Short duration depot formulations
OwnerGuohua Chen, David Priebeinventors
Life of this patent
Estimating the term…
Abstract
Methods and compositions for systemically or locally administering by implantation a beneficial agent to a subject are described, and include, for example, depot gel compositions that can be injected into a desired location and which can provide controlled release of a beneficial agent over a short duration of time. The compositions include a low molecular weight biocompatible polymer, a biocompatible solvent having low water miscibility that forms a viscous gel with the polymer and limits water uptake by the implant, and a beneficial agent.
Claims105
An injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a 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, wherein said solvent is an aromatic alcohol;
- and
- (c) a beneficial agent.
An injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent.
An injectable depot composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % of a low molecular weight bioerodible, biocompatible polymer;
- (b) an aromatic alcohol 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, 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.
A injectable depot composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % of a low molecular weight biodegradable, biocompatible lactic acid-based polymer having a weight average molecular weight in the range of approximately 1,000 to approximately 10,000;
- (b) an aromatic alcohol 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, 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.
A injectable depot composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % of a low molecular weight biodegradable, biocompatible lactic acid-based polymer having a weight average molecular weight in the range of approximately 1,000 to approximately 10,000;
- (b) a solvent selected from the group consisting of an aromatic alcohol, an ester of an aromatic acid, 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, 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.
An injectable depot composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % a low molecular weight poly(lactide-co-glycolide) (PLGA) copolymer having a weight average molecular weight in the range of approximately 3,000 to approximately 10,000;
An injectable depot composition comprising:
- (a) approximately 5 wt. % to approximately 90 wt. % of a low molecular weight poly(lactide-co-glycolide) (PLGA) copolymer having a weight average molecular weight in the range of approximately 3,000 to approximately 10,000;
- (b) approximately 5 wt. % to approximately 90 wt. % of a solvent selected from the group consisting of an aromatic alcohol, an ester of an aromatic acid, 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;
- and
- (c) a beneficial agent.
An injectable depot composition for sustained delivery of a beneficial agent to a subject comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- wherein the beneficial agent is delivered systemically in a controlled manner over a duration equal to or less than two weeks.
An injectable depot composition for sustained delivery of a beneficial agent to a subject comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- wherein the beneficial agent is delivered locally in a controlled manner over a duration equal to or less than two weeks.
A method of administering a beneficial agent to a subject in a controlled manner over a duration equal to or less than two weeks, comprising administering an injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent.
A method of administering a beneficial agent to a subject comprising administering an injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- wherein the beneficial agent is delivered systemically in a controlled manner over a duration equal to or less than two weeks.
A method of locally administering a beneficial agent to a subject in a controlled manner over a duration equal to or less than two weeks, comprising administering an injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- the system releasing within 24 hours after implantation less than or equal to 20% by weight of the amount of beneficial agent to be delivered over the duration of the delivery period, wherein the delivery period is 2 weeks.
A method of administering a beneficial agent to a subject comprising administering an injectable depot composition comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- wherein the beneficial agent is delivered locally in a controlled manner over a duration equal to or less than two weeks.
A kit for administration of a beneficial agent to a subject comprising:
- (a) a low molecular weight bioerodible, biocompatible polymer;
- (b) a solvent selected from the group consisting of aromatic alcohols, 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;
- and
- (c) a beneficial agent;
- and optionally, one or more of the following:
- (d) an emulsifying agent;
- (e) a pore former;
- (f) a solubility modulator for the beneficial agent, optionally associated with the beneficial agent;
- and
- (g) an osmotic agent;
- wherein at least the beneficial agent, optionally associated with the solubility modulator, is maintained separated from the solvent until the time of administration of the beneficial agent to a subject.
Dependencies are inferred from the claim text.