Claims for Patent: 6,562,375

Summary for Patent: 6,562,375

Title:	Stable pharmaceutical composition for oral use
Abstract:	The present invention is to provide a stable pharmaceutical composition for oral use and preparation thereof in which changes are prevented in drug release at stored even under the exposure to light by adding yellow ferric oxide and/or red ferric oxide in a matrix type sustained-release preparation containing a drug, hydrophilic base, and polyethylene oxide. The present invention is to further provide a method for preventing changes in drug release at stored under the exposure to light in a matrix type sustained-release preparation containing a drug, hydrophilic base, and polyethylene oxide. The quality assurance period of the product can be prolonged and the product value can be improved by the present invention.
Inventor(s):	Sako; Kazuhiro (Shizuoka, JP), Sawada; Toyohiro (Shizuoka, JP), Yoshihara; Keiichi (Shizuoka, JP), Yoshioka; Tatsunobu (Shizuoka, JP), Watanabe; Shunsuke (Shizuoka, JP)
Assignee:	Yamanouchi Pharmaceuticals, Co., Ltd. (Tokyo, JP)
Application Number:	09/629,405
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,562,375
Patent Claims:	1. A stable hydrogel-forming pharmaceutical composition for oral use comprising: a yellow ferric oxide and/or a red ferric oxide in an amount effective to stabilize a matrix sustained-release preparation containing (a) a drug, (b) 5 to 80 wt % of hydrophilic base having a solubility that the amount of water needed to dissolve 1 g of said hydrophilic base is 5 ml or less at 20.+-.5.degree. C., and (c) 10 to 95 wt % of polyethylene oxide (i) having a viscosity of 2,000 cP or higher as an aqueous 2% solution at 25.degree. C. or (ii) having a viscosity-average molecular weight of 2,000,000 or higher, wherein said matrix preparation contains polyethylene oxide as a base of a sustained-release preparation, wherein said drug and said hydrophilic base are dispersed in a polyethylene oxide, and wherein said amount of yellow ferric oxide is 1 to 20 wt % or red ferric oxide is 3 to 20 wt %, with physical mixing in the matrix per preparation weight, or said amount of yellow ferric oxide and/or red ferric oxide is 0.3 to 2 wt %, in film coating per tablet weight. 2. The stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 1, wherein said amount of yellow ferric oxide is 3 to 10, or red ferric oxide is 5 to 20 wt %, with physical mixing in the matrix per preparation weight. 3. The stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 2, wherein said amount of red ferric oxide is 10 to 15 wt % per preparation weight. 4. The stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 1, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.3 to 2 wt %, in film coating per tablet weight. 5. The stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 4, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.5 to 1.5 wt %, in film coating per tablet weight. 6. The stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 4 or 5, wherein the concentration in film material of a yellow ferric oxide and/or a red ferric oxide is 5 to 50%. 7. A method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability comprising adding a yellow ferric oxide and/or a red ferric oxide in an amount effective to stabilize a matrix sustained-release preparation to a drug, 5 to 80 wt % of hydrophilic base having a solubility that the amount of water needed to dissolve 1 g of said hydrophilic base is 5 ml or less at 20.+-.5.degree. C., and 10 to 95 wt % of polyethylene oxide having a viscosity of 2,000 cP or higher as an aqueous 2% solution at 25.degree. C. or having a viscosity-average molecular weight of 2,000,000 or higher, wherein said matrix preparation contains polyethylene oxide as a base of a sustained-release preparation, wherein said drug and said hydrophilic base are dispersed in a polyethylene oxide, wherein said yellow ferric oxide with amount of 1 to 20 wt % or red ferric oxide with amount of 3 to 20 wt % is added to the preparation using granulation or mixing in the matrix per preparation weight, or said yellow ferric oxide and/or red ferric oxide with amount of amount of 0.3 to 2 wt % is added to the preparation in film coating per tablet weight. 8. The method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 7, wherein said amount of yellow ferric oxide is 3 to 10 wt %, or red ferric oxide is 5 to 20 wt %, with physical mixing in the matrix per preparation weight. 9. The method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 8, wherein said amount of red ferric oxide is 10 to 15 wt % per preparation weight. 10. The method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 7, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.3 to 2 wt %, in film coating per preparation weight. 11. The method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 10, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.5 to 1.5 wt %, in film coating per preparation weight. 12. The method of producing a stable hydrogel-forming pharmaceutical composition for oral use with improved stability according to claim 10 or 11, wherein the concentration in film material of a yellow ferric oxide and/or a red ferric oxide is 5 to 50%. 13. A method of preventing chances in drug release by adding yellow ferric oxide and/or red ferric oxide in an amount effective to stabilize a matrix sustained-release preparation containing a drug, a hydrophilic base, and a polyethylene oxide, wherein said matrix preparation contains said polyethylene oxide as a base of a sustained-release preparation, wherein said drug and said hydrophilic base are dispersed in said polyethylene oxide. 14. A method for increasing physical stability in an oral composition, said method comprising: admixing a yellow ferric oxide and/or a red ferric oxide in an amount effective to stabilize a matrix sustained-release preparation containing a drug, a hydrophilic base, and a polyethylene oxide, wherein said matrix preparation contains said polyethylene oxide as a base of a sustained-release preparation. 15. The method for increasing physical stability in an oral composition according to claim 14, wherein yellow ferric oxide and/or red ferric oxide is added to the preparation using at least one of film coating, granulation and mixing. 16. The method for increasing physical stability in an oral composition according to claim 14 or 15, wherein said amount of yellow ferric oxide is 1 to 20 wt % or red ferric oxide is 3 to 20 wt %, with physical mixing in the matrix per preparation weight, or said amount of yellow ferric oxide and/or red ferric oxide is 0.3 to 2 wt %, in film coating per tablet weight. 17. The method for increasing physical stability in an oral composition according to claim 16, wherein said amount of yellow ferric oxide is 3 to 10 wt %, or red ferric oxide is 5 to 20 wt %, with physical mixing in the matrix per preparation weight. 18. The method for increasing physical stability in an oral composition according to claim 17, wherein said amount of red ferric oxide is 10 to 15 wt % per preparation weight. 19. The method for increasing physical stability in an oral composition according to claim 13 or 14, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.3 to 2 wt %, in film coating per preparation weight. 20. The method for increasing physical stability in an oral composition according to claim 19, wherein said amount of yellow ferric oxide and/or red ferric oxide is 0.5 to 1.5 wt % per preparation weight. 21. The method for increasing physical stability in an oral composition according to claim 19, wherein the concentration in film material of a yellow ferric oxide and/or a red ferric oxide is 5 to 50%.