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External eye drip preparation for treating short sight

An eye drop, myopia technology, applied in sensory diseases, drug combinations, etc., can solve problems such as mydriasis, paralysis, and clinical application limitations, and achieve increased indications, good therapeutic effects, and significant transcorneal transmittance. Effect

Inactive Publication Date: 2004-08-11
EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have reported that the M receptor blocker atropine eye drops has a certain therapeutic effect on myopia, but the effect of atropine on the M receptor is non-selective, which can cause side effects such as mydriasis and accommodation paralysis, and its clinical application is greatly restricted. limit

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Eye drops are prepared according to the following formula ratio.

[0018] Pirenzepine 5.0g

[0019] Boric acid 2.33g

[0020] Borax 0.23g

[0021] Ethylparaben 0.06g

[0022] Sodium chloride 0.44g

[0023] Distilled water up to 200ml

[0024] Preparation method: Take about 160ml of distilled water, add ethylparaben, heat in a water bath to dissolve, then add additives such as boric acid, borax, sodium chloride, stir to dissolve, let cool, add pirenzepine, stir to dissolve, Then add water to 200ml, stir well. Coarse filtration with a sand filter rod, fine filtration with a vertically fused glass funnel, and the filtrate was sterilized by steam for 1 hour, and aseptically divided into eye drops of 2ml each.

Embodiment 2

[0026] For the pirenzepine eye drops prepared in Example 1, the pH value was adjusted by adjusting the amount of the buffering agent, and the concentration of the drug in the aqueous humor of animals was investigated to determine its absorption.

[0027] There were 35 healthy albino rabbits. After the experiment started, 2 drops of the prepared pirenzepine eye drops were added to the rabbits, both in the same eye, and the other eye was used as a control. At 0.5, 1, 2, 4, 8, 12, and 24 hours after eye drops, draw 0.1ml of aqueous humor (9 o'clock inside the limbus under episesthesia), and 5 eyes at each time point. The average value of was taken as the concentration of pirenzepine in aqueous humor at this time point.

[0028] Take 0.1ml of aqueous humor, add 0.1ml of methanol, and vortex to mix to precipitate proteins and impurities. Centrifuge at 10,000 rpm for 15 minutes, take the supernatant, and measure the concentration of pirenzepine in aqueous humor by high performance ...

Embodiment 3

[0039] Inhibitory effect of local drops of pirenzepine on guinea pig myopia model on experimental myopia,

[0040] Specific method: 15 4-week-old guinea pigs were randomly divided into 2 groups. Among them, one group (7 rats) was the control group, and the other group (8 rats) was the experimental group. Both groups wore -10D myopia lenses for their right eyes, and the left eye was opened as a control. The right eye of the experimental group was given 10% pirenzepine eye drops, and the right eye of the control group was given sodium chloride buffer solution. The times of administration were all twice a day, each dosage was 75 μl, and the administration time was continued for 11 days. Before and at the end of the experiment, all guinea pigs were refracted and the axial length of the eyes was measured by A-ultrasound to observe the inhibitory effect of pirenzepine on experimental myopia. At the same time, the histological examination of the eyeball was carried out at the end o...

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PUM

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Abstract

An externally-applied eyedrops for treating myopia by using external electric field to promote its osmosis contains Paicangxiping as active component and additives not includes the thickening agent. Its advantages are high stability, high curative effect, and low irritation to eyes.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an external eye drop preparation for treating myopia, in particular to an external eye drop preparation containing an active ingredient pirenzepine. Background technique [0002] Myopia has become one of the serious diseases that endanger people's health. In recent years, the incidence of myopia is increasing worldwide, and about 25% of people suffer from myopia and must undergo vision correction treatment. About 50% of Chinese teenagers suffer from myopia. Existing treatment methods include optometry and various refractive surgeries. Although they can correct the visual abnormalities caused by myopia, they are powerless to fundamental eyeball enlargement and growth, so they cannot alleviate various eye problems caused by myopia. Internal complications, studies have shown that the relationship between myopia and glaucoma, cataract, retinal detachment is very close, more...

Claims

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Application Information

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IPC IPC(8): A61K31/5513A61P27/10
Inventor 褚仁远吴伟戴怡康
Owner EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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