Drug delivery devices manufactured from poly(orthoesters) and poly(orthocarbonates)
First Claim
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1. A drug delivery device for the controlled and continuous administration of drug, wherein the device comprises:
- (a) a shaped matrix sized and adapted for administering drug to an animal and formed of a bioerodible drug release rate controlling pharmaceutically acceptable material, which material comprises a polymer of the formula;
##STR61## wherein R1 is a member selected from the group of divalent, trivalent and tetravalent radicals consisting of alkylene of 1 to 10 carbons;
alkenylene of 2 to 10 carbons;
alkyleneoxy of 2 to 6 carbons;
cycloalkylene of 3 to 7 carbons;
cycloalkylene of 3 to 7 carbons substituted with an alkyl of 1 to 7 carbons, alkoxy of 1 to 7 carbons, an alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons;
cycloalkenylene of 4 to 7 carbons;
cycloalkenylene of 4 to 7 carbons substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons, an alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons;
arylene; and
arylene substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons, and an alkenyl of 2 to 7 carbons;
R2 and R3 are selected from the group consisting of alkyl of 1 to 7 carbons;
alkenyl of 2 to 7 carbons;
alkoxy of 1 to 7 carbons;
alkenyloxy of 2 to 7 carbons;
alkylene of 2 to 6 carbons;
alkenylene of 3 to 6 carbons;
alkyleneoxy of 2 to 6 carbons;
alkenyleneoxy of 3 to 6 carbons;
aryloxy;
aralkyleneoxy of 8 to 12 carbons;
aralkenyleneoxy of 8 to 12 carbons;
oxa;
OR1 O with R1 as defined above;
a heterocyclic ring of 5 to 8 carbon and oxygen atoms formed when R2 and R3 are taken together;
a heterocyclic ring of 5 to 8 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons formed when R2 and R3 are taken together;
a fused polycyclic ring of 8 to 12 carbon and oxygen atoms formed when R2 and R3 are taken together;
a fused polycyclic ring of 8 to 12 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons; and
wherein at least one of said R2 and R3 is a member selected from the group consisting of alkoxy, alkenyloxy and OR1 O;
R2 and R3 when taken together are a member selected from the group of heterocyclic and fused polycyclic rings having at least one oxygen atom in the ring; and
wherein n is greater than 10;
(b) a drug selected from the group consisting of locally and systemically acting pharmaceutically acceptable drugs present in the matrix; and
, (c) wherein the device when in operation bioerodes at a controlled and continuous rate over a prolonged period of time, thereby administering a therapeutically effective amount of drug to the animal at a controlled and continuous rate over a prolonged period of time.
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Abstract
The invention concerns orthoester and orthocarbonate polymers having a repeating mer comprising a hydrocarbon radical and a symmetrical dioxycarbon unit of the general formula: ##STR1## WHEREIN R1 is a multivalent hydrocarbon radical, R2 and R3 are hydrocarbon radicals with at least one of R2 or R3 bonded to the dioxycarbon through an oxygen linkage, and which polymers are synthesized by reacting a polyol with an orthoester or orthocarbonate. The polymers are useful for making articles of manufacture, including devices and coatings for delivering beneficial agents.
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Citations
31 Claims
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1. A drug delivery device for the controlled and continuous administration of drug, wherein the device comprises:
- (a) a shaped matrix sized and adapted for administering drug to an animal and formed of a bioerodible drug release rate controlling pharmaceutically acceptable material, which material comprises a polymer of the formula;
##STR61## wherein R1 is a member selected from the group of divalent, trivalent and tetravalent radicals consisting of alkylene of 1 to 10 carbons;
alkenylene of 2 to 10 carbons;
alkyleneoxy of 2 to 6 carbons;
cycloalkylene of 3 to 7 carbons;
cycloalkylene of 3 to 7 carbons substituted with an alkyl of 1 to 7 carbons, alkoxy of 1 to 7 carbons, an alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons;
cycloalkenylene of 4 to 7 carbons;
cycloalkenylene of 4 to 7 carbons substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons, an alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons;
arylene; and
arylene substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons, and an alkenyl of 2 to 7 carbons;
R2 and R3 are selected from the group consisting of alkyl of 1 to 7 carbons;
alkenyl of 2 to 7 carbons;
alkoxy of 1 to 7 carbons;
alkenyloxy of 2 to 7 carbons;
alkylene of 2 to 6 carbons;
alkenylene of 3 to 6 carbons;
alkyleneoxy of 2 to 6 carbons;
alkenyleneoxy of 3 to 6 carbons;
aryloxy;
aralkyleneoxy of 8 to 12 carbons;
aralkenyleneoxy of 8 to 12 carbons;
oxa;
OR1 O with R1 as defined above;
a heterocyclic ring of 5 to 8 carbon and oxygen atoms formed when R2 and R3 are taken together;
a heterocyclic ring of 5 to 8 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons formed when R2 and R3 are taken together;
a fused polycyclic ring of 8 to 12 carbon and oxygen atoms formed when R2 and R3 are taken together;
a fused polycyclic ring of 8 to 12 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons; and
wherein at least one of said R2 and R3 is a member selected from the group consisting of alkoxy, alkenyloxy and OR1 O;
R2 and R3 when taken together are a member selected from the group of heterocyclic and fused polycyclic rings having at least one oxygen atom in the ring; and
wherein n is greater than 10;
(b) a drug selected from the group consisting of locally and systemically acting pharmaceutically acceptable drugs present in the matrix; and
, (c) wherein the device when in operation bioerodes at a controlled and continuous rate over a prolonged period of time, thereby administering a therapeutically effective amount of drug to the animal at a controlled and continuous rate over a prolonged period of time. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 27, 28, 29, 30, 31)
- (a) a shaped matrix sized and adapted for administering drug to an animal and formed of a bioerodible drug release rate controlling pharmaceutically acceptable material, which material comprises a polymer of the formula;
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26. A drug delivery device for the controlled administration of drug, wherein the device comprises:
- (a) a shaped matrix sized and adapted for administering drug to a human and formed of a hydrophobic, bioerodible drug release rate controlling material, which material comprises a polymer of the formula;
##STR62## wherein R1 is a member selected from the group consisting of alkylene of 1 to 10 carbons;
alkenylene of 2 to 10 carbons;
alkyleneoxy of 2 to 6 carbons;
cycloakylene 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 7 carbons, an alkoxy of 1 to 7 carbons, alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons, cycloalkenylene of 4 to 7 carbons, cycloalkenylene of 4 to 7 carbons substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons;
arylene; and
arylene substituted with an alkyl of 1 to 7 carbons, an alkoxy of 1 to 7 carbons and an alkenyl of 2 to 7 carbons; and
wherein a is 0 or 1, b is 2 to 6, and n is greater than 10;
(b) a drug selected from the group consisting of physiologically and pharmacologically active drugs present in the matrix; and
(c) wherein the device when in operation bioerodes and releases drug at a rate preselected from (1) a zero order rate, (2) a continuous rate and (c) a variable rate, which rate is produced by preselecting the polymer, the drug and the geometric shape of the device.
- (a) a shaped matrix sized and adapted for administering drug to a human and formed of a hydrophobic, bioerodible drug release rate controlling material, which material comprises a polymer of the formula;
Specification