Tacrolimus eye ointment for cornea transplantation and preparation method thereof

A technology of tacrolimus and crolimus eye, which is applied in the field of tacrolimus ophthalmic precursor vesicles and its preparation, can solve problems such as difficult industrial production, difficult effective treatment level, and difficult clinical application. Achieve good development potential, improve storage stability, and increase corneal permeability

Inactive Publication Date: 2013-06-12
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main disadvantage of tacrolimus liposome preparation is that it is difficult to sterilize and sterilize, the preparation is complicated and the cost is high, and it is easy to oxidize and produce toxicity, so it is relatively difficult in clinical application; tacrolimus cyclodextrin inclusion complex eye drops is used for After topical administration to the eye, the drug on the ocular surface is easily cleared quickly, and it is difficult for the drug to maintain its efficacy for a long time; tacrolimus nanoparticle preparation can prolong the residence time of the drug in the cornea and increase the concentration of the drug entering the cornea, but the nanoparticle preparation Organic solvents are easily introduced during the preparation process, and residual solvents are not accepted clinically; tacrolimus sustained-release collagen film is a translucent and soft film similar to a contact lens, which is extracted from pig or bovine sclera. It is not easy to realize industrial production, and the patient compliance is poor
[0009] The strong hydrophobicity and unstable characteristics of tacrolimus determine its problems in topical ophthalmic use: it is easy to isomerize when it meets water, and its intraocular permeability is poor, so it is difficult to reach an effective therapeutic level in the eye, making it low bioavailability

Method used

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  • Tacrolimus eye ointment for cornea transplantation and preparation method thereof
  • Tacrolimus eye ointment for cornea transplantation and preparation method thereof
  • Tacrolimus eye ointment for cornea transplantation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of tacrolimus ophthalmic precursor vesicles

[0041]

[0042] Preparation Process:

[0043] Weigh 24.3g of Tween-80, 27g of ethanol, 24.3g of soybean lecithin, and 2.7g of cholesterol, heat in a water bath at 65±5°C and keep stirring until each component is completely dissolved and becomes uniform and transparent. Add 0.08g of tacrolimus raw material drug into the solution, and continue to stir at 65±5°C until the drug is completely dissolved in the mixed solution, as solution 1; add 21.62g of water for injection dropwise to solution 1 under magnetic stirring, 65 Continue heating and stirring at ±5°C until the solution is uniformly mixed, take the mixed solution out of the water bath and stir it magnetically until its temperature drops to room temperature, and the mixture is in a viscous gel state to obtain 100 g of tacrolimus precursor vesicles.

[0044] The tacrolimus precursor vesicles are automatically filled into 5ml, 10ml, and 20ml eye ...

Embodiment 2

[0045] Example 2 Preparation of tacrolimus ophthalmic precursor vesicle preparation:

[0046]

[0047] Preparation Process:

[0048] Weigh Span-80, ethanol, soybean lecithin, and cholesterol, heat in a water bath at 65±5°C and keep stirring until each component is completely dissolved and becomes uniform and transparent, then add tacrolimus raw material drug into the mixture under stirring , continue to stir at 65±5°C until the drug is completely dissolved in the mixed solution as solution 1; add water for injection dropwise to solution 1 under stirring, continue heating and stirring at 65±5°C until the solution is evenly mixed, and mix The solution was taken out from the water bath and stirred until its temperature dropped to room temperature, and the mixture was in a viscous gel state to obtain 224 g of tacrolimus precursor vesicles.

[0049] The tacrolimus precursor vesicles are automatically filled into 5ml, 10ml, and 20ml eye drop bottles, three specifications, t...

Embodiment 3

[0050] Example 3 Preparation of tacrolimus ophthalmic precursor vesicle preparation

[0051]

[0052] Preparation Process:

[0053] Weigh poloxamer-188, ethanol, egg yolk lecithin, and cholesterol, heat in a water bath at 65±5°C and stir continuously until each component is completely dissolved and becomes uniform and transparent, then add tacromer into the mixture while stirring Add 0.5g of raw material drug, continue to stir at 65±5°C until the drug is completely dissolved in the mixed solution, and use it as solution 1; add 0.1% glycerin aqueous solution dropwise to solution 1 under stirring, continue heating and stirring at 65±5°C Until the solution is mixed evenly, let the temperature drop to room temperature under stirring, and the mixture is in a viscous gel state to obtain 100 g of tacrolimus precursor vesicles.

[0054] The tacrolimus precursor vesicles are automatically filled into 5ml, 10ml, and 20ml eye drop bottles, three specifications, the filling volume ...

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Abstract

The invention discloses a tacrolimus eye ointment for cornea transplantation and a preparation method thereof, belongs to the field of pharmaceutical preparation and particularly relates to a tacrolimus eye precursor vesicle capsule for cornea transplantation and a preparation method thereof. The precursor vesicle capsule comprises the following raw materials in percentage by weight: 0.04-0.8% of tacrolimus, 4.0-41.0% of surfactant, 1.6-8.0% of cholesterol, 4.0-41.0% of lecithin, 1.2-30.% of alcohol, and the balance of water or 0,1% of glycerol aqueous solution or phosphate buffer with PH of 7.4, wherein the surfactant is one of span, tween, polyoxyethylene ether castor oil and poloxamer, and the alcohol is one of ethanol, isopropanol, butanol and propanol. The tacrolimus precursor vesicle capsule has limited moisture, and the storage stability of the preparation can be improved; the product organically combines the advantages of the precursor vesicle capsule, the characteristics of an eye dosing system and the indication disease of the tacrolimus drugs, so as to achieve the advantages of improving the curative effect, reducing the side effect, and bringing convenience in administration; and the preparation technique is simple and convenient and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically relates to a tacrolimus ophthalmic precursor vesicle used for corneal transplantation and a preparation method thereof. Background technique [0002] Corneal disease is currently the main blinding corneal disease, corneal transplantation is the most direct and effective method to treat such diseases, and immune rejection after corneal transplantation is the main reason for failure. At present, some drugs such as corticosteroids, immunosuppressants and cyclosporin A are used clinically to reduce the incidence of immune rejection. Glucocorticoids are the main means to prevent and treat postoperative graft rejection, but their long-term application can not only lead to various complications, but also often cannot effectively inhibit the rejection of high-risk keratoplasty. Cyclosporin A is more and more widely used in ophthalmology, but cyclosporine eye drops are oil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/436A61P27/02A61P37/06A61K9/48
Inventor 徐月红李琦
Owner SUN YAT SEN UNIV
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