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Indirect resolution of baclofen enantiomers from pharmaceutical dosage form by reversed-phase liquid chromatography after derivatization with Marfey's reagent and its structural variants

✍ Scribed by Ravi Bhushan; Virender Kumar


Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
120 KB
Volume
22
Category
Article
ISSN
0269-3879

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✦ Synopsis


A high-performance liquid chromatographic (HPLC) method was developed for chiral assay of baclofen enantiomers in pharmaceutical formulations using an indirect approach. Baclofen enantiomers were derivatized with Marfey's reagent (FDNP-L-Ala-NH 2 ) and its structural variants FDNP-L-Phe-NH 2 , FDNP-L-Val-NH 2 , FDNP-L-Leu-NH 2 and FDNP-L-Pro-NH 2 . The resultant diastereomers were separated on RP-TLC [triethylammonium phosphate buffer (pH 4.0, 50 mM)-acetonitrile, 50:50] and on a C 18 column using a linear gradient (45 min) of acetonitrile and 0.01% aqueous trifluoroacetic acid (TFA) with UV detection at 340 nm. The differences in the retention times (Δt R ) of diastereomers due to the five chiral reagents were compared. The maximum and minimum difference in retention times between separated diastereomers was for FDNP-L-Leu-NH 2 and FDNP-L-Pro-NH 2 , respectively. The effect of flow rate, acetonitrile content and TFA concentration on resolution was studied. The method was validated for linearity, repeatability, limit of detection and limit of quantification.