A kind of sustained-release capsule of dexlansoprazole sodium and preparation method thereof
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A technology of dexlansoprazole sodium and lansoprazole sodium, which is applied to the sustained-release capsule of dexlansoprazole sodium and the field of preparation thereof, can solve the problems of difficult operation, high production cost and stable dexlansoprazole Sexual problems, etc.
Active Publication Date: 2019-12-06
NANJING HERON PHARM CO LTD +1
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[0012] In view of the deficiencies in the prior art, the existing dexlansoprazole has poor stability, is sensitive to temperature and humidity, and is difficult to operate in the preparation process, the production cost is high, and the preparation product stability is not high. Due to the defects of the hot-melt extrusion process, such as obvious drug degradation in the hot-melt process, the invention provides a new crystal form A of dexlansoprazole sodium dimethylacetamide solvate and a preparation method thereof. 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 is also convenient to be processed by hot-melt extrusion technology.
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Embodiment 1
[0083] Embodiment 1 Preparation of new crystal form A of dexlansoprazole sodium dimethylacetamide of the present invention
[0084] 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 molecules, the structural formula is as follows,
[0085] .
[0086] The new crystal form A of dexlansoprazole sodium according to the present invention has characteristic diffraction 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. peak, where the error range of 2θ value is ±0.2, the spectrum is as attached to the instruction manual figure 1 shown.
[0087] 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...
Embodiment 2
[0091] Example 2 Comparative preparation of crystal form 1
[0092] 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
[0093] Example 3 Comparative preparation of crystal form 2
[0094] Refer to Example 8 on page 16 of the specification in PCT patent WO2012095859A1 for preparation.
[0095] 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 belongs to the technical field of pharmaceutical preparations, and in particular relates to a dexlansoprazole sodium enteric-coated sustained-release capsule prepared by a hot-melt extrusion process. The raw material for preparing the capsule is the new crystal form A of dexlansoprazole, and its PXRD pattern has diffraction absorption 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. peak. The sustained-release capsules comprise enteric-coated quick-release pellets A and enteric-coated sustained-release pellets B. According to the content of dexlansoprazole, the main drug content ratio of the two pellets is about 1:3, and the two are wrapped together The enteric coating with different pH value responses achieves double drug release and double controlled release. The shell of the dexlansoprazole sustained-release capsule of the present invention prevents the dexlansoprazole from being destroyed in gastric acid, and releases the dexlansoprazole in a fixed position in the intestinal tract, so as to achieve rapid onset of effect and improve bioavailability. The preparation process of the capsule avoids the use of ethanol solvent coating, eliminates the ethanol residue in the finished product, and has advanced preparation process, simple, safe and pollution-free operation, and is suitable for industrialized large-scale production.
Description
technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a slow-release capsule 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 t...
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Application Information
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