WO1994008603A1 - Compositions - Google Patents
Compositions Download PDFInfo
- Publication number
- WO1994008603A1 WO1994008603A1 PCT/US1993/009915 US9309915W WO9408603A1 WO 1994008603 A1 WO1994008603 A1 WO 1994008603A1 US 9309915 W US9309915 W US 9309915W WO 9408603 A1 WO9408603 A1 WO 9408603A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- fatty acyl
- hlb surfactant
- chain fatty
- long
- composition
- Prior art date
Links
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] (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
- A61K38/39—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
Definitions
- long-chain fatty acyl refers to a fatty acyl moiety which may be saturated, mono-unsaturated or poly-unsaturated, having from 14 to 22, preferably 14 to 18, carbon atoms which may be branched or unbranched, preferably unbranched, and which may be optionally substituted.
- the blend of low and high HLB surfactants will have an HLB value in the range of from about 7 to about 15.
- the present invention provides compositions in the form of microemulsions comprising a peptide which may be orally admimstered and which will retain biological activity, thereby overcoming the disadvantages of earlier formulations in which the bioavailability of the peptide has been less than satisfactory.
- the present invention provides compositions which by their nature permit the preparation and administration of a peptide in sufficiently high concentration to allow not only convenient oral administration but also adequate bioavailability of the peptide.
- compositions of the present invention may be avoided.
- a mono- or polyhydroxyalcohol co-surfactant such as ethanol, butanol or propylene glycol
- the hydrophilic phase of compositions of the present invention may be essentially aqueous and comprise less than 10%, preferrably less than 5% and more preferrably less than 2% by weight of the phase of an alcohol.
- microemulsions were generally formulated by initially preparing die drug- containing hydrophilic phase, either by dissolving the appropriate amount of drug in the appropriate amount of saline solution or, more preferably, using a stock solution which was then further diluted if so required, with vortex stirring if necessary to obtain complete dissolution.
- the hydrophilic phase containing the drug was then added to die appropriate amounts (by weight) of a mixture of the oil and die low HLB surfactant, to which was then added die high HLB surfactant, with gentle stirring (magnetic hot plate stirrer).
- the hydrophilic phase containing d e drug was added to die high HLB surfactant and following upon complete mixing, this was added to the oil plus low HLB surfactant mixture.
- the drug-containing microemulsion was then diluted witii die corresponding drug-free microemulsion to adjust the concentration of die drug.
- Suitable rats for use in diis assement are male Sprague-Dawley (Caesarian Delivery - Virus Antibody Free; Charles River Laboratories). The rats are fasted overnight the day before the experiment. Dosing with the microemulsion at the desired dose is done by gavage at a volume not exceeding 10 ml/kg. Upon termination of die experiment animals are euthanized with asphyxiation using carbon dioxide and exsanguinated. Abdominal incisions are then performed and gross observations of the gastric and duodenal mucosa are made at naked eyes and under a microscope (Nikon model SMZ-10 binocular microscope).
- a 0.2 ml blood sample is obtained via jugular catheter at the following intervals: -15, 0, 5, 10, 15, 30, 45, 60, 90, and 120 minutes. Blood samples are stored on ice and subsequently analyzed for Growth Hormone by an RIA method.
Abstract
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP93923917A EP0671929A4 (fr) | 1992-10-16 | 1993-10-15 | Compositions. |
JP6510316A JPH08502490A (ja) | 1992-10-16 | 1993-10-15 | 組成物 |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US96295692A | 1992-10-16 | 1992-10-16 | |
US07/962,956 | 1992-10-16 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1994008603A1 true WO1994008603A1 (fr) | 1994-04-28 |
Family
ID=25506551
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1993/009915 WO1994008603A1 (fr) | 1992-10-16 | 1993-10-15 | Compositions |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP0671929A4 (fr) |
JP (1) | JPH08502490A (fr) |
WO (1) | WO1994008603A1 (fr) |
Cited By (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5444041A (en) * | 1991-04-19 | 1995-08-22 | Ibah, Inc. | Convertible microemulsion formulations |
US5583105A (en) * | 1994-11-21 | 1996-12-10 | Biogal Gyogyszerguar Rt | Oral pharmaceutical preparation |
EP0753311A1 (fr) * | 1993-04-19 | 1997-01-15 | Institute For Advanced Skin Research Inc. | Preparation en microemulsion contenant une substance difficilement absorbable |
EP0799620A1 (fr) * | 1996-04-03 | 1997-10-08 | Research Triangle Pharmaceuticals Ltd. | Emulsions à base de cyclosporine |
US5688761A (en) * | 1991-04-19 | 1997-11-18 | Lds Technologies, Inc. | Convertible microemulsion formulations |
WO1998000169A1 (fr) * | 1996-07-02 | 1998-01-08 | Cortecs (Uk) Limited) | Preparations hydrophobes contenant des monoglycerides de chaine moyenne |
WO1999053941A1 (fr) * | 1998-04-15 | 1999-10-28 | Shionogi & Co., Ltd. | Preparations orales contenant des derives de trh |
US6008228A (en) * | 1995-06-06 | 1999-12-28 | Hoffman-La Roche Inc. | Pharmaceutical compositions containing proteinase inhibitors |
US6187993B1 (en) | 1995-02-25 | 2001-02-13 | Imperial Cancer Research Technology Limited | Transgenic animals as model of psoriasis |
WO2001034111A1 (fr) * | 1999-11-08 | 2001-05-17 | The Procter & Gamble Company | Compositions cosmetiques |
US6284268B1 (en) | 1997-12-10 | 2001-09-04 | Cyclosporine Therapeutics Limited | Pharmaceutical compositions containing an omega-3 fatty acid oil |
US6531139B1 (en) * | 1997-07-29 | 2003-03-11 | Pharmacia & Upjohn Company | Self-emulsifying formulation for lipophilic compounds |
WO2003051385A1 (fr) * | 2001-12-14 | 2003-06-26 | Jagotec Ag | Formulation pharmaceutique contenant de la ciclosporine et son utilisation |
US6720001B2 (en) * | 1999-10-18 | 2004-04-13 | Lipocine, Inc. | Emulsion compositions for polyfunctional active ingredients |
KR100508695B1 (ko) * | 2001-02-13 | 2005-08-17 | 한국과학기술연구원 | 인슐린의 경구투여용 제형과 그의 제조방법 |
WO2006024095A1 (fr) | 2004-08-31 | 2006-03-09 | Connetics Australia Pty Ltd | Procede et compositions a base de microemulsion & émulsion submicronique |
US8802087B2 (en) | 2004-03-22 | 2014-08-12 | Abbott Products Gmbh | Pharmaceutical compositions of lipase-containing products, in particular of pancreation |
US9198871B2 (en) | 2005-08-15 | 2015-12-01 | Abbott Products Gmbh | Delayed release pancreatin compositions |
EP3104841A4 (fr) * | 2014-02-14 | 2017-09-06 | Jingjun Huang | Compositions de systèmes de distribution de nano-émulsion |
EP3177262A4 (fr) * | 2014-08-08 | 2018-04-18 | Novan Inc. | Émulsions topiques |
US10072256B2 (en) | 2006-05-22 | 2018-09-11 | Abbott Products Gmbh | Process for separating and determining the viral load in a pancreatin sample |
US10226483B2 (en) | 2013-08-08 | 2019-03-12 | Novan, Inc. | Topical compositions and methods of using the same |
US10704037B2 (en) | 2005-07-29 | 2020-07-07 | Abbott Products Gmbh | Processes for the manufacture and use of pancreatin |
US10912743B2 (en) | 2016-03-02 | 2021-02-09 | Novan, Inc. | Compositions for treating inflammation and methods of treating the same |
US11266607B2 (en) | 2005-08-15 | 2022-03-08 | AbbVie Pharmaceuticals GmbH | Process for the manufacture and use of pancreatin micropellet cores |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2011504871A (ja) * | 2007-06-01 | 2011-02-17 | ノボ・ノルデイスク・エー/エス | 固体又は半固体担体中にペプチド薬剤を含む自然に分散可能なプレコンセントレイト |
EP2910571B1 (fr) | 2008-03-18 | 2016-10-05 | Novo Nordisk A/S | Analogues de l'insuline acylés, stabilisés à la protéase |
CN104364260B (zh) | 2012-04-11 | 2017-02-22 | 诺和诺德股份有限公司 | 胰岛素制剂 |
TWI700092B (zh) | 2016-12-16 | 2020-08-01 | 丹麥商諾佛.儂迪克股份有限公司 | 含胰島素醫藥組成物 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3876765A (en) * | 1968-05-03 | 1975-04-08 | Choay Sa | Pharmaceutical composition containing vitamin b' 12', process of making the same and method of treatment therewith |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4146499A (en) * | 1976-09-18 | 1979-03-27 | Rosano Henri L | Method for preparing microemulsions |
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 |
EP0532703A4 (en) * | 1990-06-08 | 1993-05-26 | Affinity Biotech, Inc. | Process for preparing microemulsion |
EP0580778B1 (fr) * | 1991-04-19 | 1999-08-11 | LDS Technologies, Inc. | Formulations de microemulsions a inversion de phase |
JPH06509577A (ja) * | 1991-07-26 | 1994-10-27 | スミスクライン・ビーチャム・コーポレイション | W/oミクロエマルジョン |
EP0597007B1 (fr) * | 1991-07-26 | 1996-10-16 | Smithkline Beecham Corporation | Micro-emulsion huileuse |
-
1993
- 1993-10-15 JP JP6510316A patent/JPH08502490A/ja active Pending
- 1993-10-15 WO PCT/US1993/009915 patent/WO1994008603A1/fr not_active Application Discontinuation
- 1993-10-15 EP EP93923917A patent/EP0671929A4/fr not_active Withdrawn
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3876765A (en) * | 1968-05-03 | 1975-04-08 | Choay Sa | Pharmaceutical composition containing vitamin b' 12', process of making the same and method of treatment therewith |
Non-Patent Citations (1)
Title |
---|
See also references of EP0671929A4 * |
Cited By (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5633226A (en) * | 1991-04-19 | 1997-05-27 | Lds Technologies, Inc. | Convertible microemulsion formulations |
US5646109A (en) * | 1991-04-19 | 1997-07-08 | Lds Technologies, Inc. | Convertible microemulsion formulations |
US5444041A (en) * | 1991-04-19 | 1995-08-22 | Ibah, Inc. | Convertible microemulsion formulations |
US5688761A (en) * | 1991-04-19 | 1997-11-18 | Lds Technologies, Inc. | Convertible microemulsion formulations |
US5948825A (en) * | 1993-04-19 | 1999-09-07 | Institute For Advanced Skin Research Inc. | Microemulsion preparation containing a slightly absorbable substance |
EP0753311A1 (fr) * | 1993-04-19 | 1997-01-15 | Institute For Advanced Skin Research Inc. | Preparation en microemulsion contenant une substance difficilement absorbable |
EP0753311A4 (fr) * | 1993-04-19 | 1997-05-21 | Inst Advanced Skin Res Inc | Preparation en microemulsion contenant une substance difficilement absorbable |
US5583105A (en) * | 1994-11-21 | 1996-12-10 | Biogal Gyogyszerguar Rt | Oral pharmaceutical preparation |
US6187993B1 (en) | 1995-02-25 | 2001-02-13 | Imperial Cancer Research Technology Limited | Transgenic animals as model of psoriasis |
US6008228A (en) * | 1995-06-06 | 1999-12-28 | Hoffman-La Roche Inc. | Pharmaceutical compositions containing proteinase inhibitors |
EP0799620A1 (fr) * | 1996-04-03 | 1997-10-08 | Research Triangle Pharmaceuticals Ltd. | Emulsions à base de cyclosporine |
WO1998000169A1 (fr) * | 1996-07-02 | 1998-01-08 | Cortecs (Uk) Limited) | Preparations hydrophobes contenant des monoglycerides de chaine moyenne |
US6258377B1 (en) | 1996-07-02 | 2001-07-10 | Provalis Uk Limited | Hydrophobic preparations containing medium chain monoglycerides |
US6531139B1 (en) * | 1997-07-29 | 2003-03-11 | Pharmacia & Upjohn Company | Self-emulsifying formulation for lipophilic compounds |
US6284268B1 (en) | 1997-12-10 | 2001-09-04 | Cyclosporine Therapeutics Limited | Pharmaceutical compositions containing an omega-3 fatty acid oil |
WO1999053941A1 (fr) * | 1998-04-15 | 1999-10-28 | Shionogi & Co., Ltd. | Preparations orales contenant des derives de trh |
US6720001B2 (en) * | 1999-10-18 | 2004-04-13 | Lipocine, Inc. | Emulsion compositions for polyfunctional active ingredients |
WO2001034111A1 (fr) * | 1999-11-08 | 2001-05-17 | The Procter & Gamble Company | Compositions cosmetiques |
KR100508695B1 (ko) * | 2001-02-13 | 2005-08-17 | 한국과학기술연구원 | 인슐린의 경구투여용 제형과 그의 제조방법 |
AU2002231703B2 (en) * | 2001-12-14 | 2007-03-29 | Jagotec Ag | Pharmaceutical formulation comprising cyclosporin and use thereof |
CN100360175C (zh) * | 2001-12-14 | 2008-01-09 | 杰格特克公司 | 包含环孢菌素的药物制剂及其用途 |
CZ302649B6 (cs) * | 2001-12-14 | 2011-08-17 | Jagotec Ag | Farmaceutická formulace zahrnující cyklosporin a její použití |
US8568748B2 (en) | 2001-12-14 | 2013-10-29 | Jagotec Ag | Pharmaceutical formulation comprising cyclosporin and use thereof |
WO2003051385A1 (fr) * | 2001-12-14 | 2003-06-26 | Jagotec Ag | Formulation pharmaceutique contenant de la ciclosporine et son utilisation |
US8802087B2 (en) | 2004-03-22 | 2014-08-12 | Abbott Products Gmbh | Pharmaceutical compositions of lipase-containing products, in particular of pancreation |
WO2006024095A1 (fr) | 2004-08-31 | 2006-03-09 | Connetics Australia Pty Ltd | Procede et compositions a base de microemulsion & émulsion submicronique |
EP2438910A1 (fr) | 2004-08-31 | 2012-04-11 | Stiefel Research Australia Pty Ltd | Procédé et compositions de micro-émulsion et d'émulsion submicronique |
US10704037B2 (en) | 2005-07-29 | 2020-07-07 | Abbott Products Gmbh | Processes for the manufacture and use of pancreatin |
US9198871B2 (en) | 2005-08-15 | 2015-12-01 | Abbott Products Gmbh | Delayed release pancreatin compositions |
US11266607B2 (en) | 2005-08-15 | 2022-03-08 | AbbVie Pharmaceuticals GmbH | Process for the manufacture and use of pancreatin micropellet cores |
US10072256B2 (en) | 2006-05-22 | 2018-09-11 | Abbott Products Gmbh | Process for separating and determining the viral load in a pancreatin sample |
US10206947B2 (en) | 2013-08-08 | 2019-02-19 | Novan, Inc. | Topical compositions and methods of using the same |
US10226483B2 (en) | 2013-08-08 | 2019-03-12 | Novan, Inc. | Topical compositions and methods of using the same |
US10828323B2 (en) | 2013-08-08 | 2020-11-10 | Novan, Inc. | Topical compositions and methods of using the same |
US11813284B2 (en) | 2013-08-08 | 2023-11-14 | Novan, Inc. | Topical compositions and methods of using the same |
EP3104841A4 (fr) * | 2014-02-14 | 2017-09-06 | Jingjun Huang | Compositions de systèmes de distribution de nano-émulsion |
EP3177262A4 (fr) * | 2014-08-08 | 2018-04-18 | Novan Inc. | Émulsions topiques |
US10912743B2 (en) | 2016-03-02 | 2021-02-09 | Novan, Inc. | Compositions for treating inflammation and methods of treating the same |
Also Published As
Publication number | Publication date |
---|---|
EP0671929A4 (fr) | 1996-09-25 |
JPH08502490A (ja) | 1996-03-19 |
EP0671929A1 (fr) | 1995-09-20 |
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