WO1999026606A2 - SUSTAINED RELEASE FORMULATIONS COMPRISING α-GLUCOSIDASE-INHIBITORS - Google Patents
SUSTAINED RELEASE FORMULATIONS COMPRISING α-GLUCOSIDASE-INHIBITORS Download PDFInfo
- Publication number
- WO1999026606A2 WO1999026606A2 PCT/EP1998/007198 EP9807198W WO9926606A2 WO 1999026606 A2 WO1999026606 A2 WO 1999026606A2 EP 9807198 W EP9807198 W EP 9807198W WO 9926606 A2 WO9926606 A2 WO 9926606A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pharmaceutical formulation
- acarbose
- sustained release
- formulation according
- inhibitors
- Prior art date
Links
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
-
- 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
- A61K31/13—Amines
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Definitions
- Acarbose is the first compound on the market of a new class of oral antidiabetic drugs, the alpha-glucosidase inhibitors. After oral administration, it competitively inhibits alpha-glucosidases, which are located in the brush-border membrane of the small intestine. As a consequence, the digestion of disaccharides, oligosaccharides and polysaccharides to monosaccharides is retarded, which delays the postprandial absorption of glucose. Thus, excessive postprandial rises of blood glucose as observed in inadequately treated diabetes patients are reduced and 24-hour blood glucose profiles smoothed.
- oral administration of an alpha-glucosidase inhibitor may result in a greater portion of dietary carbohydrates reaching the colon undigested. These carbohydrates may then be fermented by the intestinal flora resulting in an increased formation of intestinal gas, which may cause gastrointestinal adverse events such as meteorism, flatulence or diarrhoea.
- acarbose approximately 50% and 15% of the patients report flatulence and diarrhoea, respectively, compared to 18% and 5%, respectively, after treatment with placebo.
- the present invention relates to a new better tolerable formulation principle for alpha-glucosidase inhibitors based on sustained release characteristics.
- the invention relates to new pharmaceutical dosage forms of alpha glucosidase inhibitors (formulations and manufacturing processes).
- the formulations are distinguished by a delayed release of the active drug.
- Alpha glucosidase inhibitors can be used for example for the treatment of diabetes mellitus prevention of diabetes and treatment of atheriosclerosis or obesity.
- Examples for this class of drug substances are Acarbose, Noglibose, Miglitol and Emiglitate possibly in combination with other pharmaceuticals as for example sulphonyl urea (glibenelamid, tolbutamid, glimeperide) or with an insulin sensitizer (graglitazone, prioglitazone) or a biguanide (methformin).
- compositions with a sustained release of alpha glucosidase inhibitors can be formulated based on different galenic principles and therefore comprising different excipients.
- matrix building agents can be used Hydroxypropyl Methylcellulose, Hydroxy- ethyl Cellulose, Hydroxypropyl Cellulose, Methylcellulose, Xanthan Gum, Chitosan, Alginic Acid Sodium Salt or Carboxymethylcellulose Sodium e.g 2.
- Lipophilic matrix systems :
- matrix building agents can be used different kinds of wax, glycerides or polymers (Ethylcellulose, Polyvinyl Chloride, Methacrylic Acid Copolymers and the esters thereof e.g.).
- Swelling excipients that can be used are Hydroxypropyl Methylcellulose, Hydroxypropyl Cellulose or Methylcellulose. CO 2 forming additives like Sodium Carbonate can be used.
- the drug substance can be released from the dosage form within a time period of 30 minutes up to 4 hours in a linear or non linear manner.
- sustained release formulations show a dissolution of 80% of the drug substance within a time period longer than 30 minutes (dissolution method: USP basket method, 100 rpm, water).
- formulations can be manufactured as tablets, capsules, pellets, powders or liquids.
- Suitable manufacturing methods are direct compression, compression following a granulation step, formation of pellets using extrusion/spheronization or generated by a fluidized bed process (Wurster process e.g.).
- the tablets can be compressed as monolayer tablets, bilayer tablets or coat core tablets.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Claims
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU12343/99A AU1234399A (en) | 1997-11-25 | 1998-11-11 | Sustained release formulations comprising alpha-glucosidase-i nhibitors |
JP2000521808A JP2001523704A (en) | 1997-11-25 | 1998-11-11 | Sustained release formulation comprising an α-glucosidase inhibitor |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US6669897P | 1997-11-25 | 1997-11-25 | |
US60/066,698 | 1997-11-25 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO1999026606A2 true WO1999026606A2 (en) | 1999-06-03 |
WO1999026606A3 WO1999026606A3 (en) | 1999-08-12 |
Family
ID=22071124
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP1998/007198 WO1999026606A2 (en) | 1997-11-25 | 1998-11-11 | SUSTAINED RELEASE FORMULATIONS COMPRISING α-GLUCOSIDASE-INHIBITORS |
Country Status (5)
Country | Link |
---|---|
JP (1) | JP2001523704A (en) |
AR (1) | AR017664A1 (en) |
AU (1) | AU1234399A (en) |
WO (1) | WO1999026606A2 (en) |
ZA (1) | ZA9810710B (en) |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004014932A1 (en) | 2002-08-08 | 2004-02-19 | Kissei Pharmaceutical Co., Ltd. | Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof |
WO2005085267A1 (en) | 2004-03-04 | 2005-09-15 | Kissei Pharmaceutical Co., Ltd. | Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs |
AU785303B2 (en) * | 2000-05-24 | 2007-01-04 | Pfizer Inc. | Treatment of rumen acidosis with a-amylase inhibitors |
CN102631332A (en) * | 2012-04-28 | 2012-08-15 | 邹立兴 | Voglibose tablet and preparation method thereof |
US8637512B2 (en) | 2002-07-29 | 2014-01-28 | Glaxo Group Limited | Formulations and method of treatment |
CN104013590A (en) * | 2014-05-09 | 2014-09-03 | 万特制药(海南)有限公司 | Acarbose-containing medicinal composition and preparation method thereof |
US9144547B2 (en) | 2002-02-12 | 2015-09-29 | Glaxo Group Limited | Oral dosage form for controlled drug release |
WO2016001843A1 (en) * | 2014-06-30 | 2016-01-07 | Sun Pharmaceutical Industries Limited | Extended-release gastroretentive tablets of voglibose |
CN110898025A (en) * | 2019-12-12 | 2020-03-24 | 湖北欣泽霏药业有限公司 | Acarbose sustained-release preparation and preparation method thereof |
CN111265489A (en) * | 2020-03-10 | 2020-06-12 | 乐普制药科技有限公司 | Divisible acarbose pellet sustained-release tablet |
EP4364743A3 (en) * | 2014-12-17 | 2024-08-28 | Empros Pharma AB | A modified release composition of orlistat and acarbose for the treatment of obesity and related metabolic disorders |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0073428A2 (en) * | 1981-09-01 | 1983-03-09 | Bayer Ag | Medicinal preparations for glycoside-hydrolase inhibitors |
EP0194794A2 (en) * | 1985-03-08 | 1986-09-17 | Takeda Chemical Industries, Ltd. | Saccharide digestion inhibiting composition |
EP0364696A2 (en) * | 1988-08-22 | 1990-04-25 | Takeda Chemical Industries, Ltd. | Alpha-glucosidase inhibitor as a calcium absorption promotor |
EP0610854A1 (en) * | 1993-02-10 | 1994-08-17 | Takeda Chemical Industries, Ltd. | Tablets with improved abrasion resistance and method to produce them |
-
1998
- 1998-11-11 JP JP2000521808A patent/JP2001523704A/en active Pending
- 1998-11-11 AU AU12343/99A patent/AU1234399A/en not_active Abandoned
- 1998-11-11 WO PCT/EP1998/007198 patent/WO1999026606A2/en not_active Application Discontinuation
- 1998-11-24 AR ARP980105946A patent/AR017664A1/en unknown
- 1998-11-24 ZA ZA9810710A patent/ZA9810710B/en unknown
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0073428A2 (en) * | 1981-09-01 | 1983-03-09 | Bayer Ag | Medicinal preparations for glycoside-hydrolase inhibitors |
EP0194794A2 (en) * | 1985-03-08 | 1986-09-17 | Takeda Chemical Industries, Ltd. | Saccharide digestion inhibiting composition |
EP0364696A2 (en) * | 1988-08-22 | 1990-04-25 | Takeda Chemical Industries, Ltd. | Alpha-glucosidase inhibitor as a calcium absorption promotor |
EP0610854A1 (en) * | 1993-02-10 | 1994-08-17 | Takeda Chemical Industries, Ltd. | Tablets with improved abrasion resistance and method to produce them |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU785303B2 (en) * | 2000-05-24 | 2007-01-04 | Pfizer Inc. | Treatment of rumen acidosis with a-amylase inhibitors |
US9144547B2 (en) | 2002-02-12 | 2015-09-29 | Glaxo Group Limited | Oral dosage form for controlled drug release |
US8637512B2 (en) | 2002-07-29 | 2014-01-28 | Glaxo Group Limited | Formulations and method of treatment |
WO2004014932A1 (en) | 2002-08-08 | 2004-02-19 | Kissei Pharmaceutical Co., Ltd. | Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof |
WO2005085267A1 (en) | 2004-03-04 | 2005-09-15 | Kissei Pharmaceutical Co., Ltd. | Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs |
CN102631332A (en) * | 2012-04-28 | 2012-08-15 | 邹立兴 | Voglibose tablet and preparation method thereof |
CN104013590A (en) * | 2014-05-09 | 2014-09-03 | 万特制药(海南)有限公司 | Acarbose-containing medicinal composition and preparation method thereof |
WO2016001843A1 (en) * | 2014-06-30 | 2016-01-07 | Sun Pharmaceutical Industries Limited | Extended-release gastroretentive tablets of voglibose |
EP4364743A3 (en) * | 2014-12-17 | 2024-08-28 | Empros Pharma AB | A modified release composition of orlistat and acarbose for the treatment of obesity and related metabolic disorders |
CN110898025A (en) * | 2019-12-12 | 2020-03-24 | 湖北欣泽霏药业有限公司 | Acarbose sustained-release preparation and preparation method thereof |
CN111265489A (en) * | 2020-03-10 | 2020-06-12 | 乐普制药科技有限公司 | Divisible acarbose pellet sustained-release tablet |
Also Published As
Publication number | Publication date |
---|---|
ZA9810710B (en) | 1999-06-14 |
JP2001523704A (en) | 2001-11-27 |
AU1234399A (en) | 1999-06-15 |
WO1999026606A3 (en) | 1999-08-12 |
AR017664A1 (en) | 2001-09-12 |
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