JP2017528457A5 - - Google Patents

Claims (24)

A unit dosage form of abiraterone acetate, wherein the unit dosage form of 500 mg is a dose of 1,000 mg of Zytiga® for one or both of Cmax and AUC0-t in a fasted healthy male subject. ) A unit dosage form characterized by being biologically equivalent to a tablet (250 mg: US Pharmaceutical Code No. 57894-150; USFDA NDA202379) . Administered to fasting healthy male subjects compared to a dose of 1,000 mg of Zytiga® tablets (250 mg: US Drug Code No. 57894-150; USFDA NDA 202379) administered to fasting healthy male subjects The logarithmic ratio of the geometric mean of AUC _(0-∞) for a dose of 500 mg is 0.6-1.4, 0.7-1.3, 0.8-1.2, and 0.9-1 A unit dosage form of abiraterone acetate according to claim 1 selected from .1. Administered to fasting healthy male subjects compared to a dose of 1,000 mg of Zytiga® tablets (250 mg: US Drug Code No. 57894-150; USFDA NDA 202379) administered to fasting healthy male subjects that the logarithmic ratio of the geometric mean of Cm a x for dose 500mg is 0.6～1.4,0.7～1.3,0.8～1.2, and from 0.9 to 1.1 A unit dosage form of abiraterone acetate according to claim 1 selected.   [D90] of the abiraterone acetate is greater than 300 nm and 7,500 nm, 7,000 nm, 6,000 nm, 5,000 nm, 4,500 nm, 4,000 nm, 3,000 nm, 2,000 nm, 900 nm, 800 nm, and 700 nm A unit dosage form of abiraterone acetate according to claim 1, wherein the unit dosage form is less than one of   [D50] of the abiraterone acetate is more than 100 nm and is selected from 3,500 nm, 3,000 nm, 2,500 nm, 1,600 nm, 1,400 nm, 1,200 nm, 1,000 nm, 800 nm, 500 nm, 400 nm, and 300 nm The unit dosage form of abiraterone acetate according to claim 1, wherein the unit dosage form is less than 1.   [D4,3] of the abiraterone acetate is more than 300 nm and 7,000 nm, 6,000 nm, 5,000 nm, 4,000 nm, 3,000 nm, 2,500 nm, 2,400 nm, 2,200 nm, 2,000 nm, The unit dosage form of abiraterone acetate according to claim 1, wherein the unit dosage form is less than one of 1,900 nm, 1,700 nm, 1,500 nm, 1,300 nm, 1,100 nm, 900 nm, and 800 nm.   Sample containing 100 mg of abiraterone acetate using USP apparatus II at 75 rpm in 900 mL of pH 4.5 phosphate buffer containing 0.1% sodium lauryl sulfate in elution rate of the abiraterone acetate in the unit dosage form The unit dosage form of abiraterone acetate according to claim 1, wherein the unit dosage form of abiraterone acetate is at a rate such that at least 70% of the abiraterone acetate elutes in 5 to 15 minutes or 5 to 10 minutes.   Sample containing 125 mg of abiraterone acetate using USP apparatus II at 75 rpm in 900 mL of pH 4.5 phosphate buffer containing 0.12% sodium lauryl sulfate in elution rate of the abiraterone acetate in the unit dosage form The unit dosage form of abiraterone acetate according to claim 1, wherein the unit dosage form of abiraterone acetate is at a rate such that at least 70% of the abiraterone acetate elutes in 5 to 15 minutes or 5 to 10 minutes.   A unit dosage form of abiraterone acetate according to claim 1 containing 125 mg of abiraterone acetate.   The unit dosage form of abiraterone acetate according to claim 1, wherein the average plasma Cmax is 50 ng / mL to 120 ng / mL when orally administered to a population of healthy male subjects in a fasted state at a dose of 500 mg.   11. A unit dosage form according to claim 10, wherein the median plasma tmax is 1 hour to 2.5 hours when administered at a dose of 500 mg orally to a population of healthy male subjects in a fasted state.   The unit of abiraterone acetate according to claim 1, wherein when the dose of 500 mg is orally administered to a population of healthy male subjects in a fasted state, the average plasma AUC (0-∞) is 240 h * ng / mL to 650 h * ng / mL. Dosage form.   A unit dosage form according to claim 1 containing 125 mg of abiraterone acetate.   The unit dosage form of abiraterone acetate according to claim 1, wherein when a dose of 500 mg is administered to a fasting healthy male subject, the 90% confidence interval of mean plasma Cmax is a value of 50 ng / mL to 120 ng / mL.   The 90% confidence interval of mean plasma AUC (0-∞) is a value of 240 h * ng / mL to 650 h * ng / mL when administered at a dose of 500 mg to a fasting healthy male subject. Abiraterone acetate unit dosage form.   15. A unit dosage form according to claim 14 containing 125 mg of abiraterone acetate.   The unit dosage form of claim 1, further comprising an antioxidant.   A unit dosage form of abiraterone acetate containing 125 mg of abiraterone acetate, wherein the median particle size of the abiraterone acetate is 2,000 nm to 100 nm on a particle volume basis.   Sample containing 125 mg of abiraterone acetate using USP apparatus II at 75 rpm in 900 mL of pH 4.5 phosphate buffer containing 0.12% sodium lauryl sulfate in elution rate of the abiraterone acetate in the unit dosage form 19. The unit dosage form of claim 18, wherein the unit dosage form is at a rate such that at least 70% of the abiraterone acetate elutes in 5 to 15 minutes or 5 to 10 minutes when tested. When the unit dosage form is a tablet and the tablet is tested in 900 mL of pH 4.5 phosphate buffer (0.1% SLS) using a 75 rpm USP apparatus II, at least one of the abiraterone acetate 19. A unit dosage form according to claim 18 having an elution rate such that 80% elutes in 5-15 minutes or 5-10 minutes. 19. The 90% confidence interval for mean plasma AUC (0-∞) when administered at a dose of 500 mg to a fasted healthy male subject is a value between 240 h * ng / mL and 650 h * ng / mL. Unit dosage form. 19. The unit dosage form of claim 18, wherein when a dose of 500 mg is administered to a fasted healthy male subject, the 90% confidence interval for mean plasma Cmax is a value between 50 ng / mL and 120 ng / mL. A daily dose of 500 mg of abiraterone acetate dosage form that is biologically equivalent to a dose of 1,000 mg of Zytiga® tablets (250 mg: US Drug Code No. 57894-150; USFDA NDA202379) in healthy fasted male subjects And use of glucocorticoids in the manufacture of a medicament for treating castration resistant prostate cancer. 24. The use according to claim 23, wherein the glucocorticoid is selected from the group consisting of prednisone, prednisolone, and methylprednisolone.