Tranexamic Acid Injection

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 Injection is a sterile solution of Tranexamic Acid in Water for Injection. It contains 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: Transfer the content of Injection into a beaker and heat on a hot plate at 100° for 30 min, until a paste appears. Then heat it in an oven to complete dryness at 110° for about 30 min.

Acceptance criteria: Meets the requirements

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

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 lauryl sulfate, adjust with diluted phosphoric acid (10% w/w) to a pH of 2.5, and 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: Nominally 1 mg/mL of tranexamic acid prepared as follows. Transfer an accurately measured volume of Injection from a composite of contents from NLT 3 vials to a suitable volumetric flask, and dilute with water to volume.

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 220 nm
• Column: 4.6-mm × 25-cm; 5-µm packing L1
• Column temperature: 35°
• Flow rate: 1.5 mL/min
• Injection volume: 20 µL
• Run time: 2 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) in the portion of Injection 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 IMPURITIES

4.1 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 2 µg/mL of USP Tranexamic Acid Related Compound C RS in water

Sensitivity solution: 0.01 mg/mL of USP Tranexamic Acid RS in water

Standard solution: 0.05 mg/mL of USP Tranexamic Acid RS in water

Sample solution: Nominally 10 mg/mL of tranexamic acid prepared as follows. Transfer an accurately measured volume of Injection to an appropriate volumetric flask, and dilute with water to volume.

Chromatographic system

• (See Chromatography 〈621〉, System Suitability.)
• Mode: LC
• Detector: UV 220 nm
• Column: 4.6-mm × 25-cm; 5-µm packing L1
• Flow rate: 1 mL/min
• Injection volume: 20 µL
• Run time: 3.3 times the retention time of tranexamic acid

System suitability

• Samples: System suitability solution, Sensitivity solution, and Standard solution
• Suitability requirements
• Resolution: NLT 2.0 between tranexamic acid and tranexamic acid related compound C, System suitability solution
• Signal-to-noise ratio: NLT 10, Sensitivity solution
• Relative standard deviation: NMT 5.0%, Standard solution

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of each unspecified impurity in the portion of Injection taken:

Result = (rᵤ/rₛ) × (Cₛ/Cᵤ) × 100

rᵤ = peak response of each unspecified impurity 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. Disregard any impurity peaks less than 0.03%.

Table 1

ᵃ For identification only. These are process impurities monitored in the drug substance and are not included in the total impurities.

ᵇ 4-(Aminomethyl)benzoic acid.

ᶜ cis-4-(Aminomethyl)cyclohexanecarboxylic acid.

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

5 SPECIFIC TESTS

pH 〈791〉: 6.5–8.0

Particulate Matter in Injections 〈788〉: It meets the requirements for small-volume injections.

Sterility Tests 〈71〉: Meets the requirements

Bacterial Endotoxins Test 〈85〉: NMT 0.5 USP Endotoxin Units/mg of tranexamic acid

Other Requirements: It meets the requirements in Injections and Implanted Drug Products 〈1〉.

6 ADDITIONAL REQUIREMENTS

Packaging and Storage: Preserve in single-dose containers and store at controlled room temperature.

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