Formulation And Evaluation Of Novel Self Nanoemulsifying Drug Delivery System Of Sumatriptan Succinate

INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH(2020)

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摘要
In migraine disease which is an autoimmune disorder, 5-HT1 receptor agonist like Sumatriptan succinate (STS) is widely used. Its bioavailability is 15-17% due to extensive presystemic metabolism. The objective of this work was to prepare Sumatriptan succinate (STS) in a self nanoemulsifying drug delivery system (SNEDDS) and then convert it into solid-SNEDDS (S-SNEDDS) via extrusion/spheronization technique using Avicel pH 101, lactose monohydrate and Croscarmellose sodium. The component of SNEDDS was based on the solubility of STS in oily phases and surfactants. The screening of surfactants and cosurfactants were carried out in order to check its ability to emulsify the oily phase. Nanoemulsification area for the selected systems was identified by constructing the ternary phase diagrams. SNEP were characterized by scanning electron microscopy. SNEDDS composed of 30% Acrysol EL 135, 47% Tween 80 and 23% Capmul MCM C8. Its globule size was 98.4 nm, and zeta potential was -10.4 mV. S-SNEDDS possessed good mechanical strength and flow properties; angle of repose (25.79 +/- 0.167), Hausner's ratio (1.058 +/- 0.03) and Carr's index (5.55 +/- 1.23). SNE pellets of uniform size and shape were manufactured. The total friability of pellets and disintegration time showed promising results. The time required for 80% drug release of SNE pellets was found to be 18 min, which was significantly higher than SNEDDS, STS containing reference pellets and marketed preparation of STS (SUMINAT (R) 25). Therefore, STS loaded S-SNEDDS was successfully prepared with improved bioavailability and then formulated into self nanoemulsifying pellets to immediate drug release.
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关键词
Sumatriptan succinate, Self-nanoemulsifying pellets, Extrusion-spheronization
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