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Ethyl pyruvate eye drop and preparation method thereof

A technology of ethyl pyruvate and eye drops, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of low bioavailability, unclear mechanism of action, and eye Low drug concentration and other problems, to achieve the effect of prolonging the release time, improving the penetration ability, and benefiting clinical treatment

Active Publication Date: 2014-10-29
THE EYE HOSPITAL OF WENZHOU MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the drugs for preventing and treating cataract mainly include Chinese patent medicines, vitamin drugs, and antioxidant drugs. The current shortcomings of these drugs mainly include the following aspects: 1. Chinese patent medicines: the mechanism of action is unclear, the onset of effect is slow, and the curative effect is very limited; 2. Vitamins: curative effect is very limited, lack of comparability; 3. Antioxidant drugs: aldose reductase inhibitors, pyruvate, glutathione, etc., these drugs have a short residence time in the eye, Low internal drug concentration and low bioavailability

Method used

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  • Ethyl pyruvate eye drop and preparation method thereof
  • Ethyl pyruvate eye drop and preparation method thereof
  • Ethyl pyruvate eye drop and preparation method thereof

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preparation example Construction

[0027] The preparation method of described ethyl pyruvate eye drops, comprises the following steps:

[0028] (1) Preparation of water-soluble chitosan: dissolve water-soluble chitosan in water at a concentration of 0.01%-10%w / v, preferably 0.1%-2%w / v;

[0029] (2) Preparation of amphiphilic chitosan: Using cerium ammonium nitrate or ammonium persulfate as the initiator, under the protection of nitrogen atmosphere, the initiator was added to the water-soluble chitosan solution prepared in step (1) at a concentration of 1~200mmoL / L, the preferred concentration is 10~100mmoL / L, the activation time is 10~60 minutes, add vinyl acetate or caprolactone, and keep nitrogen atmosphere at the same time, the quality of vinyl acetate or caprolactone is water-soluble chitosan 0.01~20 times of sugar, the preferred solution is 0.1~10 times, at 30~90℃, the reaction time is 1~10 hours, after the reaction is completed, put it into the dialysis bag, after 1~4 days of dialysis, centrifuge, take ou...

Embodiment 1

[0034] ① Preparation of water-soluble chitosan:

[0035] The water-soluble chitosan is dissolved in water, and the concentration is 0.1%w / v;

[0036] ② Preparation of amphiphilic chitosan:

[0037] Use ceric ammonium nitrate or ammonium persulfate as the initiator, under the protection of nitrogen atmosphere, add it to the solution in step ①, the concentration is 10mmoL / L, and the activation time is 40 minutes; add vinyl acetate or caprolactone to it , while maintaining a nitrogen atmosphere, the quality of vinyl acetate or caprolactone is 0.1 times that of chitosan, at 70 ° C, the reaction time is 5 hours; 1. Take the supernatant, freeze-dry and set aside;

[0038] ③ Amphiphilic chitosan loaded with ethyl pyruvate

[0039]The amphiphilic chitosan obtained after freeze-drying in the step 2. is redissolved in water for injection, and the concentration is 0.1% w / v. In a high-speed emulsifying machine, under the effect of 20000 rpm of rotating speed, ethyl pyruvate is disperse...

Embodiment 2

[0043] ① Preparation of water-soluble chitosan:

[0044] Dissolving water-soluble chitosan in water at a concentration of 2% w / v;

[0045] ② Preparation of amphiphilic chitosan:

[0046] Use ceric ammonium nitrate or ammonium persulfate as the initiator, under the protection of nitrogen atmosphere, add it to the solution in step ①, the concentration is 100mmoL / L, and the activation time is 15 minutes; add vinyl acetate or caprolactone to it , while maintaining a nitrogen atmosphere, the quality of vinyl acetate or caprolactone is 10 times that of chitosan, at 40 ° C, the reaction time is 2 hours; 1. Take the supernatant, freeze-dry and set aside;

[0047] ③ Amphiphilic chitosan loaded with ethyl pyruvate

[0048] The amphiphilic chitosan obtained after freeze-drying in the step 2. is redissolved in water for injection, and the concentration is 2% w / v. In a high-speed emulsifying machine, under the action of 50000 revolutions / minute of the rotating speed, ethyl pyruvate is d...

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Abstract

The invention provides an ethyl pyruvate eye drop and a preparation method thereof, and is used for solving the problems of short retention time on ocular surface, low bioavailability, high stimulation and the like of ethyl pyruvate. According to the eye drop, ethyl pyruvate can be effectively supported by using amphipathic chitosan as a micelle vector, the amphipathic chitosan is used as a drug-carrying system, the amphipathic performance of the amphipathic chitosan is utilized, and ethyl pyruvate is effectively entrapped by the lyophobic end of the amphipathic chitosan to improve the penetrability and the adhesion, so that the retention time of the drug on the ocular surface can be effectively prolonged, and the drug is promoted to penetrate into eyes; furthermore, the eye drop has a sustained-release effect, the bioavailability of the drug can be further improved, and the sustained-release duration of 20mu L of the ethyl pyruvate eye drop in one dose can be over 12 hours. Compared with a pure drug of ethyl pyruvate, the ethyl pyruvate eye drop has the advantages that the penetrating capability on cornea can be remarkably improved, the release duration after one dose can be effectively prolonged, and clinical treatment is facilitated.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to ethyl pyruvate eye drops and a preparation method thereof. Background technique [0002] Cataract is a common disease in ophthalmology. Cataract is a global disease and the first blinding eye disease in the world. With the aging of the global population, the incidence of cataracts and the total number of affected people are increasing. At present, the drugs for preventing and treating cataract mainly include Chinese patent medicines, vitamin drugs, and antioxidant drugs. The current shortcomings of these drugs mainly include the following aspects: 1. Chinese patent medicines: the mechanism of action is unclear, the onset of effect is slow, and the curative effect is very limited; 2. Vitamins: curative effect is very limited, lack of comparability; 3. Antioxidant drugs: aldose reductase inhibitors, pyruvate, glutathione, etc., these drugs have a short residence time in ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/215A61K47/36A61P27/02A61P39/06A61P29/00
Inventor 俞阿勇孟永春南开辉
Owner THE EYE HOSPITAL OF WENZHOU MEDICAL UNIV
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