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Pirenzepine organic acid salt and eye drops for treating myopia

A pirenzepine, myopia technology, applied in the directions of organic chemistry, organic active ingredients, medical preparations containing active ingredients, etc., can solve problems such as eye irritation, and achieve improved corneal permeability, high fat solubility, oil and water The effect of a large distribution coefficient

Inactive Publication Date: 2006-11-08
无锡康福特药物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the suitable pH range of ophthalmic preparations is 5-9, the pH in WO 02 / 096418 is 5.0, which is already the lower limit, and it is easy to produce a situation below 5.0 during production and storage, resulting in eye irritation

Method used

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  • Pirenzepine organic acid salt and eye drops for treating myopia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of pirenzepine free base:

[0037] Dissolve 100 g of pirenzepine hydrochloride in an appropriate amount of distilled water, exchange with a cation exchange resin, elute with methanol, remove methanol, and remove methanol on a rotary evaporator to obtain pirenzepine free base.

Embodiment 2

[0039] The preparation of pirenzepine sorbate:

[0040] Take 10 g of pirenzepine free base and dissolve it in 10 mL of methanol; another 6.39 g of sorbic acid is heated and dissolved in methanol; the sorbic acid solution is added dropwise to the pirenzepine free base solution, and concentrated on a rotary evaporator to 2mL, placed in the refrigerator overnight, filtered to obtain pirenzepine sorbate.

Embodiment 3

[0042] Preparation of pirenzepine maleate:

[0043] Take 10 g of pirenzepine free base and dissolve it in 10 mL of methanol; take another 3.31 g of maleic acid and heat to dissolve in methanol; add the maleic acid solution dropwise to the pirenzepine free base solution, Concentrate to 2 mL, place in the refrigerator overnight, and filter to obtain pirenzepine maleate.

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Abstract

The present invention relates to pirenzepine organic acid salt for treating myopia and eye drops thereof. Compared with pirenzepine inorganic acid salt, such as pirenzepine hydrochloride, the pirenzepine organic acid salt of the present invention has greater lipophilicity , can increase the permeability of pirenzepine to the cornea and improve the curative effect.

Description

Technical field: [0001] The present invention relates to pirenzepine organic acid salt suitable for intraocular administration and pharmaceutical composition thereof, compared with pirenzepine inorganic acid salt, such as pirenzepine hydrochloride, this type of salt has greater lipophilicity, can increase pirenzepine Renzipine can improve the permeability of the cornea and improve the curative effect. Background technique: [0002] Myopia is a very common disease that often begins in childhood. Along with the popularization of urbanization and TV, computer, the crowd of myopia is developing towards the direction of high incidence. At present, myopia patients account for 25% of the population in the world, and there is a relatively high proportion in my country and neighboring countries, especially among young people. In recent years, it has shown an upward trend. Myopia rate is as high as more than 80%. Myopia will not only affect the normal life of patients, but also easi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61K31/5513A61P27/10C07D221/00C07D243/00
Inventor 吴建梅杨毅
Owner 无锡康福特药物科技有限公司
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