A kind of capecitabine quick-release pellets and preparation method thereof

A capecitabine, immediate-release technology, applied in the field of medicine, can solve the problems of increased drug concentration, multiple components, uneven mixing, etc., and achieve the effects of reducing irritation, high dissolution rate, and reducing adverse reactions

Active Publication Date: 2015-11-25
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation has many components, and it is prone to uneven mixing, and its price is higher than that of ordinary tablets; in addition, capecitabine pediatric tablets disintegrate rapidly in water before oral administration, and then enter the body after oral administration for direct absorption, which will cause Cause the rapid increase of drug concentration in the body, easily cause more adverse reactions, cause greater harm to the human body, and have certain clinical risks

Method used

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  • A kind of capecitabine quick-release pellets and preparation method thereof
  • A kind of capecitabine quick-release pellets and preparation method thereof
  • A kind of capecitabine quick-release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Prescription 1

[0051]

[0052] (2) Preparation method

[0053] The raw and auxiliary materials are respectively passed through a 100-mesh sieve, and fully mixed evenly; the mixed material is added to 220ml of polyvinylpyrrolidone (K30) to make a soft material; Inner spheronization, the spheronization time is 5min, drying at 55-60°C for 12h, sieving to collect pellets with a particle size of 18-32 mesh to obtain pellets.

Embodiment 2

[0055] (1) Prescription 2

[0056]

[0057] (2) Preparation method

[0058] The raw and auxiliary materials are respectively passed through a 100-mesh sieve, and fully mixed evenly; the mixed material is added to 180ml of hydroxypropyl methylcellulose to make a soft material; then added to the extruder and extruded into strips; the strips are placed in a spheronizer Inner spheronization, the spheronization time is 5min, drying at 55-60°C for 12h, sieving to collect pellets with a particle size of 18-32 mesh to obtain pellets.

Embodiment 3

[0060] (1) Prescription 3

[0061]

[0062] (2) Preparation method

[0063] The raw and auxiliary materials are respectively passed through a 100-mesh sieve, and fully mixed evenly; the mixed material is added to 165ml of hydroxypropyl methylcellulose to make a soft material; then added to the extruder and extruded into strips; the strips are placed in a spheronizer Inner spheronization, the spheronization time is 6 minutes, dried at 55-60°C for 12 hours, and sieved to collect pellets with a particle size of 18-32 mesh to obtain pellets.

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PUM

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Abstract

The present invention relates to a capecitabine immediate-release pellet and a preparation method thereof. The capecitabine immediate-release pellet includes the compositions of capecitabine, an excipient, a disintegrating agent and an adhesive. The particle size of the pellet is 0.1-10 mm. The extrusion granulator technology is used in the present invention to prepare the capecitabine immediate-release pellets and the pellets are directly filled into capsules, thus the production process is greatly simplified. The method is simple and reliable. The capecitabine immediate-release pellets prepared by the present invention are good in reproducibility and high in yield.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a capecitabine quick-release pellet and a preparation method thereof. Background technique [0002] Capecitabine (capecitabine) is an oral fluoropyrimidine nucleoside prodrug with targeting effect obtained by chemically modifying the chemical structure of fluorouracil (FU). Its chemical name is: 5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine (pyrimidine nucleoside), and its structural formula is: [0003] [0004] Capecitabine was developed by Roche with the product name "xeloda". It was approved for marketing in the United States in April 1998, and was subsequently listed in Switzerland and other countries. After oral administration, it passes through the gastrointestinal wall intact, and is catalyzed by liver carboxylesterase to 5'-deoxy-5-fluorocytidine (5'-DFCR), and then catalyzed by cytidine deaminase in liver and tumor cells It is converted into 5'-de...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7068A61K9/20A61P35/00A61P35/04
Inventor 王丽丽王志国崔婧盛荣
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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