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US 2003/0170289 A1Published application
Injectable depot compositions and uses thereof
OwnerGuohua Chen, Paul R. Houston +2inventors
InventorsGuohua Chen, Paul R. Houston, Lothar Walter Kleiner, Jeremy Corwin Wright
Life of this patent
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Abstract
Injectable depot compositions are provided that include a bioerodible, biocompatible polymer, an aromatic alcohol having miscibility in water of less than or equal to 7 wt. % at 25° C., in an amount effective to plasticize the polymer and form a gel therewith, and a beneficial agent. The composition may additionally contain an ester of an aromatic acid, or an aromatic ketone. The compositions are readily implanted beneath a patient's body surface by injection, as the aromatic alcohol not only facilitates solubilization of the polymer, but also acts as a thixotropic agent, substantially increasing the shear thinning behavior of the composition.
Claims112
An injectable depot composition comprising:
- a bioerodible, biocompatible polymer;
- an aromatic alcohol having miscibility in water of less than or equal to 7 wt. % at 25° C., in an amount effective to plasticize the polymer and form a gel therewith;
- and
- a beneficial agent,
- wherein the composition is free of monohydric lower alkanols.
2 more elements
An injectable depot composition comprising:
- approximately 5 wt. % to approximately 90 wt. % of a biodegradable, biocompatible lactic acid-based polymer having a weight average molecular weight in the range of approximately 5,000 to approximately 50,000;
- an aromatic alcohol having miscibility in water of less than or equal to 5% at 25° C., in an amount effective to plasticize the polymer and form a gel therewith, wherein the aromatic alcohol has the structural formula (I)
- Ar—(L)n—OH (I)
- in which Ar is a substituted or unsubstituted aryl or heteroaryl group, n is zero or 1, and L is a linking moiety;
- and
- a beneficial agent,
- wherein the composition is free of monohydric lower alkanols.
4 more elements
An injectable depot composition comprising:
- a bioerodible, biocompatible polymer;
- a solvent selected from the group consisting of esters of aromatic acids, aromatic ketones, and mixtures thereof, said solvent having miscibility in water of less than or equal to 7% at 25° C., and present in an amount effective to plasticize the polymer and form a gel therewith;
- an effective thixotropic amount of an aromatic alcohol having miscibility in water of less than or equal to 7%;
- and
- a beneficial agent,
- wherein the composition is free of monohydric lower alkanols.
3 more elements
An injectable depot composition comprising:
- approximately 5 wt. % to approximately 90 wt. % of a biodegradable, biocompatible lactic acid-based polymer having a weight average molecular weight in the range of approximately 5,000 to approximately 50,000;
- an ester of an aromatic acid, said ester having miscibility in water of less than or equal to 7% at 25° C., and present in an amount effective to plasticize the polymer and form a gel therewith;
- an effective thixotropic amount of an aromatic alcohol having miscibility in water of less than or equal to 7%, wherein the aromatic alcohol has the structural formula (I)
- Ar—(L)n—OH (I)
- in which Ar is a substituted or unsubstituted aryl or heteroaryl group, n is zero or 1, and L is a linking moiety;
- and
- a beneficial agent,
- wherein the composition is free of monohydric lower alkanols.
5 more elements
A method of administering a beneficial agent to a subject comprising the steps of:
- (1) administering an injectable depot composition to the subject at a site within the subject, the composition comprising:
- (a) a bioerodible, biocompatible polymer;
- (b) an aromatic alcohol having miscibility in water of less than or equal to 7 wt. % at 25° C., in an amount effective to plasticize the polymer and form a gel therewith;
- and
- (c) a beneficial agent;
- wherein the composition is free of monohydric lower alkanols;
- and
- (2) forming an implant at the site wherein the implant provides sustained release of the beneficial agent at the site.
5 more elements
A method of administering a beneficial agent to a subject comprising the steps of:
- (1) administering an injectable depot composition to the subject at a site within the subject, the composition comprising:
- (a) a bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of esters of aromatic acids, aromatic ketones, and mixtures thereof, said solvent having miscibility in water of less than or equal to 7% at 25° C., and present in an amount effective to plasticize the polymer and form a gel therewith;
- (c) an effective thixotropic amount of an aromatic alcohol having miscibility in water of less than or equal to 7%;
- and
- (d) a beneficial agent;
- wherein the composition is free of monohydric lower alkanols;
- and
- (2) forming an implant at the site wherein the implant provides sustained release of the beneficial agent at the site.
6 more elements
A method of administering a beneficial agent to a subject comprising the steps of:
- (1) administering an injectable depot composition to the subject at a site within the subject, the composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % of a biodegradable, biocompatible lactic acid-based polymer having a weight average molecular weight in the range of approximately 1,000 to approximately 120,000;
- (b) an aromatic alcohol having miscibility in water of less than or equal to 5% at 25° C., in an amount effective to plasticize the polymer and form a gel therewith, wherein the aromatic alcohol has the structural formula (I)
- Ar—(L)n—OH (I)
- in which Ar is a substituted or unsubstituted aryl or heteroaryl group, n is zero or 1, and L is a linking moiety;
- and
- (c) a beneficial agent;
- wherein the composition is free of monohydric lower alkanols;
- and
- (2) forming an implant at the site wherein the implant provides sustained release of the beneficial agent at the site.
7 more elements
A method of administering a beneficial agent to a subject comprising the steps of:
- (1) administering an injectable depot composition to the subject at a site within the subject, the composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % a poly(lactide-co-glycolide) (PLGA) copolymer having a weight average molecular weight in the range of approximately 1,000 to approximately 120,000;
- (b) approximately 5 wt. % to approximately 90 wt. % an aromatic alcohol solvent having miscibility in water of less than or equal to 7% at 25° C., in an amount effective to plasticize the polymer and form a gel therewith;
- and
- (c) a beneficial agent;
- wherein the composition is free of monohydric lower alkanols;
- and
- (2) forming an implant at the site wherein the implant provides sustained release of the beneficial agent at the site.
5 more elements
Dependencies are inferred from the claim text.