Cefminox sodium preparation for injection and preparation and use method thereof

A technology of cefminox sodium and solid sodium bicarbonate, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problem that the particle size distribution is difficult to achieve a narrow particle size distribution , It is difficult to meet the stability of pharmaceutical preparations, it is difficult to achieve the encapsulation rate and other problems, to achieve the effect of maintaining the consistency of liposome shape, no pollution of equipment cost, and simple and easy preparation method

Pending Publication Date: 2019-11-08
上海欣峰制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the repeatability of this method is not ideal, and it is difficult to achieve an encapsulation efficiency of more than 80% in practice; at the same time, the particle size distribution is also difficult to achieve a narrow particle size distribution in the range of 10 nm above and below the average particle size
In addition, when the proliposome preparation is stored for a long time (for example, more than 3 months), the drug encapsulation rate will also drop significantly, and it is difficult to meet the requirements for the stability of the drug preparation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Weigh 80 mg of cefminox sodium as medicine, 480 mg of N-(β-D-glucopyranose) octanamide, 1430 mg of HSPC and 950 mg of cholesterol as film-forming lipid material, 775 mg of tartaric acid and 155 mg of solid sodium bicarbonate particles. The solid sodium bicarbonate particles are pulverized and classified by a pharmaceutical ball mill to obtain solid sodium bicarbonate particles with a particle size of 280-320 mesh, and dried until the water content is less than 1.7%. Dissolve the membrane-forming lipid material in 30 mL of a 3:1 chloroform-ethanol mixed solvent; add the drug, N-(β-D-glucopyranose) caprylamide and tartaric acid, and dissolve it by ultrasonication; add solid sodium bicarbonate Particles, react for a certain period of time; the reaction temperature is 55 o C, the reaction time is 90min. The solvent was distilled off under reduced pressure to obtain a solid substance; the solid substance was solidified in a vacuum desiccator for 24 hours to obtain proliposo...

Embodiment 2

[0068] Weigh 60 mg of cefminox sodium as medicine, 420 mg of N-(β-D-glucopyranose) octanamide, 1590 mg of HSPC and 435 mg of cholesterol as film-forming lipid material, 145 mg of tartaric acid and 145 mg of solid sodium bicarbonate particles. The solid sodium bicarbonate particles are pulverized and classified by a pharmaceutical ball mill to obtain solid sodium bicarbonate particles with a particle size of 280-320 mesh, and dried until the water content is less than 1.7%. Dissolve the membrane-forming lipid material in 30 mL of a 3:1 chloroform-ethanol mixed solvent; add the drug, N-(β-D-glucopyranose) caprylamide and tartaric acid, and dissolve it by ultrasonication; add solid sodium bicarbonate Particles, react for a certain time; the reaction temperature is 45 o C, the reaction time is 80min. The solvent was distilled off under reduced pressure to obtain a solid substance; the solid substance was solidified in a vacuum desiccator for 12 hours to obtain proliposomes. The ...

Embodiment 3

[0070] Weigh 120 mg of cefminox sodium as medicine, 600 mg of N-(β-D-glucopyranose) octanamide, 1190 mg of HSPC and 1190 mg of cholesterol as film-forming lipid material and 1260 mg of tartaric acid and 180 mg of solid sodium bicarbonate particles. The solid sodium bicarbonate particles are pulverized and classified by a pharmaceutical ball mill to obtain solid sodium bicarbonate particles with a particle size of 280-320 mesh, and dried until the water content is less than 1.7%. Dissolve the membrane-forming lipid material in 30 mL of a 3:1 chloroform-ethanol mixed solvent; add the drug, N-(β-D-glucopyranose) caprylamide and tartaric acid, and dissolve it by ultrasonication; add solid sodium bicarbonate Particles, react for a certain time; the reaction temperature is 65 o C, the reaction time is 120min. The solvent was distilled off under reduced pressure to obtain a solid substance; the solid substance was solidified in a vacuum desiccator for 48 hours to obtain proliposomes...

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Abstract

The invention discloses a cefminox sodium preparation. The cefminox sodium preparation is prepared from the raw materials: cefminox sodium used as medicine, N-(beta-D-glucopyranose) octanamide and a film-forming lipid material; and the cefminox sodium preparation is further prepared from the raw materials: tartaric acid and solid sodium bicarbonate particles. In addition, the invention further discloses a preparation method and a use method of precursor liposomes. A precursor liposome pharmaceutical preparation is prepared by using solid dispersion, liposome suspension liquid is prepared by combining with an effervescence technology, the stability of the long-term storage of the precursor liposomes can be achieved, morphological consistency of the liposomes can further be maintained better, the particle size distribution is narrow, and the entrapment efficiency is not significantly reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations; relates to a pharmaceutical preparation of cefminox sodium, in particular to a cefminox sodium preparation and a preparation and use method thereof, more particularly to a precursor lipid of cefminox sodium for injection Plastids and methods of making and using them. Background technique [0002] Cefminox sodium is (6R,7S)-7-[(S)-2-[2-amino-2-hydroxyethylmercapto]-acetylamino]-7-methoxy-3-[[(1- Methyl-1H-tetrazol-5-yl)-mercapto]-methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt Heptahydrate, molecular weight 667.66 Daltons; belongs to β-lactam cephalosporins. [0003] Cefminox sodium is a powder for injection developed by Japan Meiji Seika Co., Ltd., and its properties are similar to those of the third-generation cephalosporins. Cefminox sodium has a high affinity to penicillin-binding protein, and binding to it can prevent the synthesis of bacterial cel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/546A61K47/26A61K9/16A61P31/04
CPCA61K9/0019A61K9/127A61K9/1676A61K31/546A61K47/26A61P31/04
Inventor 卢平平王红魏天琪吴卫清李文献吴王平范海峰
Owner 上海欣峰制药有限公司
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