ZA200104828B - Cyclosporin solution. - Google Patents
Cyclosporin solution. Download PDFInfo
- Publication number
- ZA200104828B ZA200104828B ZA200104828A ZA200104828A ZA200104828B ZA 200104828 B ZA200104828 B ZA 200104828B ZA 200104828 A ZA200104828 A ZA 200104828A ZA 200104828 A ZA200104828 A ZA 200104828A ZA 200104828 B ZA200104828 B ZA 200104828B
- Authority
- ZA
- South Africa
- Prior art keywords
- cyclosporin
- weight
- solution
- solution according
- diluent
- Prior art date
Links
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 title claims description 79
- 108010036949 Cyclosporine Proteins 0.000 title claims description 77
- 229930105110 Cyclosporin A Natural products 0.000 title claims description 74
- 229960001265 ciclosporin Drugs 0.000 title claims description 73
- 229930182912 cyclosporin Natural products 0.000 title claims description 53
- 239000002736 nonionic surfactant Substances 0.000 claims description 29
- 239000000203 mixture Substances 0.000 claims description 26
- 239000003945 anionic surfactant Substances 0.000 claims description 23
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 claims description 20
- 235000004866 D-panthenol Nutrition 0.000 claims description 20
- 239000011703 D-panthenol Substances 0.000 claims description 20
- 229960003949 dexpanthenol Drugs 0.000 claims description 20
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 18
- 239000002775 capsule Substances 0.000 claims description 15
- 239000003085 diluting agent Substances 0.000 claims description 14
- -1 glycerol-polyethylene Chemical group 0.000 claims description 10
- 239000007903 gelatin capsule Substances 0.000 claims description 8
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 8
- 229920000053 polysorbate 80 Polymers 0.000 claims description 8
- 239000002202 Polyethylene glycol Substances 0.000 claims description 7
- 229920001223 polyethylene glycol Polymers 0.000 claims description 7
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 7
- 229940068968 polysorbate 80 Drugs 0.000 claims description 7
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 6
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 6
- 229940100688 oral solution Drugs 0.000 claims description 6
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 6
- 206010062016 Immunosuppression Diseases 0.000 claims description 3
- 230000001506 immunosuppresive effect Effects 0.000 claims description 3
- 239000000243 solution Substances 0.000 description 44
- 238000009472 formulation Methods 0.000 description 11
- 238000010521 absorption reaction Methods 0.000 description 10
- 239000004480 active ingredient Substances 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 7
- 239000008280 blood Substances 0.000 description 7
- 210000004369 blood Anatomy 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 5
- 239000003995 emulsifying agent Substances 0.000 description 5
- 241000282472 Canis lupus familiaris Species 0.000 description 4
- 239000004530 micro-emulsion Substances 0.000 description 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
- 229940063121 neoral Drugs 0.000 description 3
- 238000001556 precipitation Methods 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 3
- 108010036941 Cyclosporins Proteins 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 230000036765 blood level Effects 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 229940100242 glycol stearate Drugs 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- GVJHHUAWPYXKBD-IEOSBIPESA-N (R)-alpha-Tocopherol Natural products OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- SHBUUTHKGIVMJT-UHFFFAOYSA-N Hydroxystearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OO SHBUUTHKGIVMJT-UHFFFAOYSA-N 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 229940087168 alpha tocopherol Drugs 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 235000005687 corn oil Nutrition 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 229940072106 hydroxystearate Drugs 0.000 description 1
- 230000028993 immune response Effects 0.000 description 1
- 238000003018 immunoassay Methods 0.000 description 1
- 229960003444 immunosuppressant agent Drugs 0.000 description 1
- 230000001861 immunosuppressant effect Effects 0.000 description 1
- 239000003018 immunosuppressive agent Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000002050 international nonproprietary name Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- UZRHZMLMNXWFBW-UHFFFAOYSA-N n-(3-hydroxypropyl)-3,3-dimethylbutanamide Chemical compound CC(C)(C)CC(=O)NCCCO UZRHZMLMNXWFBW-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- 239000008389 polyethoxylated castor oil Substances 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000001593 sorbitan monooleate Substances 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
- 229940035049 sorbitan monooleate Drugs 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 150000003712 vitamin E derivatives Chemical class 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19859910A DE19859910C2 (de) | 1998-12-23 | 1998-12-23 | Orales Arzneimittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200104828B true ZA200104828B (en) | 2002-09-13 |
Family
ID=7892567
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200104828A ZA200104828B (en) | 1998-12-23 | 2001-06-13 | Cyclosporin solution. |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1140135B1 (sk) |
| JP (1) | JP2002533401A (sk) |
| AT (1) | ATE249834T1 (sk) |
| AU (1) | AU762963B2 (sk) |
| CA (1) | CA2355271A1 (sk) |
| CZ (1) | CZ20012143A3 (sk) |
| DE (2) | DE19859910C2 (sk) |
| DK (1) | DK1140135T3 (sk) |
| ES (1) | ES2203235T3 (sk) |
| HK (1) | HK1037140A1 (sk) |
| HU (1) | HUP0104623A3 (sk) |
| NO (1) | NO20012932D0 (sk) |
| PL (1) | PL348180A1 (sk) |
| PT (1) | PT1140135E (sk) |
| RU (1) | RU2216342C2 (sk) |
| SK (1) | SK8702001A3 (sk) |
| WO (1) | WO2000038702A1 (sk) |
| ZA (1) | ZA200104828B (sk) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102008060549A1 (de) | 2008-12-04 | 2010-06-10 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Wirkstoff-Peptid-Konstrukt zur extrazellulären Anreicherung |
| DE102009037551A1 (de) | 2009-08-17 | 2011-02-24 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Cyclosporinderivate |
| DE102011111991A1 (de) | 2011-08-30 | 2013-02-28 | Lead Discovery Center Gmbh | Neue Cyclosporin-Derivate |
| US8957048B2 (en) | 2011-10-06 | 2015-02-17 | Allergan, Inc. | Compositions for the treatment of dry eye |
| US9907826B2 (en) | 2011-12-07 | 2018-03-06 | Allergan, Inc. | Efficient lipid delivery to human tear film using a salt-sensitive emulsion system |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8903804D0 (en) * | 1989-02-20 | 1989-04-05 | Sandoz Ltd | Improvements in or relating to organic compounds |
| US4996193A (en) * | 1989-03-03 | 1991-02-26 | The Regents Of The University Of California | Combined topical and systemic method of administration of cyclosporine |
| DK0813865T3 (da) * | 1993-04-20 | 2001-11-19 | Hexal Ag | Plaster med virksomt stof |
| US5603951A (en) * | 1994-11-09 | 1997-02-18 | Hanmi Pharm. Ind. Co., Ltd. | Cyclosporin-containing soft capsule compositions |
| US5798333A (en) * | 1996-09-17 | 1998-08-25 | Sherman; Bernard C. | Water-soluble concentrates containing cyclosporins |
| CZ301382B6 (cs) * | 1997-03-12 | 2010-02-10 | Abbott Laboratories Chad377/Ap6D-2 | Hydrofilní binární systémy pro podávání cyklosporinu |
-
1998
- 1998-12-23 DE DE19859910A patent/DE19859910C2/de not_active Expired - Fee Related
-
1999
- 1999-12-23 RU RU2001120359/14A patent/RU2216342C2/ru not_active IP Right Cessation
- 1999-12-23 AT AT99964670T patent/ATE249834T1/de not_active IP Right Cessation
- 1999-12-23 EP EP99964670A patent/EP1140135B1/de not_active Expired - Lifetime
- 1999-12-23 ES ES99964670T patent/ES2203235T3/es not_active Expired - Lifetime
- 1999-12-23 HU HU0104623A patent/HUP0104623A3/hu unknown
- 1999-12-23 JP JP2000590654A patent/JP2002533401A/ja active Pending
- 1999-12-23 DK DK99964670T patent/DK1140135T3/da active
- 1999-12-23 CZ CZ20012143A patent/CZ20012143A3/cs unknown
- 1999-12-23 PT PT99964670T patent/PT1140135E/pt unknown
- 1999-12-23 CA CA002355271A patent/CA2355271A1/en not_active Abandoned
- 1999-12-23 WO PCT/EP1999/010358 patent/WO2000038702A1/de not_active Application Discontinuation
- 1999-12-23 PL PL99348180A patent/PL348180A1/xx unknown
- 1999-12-23 SK SK870-2001A patent/SK8702001A3/sk unknown
- 1999-12-23 AU AU30434/00A patent/AU762963B2/en not_active Ceased
- 1999-12-23 DE DE59907058T patent/DE59907058D1/de not_active Expired - Fee Related
-
2001
- 2001-06-13 NO NO20012932A patent/NO20012932D0/no not_active Application Discontinuation
- 2001-06-13 ZA ZA200104828A patent/ZA200104828B/en unknown
- 2001-11-07 HK HK01107803A patent/HK1037140A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU3043400A (en) | 2000-07-31 |
| WO2000038702A1 (de) | 2000-07-06 |
| DE59907058D1 (en) | 2003-10-23 |
| CZ20012143A3 (cs) | 2002-01-16 |
| DE19859910A1 (de) | 2000-06-29 |
| ATE249834T1 (de) | 2003-10-15 |
| NO20012932L (no) | 2001-06-13 |
| EP1140135B1 (de) | 2003-09-17 |
| HUP0104623A2 (hu) | 2002-04-29 |
| NO20012932D0 (no) | 2001-06-13 |
| HUP0104623A3 (en) | 2002-08-28 |
| EP1140135A1 (de) | 2001-10-10 |
| SK8702001A3 (en) | 2002-01-07 |
| PL348180A1 (en) | 2002-05-06 |
| HK1037140A1 (en) | 2002-02-01 |
| DE19859910C2 (de) | 2001-03-22 |
| ES2203235T3 (es) | 2004-04-01 |
| PT1140135E (pt) | 2003-12-31 |
| RU2216342C2 (ru) | 2003-11-20 |
| DK1140135T3 (da) | 2003-12-08 |
| JP2002533401A (ja) | 2002-10-08 |
| CA2355271A1 (en) | 2000-07-06 |
| AU762963B2 (en) | 2003-07-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| FI116197B (fi) | Menetelmä farmaseuttisten koostumusten valmistamiseksi vaikeasti liukenevia aktiiviaineita varten | |
| AU737053B2 (en) | Oil-free pharmaceutical compositions containing cyclosporin A | |
| KR100342942B1 (ko) | 카르두스 마리아누스 추출물 또는 이로부터 정제된 실리빈을함유하는 경구용 마이크로에멀젼 조성물 | |
| RU2257917C2 (ru) | Самоэмульгирующиеся композиции для плохорастворимых в воде лекарственных препаратов | |
| FI98046C (fi) | Menetelmä syklosporiinia sisältävän farmaseuttisen koostumuksen valmistamiseksi | |
| CZ301382B6 (cs) | Hydrofilní binární systémy pro podávání cyklosporinu | |
| JP2001505928A (ja) | シクロスポリン及び陰イオン性界面活性剤を含む固体医薬組成物 | |
| KR101025641B1 (ko) | 매스틱 자가유화에멀젼 조성물 및 이를 함유하는 캡슐 | |
| HU225535B1 (en) | Microemulsion pre-concentrate and microemulsion | |
| JP2006206615A (ja) | 経口投与用シクロスポリン含有新規製剤 | |
| KR100308779B1 (ko) | 사이클로스포린을함유한신규조성물 | |
| AU762963B2 (en) | Cyclosporin solution | |
| KR100570450B1 (ko) | 가용성 로바스타틴의 연질캡슐제 조성물 및 그의 제조방법 | |
| JP2006509785A (ja) | ビフェニルジメチルジカルボン酸の経口用マイクロエマルション組成物 | |
| KR100569595B1 (ko) | 가용성 심바스타틴의 연질캡슐제 조성물 및 그의제조방법 | |
| KR100352089B1 (ko) | 페노피브레이트를 함유하는 경구용 마이크로에멀젼 조성물 | |
| KR100341203B1 (ko) | 유성 비타민 함유 약학 조성물 및 이의 제조방법 | |
| AU741923B2 (en) | Pharmaceutical compositions | |
| AP1040A (en) | A novel composition containing cyclosporin. | |
| JP2005255677A (ja) | シクロスポリン製剤 |