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Drug composition containing baricitinib and preparation method and application of drug composition

A baricitinib and composition technology, which is applied in the field of pharmaceutical compositions for improving drug dissolution, can solve the problems of poor process repeatability, unfavorable scale-up production, and high process costs, and achieves good mixing uniformity, not easy to decompose, and simple operation. Effect

Active Publication Date: 2017-11-10
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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  • Drug composition containing baricitinib and preparation method and application of drug composition
  • Drug composition containing baricitinib and preparation method and application of drug composition
  • Drug composition containing baricitinib and preparation method and application of drug composition

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Effect test

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; di...

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 liquid; spray the granula...

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Abstract

The invention discloses a drug composition containing baricitinib and a preparation method and application of the drug composition. The drug composition comprises the baricitinib and an auxiliary material which can be received pharmaceutically, wherein the auxiliary material comprises a filling agent and a disintegrating agent. The preparation method of the drug composition comprises the steps that the filling agent and the disintegrating agent are evenly mixed, so that the mixed auxiliary material is obtained; and then a baricitinib crude drug and the mixed auxiliary material are evenly mixed or pelletizing liquor containing the baricitinib crude drug is evenly mixed with the mixed auxiliary material, and drug-carrying pellets of the solid drug composition containing the baricitinib are obtained through pelletizing. According to the drug composition containing the baricitinib and the preparation method and application of the drug composition, the solid drug composition which can be dissolved out rapidly in vitro and contains the baricitinib is prepared by controlling the particle size of the baricitinib, using microcrystalline cellulose, mannitol and the like in the hydrophilic auxiliary material as the filling agent, and using croscarmellose sodium and the like as the disintegrating agent; and the preparation technique is simple and 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 Applications(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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