Cyclosporin ophthalmic emulsion and preparation method thereof

A technology for cyclosporine and ophthalmic use, which is applied in the field of cyclosporine ophthalmic emulsion and its preparation, which can solve the problems of prolonging drug release time and inapplicability, and achieve the effect of strengthening effect, promoting healing and improving absorption

Active Publication Date: 2021-03-30
WUHAN CONFORM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This oral preparation has the characteristics of stable release, but it uses microemulsion technology, which does not have the function of prolonging the release time of the drug. At the same time, it is an oral solid preparation and is not suitable for eye administration.

Method used

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  • Cyclosporin ophthalmic emulsion and preparation method thereof
  • Cyclosporin ophthalmic emulsion and preparation method thereof
  • Cyclosporin ophthalmic emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The cyclosporine ophthalmic emulsion prepared in the present embodiment, by mass percentage: cyclosporine 0.03%, collagen 2.0%, castor oil 1.4%, glycerin 2.2%, anthocyanin 0.06%, polysorbate 80 0.8%, remaining The amount is double distilled water, and the anthocyanins are ginkgo anthocyanins with a purity of 90%.

[0027] Above-mentioned cyclosporine ophthalmic emulsion preparation method:

[0028] S1. Under nitrogen protection, weigh castor oil, polysorbate 80, and cyclosporine, mix and stir at 70°C for 10 minutes to obtain the mixed solution I;

[0029] S2. Under nitrogen protection, add 80% by weight of double-distilled water, glycerin, and collagen to the mixed solution I, and shear and emulsify at 10,000 rpm at 70°C for 45 minutes to obtain the mixed solution II;

[0030] S3. Dissolve the anthocyanins in the remaining double-distilled water and mix with the mixed solution II, disperse at 60°C and 5500rpm for 100min, adjust the pH to 6.5-8.0, stir for 40min, and fi...

Embodiment 2

[0032] The cyclosporine ophthalmic emulsion prepared in the present embodiment, by mass percentage: cyclosporine 0.05%, collagen 2.5%, castor oil 1.2%, glycerin 2.0%, anthocyanin 0.05%, polysorbate 80 0.9%, remaining The amount is double distilled water, and the anthocyanins are ginkgo anthocyanins with a purity of 90%.

[0033] The preparation method of the cyclosporine ophthalmic emulsion of this embodiment is the same as that of Example 1.

Embodiment 3

[0035] The cyclosporine ophthalmic emulsion prepared in the present embodiment, by mass percentage: cyclosporine 0.05%, collagen 2.5%, castor oil 1.2%, glycerin 2.0%, anthocyanin 0.08%, polysorbate 80 0.9%, remaining The amount is double distilled water, and the anthocyanins are ginkgo anthocyanins with a purity of 88.5%.

[0036] The preparation method of the cyclosporine ophthalmic emulsion of this embodiment is the same as that of Embodiment 1.

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Abstract

The cyclosporin eye emulsion is prepared from the following components in percentage by mass: 0.01 to 0.05 percent of cyclosporin, 1.5 to 3 percent of collagen, 1.2 to 1.5 percent of castor oil, 1.8 to 2.5 percent of glycerol, 0.04 to 0.08 percent of anthocyanin, 0.8 to 1.2 percent of polysorbate 80 and the balance of double distilled water. The cyclosporin ophthalmic emulsion is prepared throughhigh-speed dispersion and shear emulsification, and collagen and anthocyanin in the emulsion are combined for use, so that the slow-release effect of the medicine can be effectively enhanced, and theresidual quantity of the medicine in corneas is increased.

Description

technical field [0001] The invention belongs to the technical field of ophthalmic drugs, and in particular relates to cyclosporine ophthalmic emulsion and a preparation method thereof. Background technique [0002] Cyclosporine, also known as cyclosporin A (i.e. Cyclosporin A or Cyclosporine, referred to as CsA), is a non-polar cyclic oligopeptide drug composed of 11 amino acid residues, soluble in organic solvents, almost insoluble in water. It is mainly used clinically for organ transplantation, anti-rejection therapy after bone marrow transplantation and the treatment of autoimmune diseases. Studies at home and abroad have shown that it plays a role by inhibiting the aggregation of inflammatory cells and the release of inflammatory factors, reducing the infiltration of lymphocytes in lacrimal gland and conjunctival tissue, and inhibiting the apoptosis of ocular surface tissues such as lacrimal gland and conjunctival goblet cells. Sporins can be used as a local immunomod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/42A61K47/44A61K47/22A61K47/26A61K38/13A61P27/02A61P37/02A61P37/06
CPCA61K9/107A61K9/0048A61K47/42A61K47/44A61K47/22A61K47/26A61K38/13A61P27/02A61P37/02A61P37/06
Inventor 牟东升周小顺刘文双吴欢
Owner WUHAN CONFORM PHARMA CO LTD
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