Eye in-situ gel of chiral anti-glaucoma medicine L-3alpha alkyla acyloxy-6belta alkyla acyloxy tropane and preparation method thereof

A glaucoma and gel technology, applied in the directions of pharmaceutical formulations, drug combinations, drug delivery, etc., can solve the problems of short drug effect time and low bioavailability, and achieve the effects of non-irritant, broad application prospects and accurate doses

Inactive Publication Date: 2009-04-01
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to overcome the shortcomings of chiral anti-glaucoma drug levosatorane eye drops with short drug effect time and low bioavailability, and provide a levosa

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 50% of water for injection, add 0.12% of levocatorane, stir to dissolve; take 12% of poloxamer and 3% of carbomer, respectively add the above solution under stirring; let the solution stand overnight until fully dissolved; then Add 7% glycerin, 0.1% benzalkonium bromide, and 0.8% sodium chloride, stir to dissolve, adjust the pH value to 4.5 with 0.1N hydrochloric acid, filter the solution through a 0.22 μm microporous membrane, and add the remainder from the filter Water for injection to 100%.

Embodiment 2

[0036] Take 50% of water for injection, add 0.12% of levosatorane, stir to dissolve; take 0.1% of sodium alginate and 2% of hydroxypropyl methylcellulose, respectively add the above solution under stirring; let the solution stand overnight until fully Dissolve; then add 10% glycerin, 0.1% benzalkonium bromide, and 0.6% sodium chloride, stir to dissolve, filter the solution through a 0.22 μm microporous membrane, and add the remaining water for injection from the filter to 100%.

Embodiment 3

[0038] Take 50% of water for injection, add 0.3% of levosatorane, stir to dissolve; take 2% of hydroxypropyl methylcellulose and 2% of carbomer, respectively add the above solution under stirring; let the solution stand overnight until fully Dissolve; then add 10% sorbitol, 0.1% benzalkonium chloride, and 0.6% sodium chloride, stir to dissolve, adjust the pH value to 4.5 with 0.1N hydrochloric acid, filter the solution through a 0.22 μm microporous membrane filter, and remove from the filter Add the remaining amount of water for injection to 100%.

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PUM

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Abstract

The invention relates to an ophthalmic in-situ jelly of chiral anti-glaucoma medicine levofloxacin tropane. The ophthalmic jellies concretely comprises 0.03 percent to 0.3 percent of levofloxacin tropane, 10 percent to 20 percent of hydrophilic polymer material, 0 percent to 20 percent of humectant, 0.1 percent to 10 percent of permeation pressure regulator, 0.01 percent to 0.3 percent of antiseptic/bacteriostat, pH value regulator and water. In a preparation method, the materials are weighted according to the percentage; the levofloxacin tropane is solved in injection water, the hydrophilic polymer material is added under the stirring state, and the solution is stood over a night; the adjuvant such as the humectant and the like is added, and the pH value is adjusted as 4 to 9; the solution is filtered, the injection water is added to the total quantity, and the ophthalmic in-situ jelly is obtained. The ophthalmic in-situ jelly has the advantages of uniform and smooth quality, proper viscosity, convenient use, exact dosage, and long-term uniform distribution on the surface of eye cornea; besides, the jelly causes no hypersusceptibility and irritation, no blurred vision, can effectively prolong the acting time of the medicine on the eye cornea, and has wide application prospect.

Description

【Technical field】 [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an ophthalmic in-situ gel of chiral anti-glaucoma drug levosatorane and a preparation method thereof. 【Background technique】 [0002] Glaucoma is a relatively common eye disease, characterized by elevated intraocular pressure, optic atrophy and visual field defect, and its main hazards are visual function impairment, vision loss and visual field defect. Clinically, glaucoma is mostly a primary lesion without a clear systemic or ocular secondary etiology. Primary glaucoma can be divided into two types: angle-closure type and open-angle type, both of which have a certain genetic predisposition. In my country, there are more patients with angle-closure glaucoma, and the prevalence ratio of angle-closure glaucoma is about 3.7:1. At present, although open-angle glaucoma has an increasing trend, the number of patients with angle-closure glaucoma is still not opt...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/46A61K47/34A61P27/06A61K47/10
Inventor 陈红专冯雪梅杨丽敏陆阳朱亮崔永耀
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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