Stable large-capacity fasudil hydrochloride injection

Abstract

The invention discloses a stable large-capacity fasudil hydrochloride injection, which comprises 30-120mg of fasudil hydrochloride and 5%-20% of glucose, or comprises 30-120mg of fasudil hydrochloride, 5%-10% of glucose and 0.9% of sodium chloride, wherein the pH (potential of hydrogen) value of the solution is 3.5-4.0, and the pH value is regulated through hydrochloric acid or NaOH.

Description

technical field [0001] The invention provides a stable large-capacity injection of fasudil hydrochloride, which belongs to the technical field of biomedicine. Background technique [0002] Cardiovascular and cerebrovascular diseases are diseases with high morbidity, mortality and disability, which seriously threaten people's lives and affect the quality of life of human beings. It is a major topic in the research field, with broad application prospects and far-reaching social significance. Epidemiological studies have shown that the prevalence, incidence and risk factors of cardiovascular and cerebrovascular diseases in the Chinese population are on the rise, and the number of deaths from cardiovascular and cerebrovascular diseases accounts for about 40% of the total population deaths, accounting for about 50% of the total number of deaths. Every year, more than 3 million people die from this disease nationwide, which is higher than most European and American countries, an...

AI Technical Summary

Problems solved by technology

[0008] Chinese Patent Application No. 200580008301.8 (Authorization No. CN1929847B) announced the patent "Preparation Containing Fasudil and Method for Improving Its Stability" applied by Japan Asahi Seika Pharmaceutical Co., Ltd. According to its patent specification, Fasudil is described The pH of the preparation is below 5.0, most preferably below pH 3.0, but the Fasudil injection under this condition cannot be directly applied to the human body due to its low pH, and needs to be diluted for use, so the patent specification also states that " The upper limit of the volume of the injection is preferably less than 50mL" (see paragraph 0055 of the patent specification), and at the same time, it is also specifically stated in this paragraph that the injection of the invention is irritating to the organism when the pH is low, and it needs to use 50mL-500mL of electrolyte or sugar It can be seen that the patentee also believes that the pH value protected by this patent is not suitable for Fasudil hydrochloride large volume injection (50-500ml)

The applicant of this patent proved through tests that the most preferred pH value of Chinese Patent Application No. 200580008301.8 (authorization number CN1929847B) is not suitable for Fasudil Hydrochloride Glucose Injection or Fasudil Hydrochloride Glucose Sodium Chloride Injection, because only The relative stability of Fasudil is satisfied, but the toxic related substance 5-hydroxymethylfurfural produced by glucose will increase a lot when the pH is too low

Images