Absorbable pharmaceutical compositions based on isomorphic copolyoxalates
First Claim
1. In a pharmaceutical depot composition for parenteral administration of effective amounts of a drug released slowly over an extended period of time which comprises a combination of(a) from 1 percent to 99 percent by weight of composition of a drug in an effective depot amount greater than the single dose amount, and(b) a solid, absorbable polymer which is nonreactive toward body tissue and which undergoes biodegradation in the presence of body fluids into products which are metabolized or excreted by the body without adverse body reaction,the improvement comprising employing as said absorbable polymer isomorphic polyoxalate polymers comprising units of cyclic and linear oxalates and having the general formula ##STR2## wherein each R is
or
space="preserve" listing-type="equation">--(CH.sub.2)--.sub. 4+2n IIand from about 5 to 95 mole percent of the R units are I;
A is trans 1,4-cyclohexylene or p-phenylene, n is 1 or 2 and is the same for I and II, and x is the degree of polymerization resulting in a polymer having an inherent viscosity of at least 0.20 determined at 25°
C. in a 0.1 g/dl solution of polymer in chloroform or hexafluoroisopropanol.
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Abstract
Absorbable copolyoxalate polymers having isomorphic sequences are formulated with drugs and introduced into the body to provide a slow, sustained release of the drug over an extended period of time in accordance with the rate of absorption of the polymer. The copolyoxalate polymers are derived from mixtures of cyclic and linear diols, each having the same number of carbon atoms. The polymers are biodegradable in animal tissue and absorb with minimal adverse tissue reaction.
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Citations
15 Claims
- 1. In a pharmaceutical depot composition for parenteral administration of effective amounts of a drug released slowly over an extended period of time which comprises a combination of
(a) from 1 percent to 99 percent by weight of composition of a drug in an effective depot amount greater than the single dose amount, and (b) a solid, absorbable polymer which is nonreactive toward body tissue and which undergoes biodegradation in the presence of body fluids into products which are metabolized or excreted by the body without adverse body reaction, the improvement comprising employing as said absorbable polymer isomorphic polyoxalate polymers comprising units of cyclic and linear oxalates and having the general formula ##STR2## wherein each R is - space="preserve" listing-type="equation">--(CH.sub.2).sub.n -- A -- (CH.sub.2).sub.n -- I
or
space="preserve" listing-type="equation">--(CH.sub.2)--.sub. 4+2n IIand from about 5 to 95 mole percent of the R units are I;
A is trans 1,4-cyclohexylene or p-phenylene, n is 1 or 2 and is the same for I and II, and x is the degree of polymerization resulting in a polymer having an inherent viscosity of at least 0.20 determined at 25°
C. in a 0.1 g/dl solution of polymer in chloroform or hexafluoroisopropanol.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
Specification
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- Resources
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Current AssigneeEthicon Incorporated (Johnson & Johnson)
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Original AssigneeEthicon Incorporated (Johnson & Johnson)
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InventorsShalaby, Shalaby W., Jamiolkowski, Dennis D.
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Primary Examiner(s)Rosen, Sam
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Application NumberUS05/837,060Time in Patent Office447 DaysField of Search424/78, 424/238US Class Current514/169CPC Class CodesA61K 9/146 with organic macromolecular...A61K 9/204 Polyesters, e.g. poly(lacti...C08G 63/18 the acids or hydroxy compou...
