Micro/sub-micro emulsion in situ gel rubber preparation of cyclosporins A for eyes and preparation thereof

A technology of in-situ gel and cyclosporine, which is applied in the direction of medical preparations of non-active ingredients, cyclic peptide ingredients, pharmaceutical formulas, etc., can solve the inconvenience of industrial production and filling, does not have pseudoplastic deformation, and clinical Inconvenient medication and other problems, to achieve the effect of easy and accurate control of dosage, good toxic and side effects, and easy industrial production

Inactive Publication Date: 2008-08-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Common gels of emulsions or microemulsions have the following defects: ① common gels have a high viscosity in vitro, poor fluidity, and inconvenient clinical use; ② high viscosity, easy to generate a large number

Method used

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  • Micro/sub-micro emulsion in situ gel rubber preparation of cyclosporins A for eyes and preparation thereof
  • Micro/sub-micro emulsion in situ gel rubber preparation of cyclosporins A for eyes and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0050] Example 1

[0051] Prescription composition:

[0052] Cyclosporin A 0.5g

[0053] Castor oil 6g

[0054] Polyoxyethylene castor oil 15g

[0055] Sodium Alginate 10g

[0056] Glycerin 26g

[0057] Appropriate amount of borax

[0058] Benzalkonium Chloride 0.05g

[0059] Add purified water to 1000ml

[0060] Preparation method: weigh each component according to the prescription composition, mix castor oil, polyoxyethylene castor oil and glycerin (6g) uniformly at 60°C, and then dissolve cyclosporin A in the mixture. Add an appropriate amount of purified water, shear and emulsify to obtain colostrum, and then use a high-pressure homogenizer to homogenize (the pressure is about 140,000kPa, homogenize for 4 hours), and the obtained product is filtered with a 0.45μm microporous membrane; then the alginic acid Sodium and the remaining amount of glycerin (20g) were dissolved in an appropriate amount of purified water, and then mixed with the emulsion, adjusted to pH 6.2...

Example Embodiment

[0065] Example 2

[0066] Prescription composition:

[0067] Cyclosporin A 4g

[0068] Castor oil 6g

[0069] Tween 80 45g

[0070] Propylene glycol 30g

[0071] Gellan Gum 10g

[0072] Glycerin 2g

[0073] Appropriate amount of trishydroxymethyl aminomethane

[0074] Chlorobutanol 0.5g

[0075] Add purified water to 1000ml

[0076] Preparation method: weigh each component according to the composition of the prescription, mix castor oil, Tween 80 and propylene glycol uniformly at 60°C, and then dissolve cyclosporin A in the mixture. Add an appropriate amount of purified water, shear and emulsify to obtain colostrum (pressure about 60,000kPa, homogenize for 1 hour), and filter the obtained colostrum with a 0.45μm microporous membrane; then dissolve gellan gum and glycerin in an appropriate amount of purified water, and then mix it with the emulsion, and adjust the pH to 6.2-8.0 with tris hydroxymethylaminomethane solution; then, add the prescribed amount of chlorobutan...

Example Embodiment

[0077] Example 3

[0078] Prescription composition:

[0079] Cyclosporin A 3g

[0080] Tricaprylic Capric Glyceride 6g

[0081] Polyoxyethylene hydrogenated castor oil 15g

[0082] Sodium Alginate 15g

[0083] Glycerin 20g

[0084] Appropriate amount of sodium hydroxide

[0085] Benzalkonium Bromide 0.05g

[0086] Add purified water to 1000ml

[0087] Preparation method: weigh each component according to the composition of the prescription, mix tricaprylic capric glyceride and polyoxyethylene hydrogenated castor oil uniformly at 60°C, and then dissolve cyclosporin A in the mixture. Add an appropriate amount of purified water, shear and emulsify to obtain colostrum, and then use a high-pressure homogenizer to homogenize (the pressure is about 100,000kPa, homogenize for 1 hour), and the obtained product is filtered with a 0.45μm microporous membrane; then the alginic acid Dissolve sodium and glycerin in an appropriate amount of purified water, mix it with the emulsion, a...

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Abstract

The invention relates to an ophthalmic microemulsion/submicron emulsion in situ gel preparation with cyclosporine A and the preparation method. The preparation is prepared through shearing and high pressure homogenization process using cyclosporine A, oil phase, emulsifier, coemulsifier, thickener, isosmotic adjustment agent, bacteriostat, pH regulator and purified water. The invention is characterized in that safe and nonirritant nonionic surface-active material polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, tween or phosphatides are adopted as the emulsifier; macromolecular material with ion and/or pH sensitive properties is used as the thickener. The average particle size of emulsion drops of the ophthalmic microemulsion/submicron emulsion in situ gel preparation is less than 200nm; the cumulative value of 90% particle size is no more than 500nm; as low-viscosity liquid with good fluidity outside the body, the ophthalmic microemulsion/submicron emulsion in situ gel preparation can rapidly form hydrogel after being dropped into eyes, thereby increasing residence time of the medicine and bioavailability. The ophthalmic microemulsion/submicron emulsion in situ gel peparation has the advantages of no stimulation and poison and side effect to eyes and stable quality of the preparation.

Description

technical field [0001] The present invention relates to a micro / submicroemulsion in-situ gel preparation, in particular to an ophthalmic micro / submicroemulsion ion and / or pH-sensitive in-situ gel preparation containing cyclosporin A, specifically a A macromolecular solution containing micro / submicroemulsion, which forms a gel on the surface of the cornea quickly after being administered in the form of eye drops, thereby achieving the purpose of delaying the elimination of drugs, improving ocular residence time and local bioavailability. The invention also relates to a preparation method of ophthalmic micro / submicroemulsion in-situ gel preparation. Background technique [0002] Cyclosporin A is a non-polar cyclic oligopeptide drug with immunosuppressive activity, mainly used for anti-rejection therapy of autoimmune diseases and organ suppression. Cyclosporine selectively inhibits immunocompetent cells, especially T lymphocytes. Therefore, cyclosporine A can be used as a loc...

Claims

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Application Information

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IPC IPC(8): A61K38/13A61K9/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P27/02A61P37/06A61K47/14A61K47/26
Inventor 甘勇甘莉马守伟朱春柳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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