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

LIU Zhihong; HU Xiongwei; TAO Chun; ZHANG Jing; SONG Hongtao

doi:10.3969/j.issn.1006-0111.2016.02.012

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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 vitro.

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

Department of Pharmacy, Fuzhou General Hospital of Nanjing Command PLA, Fuzhou 350025, China

Received Date: 2016-01-01

Rev Recd Date: 2016-01-31

Key words:

sirolimus /
self-microemulsifying drug delivery system /
solidification /
central composite design /
pellets

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 vitro.

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Reference (7)

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

doi: 10.3969/j.issn.1006-0111.2016.02.012

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