Combination products 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, and 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: 2020-10-16
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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  • Combination products of prostaglandins and nitric oxide donors
  • Combination products of prostaglandins and nitric oxide donors
  • Combination products of prostaglandins and nitric oxide donors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Reduce intraocular pressure (IOP) activity in New Zealand white (NZW) rabbits with normal intraocular pressure

[0117] The intraocular pressure (IOP) reduction activity of the composition of compound (12) (0.1%) and travoprost (0.004%) was evaluated in rabbits with normal intraocular pressure.

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

[0119] Before topical application (basic) and at different time points (30, 60, 120, 180, 240 and 300 minutes), use the barometer 30CLASSIC TM Measure IOP. Five minutes before compound (12) (0.1%) or vehicle (same as below) was applied to the conjunctiva pocket as eye drops, travoprost (0.004%) or vehicle (5% poly) was administered locally. Oxyethylene castor oil (crempphor)-EL; 0.3% DMSO; pH 6.0 0.2 mg / ml BAC in PBS). The eyes were randomly assigned to different treatment groups. Before each group of intraocular pressure measurement, each eye instilled a drop of 0.4% butoxycaine hydrochloride (Novesi...

Embodiment 2

[0125] Intraocular pressure (IOP) reduction activity in New Zealand white (NZW) rabbits with ocular hypertension

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

[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 different time points (30, 60, 120 and 240 minutes) after hypertonic saline injection and before topical administration (basic), use Tono-Pen AVIA Determine IOP.

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

[0130] Compound (12) (0.3%) or vehicle (5% polyoxyethylene castor oil-EL; 0.3% DMSO; 0.2 mg / ml BAC in PBS with pH 6.0) was administered locally immedia...

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Abstract

The present invention relates to compositions for the treatment of glaucoma and elevated intraocular pressure. The composition comprises nitric oxide releasing isomannitol derivatives and prostaglandin F 2α analog.

Description

Technical field [0001] The present invention relates to a composition comprising a nitric oxide-releasing isomannitol derivative and prostaglandin F 2α analog. More specifically, the present invention discloses a composition for reducing intraocular pressure associated with glaucoma or other eye diseases. Background technique [0002] Glaucoma, including hypertension and normal blood pressure glaucoma, is an eye disease in which the visual field is gradually lost due to irreversible damage to the optic nerve. If improperly treated, glaucoma may cause blindness or significant loss of vision. [0003] The treatment of glaucoma in the prior art includes lowering intraocular pressure by administering drugs that reduce the production of intraocular aqueous humor or increase fluid drainage, such as β-adrenergic blockers, α-agonists, cholinergic drugs, and carbonic anhydride. Enzyme inhibitors and prostaglandin analogs. [0004] Among these drugs, prostaglandin analogs help to flow out aq...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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