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Liquid preparation made from pazufloxacin leucinocaine fed through eye in application of curing ophthalmic diseases and producing method

A technology of pazufloxacin mesylate and liquid preparations, which is applied in the field of liquid preparations, can solve the problems of inconvenient clinical use, increase the burden on patients' kidneys, and large dosage of drugs, achieve good market prospects and social benefits, and reduce the burden on the kidneys , to overcome the effect of reducing the treatment rate

Active Publication Date: 2004-10-27
ZHEJIANG SHAPUAISI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the existing dosage form of pazufloxacin mesylate has three disadvantages in the treatment of ophthalmic diseases: ① the dosage is large, and after intravenous administration, the effective concentration of the drug in the eyes is very low, and it is difficult to reach the effective blood concentration in the lesion.
②Most of the drugs that enter the body are mainly eliminated through the kidneys, increasing the burden on the kidneys of patients, and patients with renal insufficiency cannot use them; ③Using large doses is prone to drug resistance; clinical use is extremely inconvenient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The drug prescription is planned to be 2-10 parts of pazufloxacin mesylate, add 2-10 parts of dilute acetic acid and stir to dissolve, add 500 parts of 1-700 parts of water for injection, and dissolve 0.3-5 parts of ethylparaben with water for injection Then add to the main drug solution, add 1-30 parts of citric acid, 1-10 parts of disodium hydrogen phosphate, and 2-10 parts of sodium chloride, stir evenly, adjust the pH value to 3.0-7.0, constant volume, and stir evenly , filtered, and semi-finished products pass inspection, sterilized, aseptically subpackaged, fully inspected, and packaged.

[0019] Liquid preparation preparation method, carry out according to the following steps:

[0020] 1) Weigh pazufloxacin mesylate, add 0.01-100 parts of dilute acetic acid (60ml acetic acid plus water to 1000ml) or 0.01-500 parts of methanesulfonic acid or 2-80 parts of formic acid and stir to dissolve, add 1 / 2-2 / 3 in the prescription amount of water for injection;

[0021] 2...

Embodiment 2

[0027] The drug prescription is planned to be 2-10 parts of pazufloxacin mesylate, add 2-10 parts of dilute acetic acid and stir to dissolve, add 500-700 parts of water for injection, dissolve 0.2-5 parts of ethylparaben with water for injection and add In the main drug solution, add 5-15 parts of citric acid, 0.5-30 parts of disodium hydrogen phosphate, 3-7 parts of sodium chloride, and 0.005-3 parts of sodium hyaluronate, stir well, and adjust the pH value to 3.0-7.0 , constant volume, stirring evenly, filtering, semi-finished product inspection after passing, sterilization, aseptic packaging, full inspection, packaging. Preparation method is the same as embodiment 1

Embodiment 3

[0029] The drug prescription is planned to be 2-10 parts of pazufloxacin mesilate, add 2-80 parts of formic acid and stir to dissolve, add 500-700 parts of water for injection, dissolve 3 parts of ethylparaben with water for injection, and then add the main drug solution In the process, add 0.002-1 part of sodium hydroxide, 10-40 parts of sodium acetate, and 3-6 parts of sodium chloride, stir evenly, adjust the pH value to 3.0-7.0, constant volume, stir evenly, filter, and semi-finished products pass the inspection , sterilization, aseptic subpackaging, full inspection, and packaging. The preparation method is the same as in Example 1.

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PUM

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Abstract

A liquid medicine of Pazhushaxing methanesulfonate for treating conjunctivitis, keratitis and keratohelcosis by applying it in eyes is prepared from 12 raw materials including Pazhushaxing methanesulfonate, acetic acid, methanesulfonic acid, formic acid, sodium hydroxide, etc. Its preparing process is also disclosed. Its advantage is high curative effect.

Description

technical field [0001] The invention relates to a liquid preparation containing pazufloxacin mesylate for ophthalmic diseases, including a preparation method thereof. Background technique [0002] Due to the wide application and abuse of antibiotics, bacteria are constantly developing resistance to drugs. In order to solve this problem, new antibiotics are constantly coming out. For the treatment of ophthalmic diseases, the current commonly used ophthalmic drug is the second-generation quinolone drug ofloxacin Eye drops, ciprofloxacin eye drops, and levofloxacin eye drops, along with the continuous generation of bacterial drug resistance, existing drugs have the defect that the cure rate decreases in the treatment of eye diseases. [0003] At present, most of the pazufloxacin mesylate declared by various companies are infusions or injections, which can also be used to treat ophthalmic diseases, but there are gaps between the blood and the eyes, which are composed of blood ve...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/5365A61P27/02
Inventor 毛幼桦赵红侠
Owner ZHEJIANG SHAPUAISI PHARMA
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