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Novel application of gastric acid secretion inhibitor

A technology for gastric mucosa and lonapridine fumarate, which is applied to medical preparations containing active ingredients, organic active ingredients, and the digestive system, and can solve problems such as the treatment and prevention of undisclosed lonapridine fumarate

Inactive Publication Date: 2017-03-22
王虹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is also no disclosure that lonapridine fumarate can treat and prevent the above-mentioned diseases through intravenous administration

Method used

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  • Novel application of gastric acid secretion inhibitor
  • Novel application of gastric acid secretion inhibitor
  • Novel application of gastric acid secretion inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Preparation of Lonapridine Fumarate Small Needle Injection:

[0105] Specification: 5ml: 10mg

[0106] 1. Prescription:

[0107]

[0108] Second, the preparation process:

[0109] 1. Weighing and dosing:

[0110] Weigh the prescribed amount of glucose and edetate calcium disodium, add it to the water for injection with 80% of the total amount prepared (water temperature <50°C), stir and dissolve; then weigh the prescribed amount of lonapridine and add it to the liquid preparation tank Stir well until completely dissolved. Then add 0.1% (g / ml) activated carbon for needles, stir evenly, let stand for adsorption for 15 minutes, and filter the medicinal solution through a 0.45 μm filter to remove carbon.

[0111] 2. pH adjustment:

[0112] Adjust the pH value to 2.5-3.5 with 0.1mol / L hydrochloric acid solution, add water for injection to the full amount, and filter the medicinal solution through a 0.22 μm microporous filter.

[0113] 3. Filling and sealing

[0114...

Embodiment 2

[0119] Preparation of Lonapridine Fumarate Injection:

[0120] Specifications: 20ml: 20mg

[0121] 1. Prescription:

[0122]

[0123] Second, the preparation process:

[0124] 1. Weighing and dosing:

[0125] Weigh the prescribed amount of glucose and edetate calcium disodium, add it to the water for injection with 80% of the total amount prepared (water temperature <50°C), stir and dissolve; then weigh the prescribed amount of lonapridine and add it to the liquid preparation tank Stir well until completely dissolved. Then add 0.1% (g / ml) activated carbon for needles, stir evenly, let stand for adsorption for 15 minutes, and filter the medicinal solution through a 0.45 μm filter to remove carbon.

[0126] 2. pH adjustment:

[0127] Adjust the pH value to 2.5-3.5 with 0.1mol / L hydrochloric acid solution, add water for injection to the full amount, and filter the medicinal solution through a 0.22 μm microporous filter.

[0128] 3. Filling and sealing

[0129] After pas...

Embodiment 3

[0134] Preparation of Lonapridine Fumarate Large Infusion Injection:

[0135] Specification: 100ml: 20mg

[0136] 1. Prescription:

[0137]

[0138] Second, the preparation process:

[0139] 1. Weighing and dosing:

[0140] Weigh the prescribed amount of glucose and edetate calcium disodium, add it to the water for injection with 80% of the total amount prepared (water temperature <50°C), stir and dissolve; then weigh the prescribed amount of lonapridine and add it to the liquid preparation tank Stir well until completely dissolved. Then add 0.1% (g / ml) activated carbon for needles, stir evenly, let stand for adsorption for 15 minutes, and filter the medicinal solution through a 0.45 μm filter to remove carbon.

[0141] 2. pH adjustment:

[0142]Adjust the pH value to 5.0-6.5 with 0.1mol / L hydrochloric acid or 0.1mol / L sodium hydroxide solution, add water for injection to the full amount, and filter the drug solution through a 0.22μm microporous filter.

[0143] 3. Pa...

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Abstract

The invention relates to a novel application of a gastric acid secretion inhibitor. The novel application is that vonoprazan fumarate is injected into human body through intravenous administration to inhibit gastric acid secretion, the pH value of stomach is increased, at the same time, the activity of pepsin is inhibited, on the other aspect, the factor of damaging mucosa is reduced, blood platelets can aggregate on the bleeding parts more easily, the solidified blood clots are difficult to dissolve, the blood can be stopped in the bleeding parts, the blood solidification is promoted, the blood crust is stabilized, and the mucosa is repaired. The gastric acid secretion inhibitor can be used to treat and prevent subsequent acute damage of gastric mucosa under a stress state, severe diseases (cerebral hemorrhage, severe wounds, etc.), and upper gastrointestinal hemorrhage caused by gastric operation.

Description

[0001] Technical field: [0002] The invention relates to a new administration route and a new application of a gastric acid secretion inhibitor. [0003] Background technique: [0004] Lonapridine fumarate has the following chemical structure: [0005] [0006] Chemical name: 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrol-3-yl]-N-methylmethylamine monofumarate [0007] English chemical name: [0008] 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate [0009] Molecular formula: C 17 h 16 FN 3 o 2 SC 4 h 4 o 4 [0010] Molecular weight: 461.46 [0011] CAS number: 881681-01-2 [0012] Lonapridine fumarate is a derivative of pyrrole and belongs to a new type of potassium ion competitive acid blocker. At present, in the world, only Japan has obtained marketing authorization for lonapridine fumarate, and its administration route is gastrointestinal administration, and the dosage form is tablets. The indications...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/08A61K9/19A61P1/04A61P1/00A61P1/14A61P35/00A61P9/10A61P17/02A61P11/06A61P31/04
Inventor 王虹
Owner 王虹
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