Eye sterile suspension containing loteprednol etabonate and preparation method thereof

A technology of loteprednol etabonate and suspension, applied in the field of ophthalmic sterile suspension, can solve the problem of affecting crystal form and stability, failing to pass through a sterile filter, and not mentioning loteprednol etabonate. Nuo sterilization problems and other issues

Inactive Publication Date: 2009-04-29
马晶
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Secondly, the sterilization process of the ophthalmic sterile suspension is very important to the quality and stability of the product, because loteprednol etabonate is insoluble in water, exists in the form of crystalline particles in the suspension, and cannot pass through the 0.22μm The bacteria-removing filter membrane, damp heat sterilization can affect its crystal form and stability, and the sterilization problem of loteprednol etabonate is not mentioned in the above-mentioned published patent

Method used

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  • Eye sterile suspension containing loteprednol etabonate and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Loteprednol etabonate 5.0g

[0018] Tobramycin 3.0g

[0019] Glycerin 25.0g

[0020] Hypromellose 3.0g

[0021] Chlorobutanol 5.0g

[0022] Tween-80 2.0g

[0023] Edetate Disodium 0.5g

[0024] Appropriate amount of water for injection

[0025] Makes 1000ml

[0026] Micronized with loteprednol carbonate, sterilized by dry heat at 150°C; hypromellose was swollen with water, sterilized at 121°C for 20 minutes, cooled, and set aside; tobramycin, glycerin, chlorobutanol, Dissolve Tween-80 and edetate disodium in water, filter and sterilize with a 0.22 μm sterile filter membrane, add hypromellose to the aqueous solution, add loteprednol etabonate microcrystals while stirring, stir Evenly, adjust the pH value to 5-6. Subpackage.

Embodiment 2

[0028] Loteprednol etabonate 5.0g

[0029] Tobramycin 3.0g

[0030] Sodium chloride 8.0g

[0031] Hypromellose 4.0g

[0032] Chlorobutanol 3.0g

[0033] Tween-80 3.0g

[0034] Edetate Disodium 0.6g

[0035] Appropriate amount of water for injection

[0036] Makes 1000ml

[0037] Micronized with loteprednol carbonate, sterilized by dry heat at 160°C; hypromellose was swollen with water, sterilized at 115°C for 30 minutes, cooled, and set aside; tobramycin, sodium chloride, chlorotert-butyl Dissolve alcohol, Tween-80, and edetate disodium in water, filter and sterilize with a 0.22 μm sterile filter membrane, add hypromellose to the aqueous solution, and add loteprednol etabonate microcrystals while stirring , stir well, and adjust the pH value to 5-6. Subpackage.

Embodiment 3

[0039] Loteprednol etabonate 5.0g

[0040] Glycerin 13g

[0041] Sodium chloride 4g

[0042] Hypromellose 2g

[0043] Chlorobutanol 0.6g

[0044] Tween-80 1.0g

[0045] Edetate Disodium 0.3g

[0046] Appropriate amount of water for injection

[0047] Makes 1000ml

[0048]Micronized with loteprednol carbonate, sterilized by dry heat at 160°C; hypromellose was swollen with water, sterilized at 121°C for 20 minutes, cooled, and set aside; glycerin, sodium chloride, chlorobutanol, spit Dissolve Wen-80 and edetate disodium in water, filter and sterilize with a 0.22 μm sterile filter membrane, add hypromellose to the aqueous solution, add loteprednol etabonate microcrystals while stirring, and stir well , adjust the pH value to 5-6.5. Subpackage.

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Abstract

The invention relates to an ophthalmic sterile suspension containing loteprednol etabonate, which contains 0.5 percent of loteprednol etabonate minicrystal particles and takes 0.3 percent to 0.8 percent of chlorobutanol as a preservative, 0.1 percent to 0.3 percent of tween-80 as a surface active agent, 0.1 percent to 0.5 percent of hydroxypropylmethyl cellulose as a suspending agent, 0.03 percent to 0.08 percent of natrium adetate as a metal ion complexing agent, and glycerin and sodium chloride as an osmotic pressure regulator. The ophthalmic sterile suspension is prepared by respectively adopting different sterilization methods to the loteprednol etabonate and other components. Apart from the components, the ophthalmic sterile suspension also contains 0.3 percent of tobramycin.

Description

technical field [0001] The invention relates to an ophthalmic sterile suspension containing loteprednol etabonate, which is prepared by adopting different sterilization methods for loteprednol etabonate and other ingredients. Background technique [0002] Loteprednol etabonate is a new type of corticosteroid carrier anti-inflammatory drug, the chemical name is 11β, 17-dihydroxy-3-oxoandrost-1,4-diene-17β-chloromethyl formate 17-(B After topical administration in the eyes, it quickly penetrates the cornea and enters the anterior chamber, and can be rapidly inactivated after entering the blood circulation, so that it retains the strong local anti-inflammatory effect of corticosteroids, but no other corticosteroids systemic toxicity of drugs. Loteprednol etabonate can bind to the glucocorticoid receptor in the eye, so it can easily penetrate the cornea. Its action strength is 1.5 times greater than that of dexamethasone. It has good local activity and a high therapeutic index....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/56A61P27/02A61P29/00
Inventor 马晶
Owner 马晶
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