JP2549285B2 - Nasal spray - Google Patents

Description

TECHNICAL FIELD The present invention relates to a nasal spray containing a quinolonecarboxylic acid antibacterial agent or a salt thereof as a main component.

“Prior Art” Ofloxacin is a useful drug having excellent antibacterial activity against Gram-positive bacteria and Gram-negative bacteria and having a broad antibacterial spectrum. The quinolonecarboxylic acid antibacterial agents are known to be used for oral administration, injections, ophthalmic agents and the like, and are widely used clinically. On the other hand, little research has been done on eradication of bacteria in the nasal cavity, and only an example of fosfomycin has been reported as an existing antibacterial agent.

[Problems to be Solved by the Invention] In order to effectively and sustainably remove bacteria in the nasal cavity, antibacterial activity and suppression of emergence of resistant bacteria are important factors. With the conventional techniques, there is a problem in the appearance of resistant bacteria, etc., and there has been a demand for the development of a nasal drop having strong antibacterial activity and in which resistant bacteria are less likely to appear.

Then, the inventors of the present invention conducted extensive studies on a nasal spray having a strong antibacterial activity against resident bacteria in the nasal cavity and in which resistant bacteria are less likely to appear.

[Constitution of Invention] The present inventors examined the direct nasal eradication effect of ofloxacin.

Since bacteria in the nasal cavity adhere to the fingers just by touching the nose, they are a problem among medical staff and cooks. Staphylococcus aureu as a typical example of bacteria resident in the nasal cavity
However, there are about 30% carriers among hospital workers, and prevention of nosocomial infection is an important issue. Therefore, the present inventors have used ofloxacin to produce Staphyloco
The eradication effect of ccus aureus was examined.

When ofloxacin is used as a nasal spray, it can be sprayed on the nose, or it can be an aerosol in which the liquid is combined with a liquefied gas or a compressed gas. The dose may be appropriately selected depending on the symptoms, age, etc., but usually 0.1 mg to 10 mg of the main drug is administered daily. The concentration of the main drug in the preparation can be usually 0.01% to 1% in the case of a liquid preparation. Further, ofloxacin may be used in the form of a pharmaceutically acceptable salt such as sodium salt.

As the solvent used when the dosage form is liquid, it is possible to use a solvent which is usually used for a liquid drug such as sterile purified water, ethanol, propylene glycol, polyethylene glycol and glycerin. As the liquefied gas of the aerosol agent, fluorohydrocarbons such as Freon 11 and Freon 12 and liquefied petroleum gas such as butane and propane are used, and as the compressed gas of the aerosol agent, nitrogen gas, carbon dioxide gas and the like are used. Further, isotonic agents such as sodium chloride and D-mannitol, buffering agents such as sodium phosphate and borax, pH adjusting agents such as sodium hydroxide and hydrochloric acid, paraoxybenzoic acid esters, benzalkonium chloride, chlorobutanol, etc. Preservatives, polysorbate 80, surfactants such as polyoxyethylene hydrogenated castor oil, stabilizers such as sodium edetate, aromatic agents such as menthol and the like may be added as necessary.

"Effect of the invention" As will be apparent from the examples described below, the target compound of the present invention has an excellent bactericidal effect against indigenous bacteria in the nasal cavity, suppresses the development of resistant bacteria, and is a nasal spray. Was confirmed to be extremely useful.

Examples of sterilization test using ofloxacin and formulation examples of liquid preparations are shown in the following examples, but the present invention is not limited to these examples.

[Examples] 1. Sterilization test (Test method) The nasal scrapes of 33 hospital workers (doctors and nurses) were used as samples, and saline agar egg medium (Nissui) was used as the separation medium. A 0.3% ofloxacin solution was sprayed twice a day to the carrier twice a day for 3 days, and Staphylococcus aureus
The bactericidal effect was investigated. Also, as a resistance test, Staphy
lococcus aureus, Staphylococcus pueumoie and Haem
The drug susceptibility of ophilus infulenza was examined by the Showa 1 concentration method disc.

(Results) Staphylococcus aureus was detected in 11 out of 33 persons, but Staphylo was detected in 9 out of 9 persons subjected to the sterilization test.
The bacteria of coccus aureus disappeared and ofloxacin showed excellent eradication effect.

As a result of the resistance test, all strains were sensitive to ofloxacin.

2. Preparation example After adding ofloxacin, sodium chloride and benzalkonium chloride to sterile purified water, the pH is adjusted to 6.5 by adding hydrochloric acid or sodium hydroxide solution to obtain a nasal propellant having the following formulation.

Ofloxacin 0.3g Sodium chloride 0.9g Benzalkonium chloride 0.0025g Sterile purified water 100ml

Claims (1)

(57) [Claims] 1. A nasal spray containing as a main component of ofloxacin or a salt thereof.