Michael A Bassett

US Patent:

20050181059, Aug 18, 2005

Filed:

Sep 30, 2004

Appl. No.:

10/954423

Inventors:

Jules Jacob - Taunton MA, US
Yong Jong - Providence RI, US
Danielle Abramson - Boston MA, US
Edith Mathiowitz - Brookline MA, US
Camilla Santos - Newport RI, US
Michael Bassett - Rumford RI, US
Stacia Furtardo - Groton CT, US

International Classification:

A61K038/28
A61K048/00
A61K009/14

US Classification:

424489000, 514003000, 514044000

Abstract:

Compositions containing particles of biologically active agents with sizes in the micron and submicron range and methods for making and using such particles are described herein. In the preferred embodiment the biologically active agents are peptides, proteins, nucleic acid molecules, or hydrophilic synthetic molecules. The particles have a size ranging from an average diameter of about 100 nm to about 2000 nm, preferably about 200 nm to 600 nm. Optionally the biologically active agents contain a polymeric coating. The particles are formed by adding a biologically active agent to an aqueous solution, mixing a nonsolvent that is miscible with water with the aqueous solution, and precipitating particles of the biologically active agents out of the nonsolvent: aqueous solution combination. The nonsolvent is typically a C1 to C6 alcohol, preferably a C2 to a C5 alcohol. In the preferred embodiment, the nonsolvent is tert-butyl alcohol.

US Patent:

20050249799, Nov 10, 2005

Filed:

Mar 3, 2005

Appl. No.:

11/072098

Inventors:

Jules Jacob - Taunton MA, US
Michael Bassett - Rumford RI, US
Marcus Schestopol - Providence RI, US
Avinash Nangia - Wrentham MA, US
Bennett Carter - Cumberland RI, US
Peyman Moslemy - Providence RI, US
Ze'ev Shaked - San Antonio TX, US
David Enscore - Alpharetta GA, US
Courtney Sikes - Providence RI, US

International Classification:

A61K009/48
A61K009/20
A61K009/14

US Classification:

424451000, 424464000, 424486000, 424488000

Abstract:

An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.