کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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5550877 | 1557302 | 2016 | 7 صفحه PDF | دانلود رایگان |
The objective of this study was to evaluate the feasibility of lauryl sulfate (LS) salt/complex as a novel carrier in oral sustained-release suspensions. Mirabegron, which has a pH-dependent solubility, was selected as the model drug. Sodium lauryl sulfate (SLS) was bound to mirabegron in a stoichiometric manner to form an LS salt/complex. LS salt/complex formulation significantly reduced the solubility of mirabegron and helped mirabegron achieve sustained-release over a wide range of pH conditions. Microparticles containing the LS salt/complex were prepared by spray drying with the aqueous dispersion of ethylcellulose (Aquacoat® ECD). The diameter of the microparticles was less than 200 μm, which will help avoid a gritty taste. In vitro results indicated the microparticles had slower dissolution profiles than the LS salt/complex. The dissolution rate could be controlled flexibly by changing the amount of Aquacoat® ECD. The microparticle suspension retained the desired sustained-release property and dissolution profile after being stored for 30 days at 40 °C. In addition, the suspension displayed sustained-release behavior in dogs without a pronounced Cmax peak, which will help prevent side effects. These results suggest that microparticles containing LS salt/complex may be useful as a novel sustained-release suspension for oral delivery.
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Journal: International Journal of Pharmaceutics - Volume 515, Issues 1â2, 30 December 2016, Pages 677-683