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Claims for Patent: 9,023,391

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Claims for Patent: 9,023,391

Title:Stable benzimidazole formulation
Abstract: A stable composition with a benzimidazole derivative, such as Omeprazole, which does not contain a separating layer between the active compound and an enteric coating layer. Instead, the enteric coating layer is applied as a solution with a pH value of at least 6.5, and more preferably in a range of from about 7 to about 10, directly to the benzimidazole derivative substrate. This solution, with the optional addition of a plasticizer, can be directly coated onto the substrate without any necessity for an intermediate layer. Furthermore, in this pH range, the enteric coating is optionally applicable in an aqueous solution, thereby obviating the need for organic solvents for dissolving the enteric coating material. The resultant formulation maintains the stability of the benzimidazole derivative during storage and at the same time protects the product during passage through the acidic environment of the stomach. The problem of interaction between the enteric coat and the alkaline core is thus completely eliminated as the enteric coat at this stage is no longer acidic.
Inventor(s): Lahav; Raffael (Qiriat Bialik, IL), Azoulay; Valerie (Pardes Hana, IL)
Assignee: Dexcel Ltd. (Or-Akiva, IL)
Application Number:11/785,300
Patent Claims: 1. A stable composition for oral administration of a benzimidazole derivative, the composition consisting essentially of: (a) a single tablet core consisting essentially of 1) a benzimidazole derivative; 2) sodium stearate in an amount between about 0.09% to about 4% by weight of the core which is effective to stabilize the benzimidazole derivative in the composition; 3) at least one excipient that is not a stabilizing material; and (b) a single layer comprising an enteric polymer selected from the group consisting of HPMCAS, CAP, polyvinyl acetate phthalate, cellulose acetate trimellitate, polymethacrylic acid methacrylate, and ethyl methacrylate, the enteric polymer having been layered directly onto the core from a solution or dispersion having a pH of at least pH 6.5 and comprising a neutralizing agent selected from the group consisting of sodium, potassium and ammonium hydroxide.

2. The composition of claim 1, wherein the non-stabilizing excipient is selected from the group consisting of sodium stearyl fumarate, sodium starch glycolate and lactose.

3. The composition of claim 1, wherein the non-stabilizing excipient is povidone.

4. The composition of claim 1, wherein the single enteric layer further comprises a plasticizer selected from the group consisting of a citric acid ester and a phthalic acid ester.

5. The composition of claim 1, wherein the single enteric layer further comprises sodium lauryl sulfate and talc.

6. The composition of claim 1, wherein the enteric polymer is at least about 60% neutralized prior to said single layer being layered directly over the single tablet core.

7. The composition of claim 6, wherein the enteric polymer is at least about 80% neutralized prior to said single layer being layered directly over the single tablet core.

8. The composition of claim 7, wherein the enteric polymer is at least about 95% neutralized prior to said single layer being layered directly over the single tablet core.

9. The composition of claim 1, wherein the single enteric layer further comprises one or more of a glidant, coloring agent or polishing agent.

10. The composition of claim 1, wherein the benzimidazole derivative is selected from the group consisting of Omeprazole, Pantoprazole, Lansoprazole, Leminoprazole, Perprazole, Rabeprazole, and pharmaceutically acceptable salts thereof.

11. The composition of claim 1, wherein the single tablet core comprises an active core for containing the benzimidazole derivative.

12. The composition of claim 1, wherein the active core is a tablet formed by compression.

13. A stable tablet composition for oral administration of a benzimidazole derivative, the composition consisting essentially of: a single tablet core, the single tablet core consisting essentially of the benzimidazole derivative, sodium stearate in an effective amount of about 4% by weight of the core to stabilize the benzimidazole derivative in the composition; and at least one excipient that is not a stabilizing material; and a single layer comprising an enteric polymer consisting essentially of neutralized HPMCAS, said HPMCAS having been neutralized to a pH of at least 6.5 by an alkalizing agent comprising ammonium hydroxide, the single layer layered directly over said single tablet core.

14. The composition of claim 1, wherein the sodium stearate is present in the core in an amount of about 4% by weight of the core.
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