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Tiaprofen acid and isoflavone pharmaceutical composition and application thereof

A technology of tiaprofenic acid and its composition, which is applied in the field of ophthalmic preparations, can solve the problems affecting the efficacy of isoflavones, etc., and achieve the effects of improving permeability, large application prospects, and reducing dosage

Active Publication Date: 2021-03-26
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The occurrence of fundus lesions is usually accompanied by a certain inflammatory reaction. Patent CN109925308A discloses the application of isoflavones in the preparation of drugs for the treatment of fundus macular degeneration. efficacy, at the same time, the permeability of isoflavones in the eye also needs to be further improved

Method used

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  • Tiaprofen acid and isoflavone pharmaceutical composition and application thereof
  • Tiaprofen acid and isoflavone pharmaceutical composition and application thereof
  • Tiaprofen acid and isoflavone pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Effect of tiaprofen acid on intraocular permeability of soybean isoflavones

[0030] 1. Method

[0031] 1. Drug preparation: Prepare 5 kinds of liquid medicines with the following final concentrations: (1) 800 μg / mL tiaprofen acid + 80 μg / mL soybean isoflavone liquid (mass ratio 1:0.1); (2) 160 μg / mL thialofen Fenac + 80 μg / mL soybean isoflavone liquid (mass ratio 1:0.5); (3) 80 μg / mL tiaprofen acid + 80 μg / mL soybean isoflavone liquid (mass ratio 1:1); (4) 40 μg / mL tiaprofen acid+80 μg / mL soybean isoflavone liquid (mass ratio 1:2); (5) 32 μg / mL tiaprofen acid+80 μg / mL soybean isoflavone liquid (mass ratio 1:2.5); (6) 80μg / mL soybean isoflavone liquid.

[0032] 2. Experimental animals and grouping: 63 healthy and clean New Zealand white rabbits, weighing 2.0-2.5 kg, half male and half male. The 63 rabbits were randomly divided into 7 groups, 9 in each group: each group was divided into 3 subgroups according to the time points of 30, 60, and 120 minutes aft...

Embodiment 2

[0043] Example 2 Effect of tiaprofen acid on retinal macular inflammation and soybean isoflavone treatment effect

[0044] 1. Method

[0045] Choroidal neovascularization (CNV) model induced by 532nm argon laser was selected from C57 / B6 mice. (The laser point should avoid the main blood vessels and be 2.5 to 3.0 optic disc diameters away from the optic nerve head.) Divide the successfully modeled mice into 7 groups, n=5 in each group; ①The liquid matrix control group (blank control group ), ②800μg / mL tiaprofen acid+80μg / mL soybean isoflavone liquid group, ③160μg / mL tiaprofen acid+80μg / mL soybean isoflavone liquid group, ④80μg / mL tiaprofen acid+80μg / mL soybean Isoflavone liquid group, ⑤80 μg / mL tiaprofen acid + 160 μg / mL soybean isoflavone liquid group, ⑥80 μg / mL tiaprofen acid + 200 μg / mL soybean isoflavone liquid group, ⑦80 μg / mL (0.008%) soybean For the isoflavone drug solution group and (8) 80 μg / mL tiaprofen acid solution group, the volume of 50 μL per eye was locally ad...

Embodiment 3～5

[0053] Prepare tiaprofen acid + soybean isoflavone eye drops with different component contents, as shown in Table 4:

[0054] Table 4 Embodiment 3~5 eye drop formula

[0055]

[0056] According to the technical scheme of the present invention, the optional adjuvant varieties for preparing tiaprofen acid+soybean isoflavone eye drops are not limited to the varieties listed in the above table, and can also have the following multiple options:

[0057] The antibacterial agent is one or more selected from ethylparaben, methylparaben, propylparaben, phenylmercuric acetate, chlorobutanol, thimerosal, benzalkonium chloride and benzalkonium bromide.

[0058] Use an osmotic pressure regulator to adjust the osmolality of the finished eye drops to be 280-330mOsmol / kg; the osmotic pressure regulator is one of sodium chloride, potassium chloride, glucose, boric acid, borax, glycerin, mannitol or Various.

[0059] Use a pH regulator to adjust the pH of the finished eye drops to 5.0 to 7...

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Abstract

The invention discloses a pharmaceutical composition. The pharmaceutical composition comprises tiaprofen acid and soy isoflavone, and the mass ratio of tiaprofen acid to soy isoflavone is 1: (0.5-2).The pharmaceutical composition can be further prepared into ophthalmic products, including ophthalmic injections, eye drops, ophthalmic gels, ophthalmic ointments and the like; and the tiaprofenic acid can further reduce inflammatory response accompanied by fundus diseases, and meanwhile, it is accidentally that the tiaprofenic acid can also serve as a penetration enhancer to improve the intraocular permeability of the soy isoflavone, so that under the condition that the treatment effect is not changed, the use dosage of the soy isoflavone is reduced, and a relatively great application prospect is achieved.

Description

technical field [0001] The invention belongs to the technical field of ophthalmic preparations, and more specifically relates to a pharmaceutical composition of tiaprofen acid and isoflavones and an application thereof. Background technique [0002] Fundus lesions include retinal, choroidal, optic nerve and vitreous inflammation, tumors, various vascular lesions, various degenerative diseases and ocular lesions caused by multi-system diseases. Not only a wide variety, but also greater damage to visual function. Common fundus diseases that affect visual function include diabetic retinopathy, age-related macular degeneration, retinal vein occlusion and so on. [0003] The occurrence of fundus lesions is usually accompanied by a certain inflammatory reaction. Patent CN109925308A discloses the application of isoflavones in the preparation of drugs for the treatment of fundus macular degeneration. At the same time, the permeability of isoflavones in the eye also needs to be fur...

Claims

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Application Information

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IPC IPC(8): A61K31/381A61K9/00A61K47/22A61P9/10A61P27/02A61P29/00A61P35/00A61K31/352
CPCA61K31/381A61K31/352A61K9/0048A61K47/22A61P27/02A61P29/00A61P9/10A61K2300/00
Inventor 吴绮峰曾凌霄
Owner GUANGDONG WHOLEWIN TECH
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