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Cyclodextrin inclusion drug composition for ocular inflammation resistance

A technology of composition and cyclodextrin, which is applied in the direction of drug combination, non-effective ingredients of polymer compounds, and pharmaceutical formulations, can solve the problems of being easily oxidized and easily damaged by metal ions, etc., so as to reduce the increase of intraocular pressure and overcome Poor stability, the effect of improving stability

Active Publication Date: 2010-06-30
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 β cyclodextrin 37.5mg

[0045] Dexamethasone sodium phosphate 0.25g

[0046] Sodium chloride 8.5g

[0047] Water for injection 1000ml

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

Embodiment 2

[0050] Vitamin C 25mg

[0051] 2-hydroxypropyl β cyclodextrin 75mg

[0052] Dexamethasone sodium phosphate 0.25g

[0053] Sodium chloride 8.5g

[0054] Water for injection 1000ml

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

Embodiment 3

[0057] Vitamin C 50mg

[0058] 2-hydroxypropyl β cyclodextrin 150mg

[0059] Dexamethasone sodium phosphate 0.25g

[0060] Sodium chloride 8.5g

[0061] Water for injection 1000ml

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

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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 application of the composition for ocular inflammation, especially its application in long-term ocular inflammation. Background technique: [0002] Glucocorticoid is a common drug used to treat ocular inflammation, "A discussion on the rational use of ocular corticosteroids" (Journal of Practical Ophthalmology, 1993, Vol. 11, Issue 10, pp. 581-584). Introduction. However, the application of glucocorticoids will affect the metabolism of mucopolysaccharides, which are found in the anterior chamber angle, trabeculae, and scleral venous sinuses. The polymerization of mucopolysaccharides can cause water retention and affect the discharge of aqueous humor, thereby increasing intraocular pressure. Long-term application of glucocorticoids systemically or locally can lead to glucocorticoid-induced glaucoma GIG. [0...

Claims

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Application Information

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Patent Type & Authority Applications(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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