KR890009377A - 방출 조절된 카비도파/레보도파 배합물 - Google Patents
방출 조절된 카비도파/레보도파 배합물 Download PDFInfo
- Publication number
- KR890009377A KR890009377A KR1019880016416A KR880016416A KR890009377A KR 890009377 A KR890009377 A KR 890009377A KR 1019880016416 A KR1019880016416 A KR 1019880016416A KR 880016416 A KR880016416 A KR 880016416A KR 890009377 A KR890009377 A KR 890009377A
- Authority
- KR
- South Korea
- Prior art keywords
- soluble polymer
- formulation
- carbidopa
- levodopa
- water soluble
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 12
- IVTMXOXVAHXCHI-YXLMWLKOSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid;(2s)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 IVTMXOXVAHXCHI-YXLMWLKOSA-N 0.000 title claims 3
- 230000001105 regulatory effect Effects 0.000 title claims 2
- 229940052036 carbidopa / levodopa Drugs 0.000 title 1
- 229920000642 polymer Polymers 0.000 claims description 9
- 229920003169 water-soluble polymer Polymers 0.000 claims 12
- 238000009472 formulation Methods 0.000 claims 11
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 6
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 6
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 6
- 229960004205 carbidopa Drugs 0.000 claims 6
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical compound NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims 6
- 229920001577 copolymer Polymers 0.000 claims 6
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 6
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 6
- 229960004502 levodopa Drugs 0.000 claims 6
- 229920002554 vinyl polymer Polymers 0.000 claims 6
- 239000001856 Ethyl cellulose Substances 0.000 claims 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 2
- 239000004698 Polyethylene Substances 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- 229920002301 cellulose acetate Polymers 0.000 claims 2
- 229920001249 ethyl cellulose Polymers 0.000 claims 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims 2
- 239000005038 ethylene vinyl acetate Substances 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- 229920000609 methyl cellulose Polymers 0.000 claims 2
- 239000001923 methylcellulose Substances 0.000 claims 2
- 235000010981 methylcellulose Nutrition 0.000 claims 2
- 229920001200 poly(ethylene-vinyl acetate) Polymers 0.000 claims 2
- 229920003229 poly(methyl methacrylate) Polymers 0.000 claims 2
- -1 polyethylene Polymers 0.000 claims 2
- 229920000573 polyethylene Polymers 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 239000004926 polymethyl methacrylate Substances 0.000 claims 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 2
- 239000004800 polyvinyl chloride Substances 0.000 claims 2
- 229920000915 polyvinyl chloride Polymers 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 239000000375 suspending agent Substances 0.000 claims 2
- VSKCCZIUZNTICH-ZPYUXNTASA-N (e)-but-2-enoic acid;ethenyl acetate Chemical group C\C=C\C(O)=O.CC(=O)OC=C VSKCCZIUZNTICH-ZPYUXNTASA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 239000011118 polyvinyl acetate Substances 0.000 claims 1
- 229920002689 polyvinyl acetate Polymers 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000011159 matrix material Substances 0.000 description 7
- 229940079593 drug Drugs 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 239000007788 liquid Substances 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000003628 erosive effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 매트릭스 내에 균일하게 분산된 약제성분 1을 보여주는 정제-형의 균질한 중합체 매트릭스의 횡단면도.
제2도는 완곡한 미세공 채널 2내로 액체가 침투된 후, 동일 채널의 경로를 통해 약제 용액이 방출됨으로써, 일부 약제가 확산에 의해 운반된 상태의 중합체 매트릭스 1의 개략도이다(이 매트릭스는 약제 성분이 운반되는 동안 반드시 원형을 유지한다)
제3도는 제제가 액체에 의해 침식되어 중합체 1 및 활성성분 2가 용질 또는 현탁질로서 유액중에 분산됨으로써 일부 약제가 운반된 후의, 중합체 매트릭스 1의 개략 횡단면도.
제3a도는 약제 2 모두가 침식에 의해 거의 운반된 후의, 중합체 매트릭스 1의 개략도(이 매트릭스는 그의 약제 성분이 운반되는 동안 완전히 붕해된다)
Claims (10)
- 하이드록시프로필 셀룰로오즈, 하이드록시프로필 메틸 셀룰로오즈, 폴리비닐 피롤리돈, 폴리에틸렌 글리콜, 전분 및 메틸 셀룰로오즈 중에서 선택된 수용성 중합체 0내지 120mg 및 폴리비닐 아세테이트-크로톤산 공중합체, 폴리비닐 클로라이드, 폴리에틸렌, 셀룰로오즈 아세테이트, 폴리비닐 알코올, 에틸렌 비닐 아세테이트 공중합체, 필리비닐 아세테이트, 폴리매틸 메타크릴레이트, 및 에틸 셀룰로오즈 중에서 선택된 약 수용성 중합체 0내지 120mg을 함유하며, 단, 양 중합체가 모두 0mg이 아닌 중합체 비히클 중에, 카비도파 5내지 300mg, 레보도파 20내지 1200mg, 정제 활탁제 0내지 25mg및 임의의 약제학적으로 허용되는 염료의 균일한 현탁액이 함유되어 있음으로써, 정제의 투여 후 카비도파 및 레보도파를 제제로부터 서서히 동시 방출함을 특징으로 하는 방출 조절성 경구 투여용 제제.
- 제1항에 있어서, 중합체 비히클이 수용성 중합체와 약 수용성 중합체와의 배합물인 제제.
- 제2항에 있어서, 수용성 중합체가 하이드록시 프로필 셀룰로오즈이고 약 수용성 중합체가 폴리비닐 아세테이트-크로톤산 공중합체인 제제.
- 제3항에 있어서, 하이드록시프로필 셀룰로오즈가 클루셀(Klucel)LF이고 폴리비닐 아세테이트-크로톤산 공중합체가 비낙크(Vinac)ASB-516인 제제.
- 제4항에 있어서, 레보도파 200mg 및 카비도파50mg, 또는 레보도파 100mg 및 카비도파 25mg을 함유하는 제제.
- 제1항에 있어서, 하이드록시프로필 셀룰로오즈, 하이드록시프로필메틸셀룰로오즈, 폴리비닐 피로릴돈, 폴리에틸렌 글리콜, 전분 및 메틸 셀룰로오즈 중에서 선택된 수용성 중합체 5내지 25mg 및 폴리비닐 아세테이트-크로톤산 공중합체, 폴리비닐 클로라이드, 폴리에틸렌, 셀룰로오즈 아세테이트, 폴리비닐 알코올, 에틸렌 비닐아세테이트 공중합체, 폴리비닐 아세테이트, 폴리매틸 메타크릴레이트, 및 에틸 셀룰로오즈 중에서 선택된 약 수용성 중합체 2내지 50mg을 함유하는 중합체 비히클 중에 카비도파 25내지 100mg, 레보도파 100내지 400mg, 정제 활탁제 1내지 10mg및 임의의 약제학적으로 허용되는 염료의 균일한 분산액이 함유되어 있음으로써, 제제의 투여 후 카비도파 및 레보도파를 제제로부터 서서히 동시 방출하는 제제.
- 제6항에 있어서, 중합체 비히클이 수용성 중합체와 약 수용성 중합체와의 배합물인 제제.
- 제7항에 있어서, 수용성 중합체가 하이드록시 프로필 셀룰로오즈이고 약 수용성 중합체가 폴리비닐 아세테이트-크로톤산 공중합체인 제제.
- 제8항에 있어서, 하이드록시프로필 셀룰로오즈가 클루셀 LF이고 폴리비닐 아세테이트-크로톤산 공중합체가 비낙크 ASB-516인 제제.
- 제4항에 있어서, 레보도파 200mg 및 카비도파 50mg, 또는 레보도파 100mg 및 카비도파 25mg을 함유하는 제제.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13160187A | 1987-12-11 | 1987-12-11 | |
US131,601 | 1987-12-11 | ||
US223861 | 1988-07-25 | ||
US07/223,861 US4832957A (en) | 1987-12-11 | 1988-07-25 | Controlled release combination of carbidopa/levodopa |
Publications (1)
Publication Number | Publication Date |
---|---|
KR890009377A true KR890009377A (ko) | 1989-08-01 |
Family
ID=26829626
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880016416A KR890009377A (ko) | 1987-12-11 | 1988-12-10 | 방출 조절된 카비도파/레보도파 배합물 |
Country Status (15)
Country | Link |
---|---|
US (1) | US4832957A (ko) |
EP (1) | EP0320051B1 (ko) |
JP (1) | JPH0667830B2 (ko) |
KR (1) | KR890009377A (ko) |
AT (1) | ATE81970T1 (ko) |
AU (1) | AU616449B2 (ko) |
CA (1) | CA1318602C (ko) |
DE (1) | DE3875705T2 (ko) |
DK (1) | DK170515B1 (ko) |
ES (1) | ES2052691T3 (ko) |
GR (1) | GR3006220T3 (ko) |
HK (1) | HK7997A (ko) |
IE (1) | IE61547B1 (ko) |
IL (1) | IL88563A0 (ko) |
PT (1) | PT89157B (ko) |
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US4983400A (en) * | 1986-06-16 | 1991-01-08 | Merck & Co., Inc. | Controlled release combination of carbidopa/levodopa |
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US5601835A (en) * | 1987-04-29 | 1997-02-11 | Massachusetts Institute Of Technology | Polymeric device for controlled drug delivery to the CNS |
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US5006344A (en) * | 1989-07-10 | 1991-04-09 | E. R. Squibb & Sons, Inc. | Fosinopril tablet formulations |
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-
1988
- 1988-07-25 US US07/223,861 patent/US4832957A/en not_active Expired - Lifetime
- 1988-12-02 DE DE8888202760T patent/DE3875705T2/de not_active Expired - Lifetime
- 1988-12-02 ES ES88202760T patent/ES2052691T3/es not_active Expired - Lifetime
- 1988-12-02 EP EP88202760A patent/EP0320051B1/en not_active Expired - Lifetime
- 1988-12-02 IL IL88563A patent/IL88563A0/xx unknown
- 1988-12-02 AT AT88202760T patent/ATE81970T1/de not_active IP Right Cessation
- 1988-12-05 PT PT89157A patent/PT89157B/pt not_active IP Right Cessation
- 1988-12-08 JP JP63309001A patent/JPH0667830B2/ja not_active Expired - Lifetime
- 1988-12-09 DK DK685888A patent/DK170515B1/da not_active IP Right Cessation
- 1988-12-09 CA CA000585578A patent/CA1318602C/en not_active Expired - Lifetime
- 1988-12-09 AU AU26733/88A patent/AU616449B2/en not_active Expired
- 1988-12-09 IE IE367988A patent/IE61547B1/en not_active IP Right Cessation
- 1988-12-10 KR KR1019880016416A patent/KR890009377A/ko not_active Application Discontinuation
-
1992
- 1992-11-12 GR GR920402556T patent/GR3006220T3/el unknown
-
1997
- 1997-01-16 HK HK7997A patent/HK7997A/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
AU616449B2 (en) | 1991-10-31 |
JPH0667830B2 (ja) | 1994-08-31 |
DK685888D0 (da) | 1988-12-09 |
JPH02209A (ja) | 1990-01-05 |
GR3006220T3 (ko) | 1993-06-21 |
DK170515B1 (da) | 1995-10-09 |
ES2052691T3 (es) | 1994-07-16 |
HK7997A (en) | 1997-01-24 |
CA1318602C (en) | 1993-06-01 |
DK685888A (da) | 1989-07-25 |
IL88563A0 (en) | 1989-07-31 |
PT89157A (pt) | 1989-12-29 |
US4832957A (en) | 1989-05-23 |
IE61547B1 (en) | 1994-11-16 |
ATE81970T1 (de) | 1992-11-15 |
EP0320051A1 (en) | 1989-06-14 |
DE3875705T2 (de) | 1993-05-13 |
AU2673388A (en) | 1989-06-15 |
PT89157B (pt) | 1993-06-30 |
IE883679L (en) | 1989-06-11 |
DE3875705D1 (de) | 1992-12-10 |
EP0320051B1 (en) | 1992-11-04 |
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