Sirolimus self-microemulsion preparation and preparation method thereof

Abstract

The invention discloses a sirolimus self-microemulsion preparation and a preparation method thereof. Sirolimus, an oil phase, an emulgator and a co-emulsifier are compounded into a liquor self-microemulsion preparation, or the obtained liquor self-microemulsion preparation and an excipient are further prepared into a solid self-microemulsion preparation. According to the sirolimus self-microemulsion preparation and the preparation method thereof, a self-microemulsion technology is adopted, so that the solubility and the dissolution rate of the sirolimus are remarkably improved, and the sirolimus self-microemulsion preparation has the advantages that the bioavailability is higher, raw materials are easily obtained, the preparation technology is simple and practicable, the yield is high, the cost is low, the large-scale industrial production can be realized, and the remarkable economic benefit can be achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a sirolimus self-microemulsion preparation and a preparation method thereof. Background technique [0002] Sirolimus, also known as rapamycin, is a macrolide antibiotic isolated from the culture medium of actinomycetes by the Ayerst Research Institute of Canada in the early 1970s. Its molecular formula is C 51 h 79 NO 13 , the relative molecular mass is 914.19, and the structural formula is: [0003] [0004] Appearance is white crystal, melting point is 183-185°C, lipophilic, soluble in organic solvents such as methanol, ethanol, propanol and chloroform, very slightly soluble in water, belongs to BCS Ⅱ drug, and has low oral bioavailability. As a third-generation immunosuppressant, sirolimus is a new type of potent immunosuppressant with less toxicity and potential discovered so far, and it is becoming the basic drug for long-term immunosuppressive treatment o...

AI Technical Summary

Problems solved by technology

There are many problems in the clinical application of this preparation: ① Sirolimus contains cis-trans isomers, and sirolimus exists in the trans configuration in the solid state, but in the solution, sirolimus exists in the cis-trans configuration. There are two configurations, which are unstable, and the proportion of configurations changes with the difference of solvent and temperature; ② Lecithin in oral solution is in solution state, easily oxidized, and has strict requirements on production conditions; ③ The bioavailability of human body is low, only ④ It is difficult to take quantitatively, and i

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