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Stable fidaxomicin composition

A technology for fidaxomicin and composition, applied in the field of stable pharmaceutical composition and preparation thereof, can solve the problem of high F heterogeneity of drugs, achieve the requirements of lowering temperature, stable dissolution, and less increase of related substances

Active Publication Date: 2019-07-23
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When testing the commercially available products of the original research company, it is found that it has relatively strict control over process impurities, such as A impurity, but relatively loose control over degraded impurities, such as F impurity, so there are high levels of F impurity in commercially available drugs. Phenomenon

Method used

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  • Stable fidaxomicin composition
  • Stable fidaxomicin composition
  • Stable fidaxomicin composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription:

[0028]

[0029]

[0030] Preparation:

[0031] 1. Weigh the raw materials, microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch, and hydroxypropyl cellulose into the granulator BoschMycromix, pre-mix for 3 minutes, and stir at a speed of 60m / min;

[0032] 2. After premixing, add ethanol and continue stirring, slowly add pure water and continue stirring, the stirring speed is 115m / min, and the granulation time is 6 minutes. After the granulation is completed, the wet granules are sized, the screen is 4*4mm square holes, and the speed is 1000rpm.

[0033] 3. Fluidized bed Solidlab drying, air inlet temperature 60°C, moisture 1.0-3.0%.

[0034] 4. Whole grain QUADRO COMIL U5-0437R, sieve aperture Φ1.5mm, rotation speed 1000rpm.

[0035] 5. Add additional sodium carboxymethyl starch and magnesium stearate according to the prescription amount, mix well, and compress the tablet with a rotary tablet machine ZPS8.

Embodiment 2-7

[0037] Embodiments 2-7 are the same as Example 1 except that the amount of water added, the stirring speed of granulation, and the granulation time are as shown in the table below.

[0038] Example Add water % Amount of water added g Linear speed(m / min) Granulation time (min) 2 52％ 270 61 6 3 42％ 220 61 3 4 52％ 270 115 3 5 42％ 220 115 6 6 52％ 270 61 3 7 47％ 245 88 4.5

Embodiment 8

[0040] prescription:

[0041]

[0042]

[0043] Preparation:

[0044] 1. Weigh raw materials, microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch, and hydroxypropyl cellulose and pour them into the granulator Pilotmix 50T granulation line wet granulator, pre-mix for 3 minutes, and stir at a speed of 88m / min;

[0045] 2. After premixing, add ethanol and continue stirring, slowly add pure water and continue stirring, the stirring speed is 88m / min, and the granulation time is 4.5min. After the granulation is completed, the wet granules are sized, the screen is 4*4mm square holes, and the speed is 1000rpm.

[0046] 3. Pilotlab L granulation line fluidized bed drying, air inlet temperature 60 ℃, MB35 fast moisture analyzer to measure moisture 1.0-3.0%.

[0047] 4. The aperture of the screen is Φ1.5mm, and the rotation speed is 1000rpm.

[0048] 5. Add additional sodium carboxymethyl starch and magnesium stearate according to the prescription am...

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Abstract

The invention discloses a pharmaceutical composition containing fidaxomicin and a preparation method thereof. The preparation method comprises the following steps: preparing granules containing fidaxomicin by adopting wet process granulation; and compacting the granules into the pharmaceutical composition. According to the composition containing the fidaxomicin disclosed by the invention, throughimproving the water addition amount in a wet process granulation procedure, the stirring velocity during granulation and the time required for wet process granulation, even if under the case of no adding an antioxidant, the prepared composition containing the fidaxomicin has high stability, less increase of related substances, meets the quality standard of drugs, can reduce a requirement on a temperature in a storage step and is stable in dissolution.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a stable pharmaceutical composition containing fidaxomicin and a preparation method thereof. Background technique [0002] Fidaxomicin (trade name Dificid) is the first of a new class of oral narrow-spectrum macrocyclic antibiotics developed by Optimer. It is a macrolide antibiotic with an 18-membered ring structure and belongs to Class B Tiacumella have a novel mechanism of action. Fidaxomycin was approved by the US FDA in May 2011 for the treatment of Clostridium difficile (Clostridium difficile) infection-associated diarrhea (CDAD). This is the first drug to treat CDAD approved by the FDA in nearly 30 years. It was approved for marketing by the European Union in December 2011. [0003] The structural formula is as follows: [0004] [0005] Belonging to polyene macrolide antibiotics, there are multiple conjugated ethylenic bonds and hydroxyl groups in its structure. The e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K31/7048A61P31/04A61P1/12
CPCA61K9/2054A61K9/2059A61K9/2095A61K31/7048A61P1/12A61P31/04
Inventor 谢羽能白海波
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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