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Application Of Hydroxypropyl Beta Cyclodextrin In Tacrolimus Capsules
Time:2020/10/31
Class:NEWS

Tacrolimus, also known as FK506, was first isolated from Streptomyces by Fujisawa Institute of pharmaceutical industry in 1984. Its chemical structure belongs to 23 membered macrolide antibiotics. It is a powerful new immunosuppressant, mainly through inhibiting the release of interleukin-2, and comprehensively inhibiting the effect of T lymphocytes, which is 100 times stronger than cyclosporine. Tacrolimus was approved for the first time in Japan on June 7, 1993. Then tacrolimus was listed in dozens of countries, such as the United Kingdom, the United States and Germany. Tacrolimus is used for acute anti rejection treatment of liver, kidney and bone marrow transplantation. The developed formulations include capsule, injection and ointment. Because tacrolimus material is crystal structure, the purpose of preparing solid dispersion is to change it into amorphous. The prior art is limited to the preparation of tacrolimus solid dispersion. If tacrolimus is prepared into amorphous by preparation technology, the same effect will be achieved, and there is no aging phenomenon of solid dispersion. Tacrolimus was dissolved in ethanol, and the solution was used as an adhesive to make granules on the auxiliary materials, and tacrolimus capsules were obtained. However, the viscosity of tacrolimus ethanol solution was small, the fluidity of the prepared granules was poor, and the volume of the granules was greatly different. The inventors combined with cyclodextrin inclusion technology, added hydroxypropyl beta cyl cyclodextrin, and prepared by simple granulation and drying The amorphous tacrolimus inclusion complex was dissolved in ethanol by hydroxypropyl beta cyclodextrin, which had a certain viscosity. When it was used as adhesive, the particles had good fluidity.


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