Cyprofloxacine solution for infusion

FIELD: pharmaceutical industry, in particular cyprofloxacine solution.

SUBSTANCE: claimed solution contains cyprofloxacine hydrochloride, sodium salt of ethylenediamine-N,N,N1,N1-tetraacetic acid, α-hydroxypropionic acid, sodium chloride, water for injections.

EFFECT: drug of increased biological availability without side effects.

3 tbl

 

The invention relates to pharmaceutical industry and for solution for infusion ciprofloxacin.

Ciprofloxacin - 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-(1-piperazinil)-3-quinoline-carboxylic acid has an antibacterial effect (Handbook "Drugs" Mashkovsky PPM, M, "Medicine", 2000, Vol.2, str).

There are various dosage forms on the basis of Ciprofloxacin mostly in the form of tablets or microcapsules.

The active ingredient ciprofloxacin has unpleasant and long-lasting bitter taste. In addition to the complete taste masking many active substances necessarily require quick and complete release. You must also consider the possibility of deviation values of pH in the stomach may be reduced acidity, often observed in the elderly. This means that in weakly acidic conditions, at about pH 4.5, must be ensured rapid dissolution of the active substance.

For example, there are:

- tablet ciprofloxacin, contains as inactive ingredients corn starch, microcrystalline cellulose, crosspovidone, Aerosil, magnesium stearate (U.S. Pat. Of the Russian Federation No. 2131265);

the microcapsule containing core ciprofloxacin, the shell of which is a film of water-insoluble neutral complex with methyl and/and and ethyl esters of polymethacrylic acid and/or Quaternary ammonium compounds of polymethacrylic acid and/or ethyl cellulose. The microcapsule further comprises a water-soluble polymer, a plasticizer, a wetting agent (U.S. Pat. Of the Russian Federation No. 2110255);

- antimicrobial composition containing-arteether, ciprofloxacin and sterile vegetable oil (U.S. Pat. No. 2241457).

Injectable forms are required to create high concentrations of ciprofloxacin in the blood in the treatment of severe forms of the disease.

As a prototype of the selected solution for infusion ciprofloxacin, have antibacterial properties, including sodium chloride and water for injection (Handbook "Drugs" Mashkovsky PPM, M, "Medicine", 2000, Vol.2, str).

The disadvantages of this tool is the inability to provide a reasonable level of mechanical purity of the solution intended for intravenous administration, the lack of domestic practice of filters-nozzles disposable to ensure mechanical purity solutions and their sterility in clinical conditions, low shelf life of the solution.

The purpose of this invention is the creation of drugs for injection with high bioavailability with no side effect when used with high consumer qualities.

This goal is achieved through the use of a solution of ciprofloxacin for input the th, have antibacterial properties, including sodium chloride and water for injection, and optionally containing-oxopropionate acid and the disodium salt of the Ethylenediamine-N,N,N1N1-tetraoxane acid, in the following ratio, wt.%:

ciprofloxacin hydrochloride0,18-0,22
the disodium salt of the Ethylenediamine-N,N,N1N1-
tetraoxane acid0,018-0,022
α-oxopropionate acid0,055-0,075
sodium chloride0,8-1,0
water for injectionthe rest is up to 100%.

The essential features that characterize the invention, are: selection of excipients, the quantitative composition of ingredients and tools.

The combination of all attributes has allowed to obtain a new result - increase bioavailability.

The claimed solution was obtained by the following method: estimated number of ciprofloxacin, sodium chloride and disodium salt Ethylenediamine-N,N,N1N1-tetraoxane acid (Trilon B) is dissolved at a temperature of 30-35°With sterile water for injection, pre-pranipatena to remove carbon dioxide is s. Add the estimated number-oxopropanoic acid. Control the pH of the solution. The resulting solution is filtered through a membrane plate type Millipor" with a pore diameter of 0.22 μm, poured into ampoules and sterilized by steam method. The sealed ampoules. Solution in sealed transparent, without sediment.

Experimental studies of pharmacological activity developed forms for injection (target compounds listed in table 1) showed that the drug causes no side effects.

As disodium salt Ethylenediamine-N,N,N1N1-tetraoxane acid used Trilon B.

To study the bioavailability of the claimed solution for infusion in comparison with the prototype studies have been conducted of the following indicators: 1) the maximum concentration of drug substance in the blood; 2) the time to reach maximum concentration.

The experiments were conducted on rabbits weighing 3 kg After 0.5, 1, 2, 4, 6 hours after a single parenterale the injection was performed blood sampling and then the obtained sample was analyzed by the method of Propsting-Gavrilova. The data obtained are summarized in table 2.

The data obtained indicate that the claimed solution has a greater bioavailability than the preparation of the prototype. This will correspondingly reduce the build therapeutic dose of the drug, that will contribute to further mitigate the side effects of the drug. At the same time, the use of ciprofloxacin in its therapeutic dose, due to the high bioavailability may increase therapeutic efficacy.

The possibility of carrying out the invention is confirmed by studies on the selection of quantitative parameters ingredients funds, the use of which it is in the claimed proportions makes it possible to achieve the goal.

The concentration of the disodium salt Ethylenediamine-N,N,N1N1-tetraoxane acid in the medium is optimal, because it is in these quantities it acts as an antioxidant, and increasing this number as a Pro-oxidant, which contributes to the destruction of ciprofloxacin. The amount of sodium chloride to bring the solution to the desired pH values (6,5-7,5).-Oxopropionate acid provides stability during storage, is a preservative, and optionally a stabilizer.

Was tested the stability of the solutions proposed medicinal product, which is confirmed by the results of the analyses of the solutions at different periods of storage. The results are summarized in table 3.

The application of the proposed solution for injection with enhanced biological dostupno is d, will reduce the treatment time and retains its properties over 2 years.

Table 1
No.The solution for infusion, %Side effects
Act. prophetic-inTrilon Bα-oxopropionate theSodium chloride
10,180,0180,0550,8Was not observed extrapyramidal disorders
20,20,020,0650,9
30,220,0220,0751,0
Table 2
Solution for infusionThe concentration of ciprofloxacin in blood (μg/ml) through (h).
0,51246
the placeholder12,5±6,811,81±3,910,99±1,47,08±0,745,94±0,78
The claimed composition according to example No. 112,61±3,113,46±4,414,59±3,49,04±0,817,84±0,86
Table 3
Quality scoreThe retention means according to example No. 1
Outcome.12 months.24 months.
Color R-RAColorlessColorlessColorless
pH6,57,56,65
The content of the act. prophetic Islands in solution, %0,210,2of € 0.195

Solution for infusion ciprofloxacin, have antibacterial properties, including sodium chloride and water for the of Nyenzi, characterized in that it further contains α-oxopropionate acid and the disodium salt of the Ethylenediamine-N,N,N1N1-tetraoxane acid in the following ratio, wt.%:

Ciprofloxacin hydrochloride0,18-0,22
the disodium salt of the Ethylenediamine-N,N,N1N1
tetraoxane acid0,018-0,022
α-oxopropionate acid0,8-1,0
Water for injectionRest



 

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