Greg P Randall

US Patent:

6395300, May 28, 2002

Filed:

Nov 4, 1999

Appl. No.:

09/433486

Inventors:

Julie Straub - Winchester MA
Howard Bernstein - Cambridge MA
Sarwat Khattak - Cambridge MA
Greg Randall - Stoneham MA

Assignee:

Acusphere, Inc. - Cambridge MA

International Classification:

A61K 914

US Classification:

424489, 264 5

Abstract:

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

US Patent:

6589557, Jul 8, 2003

Filed:

Jun 14, 2001

Appl. No.:

09/881289

Inventors:

Julie Straub - Winchester MA
Howard Bernstein - Cambridge MA
Greg Randall - Somerville MA

Assignee:

Acusphere, Inc. - Cambridge MA

International Classification:

A61K 914

US Classification:

424484, 424489, 424400, 424405

Abstract:

Celecoxib is provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of celecoxib having a mean diameter between about 0. 01 and 5 m and a total surface area greater than about 0. 5 m /mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1. 0 g/mL. The porous celecoxib matrices preferably are made using a process that includes (i) dissolving celecoxib in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of celecoxib. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

US Patent:

6610317, Aug 26, 2003

Filed:

Mar 2, 2001

Appl. No.:

09/798824

Inventors:

Julie Straub - Winchester MA
Howard Bernstein - Cambridge MA
Sarwat Khattak - Amherst MA
Greg Randall - Somerville MA

Assignee:

Acusphere, Inc. - Cambridge MA

International Classification:

A61F 200

US Classification:

424422, 424489, 424426, 514449

Abstract:

Paclitaxel is provided in a porous matrix form, which allows the drug to be formulated without Cremophor and administered as a bolus. The paclitaxel matrices preferably are made using a process that includes (i) dissolving paclitaxel in a volatile solvent to form a paclitaxel solution, (ii) combining at least one pore forming agent with the paclitaxel solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of paclitaxel. The pore forming agent can be either a volatile liquid that is immiscible with the paclitaxel solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. In a preferred embodiment, microparticles of the porous paclitaxel matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

US Patent:

6645528, Nov 11, 2003

Filed:

Oct 23, 2000

Appl. No.:

09/694407

Inventors:

Julie Straub - Winchester MA
Howard Bernstein - Cambridge MA
Sarwat Khattak - Cambridge MA
Greg Randall - Stoneham MA

Assignee:

Acusphere, Inc. - Cambridge MA

International Classification:

A61K 914

US Classification:

424489, 514951

Abstract:

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

US Patent:

6800297, Oct 5, 2004

Filed:

May 19, 2003

Appl. No.:

10/441440

Inventors:

David Altreuter - Brookline MA
Julie Straub - Winchester MA
Howard Bernstein - Cambridge MA
Paul Kopesky - Quincy MA
Greg Randall - Somerville MA

Assignee:

Acusphere, Inc. - Watertown MA

International Classification:

A51K 914

US Classification:

424484, 424489

Abstract:

One or more COX-2 inhibitors are provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of COX-2 inhibitors having a mean diameter between about 0. 01 and 5 m and a total surface area greater than about 0. 5 m /mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1. 0 g/mL. The porous COX-2 inhibitor matrices preferably are made using a process that includes (i) dissolving one or more COX-2 inhibitors in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of COX-2 inhibitors. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

US Patent:

6932983, Aug 23, 2005

Filed:

Nov 3, 2000

Appl. No.:

09/706045

Inventors:

Julie Straub - Wincherster MA, US
Howard Bernstein - Cambridge MA, US
Sarwat Khattak - Cambridge MA, US
Greg Randall - Stoneham MA, US

Assignee:

Acusphere, Inc. - Cambridge MA

International Classification:

A61K009/16

US Classification:

424489, 424400

Abstract:

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

US Patent:

RE40493, Sep 9, 2008

Filed:

Aug 26, 2005

Appl. No.:

11/213257

Inventors:

Julie A. Straub - Winchester MA, US
Howard Bernstein - Cambridge MA, US
Sarwat Khattak - Hadley MA, US
Greg Randall - Arlington MA, US

Assignee:

Acusphere, Inc. - Watertown MA

International Classification:

A61K 9/14
A61K 9/70
A61F 2/00

US Classification:

424489, 424484, 424422, 424428, 514951, 514449, 549512

Abstract:

Paclitaxel is provided in a porous matrix form, which allows the drug to be formulated without Cremophor and administered as a bolus. The paclitaxel matrices preferably are made using a process that includes (i) dissolving paclitaxel in a volatile solvent to form a paclitaxel solution, (ii) combining at least one pore forming agent with the paclitaxel solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of paclitaxel. The pore forming agent can be either a volatile liquid that is immiscible with the paclitaxel solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. In a preferred embodiment, microparticles of the porous paclitaxel matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

US Patent:

7919119, Apr 5, 2011

Filed:

Jan 22, 2002

Appl. No.:

10/053929

Inventors:

Julie Straub - Winchester MA, US
David Altreuter - Brookline MA, US
Howard Bernstein - Cambridge MA, US
Sarwat Khattak - Hadley MA, US
Greg Randall - Somerville MA, US

Assignee:

Acusphere, Inc. - Lexington MA

International Classification:

A61K 9/14
A61K 9/50
B29B 9/00

US Classification:

424489, 424484, 424501, 264 5

Abstract:

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt.