Tranexamic Acid 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

Tranexamic acid Tablets contain NLT 90.0% and NMT 110.0% of the labeled amount of tranexamic acid (C₈H₁₅NO₂).

2 IDENTIFICATION

2.1 A. Spectroscopic Identification Tests 〈197〉, Infrared Spectroscopy: 197K

Sample: Finely powder 1 Tablet. Transfer a portion of the powdered Tablet, equivalent to 75 mg of tranexamic acid, to a suitable vial. Add 1 mL of water, mix on a vortex mixer for a few seconds, and sonicate for 1 min. Pass the suspension through a suitable filter onto a suitable watchglass. Evaporate the filtrate in an oven at 60° for 2 h, and then stir gently with a glass rod. Dry in an oven at 60° for another 1 h.

Acceptance criteria: The IR spectrum of the Sample corresponds to that of USP Tranexamic Acid RS.

2.2 B. The retention time 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: Dissolve 10.5 g of monobasic sodium phosphate monohydrate in 1000 mL of water, and add 8 mL of triethylamine followed by 2.3 g of sodium dodecyl sulfate. Adjust with 85% phosphoric acid to a pH of 2.5.

Mobile phase: Acetonitrile and Solution A (15:85)

Standard solution: 2.6 mg/mL of USP Tranexamic Acid RS in water. Sonicate, if needed.

Sample solution: Nominally 2.6 mg/mL of tranexamic acid prepared as follows. Transfer a portion of finely powdered Tablets (NLT 20), equivalent to 650 mg of tranexamic acid, to a 250-mL volumetric flask. Add about 200 mL of water, sonicate for about 20 min with occasional shaking, and dilute with water to volume. Pass a portion of the solution through a suitable filter of 0.45-µm pore size.

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 210 nm
• Column: 4.6-mm × 10-cm; 3.5-µm packing L1
• Column temperature: 40°
• Flow rate: 1 mL/min
• Injection volume: 20 µL
• Run time: NLT 2 times the retention time of tranexamic acid

System suitability

• Sample: Standard solution
• Suitability requirements
• Tailing factor: NMT 2.0
• Relative standard deviation: NMT 1.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of tranexamic acid (C₈H₁₅NO₂) in the portion of Tablets taken:

Result = (rᵤ/rₛ) × (Cₛ/Cᵤ) × 100

rᵤ = peak response of tranexamic acid from the Sample solution

rₛ = peak response of tranexamic acid from the Standard solution

Cₛ = concentration of USP Tranexamic Acid RS in the Standard solution (mg/mL)

Cᵤ = nominal concentration of tranexamic acid in the Sample solution (mg/mL)

Acceptance criteria: 90.0%–110.0%

4 PERFORMANCE TESTS

4.1 Dissolution 〈711〉

4.1.1 Test 1

Medium: Water; 900 mL

Apparatus 2: 50 rpm

Time: 60 min

Solution A and Chromatographic system: Proceed as directed in the Assay.

Mobile phase: Acetonitrile and Solution A (20:80)

Standard solution: 0.72 mg/mL of USP Tranexamic Acid RS in water. Sonicate, if needed. Pass the solution through a suitable filter of 0.45-µm pore size.

Sample solution: Pass a portion of the solution under test through a suitable filter of 0.45-µm pore size.

System suitability

• Sample: Standard solution
• Suitability requirements
• Tailing factor: NMT 2.0
• Relative standard deviation: NMT 1.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of tranexamic acid (C₈H₁₅NO₂) dissolved:

Result = (rᵤ/rₛ) × Cₛ × V × (1/L) × 100

rᵤ = peak response of tranexamic acid from the Sample solution

rₛ = peak response of tranexamic acid from the Standard solution

Cₛ = concentration of USP Tranexamic Acid RS in the Standard solution (mg/mL)

V = volume of the Medium, 900 mL

L = label claim of tranexamic acid (mg/Tablet)

Tolerances: NLT 80% (Q) of the labeled amount of tranexamic acid (C₈H₁₅NO₂) is dissolved.

4.1.2 Test 2: If the product complies with this test, the labeling indicates that it meets USP Dissolution Test 2.

Medium: Simulated gastric fluid TS (without enzyme); 900 mL, deaerated

Apparatus 2: 50 rpm

Time: 90 min

Buffer: Dissolve 45 g of monobasic potassium phosphate in 4.5 L of water. Adjust with phosphoric acid to a pH of 2.2.

Mobile phase: Acetonitrile and Buffer (10:90)

Standard solution: 0.72 mg/mL of USP Tranexamic Acid RS in Medium

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

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 210 nm
• Column: 4.6-mm × 5-cm; 5-µm packing L9
• Column temperature: 25°
• Flow rate: 1.2 mL/min
• Injection volume: 15 µL
• Run time: NLT 1.6 times the retention time of tranexamic acid

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 tranexamic acid (C₈H₁₅NO₂) dissolved:

Result = (rᵤ / rₛ) × C × V × (1/L) × 100

rᵤ = peak response of tranexamic acid from the Sample solution

rₛ = peak response of tranexamic acid from the Standard solution

C = concentration of USP Tranexamic Acid RS in the Standard solution (mg/mL)

V = volume of the Medium, 900 mL

L = label claim of tranexamic acid (mg/Tablet)

Tolerances: NLT 80% (Q) of the labeled amount of tranexamic acid (C₈H₁₅NO₂) is dissolved.

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

Medium: Water; 900 mL

Apparatus 2: 50 rpm

Time: 90 min

Buffer: Dissolve 11 g of sodium phosphate monobasic anhydrous in 500 mL of water. Add 5.0 mL of triethylamine, followed by 1.4 g of sodium dodecyl sulfate. Adjust with 10% phosphoric acid TS to a pH of 2.5. Dilute with water to 600 mL.

Mobile phase: Methanol and Buffer (40:60)

Standard solution: 0.7 mg/mL of USP Tranexamic Acid RS in Medium

Sample solution: Pass a portion of the solution under test through a suitable filter of 0.45-μm pore size, discarding the first 5 mL of the filtrate.

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 220 nm
• Column: 4.6-mm × 15-cm; 5-μm packing L1
• Column temperature: 35°
• Flow rate: 1 mL/min
• Injection volume: 20 μL
• Run time: NLT 2 times the retention time of tranexamic acid

System suitability

• Sample: Standard solution
• Suitability requirements
• Tailing factor: NMT 1.5
• Relative standard deviation: NMT 2.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of tranexamic acid (C₈H₁₅NO₂) dissolved:

Result = (rᵤ/rₛ) × Cₛ × V × (1/L) × 100

rᵤ = peak response of tranexamic acid from the Sample solution

rₛ = peak response of tranexamic acid from the Standard solution

Cₛ = concentration of USP Tranexamic Acid RS in the Standard solution (mg/mL)

V = volume of the Medium, 900 mL

L = label claim of tranexamic acid (mg/Tablet)

Tolerances: NLT 80% (Q) of the labeled amount of tranexamic acid (C₈H₁₅NO₂) is dissolved.

4.2 Uniformity of Dosage Units 〈905〉

Meet the requirements

5 IMPURITIES

5.1 Organic Impurities

Solution A and Mobile phase: Prepare as directed in the Assay.

System suitability solution: 20 µg/mL of USP Tranexamic Acid RS and 2 µg/mL of USP Tranexamic Acid Related Compound C RS in Mobile phase

Standard solution: 0.01 mg/mL of USP Tranexamic Acid RS in Mobile phase

Sample solution: Nominally 10 mg/mL of tranexamic acid in Mobile phase prepared as follows. Transfer a portion of finely powdered Tablets (NLT 20), equivalent to 500 mg of tranexamic acid, to a 50-mL volumetric flask. Add about 40 mL of Mobile phase, sonicate for about 20 min with occasional shaking, and dilute with Mobile phase to volume. Pass a portion of the solution through a suitable filter of 0.45-µm pore size.

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 220 nm
• Column: 4.6-mm × 10-cm; 3.5-µm packing L1
• Column temperature: 30°
• Flow rate: 1 mL/min
• Injection volume: 20 µL
• Run time: NLT 5.3 times the retention time of tranexamic acid

System suitability

• Samples: System suitability solution and Standard solution
• Suitability requirements
• Resolution: NLT 2.0 between tranexamic acid and tranexamic acid related compound C, System suitability solution
• Relative standard deviation: NMT 5.0%, Standard solution

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of each specified and any unspecified degradation product in the portion of Tablets taken:

Result = (rᵤ/rₛ) × (Cₛ/Cᵤ) × 100

rᵤ = peak response of each specified or any unspecified degradation product from the Sample solution

rₛ = peak response of tranexamic acid from the Standard solution

Cₛ = concentration of USP Tranexamic Acid RS in the Standard solution (mg/mL)

Cᵤ = nominal concentration of tranexamic acid in the Sample solution (mg/mL)

Acceptance criteria: See Table 1.

Table 1

ᵃ Process impurity controlled in the drug substance. It is included for identification purposes only. It should not be reported for the drug product, and should not be included in the total degradation products.

ᵇ 4-(Aminomethyl)benzoic acid.

ᶜ cis-4-(Aminomethyl)cyclohexanecarboxylic acid.

ᵈ trans,trans-4,4′-[Iminobis(methylene)]dicyclohexanecarboxylic acid.

6 ADDITIONAL REQUIREMENTS

Packaging and Storage: Store in well-closed containers, at controlled room temperature.

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

Change to read:

USP Reference Standards 〈11〉

USP Tranexamic Acid RS

USP Tranexamic Acid Related Compound C RS

(RS)-4-(Aminomethyl)cyclohex-1-enecarboxylic acid hydrochloride.

C₈H₁₃NO₂ · HCl 191.66