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Details for Patent: 6,197,781

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Details for Patent: 6,197,781

Title: Pharmaceutical compositions
Abstract:A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.
Inventor(s): Guitard; Patrice (Hegenheim, FR), Haeberlin; Barbara (Riehen, CH), Link; Rainer (Staufen, DE), Richter; Friedrich (Grenzach-Wyhlen, DE)
Assignee: Novartis AG (Basel, CH)
Filing Date:Aug 13, 1999
Application Number:09/374,899
Claims:1. A method of forming a pharmaceutical composition comprising rapamycin wherein the method comprises:

(a) suspending rapamycin in a solvent to form a suspension,

(b) combining carrier components comprising a polyoxyethylene-polyoxypropylene co-polymer or block co-polymer, a polyvinylpyrrolidone, a microcrystalline cellulose and a water-soluble saccharose with the solvent,

(c) spray drying the suspension to form the pharmaceutical composition.

2. The method of claim 1, wherein the pharmaceutical composition is subsequently formed into a unit dosage form.

3. The method of claim 1, wherein the pharmaceutical composition is subsequently formed into a tablet.

4. The method of claim 1, wherein the pharmaceutical composition is subsequently filled into a capsule.

5. A method of claim 1, wherein the rapamycin is formed into a solid dispersion upon spray drying.

6. The method of claim 1, wherein the rapamycin is physically bound to the carrier component or components upon spray drying.

7. The method of claim 1, wherein the solvent is an organic solvent or a mixture of organic solvents.

8. A pharmaceutical composition comprising a rapamycin solid dispersion in a carrier medium comprising:

(a) a polyvinylpyrrolidone,

(b) a water-soluble saccharose,

(c) a microcrystalline cellulose, and

(d) a polyoxyethylene-polyoxypropylene co-polymer or block co-polymer.

9. The pharmaceutical composition of claim 8, in a unit dosage form.

10. The pharmaceutical composition of claim 8, in tablet form.

11. The pharmaceutical composition of claim 8, in capsule form.

12. The pharmaceutical composition of claim 8, in the form of a solid dispersion.

13. The pharmaceutical composition of claim 8, wherein the rapamycin is physically bound to the carrier medium.

14. A method of treating or preventing transplant rejection, comprising orally administering the pharmaceutical composition of claim 8 to a patient in need of such treatment or prevention.
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