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US 4,138,344 AGranted
Erodible agent releasing device comprising poly(orthoesters) and poly(orthocarbonates)
AssigneeAlza Corporation
InventorsNam S. Choi, Jorge Heller
Life of this patent
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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 R.sub.1 is a multivalent hydrocarbon radical, R.sub.2 and R.sub.3 are hydrocarbon radicals with at least one of R.sub.2 or R.sub.3 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.
Claims16
A device for the controlled release of an active agent to an environment of use, said device comprising:
- a matrix of an erodible release rate controlling material, said material comprising a polymer of the formula:
- ##STR61## wherein R.sub.1 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 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, an alkenyl of 2 to 7 carbons;
- wherein R.sub.2 and R.sub.3 are selected from the group consisting of alkyl of 1 to 7carbons;
- 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;
- OR.sub.1 O with R.sub.1 as defined above;
- a heterocyclic ring of 5 to 8 carbons and oxygen atoms formed when R.sub.2 and R.sub.3 are taken together;
- a fused polycyclic ring of 8 to 12 carbon and oxygen atoms formed when R.sub.2 and R.sub.3 are taken together;
- a member selected from the group consisting of a heterocyclic and fused polycyclic rings when R.sub.2 and R.sub.3 are taken together, with at least one of said R.sub.2 and R.sub.3 a member selected from the group consisting of alkoxy, alkenyloxy and OR.sub.1 O;
- and n is greater than 10;
- an active agent present in the matrix;
- and wherein the device, when in the environment of use erodes at a controlled and continuous rate, thereby releasing the active agent at a controlled and continuous rate over a period of time.
22 more elements
A device for releasing an active agent, said device comprising:
- a) a shaped matrix sized and adapted for placement in an environment of use and formed of the following formula:
- ##STR64## wherein R.sub.1 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;
- 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 7 carbons, an alkoxy of 1 to 7 carbons, an alkylene of 1 to 10 carbons, and an alkenyl of 2 to 7 carbons;
- cycloalkylene 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, an alkylene of 1 to 10 carbons, and alkenyl of 2 to 7 carbons;
- a is 0 to 1;
- b is 2 to 6;
- and n is greater than 10;
- b) an active agent distributed in the matrix;
- c) at least one surface defining at least a part of the device, and d) wherein when the device is in the environment of use the surface erodes at a controlled and continuous rate and concurrently therewith releasing the active agent at a controlled and continuous rate over a period of time.
10 more elements
A device for the release of an active agent to an environment of use, said device comprising a) an erodible release rate controlling material containing b) an active agent, the material comprising a copolymer of the following formula:
- ##STR65## wherein R.sub.1 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;
- cycloalkylene of 3 to 7 carbons;
- cycloalkylene of 3 to 7 carbons substituted with a member selected from the group consisting of 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;
- 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;
- a is 0 to 1;
- b is 2 to 6;
- m is greater than 10;
- n is greater than 10;
- said copolymer comprising at least one of R.sub.1, a, and b in mer I different than R.sub.1, a, and b in mer II;
- and wherein the material erodes when the device is in the environment of use at a controlled and continuous rate thereby releasing the active agent over time.
12 more elements
A device for the release of an active agent to an environment of use, said device comprising an erodible release rate controlling material containing an active agent, the material comprising a terpolymer of the following formula:
- ##STR66## wherein R.sub.1 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;
- cycloalkylene of 3 to 7 carbons;
- cycloalkylene of 3 to 7 carbons substituted with a member selected from the group consisting of 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, 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 a is 0 to 1;
- b is 2 to 6;
- m, n, and p each are greater than 10;
- said terpolymer comprising at least one of R.sub.1, a, and b in mers I, II and III, that is different than R.sub.1 a, and b in mers I, II and III;
- and wherein the device, when in the environment of use, erodes at a controlled and continuous rate, thereby releasing agent at a controlled and continuous rate over time.
11 more elements
Dependencies are inferred from the claim text.