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Claims for Patent: 5,879,706

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Claims for Patent: 5,879,706

Title: Valaciclovir tablets containing colloidal silicon dioxide
Abstract:A tablet comprising at least 50% w/w valaciclovir and 0.05 to 3% w/w colloidal silicon dioxide in which the valaciclovir is present within granules of the tablets and the silicon dioxide, a lubricant and a microcrystalline cellulose filler are present extragranularly has excellent hardness and friability properties while still maintaining lubrication of the tablet granules.
Inventor(s): Carter; Barry Howard (Kinston, NC), Tillman; Lloyd Gary (Carlsbad, CA)
Assignee: Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:08/875,172
Patent Claims: 1. A tablet comprising at least about 50% w/w valaciclovir or a salt thereof, a microcrystalline cellulose filler, a binding agent, a lubricant selected from the group consisting of talc, sodium lauryl sulphate and alkaline earth metal stearates and about 0.05 to about 3% w/w colloidal silicon dioxide wherein the valaciclovir or a salt thereof is present within the granules of the tablet, the lubricant, silicon dioxide and at least a portion of the filler is present extragranularly; wherein the friability of the tablet does not exceed 1%, the hardness is at least 9 kP, and the ejection force does not exceed 1000 Newtons.

2. A tablet as claimed in claim 1 wherein the colloidal silicon dioxide is present in an amount of about 0.1% to about 0.5% w/w.

3. A tablet as claimed in claim 1 wherein the filler is present in an amount of about 3% w/w to about 30% w/w.

4. A tablet as claimed in claim 3 wherein the filler is present at about 5% to about 15% w/w.

5. A tablet as claimed in claim 4, wherein the filler is present at about 10% w/w.

6. A process for preparing a tablet comprising at least about 50% w/w valaciclovir or a salt thereof, a binding agent, a lubricant selected from the group consisting of talc, sodium lauryl sulphate and alkaline earth metal stearate, about 0.05 to about 3% w/w colloidal silicon dioxide, and about 3 to about 30% w/w or microcrystalline cellulose filler; wherein the hardness of the tablet is at least 9 kPk, the friability is not more than 1%, and the ejection force is not more than 1000 N; said process comprising forming granules by mixing the valaciclovir or salt, optional binding agent or a portion thereof, and optionally a portion of filler; granulating with a granulating solution to form granules or dissolving the binding agent or a portion thereof in the granulating solution before adding to valaciclovir; drying the granules; blending the granules with the lubricant, colloidal silicon dioxide, and at least a portion of the filler; and then compressing the blended mixture to form a tablet.

7. A tablet as claimed in claim 1, wherein the particle size of filler is about 20 to about 300 .mu.m.

8. A tablet as claimed in claim 1 wherein the binding agent is present at about 1% to about 5% w/w.

9. A tablet as claimed in claim 1 wherein the binding agent is methylcellulose or povidone.

10. A tablet as claimed in claim 9 wherein the binding agent is povidone.

11. A tablet as claimed in claim 10 wherein the povidone is povidone K90 grade.

12. A tablet as claimed in claim 1 wherein the lubricant is present at about 0.1% to about 2.0% w/w.

13. A tablet as claimed in claim 12 wherein the lubricant is an alkaline earth metal stearate.

14. A tablet as claimed in claim 13 wherein the lubricant is magnesium stearate and is present at about 0.1% to about 1.0% w/w.

15. A tablet as claimed in claim 1 wherein the valaciclovir or its salt is present at about 65% to about 85% w/w.

16. A tablet as claimed in claim 1 comprising valaciclovir hydrochloride.

17. A tablet as claimed in claim 16 wherein the valaciclovir hydrochloride is anhydrous crystalline form including substantially a d spacing pattern as follows:

d spacing pattern (in Angstroms):

10. 20.+-.0.08, 8.10.+-.0.06, 7.27.+-.0.06, 6.08.+-.0.05, 5.83.+-.0.03, 5.37.+-.0.02, 5.23.+-.0.02, 4.89.+-.0.02, 4.42.+-.0.02, 4.06.+-.0.02, 3.71.+-.0.02, 3.39.+-.0.02, 3.32.+-.0.02, 2.91.+-.0.02, 2.77.+-.0.02.

18. A tablet as claimed in claim 1 wherein the tapped bulk density of valaciclovir or salt thereof is about 0.1 to about 0.9 g/cc.

19. A tablet as claimed in claim 1 which further includes a disintegrating agent present at about 0.05% to about 20% w/w.

20. A tablet as claimed in claim 19 wherein the disintegrating agent is a non-ionic disintegrating agent.

21. A tablet as claimed in claim 20 wherein the disintegrating agent is crospovidone present at about 0.5% to about 7% w/w.

22. A tablet comprising about 65% to about 85% w/w anhydrous crystalline valaciclovir hydrochloride including the d spacing diffraction pattern of claim 17, about 0.5% to about 5% w/w of povidone, about 3% to about 30% w/w of a microcrystalline cellulose filler, about 0.5 to about 7% w/w of a non-ionic disintegrating agent, about 0.1% to about 1.0% of an alkaline earth metal stearate lubricant and about 0.1% to about 0.5% w/w of colloidal silicon dioxide, wherein the valaciclovir hydrochloride is present intragranularly; and wherein the filler, stearate lubricant and colloidal silicon dioxide are present extragranularly.

23. A tablet as claimed in claim 1 which is film coated.

24. A tablet as claimed in claim 1 for use in medical therapy.

25. A method of treatment of a herpes virus infection in a human comprising administering to the host one or more tablets as claimed in claim 1 to administer an effective anti-herpes viral amount of valaciclovir or a salt thereof.

26. A process for preparing a tablet comprising at least about 50% w/w valaciclovir or a salt thereof, a binding agent, a microcrystalline cellulose filler, a lubricant selected from the group consisting of talc, sodium lauryl sulphate and alkaline earth metal stearate and about 0.05 to about 3.0% colloidal silicon dioxide, wherein the friability of the tablet does not exceed 1%, the hardness is at least 9 kP and the ejection force does not exceed 10000 N; said process having the valaciclovir or its salt present within the granules of the tablet, and the lubricant, colloidal silicon dioxide, and at least a portion of the microcrystalline cellulose filler present extragranularly.

27. A process for preparing a tablet comprising at least about 50% w/w valaciclovir or a salt thereof, a binding agent, a microcrystalline cellulose filler, a lubricant selected from the group consisting of talc, sodium lauryl sulphate and alkaline earth metal stearate, and about 0.05 to 3.0% w/w colloidal silicon dioxide; wherein the hardness of the tablet is at least 9 kP, the friability is not more than 1%, and the ejection force is not more than 1000 N; said process comprising forming granules which include valaciclovir or a salt thereof and then blending the lubricant, colloidal silicon dioxide and at least a portion of the filler with said granules.

28. A process according to claim 26 comprising forming granules by mixing said valaciclovir or salt, optionally a binding agent or a portion thereof, and optionally a portion of the filler; granulating with a granulating solution to form granules or dissolving the binding agent or a portion in the granulating solution before adding to valaciclovir; drying the granules; blending the granules with the lubricant, colloidal silicon dioxide, and filler or a portion thereof; and then compressing the blended mixture to form a tablet.
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