Patent application EP17173535A (EP), filed 2017-05-30
Publication number: EP3251661A1
Title: RALOXIFENE SPRINKLE COMPOSITION
Abstract: The present invention relates to a capsule composition of raloxifene comprising multiparticulates comprising a) a core comprising raloxifene, and b) a taste-masking coating present in amount of from about 0.5% to about 50%w/w based on the core weight.
IPC codes: A61K  31/    38            A I
A61K   9/    48            A I
A61K   9/    50            A I
Claims: number: 1
text: A capsule comprising a plurality of particulates, wherein each particulate comprises:
number: 2
text: The capsule according to claim 1,wherein the capsule releases not more than about 90% of raloxifene in 10 minutes, when measured in a United States Pharmacopeia (USP) type 2 dissolution apparatus, paddle at 100RPM, at a temperature of 37°C ±0.5°C in 1000 mL of water, 0.5% polysorbate, and an enzyme.
number: 3
text: The capsule according to claim 1 wherein the raloxifene is present in an amount of from about 15% to about 80% based on the total weight of composition.
number: 4
text: The capsule according to claim 1, wherein the taste-masking coating comprises a taste-masking polymer selected from the group consisting ofwater-soluble polymers, water-swellable polymers, water-insoluble polymers, enteric polymers
number: 5
text: The capsule according to claim 4, wherein the taste-maskingcoating further comprises a sweetener.
number: 6
text: The capsule according to claim 1, wherein the total fill weight of the capsule is from about 75 mg to about 600 mg.
number: 7
text: The capsule according to claim 1, wherein the particulates further include a lubricant, which is present in an amount of from about 0.1% to about 15% by total weight of the composition.
number: 8
text: The capsule according to claim 1, wherein the particulates do not include an alkaline excipient.
number: 9
text: The capsule composition according to claim 8,wherein the alkaline excipients are selected from the group consisting of calcium phosphate, magnesium phosphate, aluminum phosphate, magnesium carbonate, croscarmellose, and mixtures thereof.
number: 10
text: A capsule comprising a plurality of particulates, wherein each particulate comprises:
number: 11
text: 12. The capsule of claim 10, wherein the polymer comprises a taste-masking polymer selected from the group consisting of water-soluble polymers, water-swellable polymers, water-insoluble polymers, enteric polymers and combinations thereof.
number: 12
text: 13. The capsule of claim 11, wherein the particulate is further coated with a lubricant.
number: 13
text: 14. The capsule of claim 13, wherein the capsule releases not more than about 90% of raloxifene in 10 minutes, when measured in a United States Pharmacopeia (USP) type 2 dissolution apparatus, paddle at 100rpm, at a temperature of 37°C ±0.5°C in 1000 mL of water, 0.5% polysorbate, and an enzyme.
Office action: search_report, dated 2017-12-06
Rejection reasons: inventive_step_epc_56
Prior art cited: ref_id: US6458811B1
ref_type: patent
severity: background
ref_id: EP0910369A1
ref_type: patent
severity: background
ref_id: US6458811B1
ref_type: patent
severity: background
ref_id: WO2004052345A1
ref_type: patent
severity: background
ref_id: WO2012156997A2
ref_type: patent
severity: background
ref_id: EP0910369
ref_type: patent
severity: obviousness
ref_id: US6458811
ref_type: patent
severity: obviousness
ref_id: WO2004052345
ref_type: patent
severity: obviousness
ref_id: WO2012156997
ref_type: patent
severity: obviousness
Final disposition: pending (2017-12-06)