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A kind of freeze-dried preparation of esomeprazole sodium for injection and preparation method thereof

A technology of esomeprazole sodium and freeze-dried preparations, which is applied in the field of esomeprazole sodium freeze-dried preparations for injection and its preparation, and can solve the stability and safety problems of esomeprazole sodium Problems such as poor stability of esomeprazole sodium and hidden dangers of drug safety for patients have not been properly resolved, and achieved good therapeutic effect, appropriate drug loading and good stability.

Active Publication Date: 2020-12-18
SHANGHAI HANSOH BIOMEDICAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the prior art solves the poor stability of esomeprazole sodium by adding additives such as various lyophilized proppants, metal ion chelating agents and antioxidants; however, the antioxidant sodium bisulfite It is irritating to the skin, eyes, and respiratory tract, and can cause allergic reactions, corneal damage, blindness, and asthma, and bring hidden dangers to the safety of medication for patients
Therefore, the stability and safety issues of esomeprazole sodium after long-term storage are still not properly resolved

Method used

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  • A kind of freeze-dried preparation of esomeprazole sodium for injection and preparation method thereof
  • A kind of freeze-dried preparation of esomeprazole sodium for injection and preparation method thereof
  • A kind of freeze-dried preparation of esomeprazole sodium for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The esomeprazole sodium of 3 parts by weight, the gelatin of 4 parts by weight, the meglumine of 0.05 parts by weight, the L-aspartic acid of 0.15 parts by weight and the hydroxyethyl starch of 0.30 parts by weight are dissolved in 10 volume 8 parts by weight of polylactic acid-glycolic acid (polylactic acid-hydroxy The molar ratio of lactic acid and glycolic acid in acetic acid is 75 / 25, molecular weight 6000) is dissolved in the dichloromethane of 40 parts by volume and mixes evenly, prepares the oil phase organic solution; Dissolves 10 parts by weight of polyvinyl alcohol containing 2.0wt% In 70 parts by volume of water for injection at 80°C; then slowly add esomeprazole sodium aqueous solution dropwise to polylactic acid-glycolic acid oil-phase organic solution, emulsify at 20000r / min high-speed oscillation for about 4~6min, and slowly Added into polyvinyl alcohol aqueous solution, 20000r / min high-speed oscillation emulsification for 4~6min, 600r / min for 2h to evapo...

Embodiment 2

[0059] The esomeprazole sodium of 3 parts by weight, the gelatin of 3 parts by weight, the meglumine of 0.03 parts by weight, the L-aspartic acid of 0.09 parts by weight and the hydroxyethyl starch of 0.18 parts by weight are dissolved in 10 volume Parts of water, dissolved and mixed to prepare esomeprazole sodium aqueous solution; and add an appropriate amount of sodium citrate to adjust the pH of the solution to 11.0-12.0; 5 parts by weight of polylactic acid-glycolic acid (polylactic acid-hydroxy The molar ratio of lactic acid and glycolic acid in acetic acid is 75 / 25, molecular weight 6000) is dissolved in the dichloromethane of 40 parts by volume and mixes evenly, prepares the oil phase organic solution; Dissolves 10 parts by weight of polyvinyl alcohol containing 2.0wt% In 70 parts by volume of water for injection at 80°C; then slowly add esomeprazole sodium aqueous solution dropwise to polylactic acid-glycolic acid oil-phase organic solution, emulsify at 20000r / min high-...

Embodiment 3

[0061] The esomeprazole sodium of 3 parts by weight, the gelatin of 4 parts by weight, the meglumine of 0.05 parts by weight, the L-aspartic acid of 0.10 parts by weight and the xylo-oligosaccharide of 0.35 parts by weight are dissolved in 10 volume 8 parts by weight of polylactic acid-glycolic acid (polylactic acid-hydroxy The molar ratio of lactic acid and glycolic acid in acetic acid is 75 / 25, molecular weight 6000) is dissolved in the dichloromethane of 40 parts by volume and mixes evenly, prepares the oil phase organic solution; Dissolves 10 parts by weight of polyvinyl alcohol containing 2.0wt% In 70 parts by volume of water for injection at 80°C; then slowly add esomeprazole sodium aqueous solution dropwise to polylactic acid-glycolic acid oil-phase organic solution, emulsify at 20000r / min high-speed oscillation for about 4~6min, and slowly Added into polyvinyl alcohol aqueous solution, 20000r / min high-speed oscillation emulsification for 4~6min, 600r / min for 2h to evap...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly provides a stable esmeprazole freeze-dried preparation for injection and a preparation method of the stable esmeprazole freeze-dried preparation. The esomeprazole freeze-dried preparation for injection comprises esomeprazole, hydroxyethyl starch, L-aspartic acid, sodium citrate, gelatin, poly (lactic-co-glycolic acid) and water for injection. The esomeprazole freeze-dried preparation for injection is high in encapsulation efficiency, proper in drug loading capacity, high in stability and capable of effectively controlling the content of impurities I-IV, has a good treatment effect on gastric ulcer and can effectively repair the ulcer area, and effective blood concentration of the medicine can be maintained for a long time.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a stable freeze-dried preparation of esomeprazole sodium for injection and a preparation method thereof. Background technique [0002] Gastroesophageal reflux disease is caused by reflux symptoms or tissue damage such as acid reflux, regurgitation, and heartburn due to the reflux of stomach and duodenal contents into the esophagus. Esomeprazole sodium for injection, its chemical name is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl ]sulfinyl-1H-benzimidazole) sodium (trade name: Nexium® I.V). It was developed by AstraZeneca AB, and its dosage form is a sterile powder for injection with a specification of 40 mg. It is domestically approved as an alternative therapy for gastroesophageal reflux disease when oral therapy is not applicable. [0003] As a sodium salt, esomeprazole sodium has good solubility in water, but it is prone to qua...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/42A61K47/18A61K47/36A61K47/34A61K47/32A61K31/4439A61P1/04
CPCA61K9/0019A61K9/19A61K31/4439A61K47/18A61K47/183A61K47/32A61K47/34A61K47/36A61K47/42A61P1/04
Inventor 张春林袁恒立李巍宗书敏赵娜
Owner SHANGHAI HANSOH BIOMEDICAL