Application of hydroxypropyl betacyclodextrin in ezetimibe tablets

Ezetimibe is mainly used for primary hypercholesterolemia in clinic. As an adjuvant therapy other than diet control, ezetimibe can be used alone or in combination with HMG CoA reductase inhibitors such as statins in the treatment of hypercholesterolemia. It can reduce total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), apolipoprotein B (apoB), or as an adjuvant therapy for other lipid-lowering therapy (such as LDL-C) It can also be used to reduce the levels of TC and LDL-C in hofh patients when other lipid-lowering treatments are ineffective. Ezetimibe is insoluble in water. When ezetimibe is used orally, it must be dissolved in gastric juice in order to be absorbed. Pressed solid oral dosage forms, such as tablets and other common preparations, often limit their bioavailability due to their dissolution rate, thus affecting the efficacy of drugs. Reducing particle size is one of the methods commonly used in the field to increase solubility. In fact, the method of reducing particle size to improve solubility has been used in ezetimibe. However, reducing the particle size can not effectively improve the solubility of ezetimibe to a satisfactory range. Therefore, how to further improve the particle size, so as to improve the solubility and bioavailability of ezetimibe has become an urgent demand in the research of ezetimibe. Considering whether the cyclodextrin inclusion technology can be combined, the inventor added hydroxypropyl betacyclodextrin to the above solution, prepared the amorphous ezetimibe inclusion complex by simple granulation and drying, and used hydroxypropyl betacyclodextrin to dissolve in ethanol with a certain viscosity, and used it as adhesive, resulting in good fluidity of particles.

Shandong Binzhou Zhiyuan Biotechnology Co., Ltd. is a high-tech enterprise focusing on the R & D, production and application of cyclodextrin derivatives and cyclodextrin inclusion compounds. Its main products are hydroxypropyl beta cyclodextrin and sulfobutyl beta cyclodextrin 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. We sincerely look forward to working with you to create a better future!