Ambroxol hydrochloride liquid preparation and preparation method thereof

Abstract

The invention discloses an ambroxol hydrochloride liquid preparation and a preparation method thereof. The method comprises the steps: dissolving ambroxol hydrochloride, stabilizing agent and osmotic pressure regulator into water used for injection, and evenly mixing together to obtain solution I; then, filtering the solution I, and obtaining the ambroxol hydrochloride liquid preparation. The preparation method does not introduce active carbon, so as to avoid the danger of hurting human body since active carbon particle is introduced into the preparation; meanwhile, the active ingredients in the preparation is ensured to be stable, and the safety (namely, the chemical stability of the ambroxol hydrochloride can be effectively improved, the particle content in the preparation is reduced, and the purity of the preparation is improved) of the finished product can be guaranteed.

Description

technical field

[0001] The invention relates to a liquid preparation of ambroxol hydrochloride and a preparation method thereof. Background technique

[0002] Ambroxol hydrochloride is a metabolite of bromhexine in the human body, and its chemical name is trans-4[(2-amino-3,5-dibromobenzyl)amino]cyclohexanol hydrochloride. The chemical structural formula is as follows: Molecular formula: C 13 h 18 Br 2 N 2 O·HCl, molecular weight: 414.57.

[0003]

[0004] Ambroxol hydrochloride is a new mucolytic drug. Mucus hypersecretion is an important pathophysiological feature of chronic airway inflammatory diseases, which can aggravate respiratory airflow obstruction and accelerate the decline of lung function. The mucus retained in the airway also becomes a good medium for bacterial growth, leading to the occurrence and aggravation of airway infection , and the infection and subsequent inflammatory products further cause mucus hypersecretion, thereby forming a vicious circle...

Examples

Embodiment 1

[0047] Embodiment 1: the preparation of ambroxol hydrochloride injection, totally 1000ml.

[0048] One, the preparation of ambroxol hydrochloride injection

[0049] In the sterile operating room, 15 g of ambroxol hydrochloride was dissolved in water for injection at 80° C., then 18 g of sodium chloride was added, stirred until fully dissolved, 200 ml of propylene glycol was added, and stirred evenly to obtain solution I.

[0050] Adjust the pH value to 3.6 with a mixed solution of 10% glacial acetic acid and citric acid.

[0051] In the aseptic operation room, the temperature of the above solution I was lowered to 40° C., and the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0052] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0053] The filtrate b was made up to 1000 ml with water for injection, and then filtered with a 0.22 μm pore size filter to obtain filtrat...

Embodiment 2

[0095] Embodiment 2: the preparation of ambroxol hydrochloride injection, altogether 1000ml.

[0096] The preparation process and filling process are carried out under the local level 100 of the 10,000-level clean area.

[0097] One, the preparation of ambroxol hydrochloride injection

[0098] In a sterile operating room, dissolve 30 g of ambroxol hydrochloride in water for injection at 50° C., then add 20 g of mannitol, stir until fully dissolved, add 100 ml of propylene glycol, and stir evenly to obtain a solution.

[0099] Adjust the pH value to 3.8 with a mixed solution of 10% glacial acetic acid and citric acid.

[0100] In the aseptic operation room, the temperature of the above solution I was lowered to 45° C., and then the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0101] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0102] The filtrate b was made up ...

Embodiment 3

[0128] Embodiment 3: the preparation of ambroxol hydrochloride injection, totally 1000ml.

[0129] The preparation process and filling process are carried out under the local level 100 of the 10,000-level clean area.

[0130] One, the preparation of ambroxol hydrochloride injection

[0131] In the sterile operating room, dissolve 50 g of ambroxol hydrochloride in water for injection at 60° C., then add 50 g of xylitol, stir until fully dissolved, add 250 ml of Tween-80, and stir evenly to obtain solution I.

[0132] Adjust the pH to 3.7 with 10% phosphate buffer.

[0133] In the aseptic operation room, the temperature of the above solution I was lowered to 42° C., and then the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0134] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0135] The filtrate b was made up to 1000 ml with water for injection, and then filtered ...

technical field

[0001] The invention relates to a liquid preparation of ambroxol hydrochloride and a preparation method thereof. Background technique

[0002] Ambroxol hydrochloride is a metabolite of bromhexine in the human body, and its chemical name is trans-4[(2-amino-3,5-dibromobenzyl)amino]cyclohexanol hydrochloride. The chemical structural formula is as follows: Molecular formula: C 13 h 18 Br 2 N 2 O·HCl, molecular weight: 414.57.

[0003]

[0004] Ambroxol hydrochloride is a new mucolytic drug. Mucus hypersecretion is an important pathophysiological feature of chronic airway inflammatory diseases, which can aggravate respiratory airflow obstruction and accelerate the decline of lung function. The mucus retained in the airway also becomes a good medium for bacterial growth, leading to the occurrence and aggravation of airway infection , and the infection and subsequent inflammatory products further cause mucus hypersecretion, thereby forming a vicious circle...

Examples

Embodiment 1

[0047] Embodiment 1: the preparation of ambroxol hydrochloride injection, totally 1000ml.

[0048] One, the preparation of ambroxol hydrochloride injection

[0049] In the sterile operating room, 15 g of ambroxol hydrochloride was dissolved in water for injection at 80° C., then 18 g of sodium chloride was added, stirred until fully dissolved, 200 ml of propylene glycol was added, and stirred evenly to obtain solution I.

[0050] Adjust the pH value to 3.6 with a mixed solution of 10% glacial acetic acid and citric acid.

[0051] In the aseptic operation room, the temperature of the above solution I was lowered to 40° C., and the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0052] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0053] The filtrate b was made up to 1000 ml with water for injection, and then filtered with a 0.22 μm pore size filter to obtain filtrat...

Embodiment 2

[0095] Embodiment 2: the preparation of ambroxol hydrochloride injection, altogether 1000ml.

[0096] The preparation process and filling process are carried out under the local level 100 of the 10,000-level clean area.

[0097] One, the preparation of ambroxol hydrochloride injection

[0098] In a sterile operating room, dissolve 30 g of ambroxol hydrochloride in water for injection at 50° C., then add 20 g of mannitol, stir until fully dissolved, add 100 ml of propylene glycol, and stir evenly to obtain a solution.

[0099] Adjust the pH value to 3.8 with a mixed solution of 10% glacial acetic acid and citric acid.

[0100] In the aseptic operation room, the temperature of the above solution I was lowered to 45° C., and then the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0101] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0102] The filtrate b was made up ...

Embodiment 3

[0128] Embodiment 3: the preparation of ambroxol hydrochloride injection, totally 1000ml.

[0129] The preparation process and filling process are carried out under the local level 100 of the 10,000-level clean area.

[0130] One, the preparation of ambroxol hydrochloride injection

[0131] In the sterile operating room, dissolve 50 g of ambroxol hydrochloride in water for injection at 60° C., then add 50 g of xylitol, stir until fully dissolved, add 250 ml of Tween-80, and stir evenly to obtain solution I.

[0132] Adjust the pH to 3.7 with 10% phosphate buffer.

[0133] In the aseptic operation room, the temperature of the above solution I was lowered to 42° C., and then the solution I was filtered with a 0.22 μm pore size filter to obtain the filtrate a.

[0134] Filtrate a was ultrafiltered with an ultrafilter with a molecular weight cutoff of 10,000 Daltons to obtain filtrate b.

[0135] The filtrate b was made up to 1000 ml with water for injection, and then filtered ...

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