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GB929391A - Therapeutic compositions comprising polymeric amines - Google Patents

Therapeutic compositions comprising polymeric amines

Info

Publication number
GB929391A
GB929391A GB2397859A GB2397859A GB929391A GB 929391 A GB929391 A GB 929391A GB 2397859 A GB2397859 A GB 2397859A GB 2397859 A GB2397859 A GB 2397859A GB 929391 A GB929391 A GB 929391A
Authority
GB
United Kingdom
Prior art keywords
weight
molecular weight
binding
polymer
acrysol
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.)
Expired
Application number
GB2397859A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of GB929391A publication Critical patent/GB929391A/en
Expired legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/74Synthetic polymeric materials
    • A61K31/785Polymers containing nitrogen

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Orally administrable pharmaceutical compositions for binding bile-acids in the gastro-intestinal tract and having blood cholesterol lowering activity comprise a carrier and a synthetic, non-toxic polymer having a skeleton inert to digestive enzymes and a molecular weight in excess of about 3000 and containing ionizable amino groups, the polymer if water-insoluble having the property of binding at least 30% by weight of the available glycocholic acid into a form incapable of dialysis through a cellulose membrane within 5 minutes when exposed to an equal weight of the acid, and having a moisture content of at least 65% after equilibration with air at 100% humidity at 25 DEG C., and, if water-soluble, having an equivalent weight, based on the ionizable amino groups of at least 500 and the property of binding at least 80% of its weight of glycocholic acid in vitro into a form incapable of dialysis through a cellulose membrane. Suitable polymers are divinyl benzene cross-linked polystyrene quaternary ammonium salt resins, e.g. those sold under the Trade Mark "Dowex 1," linear acrylic type quaternary ammonium salt polymers having a molecular weight of the order of 2,000,000, e.g. those sold under the Trade Marks "Acryloid CQ," and "Acrysol CQ," and its tertiary amine salt "Acrysol CA," polyethyleneimine having an average molecular weight of about 30,000 and a co-polymer of acrylamide and vinyl benzene trimethylammonium chloride in a weight ratio of about 30 : 70 having an equivalent weight of about 302 and an average molecular weight of above 100,000. The compositions may be in conventional forms, e.g. a tablet, elixir, syrup or flavoured aqueous solution.
GB2397859A 1958-07-15 1959-07-13 Therapeutic compositions comprising polymeric amines Expired GB929391A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US74859858A 1958-07-15 1958-07-15

Publications (1)

Publication Number Publication Date
GB929391A true GB929391A (en) 1963-06-19

Family

ID=25010129

Family Applications (1)

Application Number Title Priority Date Filing Date
GB2397859A Expired GB929391A (en) 1958-07-15 1959-07-13 Therapeutic compositions comprising polymeric amines

Country Status (2)

Country Link
BE (1) BE580490A (en)
GB (1) GB929391A (en)

Cited By (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4198395A (en) * 1976-05-25 1980-04-15 Etablissement Viridis Novel hypocholesterolemic resin
US4340585A (en) 1978-12-21 1982-07-20 Alfa Farmaceutici, S.P.A. Salified anionic resin for cholesterol and lipid lowering
US4747881A (en) * 1985-02-05 1988-05-31 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4790991A (en) * 1985-02-05 1988-12-13 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4818539A (en) * 1985-02-05 1989-04-04 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4843098A (en) * 1985-02-05 1989-06-27 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4851392A (en) * 1985-02-05 1989-07-25 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4954339A (en) * 1987-12-23 1990-09-04 Smith Kline & French Laboratories Limited Novel polystyrene anion exchange polymers
US5098701A (en) * 1989-12-04 1992-03-24 Smithkline & French Laboratories, Ltd. Crosslinked pyridinomethacrylate polymers
US5110875A (en) * 1989-06-14 1992-05-05 Smith Kline & Franch Laboratories Limited Polystyrene anion exchange polymers
US5112922A (en) * 1989-06-14 1992-05-12 Smith Kline & French Laboratories Polystyrene anion exchange polymers
US5230885A (en) * 1987-12-23 1993-07-27 Smith Kline & French Laboratories Limited Polystyrene anion exchange polymer pharmaceutical composition
US5273740A (en) * 1989-05-22 1993-12-28 Smithkline & French Laboratories Limited Polystyrene anion exchange polymers
US5607669A (en) * 1994-06-10 1997-03-04 Geltex Pharmaceuticals, Inc. Amine polymer sequestrant and method of cholesterol depletion
US5618530A (en) * 1994-06-10 1997-04-08 Geltex Pharmaceuticals, Inc. Hydrophobic amine polymer sequestrant and method of cholesterol depletion
US5624963A (en) * 1993-06-02 1997-04-29 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US5679717A (en) * 1994-06-10 1997-10-21 Geltex Pharmaceuticals, Inc. Method for removing bile salts from a patient with alkylated amine polymers
US5703188A (en) * 1993-06-02 1997-12-30 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US5900475A (en) * 1994-06-10 1999-05-04 Geltex Pharmaceuticals, Inc. Hydrophobic sequestrant for cholesterol depletion
US5929184A (en) * 1993-06-02 1999-07-27 Geltex Pharmaceuticals, Inc. Hydrophilic nonamine-containing and amine-containing copolymers and their use as bile acid sequestrants
US6129910A (en) * 1993-06-02 2000-10-10 Geltex Pharmaceuticals, Inc. Water-insoluble noncrosslinked bile acid sequestrants
US6203785B1 (en) 1996-12-30 2001-03-20 Geltex Pharmaceuticals, Inc. Poly(diallylamine)-based bile acid sequestrants
EP1133989A2 (en) * 1993-08-11 2001-09-19 Geltex Pharmaceuticals, Inc. Polymer compositions for use in therapy
US6423754B1 (en) 1997-06-18 2002-07-23 Geltex Pharmaceuticals, Inc. Method for treating hypercholesterolemia with polyallylamine polymers
US6726905B1 (en) 1997-11-05 2004-04-27 Genzyme Corporation Poly (diallylamines)-based phosphate binders
US7014846B2 (en) 1993-08-11 2006-03-21 Genzyme Corporation Phosphate-binding polymers for oral administration
WO2010079343A2 (en) 2009-01-09 2010-07-15 Cambridge Enterprise Limited Formulations of viable cells for oral delivery
US7985418B2 (en) 2004-11-01 2011-07-26 Genzyme Corporation Aliphatic amine polymer salts for tableting
WO2012064266A1 (en) 2010-11-04 2012-05-18 Albireo Ab Ibat inhibitors for the treatment of liver diseases
WO2012064267A1 (en) 2010-11-08 2012-05-18 Albireo Ab A pharmaceutical combination comprising an ibat inhibitor and a bile acid binder
US8187631B2 (en) 1999-10-19 2012-05-29 Genzyme Corporation Direct compression polymer tablet core
US8986669B2 (en) 2005-09-02 2015-03-24 Genzyme Corporation Method for removing phosphate and polymer used therefore
US9095509B2 (en) 2005-09-15 2015-08-04 Genzyme Corporation Sachet formulation for amine polymers
US10512657B2 (en) 2011-10-28 2019-12-24 Lumena Pharmaceutials Llc Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US11267924B2 (en) 2014-12-18 2022-03-08 Genzyme Corporation Crosslinked polydiallymine copolymers for the treatment of type 2 diabetes
US12145959B2 (en) 2011-10-28 2024-11-19 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease

Cited By (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4198395A (en) * 1976-05-25 1980-04-15 Etablissement Viridis Novel hypocholesterolemic resin
US4340585A (en) 1978-12-21 1982-07-20 Alfa Farmaceutici, S.P.A. Salified anionic resin for cholesterol and lipid lowering
US4747881A (en) * 1985-02-05 1988-05-31 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4790991A (en) * 1985-02-05 1988-12-13 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4818539A (en) * 1985-02-05 1989-04-04 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4843098A (en) * 1985-02-05 1989-06-27 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US4851392A (en) * 1985-02-05 1989-07-25 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
US5230885A (en) * 1987-12-23 1993-07-27 Smith Kline & French Laboratories Limited Polystyrene anion exchange polymer pharmaceutical composition
US4954339A (en) * 1987-12-23 1990-09-04 Smith Kline & French Laboratories Limited Novel polystyrene anion exchange polymers
US5273740A (en) * 1989-05-22 1993-12-28 Smithkline & French Laboratories Limited Polystyrene anion exchange polymers
US5112922A (en) * 1989-06-14 1992-05-12 Smith Kline & French Laboratories Polystyrene anion exchange polymers
US5110875A (en) * 1989-06-14 1992-05-05 Smith Kline & Franch Laboratories Limited Polystyrene anion exchange polymers
US5098701A (en) * 1989-12-04 1992-03-24 Smithkline & French Laboratories, Ltd. Crosslinked pyridinomethacrylate polymers
US5929184A (en) * 1993-06-02 1999-07-27 Geltex Pharmaceuticals, Inc. Hydrophilic nonamine-containing and amine-containing copolymers and their use as bile acid sequestrants
US5624963A (en) * 1993-06-02 1997-04-29 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US5703188A (en) * 1993-06-02 1997-12-30 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US5840766A (en) * 1993-06-02 1998-11-24 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US6129910A (en) * 1993-06-02 2000-10-10 Geltex Pharmaceuticals, Inc. Water-insoluble noncrosslinked bile acid sequestrants
US6060517A (en) * 1993-06-02 2000-05-09 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and compositions therefor
US7459151B2 (en) 1993-08-11 2008-12-02 Genzyme Corporation Phosphate-binding polymers for oral administration
US7014846B2 (en) 1993-08-11 2006-03-21 Genzyme Corporation Phosphate-binding polymers for oral administration
EP1133989A3 (en) * 1993-08-11 2004-05-12 Genzyme Corporation Polymer compositions for use in therapy
EP1133989A2 (en) * 1993-08-11 2001-09-19 Geltex Pharmaceuticals, Inc. Polymer compositions for use in therapy
US6225355B1 (en) 1994-06-10 2001-05-01 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and alkylated compositions therefor
US5607669A (en) * 1994-06-10 1997-03-04 Geltex Pharmaceuticals, Inc. Amine polymer sequestrant and method of cholesterol depletion
US5981693A (en) * 1994-06-10 1999-11-09 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and alkylated compositions therefor
US5919832A (en) * 1994-06-10 1999-07-06 Geltex Pharmaceuticals Inc. Amine polymer sequestrant and method of cholesterol depletion
US6066678A (en) * 1994-06-10 2000-05-23 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and alkylated compositions therefor
US5917007A (en) * 1994-06-10 1999-06-29 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and alkylated compositions therefor
US5969090A (en) * 1994-06-10 1999-10-19 Geltex Pharmaceuticals, Inc. Hydrophobic sequestrant for cholesterol depletion
US5900475A (en) * 1994-06-10 1999-05-04 Geltex Pharmaceuticals, Inc. Hydrophobic sequestrant for cholesterol depletion
US5693675A (en) * 1994-06-10 1997-12-02 Geltex Pharmaceuticals Inc. Alkylated amine polymers
US7399821B2 (en) 1994-06-10 2008-07-15 Genzyme Corporation Alkylated poly(allylamine) polymers and methods of use
US6433026B2 (en) 1994-06-10 2002-08-13 Geltex Pharmaceuticals, Inc. Process for removing bile salts from a patient and alkylated compositions therefor
US7101960B2 (en) 1994-06-10 2006-09-05 Genzyme Corporation Process for removing bile salts from a patient and alkylated compositions therefor
US5618530A (en) * 1994-06-10 1997-04-08 Geltex Pharmaceuticals, Inc. Hydrophobic amine polymer sequestrant and method of cholesterol depletion
US5679717A (en) * 1994-06-10 1997-10-21 Geltex Pharmaceuticals, Inc. Method for removing bile salts from a patient with alkylated amine polymers
US6784254B2 (en) 1994-06-10 2004-08-31 Genzyme Corporation Process for removing bile salts from a patient and alkylated compositions therefor
US6610283B1 (en) 1996-12-30 2003-08-26 Genzyme Corporation Poly(diallylamine)-based bile acid sequestrants
US7125547B2 (en) 1996-12-30 2006-10-24 Genzyme Corporation Poly(diallylamine)-based bile acid sequestrants
US6203785B1 (en) 1996-12-30 2001-03-20 Geltex Pharmaceuticals, Inc. Poly(diallylamine)-based bile acid sequestrants
US6423754B1 (en) 1997-06-18 2002-07-23 Geltex Pharmaceuticals, Inc. Method for treating hypercholesterolemia with polyallylamine polymers
US6726905B1 (en) 1997-11-05 2004-04-27 Genzyme Corporation Poly (diallylamines)-based phosphate binders
US8187631B2 (en) 1999-10-19 2012-05-29 Genzyme Corporation Direct compression polymer tablet core
US9931358B2 (en) 1999-10-19 2018-04-03 Genzyme Corporation Direct compression polymer tablet core
US9579343B2 (en) 1999-10-19 2017-02-28 Genzyme Corporation Direct compression polymer tablet core
US7985418B2 (en) 2004-11-01 2011-07-26 Genzyme Corporation Aliphatic amine polymer salts for tableting
US8808738B2 (en) 2004-11-01 2014-08-19 Genzyme Corporation Aliphatic amine polymer salts for tableting
US9555056B2 (en) 2004-11-01 2017-01-31 Genzyme Corporation Aliphatic amine polymer salts for tableting
US9895315B2 (en) 2004-11-01 2018-02-20 Genzyme Corporation Aliphatic amine polymer salts for tableting
US8986669B2 (en) 2005-09-02 2015-03-24 Genzyme Corporation Method for removing phosphate and polymer used therefore
US9585911B2 (en) 2005-09-15 2017-03-07 Genzyme Corporation Sachet formulation for amine polymers
US9095509B2 (en) 2005-09-15 2015-08-04 Genzyme Corporation Sachet formulation for amine polymers
WO2010079343A2 (en) 2009-01-09 2010-07-15 Cambridge Enterprise Limited Formulations of viable cells for oral delivery
EP3023102A1 (en) 2010-11-04 2016-05-25 Albireo AB Ibat inhibitors for the treatment of liver diseases
WO2012064266A1 (en) 2010-11-04 2012-05-18 Albireo Ab Ibat inhibitors for the treatment of liver diseases
EP3777864A1 (en) 2010-11-04 2021-02-17 Albireo AB Ibat inhibitors for the treatment of liver diseases
WO2012064267A1 (en) 2010-11-08 2012-05-18 Albireo Ab A pharmaceutical combination comprising an ibat inhibitor and a bile acid binder
US10512657B2 (en) 2011-10-28 2019-12-24 Lumena Pharmaceutials Llc Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US11229661B2 (en) 2011-10-28 2022-01-25 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US11376251B2 (en) 2011-10-28 2022-07-05 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US12145959B2 (en) 2011-10-28 2024-11-19 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
US11267924B2 (en) 2014-12-18 2022-03-08 Genzyme Corporation Crosslinked polydiallymine copolymers for the treatment of type 2 diabetes

Also Published As

Publication number Publication date
BE580490A (en) 1960-01-08

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