A pharmaceutical composition containing baricitinib and its preparation method and application

A technology for baricitinib and a composition, which is applied in the field of pharmaceutical compositions for improving drug dissolution, can solve the problems of unfavorable scale-up production, poor process repeatability, and high process cost, and achieves good mixing uniformity, simple operation, and difficult decomposition. Effect

Active Publication Date: 2021-02-09
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the scheme is complex in operation, high in process cost, and has many influencing factors, resulting in poor process repeatability, which is not conducive to industrial scale-up production

Method used

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  • A pharmaceutical composition containing baricitinib and its preparation method and application
  • A pharmaceutical composition containing baricitinib and its preparation method and application
  • A pharmaceutical composition containing baricitinib and its preparation method and application

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preparation example Construction

[0068]The preparation method of the baricitinib-containing pharmaceutical composition of the present invention is specifically described below. The present invention mainly discloses a process for preparing the above-mentioned baricitinib-containing pharmaceutical composition into tablets, which mainly involves the steps of mixing, granulating and tableting. Among them, when the dosage of the main drug (such as baricitinib) is small, the present invention improves the material mixing mode of the main drug and the auxiliary material, so as to ensure the uniformity of mixing and further ensure the dissolution efficiency of the main drug. For example, when mixing materials, the main drug can be mixed with the filler first, and then mixed with other auxiliary materials; after the auxiliary materials are evenly mixed, the main drug can be added for mixing.

[0069] According to an exemplary embodiment of the present invention, the specific preparation method is: uniformly mix the f...

Embodiment 1

[0086] Embodiment 1: the preparation of the pharmaceutical composition (coated tablet) containing baricitinib

[0087] This embodiment prepares the coated tablet containing baricitinib, adopts the tablet core prescription containing baricitinib listed in Table 1, the weight gain of Opadry film coating is 2% of the tablet core weight, baricitinib The particle size of ricitinib raw material is 0.075mm-0.048mm.

[0088] Table 1 Tablet core prescription of pharmaceutical composition containing baricitinib

[0089] Main ingredients and excipients Mass percentage content (wt%) Baricitinib 1 microcrystalline cellulose 55 Mannitol 40 Croscarmellose Sodium 3 Magnesium stearate 1 Chip sum 100

[0090] The specific preparation method is as follows: weigh microcrystalline cellulose, mannitol and croscarmellose sodium according to the tablet core prescription in Table 1, and premix to obtain mixed excipients; disperse baricitinib in pure...

Embodiment 2

[0096] Embodiment 2: Preparation of the pharmaceutical composition containing baricitinib

[0097] The prescription of the pharmaceutical composition containing baricitinib in the embodiment 2 of table 3

[0098] Main ingredients and excipients Mass percentage content (wt%) Baricitinib 4 microcrystalline cellulose 46 Mannitol 46 Croscarmellose Sodium 3 Magnesium stearate 1 sum 100

[0099] The data in Table 3 shows the prescription of the pharmaceutical composition containing baricitinib used in this example, wherein the particle size of the baricitinib bulk drug is less than 0.048um.

[0100] The specific preparation method is as follows: weighing microcrystalline cellulose, mannitol and cross-linked carmellose sodium according to the prescription, stirring and mixing uniformly to obtain mixed auxiliary materials. Disperse baricitinib in pure water to prepare a granulation solution; spray the granulation solution evenly on ...

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Abstract

The invention discloses a pharmaceutical composition containing baricitinib and its preparation method and application. The pharmaceutical composition comprises baricitinib and pharmaceutically acceptable auxiliary materials, wherein the auxiliary materials include fillers and disintegrants. The preparation method of the pharmaceutical composition comprises: uniformly mixing a filler and a disintegrant to obtain mixed excipients; uniformly mixing the baricitinib bulk drug with the mixed excipients or granulating the baricitinib bulk drug The liquid is uniformly mixed with the mixing excipients, and the drug-loaded granules of the solid pharmaceutical composition containing baricitinib are obtained by granulation. The present invention controls the particle size of baricitinib, uses hydrophilic auxiliary materials microcrystalline cellulose, mannitol, etc. The solid pharmaceutical composition containing baricitinib has a simple preparation process and is suitable for industrialization.

Description

technical field [0001] The invention relates to a pharmaceutical composition for improving drug dissolution, more specifically, to a pharmaceutical composition containing baricitinib and a preparation method thereof. Background technique [0002] Baricitinb, 2-(3-(4-(7H-pyrrolo[2.3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonate Acyl)azetidin-3-yl)acetonitrile is a novel and highly effective small molecule drug compound that can selectively inhibit JAK1 and JAK2, and can inhibit the production of various inflammatory cytokines such as IL-6 and IL-23 Intracellular signal transduction can be used for the treatment of JAK-related diseases. [0003] The chemical structure of baricitinib is shown below: [0004] [0005] The selectivity and high efficiency of baricitinib for JAK-related diseases (such as autoimmune diseases, inflammatory diseases, etc.) have long been verified, such as in the patent application CN200980116857. , the saturated solubility in water is onl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/38A61K47/26A61K9/36A61K31/519A61P29/00A61P19/02A61P3/10A61P17/06A61P1/00A61P21/00A61P13/12A61P37/00A61P5/14A61P11/06A61P37/08A61P17/00A61P11/02
CPCA61K9/1623A61K9/1652A61K9/1682A61K9/2866A61K31/519
Inventor 韩志东申丽先崔博王琦王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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