Ophthalmic composition for treating neovascularization in posterior chamber of the eye and use thereof

An ophthalmic composition and neovascularization technology, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as elevated intraocular pressure, and achieve the treatment of neovascularization in the posterior chamber of the eye proliferative effect

Active Publication Date: 2018-02-06
SHANDONG BAUSCH & LOMB FREDA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the defect that the existing composition of triamcinolone acetonide and sodium hyaluronate is used to treat angioplasia in the posterior chamber of the eye and cause an increase in intraocular pressure, the present invention provides a method for treating neovascularization in the posterior chamber of the eye Composition and use of the composition for preparing medicine for neovascularization in posterior chamber of the eye

Method used

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  • Ophthalmic composition for treating neovascularization in posterior chamber of the eye and use thereof
  • Ophthalmic composition for treating neovascularization in posterior chamber of the eye and use thereof
  • Ophthalmic composition for treating neovascularization in posterior chamber of the eye and use thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: composition and preparation method thereof

[0032] Table 1, ophthalmic composition formula

[0033]

[0034] Table 2, ophthalmic composition formula

[0035]

[0036] Preparation:

[0037] 1. Micronized loteprednol etabonate

[0038] Take 1 part of loteprednol etabonate, dissolve it in 3 parts of dimethylformamide at about 60°C, quickly heat-preserve and suction filter, pour the filtrate into distilled water below 10°C for repeated washing, and then stir vigorously at a stirring speed of 220-250 revolutions per minute, continue to stir for 30 minutes, filter, wash the microcrystals repeatedly with distilled water, and vacuum-dry at 105° C. to obtain micronized loteprednol etabonate with a particle size below 3000 nanometers.

[0039] 2. Sterilize the micronized loteprednol etabonate; the aseptic treatment can be sterilized by dry heat at 105-140°C or ethylene oxide or irradiation.

[0040] 3. Preparation of sodium hyaluronate gel: take sterile s...

Embodiment 2

[0048] Embodiment 2: Animal experiment 1

[0049]For verifying the impact of the present invention on intraocular pressure, carried out the comparative experiment to the influence of rabbit intraocular pressure, experiment is as follows:

[0050] 1. Test material

[0051] Test product: prescription 1, 3, 4, 6, 7 of embodiment 1.

[0052] Reference substance: composition and preparation method are as follows

[0053] 1) Table 3 Composition of triamcinolone acetonide gel reference substance

[0054] prescription

particle size

molecular weight

The molecular weight distribution

Dosage %

triamcinolone acetonide

3000nm

--

--

8%

Sodium hyaluronate

--

1.5 million Daltons

1.5

2.3%

Sodium chloride

--

--

--

0.63%

Disodium phosphate

--

--

--

0.3%

Sodium dihydrogen phosphate

--

--

--

0.04%

Water for Injection

--

--

--

Appropriate amount

[005...

Embodiment 3

[0075] Embodiment 3: Animal experiment 2

[0076] The inhibitory effect of loteprednol etabonate gel on laser-induced choroidal neovascularization in rabbits is as follows.

[0077] 1. Test material

[0078] 1) Test product: prescriptions 1, 3, 4, 6, and 7 of Example 1.

[0079] 2) Experimental animals

[0080] 18 New Zealand rabbits, 8-12 weeks old, male and female, provided by Shandong Lukang Pharmaceutical Co., Ltd., license number: SCXK (Lu) 200500170, male or female, body weight 2.0-2.5kg. The feeding and use of experimental animals complied with the "Regulations on the Administration of Experimental Animals" promulgated by the National Science and Technology Committee.

[0081] Main reagents and instruments: 20% fluorescein sodium injection; 532 nm laser machine (IRIS company, USA); NF-505 fluorescein fundus angiography apparatus.

[0082] 2. Test method

[0083] 1) Animal grouping and modeling methods

[0084] 18 rabbits were divided into 6 groups, 3 in each group...

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Abstract

The invention relates to an ophthalmic pharmaceutical composition, in particular to a composition for treating neovascularization in the posterior chamber of the eye and its application. In order to solve the defect that the existing composition of triamcinolone acetonide and sodium hyaluronate is used to treat angiogenesis in the posterior chamber of the eye and cause an increase in intraocular pressure, the present invention provides a composition for treating neovascularization in the posterior chamber of the eye and its use . The composition comprises: (a) loteprednol etabonate, whose weight-volume content is 1%-10%; (b) sodium hyaluronate, whose weight-volume content is 1%-2.5%. The composition provided by the invention can not only effectively treat the hyperplasia of new blood vessels in the posterior chamber of the eye, but also not cause the increase of intraocular pressure.

Description

technical field [0001] The invention relates to an ophthalmic pharmaceutical composition, in particular to a composition for treating neovascularization in the posterior chamber of the eye and its application. Background technique [0002] The proliferation of new blood vessels is a complication of many posterior segment diseases, and is the main cause of vision loss in patients. Diabetic retinopathy, retinal vascular occlusive disease, and age-related macular degeneration (AMD) can all cause retinal vascular proliferation. [0003] Intravitreal administration of corticosteroids is used to treat ocular neovascularization and other hyperplasia of the posterior segment of the eye. Many products have been marketed, such as triamcinolone acetonide formulations. However, some ophthalmic compositions can cause ocular hyperplasia when intravitreal administration of steroids Hypertension, corticosteroid-induced glaucoma, and posterior subcapsular cataract. [0004] A combination of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K31/56A61P27/02
Inventor 邢贞琦李永春韩保萍李晓强韩文芳孙春霞张青贺艳丽
Owner SHANDONG BAUSCH & LOMB FREDA PHARM CO LTD
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