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TS-1 granules and preparation method thereof

A technology of granules and Gio, applied in the field of medicine, can solve problems such as the stability and water solubility of drugs are not improved, the water solubility of drugs is not improved, and the dissolution rate of Sigiol is affected, so as to improve the bioavailability and improve the Water solubility, the effect of maintaining drug concentration

Active Publication Date: 2010-09-29
鲁南新时代生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 water solubility of the drug has not been improved, which affects the dissolution rate of S-1 in the stomach , so that its bioavailability is limited, thereby affecting the efficacy
At the same time, for traditional oral administration capsules, a large number of patients, especially the elderly and children, have poor compliance with swallowing difficulties.
[0006] CN200410075803.X invented a prescription and preparation process of S-1 orally disintegrating tablets, which can mask the bad bitterness of the drug, but the stability and water solubility of the drug have not been improved

Method used

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  • TS-1 granules and preparation method thereof
  • TS-1 granules and preparation method thereof
  • TS-1 granules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]

[0042] Preparation Process:

[0043] 1) Dry tegafur, gimeracil, oteracil potassium, β-cyclodextrin and other excipients at 40-60°C for 4 hours, pass through a 100-mesh sieve for later use;

[0044] 2) Weigh three parts of β-cyclodextrin according to the prescription amount to prepare saturated aqueous solutions at 45°C, respectively, and then place them in adjustable high-speed mixers, start stirring at a speed of 1000r / min.

[0045] 3) Tegafur, gimeracil and oteracil potassium that take prescription quantity are dissolved in a small amount of 30% acetonitrile aqueous solution respectively, then the solution is slowly added dropwise in the above-mentioned corresponding saturated cyclodextrin aqueous solution, the dropping speed 2ml / min, stirring at constant temperature for 1 hour. Stop heating and continue stirring to room temperature, stop stirring after 4 hours, and spray dry to obtain cyclodextrin inclusion compound.

[0046] (4) Pass the prepared cyclodextrin...

Embodiment 2

[0048]

[0049] Preparation Process:

[0050] 1) Dry tegafur, gimeracil, oteracil potassium, β-cyclodextrin and other excipients at 40-60°C for 4 hours, pass through a 100-mesh sieve for later use;

[0051] 2) Three parts of β-cyclodextrin were weighed according to the prescription amount to make saturated aqueous solutions at 60°C respectively, and then placed in adjustable high-speed mixers respectively, and the stirring was started at a speed of 2000r / min.

[0052] 3) Tegafur, gimeracil and oteracil potassium of prescription quantity are dissolved in a small amount of 30% acetonitrile aqueous solution respectively, then the solution is slowly added dropwise in the above-mentioned corresponding saturated cyclodextrin aqueous solution, and the rate of addition is 3ml / min, stirring at constant temperature for 45min. Stop heating and continue stirring to room temperature, stop stirring after 3.5 hours, and spray dry to obtain β-cyclodextrin inclusion compound.

[0053] 4) ...

Embodiment 3

[0055]

[0056] Preparation Process:

[0057] 1) Dry tegafur, gimeracil, oteracil potassium, α-cyclodextrin and other excipients at 40-60°C for 4 hours, pass through a 100-mesh sieve for later use;

[0058] 2) Weigh three parts of α-cyclodextrin according to the prescription, add appropriate amount of water, grind them to a paste, then pour them into the colloid mill respectively, and turn on the machine.

[0059] 3) Dissolve the prescribed amount of tegafur, gimeracil and oteracil potassium in a small amount of 30% acetonitrile aqueous solution, and then slowly and continuously add the solution dropwise to the above-mentioned corresponding pasty α-cyclodextrin, and grind for 30 minutes , spray-dried to prepare α-cyclodextrin inclusion compound.

[0060] 4) Pass the obtained α-cyclodextrin inclusion compound through a 100-mesh sieve, and then mix it with the remaining auxiliary materials evenly, then use the ethanol solution of hydroxypropyl cellulose to make a soft materi...

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Abstract

The invention belongs to the technical field of medicaments, and relates to TS-1 granules for treating advanced gastric cancer and a preparation method thereof. The method comprises the following steps of: preparing active medicaments tegafur, gimeracil and potassium oxonate into a cyclodextrin inclusion compound; and sieving the inclusion compound, uniformly mixing the sieved inclusion compound and pharmaceutically acceptable auxiliary materials and performing wet granulation or dry granulation to prepare the granules. The granules have the advantages of increasing the water solubility and stability of the medicaments, covering the bitter taste of the tegafur, prolonging the action time, improving the medication compliance of patients with cancer, greatly improving the bioavailability of the medicaments and reducing the toxic or side effect of the medicaments.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a granule of S-1, a drug for treating advanced gastric cancer, and a preparation method thereof. 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 ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/53A61K31/513A61K31/4412A61P35/00A61K9/16A61K47/48A61K47/69
Inventor 赵志全张庆华郝贵周
Owner 鲁南新时代生物技术有限公司
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