Biocompatible compounds for sustained release pharmaceutical drug delivery systems
Assignee3M Innovative Properties Company
InventorsJames S. Stefely, David W. Schultz, Chester L. Leach, Daniel C. Duan
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Abstract
Methods, compounds, and medicinal formulations utilizing biocompatible polymers for delivery of a drug, particularly for solubilizing, stabilizing and/or providing sustained release of drug from topical, implantable, and inhalation systems. Many of the methods, compounds, and medicinal formulations are particularly suitable for oral and/or nasal inhalation and use polymers of the formula —[X—R1—C(O)]— wherein each R1 is an independently selected organic group that links the —X— group to the carbonyl group, and each X is independently oxygen, sulfur, or catenary nitrogen.
Claims188
A medicinal aerosol solution formulation, comprising:
- (a) a biocompatible polymer substantially completely dissolved in the formulation;
- the biocompatible polymer comprising at least one chain of units of the formula —[X—R1—C(O)]— wherein:
- (i) each R1 is an independently selected organic group that links the —X— group to the carbonyl group;
- and
- (ii) each X is independently oxygen, sulfur, or catenary nitrogen;
- (b) a propellant;
- and
- (c) a drug substantially completely dissolved in the formulation in a therapeutically effective amount.
The formulation of claim I wherein the drug exhibits increased solubility in the propellant due to the biocompatible polymer.
A sustained release medicinal formulation comprising:
- (a) a propellant;
- (b) a therapeutically effective amount of a drug;
- and
- (c) a sufficient amount of a biocompatible polymer substantially completely dissolved in the formulation so as to provide for sustained release of the drug;
- wherein the sustained release formulation results in discrete, nonfilm forming particles upon delivery.
A metered dose inhaler for delivering a sustained release medicinal formulation comprising:
- an aerosol canister equipped with a metered dose valve and containing a sustained release medicinal aerosol formulation suitable for nasal and/or oral inhalation including a propellant, a drug in a therapeutically effective amount, and a biodegradable polymer substantially completely dissolved in the formulation in an amount such that the period of therapeutic activity of the drug when delivered is extended relative to the same formulation without the biodegradable polymer, said biodegradable polymer comprising at least one chain of units of the formula -[X—R1—C(O)]— wherein:
- (i) each R1 is an independently selected organic group that links the X group to the carbonyl group;
- and
- (ii) each X is independently oxygen, sulfur, or catenary nitrogen.
A biodegradable medicinal composition comprising:
- a therapeutically effective amount of a drug;
- and
- a biodegradable polymer comprising at least one chain of units of the formula —[O—R1—C(O)]— wherein:
- (a) each R1 is an independently selected organic group that links the —O—0 atom to the carbonyl group;
- and
- (b) the polymer has a number-average molecular weight of no greater than about 1800, and a polydispersity of less than about 1.2.
A method of improving the physical and degradation characteristics of a biodegradable condensation type polymer comprising fractionating the polymer with a supercritical fluid so as to obtain a polydispersity of less than about 1.3 and a number-average molecular weight of no greater than about 1800.
A medicinal salt comprising:
- (a) an ionic drug comprising at least one ammonium, sulfonate, or carboxylate group per molecule;
- and
- (b) a biodegradable polymeric counterion comprising at least one ammonium, sulfonate, or carboxylate group and at least one chain of at least three units of the formula —[O—R1—C(O)]— wherein each R1 is an independently selected organic group that links the oxygen atom to the carbonyl group.
A medicinal formulation comprising a medicinal salt, the salt comprising:
- (a) an ionic drug comprising at least one ammonium, sulfonate, or carboxylate group per molecule;
- and
- (b) a biodegradable counterion comprising at least one ammonium, sulfonate, or carboxylate group and at least one chain of at least three units of the formula —[O—R1—C(O)]— wherein each R1 is an independently selected organic group that links the oxygen atom to the carbonyl group.
A method of forming discrete particles of a medicinal formulation, the method comprising:
- (a) preparing a medicinal formulation by combining components comprising:
- (i) a propellant;
- (ii) a biocompatible polymer substantially completely dissolved in the medicinal formulation;
- and
- (iii) a therapeutically effective amount of a drug;
- (b) placing the medicinal formulation in a device capable of generating an aerosol;
- and
- (c) actuating the device to form an aerosol of discrete particles that are sufficiently annealed to avoid aggregation and film formation under conditions of use.
Dependencies are inferred from the claim text.