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KMID : 0369820120420040191
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Jorunal of Korean Pharmaceutical Sciences
2012 Volume.42 No. 4 p.191 ~ p.202
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Formulation optimization and in vitro characterization of sertraline loaded self-nanoemulsifying drug delivery system (SNEDDS) for oral administration
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Rahman Akhlaquer
Iqbal Zeenat
Hussain Arshad
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Abstract
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Sertraline is a selective serotonin reuptake inhibitors used as major therapeutic advances in psychiatry and is drug of choice for treatment of major depressive disorders. The drug (free base) encounters problem of poor aqueous solubility and vulnerability to enzymatic degradation in liver. The hydrochloride salts of free base revert back to its original form in gastrointestinal tract leading to slow/poor absorption. In the current study, sertraline loaded self-nanoemulsifying drug delivery systems (SNEDDS) were prepared in an attempt to circumvent the problems associated with poor aqueous solubility, vulnerability to enzymatic degradation in liver and to sort out the problems associated with salt formation. Preliminary screening was carried out to select proper ingredient combinations. Ternary phase diagrams were then constructed and an optimum system was designated. Formulations selected were then compared for optimization. The systems were assessed for robustness, globule size, cloud point, percentage transmittance, surface morphology and drug release. An optimum system composed of oil (25.42 %), surfactant (49.72 %), and co-surfactant (24.86 %). It possessed a mean globule size, cloud point and percentage transmittance of 63.5 nm, 90 °C and 82.43 %, respectively. Transmission electron microscopy demonstrated spherical particle morphology. The drug release from the selected formulation was significantly higher than other SNEDDS and drug suspension as well. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions.
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KEYWORD
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Sertraline, Phase titration, Ternary-phase diagram, Oral administration, Nanoemulsion, Self-nanoemulsifying drug delivery system
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