Abiraterone Acetate Tablets

This article is compiled based on the United States Pharmacopeia (USP) – 2025 Edition

Issued and maintained by the United States Pharmacopeial Convention (USP)

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1 DEFINITION

Abiraterone Acetate Tablets contain NLT 90.0% and NMT 110.0% of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂).

2 IDENTIFICATION

A. The retention time of the major peak of the Sample solution corresponds to that of the Standard solution, as obtained in the Assay.

B. The UV spectrum of the major peak of the Sample solution corresponds to that of the Standard solution, as obtained in the Assay.

3 ASSAY

3.1 Procedure

Solution A: 10 mM of ammonium acetate in water

Mobile phase: See Table 1.

Table 1

[Note—Protect solutions from light.]

System suitability solution: 0.625 mg/mL of USP Abiraterone System Suitability Mixture RS in acetonitrile.

[Note—See Table 2 for relative retention times of the main components of the mixture.]

Table 2

Standard solution: 0.625 mg/mL of USP Abiraterone Acetate RS in acetonitrile

Sample solution: Nominally equivalent to 0.625 mg/mL of abiraterone acetate in acetonitrile, prepared from NLT 20 powdered Tablets as follows. Transfer the powder to a suitable volumetric ask. Add 50% of the ask volume of acetonitrile, shake by mechanical means for 30 min, and dilute with acetonitrile to volume. Pass a portion of the solution through a suitable fiter of 0.45-μm pore size, and use the clear solution for analysis.

Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 254 nm or diode array. [Note—Use a diode array detector to perform Identi cation B.]

Column: 3-mm × 15-cm; 3-μm packing L1

Column temperature: 15°

Flow rate: 0.45 mL/min

Injection volume: 10 μL

System suitability

Samples: System suitability solution and Standard solution

Suitability requirements

Resolution: NLT 1.0 between anhydro abiraterone and 3-deoxy 3-chloroabiraterone peaks, System suitability solution

Relative standard deviation: NMT 2.0%, Standard solution

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂) in the portion of Tablets taken:

Result = (r_u/r_s) × (C_s/C_u) × 100

r_u= peak response from the Sample solution

r_s= peak response from the Standard solution

C_s= concentration of USP Abiraterone Acetate RS in the Standard solution (mg/mL)

C_u= nominal concentration of abiraterone acetate in the Sample solution (mg/mL)

Acceptance criteria: 90.0%–110.0%

4 PERFORMANCE TESTS

Change to read:

Dissolution 〈711〉

Test 1

[Note—Protect solutions from light.]

Buffer: 56.5 mM of monobasic sodium phosphate in water. Adjust with 5 N sodium hydroxide or phosphoric acid to a pH of 4.5.

Medium: 0.25% of sodium lauryl sulfate in Buffer; 900 mL

Apparatus 2: 50 rpm

Time: 45 min

Standard solution: 0.3 mg/mL of USP Abiraterone Acetate RS in Medium prepared as follows. Transfer USP Abiraterone Acetate RS into a suitable volumetric ask. Add 4% of the ask volume of acetonitrile to dissolve, and dilute with Medium to volume.

Sample solution: Pass a portion of the solution under test through a suitable fiter of 10-μm pore size. Use the ltrate.

Mobile phase: Acetonitrile, formic acid, and water (55: 0.05: 45)

Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 252 nm

Column: 4.6-mm × 3-cm; 5-μm packing L1

Flow rate: 1 mL/min

Injection volume: 10 μL

System suitability

Sample: Standard solution

Suitability requirements

Tailing factor: NMT 2.0

Relative standard deviation: NMT 2.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of abiraterone acetate (₂₆H₃₃NO₂) dissolved:

(r_u/r_s) × (C_s/L) × V × 100

r_u= peak response from the Sample solution

r_s= peak response from the Standard solution

C_s= concentration of the Standard solution (mg/mL)

L = label claim (mg/Tablet)

V = volume of Medium, 900 mL

Tolerances: NLT 85% (Q) of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂) is dissolved.

Test 2: If the product complies with this test, the labeling indicates that it meets USP Dissolution Test 2. [Note—Protect solutions from light.]

Buffer: 56.5 mM of monobasic sodium phosphate in water. Adjust with 5 N sodium hydroxide or phosphoric acid to a pH of 4.5.

Medium: 0.25% of sodium lauryl sulfate in Buffer; 900 mL

Apparatus 2: 75 rpm

Time: 30 min

Standard solution: 0.28 mg/mL of USP Abiraterone Acetate RS in Medium prepared as follows. Transfer USP Abiraterone Acetate RS into a suitable volumetric ask. Add 4% of the ask volume of acetonitrile to dissolve, and dilute with Medium to volume.

Sample solution: Pass a portion of the solution under test through a suitable fiter of 10-μm pore size. Use the ltrate.

Mobile phase: Acetonitrile and water (90:10)

Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 254 nm

Column: 2.1-mm × 7.5-cm; 1.7-μm packing L43

Column temperature: 35°

Flow rate: 0.5 mL/min

Injection volume: 0.5 μL

Run time: NLT 1.7 times the retention time of abiraterone acetate

System suitability

Sample: Standard solution

Suitability requirements

Tailing factor: NMT 2.0

Relative standard deviation: NMT 2.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂) dissolved:

Result = (r_u/r_s) × C_s × V × (1/L) × 100

r_u = peak response of abiraterone acetate from the Sample solution

r_s = peak response of USP Abiraterone Acetate RS from the Standard solution

C_s = concentration of the Standard solution (mg/mL)

V = volume of Medium, 900 mL

L = label claim (mg/Tablet)

Tolerances: NLT 80% (Q) of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂) is dissolved.

Test 3: If the product complies with this test, the labeling indicates that it meets USP Dissolution Test 3.

[Note—Protect solutions from light.]

Buffer: 56.5 mM of sodium phosphate monobasic in water

Medium: 0.25% of sodium lauryl sulfate in Buffer, adjusted with 5 N sodium hydroxide or phosphoric acid to a pH of 4.5; 900 mL

Apparatus 2: 50 rpm

Time: 45 min

Standard solution: 0.3 mg/mL of USP Abiraterone Acetate RS in Medium prepared as follows. Transfer USP Abiraterone Acetate RS into a suitable volumetric ask. Add 4% of the ask volume of acetonitrile to dissolve, and dilute with Medium to volume.

Sample solution: Pass a portion of the solution under test through a suitable fiter.

Mobile phase: Acetonitrile, formic acid, and water (55: 0.05: 45)

Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 252 nm

Column: 4.6-mm × 3-cm; 5-μm packing L1

Column temperature: 30°

Flow rate: 1.0 mL/min

Injection volume: 10 μL

System suitability

Sample: Standard solution

Suitability requirements

Tailing factor: NMT 2.0

Relative standard deviation: NMT 2.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of abiraterone acetate (C₂₆H₃₃NO₂) dissolved:

Result = (r_u/r_s) × (C_s/L) × V × 100

r_u = peak response of abiraterone acetate from the Sample solution

r_s = peak response of abiraterone acetate from the Standard solution

C_s = concentration of USP Abiraterone Acetate RS in the Standard solution (mg/mL)

L = label claim of abiraterone acetate (mg/Tablet)

V = volume of Medium, 900 mL

Tolerances: NLT 80% (Q) of the labeled amount of abiraterone acetate (C H NO ) is dissolved.

Uniformity of Dosage Units 〈905〉: Meet the requirements

5 IMPURITIES

Organic Impurities

[Note—Protect solutions from light.]

Solution A, Mobile phase, System suitability solution, Standard solution, Sample solution, and Chromatographic system: Proceed as directed in the Assay.

Sensitivity solution: 0.3 μg/mL of USP Abiraterone Acetate RS in acetonitrile from Standard solution

System suitability

Samples: System suitability solution, Standard solution, and Sensitivity solution

Suitability requirements

Resolution: NLT 1.0 between anhydro abiraterone and 3-deoxy 3-chloroabiraterone peaks, System suitability solution

Signal-to-noise ratio: NLT 10, Sensitivity solution

Relative standard deviation: NMT 2.0%, Standard solution

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of each impurity in the portion of Tablets taken:

Result = (r_u/r_s) × (C_s/C_u) × (1/F) × 100

r_u = peak area of each impurity from the Sample solution

r_s = peak area of abiraterone acetate from the Standard solution

C_s = concentration of USP Abiraterone Acetate RS in the Standard solution (mg/mL)

C_u = nominal concentration of abiraterone acetate in the Sample solution (mg/mL)

F = relative response factor for each individual impurity (see Table 3)

Acceptance criteria: See Table 3. Disregard any peak less than 0.05%.

Table 3

^a This is a process impurity and is controlled in the drug substance monograph. It is included in the table for identification only, and it is not to be reported in the total impurities.

6 ADDITIONAL REQUIREMENTS

Packaging and Storage: Preserve in tight containers, and store at controlled room temperature.

Labeling: When more than one Dissolution test is given, the labeling states the Dissolution test used only if Test 1 is not used.

USP Reference Standards 〈11〉

USP Abiraterone Acetate RS

USP Abiraterone System Suitability Mixture RS

It contains Abiraterone Acetate and small amounts of the following:

Abiraterone

17-(Pyridin-3-yl)androsta-5,16-dien-3β-ol.

C₂₄H₃₁NO                            349.52

Abiraterone ethyl ether

3β-Ethoxy-17-(pyridin-3-yl)androsta-5,16-diene.

C₂₆H₃₅NO                            377.57

Abiraterone isopropyl ether

3β-Isopropoxy-17-(pyridin-3-yl)androsta-5,16-diene.

C₂₇H₃₇NO                            391.60

Anhydro abiraterone

17-(Pyridin-3-yl)androsta-3,5,16-triene.

C₂₄H₂₉N                              331.50

O-Chlorobutylabiraterone

3β-(4-Chlorobutoxy)-17-(pyridin-3-yl)androsta-5,16-diene.

C₂₈H₃₈ClNO                        440.07

3-Deoxy-3-acetyl abiraterone-3-ene

1-[17-(Pyridin-3-yl)androsta-3,5,16-trien-3-yl]ethanone.

C₂₆H₃₁NO                           373.53

3-Deoxy 3-chloroabiraterone

3β-Chloro-17-(pyridin-3-yl)androsta-5,16-diene.

C₂₄H₃₀ClN                            367.96

α-Epoxyabiraterone acetate

17-(Pyridin-3-yl)-16α,17α-epoxyandrost-5-en-3β-yl acetate.

C₂₆H₃₃NO₃                          407.55

β-Epoxyabiraterone acetate

17-(Pyridin-3-yl)-16β,17β-epoxyandrost-5-en-3β-yl acetate.

C₂₆H₃₃NO3                               407.55

7-Ketoabiraterone acetate

7-Oxo-17-(pyridin-3-yl)androsta-5,16-dien-3β-yl acetate.

C₂₆H₃₁NO₃