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Baicalin adhesion type nanometer eye drops and preparation method thereof

A baicalin sticky and eye drop technology is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, which can solve the problems of loss of baicalin, low bioavailability, etc. Corneal absorption, increasing drug concentration, and increasing curative effect

Active Publication Date: 2014-03-12
北京汇诚瑞祥医药生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the baicalin ophthalmic products listed in China are mainly Xiongdan Scutellaria Eye Drops. However, due to the shortcomings of the eye drops and the physical and chemical properties of baicalin itself, most of the baicalin instilled into the eyes is lost. low bioavailability

Method used

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  • Baicalin adhesion type nanometer eye drops and preparation method thereof
  • Baicalin adhesion type nanometer eye drops and preparation method thereof
  • Baicalin adhesion type nanometer eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Add 7g of poloxamer to 500g of deionized water, and dissolve it in a water bath at 70°C as the water phase; in addition, dissolve 0.08g of baicalin, 5g of glyceryl tristearate, and 5g of soybean lecithin in an appropriate amount of absolute ethanol, and heat to make the ethanol Evaporate to form the organic phase; the organic phase is magnetically stirred in a water bath, slowly inject the water phase into the stirred organic phase, and continue to stir for 0.5h to form colostrum; put the obtained colostrum in a high-pressure homogenizer, 700bar homogenization 3 times, after filtering through a microporous membrane, add 5g hydroxypropyl methylcellulose, 0.1g benzalkonium bromide, 8g sodium chloride, 40g hydroxypropyl-β-cyclodextrin and stir to dissolve, and dissolve with 10% Sodium hydroxide is used to adjust the pH to 6.8, the solution is filtered through a microporous membrane, and then deionized water is added from the filter to reach the total amount.

Embodiment 2

[0036] Add 100g of poloxamer to 500g of deionized water, and dissolve it in a water bath at 70°C as the water phase; in addition, dissolve 10g of baicalin, 50g of glyceryl tristearate, and 50g of soybean lecithin in an appropriate amount of absolute ethanol, and heat to evaporate the ethanol. to form the organic phase; the organic phase is magnetically stirred in a water bath, the water phase is slowly injected into the stirred organic phase, and the stirring is continued for 0.5h to form colostrum; the resulting colostrum is placed in a high-pressure homogenizer, 700bar homogeneous Once, after filtering through a microporous membrane, add 100g hydroxypropyl methylcellulose, 0.1g benzalkonium bromide, 8g sodium chloride, 40g hydroxypropyl-β-cyclodextrin and stir to dissolve, and use 10% hydrogen Sodium oxide is used to adjust the pH to 6.8, the solution is filtered through a microporous membrane, and deionized water is added from the filter to reach the total amount.

Embodiment 3

[0038] Add 100g of poloxamer to 300g of deionized water, and dissolve it in a water bath at 70°C as the water phase; in addition, dissolve 16g of baicalin, 70g of glyceryl tristearate, and 60g of soybean lecithin in an appropriate amount of absolute ethanol, and heat to evaporate the ethanol. to form the organic phase; the organic phase is magnetically stirred in a water bath, the water phase is slowly injected into the stirred organic phase, and the stirring is continued for 0.5h to form colostrum; the resulting colostrum is placed in a high-pressure homogenizer, 700bar homogeneous Once, after filtering through a microporous membrane, add 150g of hydroxypropylmethylcellulose, 0.1g of benzalkonium bromide, 8g of sodium chloride, and 100g of hydroxypropyl-β-cyclodextrin and stir to dissolve, and then use 10% hydrogen Sodium oxide is used to adjust the pH to 6.8, the solution is filtered through a microporous membrane, and deionized water is added from the filter to reach the tot...

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Abstract

The invention relates to baicalin adhesion type nanometer eye drops and a preparation method thereof. The baicalin adhesion type nanometer eye drops comprise the following components: 0.001-3% by weight of baicalin, 0.1-20% by weight of lipid, 0.1-20% by weight of surfactant, 0.1-10% by weight of matrix, 0.001-3% by weight of preservative, 0.1-10% by weight of isotonic regulator, 0.005-10% by weight of penetration enhancer, the amount of pH regulator which can regulate pH value of a preparation to 5-9 and the balance of deionized water.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a baicalin-adhesive nanometer eye drop and a method for preparing the adhesive nanometer eye-drop. Background technique [0002] Baicalin is a flavonoid compound extracted from the dried root of Scutellaria baicalensis. Baicalin has a strong antibacterial and bactericidal effect on common pathogenic bacteria in clinical ophthalmology, such as Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus albus, Bacillus subtilis, etc., and its therapeutic effect on conjunctivitis and keratitis has been affirmed; According to reports, the effects of baicalin on the antioxidant system of these two types of lenses were studied using selenium-induced cataract and lens oxidative damage models in vitro. The results showed that baicalin can improve their antioxidant capacity, so baicalin also has a significant effect on treating cataracts. At present, the baicalin ophthalmic p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/7048A61K47/32A61K47/34A61K47/36A61K47/38A61K47/40A61P27/02A61P27/12A61K47/10A61K47/26
Inventor 刘志东高秀梅张伯礼李佳玮张欣华刘睿李楠
Owner 北京汇诚瑞祥医药生物科技有限公司