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Details for Patent: 5,559,121

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Details for Patent: 5,559,121

Title: Rapamycin formulations for oral administration
Abstract:The present invention comprises oral rapamycin formulations which contain, per 100 ml of the formulation, from about 0.01 to about 10.0 grams per 100 ml of rapamycin, from about 0.1 to about 10 ml of surfactant, from about 0.1 to about 25 ml of N,N-dimethylacetamide, and from about 65 to about 99.8 ml of a lecithin or phospholipid solution.
Inventor(s): Harrison; Maureen M. (St. Albans, VT), Ofslager; Christian L. (Plattsburgh, NY), Waranis; Robert P. (Chazy, NY), Leonard; Thomas W. (Wilmington, NC)
Assignee: American Home Products Corporation (Madison, NJ)
Filing Date:May 23, 1995
Application Number:08/448,280
Claims:1. A composition comprising, per 100 ml composition, from about 0.01 to about 10.0 grams of rapamycin, from about 0.1 to about 10.0 ml of surfactant, from about 0.1 to about 25 ml of N,N-dimethylacetamide, and from about 65 to about 99.8 ml of a 50% lecithin or phospholipid solution.

2. The composition of claim 1 which contains, per 100 ml composition, from about 0.05 to about 5.0 grams of rapamycin, from about 0.5 to about 8.0 ml of surfactant, from about 0.5 to about 20 ml of N,N-dimethylacetamide, and from about 72 to about 99.0 ml of a 50% lecithin or phospholipid solution.

3. A composition of claim 1 which contains, per 100 ml composition, from about 0.10 to about 1.0 grams of rapamycin, from about 1.0 to about 5.0 ml of surfactant, from about 1.0 to about 10 ml of N,N-dimethylacetamide, and from about 85 to about 98.0 ml of a 50% lecithin or phospholipid solution.

4. The composition of claim 1 which is contained within a starch capsule.

5. The composition of claim 1 which is contained within a gelatin capsule.

6. The composition of claim 1 which is dispersed in a liquid.

7. The composition of claim 6 in which the liquid is water.

8. The composition of claim 7 in which the composition of matter is dispersed in water at a concentration in the range of from about 1 part of the compositon of matter into about 9 parts water to about 1 part of the compositon of matter into about 499 parts water.

9. The composition of claim 1 wherein the surfactant is polysorbate 80.

10. A composition comprising, per 100 ml of the composition,

a) a first 20 ml component of 2500 mg of rapamycin in N,N-dimethylacetamide; and

b) a second component of from about 0.05 gm/ml to about 0.07 gm/ml of surfactant in lecithin, the second component being added to the first 20 ml component to complete a 100 ml composition volume.
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