Tranexamic Acid

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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C₈H₁₅NO₂            157.21

trans-4-(Aminomethyl) cyclohexanecarboxylic acid;

Cyclohexanecarboxylic acid, 4-(aminomethyl)-, trans     CAS RN^®: 1197-18-8; UNII: 6T84R30KC1.

1 DEFINITION

Tranexamic acid contains NLT 98.0% and NMT 102.0% of tranexamic acid (C₈H₁₅NO₂), calculated on the dried basis.

2 IDENTIFICATION

A. SPECTROSCOPIC IDENTIFICATION TESTS (197), Infrared Spectroscopy: 197K

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

PROCEDURE

Buffer: Dissolve 11 g of monobasic sodium phosphate in 500 mL of water, and add 5 mL of triethylamine. Add 1.4 g of sodium dodecyl sulfate and adjust with phosphoric acid to a pH of 2.5. Dilute with water to 600 mL.

Mobile phase: Methanol and Buffer (40:60)

Standard solution: 1 mg/mL of USP Tranexamic Acid RS in water

Sample solution: 1 mg/mL of Tranexamic Acid in water

Chromatographic system

(See Chromatography (621), System Suitability.)

Mode: LC

Detector: UV 220 nm

Column: 4.6-mm x 25-cm; 5-µm packing L1

Column temperature: 35°

Flow rate: 1.5 mL/min

Injection volume: 20 µL

Run time: NLT 2.5 times the retention time of tranexamic acid

System suitability

Sample: Standard solution

Suitability requirements

Tailing factor: NMT 2.0

Relative standard deviation: NMT 0.73%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of tranexamic acid (C₈H₁₅NO₂) in the portion of Tranexamic Acid taken:

                          Result = (r_U/r_S) × (C_S/C_U) × 100

r_U = peak response of tranexamic acid from the Sample solution

r_S = peak response of tranexamic acid from the Standard solution

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

C_U = concentration of Tranexamic Acid in the Sample solution (mg/mL)

Acceptance criteria: 98.0%-102.0% on the dried basis

4 IMPURITIES

4.1 RESIDUE ON IGNITION (281)

Sample: 1 g of Tranexamic Acid

Acceptance criteria: NMT 0.1%

4.2 CHLORIDE AND SULFATE (221), Chloride

Standard solution: 0.1 mL of 0.020 N hydrochloric acid

Sample: 0.51 g of Tranexamic Acid

Acceptance criteria: The Sample shows no more chloride than the Standard solution (NMT 0.014%).

4.3 ORGANIC IMPURITIES

Buffer and Mobile phase: Prepare as directed in the Assay.

System suitability solution: 0.2 mg/mL of USP Tranexamic Acid RS and 0.002 mg/mL of USP Tranexamic Acid Related Compound C RS in water

Sensitivity solution: 5 µg/mL of USP Tranexamic Acid RS in water

Standard solution: 50 µg/mL of USP Tranexamic Acid RS in water

Sample solution: 10 mg/mL of Tranexamic Acid in water

Chromatographic system

(See Chromatography (621), System Suitability.)

Mode: LC

Detector: UV 220 nm

Column: 4.6-mm x 25-cm; 5-µm packing L1

Flow rate: 1 mL/min.

Injection volume: 20 µL

Run time: 3 times the retention time of tranexamic acid

System suitability

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

[NOTE-See Table 1 for the relative retention times.]

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

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

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of each individual specified or unspecified impurity in the portion of Tranexamic Acid taken:

                          Result = (r_U/r_S) × (C_S/C_U) × (1/F) × 100

r_U = peak response of each individual specified or unspecified impurity from the Sample solution

r_S = peak response of tranexamic acid from the Standard solution s

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

C_U = concentration of Tranexamic Acid in the Sample solution (mg/mL)

F = relative response factor (see Table 1)

Acceptance criteria: See Table 1. The reporting threshold is 0.025%.

Table 1

^a 4-(Aminomethyl)benzoic acid.

^b cis-4-(Aminomethyl) cyclohexanecarboxylic acid.

^c trans,trans-4,4'-[Iminobis (methylene)]dicyclohexanecarboxylic acid.

5 SPECIFIC TESTS

LOSS ON DRYING (731)

Sample: 1.00 g of Tranexamic Acid

Analysis: Dry the Sample at 105° under vacuum for 2 h..

Acceptance criteria: NMT 0.5%

6 ADDITIONAL REQUIREMENTS

PACKAGING AND STORAGE: Preserve in tight containers, and store at a temperature not exceeding 30°.

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 · HCI               191.66 _{▲(CN 1-Aug-2024)}