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pH sensitive fel ursi eye instant gel

A technology of gel and bear bile, which is applied in sensory diseases, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of absorption less than 10%, long-term eye action time, and limited eye ointment Application and other issues, to achieve the effect of low frequency of administration, great potential for industrial production, and no eye irritation

Active Publication Date: 2018-12-07
YUNNAN DAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special physiological structure of the eye and highly sensitive defense mechanisms such as tear secretion, blinking, etc., traditional dosage forms such as eye drops are quickly eliminated on the corneal surface, and the absorption of the drug in the eye is less than 10%, so frequent administration is required. medicine
Although eye ointment can prolong the retention time of drugs, it is mainly based on fat-soluble excipients, and the water-soluble drugs contained in them are mostly in the form of microcrystalline particles, which is not conducive to the dissolution of drugs, making it difficult for such drugs to be effective in tears. Concentration, dosage is not allowed
In addition, due to factors such as the transparency and refractive index of the matrix, it will cause discomfort symptoms such as blurred vision, strong foreign body and easy crusting, which limits the application of eye ointment
The major defects of the above traditional preparations have prompted researchers to explore and develop a new ocular drug delivery system that has a long acting time in the eye and has slow and controlled release capabilities.

Method used

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  • pH sensitive fel ursi eye instant gel
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  • pH sensitive fel ursi eye instant gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The stability of embodiment 1-bear bile powder extract under different pH conditions

[0020] Get quantitative bear bile powder extract (Zhangfeng Pharmaceutical Factory, Longchuan County, Yunnan Province) respectively in the 10mL volumetric flask, add the phosphate buffer solution of different pH values ​​and dilute to the mark (each phosphate buffer solution pH is 5.0, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0), shake well and set aside. Place in a 40°C incubator, take samples after 0, 1, 3, and 5 days, filter with a 0.45 μm microporous membrane, accurately measure 15 μL of the subsequent filtrate, inject it into a high-performance liquid chromatograph, record the chromatogram, and pass the peak Area to calculate drug content. The results are shown in Table 1.

[0021] Table 1 Stability of bear bile powder extract under different pH conditions

[0022]

[0023] The results showed that the content of tauroursodeoxycholic acid, the main active ingredient, in the extract of bea...

Embodiment 2

[0024] The oil-water partition coefficient of bear bile powder extract under the different pH conditions of embodiment 2-

[0025] The apparent partition coefficient (Papp) of bear bile powder extract in phosphate buffer / n-octanol system with different pH values ​​was determined according to the classic shake flask method. Prepare phosphate buffer solutions with pH values ​​of 5.5, 6.0, 6.5, 7.0, and 8.0, and shake them with equal volumes of n-octanol on a constant temperature oscillator for 24 hours to make them saturated with each other, then let them stand for stratification, and separate the two phases , store for later use. Take 1mL of bear bile powder extract respectively, use the above-mentioned phosphate buffer solution with different pH values ​​saturated by n-octanol as solvent into a 10mL volumetric flask, dilute to the mark, shake well, and obtain. Accurately measure 3mL of bear bile powder extracts with different pH values ​​that have been pretreated, place them ...

Embodiment 3

[0032] Embodiment 3 - the preparation of pH-sensitive bear bile instant gel

[0033] Prescription: Take bear bile powder extract 10g, Carbomer 974 respectively 0.25g, 0.30g, 0.35g, HPMC correspondingly respectively 0.62g, 0.47g, 0.21g, ethylparaben 0.06g, EDTA 0.01g, Mannitol 4.5g, add deionized water to 100g. Sprinkle the prescribed amount of carbomer and HPMC slowly in a beaker filled with an appropriate amount of deionized water under stirring conditions, and let it stand at 4°C to swell. Weigh the prescribed amount of ethylparaben, EDTA, and mannitol into a small beaker, add an appropriate amount of deionized water, heat, and dissolve completely. After cooling to room temperature, add them all to the fully swollen Carbomer / HPMC solution , and add the bear bile powder extract of the prescribed amount, and add deionized water to the full prescribed amount. Adjust its pH to 5.0±0.1 with 20% triethanolamine solution. Prepare three pH 5.0 ± 0.1 carbomer concentrations rangin...

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PUM

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Abstract

The invention provides a pH sensitive fel ursi eye instant gel. 100mg of the pH sensitive fel ursi eye instant gel contains: a, 10mg of fel ursi powder extracted solution; b, 0.29 to 0.31ml of carbomer; and c, 0.45 to 0.49mg of hydroxypropyl methyl cellulose. The pH sensitive fel ursi eye instant gel is invented based on influences of eye physiology characteristics such as lacrimation and blink oninstant gel application on eyes, the contact time of medicine with eyes is prolonged, medicine administration frequency is reduced, no eye irritation is caused, and the stability is high.

Description

technical field [0001] The invention relates to an instant ophthalmic gel, in particular to a pH-sensitive bear bile instant ophthalmic gel. The invention also relates to the preparation method and application of the ophthalmic instant gel. Background technique [0002] Bear bile powder has both significant anti-inflammatory and antibacterial effects, and has a good curative effect on clinical common and frequently-occurring diseases caused by eye bacterial infections. Traditional dosage forms for ophthalmology, such as eye drops and eye ointment, account for 90% of ophthalmic preparations, and are widely accepted by patients due to their simple preparation process, economical price, and convenient use. However, due to the special physiological structure of the eye and highly sensitive defense mechanisms such as tear secretion, blinking, etc., traditional dosage forms such as eye drops are quickly eliminated on the corneal surface, and the absorption of the drug in the eye ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/38A61P27/02A61P29/00A61P31/02
CPCA61K9/0002A61K9/0048A61K9/06A61K35/413A61K47/38
Inventor 胡海燕郭琴杨绚倪小敏丁青章溢申元娜林楚楚
Owner YUNNAN DAI PHARMA
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