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Loteprednol etabonate suspension eye drops

A technology of carteprednol and eye drops, which is applied in the direction of liquid delivery, emulsion delivery, organic active ingredients, etc., can solve the problems of drug concentration inconsistent with the nominal value, poor redispersibility, etc., and achieve good re-dispersion The effect of dispersion properties

Inactive Publication Date: 2014-02-12
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It solves the problem that the concentration of the drug dropped into the eye does not match the nominal value due to the poor redispersibility of the existing suspension eye drops
Generally, laser particle size analyzer is used for detection

Method used

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  • Loteprednol etabonate suspension eye drops
  • Loteprednol etabonate suspension eye drops
  • Loteprednol etabonate suspension eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0039] Component 2 in Example 2 is tobramycin, component 2 in Example 6 is levofloxacin hydrochloride, and component 2 in Example 10 is gatifloxacin hydrochloride.

[0040] The preparation method of the etabaclotepdnol micropowder is as follows: dissolve the drug raw material in an organic solvent (heating if necessary), pass through a 0.45 μm microporous membrane, stir with water for injection, and keep stirring with 0.5- Slowly add the organic solvent in which the drug is dissolved into the water at a rate of 1 ml / s, stop stirring after the addition, leave it to stand for 1 hour, filter and dry to obtain the drug micropowder. The particle size distribution of the drug micropowder meets the following conditions simultaneously:

[0041] D50 is 3.0-4.0μm, the maximum particle size is less than 30μm,

[0042] For fine powder with a particle size of 1-8μm, the particle percentage is 79%-85%, of which

[0043] For fine powder with a particle size of 1-4μm, the particle percentage ...

Embodiment 1

[0048] The auxiliary material formula is hydroxypropyl methylcellulose 10g

[0049] Tween-80 0.5g

[0050] Polyoxyethylene hydrogenated castor oil 60 0.5g

[0051] Propylparaben 0.5g

[0052] Methylparaben 0.5g

[0053] Edetate Calcium Sodium 1g

[0054] Sodium chloride 7g

[0055] Water for injection up to 1000ml

[0056] Example 2

[0057] The auxiliary material formula is hydroxyethyl methylcellulose 20g

[0058] Tween-80 0.5g

[0059] Glycerin 10g

[0060] Sodium Hyaluronate 1g

[0061] Polyoxyethylene hydrogenated castor oil 60 0.5g

[0062] Benzalkonium chloride

[0063] Edetate Calcium Sodium 1g

[0064] Water for injection up to 1000ml

[0065] Add tobramycin to solution during preparation and adjust the pH to 5-6 with sulfuric acid.

[0066] Embodiment 3.-8 auxiliary material formula sees the following table (based on 1000ml suspension)

[0067]

Embodiment 9

[0069] The auxiliary material formula is methyl cellulose 20g

[0070] Tween-80 3g

[0071] Propylparaben 0.5g

[0072] Methylparaben 0.5g

[0073] Edetate Calcium Sodium 1g

[0074] Sodium chloride 7g

[0075] Water for injection up to 1000ml

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Abstract

The invention discloses loteprednol etabonate suspension eye drops. The loteprednol etabonate suspension eye drops contain loteprednol etabonate as an active component, water and one or more accessory materials for suspension eye drops. The used loteprednol etabonate micro-powder meets the particle size distribution conditions comprising that D50 is in a range of 3.0-4.0 microns, the maximum particle size is less than 30 microns, a ratio of micro-powder particles having sizes of 1-8 microns is in a range of 79-85%, and a ratio of micro-powder particles having sizes of 1-4 microns is in a range of 49-56%.

Description

Technical field: [0001] The invention relates to a glucocorticoid ophthalmic suspension eye drop. Background technique: [0002] Loteprednol (CAS: 82034-46-6, Loteprednol etabonate), a new type of glucocorticoid, is used to prepare ophthalmic preparations due to its less side effects of increasing intraocular pressure. Ophthalmic preparations include Eccarteprednol Suspension Eye Drops produced by Bausch & Lomb Incorporated (trade name: Ludashu). U.S. Patents US5540930 and US5747061A disclose a kind of etaborteprednol suspension suitable for ophthalmic and nasal use, all disclosing that the particle size range of the etabacloteprednol micropowder that adopts is 0.1-30 μ m, but undisclosed More specific particle size distribution. The Chinese document "Development of Compound Tobramycin Suspension Eye Drops" (Yu Qingzhen, Shanghai Pharmaceuticals, Vol. 20, No. 11, 1999, 36-37) discloses the particle size range of dexamethasone drug micropowder as the active ingredient with...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/56A61P27/02
Inventor 韩昆颖李金禄李静
Owner TIANJIN JINYAO GRP
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