Stable oral benzimidazole compositions and process of preparation thereof

1. A process for the preparation of a stable oral benzimidazole composition, the process comprising the steps of:

a. preparing a benzimidazole core formed by dispersing one or more amorphous benzimidazole compounds and one or more pharmaceutically acceptable additives in an aqueous or hydroalcoholic medium to obtain a dispersion and spraying the dispersion on to a pharmaceutically acceptable inert carrier at a bed temperature of less than about 50° C. for a total spraying time of less than about 24 hrs;

b. coating the core of step (a) with a separating layer; and

c. coating the product of step (b) with an enteric coating, wherein the composition contains less than about 30% by weight of crystalline benzimidazole after storage at 40° C. and 75% relative humidity for 3 months.

2. The process according to claim 1 , wherein the dispersion of step (a) is prepared in more than one lot.

3. The process according to any of the claim 1 or 2 , wherein the benzimidazole compounds are selected from one or more of omeprazole, lansoprazole, rabeprazole, pantoprazole, leminoprazole, pariprazole, single enantiomers, pharmaceutically accepted salts, solvates and their mixtures.

4. The process according to claim 1 , wherein the pharmaceutically acceptable additives are selected from one or more of binders, diluents, disintegrants, lubricants and wetting agents.

5. The process according to claim 1 , wherein the separating layer comprises a substantially water-soluble material.

6. The process according to claim 4 , wherein the binder is selected from one or more of cellulose derivatives, gums, water-soluble vinyl pyrrolidone polymers, and sugars.

7. The process according to claim 4 , wherein the diluent is selected from one or more of sugars, sugar alcohols, cellulose derivatives and starches.

8. The process according to claim 4 , wherein the disintegrant is selected from one or more of sodium starch glycolate, croscarmellose sodium, crospovidone and corn starch.

9. The process according to claim 4 , wherein the lubricant is selected from one or more of magnesium stearate, talc, sodium stearylfumarate and colloidal silicon dioxide.

10. The process according to claim 4 , wherein the wetting agent is selected from one or more of sodium lauryl sulphate and polysorbate 80.

11. The process according to claim 5 , wherein the substantially water-soluble material comprises one or more of a substantially water- soluble polymer and a substantially water-soluble excipient.

12. The process according to claim 11 , wherein the substantially water-soluble polymer is selected from one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, sodium alginate, sodium carboxymethyl cellulose and copolymer of vinylpyrrolidone and vinyl acetate.

13. The process according to claim 11 , wherein the substantially water-soluble excipient is selected from one or more of lactose, mannitol, sorbitol, sucrose and glucose.

14. A process for the preparation of a stable oral benzimidazole composition, the process comprising the steps of:

a. preparing a benzimidazole core formed by dispersing one or more amorphous benzimidazole compounds and one or more pharmaceutically acceptable additives in an aqueous or hydroalcoholic medium to obtain a dispersion and spraying the dispersion on to a pharmaceutically acceptable inert carrier at a bed temperature of less than about 50° C. for a total spraying time of less than about 24 hrs;

b. coating the core of step (a) with a separating layer; and

c. coating the product of step (b) with an enteric coating, wherein the composition contains less than about 5% by weight of crystalline benzimidazole after storage at 40° C. and 75% relative humidity for 3 months.

15. The process according to claim 14 , wherein the dispersion of step (a) is prepared in more than one lot.