Injection mezlocillin sodium liposome and preparation method

A technology of mezlocillin sodium lipid and mezlocillin sodium, which is applied in the field of mezlocillin sodium liposome for injection and its preparation, can solve the problem that the dissolution time in winter is even several times that in summer, and the drug resistance and cardiotoxicity are high. , drug resistance and increased cardiotoxicity, etc., to solve the problem of insolubility, improve the therapeutic index, and reduce drug toxicity.

Active Publication Date: 2012-07-18
SHANGHAI JINCHENG PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mezlocillin is difficult to absorb from the gastrointestinal tract, and sodium salt is commonly used for parenteral administration at present; at the same time, during the clinical use of mezlocillin sodium, it is often difficult to dissolve and dissolve for a long time (the dissolution time in winter is even summer several times), seriously affecting its clinical work efficiency
Although at present, many manufacturers add excipients to improve the solubility of mezlocillin sodium during production, the effect is still not obvious. At the same time, increasing the excipients increases the clinical allergic reaction rate of mezlocillin, making it drug-resistant Significantly increased sex and cardiotoxicity
[0003] Aiming at the characteristics of poor solubility, allergy rate, drug resistance and high cardiotoxicity of existing mezlocillin sodium for injection, the present invention applies a new type of liposome to mezlocillin sodium injection preparations to solve the problem of mezlocillin sodium injection. The problem of the poor solubility of cillin sodium effectively reduces the problems of allergy rate, drug resistance and cardiotoxicity simultaneously, and achieves unexpected effects, thereby completing the present invention

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1, the preparation of mezlocillin sodium liposome for injection

[0027] Prescription: Mezlocillin Sodium 1000g

[0028] Hydrogenated egg yolk phospholipids 5500g

[0029] Polysorbate 2800g

[0030] Trehalose 2500g

[0031] Mannitol 2500g

[0032] Vitamin E 500g

[0033] Preparation Process:

[0034] (1) Dissolve 5,500 g of hydrogenated egg yolk phospholipids and 2,800 g of polysorbate in 5 L of a mixed solvent of isopropanol and ethanol with a volume ratio of 3:1, and mix well to form a liposome solution. Place on a rotary thin film evaporator to remove isopropanol and ethanol under reduced pressure to obtain a phospholipid film, add a phosphoric acid-disodium hydrogen phosphate buffer solution with a pH of 5.0, stir and dissolve, and obtain a blank liposome solution;

[0035] (2) Dissolve 1000g of mezlocillin sodium in water for injection, mix evenly with the obtained blank lipid solution, and ultrasonically treat for...

Embodiment 2

[0037] Embodiment 2, the preparation of mezlocillin sodium liposome for injection

[0038] Prescription: Mezlocillin Sodium 2000g

[0039] Soy Lecithin 15000g

[0040] Cholesterol 1000g

[0041] Glucose 12000g

[0042] Glutathione 800g

[0043] Preparation Process:

[0044] (1) Dissolve 15,000g of soybean lecithin and 2,800g of cholesterol in 10L of chloroform, mix them evenly, and form a liposome solution. Place on a rotary thin film evaporator to remove chloroform under reduced pressure to obtain a phospholipid film, add a phosphoric acid-disodium hydrogen phosphate buffer solution with a pH of 5.5, stir and dissolve, and obtain a blank liposome solution;

[0045] (2) Dissolve 2000g of mezlocillin sodium in water for injection, mix evenly with the obtained blank lipid solution, and ultrasonically treat for 60 minutes at 50°C, then add 12000g of glucose and 800g of glutathione to fully dissolve, and the microporous Membrane filtration;

[00...

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Abstract

The invention relates to the technical field of medicine and discloses injection mezlocillin sodium liposome and a preparation method. The injection mezlocillin sodium liposome is powder-injection. Mezlocillin sodium is packed with liposome carriers formed by liposome framework materials containing antioxygen and a stabilizing agent so as to obtain freezing-dried preparation. The injection mezlocillin sodium liposome is composed of 1 part of the mezlocillin sodium, 2 parts to 13 parts of the liposome framework materials, 0.3 part to 5 parts of the stabilizing agent, 4 parts to 10 parts of a freezing-dried protection agent and 0.1 part to 2 parts of the antioxygen. The injection mezlocillin sodium liposome has the obvious advantages that the mezlocillin sodium is wrapped in the liposome, thereby resolving the problem of slight solubility and guaranteeing quality of products; and medicine carrier liposome is degraded in bodies, thereby having no toxicity and immunogenicity, effectively improving therapeutic indexes of medicine, reducing toxicity of the medicine and reducing side effects of allergy rate, drug resistance, cardiotoxicity and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to mezlocillin sodium liposome for injection and a preparation method thereof. Background technique [0002] Mezloeillin Sodium is a high-efficiency benzazole penicillin antibiotic, which was discovered by German Bayer Company in 1968 when studying ampicillin a-aminophthalated derivatives. It was first listed in the Federal Republic of Germany in 1977. It was officially approved to be listed in the United States. Since the 1980s, it has been listed in the United States, Japan, Italy, the Netherlands, Switzerland and other countries. Mezlocillin is difficult to absorb from the gastrointestinal tract, and sodium salt is commonly used for parenteral administration at present; at the same time, during the clinical use of mezlocillin sodium, it is often difficult to dissolve and dissolve for a long time (the dissolution time in winter is even summer several times), seriously affecting ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/431A61P31/04
Inventor 傅苗青傅妙英
Owner SHANGHAI JINCHENG PHARMACEUTICAL CO LTD
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