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Capecitabine sustained and controlled release oral formulation and preparation method thereof

A technology of capecitabine and controlled-release preparations, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, block delivery, etc., which can solve the problems of large doses of preparations, troublesome, low drug content, etc., and achieve safety Guaranteed, stable blood drug concentration, and improved compliance

Inactive Publication Date: 2009-05-20
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the safety of this material has not yet been evaluated, and the drug content in the prepared microspheres is low, and the dry weight ratio of the drug to the microspheres is 25-50% (the encapsulation efficiency is 78.2-87.2%)
According to this ratio, it is necessary to take about 4g-8g of the preparation per day (calculated according to the conventional dose). The large dosage of the preparation may reduce the patient's compliance, especially for patients who have dysphagia. necessary trouble

Method used

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  • Capecitabine sustained and controlled release oral formulation and preparation method thereof
  • Capecitabine sustained and controlled release oral formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Membrane-controlled sustained-release pellets, the weight percentage ratio is as follows:

[0032] Capecitabine 80%

[0033] Microcrystalline Cellulose 10%

[0034] Sodium Carboxymethyl Cellulose 2%

[0035] Ethylcellulose 8%

[0036] Preparation process: adopt the method known in the pharmaceutical industry, mix the main drug and the filler microcrystalline cellulose, add the aqueous solution prepared by adding the binder carboxymethyl cellulose sodium, prepare the soft material, sieve, granulate, and prepare the drug-containing pellets, and then with ethylcellulose aqueous dispersion ( ) coating liquid for coating.

[0037] The membrane-controlled slow-release pellets can be continuously released for 12 hours under the conditions of 37°C, 900ml degassed distilled water, and 100 revolutions per minute by the basket method. The release profile of this formulation is shown in figure 1 .

Embodiment 2

[0039] The sustained and controlled release tablet of hydrophilic gel matrix material, its weight percentage proportioning is as follows:

[0040] Capecitabine 51%

[0041] Polyvinylpyrrolidone 6%

[0042] Lactose 8%

[0043] Hypromellose 34%

[0044] Magnesium Stearate 1%

[0045] Preparation process: Using a known method in the pharmaceutical industry, uniformly mix the main drug with the binder polyvinylpyrrolidone, the filler lactose and the slow-release material hydroxypropyl methylcellulose, prepare the soft material with absolute ethanol, sieve, and granulate , dried, granulated, added with lubricant magnesium stearate, mixed evenly, and compressed into tablets.

[0046]The sustained and controlled release tablet of the hydrophilic gel skeleton material can be continuously released for 16 hours at 37° C., 900 ml of degassed distilled water, and paddle method at 100 revolutions per minute.

Embodiment 3

[0048] The sustained and controlled release matrix tablet combined with two kinds of wax lipid matrix materials, its weight percentage ratio is as follows:

[0049] Capecitabine 52%

[0050] Carnauba Wax 20%

[0051] Stearic Acid 17%

[0052] Lactose 10%

[0053] Magnesium Stearate 1%

[0054] Preparation process: using a method known in the pharmaceutical industry, the main drug is mixed with the slow-release material carnauba wax and stearic acid, and the filler lactose is uniformly mixed, granulated with water, dried, granulated, and the lubricant stearic acid is added Magnesium is mixed and pressed into tablets.

[0055] The slow-controlled release matrix tablet combined with two kinds of wax lipid matrix materials can release continuously for 24 hours under the condition of 37°C, 900ml degassed distilled water, paddle method and 100 revolutions per minute.

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PUM

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Abstract

The invention discloses a capecitabine oral sustained-release preparation and a preparation method thereof. The oral sustained-release preparation comprises the following components by weight percentage: 1) 50 to 90 percent of capecitabine, or pharmaceutically acceptable salt thereof, or ester derivative thereof, and 2) 10 to 50 percent of pharmaceutically acceptable accessories which comprise 4 to 44 percent of pharmaceutically acceptable sustained-release accessory. The preparation adopts the marketed pharmaceutical accessories, has high content of pharmaceutically active components (the weight percentage is more than 50 percent), and can release for 12 to 24 hours in a sustained mode.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a capecitabine oral sustained-controlled release preparation and a preparation method thereof. Background technique [0002] Cancer is one of the most serious diseases threatening human life. In recent years, with the acceleration of people's life rhythm and the intensification of environmental pollution, the incidence of cancer has shown a rising trend. At present, cancer treatment is mainly based on surgery plus chemotherapy. [0003] Capecitabine is a new type of prodrug of 5-fluorouracil (5-FU) developed by Roche. Its chemical name is: 5-deoxy-5-fluoro-N-[(pentyloxy)carbonyl] - cytidine. Capecitabine itself has no activity, and it plays a role in the body through a three-step enzymatic reaction and finally converted to 5-FU: (1) converted to 5′-deoxy-5-fluorocytidine (5′-fluorocytidine) by intrahepatic carboxylesterase DFCR); (2) converted to deoxyfluridine (5′-...

Claims

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Application Information

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IPC IPC(8): A61K31/7068A61K9/16A61K9/22A61K9/52A61K47/44A61P35/00
Inventor 陶涛柴旭煜
Owner SHANGHAI INST OF PHARMA IND
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