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Lipid-emulsion eye drops with dexamethasone and preparation method thereof

A technology of dexamethasone lipid and dexamethasone, applied in the field of medicine, can solve the problems of subconjunctival scarring, loss, adhesion and the like, and achieve the effects of increasing drug concentration, increasing drug concentration and prolonging residence time

Inactive Publication Date: 2017-05-31
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, intraocular injection is invasive, and multiple injections need to be repeated during the treatment process, which may lead to subconjunctival scarring and adhesion; the injection process is easy to puncture the cornea or cause bleeding, which undoubtedly increases the risk of endophthalmitis. The occurrence of endophthalmitis may lead to irreversible damage or even loss of vision of the patient, which is also a technical problem that plagues those skilled in the art

Method used

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  • Lipid-emulsion eye drops with dexamethasone and preparation method thereof
  • Lipid-emulsion eye drops with dexamethasone and preparation method thereof
  • Lipid-emulsion eye drops with dexamethasone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051]

[0052]

[0053]Preparation method: Dissolve the prescription amount of egg yolk lecithin PL-100M and dexamethasone in a mixed solvent of ethanol and acetone (1:1, v / v), the mixed solvent is 200g; evaporate under reduced pressure at 40°C to remove the solvent to form the drug and A mixture of phospholipids, the mixture is dispersed into the prescription amount of medicinal soybean oil to form an oil phase, another prescription amount of Poloxamer 188 emulsifier is dissolved in an appropriate amount of water, and then the aqueous solution containing glycerin is mixed with the oil phase , 800rpm shear emulsification for 10min, vested colostrum. Adjust the pressure of the secondary valve of the high-pressure homogenizer to 200-300 bar, homogenize for 2 minutes to make the distribution of the refined particles more uniform, then adjust the primary valve between 500-600 bar, and cycle 10 times of homogenization treatment to make the material fully In the narrow area c...

Embodiment 2

[0055]

[0056]

[0057] Preparation method: Dissolve the prescribed amount of LIPOID E 80 and dexamethasone in a mixed solvent of ethanol and acetone (1:3, v / v), the mixed solvent is 100 g; evaporate the solvent under reduced pressure at 40°C to form a mixture of drug and phospholipid , disperse the mixture into the prescribed amount of medicinal soybean oil to form an oil phase, and dissolve another prescribed amount of Solutol HS15 emulsifier in an appropriate amount of water, then mix the aqueous solution containing the emulsifier with the oil phase, and emulsify at 800rpm for 10min. Vested colostrum. Adjust the pressure of the secondary valve of the high-pressure homogenizer to 200-300 bar, homogenize for 2 minutes to make the distribution of the refined particles more uniform, then adjust the primary valve between 500-600 bar, and cycle 10 times of homogenization treatment to make the material fully In the narrow area composed of the valve core, valve seat and impa...

Embodiment 3

[0059]

[0060] Preparation method: Dissolve the prescribed amount of LIPOID S 75 and dexamethasone in a mixed solvent of ethanol and acetone (1:2, v / v), the mixed solvent is 140 g; evaporate the solvent under reduced pressure at 40°C to form a mixture of drug and phospholipid , disperse the mixture into the medicinal soybean oil of the prescribed amount to form an oil phase, and dissolve the Cremophor EL emulsifier of the prescribed amount in an appropriate amount of water, then mix the aqueous solution containing the emulsifier with the oil phase, and emulsify at 800rpm for 10min. Vested colostrum. Adjust the pressure of the secondary valve of the high-pressure homogenizer to 200-300 bar, homogenize for 2 minutes to make the distribution of the refined particles more uniform, then adjust the primary valve between 500-600 bar, and cycle 10 times of homogenization treatment to make the material fully In the narrow area composed of the valve core, valve seat and impact ring,...

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Abstract

The invention provides lipid-emulsion eye drops with dexamethasone. The lipid-emulsion eye drops are in an oil-in-water sub-micro emulsion system; grease in the emulsion drops is coated with lipid nano particles formed by lipid carriers and the dexamethasone. The invention aims at providing the lipid-emulsion eye drops with the dexamethasone and a preparation method thereof so as to increase tissue distribution in the eyes, promote permeation into the eyes and further achieve the purposes of safely and effectively treating intraocular diseases and fundus oculi diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a dexamethasone lipid emulsion eye drop and a preparation method thereof. Background technique [0002] Dexamethasone is a commonly used drug for the treatment of intraocular inflammation, especially macular degeneration, but the therapeutic effect of traditional eye drops is limited by the fact that the drug is difficult to enter the intraocular tissue, and the amount of distribution in the eye is small. The effect for posterior segment disease was not significant. [0003] Therefore, the treatment of intraocular or posterior segment diseases such as iris, ciliary body and other endophthalmitis, vitreous hemorrhage or retinal macular degeneration requires clinical administration methods such as intravenous injection, vitreous injection, and conjunctival injection. [0004] However, intraocular injection is invasive, and multiple injections need to be repeated during the treatm...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/127A61K47/44A61K31/573A61P27/02
CPCA61K9/0048A61K9/1075A61K9/127A61K31/573A61K47/44
Inventor 吕竹芬班俊峰陈燕忠张彦方若槐
Owner GUANGDONG PHARMA UNIV
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