DE2854278A1 - Compsn. for removing deposits from contact lenses - contains protease and nonionic wetting agent - Google Patents

Abstract

Cleaning compsn. in the form of powder, tablets or liq. concentrate for removing deposits from contact lenses contains a protease (I) and a nonionic wetting agent (II). (III) is esp. a polyoxyethylene-polyoxypropylene block copolymer used at 0.5-10% and (I) is esp. bromelin and/or chymotrypsin, trypsin or subtilisin at total concn. 0.1-1%. Opt. the compsn. also contains (a) a nontoxic thiol cpd. as enzyme activator; (b) an amylase and (c) salts (e.g. Na or Ca chloride or phosphate, or KCl), and after dissolution in, or dilution with water the cleaning soln. is isotonic with pH 6.5-8.5. Compsns. efficiently remove deposits (consisting mainly of proteins, mucopolysaccharides and lipids from the fluid of the eye) which can interfere with vision and serve as a source of nutrients for bacteria.

Description

SHIP v. FONER STREHL SCHOBtL-HOPF IfBBlNlSHAUS FINCK

Description

In addition to inorganic salts, the conjunctival fluid of the eye contains numerous organic substances. In the latter, proteins (400 to 600 mg / 100 ml conjunctival fluid) and lipids (400 to 700 mg / 100 ml conjunctival fluid) predominate in terms of quantity. While the composition of the lipids is still largely unclear, the protein content could be largely differentiated into 28 % prealbumin, 44 % globulin and 28 % lysozyme. A large part of the globulins consists of glycoproteins, ie of mucopolysaccharides, which are composed of polysaccharides, amino sugars and proteins (P. Frauch, lacrimal secretions and precorneal film in healthy people, Pharm. Acta HeIv. J ^, 1 »1978).

A problem since the introduction of contact lenses is their optimal cleaning. Especially when wearing soft ones for a longer period of time (Hydrophilic) contact lenses form more or less opaque deposits on the lenses, which both obstruct the view as well as serve as a bacterial breeding ground and can thus lead to eye infections. The rainfall consist largely of proteins, mucopolysaccharides and lipids from the conjunctival fluid. In addition pollution caused by the environment (soot, dust) and cosmetics (skin creams, eye shadows, mascara, etc.).

Either chemical or physical methods are used to disinfect the contact lenses. Belongs to the former placing the lenses in solutions of suitable disinfectants (hydrogen peroxide or chlorhexidine and / or thimerosal), the latter includes boiling in water or isotonic salt solutions. By none of the aforementioned

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The above-mentioned precipitate is removed in the process; The precipitate is coagulated by heat when the lentils are boiled Egg white is even more firmly fixed. AS 2 417 844 describes an attempt for the first time that deposits adhering to the contact lenses with the help of proteolytic To remove enzymes such as those used in the detergent and dishwashing agents1 industry worldwide since the 1960s will.

The subject matter of the invention is set out in the preceding claims evident. More precisely, it relates to a cleaning agent for removing deposits from contact lenses, the most important components are the proteases bromeline, Chymotrypsin, trypsin and subtilisin individually or in Mixture and additionally a polyoxyethylene polyoxypropylene block polymer (commercially available under the trademark Pluronic) contains. The cleaning agent is to be marketed in concentrated form as a powder, tablets or liquid and can be dissolved in water or diluted with water by the consumer. The resulting solution is isotonic and has a pH between 6.5 and 8.5. The following additional substances can be used individually or in the concentrate the mixture contains: a non-toxic thiol compound, a non-toxic amylase, suitable salts such as sodium phosphates, Calcium phosphates, sodium chloride, calcium chloride, potassium chloride, suitable water-soluble auxiliaries, such as those used for Manufacture and preservation of powders, tablets and liquids are commonly used, for example Lactose, a mixture of dextrose and maltose, silicone compounds in small amounts, preservatives, in particular Thimerosal, chlorhexidine and complexing agents derived from acetic acid, such as those found under the wart marks Trilon A, Trilon B and Trilon C are in stores.

The working hypothesis that the simultaneous use of proteases and wetting agents results in an improved solution effect

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should give, was confirmed by the experiments described below. It was found that the additional Use of amylase brings about a further improvement in the cleaning effect.

Attempt 1

Since the connective tissue fluid was not available in sufficient quantities, a mixture of proteins, lipids and G coproteins (mucopolysaccharides) had to be produced for model experiments that was as similar as possible to the physiological conditions. The optimal mixture for our purposes consists of two parts egg albumin (practical powder) »1 part mucin from gastric mucosa (Merck index 2.» 81 6), two parts wool wax, 1 part peanut oil and 4 parts water. Of this ^{mixture, which was melted at 60 °} C. and stirred until a homogeneous emulsion was formed, 50 mg each (corresponding to 30 mg of solids) were applied to surface- ground hydrophilic contact lenses (water absorption 38% or 43 %) and then at 90% Tel, humidity and from Leave temperatures rising to 80 ^° C. for 3 days. The properties of the white coating that forms correspond - as we found in comparative tests - to a large extent to the deposits that occur on the lens surface when the contact lenses are worn in the eye.

Attempt 2

Three isotonic solutions, adjusted to pH 7.5 with the help of a phosphate buffer, were prepared, each containing alternatively 1 % bromeline (I), trypsin (II) or suetilisin (alkalase from Novo-Industrie, Copenhagen; III). Solution I also contained 0.5% cysteine hydrochloride and 1 % disodium ethylenediamine tetraacetate as activators.

For comparison, three analog solutions (IP, IIP, IHP)

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produced which additionally each contained 10 % of a polyoxyethylene polyoxypropylene block polymer (Pluronic P 68 from Wyandotte / Brbslöh, Düsseldorf).

10 ml of the solutions, I, II, III and IP, IIP, HIP were each pipetted into 5 beakers with 25 ml content, a hydrophilic contact lens prepared according to the test was inserted into each of the 30 beakers with a coating and for a period of 10 Leave hours in the cleaning solution at room temperature (18 to 20 ⁰ C). The 30 lenses were then washed with 0.9% sodium chloride solution and visually checked for deposits by 5 people in translucent light. The lenses were rated by each person using the following point system:

clear lens, with no debris 0 points ~ clear lens, with <5 dust grain-sized deposits 1 point

clear lens, with> 5 dust grain-sized deposits 2 points

slightly clouded lens 3 points

severely clouded lens 4 points

The following table 1 shows the sum of the points given by the 5 people.

Table 1

Cleaning
solution I. IP II IIP III HIP Score 78 35 19th 4th 27 7th

Experiment 2 showed a clear superiority of the solutions containing wetting agents (IP, IIP, IHP) in comparison

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to solutions with the same composition without wetting agents (I ,. II, III) * - "V

Furthermore, one of the tests is roughly equally strong Cleansing effect of the enzymes trypsin (II) and subtilisin (III.) And a comparatively weaker effect of the enzyme bromeline (I) can be seen.

Attempt 5

The experimental arrangement was identical with that of the test Reihigungslösungen contained but only 0.1% bromelin (IV), 0.1 96 trypsin (V) or 0.1 96 subtilisin (VI) and additionally 0.5% Pluronic F 68 (IVP , VP, VI P). The risks to precipitate lenses remaining in the solution at 30 ⁰ C over a period of 5 days and were in the solution, 3 times daily moved manually by 5 each horizontal rotational movement (180 °). The evaluation is carried out by 5 people according to the scheme described in Experiment 2 (Table 2)

Table 2

Cleaning
solution IV IVP V VP VI VIP Score 73 27 42 14th 26th 11

It can also be seen from experiment 3 that you did the additional Use of a suitable wetting agent further improves the cleaning effect of the protease-containing solutions can be.

Attempt 4

The experimental set-up was identical to that of the experiment. All solutions, however, also contained 0.2 % Od-Amy-

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read. The storage took place for 10 hours at room temperature, the evaluation analogous to experiment 2 with the following results:

Table 3

Cleaning
solution VII VIIP VIII VIIIP IX IXP Score 54 18th 17th 0 21st 3

As in experiments 2 and 3, a significantly better cleaning effect was found with the solutions containing wetting agents. From the comparison of the above results (Table 3) with those of Experiment 2 (Table 1) there is an additional improvement the cleansing effect of the enzyme Λ ^ -amylase evident. This is particularly evident in solutions I and IP, which contain the enzyme bromeline as a protease.

attempt p

In each case 3 hydrophilic contact lenses worn by people for a longer period of time with uniformly strong design when assessed visually whitish precipitates on the surface were in each case 10 ml of the solutions described in experiment 4 introduced, duration 10 hours, room temperature. Assessment of the cleaned lenses analogous to experiment 2. The results can be found in Table 4.

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Table 4

Cleaning
solution VII VIIP VIII VIIIP IX IXP Score 36 9 1 12th 1

The results largely coincide with those of Experiment 4 (Table 3) and the previous experiments. attempt 5 was directly practical; the good cleaning effect especially of the solutions VIIIP and IXP and the consistency the results summarized in Table 4 with the results of the previous model experiments allow analogy conclusions within attempts 1 to 5 to.

Trial 6

The 18 hydrophilic contact lenses cleaned in Experiment 5 were carefully compared with sterile ones according to visual assessment isotonic saline solution and after disinfection in 0.004% sterile and isotonic thiomersal solution of 9 test persons carried. Over an observation period From 3 weeks, neither subjective symptoms of irritation nor objective changes after a specialist check-up were reported noted on the surface of the eye. From this it can be concluded that any after Cleaning cycle remaining on the lens surface Traces of the cleaning agent cannot cause irritation or damage to the eyes.

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Claims (6)

SHIP ν. FÜNER STficHL SCHÜBEL-HOPF EBBINGHAUS FINCK MARIAHILFPLATZ 2 & 3. MÖNCHEN 9O POST ADDRESS: POST BOX 95 O1 6O, D-8OOO MÖNCHEN 95 Dr. Thilo & Co. GmbH KARL LUOWIQ SCHIFF DIPL. CHEM. DR. ALEXANUER V. FÖNER DIPL. ING. PETER STREHL DIPL. CHEM. DR. URSULA SCHÜBEL-HOPF DIPL. INQ. DIETER EBBINGHAUS DR. INQ. DIETER FINCK TELEFON (OS9) 48 QO 54 TELEX 8-23565 AURO D TELEGRAMS AUROMARCPAT MUNICH DEA-18845 December 15, 1978 CLEANING AGENTS FOR BURNING DEPOSITS ON CONTACT LENSES Claims 1. Cleaning agents in the form of powder, tablets or liquid concentrate for removing deposits on contact lenses, characterized in that it contains protease and nonionic wetting agents. 2. Cleaning agent according to claim 1, characterized g e - mark ze rejects that in addition to protease as a non-ionic Genes wetting agent a Polyoxyäthylenpolyoxypropylen-Blockpo « lymerisat is contained in a concentration of 0.5 to 10%. 3. Cleaning agent according to claim 2, characterized that the protease is the SH protease 01-027 / 0194 INSPECTED 285427a Bromelin and / or a serine protease, namely chymotrypsin, trypsin or subtilisin, is contained in a total concentration of 0.1 to 1 % . 4. Cleaning agent according to claim 2 and 3, characterized in that there is also a non-toxic Thiol compound is contained in an amount sufficient for enzyme activation. 5. Cleaning agent according to claim 1 or 4, characterized in that it also contains an amylase. 6. Cleaning agent according to claim 4 or 5, characterized in that the powder or tablet-shaped or liquid concentrate suitable salts such as sodium phosphates, calcium phosphates, sodium chloride, calcium chloride, Contains potassium chloride, which after dissolving the concentrate in water or ^ diluting with water for isotonic Provide conditions and a pH value between 6.5 and 8.5. 030027/0194