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Details for Patent: 5,043,107

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Details for Patent: 5,043,107

Title: Preparation small unilamellar vesicles including polyene antifungal antibiotics
Abstract:Formulations consisting of phospholipid small unilamellar particles encapsulating polyene antifungal antibiotics and methods for using such compositions to treat systemic fungal infections are described. In a preferred embodiment, the particles are in the form of vesicles which comprise a polyene antifungal antibiotic, preferably amphotericin B and/or nystatin, egg phosphatidylcholine and cholesterol, preferably in the molar ratio of about 0.2 (AMB):2(PL):1(CHOL). These vesicles may also have an amine modified surface. The vesicles are suspended in a low ionic strength saccharide/tris solution at a pH of from about 6.0 to about 8.0 and may be administered to deliver the anti-fungal antibiotic to treat systemic fungal infections.
Inventor(s): Adler-Moore; Jill (Altadena, CA), Gamble; Ronald C. (Altadena, CA), Proffitt; Richard T. (Arcadia, CA)
Assignee: Vestar Research, Inc. (Pasadena, CA)
Filing Date:Oct 27, 1989
Application Number:07/427,732
Claims:1. A process for preparing an injectable composition comprising small unilamellar vesicles including a polyene antifungal antibiotic, comprising the steps of:

a) dissolving at least one phospholipid and cholesterol in an aliphatic alcohol having from four to eight carbon atoms;

b) dissolving a polyene antifungal antibiotic in a solvent selected from the group consisting of dimethylsulfoxide and dimethylformamide;

c) mixing the solutions of steps (a) and (b);

d) evaporating the mixed solvents to produce a lipid cholesterol antibiotic mixture;

e) hydrating the mixture with an aqueous phase of low ionic strength; and

f) forming small unilamellar vesicles containing the polyene antifungal antibiotic from the hydrated mixture.

2. The process of claim 1 in which the aliphatic alcohol is selected from the group consisting of heptanol and octanol.

3. The process of claim 1 or 2 in which the aqueous phase is a saccharide solution.

4. The process of claim 3 in which the polyene antifungal antibiotic, at least one phospholipid, and cholesterol are in a mole percentage ratio ranging from about 5-15 mole percent polyene antifungal antibiotic, about 40-90 mole percent phospholipid and about 10-40 mole percent cholesterol.

5. The process of claim 3 in which the polyene antifungal antibiotic is selected form the group consisting of amphotericin B and nystatin.

6. The process of claim 3 in which the saccharide is selected from the group consisting of sucrose, lactose, glucose, fructose and galactose.

7. The process of claim 6 in which the polyene antifungal antibiotic, at least one phospholipid, and cholesterol are in a mole percentage ratio ranging from about 5-15 mole percent polyene antifungal antibiotic, about 40-90 mole percent phospholipid and about 10-40 mole percent cholesterol.

8. The process of claim 6 in which the polyene antifungal antibiotic is selected from the group consisting of amphotericin B and nystatin.

9. The process of claim 1 or 2 in which the polyene antifungal antibiotic, at least one phospholipid, and cholesterol are in a mole percentage ratio ranging from about 5-15 mole percent polyene antifungal antibiotic, about 40-90 mole percent phospholipid and about 10-40 mole percent cholesterol.

10. The process of claim 9 in which the polyene antifungal antibiotic is selected from the group consisting of amphotericin B and nystatin.

11. The process of claim 1 or 2 in which the polyene antifungal antibiotic is selected from the group consisting of amphotericin B and nystatin.
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