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Claims for Patent: 7,544,370

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Claims for Patent: 7,544,370

Title:Pantoprazole multiparticulate formulations
Abstract:Pantoprazole sodium multiparticulates are described which avoid sticking to nasogastric and gastronomy tubes. The pantoprazole multiparticulates have a spheroid core of pantoprazole or an enantiomer thereof, or a salt thereof, a surfactant, and a distintegrant; a sub coat which is comprised of hydroxypropyl methylcellulose (hypromellose) and water, an enteric coat on the sub-coat, and a final seal coat over the enteric coat, which is composed of hydroxypropyl methylcellulose (hypromellose) and water.
Inventor(s): Venkata Ramana Rao; Sripriya (Iselin, NJ), Shah; Syed M. (East Hanover, NJ), Tatapudy; Hanumantharao (Suffern, NJ), Saunders; Richard William (Palisades, NY), Fawzi; Mahdi (Morristown, NJ), Nagi; Arwinder (Thiells, NY), Singh; Shailesh (Bardonia, NY), Hasan; Sumon A. (Monroe, NY)
Assignee: Wyeth (Madison, NJ)
Application Number:10/955,567
Patent Claims: 1. A method of producing a multiparticulate formulation of pantoprazole having reduced release under gastric conditions and fast release at neutral pH, said method comprising the steps of: producing a spheroid core comprising about 45% w/w pantoprazole sodium sesquihydrate, as a sole active component in the multiparticulate formulation and about 25% to 30% w/w microcrystalline cellulose, about 4% to 6% w/w polysorbate 80, about 14% to 16% w/w crospovidone, about 0.5 to 2% w/w hydroxypropyl methylcellulose, and about 5% to 8% w/w sodium carbonate a surfactant via extrusion and spheronization, said core further containing about 1 to about 2% w/w water; applying an initial seal coat comprising hydroxypropyl methylcellulose to the spheroid core, applying an enteric coating to the initial seal coated spheroid core, said enteric coating comprising a copolymer of methacrylic acid and methacrylates; and optionally applying a final seal coat to the enteric-coated spheroid core, said final seal coat being about 1 wt % of the multiparticulate; wherein the multiparticulates have an average diameter of about 0.7 mm to about 1.25 mm.

2. The method according to claim 1, wherein the spheroid core is prepared by mixing the ingredients in a low shear mixer at low shear conditions at a range of about 25 rpm to 35 rpm.

3. The method according to claim 2, wherein the low shear conditions are 32 rpm.

4. The method according to claim 2, wherein the spheroid cores are dried at a low temperature not exceeding about 40.degree. C. for a period of 8 to 72 hours to a percent (%) loss-on-drying (LOD) of 3.4% to 4.3%.

5. The method according to claim 1, further comprising the step of applying a layer of talc in an amount of 0.05% w/w to 0.1% w/w of the multiparticulates.

6. The method according to claim 1, wherein the enteric coating is sprayed as a suspension onto the spheroid core.

7. Pantoprazole multiparticulates having reduced release under gastric conditions and fast release at neutral pH, wherein each of said multiparticulates comprises: a spheroid core comprising about 45% w/w pantoprazole sodium sesquihydrate as a sole active component in the multiparticulates about 25% to 30% w/w microcrystalline cellulose, about 4% to 6% w/w polysorbate 80, about 14% to 16% w/w crospovidone, about 0.5 to 2% w/w hydroxypropyl methylcellulose, about 5% to 8% w/w sodium carbonate, and about 1 to 2% w/w water; an initial seal coat comprising hydroxypropyl methylcellulose on the spheroid core; and an enteric coat on the initial seal coat, wherein said multiparticulates have an average diameter of about 0.7 mm to about 1.25 mm.

8. The multiparticulates according to claim 7, wherein said multiparticulates have an average diameter of about 1 mm.

9. The multiparticulates according to claim 7, wherein said enteric coat comprises about 48% w/w of the particulate,

10. The multiparticulates according to claim 7, further comprising a final seal coat on the enteric coat.

11. The multiparticulates according to claim 10, wherein the final seal coat comprises about 0.1 to 10 wt % of the multiparticulates.

12. The multiparticulates according to claim 10, wherein the final seal coat comprises hydroxypropyl methylcellulose (hypromellose).

13. The multiparticulates according to claim 7 wherein said initial seal coat is in the range of about 2 to about 4% w/w of the weight of the uncoated core.

14. The multiparticulates according to claim 7, wherein the enteric coating comprises about 30% w/w of methacrylic acid and methyacrylate copolymer, about 15% w/w talc, about 3% triethyl citrate and a pH adjuster; said amounts being by weight of the multiparticulates.

15. A pantoprazole formulation comprising a suspension comprising the multiparticulates of claim 7 and a physiologically compatible suspending liquid.

16. A capsule comprising the multiparticulates of claim 7.

17. A foil packet comprising the multiparticulates according to claim 7.

18. The method according to claim 1, wherein the spheroid core consists essentially of: TABLE-US-00013 pantoprazole sodium sesquihydrate about 45% w/w microcrystalline cellulose about 27% w/w polysorbate 80 about 5% w/w crospovidone about 15% w/w hydroxypropylmethylcellulose about 1% w/w sodium carbonate about 6.5% w/w: and water.

19. The pantoprazole multiparticulates according to claim 7, wherein the spheroid core consists essentially of: TABLE-US-00014 pantoprazole sodium sesquihydrate about 45% w/w microcrystalline cellulose about 27% w/w polysorbate 80 about 5% w/w crospovidone about 15% w/w hydroxypropylmethylcellulose about 1% w/w sodium carbonate about 6.5% w/w: and water.

20. A plurality of pantoprazole multiparticulates, each comprising: a spheroid core consisting essentially of about 45% w/w pantoprazole sodium sesquihydrate, about 27% w/w microcrystalline cellulose, about 5% w/w polysorbate 80; about 15% w/w crospovidone; about 1% w/w hydroxypropy methylcellulose, about 6.5% w/w sodium carbonate; and water; an inner seal coat comprising hydroxypropyl methylcellulose; and an enteric coating comprising a methacrylic acid and meth[yl]acrylate polymer, and triethylcitrate, wherein multiparticulates have an average diameter in the range of about 0.7 mm to about 1.25 mm.

21. The product according to claim 20, wherein the enteric coating further comprises talc.

22. The product according to claim 21, wherein the enteric coating further comprises sodium hydroxide.
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