Cyclodextrin inclusion drug composition for ocular inflammation resistance

A technology of composition and cyclodextrin, which is applied in the direction of drug combination, non-active ingredients of polymer compounds, and pharmaceutical formulations, can solve the problems of being easily damaged by metal ions and being easily oxidized, and achieves the purpose of overcoming poor stability and reducing intraocular pressure Elevate and improve the effect of stability

Active Publication Date: 2012-07-04
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since vitamin C itself has a series of problems such as being easily oxidized and easily destroyed by metal ions, we found through experiments that the ophthalmic preparations made of vitamin C inclusion with cyclodextrin can increase the concentration of vitamin C in the eye. Stability in the preparation, improve the bioavailability of vitamin C in the eye, prolong the storage time, especially the problem of the decline of vitamin C content during the use of eye preparations

Method used

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  • Cyclodextrin inclusion drug composition for ocular inflammation resistance
  • Cyclodextrin inclusion drug composition for ocular inflammation resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Vitamin C 12.5mg

[0044] 2-Hydroxypropyl beta-cyclodextrin 37.5mg

[0045] Dexamethasone Sodium Phosphate 0.25g

[0046] Sodium chloride 8.5g

[0047] Water for injection 1000ml

[0048] Weigh the prescribed amount of 2-hydroxypropyl β-cyclodextrin, add 2ml of freshly boiled cold distilled water, stir vigorously at 20°C to dissolve, add the prescribed amount of vitamin C, and continue to stir until it is completely dissolved to form A solution. Get prescription quantity dexamethasone sodium phosphate, sodium chloride are dissolved in the water for injection of 50% prescription quantity, adjust PH with the buffer solution of disodium hydrogen phosphate, sodium dihydrogen phosphate to be 7.0 to be B liquid, A liquid, B liquid After mixing, adjust the total volume to 1000ml, then filter through a 0.6μm membrane filter, sterilize, and pack aseptically.

Embodiment 2

[0050] Vitamin C 25mg

[0051] 2-Hydroxypropyl beta cyclodextrin 75mg

[0052] Dexamethasone Sodium Phosphate 0.25g

[0053] Sodium chloride 8.5g

[0054] Water for injection 1000ml

[0055] Weigh the prescribed amount of 2-hydroxypropyl β-cyclodextrin, add 4ml of freshly boiled cold distilled water, stir vigorously at 20°C to dissolve, add the prescribed amount of vitamin C, and continue to stir until it is completely dissolved to form A solution. Get prescription quantity dexamethasone sodium phosphate, sodium chloride are dissolved in the water for injection of 50% prescription quantity, adjust PH with the buffer solution of disodium hydrogen phosphate, sodium dihydrogen phosphate to be 7.0 to be B liquid, A liquid, B liquid After mixing, adjust the total volume to 1000ml, then filter through a 0.6μm membrane filter, sterilize, and pack aseptically.

Embodiment 3

[0057] Vitamin C 50mg

[0058] 2-Hydroxypropyl beta cyclodextrin 150mg

[0059] Dexamethasone Sodium Phosphate 0.25g

[0060] Sodium chloride 8.5g

[0061] Water for injection 1000ml

[0062] Weigh the prescribed amount of 2-hydroxypropyl β-cyclodextrin, add 8ml of freshly boiled cold distilled water, stir vigorously at 20°C to dissolve, add the prescribed amount of vitamin C, and continue to stir until it is completely dissolved to form A solution. Get prescription quantity dexamethasone sodium phosphate, sodium chloride are dissolved in the water for injection of 50% prescription quantity, adjust PH with the buffer solution of disodium hydrogen phosphate, sodium dihydrogen phosphate to be 7.0 to be B liquid, A liquid, B liquid After mixing, adjust the total volume to 1000ml, then filter through a 0.6μm membrane filter, sterilize, and pack aseptically.

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Abstract

The invention relates to a cyclodextrin inclusion drug composition for ocular inflammation resistance, which consists of vitamin C or a derivative thereof as an active ingredient, glucocorticoid, cyclodextrin and one or more pharmaceutically acceptable pharmaceutical excipients capable of acting on eyes, wherein the glucocorticoid and / or the derivative of the vitamin C are included by the cyclodextrin.

Description

Technical field: [0001] The invention relates to a pharmaceutical composition containing glucocorticoid, vitamin C and its derivatives, cyclodextrin, a preparation method and the application of the composition for ocular inflammation, especially for long-term ocular inflammation. Background technique: [0002] Glucocorticoid (glucocorticoid) is a common drug for the treatment of ocular inflammation, "A Discussion on the Rational Use of Ocular Local Corticosteroids" ("Journal of Practical Ophthalmology", Volume 11, No. 10, pp. 581-584, 1993) introduce. However, the application of glucocorticoids will affect the metabolism of mucopolysaccharides, and there are mucopolysaccharides in the anterior chamber angle, trabeculae, and scleral sinus. Mucopolysaccharide polymerization can cause water retention, affect the discharge of aqueous humor, and thus increase intraocular pressure. Long-term application of glucocorticoids systemically or locally can lead to glucocorticoid-induce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/56A61K31/375A61K47/40A61P27/02
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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