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

A pharmaceutical composition of remimazolam

A technology of remimazolam and remimazolam base meter, applied in the field of salt composition, can solve the problems of safety risk, large amount of solution, low concentration of remimazolam, etc.

Active Publication Date: 2020-07-28
FUJIAN SHENGDI PHARM CO LTD +1
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN101501019A discloses the besylate of remimazolam and its polymorph, and discloses a series of possible compositions thereof, but does not disclose how to obtain a stable composition; CN103221414A discloses remimazolam p-toluenesulfonate and its polymorphic forms, but its composition is not disclosed
[0006] At present, remimazolam is not yet on the market. CN103202815A discloses a freeze-dried preparation of remimazolam containing mannitol or glycine. Low, relatively high proportion of excipients, clinical use requires a large amount of solution, very inconvenient
[0007] CN104968348A discloses a composition of benzodiazepines and at least one hygroscopic excipient, especially lactose and / or dextran. Protein, there is a certain safety risk when a large amount of injection

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
  • A pharmaceutical composition of remimazolam
  • A pharmaceutical composition of remimazolam
  • A pharmaceutical composition of remimazolam

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 11

[0034] Pharmaceutical preparation of the present invention is usually made through the following steps:

[0035] 1. Weigh the prescription amount of hydroxyethyl starch 130 / 0.4 (containing monosaccharide added in this step), stir and dissolve in at least one water-based diluent, the water-based diluent is about 80% of the prescription amount, and the water temperature is controlled at 0 -30°C, measure the pH value of the solution, adjust the pH value of the solution with a pH regulator as needed, and control the pH value at 2-4.

[0036] 2. Weigh the prescribed amount of remimazolam, stir and dissolve in the above solution, measure the pH value of the solution after complete dissolution, and adjust the pH value of the solution with a pH regulator as needed, and control the pH value at 2-4.

[0037] 3. Add the aqueous diluent to the final volume, and continue to stir the solution until the mixture is uniform.

[0038] 4. Sterilize the above solution by filtration.

[0039] 5....

Embodiment 12

[0060] Refer to Example II lactose prescription (A01P310 prescription) published in CN104968348A patent and Example 6 glycine prescription of CN103202815A, and use a process published in the patent to freeze-dry the sample to prepare remimazolam freeze-dried powder injection, at a high temperature of 50 ° C The stability test was carried out under the same conditions, and the results are shown in Table 1. In addition, after reconstituting the lyophilized product of lactose and glycine prescription and the lyophilized product of Example 4, Example 7 and Example 10 with water for injection, the stability of the solution at room temperature was investigated, and the results were compared. The results are shown in Table 3.

[0061] The results of Table 1, Table 2 and Table 3 show that the stability of the freeze-dried product of the remimazolam composition in the present invention and the stability of the solution after reconstitution are all better than the patented prescription, es...

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

Provided is a pharmaceutical composition of remimazolam. In particular, provided is a pharmaceutical composition comprising remimazolam or a pharmaceutically acceptable salt thereof and a hydroxyethyl starch and / or a monosaccharide composition. The composition provided by the present invention has a short reconstitution time after remimazolam drying, and is convenient for clinical medication and has good stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a composition containing remimazolam and a pharmaceutically acceptable salt thereof. Background technique [0002] Remimazolam chemical name: (4S)-8-bromo-1-methyl-6-(2-pyridyl)-4H-imidazo[1,2-a][1,4]benzobis Azepine-4-methyl propionate, structural formula as shown in formula (I), this compound is designed by GSK company, developed by PAION company, code name CNS7056, is a kind of super fast-acting sedative, anesthetic, acts on GABAA receptor, Metabolized by tissue esterase, it is split into an inactive metabolite CNS7054, the structural formula of which is shown in formula (II). [0003] [0004] Remimazolam is a sedative that is superior to similar products currently in use, with rapid onset and failure, stable sedative effect, short recovery time, short half-life, inactive metabolites, predictable pharmacokinetics, and a wide therapeutic window , the potential f...

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 Patents(China)
IPC IPC(8): A61K31/5517A61K47/26A61P25/20A61K47/36
CPCA61K31/5517A61K47/26A61K47/36
Inventor 杨晓容陈钟威卢韵
Owner FUJIAN SHENGDI PHARM CO LTD