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Non-crystalline minoxidil composition, its production and application

Assignee: Liposome Technology Inc
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Filing: 1987-03-30
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Granted: 1989-05-09
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Expires: 2007-03-30
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Abstract

Abstract An aqueous, noncrystalline minoxidil composition for topical use. The composition contains minoxidil complexed with an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a sulfate, sulfonate, phosphate and phosphonate polar moiety. The composition may be formulated in ointment form, in an aqueous vehicle, or dispersed in a fluorochlorocarbon solvent, for spray delivery from a self-propelled spray device.

Inventors

  • 👤 Paul S. Uster
  • 👤 Yolanda P. Quinn

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 17:38
CPC Classifications
A; A61; A61K; A61K8/00; A61K8/02; A61K8/14; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/542; A61K47/543; A61K47/544; A61K8/18; A61K8/30; A61K8/49; A61K8/494; A61K8/4953; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61K9/127; A61K9/1271; A61K9/1272; A61P; A61P17/00; A61Q; A61Q7/00; Y; Y10; Y10S; Y10S436/00; Y10S436/829; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 49 words
A non-crystalline minoxidil composition formed by complexing mnoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.
Claim 2
Dependent Claim 49 words
A non-crystalline minoxidil composition formed by complexing mnoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.
Claim 3
Dependent Claim 26 words
The composition of claim 1, wherein the molar ratio of amphipathic compound to minoxidil is at least about 1:1, and the pH is between about 4-6.
Claim 4
Dependent Claim 25 words
The composition of claim 1, wherein the amphipathic compound is selected from the group consisting of sulfosuccinic acid hemiesters, alkyl phosphonates, and alkyl phosphate esters.
Claim 5
Dependent Claim 22 words
The composition of claim 1, which further includes phospholipids at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1.
Claim 6
Dependent Claim 20 words
The composition of claim 1, wherein the minoxidil and amphipathic compound are dispersed in non-crystalline form in a chlorofluorocarbon solvent.
Claim 7
Dependent Claim 57 words
The composition of claim 5, for use in forming a suspension of liposomes containing minoxidil in substantially monomolecular form, which further includes a phospholipid, at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1, wherein the composition is injected into an aqueous medium under conditions which result in liposome formation in the aqueous medium.
Claim 8
Dependent Claim 36 words
The composition of claim 5, for use in delivering minoxidil by means of a self-propelled atomizer device, wherein the composition is contained under pressure in a valved cannister operable to release the composition in spray form.
Claim 9
Dependent Claim 23 words
The composition of claim 7 which further includes a phospholipid, at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1.
Claim 10
Dependent Claim 37 words
The composition of claim 1, for use in administering minoxidil topically in ointment form, which further includes at least about 60% by weight of water, and minoxidil is present at a weight concentration of between about 1-5%.
Claim 11
Dependent Claim 22 words
The composition of claim 9, which further includes phospholipids, at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1.
Claim 12
Dependent Claim 27 words
A non-crystalline minoxidil composition comprising minoxidil complexed with an ethoxylated sulfosuccininc acid hemiester having a pK less than about 5 and containing a single lipophilic chain moiety.
Claim 13
Dependent Claim 27 words
A non-crystalline minoxidil composition comprising minoxidil complexed with an ethoxylated sulfosuccininc acid hemiester having a pK less than about 5 and containing a single lipophilic chain moiety.
Claim 14
Independent Claim 67 words
A method of applying minoxidil topically in a non-crystalline form which remains non-crystalline at least several hours after application to the skin, comprising complexing the minoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.
Claim 15
Independent Claim 67 words
A method of applying minoxidil topically in a non-crystalline form which remains non-crystalline at least several hours after application to the skin, comprising complexing the minoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.
Claim 16
Dependent Claim 25 words
The method of claim 12, wherein the amphipathic compound is selected from the group consisting of sulfosuccinic acid hemiesters, alkyl phosphonates, and alkyl phosphate esters.
Claim 17
Dependent Claim 47 words
The method of claim 12, for use in applying minoxidil in ointment form, which further includes formulating the minoxidil and amphipathic compound in an aqueous medium, to a final minoxidil weight concentration of between 1-5%, and a final weight concentration of water of at least about 60%.
Claim 18
Dependent Claim 30 words
The method of claim 14, which further includes adding adding phospholipids to the minoxidil and amphipathic compound, at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1.
Claim 19
Dependent Claim 39 words
The method of claim 12, for use in administering minoxidil in spray form, which further includes dispersing the minoxidil and amphipathic compound in a fluorochlorocarbon solvent, and spraying the resultant mixture from valved cannister containing the mixture under pressure.
Claim 20
Dependent Claim 28 words
The method of claim 16, wherein said dispersing includes adding a phospholipid to the mixture, at a phospholipid to minoxidil molar ratio of between about 1:1 and 4:1.
Claim 21
Independent Claim 65 words
A method of producing a topical, non-crystalline minoxidil composition which remains non-crystalline at least several hours after application to skin, comprising complexing the minoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.
Claim 22
Independent Claim 65 words
A method of producing a topical, non-crystalline minoxidil composition which remains non-crystalline at least several hours after application to skin, comprising complexing the minoxidil with the free acid form of an amphipathic compound having a pK less than about 5 and containing a single lipophilic chain moiety and a polar head group selected from the group consisting of a sulfate, sulfonate, phosphate and phosphonate group.

References Cited (Backward Citations)

US4670185A Cited
GB2145107A Cited
EP0161445A1 Cited
EP0177223A2 Cited
US4654354A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-05-08 1992-11-07 1993-05-09 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-05-08 1996-11-07 1997-05-09 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-05-08 2000-11-07 2001-05-09 $7700.00 Window Closed / Lapsed

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