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Methazolamide lipidosome and manufacture method thereof

A technology of methazolamide and methazolamide, which is applied in the field of medicine, can solve the problems of poor water solubility and large side effects, and achieve the effects of lowering intraocular pressure, simple preparation method, and obvious blood pressure lowering effect

Inactive Publication Date: 2009-10-28
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of methazolamide, the application of its ophthalmic dosage form is limited. Although the clinical application of oral preparations can reduce intraocular pressure, the side effects of systemic administration of carbonic anhydrase inhibitors are relatively large, which limits its application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dissolve the required methazolamide, phospholipids and cholesterol in the ethanol solution, and remove the organic solvent by rotary evaporation, so that the liposomes form a uniform film on the wall of the device, add the phosphate buffer solution of pH 6.5 to hydrate, add Benzalkonium bromide and osmolarity regulator.

Embodiment 2

[0023] Dissolve the methazolamide, phospholipid, and cholesterol required by the prescription in the ether solvent, inject it into the pH6.5 phosphate buffer solution containing Tween-80 at an appropriate speed, stir magnetically at 40°C until the ether evaporates to dryness, and add Benzalkonium bromide and osmolarity regulator.

Embodiment 3

[0025] Dissolve the methazolamide, phospholipid, and cholesterol required by the prescription in the ether solvent, mix the pH 6.5 phosphate buffer solution containing Tween-80 with it, emulsify, remove the organic solvent by rotary evaporation, and add benzalkonium bromide Ammonium and osmotic regulator.

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PUM

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Abstract

The invention provides a methazolamide lipidosome and a manufacture method thereof. The methazolamide lipidosome prepared by carrier materials, such as methazolamide, phospholipids, cholesterin, a surface active agent, and the like directly drips into the eyes to increase the density of medicines in the aqueous humor and prolong the detention time of the medicines in the eyes, has a certain action on glaucoma treatment and intraocular pressure reduction and has no obvious toxic side effect. The invention prepares 0.1 percent to 5 percent of methazolamide lipidosome solution for eye drop use, has simple and convenient preparation method and obvious pressure reduction effect and provides convenience for clinic application.

Description

Technical field: [0001] The invention relates to a methazolamide liposome and a preparation method thereof, belonging to the technical field of medicine. Background technique: [0002] Glaucoma is a group of clinical syndromes related to intraocular pressure (IOP) that threaten optic nerve visual function. If the intraocular pressure exceeds the limit that the tissues in the eyeball, especially the retina and optic nerve, can bear, it will cause damage to the tissues in the eyeball and visual function. Glaucoma is the second irreversible blinding sexually transmitted disease in the world. Its danger lies in its irreversible blindness. However, as long as it is detected early and treated properly, most patients can maintain useful visual function for life. Therefore, drug treatment is irreplaceable. status. [0003] Methazolamide is a carbonic anhydrase inhibitor class of intraocular pressure-lowering drugs, clinically used to treat chronic open-angle glaucoma, acute angle-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/433A61P27/06
Inventor 徐群为陈睿
Owner NANJING MEDICAL UNIV