Degarelix freeze-dried powder injection for injection and preparation method thereof

Abstract

In the process of researching a degarelix freeze-dried preparation, the inventor finds that viscosity of a medicine-containing solution can be lowered effectively and gelation time can be prolonged byadding a certain amount of tertiary butanol into a water solution before freeze-drying, the inventor further finds that adding of trehalose is conducive to further prolonging the gelation time and improving long-time stability of the preparation. On this basis, a degarelix freeze-dried preparation prescription and process are developed and are simple, easy for quality control and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a degarelix freeze-dried powder for injection and a preparation process thereof. Background technique [0002] In recent years, the incidence of prostate cancer has been increasing day by day, and it has become the male tumor type with the highest mortality rate. In 2006, the incidence rate in Europe was about 0.11%. In 2008, the incidence of prostate cancer in the United States was 186,320, and the death toll was 28,660, with a mortality rate of 15.4%. Studies have shown that testosterone levels are positively correlated with the proliferation rate of prostate cancer. If testosterone does not bind to the androgen receptor that can be expressed in most prostate cancer patients, cancer cells will undergo apoptosis. Both gonadotropin-releasing hormone (GnRH) receptor agonists and GnRH receptor antagonists can be used to control testosterone levels. [0003] Degarelix...

AI Technical Summary

Problems solved by technology

Some other organic solvents, such as ethanol, have low freezing points, and generally freeze at tens of degrees below zero. General freeze dryers cannot freeze and capture them, and eventually enter the vacuum pump, so they cannot be used in actual production.

[0021] ② The vapor pressure of tert-butanol is relatively high, which is conducive to sublimation and saves freeze-drying time, while another organic solvent, dimethyl sulfoxide, has a low vapor pressure and is difficult to sublimate, although its freezing point is 18.4°C. Difficult to freeze dry

Although cyclohexane can be frozen at room temperature (6.5°C), it is almost immiscible with water and can only be used for fat-soluble drugs, which greatly limits its application range

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