Studies on sirolimus self-microemulsifying drug delivery system and its solidification

VernacularTitle:西罗莫司自乳化给药系统及其固体化研究
Author: Zhihong LIU ¹ ; Xiongwei HU ; Chun TAO ; Jing ZHANG ; Hongtao SONG
Author Information

1. 南京军区福州总医院药学科
Keywords: sirolimus; self-microemulsifying drug delivery system; solidification; central composite design; pellets
From: Journal of Pharmaceutical Practice 2016;34(2):142-147,170
CountryChina
Language:Chinese
Abstract: Objective To screen the formulation of self-microemulsifying drug delivery system (SMEDDS) for sirolimus (SRL) and prepare the SRL-SMEDDS pellets.Methods Co-emulsifier,oil phase and emulsifier were chosen by solubility test and ternary phase diagrams,central composite design and response surface method were adopted to screen and optimize the preparation and formulation of liquid SRL-SMEDDS.The selected liquid SRL-SMEDDS formulations were prepared into pellets by extrusion-spheronization method.Results The final pellets from liquid SRL-SMEDDS formulation :SRL 0.4%,Labrafil M1944CS 9.3%,Cremophor EL 15.9%,Transcutol P 8.0%,MCC 49.8%,lactose 13.3%,CMS-Na 3.3%.Dissolution test showed superphosphate (SSP) in the dissolution water is much greater than the commercially available sirolimus tablets ;while in 0.4% SDS solution,the two formulations showed similar dissolution.Conclusion SMEDDS can improve the dissolution of SRL in v itro.