Fast disintegrating tablets of nisoldipine for intra-oral administration

Abstract

Nisoldipine is a calcium channel blocker with low and variable oral bioavailability. This was attributed to slow dissolution and presystemic metabolism. Accordingly, the objective of this work was to enhance the dissolution rate of nisoldipine to formulate fast disintegrating tablets with rapid dissolution. Binary solid dispersions (SD) were prepared for the drug with hydroxypropyl methyl cellulose E5 (HPMC), polyvinylpyrrolidone (PVP), Pluronic F68 or polyethylene glycol 6000 (PEG 6000). SD formation increased the dissolution rate compared to pure drug with the corresponding physical mixtures failing to provide the same dissolution enhancement. This indicates that the SD enhanced dissolution is not due to the solubilizing effect of the polymer and can be due to physical change in the drug crystal which was confirmed by thermal analysis. SD with HPMC and PVP were selected for preparation of fast disintegrating tablets as they liberated most of the drug in the first 5 min. HPMC-based tablets disintegrated rapidly and released most of the drug in the first 2 min which correlated with the corresponding SD. In contrast, PVP-based tablets disintegrated slowly with gradual dissolution. This can be attributed to the binding effect of PVP. The study developed fast disintegrating tablet for intra-oral administration.

Formulation and evaluation of simvastatin buccal film

“…In addition the spectrum revealed a broad band at 3442.31 which reflects the hygroscopic nature of the polymer. This is similar to the previously recorded spectrum (Giri et al, 2011) (El Maghraby andElsergany, 2014). It is important to note that the critical function groups (carbonyl and hydroxyl groups) are existing in the drug as well as in the tested polymer.…”

Design and Statistical Evaluation of a Multiunit Delivery System Containing Nisoldipine-Soluplus® Solid Dispersion for Hypertension Chronotherapy

“…Other Characteristic bands were observed at 2967, 3102, 1656, 1706, 1531 and 1349 cm -1 owing to Csp3-H stretching, Csp2-H stretching, C=N, C=O stretching (carbonyl groups of the two side chain in the structure of DHP), N = O asymmetrical stretching and N = O symmetrical stretching respectively. Among these, the N-H and C=O groups can form hydrogen bonding with the polymer [18]. The IR spectrum of all solid dispersions showed the absence of the characteristic peak at 3321 cm -1 and a peak broadening in this region was seen.…”

Insights Into Formulation Technologies and Novel Strategies for the Design of Orally Disintegrating Dosage Forms: A Comprehensive Industrial Review

“…The prepared ODTs showed equivalent dissolution profiles to the marketed product in four different media. El-Maghraby and El-Sergany [114] enhanced the intra-oral administration of nisoldipine used in the treatment of angina pectoris and hypertension by its formulation in ODTs with subsequent fast dissolution. Nisoldipine ODTs were formulated by solid dispersion technique by using solvent evaporation method.…”