US20050008692A1 - Compositions comprising pectin and ascorbic acid - Google Patents
Compositions comprising pectin and ascorbic acid Download PDFInfo
- Publication number
- US20050008692A1 US20050008692A1 US10/488,451 US48845104A US2005008692A1 US 20050008692 A1 US20050008692 A1 US 20050008692A1 US 48845104 A US48845104 A US 48845104A US 2005008692 A1 US2005008692 A1 US 2005008692A1
- Authority
- US
- United States
- Prior art keywords
- pectin
- weight
- composition according
- ascorbic acid
- composition
- 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.)
- Abandoned
Links
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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
-
- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
Definitions
- the present invention relates to a composition in the form of a powder and/or granules, which contain as principal components L-ascorbic acid and/or a pharmaceutically acceptable salt thereof, and high molecular pectin.
- the composition according to the present invention is directly compressible into tablets with good taste, improved mechanical strength and hardness, with excellent color stability and is free of sugar and starch.
- the addition of adjuvants and excipients to the composition for producing tablets is optional.
- compositions comprising L-ascorbic acid and/or a pharmaceutically acceptable salt thereof and pectin, as well as tablets manufactured using such compositions have been described in European Patent Application No.1 110 550 A2.
- tablets manufactured using a composition comprising L-ascorbic acid and/or its salts, and high molecular pectin show improved hardness as compared to tablets manufactured using conventional pectin of lower molecular weight.
- the invention relates to a composition in the form of a powder or granules comprising:
- high molecular pectin denotes pectin having an average molecular weight of about 300 kDalton or higher.
- the preferred high molecular pectins are those having an average molecular weight of from about 300 kDalton to about 400 kDalton, particularly 350 kDalton.
- Such pectins can be obtained as disclosed in U.S. Pat. No. 6,143,337 (inventors: Marshall L. Fishman and Hoa K. Chau, assignors to The United States of America as represented by the Secretary of Agriculture) the contents of which is incorporated herein by reference.
- the average molecular weight is determined by size exclusion chromatography having a multi angle laser light scattering detector as described in U.S. Pat.
- pectins of higher molecular weight e.g. up to 2000 kDalton can be used also in the present invention.
- Pectins of such molecular weight can be obtained e.g. from Asteraceae plants, especially cichory and Jerusalem artichoke, see International patent application WO 99/03892.
- Fractions of the desired high molecular weight can be obtained from such pectins by membrane filtration, e.g. using polyethersulfone or composite regenerate cellulose membranes as supplied by Millipore Corporation, Bedford, Mass. 01730, USA, under the trade name Pellicon® Tangential Flow Filtration Cassettes.
- the high molecular pectin is preferably used in quantities within the range of about 0.1% to about 10% by weight, preferably in quantities of about 0.5% to about 5% by weight and most preferably in quantities of about 0.5% to about 2% by weight, calculated to the total weight of the composition thereof.
- Adjuvants may optionally be added. Suitable adjuvants are for example starch, HPMC, polyols. Preferably no adjuvants are added.
- composition of this invention may be produced by any method known per se for the production of powders or granules. Preferred are fluidized-bed granulation, high-shear granulation, extrusion, spray-drying and wet granulation.
- composition of the present invention by spray-drying it is convenient to prepare an aqueous slurry of all the components.
- the slurry has preferably a solid content of about 10 to 70% by weight, and preferably about 30 to 70% by weight.
- the slurry is then spray-dried in a manner known per se.
- a known fluidized-bed granulating apparatus which comprises a fluidized-bed drying device fitted with spray means.
- the L-ascorbic acid and/or a pharmaceutically acceptable salt thereof form the fluidized bed, which is fluidized by air or an inert gas, e.g. nitrogen.
- the granulating process is continued until the desired amount of the pectin binder has been deposited onto the fluidized particles.
- the granules are sieved to remove the fractions of granules which are either too large or too small.
- the particle size of the granules is within 100 and 1000 micron, more preferably between 125 and 850 microns. While the so-obtained granules are substantially dry they may contain a very small percentage of water depending on the amount of pectin. For 1% pectin, the moisture content is about 0.2% or less. For 5% pectin, the moisture content may be as high as 1%.
- the composition thus obtained may be compressed into tablets with conventional tabletting methods and machinery.
- the powder or the granules may further be mixed with a lubricant or a mixture of lubricants and then compressed into tablets.
- additional lubricant it is preferably selected from the group of stearic acid or the magnesium or calcium salt thereof, or glyceryl behenate 45 (Compritol 888 ATO), preferably in an amount of about 0.5 to 4% by weight, calculated to the total weight of the composition.
- the composition may be mixed with excipients. Examples for excipients are dextrinized sucrose (Di Pac sugar), microcrystalline cellulose or starch.
- a single tablet as obtained according to the present invention contains preferably 50 mg to 1500 mg, preferably 500 mg to 1000 mg of L-ascorbic acid and/or the pharmaceutically acceptable salt thereof, corresponding to an appropriate daily doses of vitamin C.
- the following Example illustrates the invention further.
- pectins having different molecular weight were investigated. One had an average molecular weight of 200 kDalton (USP/100, lot 02635-0, CP Kelco, San Diego, USA) and another had an average molecular weight of about 350 kDalton. The 350 kDalton pectin was a sample from the United States Department of Agriculture and was prepared by the process disclosed in U.S. Pat. No. 6,143,337.
- a 1.9% pectin solution was prepared by dissolving pectin in water.
- Sodium ascorbate powder F. Hoffmann—La Roche AG, Switzerland, Ave. particle size ca. 50 microns
- was placed in a Glatt Fluidized-Bed granulator Model Uniglatt, Switzerland
- the granulation conditions were as follows:
- the granules had a particle size distribution as shown in Table 1.
- the granules (125-850 micron fraction) were mixed with the excipients as shown in Table 2 and then compressed into 700-mg tablets with a diameter of 12 mm to tablets of various thickness. The hardness of the tablets was determined and is shown in Table 3.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nutrition Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12/378,306 US8242096B2 (en) | 2001-09-03 | 2009-02-13 | Compositions comprising pectin and ascorbic acid |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP011210671 | 2001-09-03 | ||
EP01121067 | 2001-09-03 | ||
PCT/EP2002/009484 WO2003020265A2 (en) | 2001-09-03 | 2002-08-24 | Compositions comprising pectin and ascorbic acid |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US12/378,306 Continuation US8242096B2 (en) | 2001-09-03 | 2009-02-13 | Compositions comprising pectin and ascorbic acid |
Publications (1)
Publication Number | Publication Date |
---|---|
US20050008692A1 true US20050008692A1 (en) | 2005-01-13 |
Family
ID=8178509
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US10/488,451 Abandoned US20050008692A1 (en) | 2001-09-03 | 2002-08-24 | Compositions comprising pectin and ascorbic acid |
US12/378,306 Expired - Lifetime US8242096B2 (en) | 2001-09-03 | 2009-02-13 | Compositions comprising pectin and ascorbic acid |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US12/378,306 Expired - Lifetime US8242096B2 (en) | 2001-09-03 | 2009-02-13 | Compositions comprising pectin and ascorbic acid |
Country Status (13)
Country | Link |
---|---|
US (2) | US20050008692A1 (es) |
EP (1) | EP1423109B1 (es) |
JP (1) | JP4339685B2 (es) |
KR (1) | KR100628603B1 (es) |
CN (2) | CN1549710A (es) |
AT (1) | ATE307579T1 (es) |
BR (1) | BRPI0212195B8 (es) |
CA (1) | CA2458209C (es) |
DE (1) | DE60206940T2 (es) |
DK (1) | DK1423109T3 (es) |
ES (1) | ES2250711T3 (es) |
MX (1) | MXPA04001768A (es) |
WO (1) | WO2003020265A2 (es) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110039945A1 (en) * | 2007-10-29 | 2011-02-17 | Dsm Ip Assets B.V. | Compositions containing resveratrol and pectin |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7494669B2 (en) * | 2001-02-28 | 2009-02-24 | Carrington Laboratories, Inc. | Delivery of physiological agents with in-situ gels comprising anionic polysaccharides |
CN101119720B (zh) | 2005-02-15 | 2013-01-23 | 帝斯曼知识产权资产管理有限公司 | 包含多糖的组合物 |
CN101074270B (zh) * | 2006-05-17 | 2010-09-22 | 烟台安德利果胶有限公司 | 高分子苹果果胶的生产工艺 |
US20110083493A1 (en) * | 2008-06-11 | 2011-04-14 | The Curators Of The University Of Missouri | Liquid Chromatography Detector and Flow Controller Therefor |
JP5975453B2 (ja) * | 2008-11-14 | 2016-08-23 | 株式会社 アスキー | 多糖類の抽出方法 |
CZ302789B6 (cs) | 2009-11-25 | 2011-11-09 | Zentiva, K. S. | Zpusob zvýšení rozpustnosti farmaceuticky aktivních látek a cílený (kontrolovaný) transport do streva |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4983583A (en) * | 1987-10-21 | 1991-01-08 | Sanofi, Societe Anonyme | Granulated compositions of polysaccharides, process for their preparation and use |
US6004582A (en) * | 1997-05-30 | 1999-12-21 | Laboratorios Phoenix U.S.A, Inc. | Multi-layered osmotic device |
US6143337A (en) * | 1999-04-30 | 2000-11-07 | The United States Of America As Represented By The Secretary Of Agriculture | Extraction of pectin by microwave heating under pressure |
US6974832B2 (en) * | 1999-12-22 | 2005-12-13 | Dsm Nutritional Products Inc. | L-ascorbic acid and pectin composition |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3312594A (en) | 1963-06-21 | 1967-04-04 | Squibb & Sons Inc | Longlasting troche |
US3453368A (en) | 1966-01-13 | 1969-07-01 | Hoffmann La Roche | Smaller high potency compressed tablets of ascorbic acid |
US3490742A (en) | 1966-01-14 | 1970-01-20 | Staley Mfg Co A E | Compressed tablets |
US3459863A (en) | 1966-10-14 | 1969-08-05 | Merck & Co Inc | Color-stable ascorbic acid tablet |
US3615591A (en) | 1968-10-21 | 1971-10-26 | Pet Inc | Method of making a peanut butter - jelly product |
FR2036890B1 (es) | 1969-04-15 | 1973-01-12 | Orsymonde | |
DE2017373A1 (de) | 1969-04-15 | 1971-04-22 | Orsymonde S A , Paris | Lyophihsierte Produkte und Ver fahren zu ihrer Herstellung |
US3946110A (en) | 1974-05-30 | 1976-03-23 | Peter, Strong Research And Development Company, Inc. | Medicinal compositions and methods of preparing the same |
US4225628A (en) | 1979-04-30 | 1980-09-30 | Ben Hill Griffin, Inc. | Citrus fiber additive product and process for making same |
JPS5759803A (en) | 1980-09-30 | 1982-04-10 | Takeda Chem Ind Ltd | Granule of l-sodium ascorbate, its preparation, and tablet comprising it |
DE3209630A1 (de) | 1982-03-17 | 1983-09-29 | Opekta-GmbH & Co., 5000 Köln | Diaetetisches mittel, verfahren zu seiner herstellungund seine verwendung zur regulierung des cholesterinspiegels im serum |
US5008254A (en) | 1982-09-03 | 1991-04-16 | Weibel Michael K | Sugar beet pectins and their use in comestibles |
US4605666A (en) | 1983-10-24 | 1986-08-12 | Basf Corporation | Process for preparing spray-dried powders containing a water-soluble vitamin and powders prepared thereby |
US4533674A (en) | 1983-10-24 | 1985-08-06 | Basf Wyandotte Corporation | Process for preparing a sugar and starch free spray-dried vitamin C powder containing 90 percent ascorbic acid |
DE4200821A1 (de) | 1992-01-15 | 1993-07-22 | Bayer Ag | Geschmacksmaskierte pharmazeutische mittel |
RU2008015C1 (ru) * | 1992-04-10 | 1994-02-28 | Нина Павловна Максютина | Способ получения витаминного средства "витапектин" |
US6210710B1 (en) | 1997-04-28 | 2001-04-03 | Hercules Incorporated | Sustained release polymer blend for pharmaceutical applications |
DE19733094A1 (de) | 1997-07-31 | 1999-02-04 | Merck Patent Gmbh | Formulierung auf der Basis von Ascorbinsäure mit verbesserter Farbstabilität |
DE19744473A1 (de) | 1997-10-09 | 1999-04-15 | Basf Ag | Verwendung von wasserlöslichen oder wasserdispergierbaren Polyurethanen als Überzugsmittel oder Bindemittel für pharmazeutische Darreichungsformen |
US6060078A (en) | 1998-09-28 | 2000-05-09 | Sae Han Pharm Co., Ltd. | Chewable tablet and process for preparation thereof |
-
2002
- 2002-08-24 DE DE60206940T patent/DE60206940T2/de not_active Expired - Lifetime
- 2002-08-24 CA CA2458209A patent/CA2458209C/en not_active Expired - Lifetime
- 2002-08-24 CN CNA028170598A patent/CN1549710A/zh active Pending
- 2002-08-24 DK DK02774534T patent/DK1423109T3/da active
- 2002-08-24 MX MXPA04001768A patent/MXPA04001768A/es active IP Right Grant
- 2002-08-24 EP EP02774534A patent/EP1423109B1/en not_active Expired - Lifetime
- 2002-08-24 CN CN200910142584A patent/CN101653421A/zh active Pending
- 2002-08-24 JP JP2003524572A patent/JP4339685B2/ja not_active Expired - Fee Related
- 2002-08-24 WO PCT/EP2002/009484 patent/WO2003020265A2/en active IP Right Grant
- 2002-08-24 US US10/488,451 patent/US20050008692A1/en not_active Abandoned
- 2002-08-24 BR BR0212195-6 patent/BRPI0212195B8/pt not_active IP Right Cessation
- 2002-08-24 ES ES02774534T patent/ES2250711T3/es not_active Expired - Lifetime
- 2002-08-24 AT AT02774534T patent/ATE307579T1/de not_active IP Right Cessation
- 2002-08-24 KR KR1020047003110A patent/KR100628603B1/ko active IP Right Grant
-
2009
- 2009-02-13 US US12/378,306 patent/US8242096B2/en not_active Expired - Lifetime
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4983583A (en) * | 1987-10-21 | 1991-01-08 | Sanofi, Societe Anonyme | Granulated compositions of polysaccharides, process for their preparation and use |
US6004582A (en) * | 1997-05-30 | 1999-12-21 | Laboratorios Phoenix U.S.A, Inc. | Multi-layered osmotic device |
US6143337A (en) * | 1999-04-30 | 2000-11-07 | The United States Of America As Represented By The Secretary Of Agriculture | Extraction of pectin by microwave heating under pressure |
US6974832B2 (en) * | 1999-12-22 | 2005-12-13 | Dsm Nutritional Products Inc. | L-ascorbic acid and pectin composition |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110039945A1 (en) * | 2007-10-29 | 2011-02-17 | Dsm Ip Assets B.V. | Compositions containing resveratrol and pectin |
US8535724B2 (en) * | 2007-10-29 | 2013-09-17 | Dsm Ip Assets B.V. | Compositions containing resveratrol and pectin |
Also Published As
Publication number | Publication date |
---|---|
CA2458209C (en) | 2010-11-09 |
DE60206940D1 (de) | 2005-12-01 |
MXPA04001768A (es) | 2004-11-22 |
DK1423109T3 (da) | 2005-12-27 |
EP1423109B1 (en) | 2005-10-26 |
CN101653421A (zh) | 2010-02-24 |
BRPI0212195B1 (pt) | 2018-02-14 |
EP1423109A2 (en) | 2004-06-02 |
CN1549710A (zh) | 2004-11-24 |
ATE307579T1 (de) | 2005-11-15 |
WO2003020265A3 (en) | 2003-09-04 |
JP2005502676A (ja) | 2005-01-27 |
US8242096B2 (en) | 2012-08-14 |
KR100628603B1 (ko) | 2006-09-26 |
JP4339685B2 (ja) | 2009-10-07 |
US20090227536A1 (en) | 2009-09-10 |
KR20040036927A (ko) | 2004-05-03 |
DE60206940T2 (de) | 2006-04-20 |
BRPI0212195B8 (pt) | 2021-05-25 |
CA2458209A1 (en) | 2003-03-13 |
WO2003020265A2 (en) | 2003-03-13 |
BR0212195A (pt) | 2004-10-05 |
ES2250711T3 (es) | 2006-04-16 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
AS | Assignment |
Owner name: ROCHE VITAMINS AG, SWITZERLAND Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:CHEN, CHYI-CHENG;LEUENBERGER, BRUNO;REEL/FRAME:015945/0455 Effective date: 20011009 |
|
AS | Assignment |
Owner name: DSM IP ASSETS B.V., NETHERLANDS Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:ROCHE VITAMINS INC.;REEL/FRAME:015418/0141 Effective date: 20040419 Owner name: DSM IP ASSETS B.V.,NETHERLANDS Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:ROCHE VITAMINS INC.;REEL/FRAME:015418/0141 Effective date: 20040419 |
|
STCB | Information on status: application discontinuation |
Free format text: ABANDONED -- FAILURE TO RESPOND TO AN OFFICE ACTION |