A KR20130081013A KR1020120001954A KR20120001954A KR20130081013A KR 20130081013 A KR20130081013 A KR 20130081013A KR 1020120001954 A KR1020120001954 A KR 1020120001954A KR 20120001954 A KR20120001954 A KR 20120001954A KR 20130081013 A KR20130081013 A KR 20130081013A
- Authority
- KR
- South Korea
- Prior art keywords
- levocetirizine
- pharmaceutically acceptable
- acid
- montelukast
- acceptable salt
- Prior art date
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Abstract
Description
도 2는 비교예 1 및 실시예 1 내지 6의 캡슐제에 대하여 40℃ 및 75% RH 가속 조건에서 6개월 동안 안정성 시험을 수행하였을 때 생성된 몬테루카스트 기인 유연물질의 양을 나타낸 것이다.
도 3은 본 발명의 캡슐제의 모형도이다.
시간(분) | A(%) | B(%) |
0 | 100 | 0 |
2 | 100 | 0 |
30 | 25 | 75 |
40 | 100 | 0 |
50 | 100 | 0 |
시간(분) | A(%) | B(%) |
0 | 60 | 40 |
20 | 10 | 90 |
30 | 10 | 90 |
31 | 60 | 40 |
35 | 60 | 40 |
시료 | 초기 | 가속 6개월 | ||||||
유연물질 A (%) |
유연물질 B (%) |
유연물질 F (%) |
유연물질 총합(%) |
유연물질 A(%) |
유연물질 B (%) |
유연물질 F (%) |
유연물질 총합(%) |
|
실시예 1 | 0.01 | 0.02 | 0.00 | 0.08 | 0.04 | 0.04 | 0.02 | 0.14 |
실시예 2 | 0.01 | 0.01 | 0.00 | 0.06 | 0.03 | 0.03 | 0.01 | 0.11 |
실시예 3 | 0.01 | 0.01 | 0.00 | 0.06 | 0.03 | 0.03 | 0.01 | 0.10 |
실시예 4 | 0.01 | 0.02 | 0.00 | 0.07 | 0.04 | 0.05 | 0.03 | 0.18 |
실시예 5 | 0.01 | 0.02 | 0.00 | 0.08 | 0.04 | 0.04 | 0.03 | 0.17 |
실시예 6 | 0.01 | 0.02 | 0.00 | 0.08 | 0.04 | 0.04 | 0.03 | 0.17 |
비교예 1 | 0.01 | 0.02 | 0.00 | 0.12 | 0.32 | 0.31 | 0.35 | 1.13 |
비교예 2 | 0.01 | 0.02 | 0.00 | 0.08 | 0.22 | 0.19 | 0.26 | 0.86 |
비교예 3 | 0.01 | 0.02 | 0.00 | 0.08 | 0.15 | 0.13 | 0.15 | 0.62 |
비교예 4 | 0.01 | 0.02 | 0.00 | 0.09 | 0.27 | 0.29 | 0.23 | 0.93 |
비교예 5 | 0.01 | 0.02 | 0.00 | 0.09 | 0.56 | 0.62 | 0.52 | 2.13 |
비교예 6 | 0.01 | 0.02 | 0.00 | 0.08 | 0.04 | 0.04 | 0.00 | 0.12 |
시료 | 초기 | 가속 6개월 | ||||
몬테 설폭사이드(%) |
몬테 시스-이성체(%) |
유연물질 총합(%) |
몬테 설폭사이드(%) |
몬테 시스-이성체(%) |
유연물질 총합(%) |
|
실시예 1 | 0.08 | 0.03 | 0.15 | 0.15 | 0.06 | 0.28 |
실시예 2 | 0.09 | 0.03 | 0.16 | 0.12 | 0.05 | 0.23 |
실시예 3 | 0.08 | 0.03 | 0.15 | 0.10 | 0.04 | 0.19 |
실시예 4 | 0.08 | 0.03 | 0.16 | 0.15 | 0.06 | 0.30 |
실시예 5 | 0.08 | 0.03 | 0.16 | 0.16 | 0.07 | 0.31 |
실시예 6 | 0.09 | 0.03 | 0.15 | 0.17 | 0.06 | 0.33 |
비교예 1 | 0.08 | 0.04 | 0.16 | 0.33 | 0.12 | 0.65 |
비교예 2 | 0.08 | 0.03 | 0.15 | 0.25 | 0.09 | 0.55 |
비교예 3 | 0.08 | 0.03 | 0.15 | 0.26 | 0.08 | 0.52 |
비교예 4 | 0.08 | 0.03 | 0.15 | 0.34 | 0.13 | 0.67 |
비교예 5 | 0.08 | 0.03 | 0.15 | 0.14 | 0.06 | 0.25 |
Claims (15)
2) 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 포함하는 제 2 입자부를 포함하는 알레르기성 비염 또는 천식의 예방 또는 치료용 경구투여용 약학 제제.
상기 제제가 레보세티리진 또는 이의 약학적으로 허용가능한 염 100 중량부를 기준으로 유기산을 40 내지 1000 중량부의 양으로 포함하는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 제제가 레보세티리진 또는 이의 약학적으로 허용가능한 염 100 중량부를 기준으로 유기산을 50 내지 500 중량부의 양으로 포함하는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 유기산이 시트르산, 타르타르산, 숙신산, 글루탐산, 아스파르트산, 옥살산, 말산, 아세트산, 소르브산, 아스코르빈산, 알긴산, 푸마르산, 락트산 및 이의 혼합물로 이루어진 군으로부터 선택되는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 제 1 입자부 또는 제 2 입자부가 미니정제인 것을 특징으로 하는, 경구투여용 약학 제제.
상기 제제가 캡슐 제제인 것을 특징으로 하는, 경구투여용 약학 제제.
상기 캡슐이 경질 캡슐인 것을 특징으로 하는, 경구투여용 약학 제제.
상기 경질 캡슐의 기제가 젤라틴, 플루란, 히프로멜로오스 및 폴리비닐알코올로 이루어진 군에서 선택되는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 제제는 제 1 입자부와 제 2 입자부가 물리적으로 분리된 상태로 캡슐 내 충진 되어 있는 것을 특징으로 하는, 경구투여 제제.
상기 제 1 입자부 및 제 2 입자부가 각각 희석제, 붕해제, 결합제, 활택제 및 이의 혼합물로 이루어진 군에서 선택되는 약학적으로 허용 가능한 첨가제를 추가로 포함하는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 미니정제가 코팅층을 추가로 포함하는 것을 특징으로 하는, 경구투여용 약학 제제.
상기 알레르기성 비염이 비루, 비폐색, 비소양증, 재채기 및 안구소양증으로 이루어진 군에서 선택되는 것을 특징으로 하는, 경구투여용 약학 제제.
ii) 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 약학적으로 허용가능한 첨가제와 혼합한 후 타정하여 정제화하는 단계; 및
iii) 상기 단계 i)에서 제조된 레보세티리진 정제 및 단계 ii)에서 제조된 몬테루카스트 정제를 경질 캡슐에 충전하는 단계를 포함하는, 캡슐제제의 제조방법.
상기 단계 i) 또는 ii)에서 정제를 코팅하는 단계를 추가로 포함하는 것을 특징으로 하는, 제조방법.
Priority Applications (21)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020120001954A KR101418404B1 (ko) | 2012-01-06 | 2012-01-06 | 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 |
JOP/2013/0004A JO3388B1 (ar) | 2012-01-06 | 2013-01-03 | تركيبة دوائية ثابتة للإعطاء عن طريق الفم تضم ليفوسيتيريزين أو ملح منه مقبول دوائياً، و منتولوكاست أو ملح منه مقبول دوائياً |
PT137337895T PT2800558T (pt) | 2012-01-06 | 2013-01-04 | Formulação farmacêutica estável para administração oral compreendendo levocetirizina ou um sal farmaceuticamente aceitável da mesma, e montelukast ou um sal farmaceuticamente aceitável do mesmo |
ARP130100039A AR089666A1 (es) | 2012-01-06 | 2013-01-04 | Formulacion farmaceutica estable para administracion oral que comprende levocetirizina o una de sus sales aceptables desde el punto de vista farmaceutico, y montelukast o una de sus sales aceptables desde el punto de vista farmaceutico |
SI201331005T SI2800558T1 (en) | 2012-01-06 | 2013-01-04 | A stable pharmaceutical formulation for oral administration comprising levocetirizines or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
BR112014016472-0A BR112014016472B1 (pt) | 2012-01-06 | 2013-01-04 | Formulação farmacêutica estável para administração oral que compreende levocetirizina e montelukast ou seus sais, método para preparar uma formulação em cápsula e formulação em cápsula |
MX2014008059A MX354073B (es) | 2012-01-06 | 2013-01-04 | Formulacion farmaceutica estable para administracion oral que comprende levocetirizina o una de sus sales aceptables desde el punto de vista farmaceutico, y montelukast o una de sus sales aceptables desde el punto de vista farmaceutico. |
TW102100251A TWI565482B (zh) | 2012-01-06 | 2013-01-04 | 包含左旋西替利(levocetirizine)或其藥學上可接受鹽以及蒙特魯卡斯特(montelukast)或其藥學上可接受鹽之供經口投藥的穩定藥學調配物 |
RU2014132428A RU2614382C2 (ru) | 2012-01-06 | 2013-01-04 | Стабильная фармацевтическая композиция для перорального введения, включающая левоцетиризин или его фармацевтически приемлимую соль, и монтелукаст или его фармацевтически приемлимую соль |
CN201380004854.0A CN104039314B (zh) | 2012-01-06 | 2013-01-04 | 含有左旋西替利或其药用盐和孟鲁司特或其药用盐的用于口服给药的稳定的药物制剂 |
ES13733789.5T ES2671428T3 (es) | 2012-01-06 | 2013-01-04 | Formulación farmacéutica estable para administración oral, que comprende levocetirizina o una sal farmacéuticamente aceptable de la misma y montelukast o una sal farmacéuticamente aceptable del mismo |
PCT/KR2013/000057 WO2013103262A1 (en) | 2012-01-06 | 2013-01-04 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
EP13733789.5A EP2800558B1 (en) | 2012-01-06 | 2013-01-04 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
PL13733789T PL2800558T3 (pl) | 2012-01-06 | 2013-01-04 | Stabilna formulacja farmaceutyczna do podawania doustnego zawierająca lewocetyryzynę lub jej farmaceutycznie dopuszczalną sól i montelukast lub jego farmaceutycznie dopuszczalną sól |
TR2018/07978T TR201807978T4 (tr) | 2012-01-06 | 2013-01-04 | Levosetirizin veya bunun farmasötik olarak kabul edilebilen bir tuzunu ve montelukast veya bunun farmasötik olarak kabul edilebilen bir tuzunu içeren oral uygulama için stabil farmasötik formülasyon. |
US14/370,258 US9486528B2 (en) | 2012-01-06 | 2013-01-04 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
SG11201403811VA SG11201403811VA (en) | 2012-01-06 | 2013-01-04 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
JP2014551191A JP6163165B2 (ja) | 2012-01-06 | 2013-01-04 | レボセチリジンまたはその医薬的に許容される塩およびモンテルカストまたはその医薬的に許容される塩を含む経口投与用安定医薬製剤 |
PH12014501545A PH12014501545B1 (en) | 2012-01-06 | 2014-07-03 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
ZA2014/05756A ZA201405756B (en) | 2012-01-06 | 2014-08-05 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
HK15100824.5A HK1200337A1 (en) | 2012-01-06 | 2015-01-23 | Stable pharmaceutical formulation for oral administration comprising levocetirizine or a pharmaceutically acceptable salt thereof, and montelukast or a pharmaceutically acceptable salt thereof |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020120001954A KR101418404B1 (ko) | 2012-01-06 | 2012-01-06 | 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1020140053473A Division KR101843086B1 (ko) | 2014-05-02 | 2014-05-02 | 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 |
Publications (2)
Publication Number | Publication Date |
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KR20130081013A true KR20130081013A (ko) | 2013-07-16 |
KR101418404B1 KR101418404B1 (ko) | 2014-07-10 |
Family
ID=48745292
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Application Number | Title | Priority Date | Filing Date |
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KR1020120001954A KR101418404B1 (ko) | 2012-01-06 | 2012-01-06 | 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 함유하는 안정한 경구투여용 약학 제제 |
Country Status (21)
Country | Link |
---|---|
US (1) | US9486528B2 (ko) |
EP (1) | EP2800558B1 (ko) |
JP (1) | JP6163165B2 (ko) |
KR (1) | KR101418404B1 (ko) |
CN (1) | CN104039314B (ko) |
AR (1) | AR089666A1 (ko) |
BR (1) | BR112014016472B1 (ko) |
ES (1) | ES2671428T3 (ko) |
HK (1) | HK1200337A1 (ko) |
JO (1) | JO3388B1 (ko) |
MX (1) | MX354073B (ko) |
PH (1) | PH12014501545B1 (ko) |
PL (1) | PL2800558T3 (ko) |
PT (1) | PT2800558T (ko) |
RU (1) | RU2614382C2 (ko) |
SG (1) | SG11201403811VA (ko) |
SI (1) | SI2800558T1 (ko) |
TR (1) | TR201807978T4 (ko) |
TW (1) | TWI565482B (ko) |
WO (1) | WO2013103262A1 (ko) |
ZA (1) | ZA201405756B (ko) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20160004482A (ko) * | 2014-07-02 | 2016-01-13 | 한미약품 주식회사 | 몬테루카스트 또는 이의 약제학적으로 허용가능한 염의 경구투여용 액상제제 |
KR102481517B1 (ko) * | 2021-08-30 | 2022-12-27 | 주식회사 클라시아 | 약제학적 제제 |
WO2023068839A1 (ko) * | 2021-10-21 | 2023-04-27 | 한화제약주식회사 | 몬테루카스트 또는 이의 약학적으로 허용가능한 염 및 레보세티리진 또는 이의 약학적으로 허용가능한 염을 함유하는 안정성이 개선된 필름코팅 정제 |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106456535B (zh) * | 2014-04-25 | 2020-07-03 | R.P.谢勒技术有限公司 | 稳定的孟鲁司特溶液 |
JP6575031B2 (ja) * | 2014-07-28 | 2019-09-18 | 日本ケミファ株式会社 | モンテルカストナトリウム製剤 |
RU2580303C1 (ru) * | 2015-02-18 | 2016-04-10 | Общество с ограниченной ответственностью "ПРОФИТ ФАРМ" | Состав таблетированной формы лекарственного средства с действующим веществом пророксан |
PL3222279T3 (pl) | 2016-03-21 | 2022-05-09 | Invest Bielany Spółka Z Ograniczoną Odpowiedzialnością | Doustny preparat farmaceutyczny montelukastu i lewocetyryzyny oraz sposób jego wytwarzania |
KR20240045586A (ko) | 2022-09-30 | 2024-04-08 | 주식회사 제뉴원사이언스 | 레보세티리진 또는 이의 약학적으로 허용가능한 염 및 몬테루카스트 또는 이의 약학적으로 허용가능한 염을 포함하는 안정성이 향상된 이층정 정제 및 그의 제조방법 |
Family Cites Families (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1204580A (en) | 1968-10-05 | 1970-09-09 | Aspro Nicholas Ltd | Pharmaceutical dosage forms |
DK154078C (da) | 1981-02-06 | 1989-05-22 | Ucb Sa | Analogifremgangsmaade til fremstilling af 2-(2-(4-(diphenyl-methyl)-1-piperazinyl)ethoxy)-acetamider eller syreadditionssalte heraf |
US4800162A (en) | 1987-04-01 | 1989-01-24 | Sepracor, Inc. | Method for resolution of steroisomers in multiphase and extractive membrane reactors |
US5057427A (en) | 1988-04-07 | 1991-10-15 | Sepracor, Inc. | Method for resolution of stereoisomers |
GB8827391D0 (en) | 1988-11-23 | 1988-12-29 | Ucb Sa | Process for preparation of 2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-pipera-zinyl)ethoxy)-acetic acid & its dihydrochloride |
GB8827390D0 (en) | 1988-11-23 | 1988-12-29 | Ucb Sa | Process for preparation of 2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-pipera-zinyl)ethoxy)-acetic acid & its dihydrochloride |
DE4209824A1 (de) | 1991-09-06 | 1993-03-11 | Schaeffler Waelzlager Kg | Waelzlager fuer linearbewegungen |
GB9305282D0 (en) | 1993-03-15 | 1993-05-05 | Ucb Sa | Enantiomers of 1-(4-chlorophenyl)phenylmethyl)-4-(4-methylphenyl)sulphonyl)piperazine |
BE1010094A3 (fr) | 1996-04-10 | 1997-12-02 | Ucb Sa | Nouveaux [2-(1-piperazinyl)ethoxy] methyle substitues. |
BE1010095A3 (fr) | 1996-04-10 | 1997-12-02 | Ucb Sa | Procede de preparation de l'acide 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl] ethoxy]-acetique et de ses sels. |
DE10007203A1 (de) * | 2000-02-17 | 2001-08-23 | Asta Medica Ag | Neue Kombination nichtsedierender Antihistaminika mit Substanzen, die die Leukotrienwirkung beeinflussen, zur Behandlung der Rhinitis/Konjunktivitis |
WO2001078697A2 (en) | 2000-04-12 | 2001-10-25 | Merck Frosst Canada & Co. | Method and compositions for the treatment of allergic conditions using pgd2 receptor antagonists |
KR100795419B1 (ko) | 2006-01-03 | 2008-01-17 | (주)네오메딕스 | 암로디핀 및 아스피린을 함유하는 약학 제제 |
KR100910848B1 (ko) * | 2007-09-13 | 2009-08-06 | 재단법인서울대학교산학협력재단 | 알러지성 비염 치료약물을 유효성분으로 함유하는 비강분무용 마이크로스피어 및 이의 제조방법 |
WO2010107404A1 (en) * | 2009-03-16 | 2010-09-23 | Mahmut Bilgic | Stable pharmaceutical combinations |
KR20130009553A (ko) * | 2011-07-15 | 2013-01-23 | 한미약품 주식회사 | 몬테루카스트 또는 이의 약학적으로 허용가능한 염 및 레보세티리진 또는 이의 약학적으로 허용가능한 염을 함유하는 캡슐 제제 |
KR101861307B1 (ko) * | 2011-10-13 | 2018-07-06 | 한미약품 주식회사 | 정제를 포함하는 경질 캡슐 복합 제형 |
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2012
- 2012-01-06 KR KR1020120001954A patent/KR101418404B1/ko active IP Right Grant
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2013
- 2013-01-03 JO JOP/2013/0004A patent/JO3388B1/ar active
- 2013-01-04 TW TW102100251A patent/TWI565482B/zh not_active IP Right Cessation
- 2013-01-04 US US14/370,258 patent/US9486528B2/en active Active
- 2013-01-04 JP JP2014551191A patent/JP6163165B2/ja not_active Expired - Fee Related
- 2013-01-04 ES ES13733789.5T patent/ES2671428T3/es active Active
- 2013-01-04 RU RU2014132428A patent/RU2614382C2/ru not_active IP Right Cessation
- 2013-01-04 AR ARP130100039A patent/AR089666A1/es not_active Application Discontinuation
- 2013-01-04 BR BR112014016472-0A patent/BR112014016472B1/pt active IP Right Grant
- 2013-01-04 CN CN201380004854.0A patent/CN104039314B/zh active Active
- 2013-01-04 EP EP13733789.5A patent/EP2800558B1/en active Active
- 2013-01-04 SI SI201331005T patent/SI2800558T1/en unknown
- 2013-01-04 PL PL13733789T patent/PL2800558T3/pl unknown
- 2013-01-04 MX MX2014008059A patent/MX354073B/es active IP Right Grant
- 2013-01-04 PT PT137337895T patent/PT2800558T/pt unknown
- 2013-01-04 TR TR2018/07978T patent/TR201807978T4/tr unknown
- 2013-01-04 SG SG11201403811VA patent/SG11201403811VA/en unknown
- 2013-01-04 WO PCT/KR2013/000057 patent/WO2013103262A1/en active Application Filing
-
2014
- 2014-07-03 PH PH12014501545A patent/PH12014501545B1/en unknown
- 2014-08-05 ZA ZA2014/05756A patent/ZA201405756B/en unknown
-
2015
- 2015-01-23 HK HK15100824.5A patent/HK1200337A1/xx not_active IP Right Cessation
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20160004482A (ko) * | 2014-07-02 | 2016-01-13 | 한미약품 주식회사 | 몬테루카스트 또는 이의 약제학적으로 허용가능한 염의 경구투여용 액상제제 |
KR102481517B1 (ko) * | 2021-08-30 | 2022-12-27 | 주식회사 클라시아 | 약제학적 제제 |
WO2023068839A1 (ko) * | 2021-10-21 | 2023-04-27 | 한화제약주식회사 | 몬테루카스트 또는 이의 약학적으로 허용가능한 염 및 레보세티리진 또는 이의 약학적으로 허용가능한 염을 함유하는 안정성이 개선된 필름코팅 정제 |
Also Published As
Publication number | Publication date |
---|---|
BR112014016472B1 (pt) | 2022-03-15 |
BR112014016472A8 (pt) | 2017-07-04 |
PT2800558T (pt) | 2018-06-05 |
RU2614382C2 (ru) | 2017-03-24 |
CN104039314A (zh) | 2014-09-10 |
JO3388B1 (ar) | 2019-03-13 |
SG11201403811VA (en) | 2014-08-28 |
ZA201405756B (en) | 2016-08-31 |
EP2800558A1 (en) | 2014-11-12 |
TW201332590A (zh) | 2013-08-16 |
ES2671428T3 (es) | 2018-06-06 |
US20140356422A1 (en) | 2014-12-04 |
JP2015503579A (ja) | 2015-02-02 |
CN104039314B (zh) | 2017-07-14 |
MX354073B (es) | 2018-02-12 |
AR089666A1 (es) | 2014-09-10 |
MX2014008059A (es) | 2014-10-06 |
TWI565482B (zh) | 2017-01-11 |
JP6163165B2 (ja) | 2017-07-12 |
SI2800558T1 (en) | 2018-06-29 |
PH12014501545A1 (en) | 2014-10-08 |
PH12014501545B1 (en) | 2014-10-08 |
EP2800558B1 (en) | 2018-04-11 |
PL2800558T3 (pl) | 2018-08-31 |
WO2013103262A1 (en) | 2013-07-11 |
TR201807978T4 (tr) | 2018-06-21 |
HK1200337A1 (en) | 2015-08-07 |
US9486528B2 (en) | 2016-11-08 |
KR101418404B1 (ko) | 2014-07-10 |
BR112014016472A2 (pt) | 2017-06-13 |
RU2014132428A (ru) | 2016-02-27 |
EP2800558A4 (en) | 2015-08-12 |
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