Eye drop containing tranilast and its preparing process

A technology for tranilast and eye drops, applied in the field of eye drops containing tranilast and the preparation thereof, can solve the problems of easy precipitation, instability, poor low temperature stability, etc. The effect of quality control, strong practicability and high stability

Active Publication Date: 2006-11-08
药大制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, when researching and developing tranilast eye drops with reference to the Japanese prescription, we found that the prescription prepared with boric acid and borax buffer solution as solvent was unstable at low temperature and prone to precipitation
Polyvinylpyrrolidone K 25 There is no medicinal standard in China, so it cannot be applied to preparations
Benzalkonium chloride is also easy to cause precipitation
In short, the development of tranilast eye drops with reference to the Japanese prescription requires harsh production process conditions and poor stability to low temperatures. Due to easy precipitation and precipitation, adverse reactions such as stinging may occur during use.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] prescription:

[0024] Tranilast 25g

[0025] Meglumine 175g

[0026] Citric acid 55g

[0027] 4% butylparaben ethanol solution 25ml

[0028] PVP K 30 50g

[0029] Add water for injection to 5000ml

[0030] Made 1000 pieces

[0031] Process:

[0032] Take tranilast, meglumine and 2500ml water for injection, stir and dissolve, then slowly add the dissolved 10% citric acid solution in stages, adjust the pH value to 7.5, then add methylparaben solution and PVP K 30 , Stir evenly, filter, add water for injection from the filter to the full amount, fine filter with a 0.22 μm microporous membrane under sterile conditions, measure the content of the semi-finished product to pass, and then pack it into an eye drop bottle.

Embodiment 2

[0034] prescription:

[0035] Tranilast 25g

[0036] Meglumine 225g

[0037] Citric acid 77.5g

[0038] Methylparaben 1g

[0039] PVP K 30 50g

[0040] Add water for injection to 5000ml

[0041] Made 1000 pieces

[0042] Process:

[0043] Dissolve the prescribed amount of methylparaben with about 1000ml of water and set aside; dissolve the prescribed amount of citric acid with about 500ml of water and set aside; put the prescribed amount of PVP K 30 After dissolving in about 500ml of water, set aside; take the prescribed amount of tranilast and meglumine, stir and dissolve in about 2500ml of water; slowly add the citric acid solution to the above tranilast solution while stirring, to control the pH The value is about 7.5. Then add methylparaben solution and PVP K 30 solution, and add water to the full amount, after mixing, sterile filter and fill.

Embodiment 3

[0045] prescription:

[0046] Tranilast 25g

[0047] Meglumine 300g

[0048] Citric acid 150g

[0049] 2% ethanol solution of propylparaben 50ml

[0050] PVP K 30 200g

[0051] Add water for injection to 5000ml

[0052] Made 1000 pieces

[0053] Process:

[0054] Take tranilast, meglumine and 2500ml water for injection, stir and dissolve, then slowly add the dissolved 20% citric acid solution in stages, adjust the pH value to 7.5, then add propylparaben solution and PVP K 30 , Stir evenly, filter, add water for injection from the filter to the full amount, fine filter with a 0.22 μm microporous membrane under sterile conditions, measure the content of the semi-finished product to pass, and then pack it into an eye drop bottle.

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PUM

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Abstract

The present invention discloses the recipe and preparation process of eye drop containing tranilast for treating allergic conjunctivitis. The recipe contains also supplementary material, including meglumine, citric acid, PVP-K30 and nipalgin. The medicine of the present invention has high stability and no thrill on eyes.

Description

technical field [0001] The invention relates to a prescription of eye drops containing tranilast for treating allergic conjunctivitis and a preparation method thereof. Background technique [0002] Tranilast (Tranilast) chemical name is N-(3,4-dimethoxycinnamoyl) anthranilic acid, which is a new type of allergic mediator release agent, which can effectively inhibit allergic reactions and is mainly used to prevent and treat allergies Asthma and other allergic diseases. [0003] Japan KISSEI Pharmaceutical Co., Ltd. listed Tranilast eye drops (Rizaben) in Japan in 1995.  ), for allergic conjunctivitis. [0004] Tranilast is easily soluble in organic solvents such as dimethylformamide and pyridine, but is extremely difficult to dissolve in water. How to dissolve tranilast in an aqueous solution to obtain a therapeutically concentrated tranilast solution is the key to preparing tranilast eye drops. [0005] Instructions for Tranilast Eye Drops in Japan, announced its prescr...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/196A61P27/14
Inventor 王强
Owner 药大制药有限公司
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