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US 9,427,402 B2Granted
Preparation for improving solubility of poorly soluble drug
AssigneeShionogi & Co., Ltd.
InventorsSatoshi Sakuma, Hiroshi Ueda, Akira Mashimo, Hiroshi Murazato
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Abstract
The present invention relates to solubility improving preparation for enhancing the oral absorption of a poorly soluble drug, which is comprising (A) and (B); (A) a granulated substance which comprises (i) a poorly soluble drug having an acidic group in the molecule, (ii) an alkaline agent, (iii) a surfactant, and this granulated substance dose not substantially contain a disintegrator, (B) a disintegrator existing only in the external of the granulated substance.
Claims20
A solid preparation comprising:
- (A) a granulated substance comprising
- (i) a poorly soluble drug having a carboxyl group in the molecule,
- wherein the poorly soluble drug is an optically active compound represented by Formula (I):
- wherein,
- R1 is chosen from halogen atoms and C1-C3 alkyloxy groups;
- R2 is chosen from C1-C8 alkyl groups;
- R3 is chosen from C1-C8 alkyl groups;
- R4 and R5 are each independently chosen from a fluorine atom and a chlorine atom;
- R6 is chosen from C1-C3 alkyl groups and C1-C3 alkyl oxy groups;
- and
- the carbon atom with “*” attached to it is an asymmetric carbon, its pharmaceutically acceptable salt, or solvate thereof
- (ii) an alkaline agent,
- wherein the alkaline agent is chosen from magnesium oxide, magnesium hydroxide, hydroxylation alumina magnesium, synthetic hydrotalcite, calcium silicate and mixtures thereof,
- wherein the alkaline agent is present in an amount of 0.5 to 30 weight % based on the weight of the granulated substance,
- (iii) a surfactant,
- wherein the surfactant is chosen from sodium lauryl sulfate, sucrose fatty acid ester and polyoxyethylene polyoxypropylene glycol,
- wherein the surfactant is present in an amount of 0.2 to 50 weight % based on the weight of the granulated substance,
- wherein the granulated substance does not substantially contain a disintegrator, and
- (B) a disintegrator external to the granulated substance.
16 more elements
Dependencies are inferred from the claim text.