US5354562A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process for preparing micronized polypeptide drugs
Assignee: SRI International Inc
•
Filing: 1993-02-16
•
Granted: 1994-10-11
•
Expires: 2013-02-16
Abstract
Abstract Solid particle aerosol formulations of polypeptide drugs are made by lyophilizing solutions of the drugs which contain milling stabilizers that inhibit degradation of the drug during subsequent milling. The lyophilized drug is milled in fluid energy mills that have been fitted with abrasion-resistant materials and which use pure nitrogen that has been filtered to eliminate particles of greater than 0.1 mu m to transport the drug. The use of (a) milling stabilizers in the solution and (b) abrasion-resistant fluid energy mills that use pure filtered nitrogen in the milling step reduce insoluble contaminants and inactive fractions in the milled product.
Inventors
- 👤 Robert M. Platz
- 👤 Anna Ip
- 👤 Clyde L. Whitham
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 15:50
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/17; A61K38/19; A61K38/193; A61K38/21; A61K38/215; A61K38/22; A61K38/27; A61K9/00; A61K9/14
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
105 words
In a process for preparing a micronized polypeptide drug comprising lyophilizing a solution of the drug in a solvent and milling the lyophilized drug in a fluid energy mill using a pressurized gas to form a powder, the improvement comprising using a pure inert gas filtered to remove particles greater than about 0.1 μm and the improvement wherein the parts of the mill that are contacted by the pressurized gas in which the polypeptide drug is being carried are not substantially abraded by said drug-carrying gas whereby the insoluble contaminants in the micronized polypeptide drug comprise less than 2% by weight of the polypeptide drug.
Claim 2
Dependent Claim
105 words
In a process for preparing a micronized polypeptide drug comprising lyophilizing a solution of the drug in a solvent and milling the lyophilized drug in a fluid energy mill using a pressurized gas to form a powder, the improvement comprising using a pure inert gas filtered to remove particles greater than about 0.1 μm and the improvement wherein the parts of the mill that are contacted by the pressurized gas in which the polypeptide drug is being carried are not substantially abraded by said drug-carrying gas whereby the insoluble contaminants in the micronized polypeptide drug comprise less than 2% by weight of the polypeptide drug.
Claim 3
Dependent Claim
23 words
The process of claim i wherein the polypeptide drug is labile under the milling conditions and the lyophilized drug contains a milling stabilizer.
Claim 4
Dependent Claim
21 words
The process of claim 2 wherein the milling stabilizer comprises sorbitol, mannitol, sucrose, lactose, trehalose, serum albumin, polyvinylpyrrolidone, or mixtures thereof.
Claim 5
Dependent Claim
20 words
The process of claim 1 wherein the pressure of the nitrogen is in the range of 10 to 120 psig.
Claim 6
Dependent Claim
14 words
The process of claim 4 wherein the source of the nitrogen is liquid nitrogen.
Claim 7
Dependent Claim
25 words
The process of claim 1 wherein the particle size of the micronized polypeptide drug is in the range of about 0.5 to about 15 μm.
Claim 8
Dependent Claim
10 words
The process of claim 1 wherein the solvent is water.
Claim 9
Dependent Claim
19 words
The process of claim 1 wherein the micronized polypeptide drug is suitable for administration as a solid particle aerosol.
Claim 10
Dependent Claim
98 words
In a process for preparing a micronized polypeptide drug comprising lyophilizing a solution of the drug in a solvent and milling the lyophilized drug in a fluid energy mill using a pressurized gas to form a powder, the improvement comprising using a pure inert gas filtered to remove particles greater than about 0.1 μm and the improvement wherein the parts of the mill that are contacted by the pressurized gas in which the polypeptide drug is being carried are not substantially abraded by said drug-carrying gas whereby at least 85% of the polypeptide drug is in active form.
Claim 11
Dependent Claim
98 words
In a process for preparing a micronized polypeptide drug comprising lyophilizing a solution of the drug in a solvent and milling the lyophilized drug in a fluid energy mill using a pressurized gas to form a powder, the improvement comprising using a pure inert gas filtered to remove particles greater than about 0.1 μm and the improvement wherein the parts of the mill that are contacted by the pressurized gas in which the polypeptide drug is being carried are not substantially abraded by said drug-carrying gas whereby at least 85% of the polypeptide drug is in active form.
Claim 12
Dependent Claim
23 words
The process of claim 9 wherein the polypeptide drug is labile under the milling conditions and the lyophilized drug contains a milling stabilizer.
Claim 13
Dependent Claim
21 words
The process of claim 10 wherein the milling stabilizer comprises sorbitol, mannitol, sucrose, lactose, trehalose, serum albumin, polyvinylpyrrolidone or mixtures thereof.
Claim 14
Dependent Claim
20 words
The process of claim 9 wherein the pressure of the nitrogen is in the range of 10 to 120 psig.
Claim 15
Dependent Claim
20 words
The process of claim 9 wherein the pressurized gas is nitrogen and the source of the nitrogen is liquid nitrogen.
Claim 16
Dependent Claim
25 words
The process of claim 9 wherein the particle size of the micronized polypeptide drug is in the range of about 0.5 to about 15 μm.
Claim 17
Dependent Claim
10 words
The process of claim 9 wherein the solvent is water.
Claim 18
Dependent Claim
19 words
The process of claim 9 wherein the micronized polypeptide drug is suitable for administration as a solid particle aerosol.
References Cited (Backward Citations)
US4783484A
Cited
US4940588A
Cited
US4900734A
Cited
US5011678A
Cited
WO1990009781A1
Cited
EP0384752A2
Cited
WO1990009787A1
Cited
WO1990011091A1
Cited
WO1991016038A1
Cited
US5057321A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-10-10 | 1998-04-11 | 1998-10-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-10-10 | 2002-04-11 | 2002-10-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-10-10 | 2006-04-11 | 2006-10-11 | $7700.00 | Window Closed / Lapsed |