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Method for improving stability of low-concentration atropine ophthalmic preparation

A stable, atropine sulfate technology, applied to atropine ophthalmic preparations, the field of preparing said ophthalmic preparations, can solve problems such as increased preparation irritation, product safety impact, restricted product development and promotion, etc.

Active Publication Date: 2020-03-31
SHENYANG XINGQI EYE HOSPITAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present inventors found that for low concentration atropine ophthalmic preparations, a lower pH value is needed to meet the requirements of stable preparations, but the irritation of the preparations is greatly improved, which not only affects the compliance of patients in use, but also causes the formation of tears due to stimulation. secreted thereby affecting the bioavailability of atropine
In the patent US9421199B2, deuterated water is used to improve the stability of low-concentration atropine eye drops. However, the introduction of isotopes will inevitably affect the safety of the product, and the requirements for product production and quality control are higher, which limits the product. development and promotion

Method used

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  • Method for improving stability of low-concentration atropine ophthalmic preparation
  • Method for improving stability of low-concentration atropine ophthalmic preparation
  • Method for improving stability of low-concentration atropine ophthalmic preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Refining of Atropine Sulfate API

[0060] Place the commercially available atropine sulfate crude drug A or B with a purity of more than 99% in a pulverizer with a 60-mesh sieve, slowly pulverize and sieve, and collect the raw materials under the sieve for subsequent use. Take 50 g of pulverized raw materials and place them in a 3000 mL three-neck flask, add 20 times the amount of anhydrous acetone, stir and wash at 40°C for 3 hours, and filter with suction to obtain wet product 1. Take the wet product 1, put it in a 3000mL three-neck flask, add 15 times the amount of 5% acetone aqueous solution, stir and wash at 40°C for 4 hours, and filter with suction to obtain the wet product 2. The wet product 2 was placed in a 1000mL three-neck flask, 10 times the amount of acetone was added, stirred and washed at 5°C for 1.5h, suction filtered, and dried under reduced pressure for 6h to obtain 41g of atropine sulfate, yield: 82%. HPLC carries out impurity analysis, t...

Embodiment 2～ Embodiment 6

[0071] According to the corresponding prescription ratio in Table 3, the atropine ophthalmic preparation was prepared by the following preparation method.

[0072] Preparation:

[0073] (1) Take 10g of water for injection at 80-90°C, add the prescribed amount of hydroxypropyl methylcellulose or sodium hyaluronate to fully disperse and swell, make up to 20g of water for injection below 30°C, stir and dissolve to a transparent solution, and set aside;

[0074] (2) Take 50g of water for injection at 65-75°C, dissolve the prescribed amount of sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate, disodium edetate and benzalkonium chloride in turn, put it below 30°C, and add the prescribed amount The atropine sulfate refined by the method in Example 1, stirring and dissolving;

[0075] (3) mix the hydroxypropyl methylcellulose solution of (1) gained with the solution of (2) gained;

[0076] (4) Add water to the mixed solution obtained in (3) to the full amount of 1...

Embodiment 7～ Embodiment 9

[0081] According to the corresponding prescription ratio in Table 4, the atropine ophthalmic preparation was prepared by the following preparation method.

[0082] Preparation:

[0083] (1) Take 10g of water for injection at 80-90°C, add the prescribed amount of hydroxypropyl methylcellulose to fully disperse and swell, add water for injection below 30°C to 20g, stir and dissolve to a transparent solution, and set aside;

[0084] (2) Take 50g of water for injection at 65-75°C, dissolve the prescribed amount of boric acid, edetate disodium and benzalkonium chloride in turn, put it below 30°C, add the prescribed amount of refined according to the method in Example 1 Atropine sulfate, stirred to dissolve;

[0085] (3) mix the hydroxypropyl methylcellulose solution of (1) gained with the solution of (2) gained;

[0086] (4) Add water to the mixed solution obtained in (3) to the full amount of 100g, stir evenly, filter and sterilize with a 0.22 μm filter membrane, and fill.

[0...

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Abstract

The invention provides a method for improving the stability of a low-concentration atropine ophthalmic preparation. The method is characterized in that an atropine sulfate bulk drug has a total impurity content of no more than 0.25% and / or a single impurity content of no more than 0.05%. The invention also provides a method for preparing the ophthalmic preparation, the atropine ophthalmic preparation prepared by using the method, and an application of the atropine ophthalmic preparation in preparation of drugs used for preventing and / or treating visual defects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a method for improving the stability of low-concentration atropine ophthalmic preparations, a method for preparing the ophthalmic preparations, the atropine ophthalmic preparations prepared thereby, and uses thereof. Background technique [0002] Atropine ophthalmic preparations have been used clinically for many years, mainly for mydriasis, cycloplegia, and depression therapy in the treatment of amblyopia. In addition, atropine, as the only drug proven by evidence-based medicine to effectively slow down the progression of myopia, has been used to control the progression of myopia for many years. [0003] At present, there are not many drugs used to control the progression of myopia in young people at home and abroad, and the side effects are large. In the past in our country, the treatment of myopia with atropine was mostly high-concentration short-term tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K31/46A61P27/02A61P27/10C07D451/10
CPCA61K9/0048A61K9/08A61K31/46A61P27/02A61P27/10C07D451/10A61K47/38A61K47/183A61K47/186A61K47/02A61K47/10A61K47/36A61K47/547
Inventor 刘继东高坤王久亮杨强
Owner SHENYANG XINGQI EYE HOSPITAL CO LTD
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