Biodegradable oxidized cellulose esters and their uses as microspheres
AssigneeUniversity of Iowa Research Foundation
InventorsVijay Kumar, Yang Dong
Life of this patent
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Abstract
A new cellulose excipient, OCCAE, suitable for use as a binder, filler, and/or disintegrant in the development of solid dosage forms and as a bodying agent or a drug carrier in the preparation of topical formulations is described. The cellulose excipient is formed by reacting an oxidized cellulose ester with an alcohol in the presence of a catalyst. The invention also describes the formation of controlled release microspheres using OCCAE and/or oxidized cellulose esters that may be used to control the release of drug in a patient over a time period of several hours to several days.
Claims17
A biodegradable, oxidized cellulose carboxylated alkyl/aryl ester (OCCAE) having one of the following general formulas I or II, the general formula:
- wherein:
- X is H, alkyl (C1-C16) or an aryl group;
- R is H;
- CF3;
- (CH2)nCH3, where n is from 0 to 18;
- (CH2)nCOOH, where n is from 1 to 8;
- CY═CZCOOH, where Y and Z are independently selected from the group consisting of hydrogen, methyl, branched alkyl having from 1 to 20 carbon atoms and from one to three cis or trans double bonds;
- branched alkenyl having from 1 to 20 carbon atoms and having from one to three cis or trans double bonds;
- CY═CH2, where Y is H, methyl, or phenyl;
- CH═CHY, where Y is C6H5;
- CH═CYCOOH, where Y is H or CH3;
- (CH2)8CH═CH(CH2)8CH3;
- or C6H(2-6)(COOH)0-4, CH2CH(COOH)CH2—COOH;
- w, is 0.1-1.0;
- x is 0.1-2.0;
- and
- n is 30-1500;
- and
- wherein:
- X is H, alkyl (C1-C16) or an aryl group;
- R′ and R″ are each selected from the group consisting of:
- H;
- CF3;
- (CH2)nCH3, where n is from 0 to 18;
- (CH2)nCOOH, where n from 1 to 8;
- CY═CZCOOH, where Y and Z are independently selected from the group consisting of hydrogen, methyl, branched alkyl having from 1 to 20 carbon atoms and from one to three cis or trans double bonds;
- branched alkenyl having from 1 to 20 carbon atoms and having from one to three cis or trans double bonds;
- CY—CH2, where Y is H, methyl, or phenyl;
- CH═CHY, where Y is C6H5;
- CH═CYCOOH, where Y is H or CH3;
- (CH2)8CH═CH(CH2)8CH3;
- or C6H(2-6)(COOH)0-4, CH2CH(COOH)CH2—COOH;
- w is 0.1-1.0;
- x′ is 0.1-1.9;
- y is 0.1-1.9;
- and
- n is 30-850.
A pharmaceutical comprising:
- controlled release microspheres comprising at least one oxidized cellulose ester.
Dependencies are inferred from the claim text.