EYE-DROP

Abstract: The invention relates to an eye-drop, characterized by, that it contains, 0,02 - 0,1 mass % of primycin, 15,0 - 25,0 mass % of pyrrolidon-2, 12,0 - 25,0 mass % of polyoxyethylene-660-hydroxystearate, 1,0 - 5,0 mass % of polyvinyl-pyrrolidon and distilled water to complete to 100 mass percent.

Description: EYE-DROP The invention relates to a stable aqueous solution con¬ taining as active ingredient primyciπ and to a process for 5 the preparation thereof. Subjects of the present invention are further therapeu¬ tical compositions prepared from the stable aqueous solu¬ tion. 10 Pri ycin is a macrolide antibiotic agent, which is charac¬ terized in the literature (J. Chem. Soc. Perkiπ I. 1974, p. 816) by a single formula: /5-C18-( o -D-arabiπofuranosyloxy)-2-butyl- ,7,11,1 ,19,21, 15 23,25,27-noπahydroxy-4,16,32,34-tetramethyl-l-oxo-oxacyclo- hexatriakonta-16,32-diene-35-yl-)/4-hydroxyhexyl/guaπidium- -sulphate. Although the above literature describes its structure by a single formula, it is known, that it is an antibiotic-mixture 20 consisting of several components (Hungarian Applications No. 2125/84 and 2869/84). Primyciπ is a natural antibiotic agent originating from the fungal strain culture Thermopolyspora galerieπsis, its 25 preparation via fermentation is described in the Hungarian Patent Specification No. 153.593. Primycin is an antibiotic agent of a large spectrum, and it is firstly effective against gram positive bacteria and against polyresistent humaπpathogeπic strains too. 30 Primyciπ can be effectively applied for the treatment of epithelium lesions, in the urology, surgery, gyπecology, dermatology, in the case of household lesions and for the treatment of burns respectively. 35 In the course of its application neither resistance nor, allergic reactions were experienced. SUBSTITUTE SHEET There are known further combinations of primyciπ with other antibiotics (Hungarian Patent Specification No. 158.241). Although primycin is a very effective antibiotic, its therapeutical utilization was made extraordinarily difficult since it is practically insoluble in water. Thus, several efforts had earlier been made to eliminate these difficulties and to prepare pharmaceutical compositi- ons containing primyciπ in a therapeutically well utilizable form while maintaining its efficiency as a whole. The Hungarian Patent Specification No. 173.708 publishes heterocolloidal therapeutical compositions containing primyciπ. Their disadvantage is the low primycin content (0.2-1.0 %). Further the ethyl alcohol used for the preparation of the heterocolloidal solution has in some cases skin irritating effect and in the case the alcohol is vaporized from the treated surface one part of the primycin is running down from the skin without exerting a biological effect. This formulation cannot be used to prepare eye-drops. The Hungarian Patent Specification No. 194.493 describes a basic gel containing primyciπ and N-methyl-pyrrolidoπ from which therapeutical compositions and different gels were prepared. This composition having a gel consistency is useful to incorporate the active ingredient practically in all qalenic forms such as ointments, creams, foams and the like, however it is not useful to prepare eye-drops. The aim of our invention was to prepare a stable aqueous solution containing primycin as active ingredient, which is free from alcohol and does not contain eye-irritating subs¬ tances and this way it is suitable for the preparation of eye-drops. SUBSTITUTE SHEET According to the facts set forth ab ove the invention relates to eye-drops characterized by, that they contain 0,02 - 0,1 mass % of primycin, 15,0 - 25,0 mass \ of pyrrolidon, 12,0 - 25,0 mass % of polyoxyethyleπe-660-hydroxystearate, 1,0 - 5,0 mass % of polyvinyl-pyrrolidon and distilled water needed to complete to 100 mass %. The eye-drops according to the invention are prepared in a way, that primyciπ is dissolved by heating in pyrrolidoπ-2 (Soluphor P) and to the warm solution the polyoxyethylene- -660-hydroxystearate (Solutol HS 15) and polyvinyl-pyrrolidon are added. The distilled water is added to the system while stirring quickly and the solution is cooled to room-tempera- ture while stirring. The eye-drops according to our invention cause no eye- irritation by a 14 days treatment as it has been proved by animal experiments carried out on New Zealand rabbits. The eye-drops according to the invention may contain beside the primyciπ known antimicrobic active ingredients as norfloxacin, pefloxaciπ, cyprofloxacin, ofloxaciπ too. The compositions according to the invention are illustrated by the following πoπ limiting Example. SUBSTITUTESHEET EXAMPLE An eye-drop with the following composition is prepared Primyciπ 0,05 mass % Soluphor P 20,0 mass % Soluptol HS 15,0 mass % Polyvinyl-pyrrolidon 3,0 mass % Distilled water ad. 100,0 mass % SUBSTITUTESHEET

Claims: What we claim is: 1. Eye-drop, characterized by, that it contains 0,02 - 0,1 mass % of primyciπ 15,0 - 25,0 mass % of pyrrolidon-2 12,0 - 25,0 mass % of polyoxyethyleπe-660-hydroxy- stearate 1,0 - 5,0 mass % of polyvinyl-pyrrolidon and distilled water to complete to 100 mass percents. 2. Eye-drop according to claim 1, characterized by, that it contains 0,05 mass % of primyciπ 20,0 mass % of pyrrolidon-2 15,0 mass \ of polyoxyethyleπe-660-hydroxystearate 3,0 mass % of polyvinyl-pyrrolidon and distilled water to complete to 100 mass percents. SUBSTITUTE SHEET

Inventors: Z SZABO ANNA, Z.SZABO, ANNA
Applicants: CHINOIN GYOGYSZER ES VEGYESZET, CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT.
Application year: 1991
Main classification: A61K47
IPC codes: A61K9