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Oral disintegrating preparation containing tegafur, gimeracil and oteracil potassium

A technology of oral disintegration and tegafur, which is applied in the direction of pill delivery, active ingredients of heterocyclic compounds, drug combination, etc., can solve the problems of industrial production inconvenience, complex production process, poor water solubility, etc., to improve medication compliance, The preparation process is simple and the effect of reducing irritation

Active Publication Date: 2014-11-19
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] CN101574326A discloses a capsule preparation of S-1 and its preparation method. This invention improves the stability of S-1, but the dissolution rate 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.
[0005] CN1660105A discloses a prescription and preparation process of S-1 orally disintegrating tablets, which can cover up the bad bitter taste of the medicine, but the water solubility of the medicine has not been improved
CN101843621A discloses a kind of tigio 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, and the workshop industry Chemical production has many inconveniences
[0008] Tegafur is an alkaline drug with poor water solubility and shows instability in acidic solution

Method used

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  • Oral disintegrating preparation containing tegafur, gimeracil and oteracil potassium
  • Oral disintegrating preparation containing tegafur, gimeracil and oteracil potassium
  • Oral disintegrating preparation containing tegafur, gimeracil and oteracil potassium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] prescription:

[0025]

[0026]

[0027] Preparation:

[0028] Tegafur, gemostat and oteracil potassium pass through a 100-mesh sieve, carbohydrates, disintegrants and flavoring agents pass through a 80-mesh sieve, mix well, add appropriate amount of distilled water, granulate and dry, and granulate with a 20-mesh sieve , and then add the prescribed amount of lubricant, mix well, and press into tablets.

Embodiment 2

[0030] prescription:

[0031]

[0032] Preparation:

[0033] Tegafur, gemostat and oteracil potassium pass through a 100-mesh sieve, carbohydrates, disintegrants and flavoring agents pass through a 80-mesh sieve, mix well, add appropriate amount of distilled water, granulate and dry, and granulate with a 20-mesh sieve , and then add the prescribed amount of lubricant, mix well, and press into tablets.

Embodiment 3

[0035] prescription:

[0036]

[0037]

[0038] Preparation:

[0039] Tegafur, gemostat and oteracil potassium pass through a 100-mesh sieve, carbohydrates, disintegrants and flavoring agents pass through a 80-mesh sieve, mix well, add appropriate amount of distilled water, granulate and dry, and granulate with a 20-mesh sieve , and then add the prescribed amount of lubricant, mix well, and press into tablets.

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PUM

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Abstract

The invention relates to an oral disintegrating preparation containing tegafur, gimeracil and oteracil potassium. The oral disintegrating preparation also includes carbohydrates and a disintegrating agent. Active ingredients in the oral disintegrating preparation are high in dissolution rate so that a drug is ensured to work quickly. More importantly, the oral disintegrating preparation is good in stability, is free of surfactants, is reduced in irritation to human gastrointestinal tract and improves patient compliance. The oral disintegrating preparation is simple in preparation technology and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an orally disintegrating preparation containing tegafur, gimester 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, RNA 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 impact 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 in...

Claims

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Application Information

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IPC IPC(8): A61K31/53A61K9/20A61P35/00
Inventor 张贵民
Owner SHANDONG NEWTIME PHARMA
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