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US4780455A Expired / Lapsed US ⏱️ 0.0 years remaining

Lipophilic complexes of pharmacologically active organic compounds

Assignee: Columbia University
•
Filing: 1985-04-12
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Granted: 1988-10-25
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Expires: 2005-04-12
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Abstract

Abstract The present invention provides a composition with the structure (L)m(E)n wherein m and n are each integers, and m and n are different or the same; L is an ampholytic lipid or polymer, or a nonampholytic lipid with hydrophobic properties; E is a nonlipophilic ionic inorganic ester of an organic compound, E having the structural formula Z+qR-Y-X-(O)p-q wherein R is an organic moiety; Y is oxygen, sulfur or a substituted nitrogen, X is sulfur, phosphorus, nitrogen or boron; p is the integer 2 or the integer 3; Z is hydrogen or a metal, and Q is an integer indicating the elecrical charge. Suitable ampholytic lipids are phospholipids, sulfatides, and sphingomyelins. The esters can be sulfate or phosphate esters of steroid hormones. The compositions are useful for example, for altering the solubility properties of the esters, and for developing controlled-delivery systems for pharmaceuticals.

Inventors

  • 👤 Seymour Lieberman
  • 👤 V. V. K. Prasad
  • 👤 Laura Ponticorvo

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 18:50
CPC Classifications
C; C07; C07J; C07J51/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/543; A61K47/544; C07J31/00

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 57 words
A lipophilic composition having the formula: (L).sub.m (E).sub.n wherein (L) m and (E) n are bound as a complex, wherein L is selected from the group consisting of phospholipids, cardiolipins, distearins and tristearins; wherein E is cholesterol sulfate or sodium cholesterol sulfate; and wherein m and n are each integers which may be the same or different.
Claim 2
Dependent Claim 57 words
A lipophilic composition having the formula: (L).sub.m (E).sub.n wherein (L) m and (E) n are bound as a complex, wherein L is selected from the group consisting of phospholipids, cardiolipins, distearins and tristearins; wherein E is cholesterol sulfate or sodium cholesterol sulfate; and wherein m and n are each integers which may be the same or different.
Claim 3
Dependent Claim 11 words
A composition according to claim 1, wherein the phospholipid is phosphatidylethanolamine.
Claim 4
Dependent Claim 22 words
A method of forming the complex of claim 1, comprising contacting the L and the E in the presence of a solvent.
Claim 5
Dependent Claim 18 words
A method according to claim 3, wherein the lipophilic phase comprises the solvent isooctane, benzene, chloroform, or hexane.
Claim 6
Dependent Claim 40 words
A pharmaceutical complex comprising at least one composition according to claim 1 in combination with at least one pharmacologically acceptable excepient, the preparation being a preparation in the form of a solid, paste, liquid, oily suspension, powder, pill, or capsule.
Claim 7
Dependent Claim 16 words
The pharmaceutical composition according to claim 5, wherein the composition is a sustained release dosage form.

References Cited (Backward Citations)

US3919430A Cited
US3934013A Cited
US4248867A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-10-25 1992-04-25 1992-10-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-10-25 1996-04-25 1996-10-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-10-25 2000-04-25 2000-10-25 $7700.00 Window Closed / Lapsed

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