Unlock instant, AI-driven research and patent intelligence for your innovation.

Methylsulfonic acid nafamostat lyophilized powder injection

A technology of nafamostat mesylate and freeze-dried powder injection, which is applied in the field of medicine and can solve the problems that the aqueous injection cannot meet the stability requirements

Inactive Publication Date: 2012-12-26
ZHUHAI EBANG PHARMA
View PDF1 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Physical and chemical properties: This product is a white crystalline powder, easily soluble in formic acid (>1g / ml), slightly soluble in water (4.91g / ml), insoluble in ethanol, with a melting point of about 260°C (decomposition), because it is an ester It is easy to degrade in water (especially hot water), alkaline and strong acid solution, and the water injection can not meet the stability requirements of storage and clinical use, thus limiting its clinical use

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Methylsulfonic acid nafamostat lyophilized powder injection
  • Methylsulfonic acid nafamostat lyophilized powder injection
  • Methylsulfonic acid nafamostat lyophilized powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020]

[0021] Preparation Process:

[0022] Preparation of drug solution: Weigh the prescribed amount of nafamostat mesylate raw material and dissolve it in water for injection, add the prescribed amount of mannitol and stir to dissolve it, then add water for injection to the prescribed amount;

[0023] Adjust the pH value: add an appropriate amount of citric acid buffer to adjust the pH value of the liquid to 3.0-4.5.;

[0024] Pyrogen removal: add 0.02% total volume of activated carbon for injection to the above medicinal solution, stir at 40°C for 20 minutes, decarbonize by microporous membrane filtration; collect the filtrate;

[0025] Sterilization: The above solution is sterilized and filtered under positive pressure with a sterilizing filter, rubber stoppers, etc. are sterilized by moist heat, and equipment and pipelines such as batching tanks, liquid storage tanks, water for injection tanks, freeze dryers, etc. are sterilized online;

[0026] Filling: carry out ...

Embodiment 2

[0032]

[0033]

[0034] The preparation method is the same as in Example 1, and the dosage of mannitol is 30g.

Embodiment 3

[0036]

[0037] The preparation method is the same as in Example 1, and the consumption of mannitol is 60g.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the field of pharmaceutical preparation, and in particular relates to a methylsulfonic acid nafamostat lyophilized powder injection and a method for preparing the powder injection. The lyophilized powder injection consists of active ingredient methylsulfonic acid nafamostat, an excipient and a pH conditioning agent, wherein the pH conditioning agent is an organic acid or organic buffer system, the pH values of the solution before or after being lyophilized are kept in the range of 3.0-4.5 through using the pH conditioning agent, and the pharmaceutical stability is effectively maintained.

Description

technical field [0001] The invention relates to a protease inhibitor nafamostat mesylate for treating pancreatitis, in particular to a nafamostat mesylate freeze-dried powder injection and a preparation method thereof. It belongs to the field of medical technology. Background technique [0002] Nafamostat mesylate is a synthetic protease inhibitor. It is mainly used for the treatment of various pancreatitis, and it can also be used for anticoagulation during shock, open heart surgery and extracorporeal circulation, early treatment of DIC and treatment of autoimmune diseases. [0003] The molecular formula, molecular weight, structural formula and physicochemical properties of nafamostat mesylate are as follows: [0004] Molecular formula: C 19 h 17 N 5 o 2 ·2CH 4 o 3 S [0005] Molecular weight: 539.58 [0006] Structural formula: [0007] [0008] Physical and chemical properties: This product is a white crystalline powder, easily soluble in formic acid (>1...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/24A61K47/10A61P1/16A61P7/02A61P7/08A61P37/02
Inventor 李翱吴浩山
Owner ZHUHAI EBANG PHARMA