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Claims for Patent: 5,026,560

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Claims for Patent: 5,026,560

Title: Spherical granules having core and their production
Abstract:The spherical granules having a core coated with spraying powder containing a drug and low substituted hydroxypropylcellulose, because of their excellent hardness, can be coated further evenly, (e.g. sustained release coating, gastric coating, enteric coating), and at the time the granules are excellent in disintegration.
Inventor(s): Makino; Tadashi (Osaka, JP), Tabata; Tetsuro (Osaka, JP), Hirai; Shin-ichiro (Kyoto, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:07/143,957
Patent Claims: 1. Spherical granules having a core coated with a binder and spraying powder containing a drug and low substituted hydroxypropylcellulose having a mean particle diameter not more than 200 .mu.m, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.

2. The spehrical granules having a core according to claim 1, wherein the drug is a drug for the digestive system.

3. The spherical granules having a core according to claim 2, wherein the drug for the digestive system is a benzimidazole compound having antiulcer activity, cimetidine, ranitidine, pancreatin or 5-aminosalicylic acid.

4. The spherical granules having a core according to claim 3, wherein the benzimdazole compound is represented by the formula ##STR2## wherein R.sup.1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifuluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl,

R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfon

R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy,

R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4.

5. The spherical granules having a core according to claim 3, wherein the benzimidazole compound is 2-[[3- methyl-4-(2,2,2-trifluoroethoxy)-2pyridyl]methylsulfinyl]benzimidazole or 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)-methylsulfinyl]benzimidazo le.

6. The spherical granules having a core according to claim 1, wherein the content is 5.0 to 16.0%.

7. The spherical granules having a core according to claim 1, wherein the content is 10.0 to 13.0%.

8. The spherical granules having a core according to claim 1, wherein the mean particle diameter is not more then 100 .mu.m.

9. The spherical granules having a core according to claim 1, wherein the mean particle diameter is not more than 30 .mu.m.

10. The spherical granules having a core according to claim 1, wherein the granules pass through 12 mesh sieve but do not pass through 32 mesh sieve.

11. The spherical granules having a core according to claim 1, wherein the granules are enteric-coated.

12. A method for producing spherical granules having acore characterized in that seed cores are coated, while being sprayed with an aqueous binder, with spraying powder containing a drug and low substituted hydroxypropylcellulose having a means particle diameter not more than 200 .mu.m, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.

13. The method according to claim 12, wherein the seed cores are nonpareils produced by coating 75 weight parts of sucrose with 25 weight parts of corn starch

14. The method according to claim 12, wherein the seed cores are made with crystalline cellulose.

15. The method according to claim 12, wherein the aqueous binder is water or ethanol.

16. The method according to claim 12, wherein the aqueous binder is solution of binder in water or in ethanol.

17. The method according to claim 16, wherein the solution has 0.1 to 80.% (w/v) of concentration.

18. The method according to claim 16, wherein the binder is one or more selected from the group consisting of sucrose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, polyvinylpyrrolidone, pullulan and gum arabic.

19. The method according to claim 12, wherein the spraying powder is not more than 100 .mu.m in particle size.

20. The method according to claim 12, wherein the spraying powder contains 5 to 90% (w/w) of low substituted hydroxypropylcellulose.

21. The method according to claim 12, wherein the spraying powder contains 2 to 70% (w/w) of the drug.

22. The method according to claim 12, wherein the ratio of the aqueous binder to the spraying powder is 1:1 to 1:2.

23. The spherical granules having a core according to claim 1, wherein the spraying powder contains magnesium carbonate and/or calcium carbonate.

24. The spherical granules having a core according to claim 1, wherein the coated spherical granules are further coated with spraying powder containing low substituted hydroxypropylcellulose.

25. The spherical granules having a core according to claim 24, wherein the spherical granules are further coated with an enteric coating agent.

26. The spherical granules having a core 3 according to claim 25, wherein the enteric coating agent is acrylate copolymers anionic in charcter or hydroxypropylmethylcellulose phthalate.

27. The method according to claim 12, wherein the spraying powder contains magnesium carbonate and/or calcium carbonate.

28. The methdo according to claim 12, wherein the spherical granules are further coated with spraying powder containing low substituted hydroxypropylcellulose.

29. The method according to claim 28, wherein the spherical granules are further coated with an enteric coating agent.

30. The methdo according to claim 29, wherein the enteric coating agent is acrylate copolymers anionic in character or hydroxyporpylmethylcellulose phthalate.
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