Formulation, Development, and Optimization of Anti- Hypertensive Nisoldipine Extended-Release Tablet Formulation

Abstract

A drug molecule has to be water-soluble to be readily delivered to the cellular membrane. Many drugs are waterinsoluble,
which creates numerous problems in the development of dosage forms. Controlled drug delivery
formulation releases the drug with controlled kinetics for days and months, reducing the frequency of dosing,
minimizing side effects, and improving patient compliance. Nisoldipine is a calcium channel antagonist that is
indicated for the treatment of hypertension with very poor aqueous solubility. Thus, there is a need to improve
the rate of drug release. Hence, the study was carried out to design, formulate and evaluate sustained-release
tablet formulation of nisoldipine. Nisoldipine controlled release matrix tablets were prepared by roll compaction
method. Preformulation studies have confirmed the purity and compatibility of drug with excipients used in the
formulation. Pre-compression studies have confirmed the stability of formulation blends for compression. All
the prepared formulations were evaluated for various physical and compression parameters such as bulk and
tapped density, hardness, friability, and in vitro drug release studies. The results of drug release from prepared
compressed nisoldipine extended-release tablets were found to be within the desired range.