Tofacitinib gastric retention floating sustained release tablet and preparation method thereof

A technology of tofacitinib and gastric retention, which is applied in the field of medicine, can solve the unsolved problems such as low absorption in the lower part of the digestive tract, and achieve the effect of improving bioavailability

Pending Publication Date: 2022-06-24
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But it does not solve the problem of less absorption in the lower part of the digestive tract

Method used

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  • Tofacitinib gastric retention floating sustained release tablet and preparation method thereof
  • Tofacitinib gastric retention floating sustained release tablet and preparation method thereof
  • Tofacitinib gastric retention floating sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]

[0043] Preparation Process:

[0044] (1) get tofacitinib citrate, crospovidone XL, sodium bicarbonate, carbomer 934P, magnesium stearate and cross 40 mesh sieves respectively, for subsequent use;

[0045] (2) Weigh tofacitinib citrate, crospovidone XL (about 1 / 2 of the recipe) and carbomer 934P and place them in the hopper, mix them evenly, and then add the remaining crospovidone XL and sodium bicarbonate, mix evenly, and finally add magnesium stearate, mix evenly, to obtain the final mixed material;

[0046] (3) placing the above-mentioned homogeneously mixed particles in a rotary tableting machine, tableting, and obtaining tofacitinib citrate sustained-release tablet cores with a hardness of 70 to 110N;

[0047] (4) preparing a coating solution, and then the prepared tablet core is coated with a controlled release film, and the coating weight gain is about 7%;

[0048] (5) Using the aluminum-plastic blister packaging machine, the above-mentioned coated tablets ...

Embodiment 2

[0050]

[0051]

[0052] Preparation Process:

[0053] (1) get tofacitinib citrate, croscarmellose sodium starch, sodium bicarbonate, carbomer 974P, magnesium stearate and cross 40 mesh sieves respectively, for subsequent use;

[0054] (2) Weigh tofacitinib citrate, sodium cross-linked carboxymethyl starch (about 1 / 2 of the recipe), and carbomer 974P and place them in the hopper, mix them evenly, and then add the remaining cross-linked carboxymethyl Sodium starch and sodium bicarbonate, mix well, finally add magnesium stearate, mix well, and get the final mixed material;

[0055] (3) placing the above-mentioned homogeneously mixed particles in a rotary tableting machine, tableting, and obtaining tofacitinib citrate sustained-release tablet cores with a hardness of 70 to 110N;

[0056] (4) preparing a coating solution, and then the prepared tablet core is coated with a controlled release film, and the coating weight gain is about 7%;

[0057] (5) Using the aluminum-plas...

Embodiment 3

[0059]

[0060] Preparation Process:

[0061] (1) get tofacitinib citrate, sodium carboxymethyl starch, sodium bicarbonate, carbomer 974P, magnesium stearate and cross 40 mesh sieves respectively, for subsequent use;

[0062] (2) Weigh tofacitinib citrate, sodium carboxymethyl starch (about 1 / 2 of the recipe), and carbomer 974P and place them in the hopper, mix them evenly, and then add the remaining sodium carboxymethyl starch and carbonic acid. Sodium hydrogen, mix evenly, finally add magnesium stearate, mix evenly, to obtain a total mixed material;

[0063] (3) placing the above-mentioned homogeneously mixed particles in a rotary tableting machine, tableting, and obtaining tofacitinib citrate sustained-release tablet cores with a hardness of 70 to 110N;

[0064] (4) preparing a coating solution, and then the prepared tablet core is coated with a controlled release film, and the coating weight gain is about 7%;

[0065] (5) Using the aluminum-plastic blister packaging m...

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Abstract

The invention relates to the technical field of medicines, in particular to a tofacitinib gastric retention floating type sustained release tablet and a preparation method thereof. The tofacitinib gastric retention floating type sustained release preparation provided by the invention takes carbomer as gel and is matched with proper expanding agent, floating agent, controlled release material and other auxiliary materials. All the components are properly selected and reasonably matched, so that the prepared controlled release tablet can quickly float in a stomach environment, the effective components are released and absorbed in a relatively low-pH environment, and the bioavailability is improved. Experiments show that the preparation rapidly floats after being put into a dissolution cup and continuously floats in a dissolution medium for at least 10 hours. In a medium with the pH value of 6.8, the medicine is stably and completely released within 10 hours; in simulated gastric juice, the release rate of the medicine in 6h is greater than 85%.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to tofacitinib gastroretentive floating sustained-release tablet and a preparation method thereof. Background technique [0002] Rheumatoid arthritis (RA) is a common systemic autoimmune disease characterized by chronic progressive inflammation that mainly affects synovial joints. If this inflammatory process is not properly inhibited, joint deformities will develop, leading to significant functional disability and progressive incapacity to work. Cytokines such as tumor necrosis factor (TNF) and interleukin-1 (IL-1) and their signaling pathways play an extremely important role in the pathogenesis of RA and have become important therapeutic targets for RA one. JAK family members (such as JAK1, JAK2, JAK3) are involved in various cytokine (IL-2, IL-4, IL-6, IL-7, IL-9, IL-15, IL-21) signal transduction pathways It plays an important role in various diseases such as inflammation, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/32A61K31/519A61K47/32A61K47/38A61K47/36A61K47/02A61K47/12A61P19/02A61P37/02
CPCA61K31/519A61K9/0065A61K9/2027A61K9/284A61K9/2866A61K9/2059A61K9/2054A61K9/2009A61K9/2013A61P19/02A61P37/02
Inventor 辛永涛张伟明唐洋明余品香
Owner HYBIO PHARMA
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