A kind of urapidil hydrochloride injection and preparation method thereof

Abstract

The invention relates to urapidil hydrochloride injection and a preparation method thereof, and belongs to the technical field of a drug preparation. The injection comprises the following raw materials of urapidil hydrochloride, an amino acid complex salt and 2-hydroxypropyl-beta-cyclodextrin at the mass ratio of 1 to (1-1.5) to (4-7). The urapidil hydrochloride injection has the characteristics of being easy to store and transport, sterilization-resistant, good in stability, not easy to go bad, and relatively convenient in clinical application.

Description

technical field

[0001] The invention relates to a preparation and a preparation method thereof, in particular to an urapidil hydrochloride injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique

[0002] Hypertension is a common disease, frequently-occurring disease. With the improvement of people's living standards, the number of hypertensive patients is increasing day by day, especially the number of hypertensive crisis and severe patients is constantly increasing. However, there are few safe and effective injectable drugs clinically used for this type of disease. Hypertension affects people's work and life, and hypertension is the most important risk factor for coronary heart disease and cerebrovascular disease. 50% of patients with myocardial infarction are hypertensive patients, and 76% of patients with sudden cerebral death have a history of hypertension. Therefore, the risk of high blood pres...

Examples

Embodiment 1

[0029] Prescription 1:

[0030]

[0031]

[0032] (1) Add the prescribed amount of 2-hydroxypropyl-β-cyclodextrin into 1000ml of water, stir to dissolve, adjust the pH value to 9.0 with 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain solution 1 ;

[0033] (2) Add the prescribed amount of urapidil hydrochloride and L-arginine-L-aspartic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0034] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 7.5 with 0.1N hydrochloric acid solution to obtain solution 3.

[0035] (4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 115 μm afte...

Embodiment 2

[0037] Prescription 2:

[0038]

[0039] (1) Add 1000ml of water and stir to dissolve the prescribed amount of 2-hydroxypropyl-β-cyclodextrin, adjust the pH value to 11.0 with the prescribed amount of 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain a solution 1;

[0040] (2) Add the prescribed amount of urapidil hydrochloride and L-lysine-L-glutamic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0041] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 5.0 with 0.1N hydrochloric acid solution to obtain solution 3.

[0042](4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 1...

Embodiment 3

[0044] Prescription 3:

[0045]

[0046]

[0047] (1) Dissolve the prescribed amount of 2-hydroxypropyl-β-cyclodextrin in 1000ml of water, adjust the pH value to 10.5 with the prescribed amount of 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain a solution 1;

[0048] (2) Add the prescribed amount of urapidil hydrochloride and L-lysine-L-glutamic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0049] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 6.5 with 0.1N hydrochloric acid solution to obtain solution 3.

[0050] (4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 1...

technical field

[0001] The invention relates to a preparation and a preparation method thereof, in particular to an urapidil hydrochloride injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique

[0002] Hypertension is a common disease, frequently-occurring disease. With the improvement of people's living standards, the number of hypertensive patients is increasing day by day, especially the number of hypertensive crisis and severe patients is constantly increasing. However, there are few safe and effective injectable drugs clinically used for this type of disease. Hypertension affects people's work and life, and hypertension is the most important risk factor for coronary heart disease and cerebrovascular disease. 50% of patients with myocardial infarction are hypertensive patients, and 76% of patients with sudden cerebral death have a history of hypertension. Therefore, the risk of high blood pres...

Examples

Embodiment 1

[0029] Prescription 1:

[0030]

[0031]

[0032] (1) Add the prescribed amount of 2-hydroxypropyl-β-cyclodextrin into 1000ml of water, stir to dissolve, adjust the pH value to 9.0 with 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain solution 1 ;

[0033] (2) Add the prescribed amount of urapidil hydrochloride and L-arginine-L-aspartic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0034] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 7.5 with 0.1N hydrochloric acid solution to obtain solution 3.

[0035] (4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 115 μm afte...

Embodiment 2

[0037] Prescription 2:

[0038]

[0039] (1) Add 1000ml of water and stir to dissolve the prescribed amount of 2-hydroxypropyl-β-cyclodextrin, adjust the pH value to 11.0 with the prescribed amount of 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain a solution 1;

[0040] (2) Add the prescribed amount of urapidil hydrochloride and L-lysine-L-glutamic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0041] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 5.0 with 0.1N hydrochloric acid solution to obtain solution 3.

[0042](4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 1...

Embodiment 3

[0044] Prescription 3:

[0045]

[0046]

[0047] (1) Dissolve the prescribed amount of 2-hydroxypropyl-β-cyclodextrin in 1000ml of water, adjust the pH value to 10.5 with the prescribed amount of 0.1N sodium hydroxide solution, heat the solution to 40°C and stir for 1 hour to obtain a solution 1;

[0048] (2) Add the prescribed amount of urapidil hydrochloride and L-lysine-L-glutamic acid into a 50L reaction kettle, add 9000ml of water for injection and stir to dissolve, and stir at room temperature for 2h to obtain solution 1;

[0049] (3) Add solution 2 into solution 1, keep warm at 40°C and stir for 30 minutes, and adjust the pH value to 6.5 with 0.1N hydrochloric acid solution to obtain solution 3.

[0050] (4) Add 0.1% (g / v) activated carbon to solution 3 at room temperature, stir for 1 hour, remove the activated carbon by filtering with a 0.8um filter membrane, filter the filtrate with a 0.22 μm sterile microporous filter membrane, and pass the filtrate through 1...

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