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Tofacitinib citrate controlled-release capsule and preparation method thereof

A technology of tofacitinib and citric acid, which is applied in the field of tofacitinib citrate controlled-release capsules and its preparation field, can solve the problem of less research on tofacitinib citrate controlled-release preparations, poor therapeutic effect, and blood drug problems. Concentration fluctuations, etc.

Pending Publication Date: 2021-07-06
SHAOXING UNIV YUANPEI COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the treatment of RA often requires long-term medication, or even life-long medication. Ordinary release preparations and sustained release preparations, non-constant release drugs, large fluctuations in blood drug concentration, large side effects, and poor therapeutic effect
Drug controlled-release formulations can overcome this shortcoming, but there are few studies on tofacitinib citrate controlled-release formulations

Method used

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  • Tofacitinib citrate controlled-release capsule and preparation method thereof
  • Tofacitinib citrate controlled-release capsule and preparation method thereof
  • Tofacitinib citrate controlled-release capsule and preparation method thereof

Examples

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preparation example Construction

[0034] A preparation method of tofacitinib citrate controlled-release capsules, comprising the following steps:

[0035]1) Prepare immediate-release pellets by extrusion-spheronization: according tofacitinib citrate:MCC:lactose:CMS-Na:water=(1-1.5):(5-19):(6-12) :(0.2-1):(19-30) mass ratio Weigh the reagents, mix tofacitinib citrate, MCC, lactose and CMS-Na evenly, add wetting agent water and mix to make wet soft material to "group". Not sticky, cracked but not loose", put the wet and soft materials into the extrusion-spheronizing pellet machine, operating parameters: air source pressure 0.1-0.2mpa, extrusion frequency 40.00-60.00Hz, spheronization frequency 20.00-40.00Hz, spheronization Time 2-4min, extrude and spheronize to make wet pellets, dry at 50-70°C, take out 16-30 mesh screened pellets, and get immediate-release pellets;

[0036] 2) Preparation of sustained-release pellets: the composition and mass ratio of the pill core prescription are tofacitinib citrate:MCC:wate...

Embodiment 1

[0041] A preparation method of tofacitinib citrate controlled-release capsules, comprising the following steps:

[0042] 1) Prepare immediate-release pellets by extrusion-spheronization: weigh the reagents according to the mass ratio of tofacitinib citrate:MCC:lactose:CMS-Na:water=1.24:5.92:11.84:1.00:24.6, mix Evenly, add wetting agent and water to mix the wet and soft materials until "agglomerated but not sticky, cracked but not scattered", add the wet and soft materials to the extrusion-spheronizing pellet machine, operating parameters: air source pressure 0.1mpa, extrusion frequency 50.00Hz, spheronization frequency 30.00Hz, spheronization time 3min, extrude and spheronize to obtain wet pellets, dry at 60°C, take out 16-30 mesh screened pellets to obtain immediate-release pellets;

[0043] 2) Preparation of sustained-release pellets: the core prescription composition and mass ratio are tofacitinib citrate:MCC:water=10.0:190.0:220.0, and the extrusion-spheronization method ...

Embodiment 2

[0046] The difference from Example 1 is that the mass ratio of tofacitinib citrate: MCC: lactose: CMS-Na: water in step 1) is 1.08:5.98:11.94:1.00:20.0.

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Abstract

The invention relates to the field of drug controlled-release preparations, and provides a tofacitinib citrate controlled-release capsule aiming at the problem that the plasma concentration fluctuation is large when a tofacitinib citrate common preparation is used, contents of the capsule comprise quick-release pellets and sustained-release pellets, the ratio of the quick-release pellets to the sustained-release pellets is (1-4): (6-9), a filling agent of the quick-release pellets comprises microcrystalline cellulose (MCC), lactose and a wetting agent (water), and the sustained-release pellets are formed by coating a pellet core with a sustained-release coating. The invention also provides the preparation method of the tofacitinib citrate controlled-release capsule. According to the invention, drugs are prepared into skeleton type quick-release pellets and membrane control type sustained-release pellets which are combined together according to a certain proportion to prepare the controlled-release capsule, and in-vivo pharmacokinetic tests of rats show that, compared with raw medicines and tablets of the controlled-release capsule, the controlled-release capsule has the advantages that the controlled-release capsule is quick to take effects, capable of prolonging drug action time, more stable in the in-vivo plasma concentration, higher in ACU, capable of effectively reducing the plasma concentration fluctuation, beneficial to reduce toxic and side effects of drugs and capable of improving treatment effects.

Description

technical field [0001] The invention relates to the field of drug controlled-release preparations, in particular to a tofacitinib citrate controlled-release capsule and a preparation method thereof. Background technique [0002] Tofacitinib citrate, also known as tofacitinib citrate, chemical name 3-[(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3- d] pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropionitrile citrate. Tofacitinib citrate tablets, developed by Pfizer, were approved by the U.S. Food and Drug Administration (FDA) on November 6, 2012, for moderate to severe patients with insufficient response or intolerance to methotrexate treatment Treatment of adult patients with active rheumatoid arthritis (RA). Tofacitinib targets the intracellular signal transduction pathway and directly acts on the core part of the cytokine network. It is an important drug for the treatment of rheumatoid arthritis. On February 23, 2016, the US FDA approved the marketing application of Tofacitin...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/519A61K47/26A61K47/38A61K47/36A61P19/02A61P29/00
CPCA61K9/5084A61K9/5047A61K9/1623A61K9/1652A61K31/519A61P19/02A61P29/00
Inventor 杨群张宇轩张锴李晓辉
Owner SHAOXING UNIV YUANPEI COLLEGE
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