A kind of high-purity mezlocillin sodium preparation and preparation method thereof

A technology for mezlocillin sodium and mezlocillin dry powder, which is applied in the directions of organic chemistry methods, active ingredients of heterocyclic compounds, organic chemistry, etc. Slow speed, product safety risks and other problems, to achieve the effect of good fluidity and dissolution speed, process optimization, and low insoluble particles

CN105902543BActive Publication Date: 2019-02-12NORTH CHINA PHARMA COMPANY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2019-02-12

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Abstract

The invention discloses a high-purity mezlocillin sodium preparation. The high-purity mezlocillin sodium preparation comprises uniform granules with the grain sizes smaller than 50 micrometers. The content of total impurities in the high-purity mezlocillin sodium preparation is lower than or equal to 0.68%, and the content of polymers in the high-purity mezlocillin sodium preparation is lower than or equal to 0.06%. The invention further discloses a method for preparing the high-purity mezlocillin sodium preparation. The method includes six steps of preparing ampicillin sodium solution; preparing mezlocillin sodium condensation liquid; preparing mezlocillin dry powder; preparing mezlocillin sodium solution; preparing mezlocillin sodium active compounds; preparing the high-purity mezlocillin sodium preparation. The high-purity mezlocillin sodium preparation and the method have the advantages that existing problems can be solved by the aid of the high-purity mezlocillin sodium preparation prepared by the aid of novel crystallization technologies, and the quality of the high-purity mezlocillin sodium preparation can be greatly improved; the high-purity mezlocillin sodium preparation is high in dissolving rate and purity, low in impurity content and insoluble particle content, good in flowability and easy to separately package, and the like.
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Description

technical field

[0001] The invention relates to the technical field of medicine preparation, in particular to a high-purity mezlocillin sodium preparation and a preparation method thereof. Background technique

[0002] Mezlocillin sodium, English name Mezloeillin Sodium, molecular formula C 21 h 24 N 5 NaO 8 S 2 , CAS No. 5979830 0, chemical name 3,3-dimethyl-6-[(R)-2-[3-(methylsulfonyl)-2-oxo-1-imidazolidinecarboxamido]-2- Sodium phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]-heptane-2-carboxylate. Mezlocillin sodium was discovered in 1968 by the Bayer Company of the Federal Republic of Germany in the study of ampicillin a-aminophthalated derivatives. It was first listed in the Federal Republic of Germany in 1977. In 1981, the US FDA officially approved the drug to be launched in the United States. Since the 1980s, it has been listed in the United States, Japan, Italy, the Netherlands, Switzerland and other countries.

[0003] Mezlocillin sodium is a semi-syntheti...

Examples

Embodiment 1

[0032] This example provides a kind of preparation method of high-purity mezlocillin dry powder, the steps include the preparation of ampicillin sodium solution, the preparation of mezlocillin sodium condensation liquid, the preparation of mezlocillin dry powder three steps. Specifically:

[0033] 1-1) Preparation of ampicillin sodium solution.

[0034] According to the molar ratio of ampicillin and sodium hydroxide being 1:1 to 1:1.25, 20 g of the reaction raw materials ampicillin and 1.98 to 2.48 g of sodium hydroxide were weighed. Wherein, the purity of ampicillin is 98%, and the purity of sodium hydroxide is 99%. Sodium hydroxide is dissolved in water to prepare a sodium hydroxide solution with a mass concentration of 3.9-4.0%, which is ready for use.

[0035] Add 200g of water to the reaction kettle, dissolve the weighed ampicillin in the water, then add sodium hydroxide solution to the reaction kettle, control the adding speed of the sodium hydroxide solution, and carr...

Embodiment 2

[0049] This embodiment provides a kind of preparation method of high-purity mezlocillin sodium preparation, with the mezlocillin dry powder prepared in Example 1 as raw material, and then through the preparation of ampicillin sodium solution and the preparation of mezlocillin sodium condensation liquid 1. Three steps of preparing the mezlocillin sodium preparation to obtain the mezlocillin sodium preparation. Specifically:

[0050] 2-1) Preparation of mezlocillin sodium solution.

[0051] According to the mol ratio of mezlocillin and sodium bicarbonate is 1: 1~1: 2, take by weighing the mezzlocillin 100g that embodiment 1 makes, sodium bicarbonate 15g, sodium bicarbonate is dissolved in water, configures mass concentration 10% sodium bicarbonate solution, ready to use.

[0052] Slowly add the dry powder of mezlocillin into the sodium bicarbonate solution, control the pH at the end point of the feed solution to be 5.5-7.0, control the reaction temperature at 20-25°C, and cont...