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Vonoprazan fumarate injection and preparation method thereof

A technology of flunaprazan fumarate and flunaprazan fumarate, which is applied in the field of pharmaceutical preparations, can solve the effects of restricting and inhibiting gastric acid secretion and treating gastric acid-related diseases, unable to meet swallowing, poor water solubility, etc. problems, to achieve excellent long-term stability, stable product quality, and easy preparation.

Active Publication Date: 2016-10-19
NANJING YOKO PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, flunaprazan fumarate has poor water solubility, and preclinical tests have shown that the oral availability of animals is only 10%, which greatly limits the drug's ability to inhibit gastric acid secretion and treat gastric acid-related diseases
Due to the limitation of poor water solubility, its current dosage forms are mainly solid dosage forms, such as tablets, but it still cannot meet the needs of patients with dysphagia and other patients who are not suitable for tablets

Method used

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  • Vonoprazan fumarate injection and preparation method thereof
  • Vonoprazan fumarate injection and preparation method thereof
  • Vonoprazan fumarate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] 20mg / 20mL each, 1000 vials, the prescription is as follows:

[0056] Flunaprazan fumarate 0.1% (calculated as flunaprazan);

[0057] Alpha Lipoic Acid 0.2%;

[0058] Hydroxypropyl-beta-cyclodextrin 0.5%;

[0059] PEG400 0.2%

[0060] Appropriate amount of phosphate buffer solution, adjust the pH to 6.0-6.5;

[0061] The balance of water for injection.

[0062] Preparation:

[0063] (1) Dissolve hydroxypropyl-β-cyclodextrin in an appropriate amount of ethanol at 40-45°C, add flunaprazan fumarate and lipoic acid and stir to dissolve, filter through a 0.22 μm microporous membrane, add Stir with an appropriate amount of water for injection, concentrate under reduced pressure, add water for injection twice during the concentration process, and remove ethanol under reduced pressure to obtain an aqueous solution of cyclodextrin inclusion, which is set aside;

[0064] (2) Separately take 70% of the prescribed amount of water for injection, add PEG400 and stir to dissolve ...

Embodiment 2

[0068] Example 2 Each 40mg / 20mL, 1000, the prescription is as follows:

[0069] Flunaprazan fumarate 0.2% (calculated as flunaprazan);

[0070] Alpha Lipoic Acid 0.3%;

[0071] Hydroxypropyl-beta-cyclodextrin 0.8%;

[0072] PEG400 0.4%

[0073] Appropriate amount of phosphate buffer solution, adjust the pH to 6.0-6.5;

[0074] The balance of water for injection.

[0075] Preparation:

[0076] (1) Dissolve hydroxypropyl-β-cyclodextrin in an appropriate amount of ethanol at 40-45°C, add flunaprazan fumarate and lipoic acid and stir to dissolve, filter through a 0.22 μm microporous membrane, add Stir with an appropriate amount of water for injection, concentrate under reduced pressure, add water for injection twice during the concentration process, and remove the solvent under reduced pressure to obtain an aqueous solution of cyclodextrin inclusion, which is set aside;

[0077] (2) Separately take 70% of the prescribed amount of water for injection, add PEG400 and stir to d...

Embodiment 3

[0081] Example 3 Each 20mg / 20mL, 1000, the prescription is as follows:

[0082] Flunaprazan fumarate 0.1% (calculated as flunaprazan);

[0083] Lysine 0.2%;

[0084] Sulfobutyl ether-4-beta-cyclodextrin 0.6%;

[0085] PVP-K30 0.3%;

[0086] Appropriate amount of phosphate buffer solution, adjust the pH to 6.0-6.5;

[0087] The balance of water for injection.

[0088] Preparation:

[0089] (1) Dissolve sulfobutyl ether-4-β-cyclodextrin in an appropriate amount of ethanol at 40-45°C, add flunaprazan fumarate and lysine and stir to dissolve, filter through 0.22 μm microporous Membrane filtration, add water for injection and stir, concentrate under reduced pressure, add water for injection twice during the concentration process, remove ethanol under reduced pressure, obtain cyclodextrin inclusion aqueous solution, and set aside;

[0090] (2) Separately take 70% of the prescribed amount of water for injection, add PVP-K30 and stir to dissolve to obtain a clear liquid;

[009...

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Abstract

The invention belongs to the technical field of pharmaceutical preparation, and in particular to a potassium ion competitive acid blocker Vonoprazan fumarate injection with the effect of treating gastric acid-related diseases, and a preparation method thereof. The invention overcomes the defect of poor solubility of the main drug Vonoprazan fumarate, uses an inclusion form of sulfobutylether-beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin for solution increase. The prepared injection has the advantages of good stability, high safety and no precipitation during long-term placement, and can meet the medication requirement for the patients who are not convenient for oral administration.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a reversible proton pump inhibitor, i.e. flunaprazan fumarate injection and a preparation method thereof. Background technique [0002] Peptic ulcer is one of the common frequently-occurring diseases. With the development of society and the change of people's lifestyle, the incidence of peptic ulcer is increasing year by year. For this gastric acid-related disease, the current class of drugs with the strongest acid-suppressing effect includes: omeprazole, lansoprazole, pantoprazole, rabeprazole, etc. Because the above-mentioned proton pump inhibitor (PPI) agents have nocturnal acid rebound phenomenon, which affects the therapeutic effect, a new direction of inhibiting gastric acid secretion is derived, namely: potassium ion competitive acid blocker (P-CAB). Different from traditional PPIs, P-CAB works by competitively inhibiting K+ in proton pumps...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/19A61K31/4439A61K47/40A61K47/20A61K47/18A61P1/04
Inventor 闵涛成砚萍朱素华薛峪泉张峰
Owner NANJING YOKO PHARMA
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