GB2373438A - Cholesterol lowering compositions - Google Patents
Cholesterol lowering compositions Download PDFInfo
- Publication number
- GB2373438A GB2373438A GB0103368A GB0103368A GB2373438A GB 2373438 A GB2373438 A GB 2373438A GB 0103368 A GB0103368 A GB 0103368A GB 0103368 A GB0103368 A GB 0103368A GB 2373438 A GB2373438 A GB 2373438A
- Authority
- GB
- United Kingdom
- Prior art keywords
- bile
- derivatives
- complexing agent
- composition
- stimulant
- 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- Withdrawn
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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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
- A61K36/288—Taraxacum (dandelion)
-
- 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)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
-
- 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)
- A61K36/71—Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
-
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
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- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (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)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Botany (AREA)
- Biotechnology (AREA)
- Alternative & Traditional Medicine (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A composition comprising: <SL> <LI>a) a bile excretion stimulant, and <LI>b) a bile complexing agent. </SL> <SL> <LI>a) may be selected from dandelion leaves or roots golden seal roots, taraxinic acid and derivatives, hydrastine, hydroxymethylnicotinamide, berberine atropine sulphate and papaverine hydrochloride. <LI>b) may be selected from polyacrylic acids and derivatives thereof, alginic acids, starch ispaghula husk, cellulosic polysaccharides guar gum, konjak gum and pectins. </SL>
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. Lipoprotein, 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 to 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 stimulating the excretion of bile from the gall bladder in- : o the gut and at the same time complexing that bile to prevent
re-absorption. This combined activity stimulates the synthesis of more bile by the liver using cholesterol which is obtained from the plasma.
According to the present invention there is provided a cholesterol reducing composition for the reduction of cholesterol in plasma, which comprises :
a) a bile excretion stimulant selected from the group of dandelion leaves, dandelion roots, golden seal roots, taraxinic acid based materials and derivatives thereof, hydrastine,
hydroxymethylnicotinamide, fenofibrate or ciprofibrate, or mixtures thereof, and b) a bile complexing agent.
The bile complexing agent is a compound (or compounds) that is such that when administered into a mammalian gastrointestinal tract, will inhibit at least in part re-absorption of the said bile, by complexing with the bile so that it cannot be re-absorbed.
Though not wishing to be bound by theory, we believe that the compositions of the present invention by promoting excretion of bile from the liver and inhibiting re-absorption of bile lead to reduction in the level of low density lipoprotein and cholesterol circulating in blood plasma. These reduced levels of cholesterol in the blood can reduce the chance of coronary heart disease.
Preferably, the composition additionally comprises a pharmaceutically acceptable carrier or diluent.
Pharmaceutically acceptable carriers will be apparent to any man skilled in the art. They include all excipients like flavouring agents, tableting excipients etc.
The compositions according to the invention can be administered as a component of a pharmaceutical composition, together with the 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.
It can be prepared as a tincture, for example in a water based solution. When administered in a tincture in this way, the amount of the liquid in a single dose might be in the range from about 1 ml to about 20 ml.
Appropriate bile excretion stimulants can be provided as a liquid or as a solid. They can be derived from one or more of animal or plant sources, or be synthesised directly. Preferred bile excretion stimulants are choleretic agents.
The most preferred bile excretion stimulants are selected from taraxinic acid based materials (which include 11, 13-dihydrotaraxinic acid) and fibrates.
Examples of derivatives of taraxinic acid based materials include glucosides. Examples of suitable fibrates are isobutyrate fibrates which include clofibrate, gemfibrozil, bezafibrate, fenofibrate and ciprofibrate.
Naturally occurring materials providing the bile excretion stimulant, such as dandelion leaves, dandelion roots and golden seal roots can be used in the compositions according to the invention in a fresh state or after being dried at least partially, for example so that their water content is reduced to not more than about 20%, preferably not more than about 10 %. Preferably the active ingredient in these naturally
occurring materials is taraxinic acid derivatives.
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:
Polyacrylic acids and derivatives (e. g. 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
Carboxypolymethylene and alginate blends; ispaghula husk with polyacrylic acids and derivatives (e. g. carbomer) and/or guar gum; and hydroxymethyl cellulose and guar gum and pectin.
Preferably, the composition is in unit dosage form, in which the bile excretion stimulant is present in an amount of 0.5 to 70% more preferably 1 to 60 %, most preferably 1. 5 to 50 % by weight based on the weight of the composition (i. e. the unit dose) and the bile complexing agent is present in an amount of 1 to 60%,
more preferably 2 to 55 %, most preferably 5 to 50% by weight based on the total composition (i. e. the unit dose).
Preferably when the bile excretion stimulant is a herbal material, the amount present is 10 to 70%, more preferably 20 to 60%, most preferably 30 to 50%. When the bile excretion stimulant is a single drug substance, it is preferably present in an amount of 0.5 to 50%, more preferably 1 to 25%, most preferably 1.5 to 20% by weight.
Preferably, the ratio by weight of the bile excretion stimulant to the bile complexing agent is 1: 140 to 10: 1.
The compositions can further include other components such as flavourings, thickening agents, colouring components, preservatives and sweeteners (which are pharmaceutically acceptable carriers).
Further according to the invention there is provided the use of a bile complexing agent in the preparation of a medicament for co-administration with a bile excretion stimulant for reduction of cholesterol in plasma.
Further according to the invention there is provided the use of a bile excretion stimulant in 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 excretion stimulant and a bile complexing agent in the preparation of a medicament for the reduction of cholesterol in plasma.
The invention will now be illustrated by the following Examples.
Example 1
A powder formulation containing (per unit dose)
Dried powdered dandelion roots (commercially available) 3.5g
Ispaghula husk 3.5g
Sodium hydrogen carbonate 0.5g
Citric acid 3.5g
Flavouring agents 0.2g
Colouring agents 0.05g
Sweetener 0.05g is made up as follows.
The dried powdered dandelion roots and the ispaghula are granulated with water at room temperature and then dried. The mixture is then dry blended with the remaining dry ingredients.
This powder can be administered in aqueous solution after mixing it 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) Dried dandelion roots 3.5g
Polyacrylic acid carbomer 0.5g (Carbopol 974P)
Citric acid 3.5g
Flavouring agents 0.2g
Colouring agents 0. 05g
Sweetener 0. 05g is made up as follows:
The actives from the roots are extracted by combining the roots with approx. 150 mls of hot water.
This mixture is soaked for 1/2 hour and then the solid residue is removed by filtration. The carbomer is added with rapid mixing over 5 minutes (at 50 C approximately). The citric acid is added followed by flavouring, colouring and sweetening agents. 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 (per unit dose) Dried dandelion roots 2g
Ispaghula husk 2g
Citric acid O. lg
Sodium hydrogen carbonate 0.2g (or potassium salt)
Flavouring agents 0.2g
Colouring agents 0.05g
Tableting excipients-0. 05g is made up as follows:
The dandelion roots and ispaghula are granulated at room temperature with water and dried. This granulated mixture is dry blended with the remaining ingredients at room temperature and tableted by conventional means.
Example 4
A powder formulation containing (per unit dose) :
Fenofibrate O. lg
Ispaghula husk 3.50g
Citric Acid anhydrous/granulated 0.52g
Potassium Bicarbonate 0.03g
Sodium Bicarbonate 0.02g
Sweetener 0.05g
Colouring agent 0. 05g Flavour 0. 20g is made up as follows:
The ispaghula husk and fenofibrate are granulated at room temperature with isopropyl alcohol and dried.
The remaining components are added and dry blended. The powder can be administered in aqueous solution after mixing with 200 mls of water.
Claims (11)
- CLAIMS 1. A cholesterol reducing composition for the reduction of cholesterol in plasma, which comprises: a) a bile excretion stimulant selected from the group of dandelion leaves, dandelion roots, golden seal roots, taraxinic acid based materials and derivatives thereof, hydrastine, hydroxymethylnicotinamide, fenofibrate or ciprofibrate, or mixtures thereof, and b) a bile complexing agent.
- 2. A composition as claimed in claim 1 which additionally comprises a pharmaceutically acceptable carrier or diluent.
- 3. A composition as claimed in claim 1 or claim 2 in which the bile complexing agent is selected from polyacrylic acids and derivatives thereof, alginic acids, starch, ispaghula husk and its fractions, cellulosic polysaccharides and their derivatives, guar gum, konjak gum, pectins and mixtures thereof.
- 4. A composition as claimed in any one of the preceding claims which is in unit dosage form.
- 5. A composition as claimed in claim 4 wherein each unit dosage contains from 0.5 to 70%, preferably 1 to 60%, more preferably 1.5 to 50% by weight based on the weight of the unit dosage of the bile excretion stimulant and from 1 to 60%, preferablyfrom 2 to 55%, more preferably from 5 to 50% of the unit dosage of the bile complexing agent.
- 6. The use of a bile complexing agent in the preparation of a medicament for co-administration with a bile excretion stimulant for the reduction of cholesterol in plasma.
- 7. The combined use of a bile complexing agent and a bile excretion stimulant in the preparation of a medicament for the reduction of cholesterol in plasma.
- 8. The use as claimed in claim 6 or claim 7 wherein the bile complexing agent is selected from polyacrylic acids and derivatives thereof, alginic acids, starch, ispaghula husk and its fractions, cellulosic polysaccharides and their derivatives, guar gum, konjak gum, pectins and mixtures thereof.
- 9. The use as claimed in any one of claims 6 to 8 wherein the bile excretion stimulant is selected from dandelion leaves, dandelion roots, golden seal roots, taraxinic acid based materials and derivatives thereof, hydrastine, hydroxymethylnicotinamide, berberine, atropine sulphate, papaverine hydrochloride, fibrate compounds or derivatives thereof, or mixtures thereof.
- 10. A composition as claimed in claim 1 substantially ashereinbefore described with reference to any one of :) the Examples.
- 11. The use as claimed in claim 6 or claim 7 substantially as hereinbefore described with reference to any one of the Examples.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0103368A GB2373438A (en) | 2001-02-10 | 2001-02-10 | Cholesterol lowering compositions |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0103368A GB2373438A (en) | 2001-02-10 | 2001-02-10 | Cholesterol lowering compositions |
Publications (2)
Publication Number | Publication Date |
---|---|
GB0103368D0 GB0103368D0 (en) | 2001-03-28 |
GB2373438A true GB2373438A (en) | 2002-09-25 |
Family
ID=9908525
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
GB0103368A Withdrawn GB2373438A (en) | 2001-02-10 | 2001-02-10 | Cholesterol lowering compositions |
Country Status (1)
Country | Link |
---|---|
GB (1) | GB2373438A (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1796666A1 (en) * | 2004-09-17 | 2007-06-20 | Institute of Medicinal Biotechnology, Chinese Acadamy of Medical Sciences | Methods and compositions for the treatment of hyperlipidemia |
CN109549995A (en) * | 2019-01-18 | 2019-04-02 | 张掖市金盛中药饮片有限公司 | It is a kind of for treating the pulvis of coronary heart disease |
Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3495000A (en) * | 1968-01-26 | 1970-02-10 | Dart Ind Inc | Oral sustained release medicament matrix of dialdehyde starch admixed with ethyl cellulose,polyvinyl chloride or polyvinylpyrrolidone |
RO82844A2 (en) * | 1981-08-04 | 1983-11-01 | Intreprinderea De Medicamente,Ro | PROCESS FOR OBTAINING DELAYED TABLETS WITH PAPAVERINE HYDROCHLORIDE |
EP0295637A2 (en) * | 1987-06-15 | 1988-12-21 | Warner-Lambert Company | Lipid regulating compositions |
JPH0269416A (en) * | 1988-09-05 | 1990-03-08 | Tsumura & Co | Liver disorder improver |
EP0526862A1 (en) * | 1991-08-06 | 1993-02-10 | VECTORPHARMA INTERNATIONAL S.p.A. | Solid pharmaceutical compositions for oral administration with prolonged gastric residence |
EP0606742A1 (en) * | 1992-12-21 | 1994-07-20 | Rohm And Haas Company | Bile acid sequestrant |
GB2329334A (en) * | 1997-09-18 | 1999-03-24 | Reckitt & Colmann Prod Ltd | Cholesterol-lowering agents |
WO2000069445A1 (en) * | 1999-05-13 | 2000-11-23 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
-
2001
- 2001-02-10 GB GB0103368A patent/GB2373438A/en not_active Withdrawn
Patent Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3495000A (en) * | 1968-01-26 | 1970-02-10 | Dart Ind Inc | Oral sustained release medicament matrix of dialdehyde starch admixed with ethyl cellulose,polyvinyl chloride or polyvinylpyrrolidone |
RO82844A2 (en) * | 1981-08-04 | 1983-11-01 | Intreprinderea De Medicamente,Ro | PROCESS FOR OBTAINING DELAYED TABLETS WITH PAPAVERINE HYDROCHLORIDE |
EP0295637A2 (en) * | 1987-06-15 | 1988-12-21 | Warner-Lambert Company | Lipid regulating compositions |
JPH0269416A (en) * | 1988-09-05 | 1990-03-08 | Tsumura & Co | Liver disorder improver |
EP0526862A1 (en) * | 1991-08-06 | 1993-02-10 | VECTORPHARMA INTERNATIONAL S.p.A. | Solid pharmaceutical compositions for oral administration with prolonged gastric residence |
EP0606742A1 (en) * | 1992-12-21 | 1994-07-20 | Rohm And Haas Company | Bile acid sequestrant |
GB2329334A (en) * | 1997-09-18 | 1999-03-24 | Reckitt & Colmann Prod Ltd | Cholesterol-lowering agents |
WO2000069445A1 (en) * | 1999-05-13 | 2000-11-23 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
Non-Patent Citations (2)
Title |
---|
WPI ABSTRACT, Accession No. 1984-144237 [23] & RO 82844 A2 (INTR MEDICAMENTE) (01-11-1983) * |
WPI ABSTRACT, Accession No. 1990-119657 [25] & JP 02 069416 A (KITASATO) (08-03-1990) * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1796666A1 (en) * | 2004-09-17 | 2007-06-20 | Institute of Medicinal Biotechnology, Chinese Acadamy of Medical Sciences | Methods and compositions for the treatment of hyperlipidemia |
EP1796666A4 (en) * | 2004-09-17 | 2008-03-19 | Inst Medicinal Biotechnology | Methods and compositions for the treatment of hyperlipidemia |
EP2361625A1 (en) * | 2004-09-17 | 2011-08-31 | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences | Methods and compositions for the treatment of hyperlipidemia |
CN109549995A (en) * | 2019-01-18 | 2019-04-02 | 张掖市金盛中药饮片有限公司 | It is a kind of for treating the pulvis of coronary heart disease |
Also Published As
Publication number | Publication date |
---|---|
GB0103368D0 (en) | 2001-03-28 |
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Legal Events
Date | Code | Title | Description |
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WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |