Abstract
The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid.
Highlights
TMZ, 1-[(2,3,4-tri-methoxyphenyl) methyl] piperazine is a lesser known member of a new class of antian-S
Basu and reperfusion in the myocardium (Harpey et al, 1989). It selectively inhibit long chain 3-keto acyl-co-enzyme A (CoA) thiolase (3-KAT), which catalyses the terminal step of fatty acid beta-oxidation (Stanley, 2002)
A simple and inexpensive method was developed for the preparation of calcium alginate beads
Summary
TMZ, 1-[(2,3,4-tri-methoxyphenyl) methyl] piperazine is a lesser known member of a new class of antian-. TMZ was incorporated into calcium alginate beads by sequential and simultaneous methods. The wet beads were immersed and stirred for 1hr in a solution containing TMZ (concentration ranging from 2-3 % w/v), filtered and washed with distilled water. TMZ-loaded calcium alginate beads were obtained by subsequent drying. Drug content was computed using a calibration curve (R2 = 0.9998) prepared using solutions with concentrations of 1-6 μg/mL of TMZ. The particle size determination of TMZ-loaded calcium alginate beads was carried out using an optical microscope along with a stage micrometer having an accuracy of 0.01 mm. The surface morphology of drug-loaded beads obtained from various percentages of polymer, CaCl2 and drug were studied by using a scanning electron microscope (model JEOL JSM-6360, Japan). The aliquots, following suitable dilution, were analyzed for drug content using a spectrophotometer at 202 nm
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