Dapagliflozin medicinal composition and preparation method thereof

Abstract

The invention provides a dapagliflozin medicinal composition. The dapagliflozin medicinal composition is characterized by consisting of the following components in percentage by mass: 1 to 95 percent of a dapagliflozin and microcrystalline cellulose composition, 0 to 95 percent of a filling agent / an adhesive, 0 to 20 percent of a disintegrant, 0.1 to 5 percent of a lubricating agent and 0 to 10 percent of a flow aid. According to the dapagliflozin medicinal composition, microcrystalline cellulose serves as a carrier material; according to a method provided by the invention, the dapagliflozin and microcrystalline cellulose are mixed and heated so that the dapagliflozin is molten; the dapagliflozin covers the surface of the microcrystalline cellulose in a liquid form; after the dapagliflozin is cooled, the dapagliflozin is solidified on the surface of the microcrystalline cellulose to form a dapagliflozin and microcrystalline cellulose compound; the specific surface area of the dapagliflozin is increased, so that the medicine dissolving speed can be improved and the quality is stable; the preparation method provided by the invention is simple and feasible, and is suitable for industrial production.

Description

technical field [0001] The invention relates to medicine preparation, in particular to a preparation method of a sodium-glucose cotransporter 2 inhibitor dapagliflozin composition. Background technique [0002] Diabetes mellitus is a common endocrine and metabolic disease characterized by hyperglycemia accompanied by disturbances in sugar, fat and protein metabolism caused by insufficient insulin secretion and / or action defects. According to the statistics of the International Diabetes Federation (IDF), the number of diabetic patients (20 to 79 years old) in the world reached 387 million in 2014, and it is expected to reach 592 million in 2035. Type II diabetes is the most common form of diabetes, accounting for 90% of diabetes cases. Its high-frequency complications, such as diabetic foot and renal failure, not only affect the quality of life of patients, but may also lead to shortened life span. Because patients with type 2 diabetes cannot respond appropriately to insuli...

AI Technical Summary

Problems solved by technology

Patent CN 200880016902 discloses the preparation method of dapagliflozin tablets. The solubility is improved by making dapagliflozin and propylene glycol monohydrate into a co-crystal. However, although the solubility increases, the dissolution rate is very slow and still needs to be passed Micro-grinding method to reduce particle size

[0007] Studies have found that dapagliflozin has a low melting point (75-80°C). If it is micronized by ordinary machinery to reduce the particle size, it is easy to stick and needs to be pulverized by low-temperature airflow, which requires high equipment requirements, cumbersome procedures, and low production efficiency.

In addition, the raw material density of dapagliflozin is small, if the particle size is controlled in a small range, such as D 90 ≤50μm, easy to float, large dust, even if it is made into propylene glycol hydrate, it will not be improved, the contact area will be greatly increased, special protection and environmental dust control are required, and production safety hazards will be increased

Subsequent attempts to use 4%-8% hydroxypropyl cellulose aqueous solution for wet granulation, mixed unevenly, and long-term granulation generated heat, resulting in drug aggregation and particle size increase, affecting dissolution

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