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Chitosan modified triamcinolone acetonide acetate lipidosome and preparation method thereof

A technology of triamcinolone acetonide and liposome, which is applied in liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem that eye drops cannot be applied clinically and are prone to flocculation , Poor adsorption on the corneal surface, etc., to improve drug bioavailability, good therapeutic effect, and improve surface electrical properties

Active Publication Date: 2019-03-19
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, negative liposomes and neutral liposomes commonly used in clinical practice have poor corneal surface adsorption; they also have problems such as poor stability, easy flocculation, large particle size, inability to store for a long time, and low encapsulation efficiency.
Eye drops prepared with liposome-encapsulated drugs cannot be applied clinically
[0004] As a positive polysaccharide, chitosan has good biofilm adhesion, biocompatibility and antibacterial activity, can promote drug absorption, and can significantly improve drug performance when applied to eye drops. Undisclosed chitosan-modified triamcinolone acetonide liposome eye drops

Method used

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  • Chitosan modified triamcinolone acetonide acetate lipidosome and preparation method thereof
  • Chitosan modified triamcinolone acetonide acetate lipidosome and preparation method thereof
  • Chitosan modified triamcinolone acetonide acetate lipidosome and preparation method thereof

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Effect test

Embodiment 1

[0045] Triamcinolone acetonide liposomes modified by embodiment 1 chitosan preparation

[0046] Dissolve soybean lecithin and cholesterol in chloroform at a molar ratio of 8:1, and use a rotary evaporator at 35°C at a speed of 200 rpm for 15 minutes to form a film. Place in a vacuum environment overnight to completely remove residual organic solvents.

[0047] Calcium acetate solution (120 mM) was added, and ultrasonic hydration was carried out at 45° C. for 3 h under normal pressure to obtain a blank liposome suspension with blue opalescence.

[0048] The suspension was repeatedly frozen and thawed, and filtered with a 0.22 micron microporous filter under the condition of nitrogen pressure ≤ 200 psi. This step was repeated 10 times to obtain a transparent liposome suspension.

[0049] Put the suspension into a dialysis bag, use 0.9% sodium chloride solution as the dialysate, incubate overnight at room temperature, and change the dialysate every 2 hours to completely remove f...

Embodiment 2

[0053] The preparation of the triamcinolone acetonide acetate liposome eye drops of embodiment 2 chitosan modification

[0054] The triamcinolone acetonide acetate liposome suspension wrapped in chitosan in Example 1 was mixed with sodium hyaluronate eye drops, the drug concentration was adjusted, and the concentration of triamcinolone acetonide acetate was controlled to be 1.5mg / mL to obtain chitosan Sugar-modified triamcinolone acetonide liposomal eye drops. Store at 4°C.

Embodiment 3

[0055] Embodiment 3 drug loading rate and encapsulation efficiency determination

[0056] Chromatographic conditions: the chromatographic column is a Hypersil ODS column (250mm×4.6mm, 5μm), methanol-water-ether (volume ratio 68:32:4) is the mobile phase, the ultraviolet detection wavelength is 240nm, the column temperature is 30°C, and the flow rate is 1.0mL. min -1 , the injection volume was 20 μL, and the internal standard method was used for quantification.

[0057] Draw 1ml of chitosan-modified triamcinolone acetonide liposome eye drops into a 10mL volumetric flask, add methanol to disperse and dissolve completely, filter through a 0.22 μm microporous membrane, transfer to a 10mL volumetric flask and use mobile phase to make up the volume To the scale, shake well to get the sample solution, inject 20 μL for chromatographic analysis, and determine the total mass of triamcinolone acetonide acetate. 药 .

[0058] Another equivalent amount of chitosan-modified triamcinolone ...

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Abstract

The invention belongs to the field of pharmaceutical preparations and in particular relates to chitosan modified triamcinolone acetonide acetate lipidosome eye drops and a preparation method thereof.The invention provides chitosan modified triamcinolone acetonide acetate lipidosome prepared prepared by a calcium acetate gradient method. The preparation method comprises the following steps: preparing a lipid membrane from soya bean lecithin and cholesterol, adding a calcium acetate solution to prepare blank liposome, adding triamcinolone acetonide acetate to obtain triamcinolone acetonide acetate lipidosome, and performing chitosan coating, thereby obtaining the chitosan modified triamcinolone acetonide acetate lipidosome. The lipidosome has excellent pharmaceutical property, the liposomesurface presents positive charge, and the lipidosome and a sodium hyaluronate solution are prepared into the eye drops, so that the water solubility of the triamcinolone acetonide acetate and the adsorptivity to cornea can be improved, and the drug toxicity can be reduced. Compared with injection, the chitosan modified triamcinolone acetonide acetate lipidosome eye drops are simple and safe to use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a chitosan-modified triamcinolone acetate liposome and a preparation method. Background technique [0002] Triamcinolone acetonide acetate is a long-acting glucocorticoid. The drug has strong and long-lasting anti-inflammatory and anti-allergic effects. It is mainly used in the field of ophthalmology to treat diseases such as uveitis, macular edema, and age-related macular degeneration. The administration of triamcinolone acetonide acetate is mainly local administration, including subconjunctival injection, retrobulbar injection and intravitreal injection. Long-term and multiple administration is required. Complications include ocular hypertension, endophthalmitis, intraocular hemorrhage, cataract , retinal toxicity, etc. In ophthalmic clinical practice, eye drops are convenient to use and well tolerated, and are the preferred dosage form of ophthalmic medicine. Howev...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/36A61K31/58A61K9/08A61P29/00A61P37/08A61P27/02
CPCA61K9/0048A61K9/08A61K9/127A61K9/1278A61K31/58A61K47/36A61P27/02A61P29/00A61P37/08
Inventor 曲毅程同杰李靳
Owner SHANDONG UNIV QILU HOSPITAL
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