Solid sirolimus self-microemulsion preparation and preparation method thereof

A technology of sirolimus and emulsion preparation, applied in the field of medicine, can solve the problems of difficult transportation, storage and taking, affecting the disintegration and self-emulsifying effect, hardening of the capsule, etc., so as to improve the solubility and dissolution, improve the Dissolution and in vivo bioavailability, the effect of large dispersion

Inactive Publication Date: 2017-05-31
FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since self-microemulsion is a viscous liquid, it is difficult to transport, store and take, and almost all liquid self-microemulsion preparations are encapsulated in soft capsules in the form of concentrated solutions
The soft capsule shell prescription contains a certain amount of water, and the liquid self-microemulsion contains a large amount of surfactants. These ingredients continuously rob the shell of water during storage, and eventually cause the shell to harden, affecting its disintegration and self-micronization. emulsifying effect

Method used

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  • Solid sirolimus self-microemulsion preparation and preparation method thereof
  • Solid sirolimus self-microemulsion preparation and preparation method thereof
  • Solid sirolimus self-microemulsion preparation and preparation method thereof

Examples

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Embodiment 1

[0024] 【prescription】

[0025]

[0026] 【Preparation Process】

[0027] Preparation of liquid sirolimus self-microemulsion preparation: accurately weigh 10 mg of sirolimus and add it to 100 mg of co-emulsifier diethylene glycol monoethyl ether, stirring continuously until sirolimus is dissolved; Add 150 mg of oil phase polyethylene glycol glyceride oleate and 200 mg of emulsifier polyoxyethylene-35-castor oil successively, and continue to stir until a light yellow clear solution is formed to obtain a liquid sirolimus self-microemulsion preparation;

[0028] Preparation of mesoporous silica nanoparticles: Dissolve 1500 mg of cetyltrimethylammonium bromide in 1000 mL of deionized water, and add 30 mL of 0.5M sodium hydroxide solution dropwise to it. Stop stirring (speed is 500 r·min -1 ) For 30 min. Subsequently, a mixed solution of 5 mL of tetraethyl silicate and 8 mL of absolute ethanol was added. After the reaction was maintained for 2 h, the reaction was cooled to room temperature...

Embodiment 2

[0031] 【prescription】

[0032]

[0033] 【Preparation Process】

[0034] Preparation of liquid sirolimus self-microemulsion preparation: accurately weigh 50 mg of sirolimus and add it to 500 mg of co-emulsifier diethylene glycol monoethyl ether, stirring continuously until sirolimus is dissolved; Add 750 mg of oil-phase oleic acid polyethylene glycol glyceride and 1000 mg of emulsifier polyoxyethylene-35-castor oil successively, and keep stirring until a light yellow clear solution is formed to obtain a liquid sirolimus self-microemulsion preparation;

[0035] Preparation of mesoporous silica nanoparticles: Dissolve 1500 mg of cetyltrimethylammonium bromide in 1000 mL of deionized water, and add 30 mL of 0.5M sodium hydroxide solution dropwise to it. Stop stirring (speed is 500 r·min -1 ) For 30 min. Subsequently, a mixed solution of 5 mL of tetraethyl silicate and 8 mL of absolute ethanol was added. After the reaction was maintained for 2 h, the reaction was cooled to room temperatu...

Embodiment 3

[0038] 【prescription】

[0039]

[0040] 【Preparation Process】

[0041] Preparation of liquid sirolimus self-microemulsion preparation: accurately weigh 100 mg of sirolimus and add it to 1000 mg of co-emulsifier diethylene glycol monoethyl ether, stirring continuously until sirolimus is dissolved; Add 1500 mg of oil phase polyethylene glycol glyceride oleate and 2000 mg of emulsifier polyoxyethylene-35-castor oil successively, and continue to stir until a light yellow clear solution is formed to obtain a liquid sirolimus self-microemulsion preparation;

[0042] Preparation of mesoporous silica nanoparticles: Dissolve 1500 mg of cetyltrimethylammonium bromide in 1000 mL of deionized water, and add 30 mL of 0.5M sodium hydroxide solution dropwise to it. Stop stirring (speed is 500 r·min -1 ) For 30 min. Subsequently, a mixed solution of 5 mL of tetraethyl silicate and 8 mL of absolute ethanol was added. After the reaction was maintained for 2 h, the reaction was cooled to room tempera...

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Abstract

The invention discloses a solid sirolimus self-microemulsion preparation and a preparation method thereof. The solid sirolimus self-microemulsion preparation is prepared by adding a liquid self-microemulsion preparation prepared from sirolimus, polyethylene glycol oleate glyceride, polyoxyethylene-35-castor oil and diethylene glycol monoethyl ether to mesoporous silica nanoparticles, wherein the weight ratio of the liquid self-microemulsion preparation to the mesoporous silica nanoparticles is (1:1) to (10:1). The liquid self-microemulsion preparation is solidified by adopting the mesoporous silica nanoparticles, so that the disadvantages that the liquid self-microemulsion preparation is not easy to transport, store and take are reduced; compared with a commercially available tablet, the prepared solid sirolimus self-microemulsion preparation is capable of significantly improving the in-vitro dissolution rate and the in vivo bioavailability of the sirolimus. The preparation technology is simple, feasible and low in cost and has certain economic benefits and wide application prospects.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a solid sirolimus self-microemulsion preparation and a preparation method thereof. Background technique [0002] Sirolimus, also known as rapamycin, is a new type of macrolide antibiotic immunosuppressant. Recent studies have shown that it is effective in resisting transplant rejection, anti-tumor, and preventing restenosis after stent implantation. It has effects in various aspects, and can be used clinically for organ transplantation to resist rejection and treat rheumatoid arthritis, lupus erythematosus, psoriasis and other autoimmune diseases. Studies have also shown that the immunosuppressive effect of sirolimus is at least 30 times stronger than tacrolimus, which is similar in structure. The molecular formula of sirolimus is C 51 H 79 NO 13 , The relative molecular mass is 914.19, the melting point is 183~185℃, the appearance is white powder, the solubility in water...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/436A61K47/02A61K47/44A61P37/06A61P35/00A61P9/10A61P19/02A61P29/00A61P37/02A61P17/06
CPCA61K9/1075A61K31/436A61K47/02A61K47/44
Inventor 宋洪涛余越陶春刘志宏
Owner FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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