Capsule preparation containing tegafur, gimeracil and potassium oxonate

Abstract

The invention refers to a capsule preparation containing tegafur, gimeracil and potassium oxonate. The capsule preparation comprises the following components by weight parts: 20 parts of tegafur, 5-6 parts of gimeracil, 19-20 parts of potassium oxonate, 10-300 parts of lactose, and 0.9-5 parts of sodium dodecyl sulfate. According to the invention, the use level of the surfactant of sodium dodecylsulfate is greatly reduced on the premise of guaranteeing rapid dissolving-out of active components in the preparation, so that the irritation of the capsule preparation to the human gastrointestinaltract is decreased and the medicine compliance of a patient is increased.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a capsule preparation containing tegafur, gimeracil and oteracil potassium. Background technique [0002] Tegafur (FT, FT207) is one of the pyrimidine anticancer drugs. It is the prodrug of 5-fluorouracil (5-FU), and has inhibitory effect on most solid tumors. In the body, it can interfere and block the biosynthesis of DNA, RHA and protein, thereby producing its anticancer effect. Basic medical research and clinical observation have proved that tegafur has less toxic and side effects, higher chemotherapy index, less effect on immunosuppression and related immune organs, and is a safe drug that can be used continuously in clinical practice. This product is absorbed through the gastrointestinal tract after oral administration, and the blood concentration reaches the highest peak within 1-3 hours. The duration is longer than that of intravenous administration, so it ...

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Problems solved by technology

[0005] CN200910127355.6 discloses a capsule preparation of S-1 and its preparation method. This invention improves the stability of S-1, but the solubility of the drug has not been improved. In order to ensure rapid dissolution, a large amount of surfactant has been added , the minimum dosage reaches 10mg / capsule, which is more irritating to the gastrointestinal tract. At the same time, the pellet coating technology is adopted, and the production process in the workshop is complicated

[0006] ZL200410075803.X discloses a prescription and preparation process of S-1 orally disintegrating tablets, which can mask the bad bitter taste of the drug, but the water solubility of the drug has not been improved

[0007] ZL200910266511.7 discloses a S-1-Gio granule, which is solved by making the active ingredient of the drug into a cyclodextrin inclusion compound to improve the dissolution rate and bioavailability of the drug. However, the cyclodextrin inclusion process is relatively complicated. There are many inconveniences in the industrial production of the workshop

[0008] ZL200910211359.2 discloses a S-1 dispersible tablet, gimeracil and oteracil potassium can be released in the stomach prior to tegafur, which can better protect the gastrointestinal tract of oteracil potassium , gimeracil better synergizes with tegafur and improves patient compliance, but the process adopts pellet coating technology, and the workshop production process is complicated

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