Timolol maleate eye drops and preparation process

A technology of timolol acid eye drops and timolol acid nanometer, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, inorganic non-active ingredients, etc., can solve poor compliance of patients , short retention time, high dosage, etc., to achieve the effect of reducing systemic side effects, reducing the number of administrations, and increasing the residence time

Pending Publication Date: 2021-03-09
JIANGSU YUANHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the impact of blinking and tear secretion, the retention time of ordinary eye drops in the eyes is short after administration, and the absorbed drug amount usually only accounts for a very small part of ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Timolol maleate eye drops comprise following raw materials in parts by weight:

[0031] 10 parts of dispersion liquid C, 5 parts of timolol maleate nanoparticles, 20 parts of aqueous solvent, 4 parts of buffer solution, 100 parts of diluent and 0.01 part of benzalkonium chloride;

[0032] The timolol maleate eye drops are prepared through the following steps:

[0033] The first step is to mix the quaternary amino methacrylate copolymer type A and the quaternary amino methacrylate copolymer type B at a mass ratio of 1:19, add it to absolute ethanol after mixing, and ultrasonicate under the condition of 50kHz 10min, obtain dispersion C;

[0034]The second step, adding timolol maleate nanoparticles into the dispersion liquid C prepared in the first step, stirring evenly to obtain a mixed solution, adding the mixed solution in an aqueous solvent at a speed of 5mL / min, and stirring in an ice-water bath Sonicate for 10 minutes under the condition of medium and ultrasonic fr...

Embodiment 2

[0043] Timolol maleate eye drops comprise following raw materials in parts by weight:

[0044] 11 parts of dispersion C, 6 parts of timolol maleate nanoparticles, 25 parts of aqueous solvent, 5 parts of buffer, 150 parts of diluent and 0.02 parts of benzalkonium chloride;

[0045] The timolol maleate eye drops are prepared through the following steps:

[0046] The first step is to mix the quaternary amino methacrylate copolymer type A and the quaternary amino methacrylate copolymer type B at a mass ratio of 1:19, add them to absolute ethanol after mixing, and ultrasonicate at 55kHz 15min, obtain dispersion C;

[0047] In the second step, Timolol maleate nanoparticles are added to the dispersion C prepared in the first step, stirred evenly to obtain a mixed solution, and the mixed solution is added to an aqueous solvent at a speed of 6mL / min, and the mixture is mixed in an ice-water bath. Ultrasonication for 15 minutes under the condition of medium and ultrasonic frequency of...

Embodiment 3

[0056] Timolol maleate eye drops comprise following raw materials in parts by weight:

[0057] 12 parts of dispersion liquid C, 7 parts of timolol maleate nanoparticles, 30 parts of aqueous solvent, 6 parts of buffer solution, 200 parts of diluent and 0.03 parts of benzalkonium chloride;

[0058] The timolol maleate eye drops are prepared through the following steps:

[0059] The first step is to mix the quaternary amino methacrylate copolymer type A and the quaternary amino methacrylate copolymer type B at a mass ratio of 1:19, add them to absolute ethanol after mixing, and ultrasonicate under the condition of 60kHz 20min, obtain dispersion C;

[0060] The second step, adding timolol maleate nanoparticles into the dispersion liquid C prepared in the first step, stirring evenly to obtain a mixed solution, adding the mixed solution in an aqueous solvent at a speed of 7mL / min, and stirring in an ice-water bath Sonicate for 20 minutes at medium and ultrasonic frequencies of 70 ...

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Abstract

The invention discloses timolol maleate eye drops and a preparation process. The timolol maleate eye drops are prepared from the following raw materials in parts by weight: 10 to 12 parts of dispersion liquid C, 5 to 7 parts of timolol maleate nanoparticles, 20 to 30 parts of a water-based solvent, 4 to 6 parts of a buffering solution, 100 to 200 parts of a diluting agent and 0.01 to 0.03 part ofbenzalkonium chloride. The timolol maleate eye drops are prepared through the following steps: step 1, preparing the dispersion liquid C; step 2, adding the timolol maleate nanoparticles into the dispersion liquid C prepared by step 1 to prepare a nano mixed solution; and step 3, mixing a glucose solution with the mass percent of 8 percent and the nano mixed solution obtained by step 2, and carrying out vacuum freeze-drying for 8h to 10h; after freeze-drying is finished, adding a solid obtained by the freeze-drying into the buffering solution and the diluting agent; raising the temperature to80 DEG C, and keeping the heat for 30min; then cooling to 40 to 50 DEG C; adding the benzalkonium chloride and stirring and dissolving; filtering by a filter element; filling and sealing.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical preparations, and in particular relates to timolol maleate eye drops and a preparation process. 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. . The drugs for clinical treatment of glaucoma are still mainly β-receptor antagonists with low price and clear curative effect, among which timolol maleate is the most widely used clinical drug. [0003] Timolol maleate is a non-selective β-adrenoceptor blocker, has no obvious endogenous sympathe...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/02A61K47/32A61K47/26A61K31/5377A61P27/06
CPCA61K9/08A61K9/0048A61K47/02A61K47/32A61K47/26A61K31/5377A61P27/06
Inventor 王联民贾瑞巧何井亮戴丽萍吕国强
Owner JIANGSU YUANHENG PHARMA
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