US4293565A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Transdermal medication system for isosorbide dinitrate
Assignee: Sanol Schwarz GmbH
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Filing: 1979-10-09
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Granted: 1981-10-06
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Expires: 1999-10-09
Abstract
Abstract A pharmaceutical preparation comprising: (a) isosorbide dinitrate as active ingredient (b) a solvent for isosorbide dinitrate (c) an ointment consistency agent (d) an emulsifying agent (e) water, and (f) possibly customary preservatives, antioxidants, buffers and/or odorants; where the weight ratio of water: consistency agent including emulsifying agent: solvent is 30 to 80: 3 to 35: 3 to 35, the amount of emulsifying agent is from 0% to 15% by weight and the amount of isosorbide dinitrate is from 2% to 20% by weight. The preparation has an ointment-like consistency and is administered topically to the skin, where it has a high adsorption rate and a long duration of response.
Inventors
- 👤 Gunter Cordes
- 👤 Ewald Giesselmann
- 👤 Ulrich Munch
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 21:01
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/34; A61K9/00; A61K9/70; A61K9/7023
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
129 words
A pharmaceutical preparation consisting essentially of (a) isosorbide dinitrate as active ingredient, (b) a non-aqueous solvent for isosorbide dinitrate which dissolves at least 5% by weight of isosorbide dinitrate, based on the solvent, has an ointment-like consistency and is miscible with water, where said solvent is an ester of a C 8-18 fatty acid with glycerin ethoxylated with from 3 to 10 mols of ethylene oxide, (c) an ointment consistency agent selected from the group consisting of glycerin monostearate, hardened castor oil, cetyl alcohol, stearyl alcohol, stearic acid, and mixtures thereof, and (d) water, where the weight ratio of water to consistency agent to solvent is 30 to 80:3 to 35:3 to 35 and the amount of isosorbide dinitrate in the preparation is from 2% to 20% by weight.
Claim 2
Dependent Claim
129 words
A pharmaceutical preparation consisting essentially of (a) isosorbide dinitrate as active ingredient, (b) a non-aqueous solvent for isosorbide dinitrate which dissolves at least 5% by weight of isosorbide dinitrate, based on the solvent, has an ointment-like consistency and is miscible with water, where said solvent is an ester of a C 8-18 fatty acid with glycerin ethoxylated with from 3 to 10 mols of ethylene oxide, (c) an ointment consistency agent selected from the group consisting of glycerin monostearate, hardened castor oil, cetyl alcohol, stearyl alcohol, stearic acid, and mixtures thereof, and (d) water, where the weight ratio of water to consistency agent to solvent is 30 to 80:3 to 35:3 to 35 and the amount of isosorbide dinitrate in the preparation is from 2% to 20% by weight.
Claim 3
Dependent Claim
68 words
The pharmaceutical preparation of claim 1, having a further content of (e) from 0.5% to 15% by weight based on the preparation of an emulsifying agent, said emulsifying agent being considered as part of said consistency agent with respect to said weight ratio, and being selected from the group consisting of esters of a polyoxyalkylene diol with a fatty acid and polyoxyalkylene diols etherified with a fatty alcohol.
Claim 4
Dependent Claim
22 words
The pharmaceutical preparation of claim 1 wherein said fatty acid ester of glycerin is ethoxylated with about 7 mols of ethylene oxide.
Claim 5
Dependent Claim
36 words
The pharmaceutical preparation of claim 2 wherein said ester of a polyoxyalkylene diol with a fatty acid is the stearate of a polyoxyethylene glycol having an average molecular weight of said polyoxyethylene glycol of about 100.
Claim 6
Dependent Claim
21 words
The pharmaceutical preparation of claim 2 wherein component (e) is present in an amount of from 1% to 10% by weight.
Claim 7
Dependent Claim
31 words
The pharmaceutical preparation of claim 1 or 2, wherein said non-aqueous solvent dissolves at least 10% by weight of isosorbide dinitrate, based on the solvent, and is infinitely miscible with water.
Claim 8
Dependent Claim
52 words
The pharmaceutical preparation of claim 1 or 2 wherein the amount of said non-aqueous solvent is so selected that the ratio by weight of dissolved to undissolved isosorbide dinitrate is from 1 to 60:99 to 40, after application of the preparation to the human skin and after reaching of a water equilibrium.
Claim 9
Dependent Claim
18 words
The pharmaceutical preparation of claim 7 wherein said ratio by weight is from 5 to 60:95 to 40.
Claim 10
Dependent Claim
38 words
The pharmaceutical preparation of claim 1 or 3 wherein at least 90% by weight of the isosorbide dinitrate is present as particles having a length of at most 100 μm and a breadth of at most 20 μm.
Claim 11
Dependent Claim
27 words
The pharmaceutical preparation of claim 9 wherein said isosorbide dinitrate particles have a length of less than 60 μm and a breadth of less than 10 μm.
References Cited (Backward Citations)
US4112115A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-10-05 | 1985-04-06 | 1985-10-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-10-05 | 1989-04-06 | 1989-10-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-10-05 | 1993-04-06 | 1993-10-06 | $7700.00 | Window Closed / Lapsed |