GB2329334A - Cholesterol-lowering agents - Google Patents
Cholesterol-lowering agents Download PDFInfo
- Publication number
- GB2329334A GB2329334A GB9719754A GB9719754A GB2329334A GB 2329334 A GB2329334 A GB 2329334A GB 9719754 A GB9719754 A GB 9719754A GB 9719754 A GB9719754 A GB 9719754A GB 2329334 A GB2329334 A GB 2329334A
- Authority
- GB
- United Kingdom
- Prior art keywords
- complexing agent
- coa reductase
- hmg coa
- reductase inhibitor
- cholesterol
- 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.)
- Withdrawn
Links
- 239000003529 anticholesteremic agent Substances 0.000 title 1
- 229940127226 anticholesterol agent Drugs 0.000 title 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims abstract description 42
- 210000000941 bile Anatomy 0.000 claims abstract description 26
- 239000000203 mixture Substances 0.000 claims abstract description 24
- 239000008139 complexing agent Substances 0.000 claims abstract description 22
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims abstract description 17
- 235000012000 cholesterol Nutrition 0.000 claims abstract description 17
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims abstract description 17
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims abstract description 9
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229920002472 Starch Polymers 0.000 claims abstract description 6
- 229960002297 fenofibrate Drugs 0.000 claims abstract description 6
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229960002965 pravastatin Drugs 0.000 claims abstract description 6
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims abstract description 6
- 235000019698 starch Nutrition 0.000 claims abstract description 6
- 229940063644 ispaghula husk Drugs 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 5
- 229920002907 Guar gum Polymers 0.000 claims description 5
- 239000000665 guar gum Substances 0.000 claims description 5
- 235000010417 guar gum Nutrition 0.000 claims description 5
- 229960002154 guar gum Drugs 0.000 claims description 5
- 229920000642 polymer Polymers 0.000 claims description 5
- FJLGEFLZQAZZCD-MCBHFWOFSA-N (3R,5S)-fluvastatin Chemical compound C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 FJLGEFLZQAZZCD-MCBHFWOFSA-N 0.000 claims description 4
- 235000010443 alginic acid Nutrition 0.000 claims description 4
- 229920000615 alginic acid Polymers 0.000 claims description 4
- 238000011260 co-administration Methods 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 229960003765 fluvastatin Drugs 0.000 claims description 4
- 239000001814 pectin Substances 0.000 claims description 4
- 229920001277 pectin Polymers 0.000 claims description 4
- 235000010987 pectin Nutrition 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229920001282 polysaccharide Polymers 0.000 claims description 4
- 239000005017 polysaccharide Substances 0.000 claims description 4
- 150000004804 polysaccharides Chemical class 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- KPSRODZRAIWAKH-JTQLQIEISA-N Ciprofibrate Natural products C1=CC(OC(C)(C)C(O)=O)=CC=C1[C@H]1C(Cl)(Cl)C1 KPSRODZRAIWAKH-JTQLQIEISA-N 0.000 claims description 3
- HEMJJKBWTPKOJG-UHFFFAOYSA-N Gemfibrozil Chemical compound CC1=CC=C(C)C(OCCCC(C)(C)C(O)=O)=C1 HEMJJKBWTPKOJG-UHFFFAOYSA-N 0.000 claims description 3
- 229920002752 Konjac Polymers 0.000 claims description 3
- 229920000294 Resistant starch Polymers 0.000 claims description 3
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims description 3
- 150000004781 alginic acids Chemical class 0.000 claims description 3
- 229960000516 bezafibrate Drugs 0.000 claims description 3
- IIBYAHWJQTYFKB-UHFFFAOYSA-N bezafibrate Chemical compound C1=CC(OC(C)(C)C(O)=O)=CC=C1CCNC(=O)C1=CC=C(Cl)C=C1 IIBYAHWJQTYFKB-UHFFFAOYSA-N 0.000 claims description 3
- 229960002174 ciprofibrate Drugs 0.000 claims description 3
- KPSRODZRAIWAKH-UHFFFAOYSA-N ciprofibrate Chemical compound C1=CC(OC(C)(C)C(O)=O)=CC=C1C1C(Cl)(Cl)C1 KPSRODZRAIWAKH-UHFFFAOYSA-N 0.000 claims description 3
- 229960001214 clofibrate Drugs 0.000 claims description 3
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 claims description 3
- 229960003627 gemfibrozil Drugs 0.000 claims description 3
- 235000010485 konjac Nutrition 0.000 claims description 3
- 235000021254 resistant starch Nutrition 0.000 claims description 3
- 229960002855 simvastatin Drugs 0.000 claims description 3
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims description 3
- 229920002125 Sokalan® Polymers 0.000 abstract description 6
- 239000003112 inhibitor Substances 0.000 abstract description 6
- 229960001631 carbomer Drugs 0.000 abstract description 4
- 229940125753 fibrate Drugs 0.000 abstract description 3
- 229920001222 biopolymer Polymers 0.000 abstract description 2
- 239000004584 polyacrylic acid Substances 0.000 abstract description 2
- 239000010903 husk Substances 0.000 abstract 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 12
- 210000002381 plasma Anatomy 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000000796 flavoring agent Substances 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 238000004040 coloring Methods 0.000 description 4
- 102000007330 LDL Lipoproteins Human genes 0.000 description 3
- 108010007622 LDL Lipoproteins Proteins 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 235000013355 food flavoring agent Nutrition 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- 239000004150 EU approved colour Substances 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 230000000536 complexating effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 208000029078 coronary artery disease Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000002440 hepatic effect Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 229940006093 opthalmologic coloring agent diagnostic Drugs 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- WLAMNBDJUVNPJU-UHFFFAOYSA-N 2-methylbutyric acid Chemical compound CCC(C)C(O)=O WLAMNBDJUVNPJU-UHFFFAOYSA-N 0.000 description 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
- 102000004895 Lipoproteins Human genes 0.000 description 1
- 108090001030 Lipoproteins Proteins 0.000 description 1
- 244000134552 Plantago ovata Species 0.000 description 1
- 235000003421 Plantago ovata Nutrition 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000002421 cell wall Anatomy 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 239000007919 dispersible tablet Substances 0.000 description 1
- 229940050507 fluvastatin 20 mg Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229960000292 pectin Drugs 0.000 description 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 1
- 230000007505 plaque formation Effects 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/68—Plantaginaceae (Plantain Family)
-
- 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
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- 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
- A61K31/74—Synthetic polymeric materials
- A61K31/765—Polymers containing oxygen
- A61K31/78—Polymers containing oxygen of acrylic acid or derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/888—Araceae (Arum family), e.g. caladium, calla lily or skunk cabbage
Landscapes
- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Botany (AREA)
- Engineering & Computer Science (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A composition comprising a) a HMG CoA reductase inhibitor, and b) a bile complexing agent. for the reduction of cholesterol in plasma. The inhibitor is preferably a station or fibrate. The complexing agent is preferably fibrous and selected from biopolymers and starches. Exemplifield are compositions containing (a) fluvestatin and isphaghula husk; (b) fenofibrate and polyacrylic acid carbomer; (c) pravastatin and isphaghula husk.
Description
ORGANIC COMPOSITIONS
The invention relates to materials for treating patients so as to reduce the level of cholesterol in plasma, in particular to compositions for reducing cholesterol in plasma.
Raised plasma cholesterol can be a factor which contributes to coronary heart disease. Lipoproteins, especially low density lipoproteins, contribute to the transportation of cholesterol to body tissues where it can be deposited. Deposition of cholesterol can lead to the formation of plaques in arteries, resulting in turn in reduced flow of blood.
We have found a composition that ultimately leads to reduction in plasma low density lipoprotein and cholesterol levels. This is achieved by inhibiting de novo cholesterol synthesis in the liver and at the same time complexing bile (which is synthesised from cholesterol) in the GI tract to prevent its re-absorption. This combined activity stimulates hepatic uptake of cholesterol from the plasma, because it is required to replace the unreadsorbed bile in the absence of de novo synthesised cholesterol.
According to the invention, there is provided a composition comprising t a) a HMG CoA reductase inhibitor (hereinafter the
Inhibitor); and b) a bile complexing agent,
HMG CoA reductase inhibitors inhibit the activity of HMG CoA reductase, which is the committed enzyme in cholesterol synthesis, mainly in the liver.
The bile complexing agent is a compound (or compounds) that is such that when administered into a mammalian gastrointestinal tract, it will inhibit at least in part re-absorption of the said bile, by complexing with the bile so that it cannot be re-absorbed.
Further according to the invention there is provided the use of a HMG CoA reductase inhibitor for the preparation of a medicament for co-administration with a bile complexing agent for reduction of cholesterol in plasma.
Further according to the invention there is provided the use of a bile complexing agent for the preparation of a medicament for co-administration with a HMG CoA reductase inhibitor, for the reduction of cholesterol in plasma.
Further according to the invention, there is provided the use of a bile complexing agent and a HMG
CoA reductase inhibitor for the preparation of a medicament for the reduction of cholesterol in plasma.
The compositions of the present invention promote hepatic uptake of plasma cholesterol and by inhibition of the re-absorption of bile reduce the level of low density lipoprotein and cholesterol circulating in blood plasma. This can lead to reduced levels of plasma cholesterol and, significantly, to reduced chance of coronary heart disease.
The compositions according to the invention can be administered as a component of a pharmaceutical composition, together with a pharmaceutically acceptable carrier.
Further according to the invention there is provided a pharmaceutical composition comprising
a) a HMG CoA reductase inhibitor (hereinafter defined as the Inhibitor),
b) a bile complexing agent, and
c) a pharmaceutically acceptable carrier.
The pharmaceutical composition can be prepared as a powder which can be administered, for example in solution or in a suspension, generally in water or an aqueous solution, for example in a dilute ethanol solution or in a drink. When administered in a solution in this way, the amount of the liquid in a single dose might be in the range from about 100 ml to about 250 ml. A composition containing the blend can be prepared as a tablet to be swallowed whole or chewed, or to be dissolved in water or other solvent.
Pharmaceutically acceptable carriers will be apparent to any man skilled in the art. They include excipients, such as flavourings, thickening agents, colouring components, preservatives etc.
Preferred Inhibitors are statins or fibrates.
Preferred stations are
fluvastatin,
pravastatin,
simvastatin.
Preferred fibrates are
clofibrate,
gemfibrozil,
ciprofibrate,
bezafibrate and
fenofibrate.
Preferably the bile complexing agents will often be essentially fibrous in nature. Suitable bile complexing agents will often contain one or more of plant cell wall materials, non-starch polysaccharides and starches. It might include other polymers, especially biopolymers. It can include other components such as thickening agents.
More preferably the bile complexing agent is selected from:
polymers of acrylic acid and its derivatives (eg carbomer),
alginic acids,
starch (resistant starch),
ispaghula husk and its fractions,
cellulosic polysaccharides and their derivatives,
guar gum,
konjak gum,
pectins and mixtures thereof.
Preferred mixtures of the above are selected from blends of polymeric acrylic acid and alginate; ispaghula husk with polymers of acrylic acid and their derivatives and/or guar gum; hydroxymethyl cellulose and guar gum and pectin.
Preferably the compositions are in unit dose form.
Preferably the Inhibitor is present in an amount of 0.1 to 25, more preferably 0.15 to 20%, most preferably 0.2 to 15 by weight based on the total composition.
Preferably, the bile complexing agent is present in an amount of 1 to 60%, more preferably 2 to 55%, most preferably 5 to 50k by weight based on the total composition.
Preferably, the ratio by weight of the Inhibitor to the bile complexing agent is between 1:600 and 251 The compositions according to the invention can further include other components such as flavourings, thickening agents, colouring components, preservatives etc.
The invention will now be illustrated by the following Examples.
Example 1
A powder formulation containing (per unit dose)
Fluvastatin 20 mg
(commercially available)
Ispaghula husk 3.5g
Sodium hydrogen carbonate 0.5g
Citric acid 3. 5g Flavouring agent 0.2g
Colouring agent 0. osg is made up as follows.
The fluvastatin and the ispaghula husk are granulated with water at room temperature. This is then dried after granulation and then dry blended with the remaining dry components.
This powder can be administered in aqueous solution after mixing at room temperature with 200 ml of water with stirring. Alternatively, the powder can be administered directly as a powder, for example being supplied in bulk with an appropriate volume measuring scoop.
Example 2
A liquid drink containing (per unit dose) Fenof ibrate O.lg Polyacrylic acid carbomer
Carbopol 974P O.5g Citric acid 0.5g
Flavouring agents 0.2g
Colouring agents 0.05g
Sweetening agent 0.05g
is made up as follows:
The fenofibrate and the carbomer are rapidly mixed over 5 minutes. Then the citric acid is added, followed by flavouring, colouring and sweetener agent.
The resulting mixture is made up by the addition of cold water to 200 mls.
The drink can be supplied in individual portion packages, for example in glass or plastic bottles or other containers such as those formed from treated paper-based materials. The drink can be supplied in larger containers from which individual doses can be measured out, for example by volume.
Example 3
A dispersible tablet containing
Pravastatin 20g
Ispaghula husk 20g
Citric acid O.lg Sodium hydrogen carbonate 0.2g
Flavouring agents 0.2g
Colouring agents 0.05g
Tableting excipients 0.05g
is made up as follows:
The pravastatin and ispaghula are granulated with water at 250C and dried. This granulated mixture is dry blended with the remaining ingredients at room temperature and tableted by conventional means.
Claims (11)
1. A composition comprising
a) a HMG CoA reductase inhibitor , and
b) a bile complexing agent.
2. A pharmaceutical composition comprising
a) a HMG CoA reductase inhibitor,
b) a bile complexing agent, and
c) a pharmaceutically acceptable carrier.
3. A composition according to Claim 1 or Claim 2 in which the HMG CoA reductase inhibitor may be selected from:
Bezafibrate,
Clofibrate,
Gemfibrozil,
Fenofibrate,
Ciprofibrate,
Fluvastatin,
Pravastatin and
Simvastatin.
4. A composition according to any one of the preceding claims, in which the bile complexing agent may be selected from:
Polymers of acrylic acid and its derivatives,
Alginic acids,
Starch (resistant starch),
Ispaghula husk and its fractions,
Cellulosic polysaccharides and their derivatives,
Guar gum,
Konjak gum and
Pectins.
5. A composition containing an HMG CoA reductase inhibitor and a bile complexing agent, substantially as herein described with reference to any one of the
Examples.
6. The use of HMG CoA reductase inhibitor in the preparation of a medicament for co-administration with a bile complexing agent for reduction of cholesterol in plasma.
7. The use of a bile complexing agent for the preparation of a medicament for co-administration with a HMG CoA reductase inhibitor, for the reduction of cholesterol in plasma.
8. The use of a bile complexing agent and a HMG CoA reductase inhibitor for the preparation of a medicament for the reduction of cholesterol in plasma.
9. The use according any one of Claims 6 to 8 in which the HMG CoA reductase inhibitor is selected from:
Bezafibrate,
Clofibrate,
Gemfibrozil,
Fenofibrate,
Ciprofibrate,
Fluvastatin,
Pravastatin and
Simvastatin.
10. The use according any one of Claims 6 to 9, in which the bile complexing agent is selected from:
Polymers of acrylic acid and its derivatives,
Alginic acids,
Starch (resistant starch),
Ispaghula husk and its fractions,
Cellulosic polysaccharides and their derivatives,
Guar gum,
Konjak gum and
Pectins.
11. The use of HMG CoA reductase inhibitor and bile complexing agent substantially as herein described with reference to any one of the Examples.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9719754A GB2329334A (en) | 1997-09-18 | 1997-09-18 | Cholesterol-lowering agents |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9719754A GB2329334A (en) | 1997-09-18 | 1997-09-18 | Cholesterol-lowering agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB9719754D0 GB9719754D0 (en) | 1997-11-19 |
| GB2329334A true GB2329334A (en) | 1999-03-24 |
Family
ID=10819202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB9719754A Withdrawn GB2329334A (en) | 1997-09-18 | 1997-09-18 | Cholesterol-lowering agents |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2329334A (en) |
Cited By (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000069446A1 (en) * | 1999-05-13 | 2000-11-23 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
| WO2000069445A1 (en) * | 1999-05-13 | 2000-11-23 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
| US6264938B1 (en) | 1997-11-05 | 2001-07-24 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholestrolemia |
| WO2001078747A1 (en) * | 2000-04-18 | 2001-10-25 | Bayer Aktiengesellschaft | Use of cse inhibitors for treating heart failure |
| US6387924B2 (en) | 1994-09-13 | 2002-05-14 | G.D. Searle & Co. | Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake |
| US6420417B1 (en) | 1994-09-13 | 2002-07-16 | G. D. Searle & Co. | Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors |
| GB2373438A (en) * | 2001-02-10 | 2002-09-25 | Reckitt & Colmann Prod Ltd | Cholesterol lowering compositions |
| US6458850B1 (en) | 1998-12-23 | 2002-10-01 | G.D. Searle, Llc | Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications |
| US6458851B1 (en) | 1998-12-23 | 2002-10-01 | G. D. Searle, Llc | Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications |
| US6462091B1 (en) | 1998-12-23 | 2002-10-08 | G.D. Searle & Co. | Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications |
| US6489366B1 (en) | 1998-12-23 | 2002-12-03 | G. D. Searle, Llc | Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications |
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| GB9719754D0 (en) | 1997-11-19 |
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