FORMULATION AND DEVELOPMENT OF S-(-)-AMLODIPINE BESYLATE TABLETS TO IMPROVE THE DISSOLUTION PROFILE

Abstract

The object ive of the present study was to develop a tablet formulat ion of S- ( - ) - amlodipine besylate
chiral separation drug, L-Type Calcium channel blocker for better management of hypertension and also
suitable in the treatment diabetic hypertension patients, while reducing or avoiding undesirable adverse
effects, such as headache and edema, dizziness, flushing, palpitation, fatigue, nausea, abdominal pain
and somnolence which are often associated with administration of a racemic mixture of amlodipine. The
R (+) enantiomer lacks or has a lower level of antihypertensive activity.
I n the present study S- ( - ) - amlodipine besylate 5.0 mg tablets have been formulated and developed
using wet granulation and direct compression techniques respectively, to provide a safe, highly effective
method for treating severe hypertension while reducing undesirable adverse effects. Pre and post formulation
parameters were studied for the formulated batches. The study was also carried out to design
a suitable dissolution medium for S-(-)- amlodipine besylate. S-(-)- amlodipine besylate had maximum
solubility in pH 1.2 and thus the most suitable media for S-(-)- amlodipine besylate dissolution studies.
The dissolution profile of the formulated formulation was compared with the marketed preparation. The
results indicated improved dissolution profile of formulation (WMS3). The RSD below 2% indicated insignificant
batch-to-batch variation. The accelerated stability study of the optimized formulation was performed
as per the ICH guidelines. The results indicated no change in optical rotation of S-(-)- amlodipine
besylate.