A kind of dry suspension of dexlansoprazole sodium and preparation method thereof
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A kind of technology of dexlansoprazole sodium, lansoprazole sodium, is applied in the dry suspension of dexlansoprazole sodium and its preparation field, can solve difficult operation, preparation product stability is not high, dexlansoprazole Soprazole has poor stability and other problems
Active Publication Date: 2019-08-06
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
[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 a characteristic endothermic 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 descripti...
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 dexlansoprazole sodium and a preparation method thereof. The dry suspension comprises the new crystal form A of dexlansoprazole sodium, sodium bicarbonate, a solubilizer, and gastric dissolution for immediate release Pellets A, enteric-coated sustained-release pellets B, fillers, suspending agents, flavoring agents and other pharmaceutically acceptable excipients. Among them, the stomach-soluble quick-release pellet A is obtained by preparing the quick-release pellet core A with the new crystal form A of dexlansoprazole sodium as the raw material, and then wrapping it with a stomach-soluble coating. Enteric-coated sustained-release pellets B use the new crystal form A of dexlansoprazole sodium as the raw material to prepare sustained-release pellet core B, and then enteric-coated. The new crystal form A of the remaining dexlansoprazole sodium is supplemented with sodium bicarbonate, and the solubilizer is micronized in advance. The dry suspension of the invention is moderately released in the stomach, can quickly relieve symptoms such as hyperacidity, stomach pain, etc., and the remaining medicine is slowly dissolved and released in the intestinal tract to prolong the drug effect. At the same time, the dry suspension of the present invention has the advantages of good taste, rapid dissolution, convenient administration, improved patient compliance, etc., and has advanced preparation technology, simple, safe and pollution-free operation, and can be used in industrialized large-scale 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 pr...
Claims
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