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Solid preparation comprising pantoprazole sodium submicron emulsion particles

A technology of pantoprazole sodium and solid preparation, applied in the field of medicine, can solve the problem that the stability of pantoprazole sodium is not significantly improved, the active ingredient pantoprazole sodium is easily discolored, and the pantoprazole sodium is enteric-coated. It can solve problems such as sticking and punching, and achieve the effect of solving heat discoloration, reducing drug side effects and reducing drug toxicity.

Inactive Publication Date: 2011-09-28
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Patent literature CN1546025A discloses a pantoprazole sodium enteric-coated pellet, including a core composed of pantoprazole sodium and one or more pharmaceutically acceptable excipients and acrylic resin substances and other excipients. Enteric-coated layer composed of agent, the main problem it solves is that the existing pantoprazole sodium easily loses its enteric properties when taken and has a local concentration too high when it is released in the human intestine; patent document CN1883460A also discloses a Pantoprazole sodium enteric-coated pellets, comprising a ball core containing pantoprazole sodium and an enteric coating containing cellulose material, which solves the problem of low stability of pellets in the prior art; patent document CN101461809A discloses a kind of pantoprazole sodium enteric-coated tablet and preparation method thereof, is made after pantoprazole sodium plain tablet wraps isolation layer, enteric-coated layer, and plain tablet contains 0.5-5% silicon dioxide, 0.5-5% talcum powder, the main problem to be solved in this application is the technical problem of sticking and punching when pantoprazole sodium enteric-coated tablets are pressed
Above-mentioned several patents prepare pantoprazole sodium micropill and tablet and comprise enteric-coated tablet by different components and method, but these prior art all are not specific to the stability problem of pantoprazole sodium, and in above-mentioned In the patent, the coating of the isolation layer and the enteric layer needs to be heated at high temperature, which causes the active ingredient pantoprazole sodium to easily change color, resulting in unqualified products, and thus does not significantly improve the stability of pantoprazole sodium

Method used

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  • Solid preparation comprising pantoprazole sodium submicron emulsion particles
  • Solid preparation comprising pantoprazole sodium submicron emulsion particles
  • Solid preparation comprising pantoprazole sodium submicron emulsion particles

Examples

Experimental program
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Embodiment 1

[0026] The preparation of embodiment 1 pantoprazole sodium submicron emulsion particle

[0027] Add 100g of egg yolk lecithin and 60g of poloxamer 188 into 2000ml of water for injection, then add 40g of pantoprazole sodium and mix evenly, heat and stir in a water bath at 80°C for 30min until it melts, use a tissue masher to shear and stir for 20min, and the speed 10000r / min, to get the first emulsion, and then emulsified 5 times through a high-pressure homogenizer cycle to obtain an emulsion, then freeze-dried in a large plate, and pulverized to obtain 184.4g of submicron emulsion particles of pantoprazole sodium, with a yield of 92.2%.

Embodiment 2

[0028] The preparation of embodiment 2 pantoprazole sodium submicron emulsion particles

[0029] Add 240g of egg yolk lecithin and 160g of poloxamer 188 into 4000ml of water for injection, then add 80g of pantoprazole sodium and mix evenly, heat and stir in a water bath at 70°C for 50min until it melts, use a tissue masher to shear and stir for 10min, the speed 15000r / min, to obtain the primary emulsion, and then circulate emulsified by a high-pressure homogenizer for 6 times to obtain an emulsion, and then spray dry to obtain 452.6g of submicron emulsion particles of pantoprazole sodium, with a yield of 94.3%.

Embodiment 3

[0030]The preparation of embodiment 3 pantoprazole sodium enteric-coated tablets

[0031] With the pantoprazole sodium submicron emulsion particle (containing pantoprazole sodium 20g) prepared by 100g embodiment 1, 80g lactose, 50g mannitol, 10g crospovidone, 10g sodium starch glycolate, 10g anhydrous carbonic acid Sodium is passed through 80 mesh sieve, then mixed evenly, add 5% povidone K30 80% ethanol solution 200ml to make soft material, granulate with 24 mesh sieve, dry at 60°C, granulate with 20 mesh sieve, then add 3.6g stearic acid The magnesium was mixed evenly, and compressed into tablets, 0.265g / tablet, to obtain 946 plain tablets, with a yield of 94.6%.

[0032] Prepare 5% (w / v) povidone K30 ethanol solution containing 20% ​​(w / v) talcum powder as an isolation layer to coat the plain tablet, increase in weight by 17.6%, and dry; then use 5% of Ruitai The 80% ethanol solution of ES-H is used as the enteric coating layer, coated with an enteric coating, and the weig...

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PUM

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Abstract

The invention relates to pantoprazole sodium submicron emulsion particles and solid preparation such as an enteric tablet and an enteric capsule comprising the same. The pantoprazole sodium submicron emulsion particles comprise pantoprazole sodium, egg yolk lecithin and poloxamer 188.

Description

technical field [0001] The present invention relates to a kind of pantoprazole sodium submicroemulsion particle and the submicroemulsion solid preparation comprising the submicroemulsion particle, in particular to a kind of enteric-coated tablet and enteric-coated tablet containing the pantoprazole sodium submicroemulsion particle Dissolving capsules belong to the technical field of medicines. Background technique [0002] Pantoprazole sodium, its chemical name is: 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)-methyl]-sulfinyl-1H-benzo Imidazole sodium salt monohydrate, molecular formula: C 16 h 14 f 2 N 3 NaO 4 S·H 2 O, molecular weight: 423.38, structural formula: [0003] [0004] Pantoprazole sodium acts specifically on the parietal cells of the gastric mucosa to reduce H in the parietal cells + -K + -ATPase activity, thereby inhibiting the secretion of gastric acid. Compared with omeprazole, pantoprazole sodium has a weaker inhibitory effect on cytochrome ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/32A61K9/36A61K9/48A61K31/4439A61K47/34A61K47/24A61K47/38A61P1/04A61K47/10
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD