Preparation of Immediate Release Tablets of Repaglinide by a Solubility Enhancer and Hot-Melt Extrusion Method

Abstract

To enhance the solubility of Repaglinide, we attempted to use Plasdone S 630, a novel solubility enhancer. Followed by the hot-melt extrusion method and made into a tablet dosage form. The prepared dosage forms subjected to all pre-compression and post-compression parameters evaluations. The data obtained from in-vitro drug release suggested that the trial-11 is the ideal formulation among all other formulations. The in-vitro release was also profiling around 95% within 45 minutes. The hardness of the prepared tablets was around 10-12 kg/cm 2 with the friability was less than 1%. So, this method could apply on the regular basis for formulating the tablet dosage forms.

Formulation and Evaluation of Solid Dispersion Incorporated Fast Disintegrating Tablets of Tenoxicam Using Design of Experiment

“…Samples were removed after 1, 2 and 3 months and evaluated for % drug content and in vitro dissolution studies and compared with those results. [20] Preparation of Tenoxicam fast disintegrating tablets Twenty-seven formulations (TF1-TF27) for active layer were prepared by direct compression method using 3 3 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like Gellan Gum, Fenugreek Seed Mucilage and L-HPC. All the formulations were varied in concentration of superdisintegrants, magnesium stearate constituted in all the formulations.…”

“…The prepared tablets were subjected to dissolution studies. [21] Response surface methodology Study type: Response surface Design type: central composite Design mode: quadratic Twenty-seven formulations (TF1-TF27) were prepared by direct compression method using 3 3 Response surface method where 3 3 indicates 3 variables and 3 levels of superdisintegrants like Gellan Gum, Fenugreek Seed Mucilage and L-HPC (low, middle and high concentrations) by using Design of experiment software. [21][22] Pre-compression evaluation tests Preformulation studies: Prior to compression, solid dispersions were evaluated for their characteristic precompression parameters, such as bulk density, tapped density, Hausner ratio, Car's compressibility index and angle of repose.…”

“…3 3 Response surface method with superdisintegrants like Gellan Gum, Fenugreek Seed Mucilage and L-HPC, and the prepared tablets were shown in Figure 12.…”

“…[2] But the oral formulation with poor solubility is a greater limitation for the formulation scientists, solubility enhancement should be the prime concern for a dosage form to get ideal bioavailability. [3] Although salt formation, solubilization, particle size reduction has commonly used to increase dissolution rate and thereby oral absorption and bioavailability of low water-soluble drugs 2-4, there is practical limitation to these techniques. [4] Among all the techniques solid dispersions is one of the promising techniques.…”

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“…The development of solid dispersions as a practically viable method to enhance the bioavailability of poorly water-soluble drugs to overcome the limitations of previous approaches such as salt formation, solubilization by co-solvents and particle size reduction studies revealed that drugs in solid dispersion need not necessarily exist in the micronized state. Eprosartan mesylate, chemically (E)-4-({2-Butyl-5-2-carboxy-2-(thiophene-2ylmethyl) eth-1-en-1-yl-1H-imidazol-1-yl} methyl) benzoic acid is an anti-hypertensive drug which prevents the vasoconstrictor and aldosteronesecreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle 1 .…”