Ofloxacine composition for injections

FIELD: pharmacology, fluorinated quinolone-based drug, in particular ofloxacine for injections.

SUBSTANCE: claimed composition contains therapeutically acceptable amount of ofloxacine and trilon-B, sodium chloride, water for injections as additives.

EFFECT: high therapeutic effectiveness; non-crystallized active agent for a long-time storage.

1 ex


The invention relates to medicine, namely to the drug from the group of fluorinated quinolones, namely ofloxacin for injection.

Ofloxacin 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinil)-7-oxo-7H-pyrido/1,2,3-de/1,4-benzoxazinones acid has a broad spectrum antibacterial action. Practically insoluble in water and alcohol. Available only in pill form (Medmaravis, Medicines, Vol.2, str-346).

Known dosage form of ofloxacin in the form of tablets (U.S. Pat. U.S. No. 4639458) and in the form of ointments (U.S. Pat. Of the Russian Federation No. 2145497).

So in patent No. 2145497 described for the treatment of purulent-necrotic processes in the form of ointments containing antibiotic (ofloxacin) and local anaesthetic (trimekain or lidocaine) tool, gelling (proxanol is chosen), a protease, a polyethylene oxide-400 and water. The tool is intended for external use only. In this method of obtaining ointment ofloxacin managed to dissolve in water when heated only by the presence of trimekainom.

The prototype of the present invention is a composition containing a therapeutically allowed number of ofloxacin, and auxiliary additives (U.S. Pat. Of the Russian Federation No. 2207115). Known composition in the form of coated tablets. As of excipients contains lactose, starch, hydroxypropylcellulose, the AOC is povidone, magnesium stearate. This structure has all the disadvantages of tablet forms of drugs: insufficient therapeutic availability of low strength tablets.

The objective of the invention is the creation of composition ofloxacin for injection, easy to use, providing a high therapeutic efficacy, no crystallization of the active substance for a long time.

This goal is achieved through the use of a composition containing a therapeutically allowed number of ofloxacin, and auxiliary additives, which are used Trilon-B, sodium chloride, water for injections. The composition obtained as solution for injection. The mass ratio of ingredients, wt.%:

Ofloxacin 1,9-2,1

Trilon-B for 0,19 0,22

Sodium chloride is 8.5-9.5

Water for injection stop up to 100%

During the study it was found that the combination of ofloxacin with Trilon-B and sodium chloride in a certain ratio prevents crystallization of active compounds and increases the solubility of ofloxacin in the water.

As a result of research it was found that the Trilon-B - disodium salt ethylendiaminetetraacetic acid capable of forming complex compounds with fluorine-containing compounds, namely with ooxacin, turning it into vocarstvo imoe state.

The invention is illustrated by the following examples.

Example 1. In capacitive heated apparatus, equipped with a stirrer, a pre-prepared solution of sodium chloride to obtain 0,85-0,95%isotonic add Trilon-B based obtain 0,0190-0,022% solution. Add ofloxacin 1.9 to 2.1 g/l at a temperature of 50-60°C for 60 min To the resulting solution was added a buffer (NaOH solution) pH 6,0-7,3 with the calculated amount of water. Membrane filtration is carried out with the use of the disc holder of the company “Millipor”. The filter holder is placed in a membrane with a pore diameter of 0.2 μm “Vladipor” type FMAC. For sterilizing filtration using a hydrophilic membrane 0.2 μm Sartobran P company “Srtrius”. The bottling is carried out according to GOST 10782-85 dose of 100 ml Capping produce tubes of rubber compound 52-369/1, compressed aluminum caps. After filling sterilized finished product in an autoclave at a temperature of 120°C for 15 minutes

Ofloxacin has a broad antibacterial spectrum of action. Affects mostly gram-negative bacteria. Effective against microorganisms resistant to most antibiotics and sulfonamides. Bactericidal action. Used for infections of the respiratory tract, ear, throat, nose, skin, kidneys. Ofloxacin in view of injection solution is rapidly absorbed from the gastrointestinal tract (bioavailability over 95%). The maximum concentration in the blood is achieved within 30-60 minutes. The half-life of 6-7 hours. There is metabolized. 75-90% is excreted in the urine.

Were conducted clinical trials of the drug for injection Ofloxacin in comparison with drug Tarifaire (act. Conn. ofloxacin) in the form of tablets, coated tablets 200 mg firm Hoechst Marion Roussel Ltd., India, series-020020, release date, 11.00, shelf life of up to 10.03, registration number 008163, the date of registration.

The study was conducted on 10 healthy subjects: 6 men and 4 women aged 18-45 years. Taking drugs was carried out at 9 a.m. at the dose of 200 mg (1 tablet drug comparison or 1 injection in the vein of the claimed preparation). Blood sampling was carried out from the cubital vein in an amount of 5 ml glass test tubes before taking the drug and after 0,5; 1; 1,5; 6; 12 and 24 hours after administration of the drug.

To 1 ml of plasma was added 500 μl of phosphate buffer and 5 ml of chloroform, shake for 15 minutes. Then the samples were centrifuged for 10 minutes at 3000 Rev/min the Organic layer was quantitatively transferred into a clean test tube and add 200 ál of 0.1 M sodium hydroxide solution. The samples were mixed on a "vortex" 1 minute, centrifuged for 5 minutes at 3000 rpm and 100 μl of the aqueous phase was injected into the column of the chromatograph. The analysis was performed on the high performance liquid chromatograph "Shimadzi" flew americasteam detector "Krato8".

The data obtained indicate that after taking as reference product in tablet form, and the test drug in the injectable solution ofloxacin rapidly absorbed into the systemic blood flow, reaching a maximum level to 1.5 hours (2,04 and 2.14 µg/ml, respectively). The average value of the maximum extent of absorption of the drug Tarifaire in relation to the claimed drug is 0,96.

Antibacterial composition containing a therapeutically allowed number of ofloxacin and auxiliary additives, characterized in that the composition is made in the form of an aqueous solution for injection, at the same time as auxiliary additives used Trilon-B, sodium chloride at a ratio of ingredients, wt.%:

Trilon-Bfor 0,19 0,22
Sodium chloride8,5-9,5
Water for injectionRest


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