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A kind of preparation method of tacrolimus solid dispersion tablet

A technology of tacrolimus and solid dispersion, applied in the field of medicine, to achieve the effect of good application prospect, low production cost and good release uniformity

Active Publication Date: 2021-03-05
NANJING RUIJIE PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantages of this preparation method are also obvious. It is impossible to melt and spray the first carrier on a conventional fluidized bed. Only a specific device can be used to ensure that the first carrier in the molten state will not condense in the spray pipe. , there will be no blockage in the spray gun, which requires similar fluidized bed devices to install heating and temperature control equipment throughout the pipeline and spray gun, and the temperature should be at least higher than 60°C to ensure its molten state

Method used

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  • A kind of preparation method of tacrolimus solid dispersion tablet
  • A kind of preparation method of tacrolimus solid dispersion tablet
  • A kind of preparation method of tacrolimus solid dispersion tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Batch of 3000 tablets, tablet weight: 253.5mg / tablet.

[0050] Prescription composition:

[0051]

[0052]

[0053] The preparation method is as follows:

[0054] Carbomer 943 and polysorbate were dissolved in purified water, Tween 80 and tacrolimus were dissolved in ethanol, the ethanol solution and aqueous solution were mixed, the homogenizer was dispersed at 2000rpm for 1min, and then stirred at 1000rpm for 5min. Put the suspension into the hopper of the media mill, the medium is zirconium silicate, the particle size is about 1-1.2mm, and the flow rate is about 100ml / min. Grinding time is 30min. Put the lactose and HPMC into the fluidized bed pot after being fully mixed, and spray the ground nanostructured suspension on the second. The air inlet temperature of the fluidized bed is 65°C, the material temperature is controlled at about 55°C, the exhaust frequency is 40%, the atomization pressure is 0.15mpa, and the liquid supply rate is 0.6g / min. Compressed w...

Embodiment 2

[0059] Batch of 3000 tablets, tablet weight: 253.5mg / tablet.

[0060] Prescription composition:

[0061]

[0062]

[0063] The preparation method is as follows:

[0064] Preparation method is with embodiment 1.

[0065] Embodiment 1, the degree of release of 2

[0066] time Embodiment 1 release degree Embodiment 2 release degree commercial sample release 0.5h 1.72 5.07 2.42 1h 4.36 10.49 6.35 2.5h 10.22 25.61 19.07 4.5h 30.28 48.63 38.08 6.5h 55.63 67.76 58.87 8.5h 69.20 79.23 82.53 12h 87.91 97.77 100.28

[0067] See attached figure 1 .

Embodiment 3

[0069] Batch of 4000 tablets, tablet weight: 203mg / tablet.

[0070] Prescription composition:

[0071]

[0072]

[0073] The preparation method is as follows:

[0074] Dissolve CMC-Na and PEG6000 in purified water, dissolve poloxamer 188 and tacrolimus in ethanol, mix the ethanol solution and aqueous solution, disperse with a homogenizer at 2000rpm for 1min, and then stir at 1000rpm for 5min. Put the suspension into the hopper of the media mill, the medium is zirconium silicate, the particle size is about 1-1.2mm, and the flow rate is about 80ml / min. Grinding time is 40min. After fully mixing the microcrystalline cellulose and HPMC, put them into a fluidized bed pot, and spray the ground nanostructured suspension on the second carrier mixture. The air inlet temperature of the fluidized bed is 60°C, the material temperature is controlled at about 50°C, the exhaust frequency is 45%, the atomization pressure is 0.12mpa, and the liquid supply rate is 0.8g / min. Compressed...

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Abstract

The invention discloses a method for preparing a tacrolimus solid dispersion tablet, which belongs to the field of pharmaceutical preparations. The invention adopts a suitable solvent to disperse a carrier material and tacrolimus in a solvent to prepare a suspension, and adopts a bead mill machine to pulverize the suspension to the micron or even nanometer level, spray it onto the surface of the second carrier particle to obtain a drying effect, and attach to the surface of the second carrier mixture particle for tableting. The present invention prepares tacrolimus by improving The process step of solid dispersion makes the drug-containing particles attached to the surface of the second carrier mixture particles more finely distributed and uniform. The invention has strong operability and low condition requirements, and enables the tacrolimus sustained-release tablet to have the same or better release behavior.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a preparation method of tacrolimus solid dispersion tablet. Background technique [0002] Tacrolimus (tacrolimus, FK-506) is a macrolide antibiotic (erythromycin family), the chemical name is [3S-[3R*[E(1S*,3S*,4S*)],4S* ,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-5,6,8,11,12,13,14,15,16, 17,18,19,24,25,26a-hexa-decanehydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]- 14,16-dimethoxy-4,10,12,18-tetramethyl 8-(2-propenyl)-15,19-epoxy-3H-pyrido[2,1-c][1,4 ]oxazacyclotricodecene-1,7,20,21(4H,23H)-tetraketone monohydrate, the chemical structure is shown in formula I: [0003] [0004] Tacrolimus is mainly used to treat the rejection of the body before and after organ and tissue transplantation. It has a similar and broader immunosuppressive effect to cyclosporine A (CsA), and its efficacy is 10-100 times higher than that of CsA, wit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/436A61K47/38A61K47/26A61K47/32A61P37/06
CPCA61K9/2018A61K9/2027A61K9/2054A61K31/436A61P37/06
Inventor 张军波王培培李迁徐晓寒
Owner NANJING RUIJIE PHARMATECH CO LTD
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