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Compound medicine composition for treating glaucoma and application thereof

A composition and drug technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of lowering intraocular pressure, incompatibility, etc., and achieve the effect of reducing intraocular pressure

Pending Publication Date: 2022-07-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the shortcomings of existing single preparations, double compound preparations and triple compound preparations for the treatment of glaucoma, such as poor curative effect, many side effects, and poor patient compliance, the present invention provides an adrenergic β-receptor blocker and A dual compound pharmaceutical composition of netadil; and a triple compound pharmaceutical composition comprising adrenergic β-receptor blocker, netadil and prostaglandin analogues, and successfully solved the problem of adrenaline through a salt engineering strategy Beta-blockers (timolol free base or its salts, carteolol free base or its salts, betaxolol free base or its salts, metopolol free base or its salts) and natamolol The problem of the incompatibility of certain types of salts of dil, and the pharmaceutical composition of the present invention can reduce intraocular pressure more significantly than the commercially available compound ophthalmic preparations

Method used

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  • Compound medicine composition for treating glaucoma and application thereof
  • Compound medicine composition for treating glaucoma and application thereof
  • Compound medicine composition for treating glaucoma and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-5

[0070] Examples 1-5: Formulations Containing Netadil Dimesylate and Carteolol Mesylate

[0071] Table 1. Preparation of topical ophthalmic pharmaceutical composition solutions for lowering intraocular pressure and formulated as follows:

[0072]

[0073] The preparation process is as follows: 1) Weigh 95% of the water for injection of the recipe, add the active ingredient and auxiliary materials of the recipe and stir until completely dissolved, and adjust the pH to 4.5-5.4 with sodium hydroxide solution (10%); 2) Supplement water for injection To the full amount of the prescription, stir evenly and make the volume reach 100%; 3) Put the solution of step 2 into a low density polyethylene medicinal eye drop bottle, and study its stability under different storage temperature conditions.

[0074] Table 2. When stored at 5°C for 24 months, the content of each main drug component in Examples 1-5

[0075]

[0076] Table 3. Commercially available eye drops when stored at 5°C f...

Embodiment 6-10

[0089] According to Examples 1-5, the formulations containing NET and carteolol mesylate have good stability under the storage condition of 40°C for 14 days, which satisfies the requirements for commercially available eye drops. Short-term deviations from storage conditions. Examples 6-10: Formulations Containing Netandilol Dihydrochloride and Carteolol Hydrochloride

[0090] Table 8. Preparation of topical ophthalmic pharmaceutical composition solutions for lowering intraocular pressure and formulated as follows:

[0091]

[0092] Preparation process: Refer to the preparation process described in Examples 1-5.

[0093] Table 9. When stored at 5°C for 24 months, the content of each main ingredient in Examples 6-10

[0094]

[0095] According to Examples 6-10, the formulations containing NET and carteolol hydrochloride have good stability for 24 months under the storage condition of 5°C, which satisfies the requirements for commercially available eye drops. Requireme...

Embodiment 11

[0102] Example 11: Evaluating the efficacy of the ophthalmic pharmaceutical composition solutions of Examples 1-10 using the Japanese white rabbit glaucoma model

[0103] Experimental animals: healthy male Japanese white rabbits (Shenyang Pharmaceutical University, license number: SYXK (Liao) 2018-0009), with an initial weight of 2.5-3.0 kg, 3 rabbits / group.

[0104] Experimental group:

[0105] Normal control group: did not do any treatment.

[0106] Model group: establish a high intraocular pressure model without giving any eye drops.

[0107] Treatment group 1: establish a model of high intraocular pressure, and give commercially available netatadil eye drops Treatment group 2: established intraocular hypertension model, and given commercially available carteolol hydrochloride eye drops

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Abstract

The invention provides an ophthalmic bigeminy and trigeminy compound pharmaceutical composition for treating glaucoma and ocular hypertension, the stability of the pharmaceutical composition is obviously improved through a salt modification technology, and the bigeminy compound pharmaceutical composition is prepared from netardil free alkali or pharmaceutically acceptable salt thereof and an epinephrine beta receptor blocker; the triplet compound pharmaceutical composition is prepared from netardil free alkali or pharmaceutically acceptable salt thereof, an epinephrine beta receptor blocker and a prostaglandin analogue, and has excellent stability when the pH value is 4.5-5.4; according to the present invention, the effective dose of the pharmaceutical composition is applied to the eyes of the patient requiring the intraocular pressure at the sleeping time or at the time close to the sleeping time once a day, such that the intraocular pressure can be efficiently and rapidly reduced so as to maintain the intraocular pressure in the physiological range for a long time, the side effect is small, and the patient compliance is high.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to an ophthalmic dual and triple compound pharmaceutical composition and its use in preparing a medicine for preventing or treating glaucoma or for reducing intraocular pressure. Background technique [0002] Glaucoma is a common disease in ophthalmology, and pathological intraocular pressure elevation and optic nerve insufficiency are the primary risk factors for its onset. Due to the increased intraocular pressure, the optic nerve is compressed, resulting in thinning of the optic nerve fiber layer and damage to the optic nerve cells, resulting in decreased vision, visual field defect, optic nerve atrophy, etc. Severe glaucoma patients may even lead to blindness. Therefore, glaucoma has been Become the number one killer of human blindness. [0003] At present, the commonly used unilateral preparations include the following categories: (1) Rho kinase inhibitors: intraocular hypotensive drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/472A61K31/5377A61K45/06A61K9/08A61P27/02A61P27/06A61K31/138A61K31/137
CPCA61K31/5377A61K31/4704A61K31/138A61K31/137A61K31/472A61K45/06A61K9/0048A61K9/08A61P27/02A61P27/06A61K2300/00
Inventor 姜琪坤王涛迟美玲赵晨
Owner SHENYANG PHARMA UNIVERSITY
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