Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-03-25
1998-07-28
Weddington, Kevin E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514311, 514312, 514314, A61K 3144, A61K 3147
Patent
active
057863636
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/ES96/00155 filed Jul. 26, 1996.
This invention relates to aqueous ciprofloxacine-containing compositions, useful for the manufacture of single-dose pharmaceutical preparations for topical use in the treatment of otitis media with perforation of the ear-drum. The invention also relates to the use of these compositions and to a process for the preparation thereof.
In accordance with The Merck Index 11th Edition, p. 360 (1989), ciprofloxacine is the International Non-proprietary Name (INN) for 1-cyclopropyl-6-fluor-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarbo xylic acid, of developed formula ##STR1## disclosed, together with the process for the preparation thereof, in U.S. Pat. No. 4,670,444. Ciprofloxacine is a broad spectrum antibacterial active principle.
The chapter of the European Pharmacopoeia dealing with ear preparations, provides that where the ear-drum is perforated, the pharmaceutical preparations must be sterile, free from preservatives and supplied in single-dose packages.
European patent 0 219 784 discloses aqueous ciprofloxacine solutions, at a pH ranging from 3.0 to 5.2, with a concentration ranging from 0.015 to 0.5 g of active principle per 100 ml of solution. The solutions disclosed in the above document are for use in infusion or perfusion, i.e. for systemic and not topical administration, in a wide range of antibacterial preparations for combatting various types of disorders, among which otitis is mentioned.
In turn, PCT application WO93/05816 discloses quinolone based aqueous solutions, among them ciprofloxacine, for combatting eye and ear disorders. The main objective of this patent application is to achieve stabilization of the solutions at, or close to, a physiological pH, by combining the quinolones with a sulfonated polystyrene type polymer. The compositions disclosed contain preservatives such as benzalkonium chloride.
The present inventors are unaware of the existence of prior art describing preservative-free single-dose ciprofloxacine pharmaceutical preparations which may be used topically for combatting otitis with perforation of the ear-drum, whereby, in view of the high efficacy and broad spectrum of this antibacterial active principle, there is felt the desirability of developing new compositions containing it, suitable for such application.
The invention seeks to provide aqueous ciprofloxacine compositions suitable for use in the topical treatment of otitis media with perforation of the ear-drum.
This objective is achieved by compositions of the type named at the beginning which are characterized in that they comprise the following essential components, in the amounts given hereinafter in %w/v (g/100 ml): i) 0.12-0.6% of ciprofloxacine hydrochloride monohydrate (equivalent to 0.1-0.5% of free base); ii) 0.5-3.0% of a buffer system capable of ing the pH between 4 and 5; iii) 0.05-0.3% of a non ionic surfactant; iv) 0.5-2.0% of a thickening agent; and v) water ad 100 ml.
According to the invention, these compositions are preferably free from preservative additives.
Further to the essential components mentioned above, the compositions of the invention may include optionally other components of the type usually used in liquid galenic formulations, provided that such components do not exhibit a significant ototoxicity.
The ciprofloxacine hydrochloride monohydrate may easily be obtained on the marketplace or may be prepared by any of the methods disclosed in Spanish patents ES-2006099 and ES-2006098.
The buffer system may be any pharmaceutically acceptable one allowing the pH to be maintained between 4 and 5. Particularly preferred is the acetic acid--sodium acetate system, with the molar proportions adjusted in such a way as to maintain the pH to between 4.5 and 4.9, more preferably between 4.6 and 4.8.
The non ionic surfactant may be a polysorbate, i.e., a fatty acid ester of oxyethylenated sorbitan, for example polysorbate 20 or polysorbate 80 and soya bean lecithin derivatives.
The thickening agents serve to adjust the viscosity of the
REFERENCES:
patent: 4670444 (1987-06-01), Grohe et al.
Canovas Soler Pedro
Delgadillo Duarte Joaquin
Moreno Rueda Juan
Bayvit, S.A.
Weddington Kevin E.
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