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Ciprofloxacin mandelate, ofloxacin mandelate and preparation process thereof

A technology of ofloxacin mandelate salt and ofloxacin mandelate, applied in the field of pharmacy

Inactive Publication Date: 2005-05-04
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, there is no dual-action drug that can realize contraception, avoid sexually transmitted diseases, and have a therapeutic effect on local vaginal inflammation in China.

Method used

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  • Ciprofloxacin mandelate, ofloxacin mandelate and preparation process thereof
  • Ciprofloxacin mandelate, ofloxacin mandelate and preparation process thereof
  • Ciprofloxacin mandelate, ofloxacin mandelate and preparation process thereof

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0018] 1. Process

[0019] ①Theoretical basis

[0020] Both ciprofloxacin and ofloxacin are amphoteric compounds. Its structure has a weakly subtractive tertiary nitrogen atom and a weakly acidic fatty acid carboxyl group. It can exist in the form of an internal salt with low water solubility. In order to increase its water solubility, it can be combined with a strong inorganic acid or a strong organic acid. .

[0021] Mandelic acid is a strong aromatic α-OH group with a pH of 2. The tertiary nitrogen atoms in the structures of ciprofloxacin and ofloxacin can be combined with mandelic acid to form a salt.

[0022] The reaction formula of ciprofloxacin mandelic acid salt is as follows:

[0023]

[0024] The reaction formula of ofloxacin mandelic acid salt is as follows:

[0025]

[0026] ②Process

[0027] a. Feeding mol ratio

[0028] Mandelic acid: Ciprofloxacin or Ofloxacin = 1.5-2.0:1

[0029] b. Operation process

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PUM

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Abstract

The invention discloses mandelic acid ciprofloxacin salt and mandelic acid ofloxacin salt which combine mandelic acid capable of killing spermatozoa and trichomoniasis with third-generation quinolone broad-spectrum antibacterial and anti-inflammatory drugs and preparation thereof Technology, mandelic acid is an aromatic α-OH group strong acid, pH is 2, the tertiary nitrogen atom in the structure of ciprofloxacin and ofloxacin can be combined with mandelic acid to form a salt in the same way. The mandelic acid ciprofloxacin salt and mandelic acid ofloxacin salt can be decomposed into two original components under the condition of pH4.6-pH4.8, and exert the pharmacological effects of each single component. The mandelic acid ciprofloxacin salt and the mandelic acid ofloxacin salt of the present invention have been proved by clinical tests to have ideal effects.

Description

1. Technical Field [0001] The invention belongs to the field of pharmacy, and relates to medicines and preparation processes thereof, in particular to ciprofloxacin mandelate and almonds that combine mandelic acid with spermicide and trichomoniasis and third-generation quinolone broad-spectrum anti-inflammatory drugs together Ofloxacin acid salt and its preparation process. 2. Background technology [0002] Ciprofloxacin and Ofloxacin are the third-generation quinolone antibacterial and anti-inflammatory drugs, which are widely used in clinical practice, mainly for infections of the respiratory system and urinary system, especially for the treatment of gonorrhea. However, due to the poor water solubility of such drugs, manufacturers currently prepare them into hydrochloric acid or lactate in order to increase their water solubility and drug absorption, and improve the bioavailability of the preparations for clinical applications. Neither hydrochloric acid nor lactic acid has any ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/56C07D498/06
Inventor 李生正王云彩
Owner XI AN JIAOTONG UNIV
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