JPH08505367A - 医薬用エマルジョン組成物 - Google Patents
医薬用エマルジョン組成物Info
- Publication number
- JPH08505367A JPH08505367A JP6510317A JP51031794A JPH08505367A JP H08505367 A JPH08505367 A JP H08505367A JP 6510317 A JP6510317 A JP 6510317A JP 51031794 A JP51031794 A JP 51031794A JP H08505367 A JPH08505367 A JP H08505367A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- medium
- chain
- oil
- aliphatic acyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- 239000008346 aqueous phase Substances 0.000 claims abstract description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 16
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 78
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 65
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical group CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 50
- 239000003921 oil Substances 0.000 claims description 46
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- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims description 37
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- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 28
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- 239000000194 fatty acid Substances 0.000 claims description 27
- 229930195729 fatty acid Natural products 0.000 claims description 27
- 229940079593 drug Drugs 0.000 claims description 26
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- 238000010587 phase diagram Methods 0.000 claims description 18
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- 125000002252 acyl group Chemical group 0.000 claims description 16
- 125000001931 aliphatic group Chemical group 0.000 claims description 16
- 108010077689 gamma-aminobutyryl-2-methyltryptophyl-2-methyltryptophyl-2-methyltryptophyl-lysinamide Proteins 0.000 claims description 15
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- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 9
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims description 7
- 238000002844 melting Methods 0.000 claims description 7
- 230000008018 melting Effects 0.000 claims description 7
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims description 6
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical group OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 claims description 6
- 150000002190 fatty acyls Chemical group 0.000 claims description 6
- 108060001064 Calcitonin Proteins 0.000 claims description 5
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- GXBMIBRIOWHPDT-UHFFFAOYSA-N Vasopressin Natural products N1C(=O)C(CC=2C=C(O)C=CC=2)NC(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C1CC1=CC=CC=C1 GXBMIBRIOWHPDT-UHFFFAOYSA-N 0.000 claims description 5
- 102000002852 Vasopressins Human genes 0.000 claims description 5
- 108010004977 Vasopressins Proteins 0.000 claims description 5
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 claims description 5
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims description 5
- 229960004015 calcitonin Drugs 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 229940125396 insulin Drugs 0.000 claims description 5
- 150000004667 medium chain fatty acids Chemical class 0.000 claims description 5
- 229960003726 vasopressin Drugs 0.000 claims description 5
- 239000005639 Lauric acid Substances 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 3
- 229910052783 alkali metal Inorganic materials 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 229940088623 biologically active substance Drugs 0.000 claims description 2
- 230000036760 body temperature Effects 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims description 2
- 239000006069 physical mixture Substances 0.000 claims description 2
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims description 2
- JPOKAKNGULMYHZ-UILVTTEASA-N (2s)-6-amino-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-6-amino-2-[[(2s)-2-[[(2s)-6-amino-2-[[(2s)-6-amino-2-[[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-3-(4-hydroxyp Chemical compound C([C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCN=C(N)N)C1=CC=C(O)C=C1 JPOKAKNGULMYHZ-UILVTTEASA-N 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 150000003863 ammonium salts Chemical class 0.000 claims 1
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- 229940126585 therapeutic drug Drugs 0.000 claims 1
- 239000013543 active substance Substances 0.000 abstract description 4
- 235000019198 oils Nutrition 0.000 description 39
- 102000004196 processed proteins & peptides Human genes 0.000 description 31
- GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 description 28
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- 239000008280 blood Substances 0.000 description 21
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- 239000012266 salt solution Substances 0.000 description 15
- 238000000034 method Methods 0.000 description 13
- BYKRNSHANADUFY-UHFFFAOYSA-M sodium octanoate Chemical compound [Na+].CCCCCCCC([O-])=O BYKRNSHANADUFY-UHFFFAOYSA-M 0.000 description 13
- DEGAKNSWVGKMLS-UHFFFAOYSA-N calcein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC(CN(CC(O)=O)CC(O)=O)=C(O)C=C1OC1=C2C=C(CN(CC(O)=O)CC(=O)O)C(O)=C1 DEGAKNSWVGKMLS-UHFFFAOYSA-N 0.000 description 11
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- LDVVMCZRFWMZSG-UHFFFAOYSA-N captan Chemical compound C1C=CCC2C(=O)N(SC(Cl)(Cl)Cl)C(=O)C21 LDVVMCZRFWMZSG-UHFFFAOYSA-N 0.000 description 10
- 150000001875 compounds Chemical class 0.000 description 10
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- 150000004665 fatty acids Chemical class 0.000 description 10
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 10
- 238000012360 testing method Methods 0.000 description 10
- 239000000126 substance Substances 0.000 description 9
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 9
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 8
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 8
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- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 8
- 239000005642 Oleic acid Substances 0.000 description 8
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- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 8
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- 238000010561 standard procedure Methods 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
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- 235000013311 vegetables Nutrition 0.000 description 1
- WHNFPRLDDSXQCL-UAZQEYIDSA-N α-msh Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(N)=O)NC(=O)[C@H](CO)NC(C)=O)C1=CC=C(O)C=C1 WHNFPRLDDSXQCL-UAZQEYIDSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/25—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/23—Calcitonins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/39—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG]
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Dispersion Chemistry (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US96295592A | 1992-10-16 | 1992-10-16 | |
US07/962,955 | 1992-10-16 | ||
PCT/US1993/009916 WO1994008610A1 (fr) | 1992-10-16 | 1993-10-15 | Compositions pour emulsions pharmaceutiques |
Publications (1)
Publication Number | Publication Date |
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JPH08505367A true JPH08505367A (ja) | 1996-06-11 |
Family
ID=25506549
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP6510317A Pending JPH08505367A (ja) | 1992-10-16 | 1993-10-15 | 医薬用エマルジョン組成物 |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP0671937A4 (fr) |
JP (1) | JPH08505367A (fr) |
WO (1) | WO1994008610A1 (fr) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002544155A (ja) * | 1999-05-07 | 2002-12-24 | ファルマソル ゲーエムベーハー | 流体および固体脂質の混合物を基礎とする脂質粒子、およびそれらを製造するための方法 |
JP2004505033A (ja) * | 2000-08-01 | 2004-02-19 | ユニバーシティ オブ フロリダ | 薬物を可溶化するための新規なマイクロエマルジョンおよびミセルシステム |
JP2009538221A (ja) * | 2006-03-31 | 2009-11-05 | エニ、ソシエタ、ペル、アチオニ | 油中水滴及び水中油滴のナノエマルジョンの調製方法 |
JP2010536838A (ja) * | 2007-08-22 | 2010-12-02 | カムルス エービー | 酸含有脂質製剤 |
JP2013500292A (ja) * | 2009-07-30 | 2013-01-07 | エボニック レーム ゲゼルシャフト ミット ベシュレンクテル ハフツング | コポリマー、脂肪モノカルボン酸の塩および脂肪モノカルボン酸および/または脂肪アルコールを含む粉末状または粒状組成物 |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5688761A (en) * | 1991-04-19 | 1997-11-18 | Lds Technologies, Inc. | Convertible microemulsion formulations |
DE69229779T2 (de) * | 1991-04-19 | 1999-12-23 | Lds Technologies, Inc. | Konvertierbare mikroemulsionsverbindungen |
US5948825A (en) * | 1993-04-19 | 1999-09-07 | Institute For Advanced Skin Research Inc. | Microemulsion preparation containing a slightly absorbable substance |
CA2185803C (fr) * | 1994-03-18 | 2006-07-11 | Edward M. Rudnic | Systemes d'administration de medicaments emulsionnes |
US6790435B1 (en) | 1999-10-01 | 2004-09-14 | Unilever Home & Personal Care Usa Division Of Conopco, Inc. | Antiperspirant compositions comprising microemulsions |
IT1318539B1 (it) * | 2000-05-26 | 2003-08-27 | Italfarmaco Spa | Composizioni farmaceutiche a rilascio prolungato per lasomministrazione parenterale di sostanze idrofile biologicamente |
EP1414497A4 (fr) * | 2001-08-08 | 2007-11-21 | Univ Florida | Nouveaux systemes de micelles et de micro-emulsions pour la solubilisation de medicaments |
WO2005016312A1 (fr) | 2003-08-13 | 2005-02-24 | Nobex Corporation | Formulation de dosage de solides de sels d'acides gras destinee a des agents therapeutiques |
US8492369B2 (en) | 2010-04-12 | 2013-07-23 | Clarus Therapeutics Inc | Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same |
RU2429850C2 (ru) | 2005-04-15 | 2011-09-27 | Кларус Терапьютикс, Инк. | Фармацевтические системы доставки для гидрофобных лекарственных средств и композиций, их содержащих |
EP1787658B1 (fr) | 2005-11-10 | 2012-03-14 | CHEMI S.p.A. | Formulations à libération prolongée contenant des inhibiteurs de l'hormone de croissance analogues de la somatostatine |
EP1961412A1 (fr) | 2006-12-27 | 2008-08-27 | LEK Pharmaceuticals D.D. | Systèmes auto-microémulsifiants pour l'administration de médicaments |
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WO2019161263A1 (fr) * | 2018-02-16 | 2019-08-22 | Ohio State Innovation Foundation | Nanoparticules de lipide-tensioactif pour l'administration de médicament, et leurs procédés de fabrication et d'utilisation |
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GB1171125A (en) * | 1966-06-08 | 1969-11-19 | Glaxo Lab Ltd | Improvements in or relating to Injectable Preparations |
US4146499A (en) * | 1976-09-18 | 1979-03-27 | Rosano Henri L | Method for preparing microemulsions |
FR2502951B1 (fr) * | 1981-04-06 | 1985-12-06 | Sandoz Sa | Compositions pharmaceutiques topiques sous forme d'une micro-emulsion |
DE3406497A1 (de) * | 1984-02-23 | 1985-09-05 | Mueller Bernhard Willi Werner | Hochdisperse pharmazeutische mehrkomponentensysteme und verfahren zu ihrer herstellung |
IE60024B1 (en) * | 1987-02-03 | 1994-05-18 | Stiefel Laboratories Ltd | Microemulsions |
DE3908047A1 (de) * | 1989-03-13 | 1990-09-20 | Desitin Arzneimittel Gmbh | Hochdisperse pharmazeutische zusammensetzung |
CA2083711A1 (fr) * | 1990-06-08 | 1991-12-09 | Seang H. Yiv | Procede pour la preparation de micro-emulsion |
DE69229779T2 (de) * | 1991-04-19 | 1999-12-23 | Lds Technologies, Inc. | Konvertierbare mikroemulsionsverbindungen |
-
1993
- 1993-10-15 JP JP6510317A patent/JPH08505367A/ja active Pending
- 1993-10-15 WO PCT/US1993/009916 patent/WO1994008610A1/fr not_active Application Discontinuation
- 1993-10-15 EP EP93923918A patent/EP0671937A4/fr not_active Withdrawn
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2002544155A (ja) * | 1999-05-07 | 2002-12-24 | ファルマソル ゲーエムベーハー | 流体および固体脂質の混合物を基礎とする脂質粒子、およびそれらを製造するための方法 |
JP2004505033A (ja) * | 2000-08-01 | 2004-02-19 | ユニバーシティ オブ フロリダ | 薬物を可溶化するための新規なマイクロエマルジョンおよびミセルシステム |
JP2009538221A (ja) * | 2006-03-31 | 2009-11-05 | エニ、ソシエタ、ペル、アチオニ | 油中水滴及び水中油滴のナノエマルジョンの調製方法 |
JP2010536838A (ja) * | 2007-08-22 | 2010-12-02 | カムルス エービー | 酸含有脂質製剤 |
JP2013500292A (ja) * | 2009-07-30 | 2013-01-07 | エボニック レーム ゲゼルシャフト ミット ベシュレンクテル ハフツング | コポリマー、脂肪モノカルボン酸の塩および脂肪モノカルボン酸および/または脂肪アルコールを含む粉末状または粒状組成物 |
Also Published As
Publication number | Publication date |
---|---|
EP0671937A1 (fr) | 1995-09-20 |
EP0671937A4 (fr) | 1996-09-18 |
WO1994008610A1 (fr) | 1994-04-28 |
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