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Acetazolamide eye droplet and its application method in treating glaucoma

A technology of acetazolamide and eye drops, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as instability of aqueous solutions, and achieve increased and stable penetration rates sex enhancing effect

Inactive Publication Date: 2004-12-29
JC (WUXI) CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, due to the specific chemical structure of acetazolamide, the 2000 edition of the Chinese Pharmacopoeia pointed out that the compound is very slightly soluble in water or ethanol, and the aqueous solution is unstable

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment one prescription

[0062] Composition W / W(%)

[0063] Acetazolamide 0.3

[0064] Pluronic F68 1.0

[0065] 2-Hydroxypropyl-β-cyclodextrin 3.5

[0066] Hypromellose 0.1

[0067] Edetate disodium 0.05

[0068] Acetic acid 0.042

[0069] Sodium acetate 0.033

[0070] Appropriate amount of sodium hydroxide

[0071] Add pure water to 100ml

[0072] This formulation yielded a clear, transparent solution with a pH of 4.51. It is still stable at 40°C for three months.

Embodiment 2

[0073] Embodiment two prescription

[0074] Composition W / W(%)

[0075] Acetazolamide 0.1

[0076] Pluronic F77 0.01

[0077] 2-Hydroxypropyl-β-cyclodextrin 0.4

[0078] Hypromellose 0.01

[0079] Edetate disodium 0.05

[0080] Acetic acid 0.042

[0081] Sodium acetate 0.033

[0082] Sodium chloride 0.6

[0083] Appropriate amount of sodium hydroxide

[0084] Add pure water to 100ml

[0085] Compared with Example 1, this prescription adds sodium chloride as an isotonic regulator to make it close to physiological isotonicity.

Embodiment 3

[0086] Embodiment three prescription

[0087] Composition W / W(%)

[0088] Acetazolamide 0.4

[0089] Pluronic F127 1.0

[0090] 2-Hydroxypropyl-β-cyclodextrin 4.5

[0091] Hypromellose 0.2

[0092] Edetate disodium 0.05

[0093] Acetic acid 0.042

[0094] Sodium acetate 0.033

[0095] Sodium chloride 0.6

[0096] Benzalkonium Chloride 0.005

[0097] Appropriate amount of sodium hydroxide

[0098] Add pure water to 100ml

[0099] Compared with Example 2, this prescription adds benzalkonium chloride as a preservative to prevent the liquid from being contaminated by microorganisms.

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PUM

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Abstract

The present invention relates to acetazolamide eye drop and its application in treating glaucoma, is the recipe of acetazolamide solution for local use to treat glaucoma. The recipe of the acetazolamide eye drop consists of acetazolamide, poloxamer as polyoxyethylene polyoxypropylene block copolymer with solubilizing, effect-prolonging, moistening and local absorption promoting effects, and synergistic solubilizing liquid state carrier system. Into the recipe, buffering system, isotonic regulator and / or preservative may be added. The recipe has increased acetazolamide solubility, raised acetazolamide stability, and strengthened cornea penetrability of acetazolamide. The local application of the recipe can avoid the side effect of acetazolamide on cardio vascular system, breath system, etc.

Description

technical field [0001] In the invention, the acetazolamide is prepared into a clinically applicable solution type eye drop by using medicinal macromolecular materials and other auxiliary materials through rational formulation. The invention belongs to the field of eye care and treatment. Background technique [0002] Acetazolamide (Acetazolamide), also known as acetazolamide, acetazolamide, and daimax, is a carbonic anhydrase inhibitor. The drug mainly inhibits the carbonic anhydrase in the proximal convoluted tubule, reduces the carbonic acid, reduces the production of hydrogen ions, slows down the exchange of hydrogen and sodium ions, increases the excretion of water and bicarbonate, and produces a diuretic effect. It can be used clinically for mild cardiac Edema. [0003] However, the diuretic effect of acetazolamide is not strong enough, and long-term use will produce drug resistance. So it has been replaced by thiazide diuretics. At present, acetazolamide is not use...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/433A61K47/10A61P27/06
Inventor 李飞程景才林艳琼
Owner JC (WUXI) CO INC
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