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Claims for Patent: 6,645,961

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Claims for Patent: 6,645,961

Title: Dry granulation formulation for an HIV protease inhibitor
Abstract:This invention relates to a dry granulation capsule formulation of the HIV protease inhibitor, indinavir sulfate, which is useful in the treatment of AIDS, ARC or HIV infection. Processes for making the oral formulation are also disclosed.
Inventor(s): Lui; Chung Y. (Lansdale, PA), Ostovic; Drazen (Lansdale, PA), Katdare; Ashok V. (Norristown, PA), Stelmach; Christine (Tinton Falls, NJ)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:09/045,885
Patent Claims: 1. A pharmaceutical composition which comprises about 50 to 90% by weight of an active ingredient which is indinavir sulfate, about 10 to 50% by weight of a low moisture or anhydrous excipient and about 0.5 to 2% by weight of a lubricant.

2. The pharmaceutical composition of claim 1, wherein the excipient is selected from anhydrous lactose, low moisture microcrystalline cellulose or anhydrous calcium phosphate dibasic, and the lubricant is selected from magnesium stearate, sodium lauryl sulfate, sodium stearyl fumarate or hydrogenated vegetable oil.

3. The pharmaceutical composition of claim 2 which comprises by weight, about 70 to 80% by weight indinavir sulfate, about 20 to 30% by weight of the excipient and about 0.8% to 1.5% by weight of the lubricant.

4. The pharmaceutical composition of claim 3, wherein the excipient is anhydrous lactose and the lubricant is magnesium stearate.

5. The pharmaceutical composition of claim 4 which comprises by weight, about 75 to 78% by weight indinavir sulfate, about 22 to 25% by weight anhydrous lactose and about 0.9% to 1.1% by weight magnesium stearate.

6. The pharmaceutical composition of claim 5 which comprises by weight, about 76% by weight indinavir sulfate, about 23% by weight anhydrous lactose and about 1% by weight magnesium stearate.

7. The pharmaceutical composition of claim 6 in the form of a capsule.

8. A process for making a pharmaceutical composition containing an active ingredient of indinavir sulfate, comprising the steps of: (a) mixing about 50 to 90% by weight of the active ingredient with about 10 to 50% by weight of a low moisture or anhydrous excipient and about 0.25 to 1% by weight of a first lubricant; (b) compacting the mix from step (a) to form compacts; (c) milling the compacts from step (b) to form granules; (d) lubricating the granules from step (c) with about 0.25 to 1% by weight of a second lubricant; and (e) forming the lubricated granules from step (d) into a pharmaceutical composition.

9. The process of claim 8, wherein the pharmaceutical composition is formed by encapsulating the lubricated granules from step (d) to form a capsule.

10. The process of claim 8, further comprising the steps of: (f) bieving the compacts discharged from the compactor in step (b) prior to milling; (g) collecting the uncompacted material from step (f); and (h) recycling the collected material back to the compactor.

11. The process of claim 9, wherein the excipient is selected from anhydrous lactose, low moisture microcrystalline cellulose or anhydrous calcium phosphate dibasic, and the first and second lubricants are each independently selected from magnesium stearate, sodium lauryl sulfate, sodium stearyl fumarate or hydrogenated vegetable oil.

12. The process of claim 11, wherein the excipient is anhydrous lactose and the first and second lubricants are both magnesium stearate.

13. The process of claim 11, wherein the capsule contains about 70 to 80% by weight indinavir sulfate, about 20 to 30% by weight anhydrous lactose and about 0.8% to 1.5% by weight magnesium stearate.

14. The process of claim 13, wherein the capsule contains about 75 to 78% by weight indinavir sulfate, about 22 to 25% by weight anhydrous lactose and about 0.9% to 1.1% by weight magnesium stearate.

15. The process of claim 14, comprising the steps of: (a) mixing about 76% by weight indinavir sulfate, with about 23% by weight anhydrous lactose and about 0.5% by weight magnesium stearate; (b) compacting the mix from step (a) in a roller compactor to form compacts; (c) milling the compacts from step (b) to form granules; (d) lubricating the granules from step (c) with about 0.5% by weight magnesium stearate; and (e) encapsulating the lubricated granules from step (d) to form the capsule.

16. The process of claim 9, comprising the steps of: (a) mixing about 70 to 80% by weight indinavir sulfate with about 20 to 30% by weight of the excipient and about 0.4 to 0.75% by weight of the first lubricant in a ribbon mixer for approximately ten minutes at 20 rpm; (b) compacting the mix from step (a) in a roller compactor at four to ten tons force to form compacts; (c) milling the compacts from step (b) using a 0.062 inch screen at a speed of 2000 to 2500 rpm to form granules; (d) lubricating the granules from step (c) with about 0.4 to 0.75% by weight of the second lubricant; and (e) encapsulating the lubricated granules from step (d) to form the capsule.

17. The process of claim 16, wherein the excipient is anhydrous lactose, and the first and second lubricants are magnesium stearate.

18. The process of claim 17, comprising the steps of: (a) mixing about 75 to 78% by weight indinavir sulfate with about 22 to 25% by weight anhydrous lactose and about 0.45 to 0.55% by weight magnesium stearate in a ten cubic foot ribbon mixer for approximately ten minutes at 20 rpm for a total of approximately 200 revolutions; (b) compacting the mix from step (a) in a roller compactor at four to ten tons force at a speed of 7 to 15 rpm and a feed speed of 10 to 60 rpm to form compacts; (c) milling the compacts from step (b) in a CoMil.RTM. using a 0.062 inch screen at a speed of 2000 to 2500 rpm to form granules; (d) lubricating the granules from step (c) with about 0.45 to 0.55% by weight magnesium stearate in a ten cubic foot ribbon mixer for approximately five minutes at 20 rpm for a total of approximately 100 revolutions; and (e) encapsulating the lubricated granules from step (d) in a Bosch GKF encapsulation machine to form the capsule.

19. A pharmaceutical composition made by the process of claim 8.
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