阅读说明：本技术 一种注射用甲磺酸帕珠沙星组合物及其制备方法 (Pazufloxacin mesylate composition for injection and preparation method thereof ) 是由 李一青 韩勇 路国荣 于 2021-10-28 设计创作，主要内容包括：本申请公开了一种注射用甲磺酸帕珠沙星组合物,包括以下原料：甲磺酸帕珠沙星、牛磺酸、氯化钠、葡萄糖和注射用水。本申请还公开了一种注射用甲磺酸帕珠沙星组合物的制备方法。本申请所述的注射用甲磺酸帕珠沙星组合物不仅能为人体补充条件必需氨基酸,还能够减少腹泻、恶心、呕吐、过敏刺激等单一使用甲磺酸帕珠沙星引起的不良反应。本申请所述的注射用甲磺酸帕珠沙星组合物,具有很好的稳定性,甲磺酸帕珠沙星与牛磺酸不会发生化学反应,能够保持相对稳定。(The application discloses a pazufloxacin mesilate composition for injection, which comprises the following raw materials: pazufloxacin mesylate, taurine, sodium chloride, glucose and water for injection. The application also discloses a preparation method of the pazufloxacin mesylate composition for injection. The pazufloxacin mesylate composition for injection not only can supplement essential amino acids for human body conditions, but also can reduce adverse reactions caused by single use of pazufloxacin mesylate, such as diarrhea, nausea, vomiting, allergic stimulation and the like. The pazufloxacin mesylate composition for injection has good stability, and the pazufloxacin mesylate and taurine cannot generate chemical reaction and can keep relatively stable.)

1. The pazufloxacin mesylate composition for injection is characterized in that: the method comprises the following raw materials: pazufloxacin mesylate, taurine, sodium chloride, glucose and water for injection.

2. The pazufloxacin mesylate composition for injection as claimed in claim 1, wherein: the weight ratio of the raw materials is as follows: 3-5 parts of pazufloxacin mesilate, 5-10 parts of taurine, 9-12 parts of sodium chloride, 5-8 parts of glucose and 1000 parts of water for injection 800-.

3. The method for preparing pazufloxacin mesylate composition for injection as claimed in claim 1 or 2, wherein the method comprises the following steps: the method sequentially comprises the following steps:

(1) firstly, adding sodium chloride, glucose and taurine into water for injection to prepare a first solution;

(2) adding pazufloxacin mesylate into the first solution for dissolving, and adjusting the pH value to 3.0-3.3 to prepare a second solution;

(3) and heating the second solution, adding activated carbon for injection, stirring, sterilizing while the solution is hot, and filtering to obtain the pazufloxacin mesylate composition for injection.

4. The method for preparing pazufloxacin mesylate composition for injection according to claim 3, wherein the method comprises the following steps: and (3) adjusting the pH value in the step (2) by using a NaOH solution or an HCl solution.

5. The method for preparing pazufloxacin mesylate composition for injection according to claim 3, wherein the method comprises the following steps: the heating temperature in the step (3) is 70-80 ℃, and the stirring time is 5-10 min.

6. The method for preparing pazufloxacin mesylate composition for injection according to claim 3, wherein the method comprises the following steps: the sterile filtration in the step (3) is sterile filtration with a 0.22 μm pore filter.

7. The method for preparing pazufloxacin mesylate composition for injection according to claim 3, wherein the method comprises the following steps: said steps (1) and (2) are carried out at a temperature of between 15 and 35 ℃.

8. The application of taurine in pazufloxacin mesylate injection is provided.

Technical Field

The invention relates to the technical field of pharmaceutical preparations, in particular to a pazufloxacin mesilate composition for injection and a preparation method thereof.

Background

Pazufloxacin mesylate with chemical name of (-) -3S-10- (1-amino-cyclopropyl) -9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido [1, 2, 3-de]-[1，4]Benzoxazine-6-carboxylic acid methanesulfonate; molecular formula C₁₆H₁₅FN₂O₄·CH₄O₃S, a fourth-generation quinolone antibacterial agent developed by Fushan chemical industries, Japan, and used for treating various infections caused by gram-positive bacteria and gram-negative bacteria.

Furthermore pazufloxacin mesylate may present a gastrointestinal reaction leading to diarrhea (gastrointestinal dysbacteriosis) and thus electrolyte disturbance, and in addition there is a risk of hypoglycemia.

Disclosure of Invention

Therefore, the invention aims to provide a pazufloxacin mesilate composition for injection and a preparation method thereof, and the technical scheme of the invention is realized as follows:

the pazufloxacin mesylate composition for injection comprises the following raw materials: pazufloxacin mesylate, taurine, sodium chloride, glucose and water for injection.

The further technical scheme is that the weight ratio of the raw materials is as follows: 3-5 parts of pazufloxacin mesilate, 5-10 parts of taurine, 9-12 parts of sodium chloride, 5-8 parts of glucose and 1000 parts of water for injection 800-.

The preparation method of the pazufloxacin mesilate composition for injection sequentially comprises the following steps of:

(1) firstly, adding sodium chloride, glucose and taurine into water for injection to prepare a first solution;

(2) adding pazufloxacin mesylate into the first solution for dissolving, and adjusting the pH value to 3.0-3.3 to prepare a second solution;

(3) and heating the second solution, adding activated carbon for injection, stirring, sterilizing while the solution is hot, and filtering to obtain the pazufloxacin mesylate composition for injection.

The further technical proposal is that NaOH solution or HCl solution is used for adjusting the pH value in the step (2).

The further technical scheme is that the heating temperature in the step (3) is 70-80 ℃, and the stirring time is 5-10 min.

The further technical proposal is that the sterilization filtration in the step (3) is sterilization filtration by a 0.22 mu m pore filter membrane.

The further technical proposal is that the steps (1) and (2) are operated at 15-35 ℃.

The further technical scheme is that the taurine is applied to the pazufloxacin mesylate medicine for injection.

The taurine is the best compatible raw material of the pazufloxacin mesilate injection, and is not only essential amino acid for human condition, so that the normal physiological activity of the organism can be regulated, and the immunity of the organism can be enhanced; is a growth promoting factor of bifidobacterium in human intestinal tracts and can optimize the structure of a bacterial colony in the intestinal tracts; and the dilute solution is neutral, is stable to heat, does not participate in the synthesis of protein, is convenient for the regulation and control of pH and temperature in the preparation process of the pazufloxacin mesylate composition, and can be possibly used together with other amino acid or protein injection in the future.

In addition, the pH is adjusted after the taurine is added, and the taurine can play a role of a pH buffering agent so as to prevent the pazufloxacin mesylate from reacting or crystallizing out due to overlarge pH change. In addition, taurine is added to avoid the stimulation response of the organism caused by local acid stimulation when the pazufloxacin mesylate composition for injection is clinically used.

Compared with the prior art, the invention has the beneficial effects that:

(1) the pazufloxacin mesylate composition for injection not only can supplement essential amino acids for human body conditions, but also can reduce adverse reactions caused by single use of pazufloxacin mesylate, such as diarrhea, nausea, vomiting, allergic stimulation and the like.

(2) The method reasonably controls the dosage of glucose, and can relieve hypoglycemia symptoms caused by single use of pazufloxacin mesylate.

(3) The pazufloxacin mesylate composition for injection has good stability, and the pazufloxacin mesylate and taurine cannot generate chemical reaction and can keep relatively stable.

Detailed Description

For clear and complete description of the technical solutions in the present invention, it is obvious that the inventor combines the embodiments to describe, but the following embodiments describe only some embodiments of the present invention, not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.

Example 1

The pazufloxacin mesylate composition for injection comprises the following raw materials in parts by weight: 3 parts of pazufloxacin mesilate, 5 parts of taurine, 9 parts of sodium chloride, 5 parts of glucose and 800 parts of water for injection.

Example 2

The pazufloxacin mesylate composition for injection comprises the following raw materials in parts by weight: 5 parts of pazufloxacin mesilate, 10 parts of taurine, 12 parts of sodium chloride, 8 parts of glucose and 1000 parts of water for injection.

Example 3

The pazufloxacin mesylate composition for injection comprises the following raw materials in parts by weight: 4 parts of pazufloxacin mesilate, 8 parts of taurine, 10 parts of sodium chloride, 6 parts of glucose and 900 parts of water for injection.

The preparation method of pazufloxacin mesylate composition for injection of the embodiment 1 to 3 sequentially comprises the following steps:

(1) firstly, adding sodium chloride, glucose and taurine into water for injection to prepare a first solution;

(2) adding pazufloxacin mesylate into the first solution for dissolving, and adjusting the pH value to 3.2 to prepare a second solution;

(3) and heating the second solution, adding activated carbon for injection, stirring, sterilizing while the solution is hot, and filtering to obtain the pazufloxacin mesylate composition for injection.

And (3) adjusting the pH value in the step (2) by using a NaOH solution. The heating temperature in the step (3) is 75 ℃, and the stirring time is 5-10 min. The sterile filtration in the step (3) is sterile filtration with a 0.22 μm pore filter. Said steps (1) and (2) are carried out at 25 ℃.

Example 4

A preparation method of pazufloxacin mesylate composition for injection sequentially comprises the following steps:

(1) firstly, adding sodium chloride, glucose and taurine into water for injection to prepare a first solution;

(2) adding pazufloxacin mesylate into the first solution for dissolving, and adjusting the pH value to 3.0 to prepare a second solution;

(3) and heating the second solution, adding activated carbon for injection, stirring, sterilizing while the solution is hot, and filtering to obtain the pazufloxacin mesylate composition for injection.

And (3) adjusting the pH value in the step (2) by using an HCl solution. The heating temperature in the step (3) is 70 ℃, and the stirring time is 5 min. The sterile filtration in the step (3) is sterile filtration with a 0.22 μm pore filter. Said steps (1) and (2) are carried out at 15 ℃.

Example 5

A preparation method of pazufloxacin mesylate composition for injection sequentially comprises the following steps:

(1) firstly, adding sodium chloride, glucose and taurine into water for injection to prepare a first solution;

(2) adding pazufloxacin mesylate into the first solution for dissolving, and adjusting the pH value to 3.3 to prepare a second solution;

(3) and heating the second solution, adding activated carbon for injection, stirring, sterilizing while the solution is hot, and filtering to obtain the pazufloxacin mesylate composition for injection.

And (3) adjusting the pH value in the step (2) by using a NaOH solution. The heating temperature in the step (3) is 80 ℃, and the stirring time is 10 min. The sterile filtration in the step (3) is sterile filtration with a 0.22 μm pore filter.

Stability survey

According to the national food and drug administration standard YBH03252010, 100mL of samples of examples 1-3 are taken, placed at 20 ℃ for 3h, 6h and 12h and observed, and the content of pazufloxacin mesylate and taurine is measured. The results are shown in Table 1.

TABLE 1

As can be seen from Table 1, the pazufloxacin mesylate composition for injection, which is described in the embodiments 1 to 3 of the application, is colorless and transparent in appearance within 12 hours, has no obvious change in pH value, and has basically stable contents of pazufloxacin mesylate and taurine, thereby meeting clinical requirements.

The above description is only for the purpose of illustrating the preferred embodiments of the present invention and is not to be construed as limiting the invention, and any modifications, equivalents, improvements and the like that fall within the spirit and principle of the present invention are intended to be included therein.