Moreover, the salts that are formed may convert back to their original acid or base forms leading to aggregation in the gastrointestinal tract (GIT) leads to slow/poor absorption ( Serajuddin, 1999 Serajuddin ATM. For instance, salt formation of neutral compound is not feasible, and the synthesis of weak acid and weak base salts may not always be practical. But in general, these methods have their own limitations. Modification of the physicochemical properties such as salt formation of the compound is in practice as one of the approach to improve the dissolution rate of such drugs. 1999 14(5):259-275.), reported as most prescribed antidepressant in U.S.
Predictors of an acute antidepressant response to fluoxetine and sertraline. Sertraline was found to be safer than other SSRIs, work better than fluoxetine for some subtypes of depression ( Flament et al., 1999 Flament MF, Lane RM, Zhu R, Ying Z.
#RHEOCALC 3.3 FREE#
Sertraline (SRT) free base ( Figure 1) is lipophilic (log P, 5.1), poorly water-soluble drug (3.5 mg/L) belonging to the category “Selective Serotonin Reuptake Inhibitors (SSRIs)” commercially available as hydrochloride salt with around 44% oral bioavailability. SNEDDS Phase diagrams Solubility Thermodynamic stability Oral delivery Bioavailability These studies demonstrate that the solid SNEDDS are promising strategies for successful delivery of poorly water-soluble drug like sertraline. Pharmacokinetic studies after oral administration of liquid and solid SNEDDS in rats showed about 6-and 5-fold increased absorption of sertraline compared to the aqueous suspension of sertraline. In vitro release of sertraline from liquid and solid SNEDDS was found to be highly significant compared to plain sertraline (p<0.01). Liquid SNEDDS was transformed into free-flowing powder by solid adsorption technique followed by compression into tablets. Aqueous titration method was used to prepare the liquid SNEDDS ternary phase diagrams were constructed and based on smaller droplet size (24.8 nm), minimum viscosity (153.63 cP) and polydispersity index (0.182), higher percentage transmittance (95%) and in vitro drug release (97%), an optimum system was designated. Self-nanoemulsifying drug delivery system (SNEDDS) was prepared to enhance the solubility and thus oral bioavailability of sertraline. The purpose of the study was to combine the advantages of self-nanoemulsifying drug delivery systems and tablets as a conventional dosage form.
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