Solubilization preparation
AssigneeDainippon Sumitomo Pharma Co., Ltd.
InventorsKazuya Otoda, Mayumi Nakamura, Teruko Ariyama, Takashi Nakagawa
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Abstract
A solution-type preparation of lurasidone comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboxyimide hydrochloride (lurasidone) as an active ingredient and containing at least one substance selected from benzyl alcohol, N,N-dimethylacetamide, lactic acid and propylene glycol.
Claims9
A stable aqueous solution-type preparation comprising as an active ingredient N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide, which is a free form of lurasidone, or a pharmaceutically acceptable acid addition salt thereof, wherein the active ingredient is solubilized by the following additives (i)
- (i) 50 to 75% (W/W) of propylene glycol, 6 to 24% (W/W) of water and 5 to 33% (W/W) of anhydrous ethanol, and the active ingredient is present in a concentration of 1 to 20 mg/mL.
A stable aqueous solution-type preparation that is one selected from the group consisting of preparations i) to viii) set forth below:
- Lurasidone
- Anhydrous
- Propylene
- Water for
- Preparation
- (mg/mL)
- ethanol (%)
- glycol (%)
- injection (%)
- i)
- 10
- 5
- 75
- 19
- ii)
- 10
- 10
- 75
- 14
- iii)
- 10
- 15
- 60
- 24
- iv)
- 10
- 15
- 75
- 9
- v)
- 10
- 25
- 50
- 24
- vi)
- 10
- 25
- 60
- 14
- vii)
- 10
- 33
- 50
- 16
- viii)
- 10
- 33
- 60
- 6.
Dependencies are inferred from the claim text.