Compound nano eye drops and preparation method thereof

An eye drop, nanotechnology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of insufficient retention time, avoid systemic adverse reactions, The effect of reducing water production and lowering intraocular pressure

Pending Publication Date: 2022-04-12
SHANDONG INOMIC INST OF PHARM RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the residence time of the above-mentioned eye ...

Method used

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  • Compound nano eye drops and preparation method thereof
  • Compound nano eye drops and preparation method thereof
  • Compound nano eye drops and preparation method thereof

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preparation example Construction

[0029] The present invention provides the preparation method of the compound nanometer eye drop described in above-mentioned technical scheme, comprises the following steps:

[0030] Brinzolamide, adhesive, stabilizer, brimonidine tartrate, osmotic pressure regulator and water are mixed, homogenized and then ground to obtain compound nano eye drops.

[0031] The present invention has no special limitation on the mixing method, and the mixing method well-known to those skilled in the art can be adopted, such as stirring and mixing; the present invention has no special limitation on the speed and time of the stirring and mixing, and the raw materials can be mixed evenly Can.

[0032] In the present invention, the pressure of the homogeneous treatment is preferably 10 to 20 MPa, more preferably 12 to 18 MPa, further preferably 14 to 15 MPa, and the rotational speed of the homogeneous treatment is preferably 5000 to 10000 r / min, more preferably 6000-9000r / min, more preferably 700...

Embodiment 1

[0038] Mix 1g of brinzolamide, 2g of chitosan, 10g of polysorbate 80 and 50g of water for injection to obtain a mixed solution of brinzolamide;

[0039] 1g of brimonidine tartrate is added to 20g of water for injection, fully stirred to dissolve, and brimonidine tartrate solution is obtained;

[0040] Under stirring conditions, the brimonidine tartrate solution was added to the brinzolamide mixed solution, 0.5g sodium chloride was added, and a high-pressure homogenizer was used for 30min under the conditions of 20MPa and 10000r / min, Obtain homogeneous liquid;

[0041] Use a high-energy grinder, use 0.2mm zirconia grinding beads as the grinding medium, grind the homogeneous solution at 2000r / min for 30min, add a 10wt% sodium hydroxide aqueous solution to adjust the pH to 6.8, add water for injection The volume was increased to 100mL to obtain a compound nano eye drop with a particle size of 132nm, wherein the mass ratio of the homogeneous solution to zirconia was 1:5, and the ...

Embodiment 2

[0043] 1g of brinzolamide, 0.5g of chitosan, 20g of polysorbate 60 and 50g of water for injection were mixed to obtain a brinzolamide mixed solution;

[0044] 1g of brimonidine tartrate is added to 20g of water for injection, fully stirred to dissolve, and brimonidine tartrate solution is obtained;

[0045] Under stirring conditions, the brimonidine tartrate solution was added to the brinzolamide mixed solution, 0.5g sodium chloride was added, and a high-pressure homogenizer was used for 20min under the conditions of 15MPa and 8000r / min, A homogeneous solution was obtained.

[0046] Use a high-energy grinder, use 0.2mm zirconia grinding beads as the grinding medium, grind the homogeneous solution at 2000r / min for 30min, add a 10wt% sodium hydroxide aqueous solution to adjust the pH to 6.8, add water for injection The volume was increased to 100mL to obtain a compound nano eye drop with a particle size of 240nm, wherein the mass ratio of the homogeneous solution to zirconia wa...

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Abstract

The invention provides compound nano eye drops and a preparation method thereof, and belongs to the technical field of eye drops. The compound nano eye drops provided by the invention simultaneously contain two medicines, namely the plinzolamide and the brimonidine tartrate, and the adhesive, the stabilizer and the osmotic pressure regulator are used in a matched manner, so that the complexity and the medication frequency of combined medication can be reduced; the particle size of solid particles in the eye drops is nanoscale, the specific surface area of the medicine is large, the residence time of the medicine in front of the cornea can improve the irritation effect of the large-particle medicine on eyes, and the compliance of a patient is improved. The adhesive increases the specific surface area of the brinzolamide medicine, increases the residence time of the hydrophobic medicine in front of cornea, reduces the loss of the medicine in eyes, reduces systemic side effects caused by loss through nasolacrimal ducts, improves the bioavailability, prolongs the medication cycle of the eye drops through slow release, and improves the antibacterial and anti-inflammatory effects; no preservative is contained, so that secondary injury to eyes of a patient is avoided.

Description

technical field [0001] The invention relates to the technical field of eye drops, in particular to a compound nano eye drop and a preparation method thereof. Background technique [0002] Since most patients with ocular hypertensive diseases (such as glaucoma) need long-term or even life-long topical anti-ocular hypertensive drugs, the systemic adverse reactions caused by them have been paid attention to. At present, the ocular hypotensive drugs in clinical application mainly include eye drops, ophthalmic ointments and oral tablets. Among them, eye drops will not cause blurring and irritation, and have the characteristics of low price, easy acceptance by patients, and easy preparation, so they are the most widely used. [0003] For example, Chinese patent CN103142462A discloses a nanosuspension of brinzolamide. In 100 mL of nanosuspension, the following components are contained: the amount of brinzolamide or brinzolamide salt is 0.1-10.0 g, The amount of stabilizer is 0.01...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/36A61K47/26A61K47/10A61K31/542A61K31/498A61P27/06
Inventor 李明丽胡传燕冯华东吕英坤高万玉
Owner SHANDONG INOMIC INST OF PHARM RES CO LTD
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