Tofacitinib citrate enteric-coated sustained-release pellet and preparation method thereof

A technology of sustained-release pellets and tofacitinib, which is applied in pharmaceutical formulations, microcapsules, medical preparations of non-active ingredients, etc., can solve problems such as difficult extrusion and difficult adjustment of release curves, and achieve stable release speed, The effect of good process reproducibility and simple preparation process

Active Publication Date: 2018-05-25
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] When the inventors of the company studied the preparation technology of tofacitinib, they found that a kind of tofacitinib citrate skeleton-type sustained-release pellets disclosed in WO2014/147526A1 wa

Method used

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  • Tofacitinib citrate enteric-coated sustained-release pellet and preparation method thereof
  • Tofacitinib citrate enteric-coated sustained-release pellet and preparation method thereof
  • Tofacitinib citrate enteric-coated sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Preparation of tofacitinib citrate enteric-coated sustained-release pellets:

[0046] Prescription composition of tofacitinib citrate enteric-coated sustained-release pellets: specification 11mg (calculated as tofacitinib)

[0047] Ball core composition:

[0048]

[0049] Coating liquid composition:

[0050]

[0051] Preparation Process:

[0052] (1) Weighing of raw and auxiliary materials

[0053] The raw and auxiliary materials were weighed in turn, and the purified water was weighed separately.

[0054] (2) Preparation of soft materials

[0055] ① Mix the weighed raw and auxiliary materials evenly according to the principle of equal increase.

[0056] ② Slowly add the binder under stirring, and stir until there is no lump-like material, and the over-wet soft material is obtained.

[0057] (3) Extrusion and spheronization to prepare pellets

[0058] Put the above-mentioned soft material in the extruder, adjust the speed of the extruder, then pl...

Embodiment 2

[0066] Example 2: Preparation of tofacitinib citrate enteric-coated sustained-release pellets:

[0067] Prescription composition of tofacitinib citrate enteric-coated sustained-release pellets: specification 11mg (calculated as tofacitinib)

[0068] Ball core composition:

[0069]

[0070] Coating liquid composition:

[0071]

[0072] Preparation process: with embodiment 1.

Embodiment 3

[0073] Example 3: Preparation of tofacitinib citrate enteric-coated sustained-release pellets:

[0074] Prescription composition of tofacitinib citrate enteric-coated sustained-release pellets: specification 11mg (calculated as tofacitinib)

[0075] Ball core composition:

[0076]

[0077] Coating liquid composition:

[0078]

[0079] Preparation process: with embodiment 1.

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Abstract

The invention discloses a tofacitinib citrate enteric-coated sustained-release pellet and a preparation method thereof. The tofacitinib citrate enteric-coated sustained-release pellet contains a matrix type drug-containing pellet core and an enteric coating which coats the pellet core, wherein the matrix type drug-containing pellet core comprises a compound matrix type sustained-release material which is two or three selected from a group consisting of a hydrophilic gel matrix material, a corrosive matrix material and a non-corrosive matrix material. The tofacitinib citrate enteric-coated sustained-release pellet of the invention is stable in drug release and smooth in extrusion; the pellet is a multi-unit administration preparation, has the advantages of small local irritation and high bioavailability and guarantees the effectiveness and safety of drug usage; and the sustained-release pellet can reduce the drug taking frequency of patients and improve the compliance of patients in drug taking.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to tofacitinib citrate enteric-coated sustained-release pellets and a preparation method thereof. Background technique [0002] Pfizer has successfully developed tofacitinib sustained-release preparations and immediate-release tablets. The active ingredient of tofacitinib sustained-release preparations is tofacitinib citrate, 11mg / tablet, which was launched in the United States on February 23, 2016. Name: XELJANZ XR. The active ingredient of tofacitinib immediate-release tablets is tofacitinib citrate, 5mg / tablet, which was launched in the United States on November 6, 2012 and in Japan in May 2013, under the trade name: XELJANZ. The drug is indicated for adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate therapy and is a novel oral JAK inhibitor. Unlike most other current RA ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/519A61K47/38A61K47/32A61K47/14A61K47/36A61P29/00A61P19/02
CPCA61K47/14A61K47/32A61K47/36A61K47/38A61K9/0002A61K9/5026A61K31/519
Inventor 郑弯李宛蓉陈颖李玲嵇元欣
Owner JIANGSU SIMCERE PHARMA
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