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Capecitabine granule and preparation method thereof

A technology of capecitabine and granules, applied in the field of medicine

Active Publication Date: 2013-10-23
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there are no reports on capecitabine granules in any literature, and the present invention provides a kind of capecitabine granules and a preparation method thereof, which are used to solve the deficiencies in the prior art

Method used

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  • Capecitabine granule and preparation method thereof
  • Capecitabine granule and preparation method thereof
  • Capecitabine granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]The prescription composition of capecitabine granules: the specification is 0.5g (calculated as capecitabine), and the prescription quantity is 1000 bags.

[0044]

[0045] Preparation Process:

[0046] 1) Pass capecitabine, β-cyclodextrin and auxiliary materials through an 80-mesh sieve for later use; take the prescribed amount of hydroxypropyl methylcellulose, add an appropriate amount of water to prepare a 2% hydroxypropyl methylcellulose aqueous solution, and set aside;

[0047] 2) Weigh the cyclodextrin according to the prescription amount to make a saturated aqueous solution at 50°C, then place it in a high-shear wet granulator, start stirring, and the stirring speed is 600rpm / min;

[0048] 3) Weigh capecitabine according to the prescription amount and add it to the above solution, stir at constant temperature for 45 minutes, stop heating and continue stirring to room temperature, stop stirring after 3 hours, spray dry, and obtain cyclodextrin inclusion compound...

Embodiment 2

[0051] The prescription composition of capecitabine granules: the specification is 0.5g (calculated as capecitabine), and the prescription quantity is 1000 bags.

[0052]

[0053] Preparation Process:

[0054] 1) Pass capecitabine, hydroxy-β-cyclodextrin and auxiliary materials through an 80-mesh sieve for later use; take the prescribed amount of hydroxypropyl cellulose, add appropriate amount of water to prepare a 5% aqueous solution of hydroxypropyl cellulose for later use;

[0055] 2) Weigh hydroxy β-cyclodextrin according to the prescription amount to make a saturated aqueous solution at 60°C, then place it in a high-shear wet granulator, start stirring, and the stirring speed is 800rpm / min;

[0056] 3) Weigh capecitabine according to the prescription amount and add it to the above solution, stir at constant temperature for 45 minutes, stop heating and continue stirring to room temperature, stop stirring after 5 hours, spray dry, and obtain cyclodextrin inclusion compou...

Embodiment 3

[0059] The prescription composition of capecitabine granules: the specification is 0.5g (calculated as capecitabine), and the prescription quantity is 1000 bags.

[0060]

[0061] Preparation Process:

[0062] 1) Pass capecitabine, gamma-cyclodextrin and auxiliary materials through an 80-mesh sieve for subsequent use; take the povidone of the prescribed amount, add appropriate amount of water to prepare a 4% aqueous solution of povidone for subsequent use;

[0063] 2) Weigh γ-cyclodextrin according to the prescription amount to make a saturated aqueous solution at 55°C, then place it in a high-shear wet granulator, start stirring, and the stirring speed is 400rpm / min;

[0064] 3) Weigh capecitabine according to the prescription amount and add it to the above solution, stir at constant temperature for 45 minutes, stop heating and continue stirring to room temperature, stop stirring after 4 hours, spray dry, and obtain cyclodextrin inclusion compound;

[0065] 4) Pass the pr...

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Abstract

The invention relates to an oral anti-tumor drug capecitabine granule and a preparation method thereof. The capecitabine granule exists in the form of a cyclodextrin inclusion compound and is prepared from capecitabine serving as a raw material drug and auxiliary materials comprising cyclodextrin, a diluting agent, a disintegrating agent, an adhesive and a flavoring agent by wet granulation. The capecitabine granule disclosed by the invention not only covers the bitterness of a capecitabine drug and enhances the drug compliance of a cancerous person, but also enhances the stability of the capecitabine in gastrointestinal tracts and accelerates the digestion velocity, thereby preventing the peak valley phenomenon of the blood concentration of a drug, outstandingly reducing the adverse reactions of the drug, such as irritation and toxic side effect, on the gastrointestinal tracts due to the stable release of capecitabine in the gastrointestinal tracts, enhancing the drug safety and better taking the anti-tumor effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an antitumor drug capecitabine oral granule and a preparation method thereof. Background technique [0002] As an intravenous chemotherapy drug, fluorouracil antineoplastic drug fluorouracil has been clinically used in the treatment of malignant tumors for more than 40 years, and is still widely used in clinical practice, but its adverse reactions significantly reduce neutrophils or white blood cells limit the use of many patients. And prolonged intravenous infusion can also cause stomatitis, hand-foot syndrome, and other complications related to intravenous catheters, such as infection and venous thrombosis. [0003] Capecitabine is a fluoropyrimidine deoxynucleoside carbamate oral antineoplastic drug developed by Roche. It has no cytotoxicity and can be rapidly and completely absorbed from the gastrointestinal tract after oral administration. The three-step activa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/7068A61K47/40A61P35/00
Inventor 王晶翼郑晓清杨清敏李颖耿伟峰张明会
Owner QILU PHARMA HAINAN
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