Application of hydroxypropyl betadex in tacrolimus capsules

Tacrolimus, also known as FK506, is the first fermentation product isolated from Streptomyces by fujiwa Pharmaceutical Industry Institute in 1984. Its chemical structure is 23 yuan macrolides antibiotics. It is a powerful new immunosuppressant, which can inhibit the release of IL-2 and inhibit the effect of T-lymphocyte, 100 times stronger than cyclosporine. Tacrolimus was approved for listing in Japan for the first time on June 7, 1993, and then successively listed in the UK, the United States, Germany and other dozens of countries. It was used for acute anti rejection treatment of liver, kidney, and bone marrow transplantation. The development of formulations include capsule, injection and ointment. Because tacrolimus is a crystal structure, the purpose of the preparation of solid dispersion is to change it into amorphous. The existing technology is limited to the preparation of tacrolimus solid dispersion, and if tacrolimus is prepared into amorphous form by preparation technology, the same effect can be achieved, and there is no aging phenomenon of solid dispersion. Tacrolimus was dissolved in ethanol, and the solution was used as binder to prepare the granules on the auxiliary materials. The tacrolimus capsule was also rapidly dissolved. However, tacrolimus ethanol solution had a small viscosity, poor fluidity and large loading difference. The inventor combined with cyclodextrin inclusion technology and added hydroxypropylbetadicyclodextrin, and prepared by simple granulation and drying The amorphous tacrolimus inclusion complex was dissolved in ethanol with a certain viscosity by hydroxypropylbetachrin. The particles obtained by using it as binder had good fluidity.

Shandong Binzhou Zhiyuan Biotechnology Co., Ltd. is a high-tech enterprise focusing on the research, development, production and application of cyclodextrin derivatives and cyclodextrin inclusion complexes. Its main products are hydroxypropyl beta cyclodextrin and sulfobutyl betahydrocyclodextrin sodium. The company has a comprehensive R & D, quality inspection center and professional research team, and has maintained long-term cooperation with Shandong University. The company's products currently have more than 50 varieties, involving medicine, cosmetics, functional foods, flavors and fragrances, environmental protection, building materials, fine chemicals, new materials and other applications. It is a production enterprise with many types of cyclodextrins and complete specifications. Wisdom, long history "Zhiyuan biological sincerely looks forward to working with you to create the future!