Patent EP0315467A2 successfully refreshed from Google Patents.
EP0315467A2
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EP
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Pentamidine salts useful in the treatment and prophylaxis of pneumocystis carinii pneumonia
Assignee: Fujisawa USA Inc
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Filing: 1988-11-04
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Granted: —
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Expires: 2008-11-04
Abstract
Abstract Salts of pentamidine, formulations containing such salts and the use of such salts for treatment or prophylaxis of pneumocystis carinii. Pentamidine gluconate and lactate has been discovered and found to have high water solubility while providing potentially less toxic alternatives to pentamidine isethionate, especially for aerosolized administration to patients suffering from acquired immunodeficiency syndrome, AIDS, or AIDS related complex, ARC.
Inventors
- 👤 Sadanand Pai
- 👤 Abu S. Alam
- 👤 John N. Kapoor
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 07:40
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/13; A61K31/155; C; C07; C07C; C07C59/00; C07C59/235; C07C59/245; C07C59/255; A61K9/00; A61K9/10; A61K9/127; A61P; A61P11/00; A61P33/00; A61P33/02; C07C53/00; C07C53/08; C07C53/10; C07C59/01; C07C59/08; C07C59/10; C07C59/105; C07C59/265
Claims Analysis
Total Claims: 43
Claim 1
Independent Claim
32 words
A salt of pentamidine with an acid selected from the group consisting of gluconic acid, lactic acid, acetic acid, tartaric acid, citric acid, phosphoric acid, boric acid, nitric acid, and sulfuric acid.
Claim 2
Dependent Claim
32 words
A salt of pentamidine with an acid selected from the group consisting of gluconic acid, lactic acid, acetic acid, tartaric acid, citric acid, phosphoric acid, boric acid, nitric acid, and sulfuric acid.
Claim 3
Dependent Claim
42 words
Pharmaceutical composition suitable for intravenous or intramuscular injection comprising a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate, and a pharmaceutically acceptable carrier.
Claim 4
Dependent Claim
42 words
Pharmaceutical composition suitable for intravenous or intramuscular injection comprising a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate, and a pharmaceutically acceptable carrier.
Claim 5
Dependent Claim
19 words
The composition of claim 2 wherein the salt is pentamidine gluconate or pentamidine lactate and the carrier comprises water.
Claim 6
Dependent Claim
10 words
The composition of claim 3 also comprising a buffering agent.
Claim 7
Dependent Claim
9 words
The composition of claim 3 which has been lyophilized.
Claim 8
Dependent Claim
19 words
The composition of claim 5 wherein the composition also comprises an agent for adjusting the tonicity of the composition.
Claim 9
Dependent Claim
17 words
7 A lipospmal pharmaceutical formulation comprising discrete lipid vesicles having entrained within the vesicles a pentamidine salt.
Claim 10
Dependent Claim
17 words
7 A lipospmal pharmaceutical formulation comprising discrete lipid vesicles having entrained within the vesicles a pentamidine salt.
Claim 11
Dependent Claim
41 words
The liposomal pharmaceutical formulation of claim 7 wherein the pentamidine salt is selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine hydrochloride, pentamidine phosphate, pentamidine borate, pentamidine nitrate, pentamidine sulfate, and pentamidine isethionate.
Claim 12
Dependent Claim
31 words
The formulation of claim 8 wherein the pentamidine salt is pentamidine gluconate, pentamidine isethionate or pentamidine lactate and said pentamidine salt is substantially entrained within a hydrophilic center of the liposomes.
Claim 13
Dependent Claim
31 words
The formulation of claim 9 wherein the formulation is in the form of a lyophilizate, which upon reconstitution with a physiologically acceptable carrier results in the formation of a liposomal suspension.
Claim 14
Dependent Claim
52 words
The formulation of claim 8 wherein the pentamidine salt is selected from the group consisting of pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine hydrochloride, pentamidine phosophate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate, and the pentamidine salt is substantially entrained within a hydrophobic lipid bilayer which forms a portion of the liposomes.
Claim 15
Dependent Claim
19 words
The formulation of claim 8 or claim 11 wherein the liposomes are suspended in a physiologically acceptable liquid carrier.
Claim 16
Dependent Claim
11 words
The formulation of claim 12 wherein the liquid carrier comprises water.
Claim 17
Dependent Claim
28 words
The formulation of claim 11 wherein the formulation is in the form of a lyophilizate, which upon reconstitution with a physiologically acceptable carrier will form a liposomal suspension.
Claim 18
Dependent Claim
87 words
A pharmaceutical formulation suitable for administration as an aerosol, by inhalation, comprising a solution or suspension of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine hydrochloride, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate; a physiologically acceptable carrier; such that the solution or suspension upon being ultrasonically nebulized will form a plurality of liquid droplets comprising the pentamidine salt and having a particle size in the range of about 0.5 to about 5 microns.
Claim 19
Dependent Claim
87 words
A pharmaceutical formulation suitable for administration as an aerosol, by inhalation, comprising a solution or suspension of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine hydrochloride, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate; a physiologically acceptable carrier; such that the solution or suspension upon being ultrasonically nebulized will form a plurality of liquid droplets comprising the pentamidine salt and having a particle size in the range of about 0.5 to about 5 microns.
Claim 20
Dependent Claim
26 words
The formulation of claim 15 wherein the pentamidine salt is selected from the group consisting of pentamidine gluconate and pentamidine lactate and the carrier comprises water.
Claim 21
Dependent Claim
28 words
The formulation of claim 15 wherein the solution upon being nebulized forms a plurality of liquid droplets having a particle size from about 1 to about 2 microns.
Claim 22
Independent Claim
50 words
A method for treating pneumocystis carinii pneumonia comprising administering to a patient suffering from pneumocystis carinii pneumonia, a therapeutically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 23
Independent Claim
50 words
A method for treating pneumocystis carinii pneumonia comprising administering to a patient suffering from pneumocystis carinii pneumonia, a therapeutically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 24
Dependent Claim
20 words
The method of claim 18 wherein the pentamidine salt is administered either intramuscularly or intravenously as a solution or suspension.
Claim 25
Dependent Claim
18 words
The method of claim 18 wherein the pentamidine salt is administered intravenously or intramuscularly as a liposomal formulation.
Claim 26
Independent Claim
76 words
A method for prophylaxis against pneumocystis carinii pneumonia in an immuno-compromised patient who has had at least one episode of pneumocystis carinii pneumonia but who at the time of treatment is not exhibiting signs of pneumocystis carinii pneumonia, comprising administering to said patient a prophylactically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 27
Independent Claim
76 words
A method for prophylaxis against pneumocystis carinii pneumonia in an immuno-compromised patient who has had at least one episode of pneumocystis carinii pneumonia but who at the time of treatment is not exhibiting signs of pneumocystis carinii pneumonia, comprising administering to said patient a prophylactically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 28
Dependent Claim
14 words
The method of claim 21 wherein the pentamidine salt is administered as a solution.
Claim 29
Dependent Claim
15 words
The method of claim 21 wherein the pentamidine salt is administered as a liposomal formulation.
Claim 30
Dependent Claim
14 words
The method of claim 21 wherein the pentamidine salt is administered as an emulsion.
Claim 31
Independent Claim
64 words
A method for prophylaxis against an initial episode of pneumocystis carinii pneumonia in an immunocompromised patient who has never experienced an episode of pneumocystis carinii pneumonia, comprising administering to said patient a prophylactically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 32
Independent Claim
64 words
A method for prophylaxis against an initial episode of pneumocystis carinii pneumonia in an immunocompromised patient who has never experienced an episode of pneumocystis carinii pneumonia, comprising administering to said patient a prophylactically effective amount of a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 33
Dependent Claim
14 words
The method of claim 25 wherein the pentamidine salt is administered as a solution.
Claim 34
Dependent Claim
15 words
The method of claim 25 wherein the pentamidine salt is administered as a liposomal suspension.
Claim 35
Dependent Claim
17 words
The method of claim 18 or claim 25 wherein the pentamidine salt is administered as an emulsion.
Claim 36
Dependent Claim
37 words
The method of claim 18 or claim 21 or claim 25 wherein the pentamidine salt is administered by inhalation in the form a plurality of droplets having a particle size from about 0.5 to about 5 microns.
Claim 37
Dependent Claim
84 words
An injectable, stable, sterile composition comprising a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosophate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate in a unit dosage form in a sealed container, the composition being capable of being reconstituted with a suitable pharmaceutically acceptable carrier to form a liquid composition suitable for injection thereof into man, the unit dosage form comprising from about 10 mg to about 10 grams of the pentamidine salt.
Claim 38
Dependent Claim
84 words
An injectable, stable, sterile composition comprising a pentamidine salt selected from the group consisting of pentamidine gluconate, pentamidine lactate, pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine phosophate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate in a unit dosage form in a sealed container, the composition being capable of being reconstituted with a suitable pharmaceutically acceptable carrier to form a liquid composition suitable for injection thereof into man, the unit dosage form comprising from about 10 mg to about 10 grams of the pentamidine salt.
Claim 39
Dependent Claim
15 words
The composition of claim 30 wherein the pentamidine salt is pentamidine lactate or pentamidine gluconate.
Claim 40
Dependent Claim
25 words
A pharmaceutically useful composition comprising a substantially water insoluble pentamidine salt, water, and a sufficient amount of an emulsifying agent to emulsify the pentamidine salt.
Claim 41
Dependent Claim
25 words
A pharmaceutically useful composition comprising a substantially water insoluble pentamidine salt, water, and a sufficient amount of an emulsifying agent to emulsify the pentamidine salt.
Claim 42
Dependent Claim
33 words
The composition of claim 32 wherein the pentamidine salt is selected from the group consisting of pentamidine acetate, pentamidine tartarate, pentamidine citrate, pentamidine hydrochloride, pentamidine phosphate, pentamidine borate, pentamidine nitrate, and pentamidine sulfate.
Claim 43
Dependent Claim
13 words
The composition of claim 33 wherein the emulsifying agent comprises a phosphatidyl choline.
References Cited (Backward Citations)
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