Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1991-01-29
1994-01-18
Kight, III, John
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514819, 514823, A61K 3173
Patent
active
052800172
DESCRIPTION:
BRIEF SUMMARY
This relates to certain dextrin derivatives, the treatment of acidic conditions and to compositions for the use in such treatment.
According to a first aspect of the present invention, there is provided a dextrin derivative in which a proportion of the hydroxyl groups of dextrin are replaced by basic groups. Such basic groups may be any groups capable of binding acidic moieties present in body compartments such as the intestine, the peritoneum or the blood compartment. A preferred basic group is an amine group, more preferably a tertiary amine or a quaternary ammonium group.
It is well known that the binding of bile acids, which are secreted into the intestines, leads to a feedback activation of enzymes in the liver which metabolise cholesterol. This results in a lowering of blood cholesterol levels. Two agents are known for regulating the level of cholesterol by binding with the bile acids. Cholestyramine is the chloride salt of a basic anion-exchange resin in which the anion-exchange sites are provided by quaternary ammonium groups. The other agent is a resin called colestipol hydrochloride, a copolymer of diethyl pentamine and epichlorohydrin. Both these materials are hydrophilic but insoluble in water. They are unaffected by digestive enzymes, they remain unchanged in the gastro-intestinal tract and they are not absorbed into the bloodstream. However, these agents are resins and as a result have a sandy or gritty quality which makes them unpleasant to assimilate. In addition, they may cause nausea, abdominal discomfort, indigestion and constipation. Furthermore, in the case of cholestyramine, which is a chloride form of an anion-exchange resin, hyperchloremic acidosis can occur, especially in younger and smaller patients in whom the relative dosage is higher.
Another problem with these known agents is that they may also bind other compounds in the intestine including drugs administered concurrently.
Acid poisoning can occur as a result not only of the assimilation of substances which are normally regarded as poisons but also of pharmaceutical preparations which can be poisonous if taken in overdose. Examples of acid poisons include acetylsalicylic acid (aspirin) and barbiturates such as amylobarbitone, butobarbitone, pentobarbitone, phenobaritone and quinalbaritone.
The present invention accordingly also provides the use of the dextrin derivative to lower blood cholesterol levels and to treat acid poisoning. The present invention further provides a pharmaceutical composition comprising the dextrin derivative of the invention together with a inert carrier or diluent therefor. In addition the present invention provides a method for lowering blood cholesterol levels or treating acid poisoning in an animal subject, including a human being, comprising administering to the animal subject an effective amount of a dextrin derivative of the invention.
In a further aspect the invention provides a method of making a pharmaceutical composition of the invention comprising formulating together a dextrin derivative of the invention together with at least one inert carrier or diluent.
BRIEF DESCRIPTION OF THE DRAWINGS
The FIGURE graphically compares the percent loss of taurocholate over time for unsubstituted dextrin, quaternary ammonium ethyl dextrin, and cholestyramine.
Dextrin is made by hydrolysis of starch, typically by treatment of various starches with dilute acids or by heating a dry starch. Such methods produce glucose polymers with a large range of polymerisation. The degree of polymerisation (D.P) varies from one or two up to comparatively high numbers. The direct hydrolysis product of starch might contain un to 60% by weight of material having a D.P less than 12. In a preferred aspect of the present invention the dextrin derivative contains a relatively high proportion of glucose polymers of D.P. greater than 12. Preferably the dextrin derivative contains at least 50% by weight of glucose polymers of D.P. greater than 12.
More preferably the dextrin derivative contains less than 10% by weight of glucose
REFERENCES:
patent: 2813093 (1957-11-01), Caldwell et al.
patent: 3639389 (1972-02-01), Hull
patent: 4436731 (1984-03-01), Maltz
patent: 5059685 (1991-10-01), Conti
Die Starke, vol. 4, No. 10 Oct. 1952, pp. 253, 256, 257, Weinheim, DE; R. W. Kerr, The Reaction of Starch with Ethylenimine.
Kight III John
M L Laboratories PLC
Mullis Jeffrey C.
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