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Claims for Patent: 5,989,591

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Claims for Patent: 5,989,591

Title: Rapamycin formulations for oral administration
Abstract:This invention provides rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising rapamycin, one or more surface modifying agents, one or more sugars, and optionally one or more binders.
Inventor(s): Nagi; Arwinder S. (Thiells, NY)
Assignee: American Home Products Corporation (Madison, NJ)
Application Number:09/038,541
Patent Claims: 1. A rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising:

(a) rapamycin in an amount from about 0.05-20 mg,

(b) poloxamer 188 in an amount from about 0.008-10 mg, and

(c) sucrose in an amount comprising up to about 40-99% weight of the sugar overcoat.

2. A rapamycin solid dosage unit which comprises a core and a sugar overcoat; said sugar overcoat comprising

(a) rapamycin in an amount from about 0.05-20 mg,

(b) poloxamer 188 in an amount from about 0.008-10 mg,

(c) povidone in a range from 0.02-1.0% weight of said sugar overcoat,

(d) microcrystalline cellulose in a range from about 0.1-3% weight of said sugar overcoat, and

(e) sucrose in a range from about 35-99% weight of said sugar overcoat.

3. The dosage unit according to claim 2, wherein the poloxamer 188 is contained in an amount from about 0.25-10 mg.

4. The dosage unit according to claim 3, wherein the povidone is contained as about 0.5% weight of said sugarcoat.

5. The dosage unit according to claim 4, wherein the microcrystalline cellulose as about 1% weight of said sugarcoat.

6. The dosage unit according to claim 2, wherein

(a) rapamycin is contained in an amount of about 1 mg,

(b) poloxamer 188 is contained in an amount of about 0.5 mg,

(c) povidone is contained as about 0.5% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a range from about 95-99% weight of said sugar overcoat.

7. The dosage unit according to claim 2, wherein

(a) rapamycin is contained in an amount of about 0.5 mg,

(b) poloxamer 188 is contained in amount of about 0.25 mg,

(c) povidone is contained as about 0.05% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a rage from about 96-99% weight of said sugar overcoat.

8. The dosage unit according to claim 2, wherein

(a) rapamycin is contained in an amount of about 3 mg,

(b) poloxamer 188 is contained in amount of about 1.5 mg,

(c) povidone is contained as about 0.5% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a range from about 90-96% weight of said sugar overcoat.

9. The dosage unit according to claim 2, wherein

(a) rapamycin is contained in an amount of about 5 mg,

(b) poloxamer 188 is contained in an amount of about 2.5 mg,

(c) povidone is contained as about 0.5% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a range from about 80-96% weight of said sugar overcoat.

10. The dosage according to claim 2, wherein

(a) rapamycin is contained in an amount of about 7.5 mg,

(b) poloxamer 188 is contained in an amount of about 3.75 mg,

(c) povidone is contained as about 0.5% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a range from about 75-90% weight of said sugar overcoat.

11. The dosage unit according to claim 2, wherein

(a) rapamycin is contained in an amount of about 10 mg,

(b) poloxamer 188 is contained in an amount of about 5 mg,

(c) povidone is contained as about 0.5% weight of said sugar overcoat,

(d) microcrystalline cellulose is contained as about 1% weight of said sugar overcoat, and

(e) sucrose is contained in a range form about 65-90% weight of said sugar overcoat.

12. A process for preparing a rapamycin oral dosage tablet which comprises preparing a sugar overcoat by employing to the following steps,

(a) preparing rapamycin dispersion in one or more surface modifying agents, wherein at least one of the surface modifying agents is poloxamer 188 in which the ratio of rapamycin to poloxamer 188 is between about 2:1 to 6:1 by weight,

(b) adding two or more binders to the dispersion, wherein at least two of the binders are povidone and microcrystalline cellulose

(c) adding one or more sugars to the dispersion and stirring until dissolved,

wherein at least one of the sugars is sucrose in a quantity of about 35-99% weight of the dried overcoat,

(d) adding water to the mixture, and stirring until dissolved, and spraying the overcoat onto a core and drying until the desired quantity of rapamycin has been sprayed onto the core.

13. The process according to claim 12, wherein the quantity of povidone is about 0.2-1% weight of the dried overcoat.

14. The process according to claim 13, wherein the quantity of microcrystalline cellulose is about 0.1-3% of the dried overcoat.
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