Ophthalmic medicinal composition containing sirolimus

A composition and drug technology, applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as adverse reactions and unsatisfactory drug effects, and achieve the effect of less adverse reactions

Inactive Publication Date: 2014-06-18
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The inventor's Chinese patent applications No. 201210188186.9 and No. 201210188187.3 are based on the significant immunosuppressive effect of sirolimus in organ transplant patients, using a sustained release system to prepare sirolimus eye drops for the treatment of uvea Inflammation, although it has a certain curative effect, its efficacy is not ideal, and there are many adverse reactions

Method used

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  • Ophthalmic medicinal composition containing sirolimus
  • Ophthalmic medicinal composition containing sirolimus
  • Ophthalmic medicinal composition containing sirolimus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0024] Example 1-3 Preparation of Compound Sirolimus Eye Drops

[0025] The raw material components and consumptions used for preparing compound sirolimus eye drops are as follows:

[0026]

[0027] Preparation method: take a small amount of water for injection, first add co-solvent, then add sirolimus, astragalus polysaccharide, sodium tanshinone IIA sulfonate and rehmannia glutinosa extract, stir and dissolve into liquid A, set aside; thickener and surfactant Use water for injection to disperse and let it cool down, the liquid is B liquid, and use it for later use; in addition, dissolve the osmotic pressure regulator and bacteriostatic agent with water for injection, stir well and filter to obtain C liquid. Combine the two liquids B and C, then add the dissolved liquid A, add water for injection to the full amount, filter, and pack to obtain. A pH regulator is used to adjust the pH value of the finished eye drops to 5.5-7.5.

Embodiment 4-6

[0028] Example 4-6 Preparation of compound sirolimus ophthalmic gel

[0029] The raw material components and consumptions used for preparing the compound sirolimus ophthalmic gel are as follows:

[0030]

[0031] Preparation method: take a small amount of water for injection, first add co-solvent, then add sirolimus, astragalus polysaccharide, sodium tanshinone IIA sulfonate and rehmannia glutinosa extract, stir and dissolve into liquid A, set aside; thickener and surfactant Use water for injection to disperse and let it cool down, the liquid is B liquid, and use it for later use; in addition, dissolve the osmotic pressure regulator and bacteriostatic agent with water for injection, stir well and filter to obtain C liquid. Combine the two liquids B and C, then add the dissolved liquid A, add water for injection to the full amount, filter, and pack to obtain. A pH regulator is used to adjust the pH value of the finished eye drops to 5.5-7.5.

[0032] Preparation method:...

Embodiment 7-9

[0034] Example 7-9 Preparation of Compound Sirolimus Ophthalmic Ointment

[0035] The used raw material components and consumption of preparation compound sirolimus eye ointment are as follows:

[0036]

[0037] Preparation method: take a small amount of water for injection, first add co-solvent, add sirolimus, astragalus polysaccharide, sodium tanshinone ⅡA sulfonate and rehmannia glutinosa extract, stir to dissolve, filter aseptically; add appropriate amount of sterilized and cooled liquid paraffin , grind into a fine paste, pass through a 200-mesh sieve, then gradually add sterile and filtered lanolin and yellow petrolatum mixture, mix well, and obtain.

[0038] According to the technical solution of the present invention, the types of excipients that can be used to prepare sirolimus ophthalmic preparations are not limited to those listed in the above table, and the following multiple options can also be selected.

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Abstract

The invention discloses an ophthalmic medicinal composition containing sirolimus. The composition comprises the following active components: sirolimus, astragalus polysaccharide, sodium tanshinone IIA silate and raw rehmannia extract. The active components are prepared into an ophthalmic external preparation by a conventional method, and the preparation is suitable for treatment of uveitis, rejection reaction after corneal transplantation and other ophthalmic immunological diseases, and has good drug effect and small side effect compared with common sirolimus ophthalmic preparations.

Description

technical field [0001] The invention relates to medical preparations, in particular to pharmaceutical compositions for treating ocular immune diseases such as uveitis and rejection after corneal transplantation. Background technique [0002] Uveitis is a general term for a class of intraocular inflammatory diseases, including inflammation that occurs in the uvea, retina, retinal blood vessels, and vitreous body. It is a common blinding eye disease worldwide. Most uveitis is caused by immune mechanism, and its treatment mainly uses immunosuppressant, such as glucocorticoid. However, immunosuppressants are mostly used systemically, which can cause a variety of side effects, and some drugs also have hepatotoxicity, nephrotoxicity and gastrointestinal reactions. [0003] Graft rejection occurs in about 30% of corneal transplants, which is the main cause of corneal transplant failure. Hormone therapy and cyclosporine therapy have certain effects, but often cannot completely con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/804A61P27/02A61P37/06A61P37/02A61K31/436A61K31/715A61K31/58
Inventor 刘奕志王延东曾阳发刁红星
Owner ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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