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Good-stability eye-drop preparation containing PGF2alpha derivative and preparation method thereof

A technology for ophthalmic preparations with good stability, which is applied in the field of ophthalmic preparations for lowering intraocular pressure and its preparation, and can solve the problems of reduced dosage, poor water solubility, and high biological activity of tafluprost

Inactive Publication Date: 2015-11-04
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the high biological activity of tafluprost, the clinical dosage is very small, and the drug concentration of eye drops on the market is 0.0015% (15 μg / ml), and it has strong fat solubility (almost all PGF 2α Derivatives are poor in water solubility), may be adsorbed on the resin container to reduce the dosage

Method used

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  • Good-stability eye-drop preparation containing PGF2alpha derivative and preparation method thereof
  • Good-stability eye-drop preparation containing PGF2alpha derivative and preparation method thereof
  • Good-stability eye-drop preparation containing PGF2alpha derivative and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: Preparation of multi-dose tafluprost ophthalmic preparation containing bacteriostatic agent

[0043] prescription:

[0044] Element

[0045] Preparation method: Take benzalkonium chloride and add 9 times the amount of water, stir to dissolve completely and mix evenly to obtain an aqueous solution of about 10% benzalkonium chloride; take 15-hydroxypolyethylene glycol stearate and add 2.5ml for injection Stir with water, dissolve, add tafluprost, and stir until the tafluprost is completely dissolved to obtain a premixed solution containing tafluprost. Add the premixed solution of tafluprost to 4000ml of water for injection, then add 10% benzalkonium chloride aqueous solution, edetate disodium, sodium dihydrogen phosphate, glycerin, stir to dissolve completely and mix evenly, use 0.1 mol / L sodium hydroxide solution or / and 0.1mol / L hydrochloric acid solution to adjust the pH value of the liquid to about 5.5-6.0, add water for injection to the full ...

Embodiment 2

[0046] Embodiment 2 Preparation of multi-dose tafluprost ophthalmic preparation containing bacteriostatic agent

[0047] prescription:

[0048] Element

[0049] Preparation method: take benzalkonium chloride and add 9 times the amount of water, stir to dissolve completely and mix evenly to obtain an aqueous solution of about 10% benzalkonium chloride; take 15-hydroxypolyethylene glycol stearate and add 50ml water for injection dissolve, add tafluprost, and stir until the tafluprost is completely dissolved to obtain a premixed solution containing tafluprost. Add the premixed solution of tafluprost into 8000ml of water for injection, then add 10% aqueous solution of benzalkonium chloride, sodium calcium edetate, sodium dihydrogen phosphate, glycerin, stir to completely dissolve and mix, and use 0.1 mol / L sodium hydroxide solution or / and 0.1mol / L hydrochloric acid solution to adjust the pH value of the liquid to about 5.8-6.6, add water for injection to the full amoun...

Embodiment 3

[0050] Embodiment 3 Preparation of multi-dose tafluprost ophthalmic preparation containing bacteriostatic agent

[0051] prescription:

[0052] Element

[0053] Preparation method: take benzalkonium chloride and add 9 times the amount of water, stir to dissolve completely and mix evenly to obtain an aqueous solution of about 10% benzalkonium chloride; take 15-hydroxypolyethylene glycol stearate and add 200ml water for injection dissolve, add tafluprost, and stir until the tafluprost is completely dissolved to obtain a premixed solution containing tafluprost. Add 10% benzalkonium chloride aqueous solution, edetate disodium, sodium dihydrogen phosphate, and sodium chloride to 7000ml of water for injection, stir to dissolve completely and mix well, and use 0.1mol / L sodium hydroxide solution or / and 0.1mol / L hydrochloric acid solution to adjust the pH value of the liquid to about 6.0-6.5, add the premixed solution of tafluprost, add water for injection to the full amo...

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PUM

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Abstract

The invention provides a good-stability eye-drop preparation containing a PGF2alpha derivative. The eye-drop preparation comprises the PGF2alpha derivative serving as an active constituent and also comprises 15-hydroxy stearic acid polyglycol ester. It is surprised to find that after the 15-hydroxy stearic acid polyglycol ester serves as a solutizer of the PGF2alpha derivative (such as tafluprost) eye-drop preparation, the stability of active medicine is obviously improved; after the product is subjected to tests of the high temperature, the hard light, the acceleration stability and the long-term stability, compared with existing eye drops, the increase amount of related substances is obviously smaller, and the pharmacological activity and safety of the product are further guaranteed.

Description

technical field [0001] The present invention relates to a kind of PGF 2α Ophthalmic preparation for lowering intraocular pressure with good derivative stability and preparation method thereof. Background technique [0002] Glaucoma is an eye disease in which elevated intraocular pressure compresses the optic nerve, leading to optic nerve damage and visual dysfunction. Its main features are high intraocular pressure, optic nerve atrophy, visual field defect and decreased vision. It is second only to cataract and is the second leading cause of blindness in the world. At present, there are approximately 66.8 million glaucoma patients in the world, and an estimated 5.2 to 6.7 million people worldwide are blinded due to glaucoma. Glaucoma is the second most common eye disease in my country, accounting for about 14.36% of eye diseases, and the national prevalence rate is about 1% to 2%. [0003] In recent years, the research on anti-glaucoma drugs has made great progress. Prost...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/06A61K31/5575A61K47/34A61P27/06
Inventor 徐雄良赵栋胡君艳王利春胡思玉王晶翼程志鹏
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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