Preparation method of mycophenolate sodium

Abstract

The invention belongs to the field of medicines, and particularly relates to a preparation method of mycophenolate sodium. According to the invention, mycophenolic acid is used as a raw material to prepare an M2 crystal form mycophenolate sodium bulk drug suitable for a preparation. According to the preparation method of the mycophenolate sodium, mycophenolic acids with various purities are used as raw materials and can be commercially purchased, and the raw materials are easy to obtain; according to the method, methyl isobutyl ketone which is low in toxicity is adopted as a solvent and is easy to recycle, the production cost is low, meanwhile, methyl isobutyl ketone serves as a crystallization solvent, the crystallization condition is mild, the obtained mycophenolate sodium is in an M2 crystal form, the stacking density ranges from 0.3 g/mL to 0.5 g/mL, and use of pharmaceutical preparations is facilitated. According to the preparation method of the mycophenolate sodium, the crystallization yield reaches up to 93% or above, the process is simple, and industrial production is facilitated.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of mycophenolate sodium. Background technique [0002] The statements in this section merely provide background information related to the present disclosure and do not necessarily constitute prior art. [0003] Mycophenolate Sodium (trade name of the original research drug "Miff") is also called mycophenolate sodium, which is another mycophenolic acid (also known as mycophenolate mofetil Mycophenolic acid) is an immunosuppressant active pharmaceutical ingredient, which is metabolized in the body to produce mycophenolic acid (MPA). [0004] Xiaoxi was approved by the US FDA for kidney transplantation in May 1995, and has been approved for heart transplantation and liver transplantation successively. It was approved by China SFDA in 1997, and has entered the National Medical Insurance List (Class A) and the Essential Drug List. The listed dosage forms inc...

AI Technical Summary

Problems solved by technology

[0010] To sum up, the following technical problems generally exist in the prior art: (1) The use of highly toxic solvents is not suitable for pharmaceutical production and use, and is likely to cause serious environmental pollution; (2) The use of two or more organic solvents Solvents are soluble in each other, which is not conducive to solvent recovery and high production costs; (3) The crystallization yield is low or the preparation process is harsh or the technical requirements are high, the production efficiency is low, and it is not conducive to large-scale production and use; (4) The crystals obtained by crystallization are small , which is not conducive to crystal separation; (5) The bulk density is too small, which affects the compressibility and fluidity, which is not conducive to the production of preparations; (6) Only crystal products can be obtained, but the impurity content in mycophenolic acid cannot be reduced, and the obtained The purity of mycophenolate sodium does not meet the requirements of the Pharmacopoeia