US5663198A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Drug formulations comprising coated, very sparingly water-soluble drugs for inhalational pharmaceutical forms, and process for their preparation
Assignee: Hoechst AG
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Filing: 1994-07-13
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Granted: 1997-09-02
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Expires: 2014-07-13
Abstract
Abstract Drug formulations comprising coated, very sparingly water-soluble drugs for inhalational pharmaceutical forms, and process for their preparation. Drug formulations comprising micronized particles of very sparingly water-soluble drugs which are coated with a natural, physiologically acceptable ampholytic surfactant soluble in water to give a micellar/colloidal solution, and a process for the preparation of these drug formulations, are described. When placed in an appropriate final container and after the addition of a chlorine-free, partially fluorinated propellant gas liquefiable under pressure, these formulations are suitable for inhalation.
Inventors
- 👤 Bernhard Reul
- 👤 Walter Petri
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 17:04
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/007; A61K9/0073; A61K9/0075; A61K9/008; A61K9/14; A61K9/141; A61K9/145; A61K9/48; A61K9/50; A61K9/5005; A61K9/5015
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
41 words
A drug formulation comprising a chlorine-free, partially fluorinated hydrocarbon formulated with micronized particles of a very sparingly water-soluble drug that are sufficiently coated with a natural, physiologically acceptable ampholytic phospholipid surfactant that is soluble in water to give a micellar/colloidal solution.
Claim 2
Dependent Claim
41 words
A drug formulation comprising a chlorine-free, partially fluorinated hydrocarbon formulated with micronized particles of a very sparingly water-soluble drug that are sufficiently coated with a natural, physiologically acceptable ampholytic phospholipid surfactant that is soluble in water to give a micellar/colloidal solution.
Claim 3
Dependent Claim
23 words
A drug formulation as claimed in claim 1, wherein the drug is coated with a phospholipid mixture having a phosphatidylcholine content of 20-95%.
Claim 4
Dependent Claim
42 words
A process for the preparation of a drug formulation as claimed in claim 1 or 2, which comprises the steps of suspending the micronized drug in an aqueous micellar/colloidal solution of the ampholytic phospholipid mixture surfactant and spray-drying or lyophilizing the suspension.
Claim 5
Dependent Claim
76 words
An aerosol which contains a drug formulation comprising micronized particles of a very sparingly water-soluble drug which are coated with a natural, physiologically acceptable ampholytic phospholipid surfactant mixture that is soluble in water to give a micellar/colloidal solution and a chlorine-free, partially fluorinated propellant gas liquefiable under pressure selected from the group consisting of heptafluoropropane (R 227), tetrafluoroethane (R 134a) and a mixture thereof, said aerosol being free of any other flow improving or suspension-stablilizing adjunct.
Claim 6
Dependent Claim
76 words
An aerosol which contains a drug formulation comprising micronized particles of a very sparingly water-soluble drug which are coated with a natural, physiologically acceptable ampholytic phospholipid surfactant mixture that is soluble in water to give a micellar/colloidal solution and a chlorine-free, partially fluorinated propellant gas liquefiable under pressure selected from the group consisting of heptafluoropropane (R 227), tetrafluoroethane (R 134a) and a mixture thereof, said aerosol being free of any other flow improving or suspension-stablilizing adjunct.
Claim 7
Dependent Claim
73 words
A process for the preparation of an aerosol as claimed in claim 4, comprising the steps of a. dosing the drug formulation into an appropriate container; sealing the container with a metering valve and adding an amount of chlorine-free propellant gas required to form the aerosol, or b. preparing the aerosol from the drug formulation in a separate, pressure-resistant first container homogenizing the aerosol and filling the homogenized aerosol into a second container.
Claim 8
Dependent Claim
26 words
A process for the production of an aerosol, which comprises filling the drug formulation as claimed in claim 1 into a suitable capsule or reservoir system.
Claim 9
Dependent Claim
12 words
A drug formulation as claimed in claim 1 which contains a diuretic.
Claim 10
Dependent Claim
11 words
A drug formulation as claimed in claim 1 which contains furosemide.
Claim 11
Dependent Claim
12 words
A drug formulation as claimed in claim 1 which contains an antidiabetic.
Claim 12
Dependent Claim
12 words
A drug formulation as claimed in claim 1 which contains an antimycotic.
Claim 13
Dependent Claim
11 words
A drug formulation as claimed in claim 1 which contains rilopirox.
Claim 14
Dependent Claim
14 words
A drug formulation as claimed in claim 2 wherein the phosphatidylcholine content is 40-80%.
Claim 15
Dependent Claim
25 words
An aerosol which contains a drug formulation as claimed in claim 2 wherein said chlorine-free, partially fluorinated hydrocarbon is a propellant gas liquefiable under pressure.
Claim 16
Dependent Claim
32 words
An aerosol as claimed in claim 13, wherein the chlorine-free, partially fluorinated propellant gas liquefiable under pressure is heptafluoropropane (R 227) or tetrafluoroethane (R 134a) or a mixture of these two substances.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 2000-09-01 | 2001-03-03 | 2001-09-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2004-09-01 | 2005-03-03 | 2005-09-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2008-09-01 | 2009-03-03 | 2009-09-02 | $7700.00 | Window Closed / Lapsed |