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Medicinal composition for eradicating helicobacter pylori and preparation method thereof

A technology of Helicobacter pylori and its composition is applied in the field of medicines and manufacturing for inhibiting Helicobacter pylori, can solve the problems of reducing the effectiveness of antibiotic eradication, poor drug absorption, and not as expected, and achieves the effect of improving the bioavailability rate

Inactive Publication Date: 2011-08-10
SYNMOSA BIOPHARMA CORP +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The study found that although the three-in-one therapy has the effect of eradicating H. pylori, the actual rate of successful eradication of H. pylori is not as expected. Take the domestic clinical three-in-one treatment as an example. The first treatment method is to take 5 pills each time, including one 20mg omeprazole, two 500mg amoxicillin and two 250mg clistomycin According to this dose, it should be taken once in the morning and once in the evening, and taken continuously for seven to fourteen days; in addition, there is a second treatment method of taking The three-in-one drug package also needs to be taken three times a day, and an additional 20mg omeprazole is taken in the morning and evening
The disadvantages of these two treatment methods are that there are too many pills to take, it is easy to confuse the dosage or type of medicine to be taken, it is not easy to carry, and it is difficult to swallow, and patients who take the second treatment often forget to take Ogilvy again. The condition of prazole caused the inability to take the medicine in a timely and quantitative manner, resulting in poor compliance with the medication; 2. The dosage of the drug during the entire treatment period was not enough, which was also caused by the failure to take the prescribed dose; 3. The stability of the drug in the stomach was not good 4. The patient's specific constitution and allergic reaction lead to early withdrawal of the drug; and 5. H.pylori is resistant to the drug, and the antibiotic metronidazole used in the three-in-one therapy fails to treat the drug. Patients are prone to develop secondary drug resistance, so when using this drug, attention should be paid to its dose, course of treatment and patient cooperation
In addition, U.S. Patent No. 5,196,205 discloses a method for treating gastritis and gastroduodenal ulcer and other digestive system diseases caused by H. pylori, which uses bismuth compounds (bismuth), penicillins and tetracyclines antibiotics, And given three tablets (one for each active ingredient) several times a day, this treatment is complicated
[0006] On the other hand, the stability of antacids such as omeprazole will change with the pH value of the environment in which it exists. When it exists in an alkaline environment, it can maintain its stability. In an acidic environment, it will decompose rapidly. Therefore, omeprazole cannot exist stably in the gastric juice and is easily decomposed. Therefore, it is usually given in the form of an intestinal coating, so that omeprazole can be absorbed in the intestinal tract and inhibit the gastric gland cells from secreting gastric acid through the internal circulation system. Therefore, if If omeprazole acts directly in the acidic environment of the stomach, omeprazole cannot effectively inhibit the secretion of gastric acid, causing the antibiotics to still act in the acidic environment of the stomach, reducing the effectiveness of antibiotics in eradicating H.pylori

Method used

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  • Medicinal composition for eradicating helicobacter pylori and preparation method thereof
  • Medicinal composition for eradicating helicobacter pylori and preparation method thereof
  • Medicinal composition for eradicating helicobacter pylori and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Manufacturing method of suspension dosage form pharmaceutical composition for eradicating H.pylori

[0034] The active ingredients of the suspension formulation pharmaceutical composition for eradicating H. pylori in the embodiment of the present invention include 20 mg of famotidine, 500 mg of clarithromycin and 1 g of amoxicillin; 20mg of famotidine can be replaced by 290mg of ranitidine / bismuth citrate, where both famotidine and ranitidine are hydrogen Proton blocker (H 2 Blocker). The production method of the suspension dosage pharmaceutical composition for eradicating H. pylori in the embodiment of the present invention is exemplified by the production method of the pharmaceutical composition containing famotidine (famotidine), the pharmaceutical composition contains 20mg of famotidine (famotidine) , 500 mg of clarithromycin and 1 g of amoxicillin, Ac-Di-Sol as a disintegrating agent, colloidal silicon dioxide as a sliding agent, xanthan gum, carboxymethylcellu...

Embodiment 2

[0116] Manufacturing method of effervescent lozenge type pharmaceutical composition for eradicating H.pylori

[0117] The active ingredients of the effervescent lozenge-type medical composition for eradicating H. pylori in the embodiment of the present invention include 20 mg of omeprazole, 500 mg of clarithromycin and 1 g of amoxicillin, Sodium bicarbonate (sodium bicarbonate) and anhydrous citric acid (anhydrous citric acid) as a foaming agent, sodium benzoate (sodium propionate) as an antibacterial agent, and colloidal silicon dioxide (colloidal silicon dioxide) as a slip agent, as Suspending agent carboxymethylcellulose sodium (Carboxymethylcellulose Sodium) and hydroxypropylmethylcellulose (hydroxypropylmethylcellulose), and flavoring agent, its ingredient list and production process are as follows:

[0118]

Ingredients of Foaming Tablet Type Pharmaceutical Composition

theoretical weight

(mg) / 20ml

scope

Amoxycilli...

Embodiment 3

[0128] The manufacture method of the powder dosage form pharmaceutical composition for eradicating H.pylori:

[0129]

Components of powder dosage form pharmaceutical composition

theoretical weight

(mg) / 20ml

scope

Amoxycillin

101.6

11.5%

250~1000mg

Clithomycin

51.2

5.8%

125~500mg

Omeprazole

4.0

0.5%

5~20mg

Mannitol

350.0

39.6%

15~75%

Carboxypropylmethylcellulose (HPMC)

42.0

4.7%

2~15%

Sanxianjiao

3.0

0.3%

0.2~15%

Sodium Propionate

14.0

1.6%

0.02~1.5%

aspartame

75.0

8.5%

1~25%

sodium benzoate

168.0

19.0%

5~25%

Polyvinylpyrrolidone

2.0

0.2%

0.1~8%

Magnesium stearate

3.5

0.4%

0.2~5%

[0130] lemon powder

70.0

7.9%

2~15%

Total

884.3

100.0%

...

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PUM

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Abstract

The invention discloses a medicinal composition for eradicating helicobacter pylori, comprising an effective dose of hydantoinate antibiotics, an effective dose of macrolide antibiotics, an effective dose of antacid and a pharmaceutically-acceptable carrier, wherein the medicinal composition is of a powder form, a suspension form or an effervescent tablet form. The invention further discloses a method for producing the medicinal composition for eradicating the helicobacter pylori, comprising the following steps of: mixing the effective dose of hydantoinate antibiotics with the pharmaceutically-acceptable carrier to form a first mixture; mixing the effective dose of macrolide antibiotics with the pharmaceutically-acceptable carrier to form a second mixture; mixing the first mixture with the second mixture, adding the antacid and mixing to form a third mixture; and mixing a slipping agent, an antibacterial agent, a lubricating agent, a suspending aid and the third mixture to form the medicinal composition in a suspension form.

Description

technical field [0001] The present invention relates to a drug and a manufacturing method for inhibiting Helicobacter pylori, in particular to a pharmaceutical composition in the form of foaming tablets, suspensions or powders for eradicating Helicobacter pylori and a manufacturing method thereof. Background technique [0002] Helicobacter pylori (Helicobacter pylori, hereinafter referred to as H. pylori) is a micro-aerobic Gram-negative (Gram-negative) bacillus that mainly lives in the mucosal surface layer of the stomach of humans or other animals, that is, gastric epithelial cells and gastric mucus. Between layers (gastric mucus layer). H. pylori infection is very common, more than half of the world's people have been infected by H. pylori. Studies have pointed out that the persistent infection of H. pylori can cause lesions in the upper gastrointestinal tract. It is known that the infection of this bacteria may cause chronic active gastritis, peptic ulcer, and non-ulcer...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K9/14A61K9/20A61K9/10A61P31/04A61P1/00
Inventor 周瑞铭鲍力恒林智晖张嘉纹林家萱
Owner SYNMOSA BIOPHARMA CORP
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