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Injection esomeprazole composition and preparation method thereof

A technology of esomeprazole and esomeprazole sodium is applied in the field of esomeprazole composition for injection and its preparation, which can solve the problems such as not having dual controlled release function, achieve good stability and improve Therapeutic index, the effect of improving quality

Active Publication Date: 2013-07-31
苏州特瑞药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the injection formulation it provides is a liposomal formulation and does not have dual controlled release functions

Method used

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  • Injection esomeprazole composition and preparation method thereof
  • Injection esomeprazole composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] This example provides a kind of esomeprazole sodium composition for injection, it is prepared by following steps:

[0026] (1): Dissolve 3g of esomeprazole sodium and 15g of polylactic-co-glycolic acid copolymer (number average molecular weight 5000) in 100ml of dichloromethane as the oil phase; then add 1.5wt% polyvinyl alcohol (PVA) ( 35g of an aqueous solution with a viscosity of 30~45mPa.s at 20°C is the water phase. The oil phase was added to the water phase stirred at a speed of 5000 rpm, and stirred for 15 minutes to form an O / W emulsion droplet type emulsion. Then control the temperature of the emulsion to below 20° C. and reduce the rotational speed to 500 rpm, stir for 3 hours to volatilize the solvent and solidify the formed microspheres, wash with water and vacuum-dry at room temperature to obtain white powdery microspheres. And sterilized by cobalt-60 (dose of 10KGY) radiation to obtain slow-release microspheres with an average particle size of about 5...

Embodiment 2

[0029] This example provides a kind of esomeprazole sodium composition for injection, it is prepared by following steps:

[0030] (1): Dissolve 3g of esomeprazole sodium and 15g of poly(lactic-co-glycolic acid) copolymer (number average molecular weight 10,000) in 100ml of dichloromethane as the oil phase; then add 2.0wt% polyvinyl alcohol (PVA) ( 40g of an aqueous solution with a viscosity of 40~50mPa.s at 20°C is the water phase. The oil phase was added to the water phase stirred at a speed of 5000 rpm, and stirred for 15 minutes to form an O / W emulsion droplet type emulsion. Then control the temperature of the emulsion to below 20° C. and reduce the rotational speed to 500 rpm, stir for 3 hours to volatilize the solvent and solidify the formed microspheres, wash with water and vacuum-dry at room temperature to obtain white powdery microspheres. And sterilized by cobalt-60 (dose 10KGY) radiation to obtain slow-release microspheres with an average particle size of about ...

Embodiment 3

[0033] This example provides a kind of esomeprazole sodium composition for injection, it is prepared by following steps:

[0034] (1): Dissolve 3g of esomeprazole sodium and 20g of poly(lactic-co-glycolic acid) copolymer (number average molecular weight 10,000) in 100ml of dichloromethane as the oil phase; then add 2.0wt% polyvinyl alcohol (PVA) ( 50g of an aqueous solution with a viscosity of 40~50mPa.s at 20°C is the water phase. The oil phase was added to the water phase stirred at a speed of 5000 rpm, and stirred for 15 minutes to form an O / W emulsion droplet type emulsion. Then control the temperature of the emulsion to below 20° C. and reduce the rotational speed to 500 rpm, stir for 3 hours to volatilize the solvent and solidify the formed microspheres, wash with water and vacuum-dry at room temperature to obtain white powdery microspheres. And sterilized by cobalt-60 (dose of 10KGY) radiation to obtain slow-release microspheres with an average particle size of abo...

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Abstract

The invention relates to an injection esomeprazole composition. The injection esomeprazole composition comprises an active component and assisting agents, the active component is esomeprazole or esomeprazole sodium or an esomeprazole crystalline hydrate, the injection esomeprazole composition also comprises slow release microspheres containing the active component, the slow release microspheres comprise 10-30wt% of the active component, 60-80wt% of a biodegradable carrier material and 0.2-10wt% of a stabilizer, and the assisting agents comprise an excipient and a pH adjusting agent; and the injection esomeprazole composition is obtained through lyophilizing the active component, the assisting agents, the slow release microspheres and an aqueous solution having a pH value in a range of 11.0-12.0. The injection esomeprazole composition is a dual-controlled-release proton pump inhibitor releasing drugs two times, increases the treatment indexes of the drugs, and raises the qualities of preparation products.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to an esomeprazole composition for injection and a preparation method thereof. Background technique [0002] Esomeprazole is the S-isomer of omeprazole, which reduces gastric acid secretion through a specific targeting mechanism and is a specific inhibitor of proton pumps in parietal cells. The R-isomer and S-isomer of omeprazole have similar pharmacodynamic properties. Esomeprazole is a weakly basic drug that concentrates and converts into an active form in the high-acid environment of the acid-secreting microtubules of the parietal cells, thereby inhibiting the H+ / K+-ATPase (proton pump) at this site, and affecting the basic Both gastric acid secretion and stimulated gastric acid secretion are inhibited. [0003] Patent document CN 102327236A discloses a liposome injection of esomeprazole sodium, which includes the following components: (1) active ingredient: esomep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/16A61K31/4439A61P1/04
Inventor 宋玉玲季建祥王浩
Owner 苏州特瑞药业股份有限公司
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