초록 ▼

Erodible devices are disclosed for delivering a drug to an environment of use. The devices comprise a body sized and adapted for delivering the drug to the environment of use, which body comprises (1) a poly(orthoester) or a poly(orthocarbonate) having a repeating unit consisting of a hydrocarbon ra

Erodible devices are disclosed for delivering a drug to an environment of use. The devices comprise a body sized and adapted for delivering the drug to the environment of use, which body comprises (1) a poly(orthoester) or a poly(orthocarbonate) having a repeating unit consisting of a hydrocarbon radical and a symmetrical dioxycarbon unit of the general formula: [Figure] wherein R1 is a multivalent hydrocarbon radical, R2 and R3 are hydrocarbon radicals with at least one of the R2 or R3 bonded to the dioxycarbon through an oxygen covalent bond, (2) a beneficial drug, and (3) an erosion rate modifier. The devices are useful for delivering both locally and systemically acting drugs over a prolonged period of time. A composition of matter is also disclosed comprising the poly(orthoesters) or the poly(orthocarbonates) and an erosion rate modifier.

대표청구항 ▼

A device for delivering a beneficial drug at a controlled rate over a prolonged period, said device shaped, sized and adapted for delivering a drug to an animal environment of use, the device comprising: (A) an erodible released rate controlling polymer of the formula: [Figure] wherein (I) R1 is a m

A device for delivering a beneficial drug at a controlled rate over a prolonged period, said device shaped, sized and adapted for delivering a drug to an animal environment of use, the device comprising: (A) an erodible released rate controlling polymer of the formula: [Figure] wherein (I) R1 is a member selected from the group consisting 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 alkenyl of 2 to 7 carbons, and an alkylene of 1 to 10 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, alkenyl of 2 to 7 carbons, and an alkylene of 1 to 10 carbons; arylene of 6 to 12 carbons; arylene of 6 to 12 carbons substituted with an alkyl of 1 to 7 carbons, alkyloxy of 1 to 7 carbons, alkenyl of 2 to 7 carbons, and alkylene of 1 to 10 carbons; wherein (II) R2 and R3 are selected from the grop consisting of alkyl of 1 to 7 carbons, alkenyl of 2 to 7 carbons, aryl or 6 to 12 carbons, an oxygen atom covalently bonded to the dioxycarbon atom, and when an oxygen atom R2 and R3 are a member selected from the group consisting of alkyloxy of 1 to 7 carbons; alkenyloxy of 2 to 7 carbons; and aryloxy of 6 to 12 carbons; and when only one of R2 and R3 is selected from said member the other R2 and R3 is selected from the group consisting of alkyl of 1 to 7 carbons; alkenyl of 2 to 7 carbons; and aryl of 6 to 12 carbons; wherein (III) R2 and R3 are intramolecularly covalently bonded to each other and to the same dioxycarbon atom, with at least one of R2 and R3 a ring oxygen atom forming a heterocyclic ring of 5 to 8 carbon and oxygen atoms when R2 and R3 are selected from the group consisting of alkylene of 2 to 6 carbons; alkenylene of 2 to 6 carbons; alkyleneoxy of 2 to 6 carbons; alkenyleneoxy of 2 to 6 carbons; alkylenedioxy of 2 to 5 carbons; alkenylenedieoxy of 2 to 5 carbons; oxa; and a heterocyclic ring of 5 to 8 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkyloxy of 1 to 7 carbons, an alkenyl of 2 to 7 carbons, and an alkenyloxy of 2 to 7 carbons; wherein (IV) R2 and R3 are intramolecularly covalently bonded to each other and to the same dioxycarbon atom with at least one of R2 and R3 is a ring oxygen atom forming a fused polycyclic ring of 8 to 12 carbon and oxygen atoms when R2 and R3 are a member selected from the group consisting of aralkylene of 8 to 12 carbons; aralkenylene of 8 to 12 carbons, aryloxy of 8 to 12 carbons; aralkyleneoxy of 8 to 12 carbons; aralkenyleneoxy of 8 to 12 carbons, aralkylenedioxy of 8 to 12 carbons; aralkenylenedioxy of 8 to 12 carbons; oxa; and a fused polycyclic ring of 8 to 12 carbon and oxygen atoms substituted with an alkyl of 1 to 7 carbons, an alkyloxy of 1 to 7 carbons, an alkenyl of 2 to 7 carbons and an alkenyloxy of 2 to 7 carbons; wherein (V) R2 and R3 are intramolecularly covalently bonded to each other and to the same dioxycarbon atom to form a 5 to 6 member carbocyclic ring; (B) a beneficial drug in the device; (C) an erosion rate modifier in the device in an amount that effects the period of time the device erodes and effects the amount of drug released as the device erodes over time; and wherein n is greater than 10.