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US4322433A Expired / Lapsed US ⏱️ 0.0 years remaining

Percutaneous administration of nitroglycerine

Assignee: Euro Celtique SA
•
Filing: 1980-11-03
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Granted: 1982-03-30
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Expires: 2000-11-03
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Abstract

Abstract A preparation for percutaneous administration of nitroglycerine, said preparation comprising nitroglycerine incorporated in a cream base in an amount not less than about 0.05% by weight based on the total weight of the preparation. The composition may also contain other medicaments, the bioavailability of which is enhanced by the nitroglycerine. The action of the preparation against for example angina may be brought about by having an appropriate amount of nitroglycerine or as additional medicament another medicament active against angina. The preparation may contain an hydroxyalkylcellulose which may provide, in combination with a waxy component in the cream, for example a higher aliphatic alcohol, a prolonged release effect. The preparation has advantages particularly as regards bioavailability over prior uniphasic ointments.

Inventors

  • 👤 Stewart T. Leslie
  • 👤 Alan Rhodes
  • 👤 Cyril Boroda
  • 👤 Alfred Halpern

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 11:20
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K31/00; A61K31/21

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 69 words
Composition for the percutaneous administration of nitroglycerine, said composition comprising a physiologically compatible biphasic lipophilic/hydrophilic carrier having a hydrophilic/lipophilic balance value of 8-14 and having distributed therein nitroglycerine for percutaneous administration by topical application in an antianginally effective amount, and also having distributed therein to promote the percutaneous absorption of said nitroglycerine upon topical application of said composition an additional amount of at least 0.05% by weight of nitroglycerine.
Claim 2
Dependent Claim 69 words
Composition for the percutaneous administration of nitroglycerine, said composition comprising a physiologically compatible biphasic lipophilic/hydrophilic carrier having a hydrophilic/lipophilic balance value of 8-14 and having distributed therein nitroglycerine for percutaneous administration by topical application in an antianginally effective amount, and also having distributed therein to promote the percutaneous absorption of said nitroglycerine upon topical application of said composition an additional amount of at least 0.05% by weight of nitroglycerine.
Claim 3
Dependent Claim 32 words
Composition according to claim 1 wherein the hydrophilic component of said carrier is water, propylene glycol or glycerine and wherein the lipophilic component is a higher aliphatic alcohol or an ester thereof.
Claim 4
Dependent Claim 32 words
Composition according to claim 1 wherein said nitroglycerine, for percutaneous administration is present in a total amount with said nitroglycerine for promoting absorption thereof of about 0.75-1.25% by weight of the composition.
Claim 5
Dependent Claim 18 words
Composition according to claim 3 wherein said nitroglycerine is used in the form of a stabilized lactose adsorbate.
Claim 6
Dependent Claim 15 words
Composition according to claim 1 wherein said carrier includes emulsifiers to provide said hydrophilic/lipophilic balance.
Claim 7
Dependent Claim 16 words
Composition according to claim 1 wherein said carrier is in the form of a cream base.
Claim 8
Dependent Claim 12 words
Composition according to claim 1 and also including hydroxyloweralkylcellulose in the carrier.
Claim 9
Dependent Claim 21 words
Method of achieving percutaneous administration of nitroglycerine, which comprises topically applying the composition of claim 1 to a patient requiring nitroglycerine.
Claim 10
Dependent Claim 56 words
Method of producing the composition of claim 1, which comprises dispersing said nitroglycerine in a lipophilic phase of a higher aliphatic alcohol of 8-18 carbon atoms, mixing the resultant lipophilic phase containing nitroglycerine with a hydrophilic phase of water, propylene glycol or glycerine and with said nitroglycerine for percutaneous administration, and emulsifying the thus obtained mixture.
Claim 11
Dependent Claim 20 words
Method according to claim 9 wherein said aliphatic alcohol is substituted by a further aliphatic group containing 8-18 carbon atoms.
Claim 12
Dependent Claim 17 words
Method according to claim 9 wherein said nitroglycerine is dispersed in the form of a lactose adsorbate.
Claim 13
Dependent Claim 12 words
Method according to claim 9 wherein the emulsion is modified with hydroxyloweralkylcellulose.
Claim 14
Dependent Claim 27 words
Method according to claim 12 wherein the amount of said hydroxylowerlakylcellulose is one part by weight per each 2-4 parts by weight of said higher aliphatic alcohol.

References Cited (Backward Citations)

US3609102A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-03-29 1985-09-28 1986-03-30 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-03-29 1989-09-28 1990-03-30 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-03-29 1993-09-28 1994-03-30 $7700.00 Window Closed / Lapsed

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