US5932243A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Galenical formulations
Assignee: Novartis AG
•
Filing: 1997-08-22
•
Granted: 1999-08-03
•
Expires: 2017-08-22
Abstract
Abstract A pharmaceutical composition containing macrolide, e.g. a rapamycin compound in an emulsion preconcentrate or microemulsion preconcentrate for oral administration. The carrier medium for the rapamycin compound includes a hydrophilic phase, a lipophilic phase and a surfactant. The composition is stable and provides high absorption efficiency.
Inventors
- 👤 Gerd Fricker
- 👤 Barbara Haeberlin
- 👤 Armin Meinzer
- 👤 Jacky Vonderscher
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 17:25
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/33; A61K31/395; A61K31/435; A61K31/4353; A61K31/436; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61K9/48; A61K9/4841; A61K9/4858; A61P; A61P37/00; A61P37/02; A61P37/06; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/44
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
167 words
A pharmaceutical composition for oral administration which is a microemulsion preconcentrate comprising 40-O-(2-hydroxy)ethyl rapamycin as active ingredient in a carrier medium which comprises i) a hydrophilic component, which, with co-components, if present, comprises 10 to 50% by weight of the carrier medium and which is Transcutol, Glycofurol, 1,2-propylene glycol, or mixtures thereof; ii) a lipophilic component, which comprises 10 to 85% by weight of the carrier medium and which is selected from the group consisting of 1) fatty acid triglycerides, 2) mixed mono-, di-,and tri-glycerides, and 3) transesterified ethoxylated vegetable oils; and iii) a surfactant, which comprises 5 to 80% by weight of the carrier medium and which is selected from the group consisting of polyethyleneglycol, natural or hydrogenated castor oils, polyethylene-sorbitan fatty acid esters, polyoxyethylene fatty acid esters, polyoxyethylene-polyoxypropylene co-polymers, and block co-polymers the relative proportion of the active ingredient and components i), ii) and iii) being such that on dilution with water, a microemulsion having an average particle size of <1,500 Å is spontaneously formed.
Claim 2
Dependent Claim
167 words
A pharmaceutical composition for oral administration which is a microemulsion preconcentrate comprising 40-O-(2-hydroxy)ethyl rapamycin as active ingredient in a carrier medium which comprises i) a hydrophilic component, which, with co-components, if present, comprises 10 to 50% by weight of the carrier medium and which is Transcutol, Glycofurol, 1,2-propylene glycol, or mixtures thereof; ii) a lipophilic component, which comprises 10 to 85% by weight of the carrier medium and which is selected from the group consisting of 1) fatty acid triglycerides, 2) mixed mono-, di-,and tri-glycerides, and 3) transesterified ethoxylated vegetable oils; and iii) a surfactant, which comprises 5 to 80% by weight of the carrier medium and which is selected from the group consisting of polyethyleneglycol, natural or hydrogenated castor oils, polyethylene-sorbitan fatty acid esters, polyoxyethylene fatty acid esters, polyoxyethylene-polyoxypropylene co-polymers, and block co-polymers the relative proportion of the active ingredient and components i), ii) and iii) being such that on dilution with water, a microemulsion having an average particle size of <1,500 Å is spontaneously formed.
Claim 3
Dependent Claim
24 words
A composition of claim 1 wherein the surfactant is a polyoxyethylene sorbitan monolaurate, a polyoxyethylene sorbitan monopalmitate, a polyoxyethylene stearate, or a polyoxyethylene oleate.
Claim 4
Dependent Claim
16 words
A composition of claim 1 which further comprises one or more lower alkanols as hydrophilic co-component.
Claim 5
Dependent Claim
11 words
A composition of claim 3 wherein the hydrophilic co-component is ethanol.
Claim 6
Dependent Claim
25 words
A composition of to claim 1 in which the active ingredient is present in an amount of 1 to 15% by weight of the composition.
Claim 7
Dependent Claim
11 words
A composition of claim 1 in a soft gelatine encapsulated form.
Claim 8
Dependent Claim
31 words
A method of administering an antibiotic to a person in need of such treatment which comprises orally administering to said person a pharmaceutically effective amount of a composition of claim 1.
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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) | 2002-08-02 | 2003-02-01 | 2003-08-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2006-08-02 | 2007-02-01 | 2007-08-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2010-08-02 | 2011-02-01 | 2011-08-03 | $7700.00 | Window Closed / Lapsed |