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A kind of orally disintegrating tablet of dexlansoprazole sodium and preparation method thereof
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A technology of dexlansoprazole sodium and lansoprazole sodium, which is applied to the orally disintegrating tablet of dexlansoprazole sodium and the field of preparation thereof, can solve the problems of poor stability of dexlansoprazole, high production cost, temperature and humidity sensitive issues
Active Publication Date: 2020-07-07
NANJING HERON PHARM CO LTD +1
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[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
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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 descr...
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 a dexlansoprazole sodium orally disintegrating tablet and a preparation method thereof. The dexlansoprazole sodium orally disintegrating tablet is composed of new crystal form A of dexlansoprazole sodium, sodium bicarbonate, enteric-soluble release pellets A, enteric-coated sustained-release pellets B, premixed excipient complexes, and other pharmaceutically acceptable excipients are compressed into tablets, wherein the new crystal form A of dexlansoprazole sodium is 5.9 at the diffraction angle 2θ , There are characteristic diffraction peaks at 7.6, 12.2, 12.7, 16.6, 18.4, 20.5, 25.8, 26.8, and 31.4 degrees; enteric-coated immediate-release pellets A and enteric-coated sustained-release pellets B are all made of dexlansoprazole sodium The new crystal form A is prepared by hot-melt extrusion process of the raw material drug, and is coated with an enteric coating that degrades under different pH conditions. be made of. The orally disintegrating tablet of the present invention releases medicine in a small amount in the stomach, thereby reducing the disadvantages of being irritating to the stomach and being unstable in gastric acid. Subsequent pellets are mainly dissolved and released in the intestinal tract, prolonging the drug effect. The orally disintegrating tablet of the present invention has the advantages of good taste, rapid disintegration, rapid dissolution, convenient administration, improved patient compliance, etc., and has advanced preparation technology, simple, safe and pollution-free operation, and is suitable for large-scale 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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