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Pharmaceutical comprising myramistin

A myristoyl amino, pharmaceutical preparation technology, applied in the directions of medical preparations containing active ingredients, drug combinations, drug delivery, etc., can solve the problems of limited scope of effectiveness, insufficient efficacy, inability to combine and the like

Active Publication Date: 2013-01-09
MEGAINPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of these pharmaceutical preparations is that the range of effectiveness of the specific regimen is very limited, or the potency is insufficient compared to the proposed technical regimen
Moreover, this pharmaceutical preparation cannot be effectively combined with some matrices and pharmaceutical preparations with different expected effects, because of the formation of deposited coordination compounds

Method used

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  • Pharmaceutical comprising myramistin
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  • Pharmaceutical comprising myramistin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In order to demonstrate the technical solution of the invention, various variants of the composition of the formulation of the patent application were used. In Table 1, some of the compositions investigated, in particular those used in the Examples discussed below, are shown.

[0035] Variants of the composition of Table 1 (in % by weight)

[0036]

[0037] Notes: *Monohydrate

Embodiment 2

[0039]The minimum inhibitory concentration (MIC) for a test culture of a coronavirus (human coronavirus OC43) was determined in vitro on human embryonic kidney cell cultures. Using composition Z1 (two components in a ratio of 6:1) and the formulation of reference 3 (pure benzyldimethyl-(3-myristoylamino]propyl) chlorinated ammonium) and pure dimethyl-[3-(myristoylamino)propyl]amine oxide (AA). Research was conducted in parallel through the following protocols:

[0040] Phase 1 test virus + myrismidopropyl dimethyl benzyl ammonium chloride (myramistin) (appropriate concentration)

[0041] Stage 2 incubation (2 hours)

[0042] Phase 3 Mix the neutralizing substance of the composition (eg 25% embryonic serum from cows) and incubate the composition for 10-20 min.

[0043] Stage 4 infection of susceptible cell cultures (e.g. human embryonic kidney)

[0044] Phase 5 incubation (5-8 days)

[0045] Results of Phase 6 assays for hemadsorption and cytopathic effects and symplast fo...

Embodiment 3

[0051] Guinea pigs and rabbits were used to study the local irritation caused by the formulations of the patent application to the skin and connective tissue membranes as well as to the vaginal mucosa. Dogs were used to study local irritation of the urethral and bladder mucosa.

[0052] The data found demonstrate that application of compositions Z4 and Z9 to the skin does not cause visible and histological changes over the course of 40 days. Increasing the total concentration of ingredients in the formulation to 5.0% by weight resulted in mild xeroderma and insignificant atrophy of the epidermis upon application to day 30.

[0053] Meanwhile, in references 8, 20, and 23, solutions of pure Ach already caused skin irritation at concentrations exceeding 1% by weight, and higher concentrations (2-3% by weight) brought Come visibly greater skin changes.

[0054] Skin irritation was evident by day 10 when a 0.01% solution of pure AA in 70% alcohol was applied.

[0055] A solution...

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PUM

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Abstract

The invention relates to a pharmaceutical including benzyldimethyl(3-[myristoylamino]propyl)ammonium chloride in the monohydrate form or in unhydrated form. The pharmaceutical further comprises dimethyl(3-[myristoylamino]propyl)ammonium oxide and / or dimethyl(3-[myristoylamino]propyl)amine in the appropriate pharmaceutical solvent.

Description

technical field [0001] The present invention relates to the field of medicine and pharmaceutical industry. It can be used for the development, preparation and use of therapeutic and prophylactic formulations for humans and animals. Background technique [0002] The synthesis and use of quaternary ammonium salts also containing amide groups was first described in US Patent 2,459,062 (Ref. 1). Specifically, in Example 1, [myristoylamido]propyl)dimethylbenzyl chloride was synthesized by reacting [(myristoylamido)propyl]dimethylamine with benzyl chloride in benzene Ammonium. [0003] In this patent, the activity of the prepared product against standard Staf strains was demonstrated. At room temperature, the product described by the inventor is a semi-hard substance with a melting temperature of 54°C (column 3, lines 69-70). In Example 1 no further studies confirming the structure of the product obtained are mentioned. However, the studies of the present invention on the iso...

Claims

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Application Information

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IPC IPC(8): A61K31/131A61K31/14A61K31/16A61K45/06
CPCA61K31/16A61K31/131A61K45/06A61K31/14A61P1/02A61P1/04A61P11/00A61P13/00A61P15/00A61P17/02A61P27/02A61P27/16A61P29/00A61P31/00A61P31/10A61P31/12A61K2300/00A61K9/0043A61K9/0046A61K9/0048A61K9/06A61K9/08
Inventor A·鲁德科
Owner MEGAINPHARM
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