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Tofacitinib nanocrystal eye drops and preparation method thereof

A technology of tofacitinib and nanocrystals, applied in anti-inflammatory agents, liquid delivery, pharmaceutical formulations, etc., to achieve the effects of improving stability and adhesion, avoiding systemic side effects, and high drug loading rate

Active Publication Date: 2022-03-04
THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, in the prior art, tofacitinib is made into tablets in the form of citrate or citrate, and is applied to the treatment of autoimmune diseases, while the unsalted tofacitinib is made into nanocrystals Eye drops research has not been reported

Method used

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  • Tofacitinib nanocrystal eye drops and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] A preparation method of tofacitinib nanocrystal eye drops, comprising the following steps:

[0032] S1, preparation of drug coarse suspension

[0033] S1.1. Weigh 150 mg of micronized tofacitinib, 30 mg of surfactant P188-lecithin, 65 mg of stabilizer HPMC (hydroxypropyl methylcellulose), and 100 mL of distilled water;

[0034] S1.2. Disperse the micronized tofacitinib in a part of water to obtain solution A;

[0035] Dispersing the surfactant in the remaining water to obtain solution B;

[0036] S1.3. Slowly add solution A to solution B, stir for 10 minutes, and cut with a high-speed shearer at 10,000 rpm for 5 minutes. After the dispersion is uniform, mix it with a stabilizer, and use a high-speed shearer to shear and disperse evenly to obtain a coarse suspension of the drug. ;

[0037] S2. Preparation of tofacitinib nanocrystal eye drops

[0038] Place the drug suspension of S1 in a high-pressure homogenizer, first cycle 5 times with a pressure of 500bar, perform...

Embodiment 2

[0040] A preparation method of tofacitinib nanocrystal eye drops, comprising the following steps:

[0041] S1, preparation of drug coarse suspension

[0042] S1.1. Weigh 150 mg of micronized tofacitinib, 7.5 mg of surfactant P188-lecithin, 7.5 mg of stabilizer HPMC (hydroxypropyl methylcellulose), and 100 mL of distilled water;

[0043] S1.2. Disperse the micronized tofacitinib in a part of water to obtain solution A;

[0044] Dispersing the surfactant in the remaining water to obtain solution B;

[0045] S1.3. Slowly add solution A to solution B, stir for 10 minutes, and cut with a high-speed shearer at 10,000 rpm for 5 minutes. After the dispersion is uniform, mix it with a stabilizer, and use a high-speed shearer to shear and disperse evenly to obtain a coarse suspension of the drug. ;

[0046] S2. Preparation of tofacitinib nanocrystal eye drops

[0047]Place the crude drug suspension of S1 in a high-pressure homogenizer, first cycle 10 times with a pressure of 500bar,...

Embodiment 3

[0049] A preparation method of tofacitinib nanocrystal eye drops, comprising the following steps:

[0050] S1, preparation of drug coarse suspension

[0051] S1.1. Weigh 150 mg of micronized tofacitinib, 15 mg of surfactant P188-lecithin, 155 mg of stabilizer HPMC (hydroxypropyl methylcellulose), and 100 mL of distilled water;

[0052] S1.2. Disperse the micronized tofacitinib in a part of water to obtain solution A;

[0053] Dispersing the surfactant in the remaining water to obtain solution B;

[0054] S1.3. Slowly add solution A to solution B, stir for 10 minutes, and cut with a high-speed shearer at 10,000 rpm for 5 minutes. After the dispersion is uniform, mix it with a stabilizer, and use a high-speed shearer to shear and disperse evenly to obtain a coarse suspension of the drug. ;

[0055] S2. Preparation of tofacitinib nanocrystal eye drops

[0056] Place the crude drug suspension of S1 in a high-pressure homogenizer, first cycle 15 times with a pressure of 500bar,...

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Abstract

The invention provides tofacitinib nanocrystal eye drops for treating immunity-related eye diseases and a preparation method thereof, and the tofacitinib nanocrystal eye drops are prepared by the following steps: dispersing micronized tofacitinib in a surfactant solution at a high speed, then mixing with a stabilizer, uniformly dispersing, and then carrying out high-pressure homogenization circulation, so as to obtain the tofacitinib nanocrystal eye drops. The tofacitinib nanocrystal eye drops meeting the particle size requirement are obtained. Wherein the surfactant is P188-lecithin, and the stabilizer is any one or a mixture of more of HPMC (Hydroxy Propyl Methyl Cellulose), polyvinyl alcohol and HPMC-docusate sodium. Through cooperation of the surfactant and the stabilizer, the particle size and the potential of the eye drops are influenced, the stability and the adhesiveness are improved, the residence time of the medicine in eyes is prolonged, and the medicine carrying rate is high. The loss speed of the medicine in front of the cornea is reduced, so that the medicine can be slowly released, the eye drop frequency of a patient is reduced, the compliance of the patient is improved, and a good clinical application prospect is achieved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a tofacitinib nanocrystal eye drop for treating immune-related eye diseases and a preparation method thereof. Background technique [0002] Immune response is an important physiological function of the body to "identify itself and reject others". Immune-related eye diseases are diseases that are closely watched all over the world, including uveitis, keratitis, blepharitis, conjunctivitis, episcleritis and scleritis, idiopathic retinitis, and uveitis is the most common. Immune eye diseases can cause symptoms such as redness and swelling of the eyes, impaired vision, and even blindness, seriously affecting the quality of life. [0003] Various systemic autoimmune diseases, such as spondyloarthritis, Behcet's disease, retinal vascular disease, Sjogren's syndrome, granulomatous vasculitis, etc., can cause eye diseases. For example, 45% to 90% of patients with Be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/519A61K47/24A61K47/26A61K47/38A61K47/20A61P27/02A61P29/00A61P37/02
CPCA61K31/519A61K9/0048A61K47/24A61K47/26A61K9/10A61K47/38A61K47/20A61P37/02A61P27/02A61P29/00
Inventor 郑朝晖王倩倩高聪聪张纯祎
Owner THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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