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

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...

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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

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