Mycophenolate mofetil capsule and preparation method thereof

A technology for mycophenolate mofetil and capsules, which is applied in the field of mycophenolate mofetil and its preparation, can solve problems such as bad smell, and achieve the effects of good fluidity, rapid dissolution and simple process

Pending Publication Date: 2020-07-28
JIANGSU SIMCERE PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Capsules are one of the common dosage forms. Compared with tablets or dispersions, they have the advantages of fast absorption, high bioavailability, impr

Method used

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  • Mycophenolate mofetil capsule and preparation method thereof
  • Mycophenolate mofetil capsule and preparation method thereof
  • Mycophenolate mofetil capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Formula: mycophenolate mofetil 750g, pregelatinized starch 89.28g, croscarmellose sodium 35.7g, povidone K-90 17.85g, magnesium stearate 13.5g

[0036] Preparation Process:

[0037] a. According to the dosage of 3000 capsules, take 750g of mycophenolate mofetil, 89.28g of pregelatinized starch, 35.7g of croscarmellose sodium, 17.85g of povidone K-90, 13.5g of magnesium stearate g, pass through a 40 mesh sieve respectively for subsequent use;

[0038] b. Mix croscarmellose sodium and povidone K-90 for 3 minutes, then add pregelatinized starch and mix for 3 minutes, then add one-fifth of the raw materials and mix for 5 minutes; then add the remaining prescription amount of raw materials Mix for 10 min.

[0039] c. Add the above mixture into a wet granulator, start stirring (200rpm), add purified water with a total weight of 45% of raw and auxiliary materials, cut and make soft materials, and the obtained granules are granulated through a conical granulator;

[0040] d....

Embodiment 2

[0043] Formula: mycophenolate mofetil 750g, pregelatinized starch 60g, croscarmellose sodium 45g, povidone K-907.5g, magnesium stearate 18.75g

[0044] Preparation Process:

[0045] a. According to the dose of preparing 3000 capsules, take mycophenolate mofetil, pregelatinized starch, croscarmellose sodium, povidone K-90, and magnesium stearate, and pass through a 40-mesh sieve for use;

[0046] b. Mix croscarmellose sodium and povidone K-90 for 2 minutes, then add pregelatinized starch and mix for 2 minutes, then add one-fifth of the raw materials and mix for 3 minutes; then add the remaining prescription amount of raw materials Mix for 8 min.

[0047] c. Add the above mixture into the wet granulator, start stirring (300rpm), add purified water with 40% of the total weight of raw and auxiliary materials, cut the soft material, and the obtained granules are granulated through the cone granulator;

[0048] d. Fluidized bed drying (50°C, air intake frequency 40%) until the moi...

Embodiment 3

[0051] Formula: mycophenolate mofetil 750g, pregelatinized starch 112.5g, croscarmellose sodium 60g, povidone K-90 11.25g, magnesium stearate 22.5g

[0052] Preparation Process:

[0053] a. According to the dose of preparing 3000 capsules, take mycophenolate mofetil, pregelatinized starch, croscarmellose sodium, povidone K-90, and magnesium stearate, and pass through a 40-mesh sieve for use;

[0054] b. Mix croscarmellose sodium and povidone K-90 for 2 to 5 minutes, then add pregelatinized starch and mix for 5 minutes, then add one-fifth of the raw materials and mix for 8 minutes; then add the remaining prescription amount The raw materials were mixed for 12min.

[0055] c. Add the above mixture into the wet granulator, start stirring (400rpm), add purified water with 50% of the total weight of raw and auxiliary materials, cut and make soft materials, and the obtained granules are granulated by a conical granulator;

[0056] d. Fluidized bed drying (55°C, air intake frequenc...

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PUM

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Abstract

The invention discloses a mycophenolate mofetil capsule and a preparation method thereof. The mycophenolate mofetil capsule contains mycophenolate mofetil, pregelatinized starch, croscarmellose sodium, povidone and magnesium stearate, wherein the weight ratio of the mycophenolate mofetil to the pregelatinized starch to the croscarmellose sodium to the povidone to the magnesium stearate is 1: (0.08-0.15): (0.05-0.08): (0.01-0.02): (0.02-0.03). The mycophenolate mofetil capsule provided by the invention is rapid in dissolution, the dissolution rate is consistent with that of a reference preparation, and related substances are stable and controllable in the preparation acceleration process; and moreover, the provided preparation method is simple in process, and particles obtained by fluidizedbed drying are uniform in granularity and high in flowability and are suitable for large-scale production requirements.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a mycophenolate mofetil capsule and a preparation method thereof. Background technique [0002] Mycophenolate mofetil, chemical name: 2-morpholinoethyl(E)-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo -5-isobenzoyl)-4-methyl-4-vinyl salt, molecular formula C 23 h 31 NO 7 , molecular weight 433.50, chemical structure formula is: [0003] [0004] Mycophenolate mofetil was developed by Swiss Roche (Roche) company, and its trade name was Cellcept (Cellcept). On August 12, 1998 and October 1, 1998, it was approved by the FDA for marketing, and the original capsule was launched in China in 2013. Mycophenolate mofetil is an immunosuppressant with high oral bioavailability. After oral administration, it is rapidly absorbed and metabolized into the active ingredient mycophenolic acid (MPA). MPA is a highly efficient, selective, non-competitive and revers...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/5377A61K47/36A61K47/38A61K47/32A61P37/08
CPCA61K9/4866A61K31/5377A61P37/08
Inventor 谈颖阮春晖郭金林巧平李玲任晋生
Owner JIANGSU SIMCERE PHARMA
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