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Tacrolimus nanocrystal and artificial tear compound and preparation method thereof

A technology of tacrolimus and artificial tears, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of low drug efficacy, poor stability and bioavailability, and low patient compliance , to achieve good reproducibility, good application prospects, and reduce the effect of direct stimulation

Active Publication Date: 2018-08-10
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned drugs all have poor stability and bioavailability, low drug efficacy and low patient compliance

Method used

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  • Tacrolimus nanocrystal and artificial tear compound and preparation method thereof
  • Tacrolimus nanocrystal and artificial tear compound and preparation method thereof
  • Tacrolimus nanocrystal and artificial tear compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1, the preparation of tacrolimus nanocrystal

[0044] The preparation method of tacrolimus nanocrystal specifically comprises the following steps:

[0045] Mix the tacrolimus drug crystals with the absolute ethanol solution so that the concentration is 4 mg / mL to obtain the tacrolimus absolute ethanol solution. The above solution was added to the aqueous solution at a dropping rate of 2 mL / min (the volume ratio of tacrolimus absolute ethanol solution to aqueous solution was 1:10), and stirred at a high speed of 7200 rpm to obtain a suspension. The suspension was continuously stirred at a rate of 800 rpm for 12 h, and absolute ethanol in the solution was volatilized to obtain a final solution. The final solution was centrifuged several times to remove the supernatant to obtain tacrolimus nanocrystals.

[0046] Its electron microscope picture is as figure 1 As shown in (a), by figure 1 (a) It can be seen that the crystal form of the tacrolimus nanocrystal i...

Embodiment 2

[0047] Embodiment 2, the preparation of tacrolimus nanocrystal

[0048] The preparation method of tacrolimus nanocrystal specifically comprises the following steps:

[0049] Mix the tacrolimus drug crystals with the absolute ethanol solution so that the concentration is 4 mg / mL to obtain the tacrolimus absolute ethanol solution. Add the above solution to a polyvinyl alcohol (PVC for short) aqueous solution with a mass volume concentration of 1 g / L at a dropping rate of 2 mL / min (the volume ratio of tacrolimus absolute ethanol solution to PVC aqueous solution is 1:10) , stirring at a high speed of 7200rpm to obtain a suspension. The suspension was continuously stirred at a rate of 800 rpm for 12 h, and absolute ethanol in the solution was volatilized to obtain a final solution. The final solution was centrifuged several times to remove the supernatant to obtain tacrolimus nanocrystals.

[0050] Its electron microscope picture is as figure 1 (b), shown by figure 1 (b) It ca...

Embodiment 3

[0051] Embodiment 3, the preparation of tacrolimus nanocrystal

[0052] The preparation method of tacrolimus nanocrystal specifically comprises the following steps:

[0053] Mix the tacrolimus drug crystals with the absolute ethanol solution so that the concentration is 4 mg / mL to obtain the tacrolimus absolute ethanol solution. The above solution was added to a polyvinyl alcohol aqueous solution with a mass volume concentration of 1 g / L (the volume ratio of tacrolimus absolute ethanol solution to PVC aqueous solution was 1:10) at a dropping rate of 2 mL / min, and was added at a rate of 11200 rpm. Stir at high speed to obtain a suspension. The suspension was continuously stirred at a rate of 800 rpm for 12 h, and absolute ethanol in the solution was volatilized to obtain a final solution. The final solution was centrifuged several times to remove the supernatant to obtain tacrolimus nanocrystals.

[0054] Its electron microscope picture is as figure 2 As shown in (a), by ...

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Abstract

The invention discloses a tacrolimus nanocrystal and an artificial tear compound and preparation method thereof. Tacrolimus is a nanocrystal. The tacrolimus nanocrystal is prepared through a recrystallization method. The artificial tear compound of the tacrolimus nanocrystal comprises a nanocrystal of tacrolimus as a core and a shell layer covering the core; the shell layer comprises a plurality of double layers, and each double layer comprises a sodium carboxymethyl cellulose layer and a cationic polymer layer from inside to outside in sequence; a cationic polymer is at least one of polyallylamine hydrochloride, polylysine and polyethyleneimine. The compound is prepared by a layer-by-layer self-assembling method. The tacrolimus nanocrystal as hydrophilicity, high bioavailability and low toxicity, and the artificial tear compound of the tacrolimus nanocrystal has the effects of reducing direct stimulation of high-concentration medicine and exerting immunomodulatory anti-inflammatory and lubrication synergy. The tacrolimus nanocrystal and the artificial tear compound and preparation method thereof can be applied to preparation of medicine for treatment of ocular diseases.

Description

technical field [0001] The present invention relates to tacrolimus nanocrystal and its artificial tear compound and preparation method thereof; in particular to a tacrolimus nanocrystal and its preparation method and application, tacrolimus nanocrystal artificial tear compound and its preparation method The invention belongs to the field of preparation of pharmaceutical dosage forms and compound medicines. Background technique [0002] With the popularization of TV, computer and mobile phone and severe environmental pollution such as smog, the incidence of dry eye (DE) has been increasing year by year, and it has become one of the most common diseases in ophthalmology, seriously affecting the eye health and Quality of life (Zeev M S, Miller D D, Latkany R. Clinical Ophthalmology, 2014, 8, 581). At present, there are many kinds of drugs for the clinical treatment of dry eye. Artificial tears are often used to improve and relieve dry eye symptoms because of their lubricating ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/18A61K31/436A61K9/51A61K47/38A61K47/32A61P27/04A61P29/00A61P37/02A61P27/02
CPCA61K9/5138A61K9/5161A61P27/02A61P27/04A61P29/00A61P37/02C07D498/18
Inventor 周志敏赵少贞郑莹莹
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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