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A warfarin sodium orally disintegrating tablet capable of individual administration prepared by 3D printing and its preparation method

A technology of orally disintegrating tablets and warfarin sodium, applied in the field of preparation of the warfarin sodium orally disintegrating tablets, can solve problems such as narrow therapeutic window, large individual differences in curative effect, and failure to satisfy patients, and achieve drug release speed Fast, low drug side effects, and improved compliance

Active Publication Date: 2020-04-14
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Warfarin sodium is currently an important clinical oral anticoagulant drug, which is widely used in the treatment of deep vein thrombosis, pulmonary embolism, atrial fibrillation, etc., and its prescription volume can reach 0.5% to 1.5% of the population. There are large individual differences in the curative effect of Lin, and the clinical dosage can vary by about 20 times, and the blood concentration is easily affected by other factors. The therapeutic window is very narrow, and even a small dose-response change may lead to thrombosis or bleeding, and most of the patients are elderly. , difficult to take medicine, poor compliance
The existing ordinary tablet specifications on the market are only 2.5mg, 3.0mg and 5.0mg. Most patients need to cut the tablet into smaller doses before taking the medicine, and the disintegration time is as long as 3 minutes, which can no longer meet the needs of patients

Method used

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  • A warfarin sodium orally disintegrating tablet capable of individual administration prepared by 3D printing and its preparation method
  • A warfarin sodium orally disintegrating tablet capable of individual administration prepared by 3D printing and its preparation method
  • A warfarin sodium orally disintegrating tablet capable of individual administration prepared by 3D printing and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (Target dose: 2.50mg)

[0030] The formula is as follows:

[0031]

[0032] 3D printing parameters are as follows:

[0033]

[0034] The preparation method is as follows:

[0035] (1) According to the pre-set parameters, use CAD and other software to model, and convert it into an stl format file and import it into the LTY software control system of the 3D printer.

[0036] (2) Mix warfarin sodium, sucrose and micropowdered silica gel evenly, and put it into the powder box of the 3D printing rapid prototyping machine as a medicine powder.

[0037] (3) Put 50% ethanol solution into the cartridge.

[0038] (4) The control system outputs instructions to control the 3D printing rapid prototyping machine to print warfarin sodium orally disintegrating tablets: the powder spreading device first spreads a layer of powder with a thickness of 0.20mm on the powder bed, and then prints the nozzle in the direction of the X-Y axis. Move and spray the adhesive in a fixed area...

Embodiment 2

[0045] (Target dose: 3.00mg)

[0046] The preparation method and raw material ratio are the same as in Example 1, except that the number of printing layers is 18 and the thickness is 3.60mm. The quality inspection of warfarin sodium orally disintegrating tablets is as follows:

[0047] The content of warfarin sodium in the warfarin sodium orally disintegrating tablets determined by high performance liquid chromatography (HPLC) was 2.85 ± 0.08 mg / tablet.

[0048] Disintegration time limit test of warfarin sodium orally disintegrating tablets:

[0049] According to the "Chinese Pharmacopoeia" 2015 edition disintegration time determination method, the disintegration time limit of warfarin sodium orally disintegrating tablets was determined. The disintegration time is 8±2s, meeting the requirements of the 2015 edition of the Chinese Pharmacopoeia.

Embodiment 3

[0051] (Target dose: 5.00mg)

[0052] The preparation method and raw material ratio are the same as in Example 1, except that the number of printing layers is 30 and the thickness is 6.00mm. The quality inspection of warfarin sodium orally disintegrating tablets is as follows:

[0053] The content of warfarin sodium in the warfarin sodium orally disintegrating tablets determined by high performance liquid chromatography (HPLC) was 5.37 ± 0.34 mg / tablet.

[0054] Disintegration time limit test of warfarin sodium orally disintegrating tablets:

[0055] According to the "Chinese Pharmacopoeia" 2015 edition disintegration time determination method, the disintegration time limit of warfarin sodium orally disintegrating tablets was determined. The disintegration time is 10±2s, meeting the requirements of the 2015 edition of the Chinese Pharmacopoeia.

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Abstract

The invention discloses an individually taken warfarin sodium orally disintegrating tablet prepared in the manner of 3D printing. The orally disintegrating tablet is mainly prepared from the following materials by weight percent based on a 3D printing technique: 1-10% of warfarin sodium, 90-99% of filler, 0.1-1.0% of silica gel powder and 0-2% of corrigent, wherein the sum of the weight percent of all the components is equal to 100%. The invention also discloses a preparation method for the warfarin sodium orally disintegrating tablet. The warfarin sodium orally disintegrating tablet provided by the invention has high drug release speed. Under the condition of same prescription and technological parameters, the content of the tablet is confirmed on the basis of the printing layer number considered as variable, i.e., the tablet dosage can be individually designed in the manner of changing the printing layer number, the dosage suitable for the patient can be custom-made according to the individual difference of the patient and the individual drug dosage and accurate therapy can be realized, so that the number of the tablets taken by the patient can be reduced or the step of cutting the tablet by the pharmacist can be reduced, the pharmaceutical preparation can exert the maximum curative effect and the toxic side effect of the drug can be reduced to the minimum.

Description

technical field [0001] The invention relates to an orally disintegrating tablet of warfarin sodium, in particular to an orally disintegrating tablet of warfarin sodium prepared by 3D printing and capable of individual administration. The invention also relates to a preparation method of the warfarin sodium orally disintegrating tablet. Background technique [0002] Three-dimensional printing technology (three dimension printing, 3DP) is a rapid prototyping technology, which is based on a digital model, using powdered metal or plastic and other bondable materials to construct objects by layer-by-layer printing. It was first proposed by Sachs of the Massachusetts Institute of Technology in the United States. According to the concept of "printing layer by layer, layer by layer", under the control of the computer, according to the CAD model or CT data of the object, it can be quickly and accurately manufactured through the accumulation of materials. An object with a special sha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K31/37A61K47/04A61P7/02A61P11/00A61P9/04B29C64/165B33Y10/00
CPCA61K9/0056A61K9/2009A61K9/2072A61K9/2086A61K9/2095A61K31/37B33Y10/00
Inventor 黄思玉陈燕忠吕竹芬
Owner GUANGDONG PHARMA UNIV
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