Bioerodible polymers for solid controlled release pharmaceutical compositions
First Claim
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1. A method for preparing a bioerodible polymer comprising:
- reacting a monomeric ortho ester having the general formula ##STR11## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and R'"'"' is lower alkyl with a triol having the general formula ##STR12## wherein n is 1 to 5 carbon atoms, to form a rigid, bioerodible ortho ester polymer containing mer units of the structure ##STR13##
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Abstract
Bioerodible ortho ester polymers useful for preparing solid form bioerodible pharmaceutical compositions such as pellets, capsules, suppositories and the like are provided. A novel synthetic method for preparing the polymers is provided as well as is a novel triol reactant. Synthesis involves a one-step reaction between a monomeric ortho ester and a triol. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes.
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28 Claims
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1. A method for preparing a bioerodible polymer comprising:
reacting a monomeric ortho ester having the general formula ##STR11## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and R'"'"' is lower alkyl with a triol having the general formula ##STR12## wherein n is 1 to 5 carbon atoms, to form a rigid, bioerodible ortho ester polymer containing mer units of the structure ##STR13##
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2. A compound of the formula ##STR14## wherein n is an integer in the range of 1 to 5 inclusive.
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3. A composition comprising a polymer comprising mer units of the chemical formula ##STR15## wherein R is hydrogen or (C1 -C10)alkyl, and n is 1 to 5;
- or co-polymers thereof or mixtures thereof.
- View Dependent Claims (4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)
- 23. A method for preparing a bioerodible polymer, comprising contacting at least one monomeric ortho ester of the chemical formula ##STR16## wherein R is hydrogen or (C1 -C10)alkyl, and R'"'"' is (C1 -C5)alkyl, with at least one triol of the chemical formula ##STR17## wherein n is 1 to 5, under conditions effective to form a bioerodible ortho ester polymer comprising mer units of the chemical formula ##STR18##
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