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Dry suspension of sodium dexlansoprazole and preparation method of dry suspension

A kind of technology of dexlansoprazole sodium, lansoprazole sodium, is applied in the dry suspension of dexlansoprazole sodium and preparation field thereof, can solve the poor stability of dexlansoprazole, high production cost, temperature Sensitivity to humidity etc.

Active Publication Date: 2017-05-10
NANJING HERON PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] For the deficiencies in the prior art, for the existing dexlansoprazole poor stability, sensitive to temperature and humidity, it is difficult to operate in the preparation process, the production cost is high, and the defects of its preparation product stability are not high, especially some unsatisfactory products. It is suitable for the defects of the hot-melt extrusion process, such as obvious drug degradation in the hot-melt process, etc. The invention provides a new crystal form A of dexlansoprazole sodium dimethylacetamide solvate and a preparation method thereof. The new crystal form A has better physical and chemical properties, suitable melting point and strong stability. It is very convenient to be made into various pharmaceutical dosage forms, and it is also convenient to be processed by hot-melt extrusion process

Method used

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  • Dry suspension of sodium dexlansoprazole and preparation method of dry suspension
  • Dry suspension of sodium dexlansoprazole and preparation method of dry suspension
  • Dry suspension of sodium dexlansoprazole and preparation method of dry suspension

Examples

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Embodiment 1

[0084] Embodiment 1 Preparation of new crystal form A of dexlansoprazole sodium dimethylacetamide of the present invention

[0085] The new crystal form A of a kind of dexlansoprazole sodium dimethylacetamide solvate provided by the present invention, every mole of this new crystal form A contains 1 mole of dimethylacetamide solvent molecule, structural formula is as follows:

[0086] .

[0087] The new crystal form A of dexlansoprazole sodium according to the present invention has characteristics at diffraction angles 2θ of 5.9, 7.6, 12.2, 12.7, 16.6, 18.4, 20.5, 25.8, 26.8, and 31.4 degrees. Diffraction peaks, where the 2θ value error range is ±0.2, and the spectrum is as attached to the description figure 1 shown.

[0088] The new crystal form A of dexlansoprazole sodium according to the present invention has an endothermic characteristic peak at 132.4±1°C in its DSC spectrum and an exothermic characteristic peak at 204.6±1°C. The spectrum is as attached to the descript...

Embodiment 2

[0092] Example 2 Comparative preparation of crystal form 1

[0093] Refer to Example 5 on page 15 of the specification in PCT patent WO2012095859A1 for preparation. Dissolve 25g of dexlansoprazole in 250mL of absolute ethanol, add 32.5g of sodium isooctanoate, stir for 30min, remove the solvent under reduced pressure, add 250mL of n-heptane to the residue, stir at room temperature for 3h, filter, and dry to obtain a comparative Form 1 is about 18.5g.

Embodiment 3

[0094] Example 3 Comparative preparation of crystal form 2

[0095] Refer to Example 8 on page 16 of the specification in PCT patent WO2012095859A1 for preparation.

[0096] Dissolve 10 g of dexlansuprazole in a mixed solvent of 100 mL of absolute ethanol and 5 mL of water, cool down to -5 °C, add 2.2 g of sodium hydroxide, stir at -5 °C for 30 min, add 80 mL of n-heptane to the reaction solution, Stirring was continued for 30 min, the solid was collected and dried to obtain about 6 g of comparative crystal form 2.

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Abstract

The invention relates to a dry suspension of sodium dexlansoprazole and a preparation method of the dry suspension. The dry suspension is prepared from a new crystal form A of sodium dexlansoprazole, sodium bicarbonate, a solubilizer, gastric-soluble quick-release pellets A, enteric sustained-release pellets B, filler, a suspending agent, a flavoring agent and other pharmaceutically acceptable auxiliary materials, wherein the gastric-soluble quick-release pellets A are prepared by coating quick-release pellet cores A prepared from a raw material, namely, the new crystal form A of sodium dexlansoprazole with gastric-soluble coats, and the enteric sustained-release pellets B are prepared by coating slow-release pellet cores B prepared from a raw material, namely, the new crystal form A of sodium dexlansoprazole with enteric coats; the rest new crystal form A of sodium dexlansoprazole is supplemented by sodium bicarbonate and the solubilizer for micronization pretreatment. The dry suspension is moderately released in the stomach and can quickly relieve excessive gastric acid, stomachache and other symptoms, residual medicines are slowly dissolved and released in intestinal tracts, and the efficacy is prolonged. Meanwhile, the dry suspension has the advantages that the dry suspension tastes good, dissolves out quickly, is convenient to take, can improve patient compliance and the like, the preparation process is advanced, simple to operate, safe, pollution-free and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a dry suspension of dexlansoprazole sodium and a preparation method thereof. Background technique [0002] Dexlansoprazole (Dexlansoprazole, R-(+)-Lansoprazole), the chemical name is (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy Base) pyridin-2-yl] methylsulfinyl) -1H-benzimidazole, its structural formula is as follows, [0003] . [0004] Dexlansoprazole is a new drug for the treatment of esophagitis developed by Japan's Takeda Pharmaceutical Company, which was approved for listing by the U.S. FDA on January 30, 2009. The drug is a single enantiomer of the proton pump inhibitor lansoprazole, used for the treatment of heartburn and varying degrees of erosive esophagitis associated with non-erosive gastroesophageal reflux disease, and has a higher activity than lansoprazole Bioavailability and fewer side effects. [0005] Dexlansoprazole belongs to the p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/32A61K47/02A61K47/28A61K31/4439A61P1/04
CPCA61K9/143A61K9/145A61K9/2846A61K31/4439
Inventor 闵涛曹卫张爱洁马冲陆晔枫叶海周桂梅刘飞
Owner NANJING HERON PHARM CO LTD
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