Printed on: Fri Jan 05 2024, 09:41:39 PM(EST) Status: Currently Official on 06-Jan-2024 DocId: GUID-3ED89AF2-51AF-4471-BACE-94AD0510DE2A_5_en-US

Printed by: USP NF Official Date: Official as of 01-Jan-2024 Document Type: USP @2024 USPC
Do Not Distribute DOI Ref: 0kylr DOI: https://doi.org/10.31003/USPNF_M115_05_01
1

CS = concentration of USP Acarbose RS in the Standard

Acarbose solution (mg/mL)
CU = concentration of the Sample solution (mg/mL)

Acceptance criteria: 95.0%–102.0% on the anhydrous

basis
IMPURITIES
• RESIDUE ON IGNITION á281ñ
Sample: 1.0 g
Acceptance criteria: NMT 0.2%
C25H43NO18 645.60
D-Glucose, O-4,6-dideoxy-4-[[[1S-(1α,4α,5β,6α)]-4,5,6- Change to read:
trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-α-
D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-; • CHROMATOGRAPHIC PURITY
O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3- Mobile phase, System suitability solution, Sample
(hydroxymethyl)-2-cyclohexen-1-yl]amino}-α-D- solution, and Chromatographic system: Proceed as
glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-D- directed in the Assay.
glucose CAS RN®: 56180-94-0; UNII: T58MSI464G. Diluted sample solution: Dilute 1.0 mL of the Sample
solution with water to 100.0 mL.
DEFINITION Analysis
Acarbose is produced by certain strains of Actinoplanes Samples: Sample solution and Diluted sample solution
utahensis. It contains NLT 95.0% and NMT 102.0% of Calculate the percentage of each impurity in the portion of

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acarbose (C25H43NO18), calculated on the anhydrous basis. Acarbose taken:
IDENTIFICATION Result = (r U/r A) × (1/F) ▲▲ (ERR 1-Jan-2024)
• A. SPECTROSCOPIC IDENTIFICATION TESTS á197ñ, Infrared
Spectroscopy: 197K rU = peak response of each impurity from the Sample
• B. The retention time of the major peak of the Sample
solution corresponds to that of the Standard solution, as
obtained in the Assay.
ASSAY
ci rA

F
solution
= peak response of the main acarbose peak from
the Diluted sample solution
= relative response factor for each impurity (see
• PROCEDURE Table 1)
ffi
Solution A: 0.6 mg/mL of monobasic potassium phosphate
and 0.35 mg/mL of dibasic sodium phosphate in water Acceptance criteria: See Table 1.
Mobile phase: Acetonitrile and Solution A (3:1)
System suitability solution: 20 mg/mL of USP Acarbose Table 1
System Suitability Mixture RS in water Relative Relative Acceptance
Standard solution: 20 mg/mL of USP Acarbose RS in water Retention Response Criteria,
Name Time Factor NMT (%)
O

Sample solution: 20 mg/mL of Acarbose in water

Chromatographic system Impurity Aa 0.9 1 0.6
(See Chromatography á621ñ, System Suitability.)
Impurity Bb 0.8 1.6 0.5
Mode: LC
Detector: UV 210 nm Impurity Cc 1.2 1 1.5
Column: 4-mm × 25-cm; packing L8
Impurity Dd 0.5 1.33 1.0
Column temperature: 35°
Flow rate: 2 mL/min Impurity E e
1.7 0.8 0.2
Injection volume: 10 µL
Impurity Ff 1.9 0.8 0.3
System suitability
Sample: System suitability solution Impurity G g
2.2 0.8 0.3
Identify the acarbose peak and the peaks due to the
Impurity Hh 0.6 1 0.2
impurities listed in Table 1.
Suitability requirements Any individual
Peak-to-valley ratio: The ratio of the height of the unknown impur- — —
ity 0.2
impurity A peak to the height of the valley between the
impurity A peak and the acarbose peak is NLT 1.2. Total impurities — — 3.0
Chromatogram comparability: The chromatogram
a O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)
obtained is similar to the chromatogram provided with
cyclohex-2-enyl]amino}-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-
USP Acarbose System Suitability Mixture RS for the (1→4)-D-arabino-hex-2-ulopyranose.
known impurities found. b (1R,4R,5S,6R)-4,5,6-Trihydroxy-2-(hydroxymethyl)cyclohex-2-enyl 4-O-[4,6-
Analysis dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-
Samples: Standard solution and Sample solution enyl]amino}-α-D-glucopyranosyl]-α-D-glucopyranoside.
c α-D-Glucopyranosyl 4-O-[4,6-dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-
Calculate the percentage of acarbose (C25H43NO18) in the
(hydroxymethyl)cyclohex-2-enyl]amino}-α-D-glucopyranosyl]-α-D-
portion of Acarbose taken: glucopyranoside.
d 4-O-[4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)
Result = (r U/r S) × (C S/C U) × 100 cyclohex-2-enyl]amino}-α-D-glucopyranosyl]-D-glucopyranose.
e O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)
rU = peak response from the Sample solution cyclohex-2-enyl]amino}-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-
rS = peak response from the Standard solution (1→4)-O-α-D-glucopyranosyl-(1→4)-D-arabino-hex-2-ulopyranose (4-O-α-
acarbosyl-D-fructopyranose).

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Printed on: Fri Jan 05 2024, 09:41:39 PM(EST) Status: Currently Official on 06-Jan-2024 DocId: GUID-3ED89AF2-51AF-4471-BACE-94AD0510DE2A_5_en-US
Printed by: USP NF Official Date: Official as of 01-Jan-2024 Document Type: USP @2024 USPC
Do Not Distribute DOI Ref: 0kylr DOI: https://doi.org/10.31003/USPNF_M115_05_01
2

f O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl) Acceptance criteria: +168° to +183°

cyclohex-2-enyl]amino}-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl- • PH á791ñ
(1→4)-O-α-D-glucopyranosyl-(1→4)-D-glucopyranose (4-O-α-acarbosyl-D-
glucopyranose). Sample solution: 50 mg/mL
g α-D-Glucopyranosyl O-4,6-dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3- Acceptance criteria: 5.5–7.5
(hydroxymethyl)cyclohex-2-enyl]amino}-α-D-glucopyranosyl-(1→4)-O-α-D- • WATER DETERMINATION, Method Ic á921ñ : NMT 4.0%
glucopyranosyl-(1→4)-O-α-D-glucopyranoside (α-D-glucopyranosyl α-
acarboside). ADDITIONAL REQUIREMENTS
h O-4,6-Dideoxy-4-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl) • PACKAGING AND STORAGE: Preserve in tight containers.
cyclohex-2-enyl]amino}-α-D-glucopyranosyl-(1→4)-O-6-deoxy-α-D- • USP REFERENCE STANDARDS á11ñ
glucopyranosyl-(1→4)-D-glucopyranose.
USP Acarbose RS
USP Acarbose System Suitability Mixture RS
SPECIFIC TESTS
• OPTICAL ROTATION, Specific Rotation á781Sñ
Sample solution: 10 mg/mL in water

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