US4155992A
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Pharmaceutical composition of poly(orthoester) co- and homopolymers and poly(orthocarbonate) co- and homopolymers having carbonyloxy functionality with drug
Abstract Poly(orthoester) co- and homopolymers and poly(orthocarbonate) co- and homopolymers comprising (1) a repeating dioxycarbon unit in the polymeric backbone having a plurality of organic groups pendant therefrom, and (2) a bridging moiety having at least one carbonyloxy group contained therein are disclosed. The polymers are represented by the formula: <IMAGE> WHEREIN R is a bridging moiety and is either R1 or R2 arranged in a random manner along the polymeric backbone to form a copolymer containing both R1 and R2 with R1 an aliphatic, an alicyclic or an aromatic group and R2 is a <IMAGE> GROUP WITH R1 as defined and R3 an aliphatic, an alicyclic or aromatic group, or wherein R is a bridging moiety and is only R2 to form a homopolymer with R1, R2, and R3 as defined above, and a is 0 to 1, b is 2 to 6, and n and the sum of x and y are positive integers. The copolymers are useful for making articles of manufacture, including devices and coatings for delivering beneficial agents.
A composition of matter comprising a homopolymer of the general formula: ##STR34## wherein R 1 is a member selected from the group consisting of alkylene of 1 to 10 carbons; alkenylene of 2 to 10 carbons; cycloalkylene of 3 to 7 carbons; cycloalkylene of 3 to 7 carbons substituted with a member selected from the group consisting of an alkyl of 1 to 10 carbons; alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and alkylene of 1 to 10 carbons; cycloalkenylene of 5 to 7 carbons; cycloalkenylene of 5 to 7 carbons substituted with a member selected from the group consisting of an alkyl of 1 to 10 carbons, alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and akylene of 1 to 10 carbons; arylene, arylene of 6 to 20 carbons substituted with an alkyl of 1 to 10 carbons, alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and alkylene of 1 to 10 carbons; R 3 is the same as R 1 , a is 0 to 1, b is 2 to 6, n is 10 to 1000, ans x and y are 0 to 100 with at least one of x and y at least one, a drug dispersed in said homopolymer, and wherein the drug is released in a therapeutically effective amount at a controlled rate to an environment of use as the homopolymer erodes when in the environment over a prolonged period of time.
Claim 2
Dependent Claim
250 words
A composition of matter comprising a homopolymer of the general formula: ##STR34## wherein R 1 is a member selected from the group consisting of alkylene of 1 to 10 carbons; alkenylene of 2 to 10 carbons; cycloalkylene of 3 to 7 carbons; cycloalkylene of 3 to 7 carbons substituted with a member selected from the group consisting of an alkyl of 1 to 10 carbons; alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and alkylene of 1 to 10 carbons; cycloalkenylene of 5 to 7 carbons; cycloalkenylene of 5 to 7 carbons substituted with a member selected from the group consisting of an alkyl of 1 to 10 carbons, alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and akylene of 1 to 10 carbons; arylene, arylene of 6 to 20 carbons substituted with an alkyl of 1 to 10 carbons, alkenyl of 2 to 10 carbons, alkoxy of 1 to 10 carbons and alkylene of 1 to 10 carbons; R 3 is the same as R 1 , a is 0 to 1, b is 2 to 6, n is 10 to 1000, ans x and y are 0 to 100 with at least one of x and y at least one, a drug dispersed in said homopolymer, and wherein the drug is released in a therapeutically effective amount at a controlled rate to an environment of use as the homopolymer erodes when in the environment over a prolonged period of time.