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Preparation method of famotidine preparation for injection

A technology of famotidine and water for injection, which is applied in the field of preparation of injection famotidine preparations, can solve problems such as the increase of related substances, influence on drug safety, poor stability of famotidine, etc., and achieve the reduction of the content of related substances and accelerate Dissolution speed and effect of shortening dosing time

Pending Publication Date: 2020-12-01
江苏大同盟制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] (1) There is no restriction on the dosing temperature in the formula, because the stability of famotidine is poor, if a higher dosing temperature is used, the related substances may increase significantly
[0005] (2) There is no clear control statement on the weight loss on drying of the rubber stopper, because the preparation is generally small in size (20 mg), and the moisture in the rubber stopper may migrate into the drug during storage, resulting in an increase in water content, accelerating drug degradation, and affecting drug safety;

Method used

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  • Preparation method of famotidine preparation for injection
  • Preparation method of famotidine preparation for injection
  • Preparation method of famotidine preparation for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation method of the injection famotidine preparation of the present embodiment is to use famotidine as raw material, use water for injection as solvent, use mannitol, aspartic acid, poloxamer-188 as auxiliary materials, and use activated carbon as Sorbent, wherein the weight-to-volume ratio of famotidine and water for injection is 1:50 (g / ml)

[0028] The preparation process is as follows:

[0029] 1) Weigh 8g of aspartic acid, add an appropriate amount of water for injection, keep the dosing temperature within the range of 20-30°C, stir to dissolve, then add 20g of famotidine, 40g of mannitol, and poloxamer-1880.75 g, add water for injection cooled to the range of 20-30 ℃ to the full amount;

[0030] 2) Add 1 g of activated carbon according to 0.1% (g / mL) of the total amount of the liquid medicine, and stir at room temperature;

[0031] 3) Use a 1.2um microporous membrane filter to remove carbon, pre-filter through a 0.45um filter membrane, and then pass th...

Embodiment 2

[0056] Embodiment 2 effect verification

[0057] This example verifies the effect of the injection famotidine prepared in Example 1, Comparative Example 1, and Comparative Example 2.

[0058] Table 1 Comparison of detection results of injection famotidine prepared by different processes

[0059]

[0060] As can be seen from the comparative results in Table 1, the famotidine for injection prepared by using Example 1 of the present invention with a dosing temperature of 20-30°C and increasing the number of vacuum drying cycles and hot air drying time of the rubber stopper, the level of related substances Significantly reduced and qualified, the moisture test index is also qualified.

Embodiment 3

[0062] This example is a comparison of the stability of the products made in Comparative Example 2 and Example 1 of the present invention, focusing on the changing trend of related substances and moisture. The related substances of the product prepared in Comparative Example 1 have exceeded the standard limit, so the follow-up stability test was not carried out.

[0063] The injection famotidine prepared in Comparative Example 2 and Example 1 was placed for 6 months at a temperature of 40 ± 2°C and a relative humidity of 75% ± 5%. Monthly samples were taken to detect its properties, osmotic pressure ratio, clarity and color of the solution, related substances (total impurities), moisture, bacterial endotoxin, and content. The results are shown in Table 2.

[0064] Table 2 40±2℃, relative humidity 75%±5% accelerated stability data of reserved samples

[0065]

[0066] The injection famotidine prepared in Comparative Example 2 and Example 1 was placed for 12 months at a tem...

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Abstract

The invention provides a preparation method of a famotidine preparation for injection, and relates to the technical field of medicaments. The method comprises the following steps: s1, weighing a prescription amount of aspartic acid, adding a proper amount of water for injection, keeping the liquid preparation temperature within the range of 20-30 DEG C, performing stirring to dissolve the asparticacid, sequentially adding prescription amounts of famotidine, mannitol and poloxamer-188, and adding the water for injection to full dose; s2, adding activated carbon, and performing stirring at normal temperature, wherein the dosage of the activated carbon is 0.1% (g / mL) of the total amount of the liquid medicine; and s3, after sterilization, filtration and split charging, adopting a rubber plughalf-pressure plug of which the drying weight loss is controlled to be 0.15% or below after cleaning and sterilization, and performing freeze-drying according to set freeze-drying parameters. According to the invention, moisture can be kept stable in the storage period, the main drug dissolving speed can be increased, and the liquid preparation time is obviously shortened.

Description

technical field [0001] The invention belongs to the technical field of medicaments, and in particular relates to a preparation method of an injection famotidine preparation. Background technique [0002] Famotidine, its chemical name is: [1-amino-3-[[[2-[(diaminomethylene)amino]-4-thiazolyl]-methyl]thio]propylene]sulfonate amides. It is the cyclization of amidinothiourea and 1,3-dichloroacetone to generate 2-guanidino-4-chloromethylthiazole, and then react with thiourea, and then react with chloropropionitrile to generate 2-guanidino-4- [(cyanoethylthio)methyl]thiazole, and then carry out alcoholysis with methanol, and obtain famotidine through amination, which has obvious inhibitory effect on gastric acid secretion; injection famotidine is the lyophilized form of famotidine Powder, as a histamine H2 receptor antagonist, is clinically used in the treatment of gastric and duodenal ulcers, stress ulcers, acute gastric mucosal bleeding, gastrinoma and reflux esophagitis, etc....

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/26A61K47/18A61K47/10A61K31/426A61P1/04A61P7/04A61P35/00F26B5/06
CPCA61K9/0019A61K9/19A61K47/26A61K47/183A61K47/10A61K31/426A61P1/04A61P7/04A61P35/00F26B5/06
Inventor 柳海波葛晓进
Owner 江苏大同盟制药有限公司
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