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Medicament combination preparation of medicinal compound containing cy-ethyl razepam

A technology of composition and complex, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., and can solve problems such as increased solubility, narrow therapeutic window, and poor safety in clinical application

Inactive Publication Date: 2011-05-11
LIAONING LIFENG SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is cyclopyrimidine or stereoisomers, prodrugs, pharmaceutically acceptable salts, double salts or solvated cyclopyrimidines, which are representative active ingredients of aromatic heterocyclic pyrimidine derivatives and analogs. The drug delivery system of Naiping compound as the active ingredient is studied, and a safe drug delivery system suitable for it is obtained, which solves technical problems such as a very narrow therapeutic window and poor safety in clinical application. For aromatic heterocyclic pyrimidine derivatives and similar Modified the chemical structure of the drug to obtain cyclopyridine. After the safety and effectiveness of cyclopyridine were studied, they were better than vancomycin and ciprofloxacin, and the antibacterial spectrum was better than that of vancomycin and ciprofloxacin. Broad, solubility increased significantly

Method used

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  • Medicament combination preparation of medicinal compound containing cy-ethyl razepam
  • Medicament combination preparation of medicinal compound containing cy-ethyl razepam
  • Medicament combination preparation of medicinal compound containing cy-ethyl razepam

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1, cyclopyriminapine maleate injection

[0028] 【prescription】

[0029] Cyclopyrene Maleate 125g

[0030] Glucose 50g

[0031] Add water for injection to 1000ml

[0032] 【Method】

[0033] ①Dissolve glucose powder in water for injection to make a solution of about 50%~60%, adjust the pH value to about 4.2~4.6 with 10% HCl, heat and boil for 10~20min, add 0.05% activated carbon, stir well, and cool to room temperature, filter out activated carbon, measure the content, and set aside.

[0034] ②Take the dosing amount of glucose (calculated as volume according to the content), add cyclopyridine maleate, heat to 40-50°C, stir to dissolve, dilute to the dosing amount, cool to room temperature, and measure the pH value at 4.2-4.8 Finely filter until clear, fill and seal in 2ml ampoules, and sterilize with circulating steam at 100°C for 30 minutes.

Embodiment 2

[0035] Embodiment 2, cyclopyriminapine maleate injection

[0036] This product is a sterilized aqueous solution of cordocaine hydrochloride. Cyclopyriminapine containing maleate should be 95% to 105% of the labeled amount.

[0037] 【prescription】

[0038] Cyclopyrene Maleate 125g

[0039] Sodium chloride 9g

[0040] Add water for injection to 1000ml

[0041] [Preparation method] Dissolve sodium chloride in water for injection, add cyclopyrimidine maleate and stir to dissolve, dilute to the full amount, adjust the pH to 3.5-5.0 with dilute hydrochloric acid, add activated carbon, filter, potting, 100°C Circulating steam sterilization for 3 minutes, that is.

Embodiment 3

[0042] Embodiment 3, Cyclopyrimine Injection

[0043] 【prescription】

[0044] Cyclopyrene 1250g Glycerin 500g

[0045] Ethanol (95%) 1000ml water for injection to 10000ml

[0046] [Preparation method] Dilute ethanol with water for injection to about 70%, add lanatoside triacetate, stir continuously to dissolve, add glycerin, dilute with water for injection to the total amount, filter until clear, and seal in a 2ml ampoule. Sterilize with flowing steam at 100°C for 30 minutes.

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PUM

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Abstract

The invention relates to medicament combination preparation of medicinal compound taking cy-ethyl razepam medicinal compound containing cy-ethyl razepam or stereoisomer, pro-medicinal, medicinal salt, complex salt or / and salvation as effective constituent. The medicament combination preparation adopts the technical scheme that the cy-ethyl razepam medicinal compound, which has a general formula (1) structure and contains the cy-ethyl razepam or the stereoisomer, the pro-medicinal, the medicinal salt, the complex salt and the solvation, is taken as the effective constituent and forms the medicament combination preparation with a medicament carrier capable of being received on the pharmacy; and the preparation formulation is any preparation formulation said on the pharmacy. The invention also discloses an application of the medicament combination preparation in the process of treating the infection of bacteria taken as gram-positive bacteria like staphylococcus, pneumococcus, enterococcus faecalis, streptococcus, streptococcus bovis, streptococcus pneumoniae, peptostreptococcus, festering streptococcus pneumoniae, festering streptococcus pneumoniae, streptococcus pyogenes, streptococcus agalactiae, viridans streptococci, streptococcus bovis, streptococcus agalactiae B, group green streptococcus, corynebacterium diphtheriae and other bacteria.

Description

technical field [0001] The present invention belongs to the field of pharmacy, and particularly relates to novel aromatic heterocyclic pyrimidine derivatives and analogs, and cyclopyrimidine drugs or stereoisomers, prodrugs, pharmaceutically acceptable salts, double salts or solvents represented by them The modified cyclic pyrimidine compound is used as an active ingredient, and the medicinal compound is used as an active ingredient and a pharmaceutical composition preparation formed by a pharmaceutically acceptable drug carrier, and the pharmaceutical composition preparation is Gram-positive bacteria in the treatment of bacteria: Staphylococcus, Pneumococcus, Enterococcus faecalis, Streptococcus, Streptococcus bovis, Streptococcus pneumoniae, Peptostreptococcus, Streptococcus pyogenes, Streptococcus pyogenes, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, bovine Streptococcus, Streptococcus agalactiae B, Group viridans Streptococcus, diphtheriae, Ba...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P31/04A61P31/00
CPCA61K9/0004A61K9/0014A61K9/0019A61K9/0048A61K9/06A61K9/1075A61K9/146A61K9/1652A61K9/19A61K9/2059A61K9/284A61K9/4858A61K31/519A61P31/00A61P31/04C07D487/04
Inventor 徐利锋陈烨周云鹏刘举王洋刘革萍
Owner LIAONING LIFENG SCI & TECH DEV
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