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Orally disintegrating tablet of (R)-Lansoprazole sodium and preparation method thereof

A technology of dexlansoprazole sodium and lansoprazole sodium is applied in the orally disintegrating tablet of dexlansoprazole sodium and its preparation field, which can solve the problem of low stability of preparation products and poor stability of dexlansoprazole , temperature and humidity sensitivity and other issues

Active Publication Date: 2017-05-31
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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  • Orally disintegrating tablet of (R)-Lansoprazole sodium and preparation method thereof
  • Orally disintegrating tablet of (R)-Lansoprazole sodium and preparation method thereof
  • Orally disintegrating tablet of (R)-Lansoprazole sodium and preparation method thereof

Examples

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Embodiment 1

[0085] Embodiment 1 Preparation of new crystal form A of dexlansoprazole sodium dimethylacetamide of the present invention

[0086] 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:

[0087] .

[0088] 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.

[0089] The new crystal form A of dexlansoprazole sodium according to the present invention has a DSC spectrum with an endothermic characteristic peak at 132.4±1°C and an exothermic characteristic peak at 204.6±1°C; and the spectrum is as attached to the descri...

Embodiment 2

[0093] Example 2 Comparative preparation of crystal form 1

[0094] 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

[0095] Example 3 Comparative preparation of crystal form 2

[0096] Refer to Example 8 on page 16 of the specification in PCT patent WO2012095859A1 for preparation.

[0097] 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 an orally disintegrating tablet of (R)-Lansoprazole sodium and a preparation method thereof. The orally disintegrating tablet of (R)-Lansoprazole sodium is prepared by the new crystal form A of the (R)-Lansoprazole sodium, sodium bicarbonate, enteric quick-release pellets A, enteric quick-release pellets B, a premixing accessory compound, and other pharmaceutically acceptable accessory tablet, wherein the new crystal form A of the (R)-Lansoprazole sodium has the feature diffraction peak in the position where the diffraction angle 2Theta is 5.9, 7.6, 12.2, 12.7, 16.6, 18.4, 20.5, 25.8, 26.8, and 31.4 degrees; the enteric quick-release pellets A and the enteric quick-release pellets B are prepared by using the new crystal form A of the (R)-Lansoprazole sodium as the bulk pharmaceutical chemicals through the hot-melting extrusion process, and coated by the enteric coating degraded under different pH conditions, and the premixing accessory compound is prepared by the suitable accessory of the orally disintegrating tablet through the hot-melting extrusion process. The orally disintegrating tablet is capable of releasing a small amount of drugs in the stomach, the irritation to the stomach is reduced and the defect of the instability in the gastric acid is overcome. The follow-up pellets are mainly dissolved and released in the intestinal tract, and the pharmacological function is prolonged. The orally disintegrating tablet has the good taste, the disintegration is rapid, the digestion is quick, the patient adaptability is improved, the preparation process is advanced, and the operation is simple, safe and pollution-free. The orally disintegrating tablet is suitable for the industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an orally disintegrating tablet 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 b...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4439A61K47/32A61K47/38A61K47/02A61K47/18A61P1/04A61P31/04C07D401/12
CPCA61K9/0002A61K9/2009A61K9/2054A61K9/2081A61K9/5015A61K9/5026A61K31/4439C07B2200/07C07B2200/13C07D401/12
Inventor 闵涛包玉胜刘婷婷芮清清叶海晁阳周桂梅刘飞
Owner NANJING HERON PHARM CO LTD
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