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Timolol maleate cubic liquid crystal nanoparticle eye drops and preparation method thereof

A technology of timolol maleate and nanoparticles, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve irritation, timolol maleate Eye drops have short retention time in the eye and short retention time of drugs in the eye, etc., to achieve the effect of maintaining moisture, improving medication compliance, and increasing corneal penetration

Active Publication Date: 2017-05-10
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN101474146A discloses a timolol maleate eye drop without bacteriostatic agent and its preparation method, but the patent is a solution type eye drop, which does not solve the problem of short retention time of the drug in the eye
In a word, the existing timolol ophthalmic products and the published literature fail to solve the short retention time of timolol maleate eye drops in the eye and the irritation caused by long-term use

Method used

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  • Timolol maleate cubic liquid crystal nanoparticle eye drops and preparation method thereof
  • Timolol maleate cubic liquid crystal nanoparticle eye drops and preparation method thereof
  • Timolol maleate cubic liquid crystal nanoparticle eye drops and preparation method thereof

Examples

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Effect test

Embodiment 1

[0049] Embodiment 1: Preparation of timolol maleate cubic liquid crystal nanoparticle eye drops

[0050] The timolol maleate cubic liquid crystal nanoparticle eye drops of the present embodiment is prepared from the following raw materials:

[0051]

[0052] The preparation method of the timolol maleate cubic liquid crystal nanoparticle eye drops of the present embodiment comprises the following steps:

[0053] Accurately weigh glycerol monooleate and poloxamer 407, heat in a water bath at 65°C until melting to obtain an oil phase mixture; in addition, accurately weigh timolol maleate, dissolve in 100g of water, and stir evenly to obtain Water phase mixture; put the water phase mixture in a high-shear homogenizer, slowly add the oil phase mixture into the water phase mixture, and disperse under high shear at 10000rpm for 3 minutes; then transfer the resulting mixture into a high-pressure homogenizer , under 500MPa high pressure homogenization 5 times, that is.

Embodiment 2

[0054] Embodiment 2: Preparation of timolol maleate cubic liquid crystal nanoparticle eye drops

[0055] The timolol maleate cubic liquid crystal nanoparticle eye drops of the present embodiment is prepared from the following raw materials:

[0056]

[0057] The preparation method is the same as in Example 1.

Embodiment 3

[0058] Embodiment 3: Preparation of timolol maleate cubic liquid crystal nanoparticle eye drops

[0059] The timolol maleate cubic liquid crystal nanoparticle eye drops of the present embodiment is prepared from the following raw materials:

[0060]

[0061] The preparation method is the same as in Example 1.

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Abstract

The invention relates to timolol maleate cubic liquid crystal nanoparticle eye drops and a preparation method thereof. The imolol maleate cubic liquid crystal nanoparticle eye drops are mainly prepared from, by weight, 0.4-1.0 part of timolol maleate, 1.0-18.0 parts of liquid crystal material, 0.2-3.0 parts of surface active agent and 100 parts of water. The liquid crystal material is glycerol monoolein. The surface active agent is poloxamer. According to the timolol maleate cubic liquid crystal nanoparticle eye drops, the cornea infiltration capacity of timolol maleate can be remarkably improved, intra-ocular pressure can be remarkably and stably reduced, the retention time of a drug in the eyes can be prolonged, no preservative is added, and the problems that in the prior art, the retention time of timolol maleate eye drops in the eyes is short and irritation is caused by long-time use can be effectively solved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a timolol maleate cubic liquid crystal nanoparticle eye drop and a preparation method thereof. Background technique [0002] Glaucoma is an eye disease characterized by optic neuropathy and loss of visual function. Elevated intraocular pressure is the main blinding factor of glaucoma, and drug therapy is the main treatment. At present, the clinical medicine for glaucoma is mainly based on eye drops, including β-receptor antagonists, prostaglandin analogs, carbonic anhydrase inhibitors, adrenergic receptor agonists, choline receptor agonists and optic nerve protection drugs, etc. . Although prostaglandin analogues, such as latanoprost, bimatoprost and travoprost, are increasingly listed as clinical first-line drugs in Europe, America and other countries, the high price will increase the cost of long-term medication for patients. The economic burden limits its use as th...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/5377A61K47/14A61K47/10A61P27/06
CPCA61K9/0002A61K9/0048A61K9/5015A61K9/5031A61K31/5377
Inventor 吴传斌杨莉李彦蓉潘昕黄莹陈航平
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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