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Cyclosporine-containing ophthalmic emulsion gel and preparation method thereof

A technology of cyclosporine and emulsion, which is applied in the field of medicine, can solve the problems of patients' intolerance, high permeability, eye irritation, etc., and achieve the goal of reducing gastrointestinal irritation, fully absorbing and utilizing it, and reducing other side effects Effect

Inactive Publication Date: 2012-07-04
WUXI XINRENTANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large molecular weight and high permeability of cyclosporine, it is difficult to achieve therapeutic effects for the treatment of intraocular inflammation, such as autoimmune uveitis, and systemic administration is prone to high blood pressure, liver and kidney toxicity, so the development Topically administered cyclosporine A extended-release formulation as a breakthrough
Cyclosporine A has a large relative molecular weight and strong lipophilicity. It is almost insoluble in water and has poor corneal permeability when administered locally.
Therefore, cyclosporine is mostly made into various vegetable oil eye drops at home and abroad, but these oily eye drops have low bioavailability and are irritating to the eyes, and patients usually cannot tolerate them.

Method used

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  • Cyclosporine-containing ophthalmic emulsion gel and preparation method thereof
  • Cyclosporine-containing ophthalmic emulsion gel and preparation method thereof
  • Cyclosporine-containing ophthalmic emulsion gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Ophthalmic emulsion gel containing cyclosporine, the formula is as follows: cyclosporine A 0.2%, peanut oil 2%, carbomer 5%, sodium chloride 0.1%, Tween 80 5%, NAOH appropriate amount, add water for injection into 150g ophthalmic emulsion gel containing cyclosporine.

[0033] The steps are:

[0034] (1) Preparation of emulsion:

[0035] a. Preparation of oil phase: Precisely weigh cyclosporine A into a 10mL eggplant-shaped bottle, add peanut oil to dissolve cyclosporine A, then add pH regulator sodium hydroxide to adjust pH to 7, and obtain the oil phase;

[0036] b. Preparation of the water phase: accurately weigh the prescription amount of Tween 80 to 1 part of water for injection to obtain the water phase;

[0037] c. Mixing: Weigh the oil phase according to the ratio of oil phase: water phase to 1:5 and add it to the water phase to obtain the emulsion after mixing;

[0038] (2) Swelling of the gel matrix: Take 10 parts of water for injection into a beaker, spread...

Embodiment 2

[0041] Ophthalmic emulsion gel containing cyclosporine, the formula is as follows: cyclosporine A 0.4%, dimethyl sulfoxide 3%, glyceryl monostearate 0.3%, sodium hyaluronate 5%; mannitol 4%; hydrogen Appropriate amount of sodium oxide, add water for injection to make 150g ophthalmic emulsion gel containing cyclosporine.

[0042] The steps are:

[0043] (1) Preparation of emulsion:

[0044] a. Preparation of oil phase: Accurately weigh cyclosporine A into a 10mL eggplant-shaped bottle, add dimethyl sulfoxide to dissolve cyclosporine A, then add a pH regulator to adjust the pH to 7, and then obtain the oil phase;

[0045] b. Preparation of the water phase: Accurately weigh glycerol monostearate into 1 part of water for injection to obtain the water phase;

[0046] c. Mixing: Weigh the oil phase according to the ratio of oil phase: water phase of 1:15 and add it to the water phase, and then get the emulsion after mixing;

[0047] (2) Swelling of the gel matrix: Take 10 parts o...

Embodiment 3

[0050] Ophthalmic emulsion gel containing cyclosporine, the formula is as follows: cyclosporine A 0.1%, soybean oil 3%, polyvinyl alcohol 0.3%, hydroxymethylcellulose sodium 3%; glycerin 3%; sodium hydroxide appropriate amount, Add water for injection to make 150 g ophthalmic emulsion gel containing cyclosporine.

[0051] The steps are:

[0052](1) Preparation of emulsion:

[0053] a. Preparation of oil phase: Accurately weigh cyclosporine A into a 10mL eggplant-shaped bottle, add soybean oil to dissolve cyclosporine A, then add a pH regulator to adjust the pH to 7, and then obtain the oil phase;

[0054] b. Preparation of the water phase: Precisely weigh polyvinyl alcohol into 1 part of water for injection to obtain the water phase;

[0055] c. Mixing: Weigh the oil phase according to the ratio of oil phase: water phase of 1:20 and add it to the water phase to obtain the emulsion after mixing;

[0056] (2) Swelling of the gel matrix: Take 10 parts of water for injection in...

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Abstract

The invention relates to cyclosporine-containing ophthalmic emulsion gel and a preparation method thereof, and belongs to the technical field of medicine. The preparation method for the cyclosporine-containing ophthalmic emulsion gel comprises the following steps of: mixing and dissolving high-grade fatty acid glyceride and hydrophobic medicinal cyclosporine in a ratio, adding a pH regulator to regulate the pH, and thus obtaining an oil phase; dissolving a hydrophilic polymer into injection water in a ratio, and thus obtaining an aqueous phase; weighing the oil phase in a certain ratio, adding the oil phase into the aqueous phase, and mixing to obtain emulsion; taking a prescription dose of injection water to a beaker, spreading a prescription dose of gel matrix on the surface of the injection water, standing and swelling; mixing and stirring the emulsion and the gel uniformly, adding the pH regulator to regulate the pH, and adding an osmotic pressure regulator to regulate the osmotic pressure of a mixed solution to be 200-350 Osmol / kg; and packaging the obtained emulsion gel, performing hot pressing and sterilization, and thus obtaining the cyclosporine-containing ophthalmic emulsion gel. The cyclosporine A emulsion gel directly acts on an affected part, and can fully and effectively exert the effects and reduce gastrointestinal irritation and other side effects caused by oral medicaments.

Description

technical field [0001] The invention relates to an ophthalmic emulsion gel containing cyclosporine and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cyclosporin is cyclosporine (cyclosporin A), which is a specific immunosuppressant. Cyclosporin A is commonly used in clinical practice and is currently recognized as an effective drug against organ transplant rejection. It selectively inhibits Helper lymphocytes interfere with the activity of lymphocytes, block the humoral and cellular effector mechanisms involved in rejection, thereby inhibiting rejection and immune responses. Oral preparations and injections of ciclosporin are widely used for rejection after organ transplantation, and cyclosporine eye drops are mainly used in the treatment of corneal transplant rejection, autoimmune eye disease, and dry eye in ophthalmology. Due to the large molecular weight and high permeability of cyclosporine, it is difficult to ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K38/13A61P37/06A61P27/02
Inventor 毛宇锋
Owner WUXI XINRENTANG PHARMA TECH
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