Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
1995-06-07
2001-01-30
Peselev, Elli (Department: 1623)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C514S055000, C514S057000, C514S167000, C514S762000
Reexamination Certificate
active
06180617
ABSTRACT:
TECHNICAL FIELD
This invention relates to a method for reducing the biologically active level of undesired lipids in the gastrointestinal tract and to novel compositions for use with the method.
BACKGROUND ART
The adverse effects of high plasma cholesterol have been extensively studied and a correlation has been described between plasma cholesterol and heart disease.
Numerous compositions have been proposed for controlling the amount of cholesterol present in the blood stream. Disclosed, for example, is use of certain nonfat esters as a fat substitute to control the intake of fat and the amount of lipids in the bloodstream (U.S. Pat. No. 2,962,419); administration of a special class of polysaccharides consisting of at least two glucopyronosic units, each linked to the other by a 1-3-glycosidic linkage (U.S. Pat. No. 3,081,226); oral administration of certain naturally occurring mucilaginous substances which exert a hypocholesteremic adjuvant action (U.S. Pat. No. 3,148,114); oral administration of non-toxic glycocholic acid-binding polymeric amines for binding bile acids in the gut (U.S. Pat. No. 3,308,020); oral administration of heat-modified guar gum (U.S. Pat. No. 3,415,927); incorporation of certain polysaccharide substances in food products (U.S. Pat. No. 3,511,910); oral administration of ether-type anion exchangers prepared from hydroxyl-containing polysaccharides and cross-linked polysaccharides containing amino, morpholino and guanidino basic functioning groups (U.S. Pat. No. 3,627,872); administration of a defined diet composition incorporating certain carbohydrates (U.S. Pat. No. 3,849,554); oral administration of diethylaminoethyl dextran (U.S. Pat. No. 3,851,057); oral administration of water-soluble konjac mannan (U.S. Pat. No. 3,856,945); oral administration of sucrose-containing sweeteners to which maltitol and/or lactitol is added (U.S. Pat. No. 3,957,976); use of liquid polyol fatty acid polyesters in combination with anti-anal leakage agents (U.S. Pat. No. 4,005,195); oral administration of Levorin (U.S. Pat. No. 4,039,659); and oral administration of oat or barley gum (U.S. Pat. No. 4,175,124).
DISCLOSURE OF INVENTION
Disclosed is a method of reducing the availability of undesired lipids, such as cholesterol, in the fluid media of the gastrointestinal tract prior to absorption of the lipids across the cells lining the tract. A novel composition is orally administered, the composition utilizing a nontoxic, substantially nondigestible polymer to which ligands are chemically bonded through biologically stable ether groups, the ligands attracting and scavenging undesired lipids from the fluid media of the gastrointestinal tract. The composition, with the scavenged lipids, is discharged from the gastrointestinal tract with the feces.
The invention provides a unique and effective way of reducing the availability of undesired lipids, prior to absorption of such lipids across the gastrointestinal mucosalcells, and prior to the lipids going into the lymph where it is deposited in the thoracic duct and enters the blood circulatory system at the juncture of the internal jugular and subclavian veins.
BEST MODE FOR CARRYING OUT THE INVENTION
The novel compositions described herein are employed for reducing the biologically active level of undesired lipids present in the gastrointestinal tract of animals prior to any substantial absorption of the lipids through the intestinal lining and into the bloodstream. The compositions are prepared by bonding ligands as pendant groups to nontoxic, substantially nondigestible polymers having multiple reactive hydroxyl groups thereon which form biologically stable ether linkages with the ligand. Polymers which may be employed include cellulose, cellulosic and modified cellulosic polymers, polysaccharides and synthetic polymers such as polyvinyl alcohol (PVA) and hydroxyethylmethacrylate (HEMA). In particular, alpha-cellulose, carboxymethylcellulose (CMC), hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), hydroxyethylcellulose, algin, dextrose, pectin, agar, and chitin may be used. Combinations of different polymers and/or copolymers and mixed ligands may be employed. For example, cholesterol (as a ligand) and a hydrocarbon (as a ligand) may be attached to the backbone of a suitable polymer.
The ligand employed depends on the particular lipid to be removed. In general, the ligand should be substantially hydrophobic, capable of attracting and bonding, by secondary chemical forces, to the lipid desired to be removed, and capable of being bonded to the polymer through biologically stable ether groups. For example, the cholesterol molecule has a substantially planar shape. If cholesterol is desired to be removed, ligands having substantially straight-chain aliphatic groups ranging from 12 to 24 carbon atoms are capable of binding to cholesterol present in the gastrointestinal tract to hold it and prevent its absorption until the polymer to which the ligand is attached is discharged from the gastrointestinal tract. Cholesterol itself may also be used as a ligand, the cholesterol molecule bound to the polymer by (1) converting the single hydroxyl group of the cholesterol molecule to a reactive epoxy group for reaction with the polymer or (2) by use of an intermediate compound reactive with both the polymer and cholesterol or (3) by other suitable means. Other ligand substances which may be used include saturated and unsaturated alcohols which can be converted to epoxides by the addition and subsequent dehydrohalination of epichlorohydrin or by the use of other intermediate compounds reactive with both the polymer and cholesterol, such as 1,2-epoxyoctadecane, and butane diglycidylether, followed by reaction with lipid molecules having a group which may be bonded to the pendant epoxy group on the polymer backbone.
The percentage of ligand groups employed relative to the polymer may range widely from 1 to 50%, depending on the particular polymer used, the particular ligand employed, and the lipid to be removed.
Undesired lipids which can be removed using the compositions of this invention include cholesterol, and cholesterol esters, steroids, fat soluble drugs, fatty acids and fatty esters and their derivatives.
The lipids are attracted to and bound to the ligand by secondary chemical or VanderWaal's forces.
The compositions are used by oral administration The dosage will vary depending on the length of treatment and the condition being treated. Dosages can range from 0.1 gm/kg body weight to 5.0 gm/kg body weight. The com- positions may be admixed with a carrier, such as a liquid or solid filler, diluent, food stuff etc. The carrier may comprise from 1 to 99% by weight of the total composition.
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Choi N. S.
Hoffman Allan S.
Peselev Elli
Seed Intellectual Property Law Group PLLC
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