Acarbose 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

Acarbose Tablets contain NLT 90.0% and NMT 110.0% of the labeled amount of acarbose (C₂₅H₄₃NO₁₈).

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.

Change to read:

B. Spectroscopic Identification Tests 〈197〉, Infrared Spectroscopy: 197K: The spectrum obtained from the sample preparation _{(ERR 1-May-2023)} shows IR maxima in the regions of 3500–3200, 2950–2890, 1653–1633, and 1070–1000 cm^_–1

3 ASSAY

3.1 Procedure

Buffer: 0.6 mg/mL of monobasic potassium phosphate and 0.35 mg/mL of dibasic sodium phosphate in water. Filter and degas.

Mobile phase: Acetonitrile and Buffer (75:25)

System suitability solution: 20 mg/mL of USP Acarbose System Suitability Mixture RS in water

Standard solution: 10 mg/mL of USP Acarbose RS

Sample solution: Nominally 10 mg/mL of acarbose in water, prepared as follows. Transfer a portion of the powder, from NLT 20 Tablets, equivalent to 100 mg of acarbose to a suitable volumetric ask and add water to 50%–70% of the ask volume. Sonicate to dissolve and dilute with water to volume. Pass through a suitable filter of 0.45-μm pore size.

3.2 Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 210 nm

Column: 4.0-mm × 25-cm; 5-μm packing L8

Column temperature: 35°

Flow rate: 2 mL/min

Injection volume: 10 μL

Run time: NLT 2.5 times the retention time of acarbose

System suitability

Samples: System suitability solution and Standard solution

Suitability requirements

Peak-to-valley ratio: The ratio of the height of the impurity A peak to the height of the valley between the impurity A peak and the acarbose peak is NLT 1.2, System suitability solution

Tailing factor: NMT 2.0, Standard solution

Relative standard deviation: NMT 2.0%, Standard solution

3.3 Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of acarbose (C₂₅H₄₃NO₁₈) in the portion of Tablets taken:

Result = (r_U/r_S ) × (C_S/C_U) × 100

r_U = peak response of acarbose from the Sample solution

r_S = peak response of acarbose from the Standard solution

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

C_U = nominal concentration of acarbose in the Sample solution (mg/mL)

Acceptance criteria: 90.0%–110.0%

4 PERFORMANCE TESTS

4.1 Dissolution 〈711〉

Medium: Water, 900 mL, deaerated

Apparatus 2: 75 rpm

Time: 30 min

Determine the percentage of the labeled amount of acarbose (C₂₅H₄₃NO₁₈) dissolved by using the following procedure.

Buffer: 0.6 mg/mL of monobasic potassium phosphate and 0.35 mg/mL of dibasic sodium phosphate in water, adjusted to a pH of 6.8. Filter and degas.

Mobile phase: Acetonitrile and Buffer (5:95)

Standard stock solution: 10 mg/mL of USP Acarbose RS in Medium

Standard solution A (for Tablets labeled to contain 100 mg of acarbose): 0.1 mg/mL of USP Acarbose RS from the Standard stock solution in Medium

Standard solution B (for Tablets labeled to contain 50 mg of acarbose): 0.05 mg/mL of USP Acarbose RS from Standard solution A in Medium

Standard solution C (for Tablets labeled to contain 25 mg of acarbose): 0.025 mg/mL of USP Acarbose RS from Standard solution A 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: 4.0-mm × 12.5-cm; 5-μm packing L1

Column temperature: 40°

Flow rate: 1.8 mL/min

Injection volume: 100 μL

System suitability

Samples: Standard solution A, Standard solution B, or Standard solution C

Suitability requirements

Relative standard deviation: NMT 2.0% for the acarbose peak of Standard solution A, Standard solution B, or Standard solution C

Analysis

Samples: Standard solution A, Standard solution B, or Standard solution C; and Sample solution

Calculate the percentage of the labeled amount of acarbose (C₂₅H₄₃NO₁₈) dissolved:

Result = (r_U/r_S) × C_S × (1/L) × V × 100

r_U = peak response from the Sample solution

r_s = peak response from Standard solution A, Standard solution B, or Standard solution C

CS = concentration of USP Acarbose RS in Standard solution A, Standard solution B, or Standard solution C (mg/mL)

L = label claim (mg/Tablet)

V = volume of Medium, 900 mL

Tolerances: NLT 80% (Q) of the labeled amount of acarbose (C₂₅H₄₃NO₁₈) is dissolved.

4.2 Uniformity of Dosage Units 〈905〉

Meet the requirements

5 IMPURITIES

5.1 Organic Impurities

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

Standard solution 1: Prepare a 0.2-mg/mL solution of USP Acarbose RS in water by pipetting 1.0 mL of the Standard solution from the Assay into a 50-mL volumetric ask. Dilute with water to volume.

Sensitivity solution: Prepare a 0.02-mg/mL solution of USP Acarbose RS in water by pipetting 10.0 mL of Standard solution 1 into a 100-mL volumetric ask. Dilute with water to volume.

5.2 System suitability

Samples: System suitability solution, Standard solution 1, and Sensitivity solution

5.3 Suitability requirements

Peak-to-valley ratio: The ratio of the height of the impurity A peak to the height of the valley between the impurity A peak and the acarbose peak is NLT 1.2, System suitability solution

Tailing factor: NMT 2.0, Standard solution 1

Relative standard deviation: NMT 2.0%, Standard solution 1

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

5.4 Analysis

Samples: Sample solution and Standard solution 1

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 response of any individual impurity from the Sample solution

r_S = peak response of acarbose from Standard solution 1

C_S = concentration of USP Acarbose RS in Standard solution 1 (mg/mL)

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

F = relative response factor (see Table 1)

Acceptance criteria: See Table 1.

Table 1

^a 4-O-(4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino}-α-d-glucopyranosyl)-d-glucose.

^b (1R,4R,5S,6R)-4,5,6-Trihydroxy-2-(hydroxymethyl)cyclohex-2-en-1-yl 4-O-(4,6-dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3- (hydroxymethyl)cyclohex-2-en-1-yl]amino}-α-d-glucopyranosyl)-α-d-glucopyranoside.

^c O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino}-α-d-glucopyranosyl-(1→4)-O-α-d-glucopyranosyl-(1→4)-D-arabino-2-hexulopyranose.

^d α-d-Glucopyranosyl 4-O-(4,6-dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino}-α-d-glucopyranosyl)-α-d-glucopyranoside.

Microbial Enumeration Tests 〈61〉 and Tests for Specified Microorganisms 〈62〉: The total aerobic microbial count is NMT 10³ cfu/g, and the total combined yeasts and molds count is NMT 10² cfu/g. It meets the requirements of the testing of products for the absence of Escherichia coli (per gram).

6 ADDITIONAL REQUIREMENTS

Packaging and Storage: Preserve in tight, light-resistant containers at controlled room temperature.

USP Reference Standards 〈11〉

USP Acarbose RS

USP Acarbose System Suitability Mixture RS