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Combinations of prostaglandins and nitric oxide donors

A technology of nitric oxide and prostaglandin, which is applied in the directions of drug combinations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve the problem of not providing prostaglandin analogs, etc., and achieve the effect of eliminating side effects

Active Publication Date: 2017-08-01
NICOX SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the patent does not provide evidence regarding the effect of the combination of nitric oxide releasing isohexene derivatives and prostaglandin analogs

Method used

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  • Combinations of prostaglandins and nitric oxide donors
  • Combinations of prostaglandins and nitric oxide donors
  • Combinations of prostaglandins and nitric oxide donors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Intraocular Pressure (IOP) Lowering Activity in Normotensive New Zealand White (NZW) Rabbits

[0117] The intraocular pressure (IOP) lowering activity of the combination of compound (12) (0.1%) and travoprost (0.004%) was evaluated in normotensive rabbits.

[0118] Adult male NZW rabbits weighing 1.8-2.0 kg were used in the experiment.

[0119] Before topical application (base) and at different time points (30, 60, 120, 180, 240 and 300 minutes), use the barometer 30CLASSIC TM Measure IOPs. Travoprost (0.004%) or vehicle (5% poly Crempphor-EL; 0.3% DMSO; 0.2 mg / ml BAC in PBS pH 6.0). Eyes were randomly assigned to different treatment groups. One drop of 0.4% butoxycaine hydrochloride (Novesine, Sandoz) was instilled in each eye before each group of intraocular pressure measurements.

[0120]Results As shown in the table, the IOP-lowering activity of the combination of compound (12) and travoprost is expressed as the change in IOP relative to vehicle and relative to...

Embodiment 2

[0125] Intraocular Pressure (IOP) Lowering Activity in Ocular Hypertensive New Zealand White (NZW) Rabbits

[0126] The intraocular pressure (IOP) lowering activity of the combination of compound (12) (0.3%) and travoprost (0.004%) was evaluated in ocular hypertensive rabbits.

[0127] Adult male NZW rabbits weighing 1.8-2.0Kg were used in the experiment.

[0128] 0.1 ml of hypertonic saline (5%) was injected into the vitreous humor of both eyes of NZW rabbits. At various time points (30, 60, 120 and 240 minutes) after hypertonic saline injection and before topical (basal) administration, AVIA with Tono-Pen Measure IOP.

[0129] Travoprost (0.004%) or vehicle (5% polyoxyethylene castor oil-EL; 0.3% DMSO; 0.2 mg / ml BAC in PBS pH 6.0) was applied topically 15 minutes before hypertonic saline injection.

[0130] Compound (12) (0.3%) or vehicle (5% polyoxyethylene castor oil-EL; 0.3% DMSO; 0.2 mg / ml BAC in PBS pH 6.0) was administered topically immediately after hypertonic sal...

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PUM

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Abstract

The present invention relates to compositions for treating glaucoma and elevated ocular pressure. The compositions comprise a nitric oxide releasing isomannide derivative and a prostaglandin F2[alpha] analog.

Description

technical field [0001] The present invention relates to compositions comprising nitric oxide releasing isomannitol derivatives and prostaglandin F 2α analog. More specifically, the present invention discloses compositions for reducing intraocular pressure associated with glaucoma or other ocular diseases. Background technique [0002] Glaucoma, including hypertensive and normotensive glaucoma, is an eye disease characterized by progressive loss of visual field caused by irreversible damage to the optic nerve. If not treated properly, glaucoma can lead to blindness or significant loss of vision. [0003] Prior art glaucoma treatment involves lowering intraocular pressure by administering drugs that reduce intraocular aqueous humor production or increase fluid drainage, such as beta-adrenergic blockers, alpha-agonists, cholinergics, carbonic anhydride Enzyme inhibitors and prostaglandin analogues. [0004] Among these drugs, prostaglandin analogs help outflow of aqueous hum...

Claims

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Application Information

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IPC IPC(8): A61K31/164A61K31/343A61K31/191A61P27/06A61P27/02
CPCA61K31/164A61K31/191A61K31/343A61K2300/00A61K31/34A61K31/5575A61P27/02A61P27/06A61P43/00A61K9/0048
Inventor N·阿尔米兰特L·斯托洛尼E·巴斯蒂亚F·因派纳提洛
Owner NICOX SA
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