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Mycophenolic acid and its salt enteric-coated preparation and preparation method

A technology of mycophenolate mofetil and enteric-coated preparations, which is applied in anti-inflammatory agents, antiviral agents, and pharmaceutical formulations, and can solve the problems of inconvenient taking and complicated process for patients, and achieve stable drug effect, simple process, and good intestinal The effect of solubility

Inactive Publication Date: 2018-02-02
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a new preparation method of mycophenolic acid or its salt enteric-coated granules, so as to overcome the shortcomings of the enteric-coated preparations prepared by the prior art methods such as inconvenient taking for patients and complicated process.

Method used

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  • Mycophenolic acid and its salt enteric-coated preparation and preparation method
  • Mycophenolic acid and its salt enteric-coated preparation and preparation method
  • Mycophenolic acid and its salt enteric-coated preparation and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 prepares mycolate sodium enteric-coated granules

[0043] (1) Prescription:

[0044]

[0045] A total of 1000 bags were made

[0046] (2) Preparation method:

[0047] 1) Mix sodium mycophenolate mofetil (calculated as mycophenolic acid as 650g), 690g acrylic resin No. Ⅱ, and 460g acrylic resin No. Ⅲ, pulverize with a pulverizer to obtain fine powder, and set aside;

[0048] 2) Put the micropowder in a high-efficiency wet granulator, add 6.5g triacetin, then add an appropriate amount of 95% ethanol, shear and stir, and mix well;

[0049] 3) Add 4225g of microcrystalline cellulose and 325g of croscarmellose sodium to the above-mentioned homogeneously mixed material, after stirring, add 189g of povidone K30 and appropriate amount of water, and continue stirring to make a soft material.

[0050] 4) Put the soft material into the single-screw extruder, extrude it into strips, and then transfer it to the spheronizer for spheronization to obtain wet granules...

Embodiment 2~6

[0052] Examples 2-6: The prescription is shown in Table 1, and the preparation method is the same as that of Example 1, but the raw materials and adjuvants added are shown in the following table.

[0053] Prescription used to prepare enteric-coated granules in table 1 embodiment 1~6

[0054]

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PUM

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Abstract

A preparation method of mycophenolic acid or its salt enteric-coated preparation, which is characterized in that the enteric-coated material is directly mixed with the active ingredient, and a wetting agent suitable for pharmaceutical preparations is added to mix evenly, and then granulated; the enteric-coated material It is Acrylic No. II and / or Acrylic No. III. The invention simplifies the technological process of preparing the enteric preparation and does not need a separate coating process. Experiments have proved that the preparation has better enteric properties than the prior art enteric preparations, and the release of active ingredients is not affected by gastric emptying and food, and has a faster release speed in the intestinal tract. Moreover, the prepared preparation has stable drug effect, is in the form of granules, and is convenient to take.

Description

Technical field: [0001] The invention relates to a preparation method of an enteric-coated preparation containing mycophenolic acid or mycophenolic acid salt and the enteric-coated preparation prepared according to the method. Background technique: [0002] Mycophenolic acid (MPA) or its salt is a drug with various activities such as antitumor, antiviral, immunosuppressive, and anti-inflammatory. In order to exert its medicinal effect and improve bioavailability, most of its preparations are enteric-coated preparations. Enteric-coated preparation is a preparation with enteric properties, that is, the active ingredient in the preparation is not released in the stomach, but is released in the intestinal tract. [0003] For example, in CN97193760.5, Novatis Company prepared mycophenolate mofetil into granules, pellets, tablets, etc., and then used acetic acid phthalic acid, cellulose trimellitate or methacrylic acid as coating materials. , coated with an enteric coating, and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K9/16A61K47/32A61K47/38A61P35/00A61P31/12A61P37/06A61P29/00
Inventor 徐飞虞忠杨春维
Owner CHONGQING HUAPONT PHARMA
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