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Medicament of ilaprazole chemical structure and application thereof

A technology of ilaprazole and drugs, applied in the field of drugs with chemical structure of ilaprazole and its application, capable of solving problems such as increasing the risk of gastric cancer

Active Publication Date: 2011-07-13
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Epidemiological surveys have shown that Hp infection increases the risk of gastric cancer; eradicating Hp can block or delay the further development of gastric mucosal atrophy and intestinal metaplasia, but whether it can reverse these two lesions needs further research; eradicating Hp can reduce early The recurrence rate of gastric cancer after surgery; simple Hp infection can induce gastric cancer in Mongolian gerbils; Hp carrying certain virulence genes may be more closely related to the occurrence of gastric cancer, but there is no clear conclusion yet

Method used

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  • Medicament of ilaprazole chemical structure and application thereof
  • Medicament of ilaprazole chemical structure and application thereof
  • Medicament of ilaprazole chemical structure and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Research on the Anti-Helicobacter Pylori Activity of Pharmaceutical Compositions Containing Ilaprazole

[0021] This example investigates the inhibitory effect of a pharmaceutical composition containing ilaprazole on clinical isolates of Helicobacter pylori. The minimum inhibitory concentrations (MICs) of dual drugs, that is, the pharmaceutical composition of ilaprazole and levofloxacin, and the pharmaceutical composition of ilaprazole and metronidazole on clinically isolated Helicobacter pylori strains were determined by agar dilution method .

[0022] Serially dilute ilaprazole and antibiotics (levofloxacin or metronidazole) 2 times with sterile water. Both azole (IY) and omeprazole (OMP) were 12.5-1.57 μg / ml. Table 1 shows the grouping situation of the dual drug combination and the minimum inhibitory concentration results against Helicobacter pylori.

[0023] Table 1 The minimum inhibitory concentration results (μg / ml) of anti-Helicobacter pylori of dua...

Embodiment 2

[0026] Example 2: Research on the Anti-Helicobacter Pylori Activity of Pharmaceutical Compositions Containing Ilaprazole

[0027] This example investigates the inhibitory effect of a pharmaceutical composition containing ilaprazole on clinical isolates of Helicobacter pylori. The minimum inhibitory concentrations (MICs) of the triple drug combination, i.e. ilaprazole, levofloxacin and metronidazole, against clinically isolated Helicobacter pylori strains were determined by agar dilution method.

[0028] Triple drugs are divided into the following 4 groups: ilaprazole (IY) 1.57μg / ml + metronidazole + levofloxacin; ilaprazole (IY) 1.57μg / ml + metronidazole + gemifloxacin; omeprazole (OMP ) 1.57 μg / ml+metronidazole+levofloxacin; ilaprazole (IY) 1.57 μg / ml+amoxicillin+clarithromycin triple drug anti-H. pylori minimum inhibitory concentration results are shown in Table 2.

[0029] Table 2 The minimum inhibitory concentration results (μg / ml) of triple drug anti-helicobacter pylori ...

Embodiment 3

[0033] Embodiment 3: the preparation method of pharmaceutical composition of the present invention

[0034] The preparation method of the pharmaceutical composition of the present embodiment comprises the following steps:

[0035] 1) Take materials according to the following parts by weight ratio: 1 part of ilaprazole, 100 parts of metronidazole, 200 parts of levofloxacin, 10-75 parts of microcrystalline cellulose, 5-50 parts of mannitol, hydroxypropylmethyl 0.2-30 parts of base cellulose, 1-30 parts of crospovidone, 0.1-5.0 parts of magnesium stearate; Azole and levofloxacin are passed through a 60-100 mesh nylon sieve, microcrystalline cellulose and crospovidone are respectively passed through a 60-100 mesh nylon mesh, and mannitol is crushed and passed through a 80-120 mesh (preferably 100 mesh) nylon mesh sieve ;

[0036] 3) The hydroxypropyl methylcellulose is formulated into an adhesive with a viscosity of 5-35 centipoise with 50-95% medicinal ethanol by volume percent...

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Abstract

The invention provides a medicament of an ilaprazole chemical structure and application thereof. The medicament comprises the following components in parts by weight: 200 parts of ilaprazole or pharmaceutically acceptable salts and hydrates thereof, 0.5-2 parts of nitromidazoles antibiotics and 1-5 parts of quinolones antibiotics. The inhibition activity of the medicament composition is at least 3-4 times higher than the activities of the omeprazole and the antibiotic medicaments or the combined activity of ilaprazole, amoxicillin and clarithromycin, the medicament can be used for more effectively inhibiting or killing helicobacter pylori and treating duodenal ulcer, gastric ulcer and / or chronic gastritis.

Description

technical field [0001] The invention relates to a pharmaceutical composition for inhibiting or killing Helicobacter pylori, in particular to a pharmaceutical composition containing ilaprazole and use thereof. Background technique [0002] Helicobacter pylori (Hp) is an important pathogenic factor of chronic gastritis and peptic ulcer, and Hp is also related to gastric cancer. Epidemiological surveys have shown that Hp infection increases the risk of gastric cancer; eradicating Hp can block or delay the further development of gastric mucosal atrophy and intestinal metaplasia, but whether it can reverse these two lesions needs further research; eradicating Hp can reduce early The recurrence rate of gastric cancer after surgery; simple Hp infection can induce gastric cancer in Mongolian gerbils; Hp carrying certain virulence genes may be more closely related to the occurrence of gastric cancer, but there is no clear conclusion yet. The occurrence of gastric cancer is the resul...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/4439A61P31/04A61P1/04
Inventor 周淦张伟周宏灏侯雪梅谭竞解荷芝
Owner LIVZON PHARM GRP INC
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