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

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 ...

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 was a single-skeleton sustained-release material, and it was difficult to adjust a suitable release curve. And it adopts the method of extrusion and spheronization, and it is difficult to extrude when extruding.

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