Abstract

A REVIEW ON ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR DETERMINATION OF AZELNIDIPINE IN PHARMACUETICAL DOSAGE FORM

Sanjana M.* and Ajitha A.

ABSTRACT

Azelnidipine (AZEL) is chemically (±)-3-(1-diphenylmethylazetidin3- yl) 5-isopropy12-amino-1, 4-dihydro-6-methyl-4-(3-nitrophenyl) 3, 5- pyridine. It is dihydropyridine (DHP) type of calcium channel blocker (CCB) used for the treatment of hypertension. AZEL has two enantiomers due to asymmetric carbon at the 4-position of the DHP ring. The pharmacological action of AZEL resides in the (R)-enantiomer. This is in marketed contrast to other CCBs in which the (S)-enantiomer is responsible for the biological activity. The peculiar three-dimensional structure of the active enantiomer of AZEL may be related to its unique pharmacological features that are not shared by other DHPs such as long-lasting reduction in blood pressure, decreased heart rate and Anti Atherosclerotic effect. AZEL also shows diuretic effect by increasing urine volume and thus reduction in retention of ions. The Antihypertensive effect of Azelnidipine is primarily based on the inhibition of trans-membrane Ca2+ influx through the voltage-dependent channels of vascular smooth muscles. Ca2+ channels are categorized into several subtypes, including L-type, N-type, T-type, P/Q-type and R-type Ca2+ channels depend on their electrophysiological properties. Clinical studies have demonstrated that Azelnidipine markedly reduced heart rate and proteinuria in hypertensive patients by inhibiting sympathetic nerve activity. Azelnidipine has also been confirmed to have Cardio-protective, Neuroprotective and Anti- atherosclerotic properties, and has also been found to prevent insulin resistance. Some analytical methods for the quantitative determination of Azelnidipine in pharmaceutical formulations like UV, RPHPLC, HPLC, UFLC, LC-ESI-MS HPLC-ESI-MS¹.

Keywords: Azelnidipine, Hypertension, UV, RP-HPLC, HPLC-ESI-MS, UFLC, LC-ESI-MS.