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期刊论文

Solid self-nanoemulsifying cyclosporine A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility.

吴伟Yang Lei Yi Lu Jianping Qi Sufang Nie Fuqiang Hu Weisan Pan* Wei Wu*.

Int J Nanomedicine 2011,6:795-805.,-0001,():

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摘要/描述

The objective of this study is to evaluate fluid-bed coating as a new technique to prepare pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporine A as a model poorly water-soluble drug. The rationale of this technique is to entrap SNEDDS liquid in the matrix of the coating material PVP K30 by fluid-bed coating. Pseudo-ternary phase diagrams were employed to screen the SNEDDS liquid formulations. The optimal formulation was composed of Labrafil M 1944 CS, Transcutol P and Cremophor EL in the ratio of 9:14:7. To prepare solid SNEDDS pellets, the SNEDDS liquid was first dispersed in aqueous solution of PVP and then sprayed onto the surface of non-pareil pellets. Upon evaporation of water, PVP precipitated and formed tight films to entrap SNEDDS liquid. Visual observation and SEM analysis confirmed a good appearance of solid SNEDDS pellets. Results indicated that as much as 40% SNEDDS liquid could be entrapped in the coating layer. Powder X-ray diffraction analysis confirmed nonexistence of CyA crystalline in the formulation. Solid SNEDDS pellets showed a slower redispersing rate than the SNEDDS liquid counterpart. Increase in total SNEDDS liquid loading led to faster redispersing, whereas the increase of coating weight (up to 400%) significantly decreased the redispersing rate. Both CyA loading and protective coating with 5% PVP K30 did not significantly affect the redispersing rate. It is concluded that fluid-bed coating is a new technique with great potential to prepare pellet-based solid SNEDDS formulations.

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