JPS6159420A - Solution for normal temperature sterilization and cleaning of soft contact lens - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION There are significant differences in structure and composition between hard and soft contact lenses.

Furthermore, there are significant differences in the maintenance, storage, and management of contact lenses among various types of contact lenses, such as hard types, semi-hard types, and soft types. Storage and management of hard contact lenses and conventional simple contact lenses are relatively simple and easy, but proper storage and management of new types of soft lenses and hydrophilic lenses has been found to be more complex and time-consuming. are doing.

The main difference between conventional hard contact lenses and more complex soft lenses is that hydrophilic gel materials have significantly more polar or water-attracting centers. It is this property of hydrophilic gel lenses that gives soft lenses their unique physical properties and clinical functionality. This polar gel material
The center or water-attracting center is represented in the hydroxyethyl methacrylate bond as a hydroxy group (-OH) that attracts and retains large amounts of water. What makes hydrophilic soft lenses particularly difficult to sterilize or aseptically process is the expanded matrix of hydrophilic gel lenses.
This is because a large amount of water is retained in ix). Due to their hydrophilic nature, soft contact lenses are susceptible to bacteria.
ia) is susceptible to contamination. Although research has established that it is impossible for bacteria to enter the actual intermolecular pores of hydrophilic lenses unless the lens is defective, bacteria can Shows an affinity for tears.

In particular, tears and fluids absorbed into soft lenses constitute an optimal bacterial culture medium. If defects or scratches occur in the lens during manufacturing or wear, bacteria can find suitable shelter to grow and escape from superficial lens cleaning and sterilization.

Potentially harmful fungi (fungi) can also be dangerous to soft contact lenses. Fungi, like bacteria, can also reproduce in secreted tears or deposits and can directly invade lens materials if enzymatic degradation of the lens materials occurs.

In addition to the above, various other problems may occur if the user fails to handle the soft lens correctly and carefully.

Many potential contaminants and lens deposits can easily be transferred to the surface of soft lenses from unclean hands. These substances include oily deposits from the skin, sweat, skin lotions and creams, mascara, detergents, lipstick stains, and nicotine. According to controlled tests, 43% of women's cosmetics
1 contains bacterial contaminants and 12 contains fungal contaminants. For example, sterilizing lenses by boiling is not easy and can cause permanent damage to the lenses if not done correctly.6 If users use impure water to store and clean lenses, calcium,
Unwanted deposits such as iron, divalent and trivalent insoluble metal salts, and other chemical deposits can collect on the lens surface.

Accordingly, there is a need for effective compositions to alleviate the above-mentioned consequences of incorrect hygiene and lens handling, and to provide optimal conditions for disinfection and storage of soft lenses outside of the period of lens wear. Ta. Additionally, the active ingredients of an effective solution for contact lenses preferably: (1) disinfect clean soft lenses within 4-6 hours and have a D value of 90% for microbial pathogens such as fungi and yeasts and viral pathogens such as herpes simplex; % bactericidal rate; (2) not be easily inactivated by small amounts of proteins, lipids, or other lachrymal fluid and foreign components and adherents; (3) proteins and other ocular substances. and (4) meet the conditions of not reacting with or being absorbed by the material or matrix of the soft lens. For example, several disinfectants meeting the above requirements for rapidly and effectively killing a wide range of microorganisms have been found to be unsuitable for soft lens treatment solutions. This is because these substances are either incompatible with the material of the soft lens or bind to protein deposits on the surface of the lens. Besides that,
Bactericidal agents that can concentrate in the lens material and cause irritation and damage to the wearer's corneal surface are unsuitable for soft lens solutions. Benzalkonium chloride is one such disinfectant, which meets the requirements of effective and rapid killing of microorganisms, but also combines with many types of soft lens materials and reduces the amount of tan, chloride and dirt on lens surfaces. It is not eligible because it is also combined with a kimono.

An example of a low-temperature disinfectant for soft contact lenses uses chlorhexidine. However, chlorhexidine is absorbed into the soft contact lens material and can subsequently leach into the eye, often resulting in severe irritation, irritation, redness, and discoloration of the soft lens. Therefore, it becomes impossible to wear the lens.

Given the above circumstances, there is a need for highly effective cryogenic storage disinfection solutions and methods that can meet the aforementioned requirements for disinfecting and preserving silicone lenses, silicone copolymer lenses, and soft contact lenses overnight or during non-wearing periods. has arisen.

According to the present invention, an aqueous solution for preservation and disinfection containing trimethoprim and benzyl alcohol is provided for preservation and disinfection of silicone lenses, silicone copolymer lenses, and soft contact lenses at room temperature or low temperature. More particularly, the present invention relates to hydrophilic gel lenses, (HEMA
) Provides an effective ambient temperature storage disinfection solution for the disinfection and preservation of silicone and silicone copolymer contact lenses, soft lenses made of gelflex materials. These lenses are made of plastic gel materials such as, for example, hydroxyethyl methacrylate (IMA) or its analogs, ethylene glycol dimethacrylate (EGMA) or its analogs, silicones, silicone copolymers.

The present invention also provides a contact lens treatment method that kills bacteria that may bind to the lens. In the method of the present invention,
A lens is brought into contact with an aqueous composition containing both trimethoprim and benzyl alcohol at a concentration effective for eradicating bacteria. This method is particularly suitable for processing silicone lenses, silicone copolymer lenses and soft contact lenses. No thermal disinfection is required, thus completely eliminating the problems associated with high temperature processing.

The aqueous composition of the present invention co-contains trimethoprim and benzyl alcohol at a concentration effective for eradicating bacteria. Generally, the effective concentration of trimethoprim will be about 0.01-4.0% by weight of the total composition, and the effective amount of indyl alcohol, which acts as a co-bactericide, will be about 0.10% by weight of the total composition.
~5.0% by weight.

The combination of trimethoprim and indyl alcohol provides a cold disinfectant solution that is effective in killing microbial, fungal microorganisms, and viral pathogens such as herpes simplex. Usually, the amount of benzyl alcohol present is about 0.10 to 0.10 of the total composition.
It is about 5.0% by weight. Furthermore, another important function of benzyl alcohol is to make trimethoprim more soluble in aqueous compositions, making it more effective.

A salt of ethylenediaminetetraacetic acid may be included as a anti-inflammatory agent to enhance the bactericidal properties. Other 6-sof agents, such as those described below, may also be used.

The remainder of the composition may consist solely of water or may contain water-soluble salts of various alkali metals and alkaline earth metals, ranging from about 0.8% to about 1.8% by weight of the total composition of the aqueous composition. It is also possible to give an equal degree of salinity to 11 um. The composition may also optionally contain a wetting agent such as propylene glycol.

Silicone lens of the present invention, silicone lens)? I.J.
The aqueous composition for disinfecting mom's and soft contact lenses at room temperature contains trimethoprim and benzyl alcohol. The composition of the present invention acts as a contact lens disinfectant that does not require heat disinfection.

The composition is particularly effective for silicone lenses, silicone copolymer lenses and soft contact lenses, and may also be used for hard lenses. The term "disinfectant" as used herein means a substance that exterminates or kills bacteria, fungi, yeast or viruses.

Trimethoprim and benzyl alcohol are present in the composition in sufficient concentrations to form a soft contact lens disinfecting solution. Generally, about 0.01% to about 4.0% trimethoprim by weight of the total composition and about 0.10% to about 0.10% by weight of the total composition
About 5.0% by weight benzyl alcohol is a sufficient concentration to form a soft contact lens bulking solution. Trimethoprim is also known as 2,4-diamino-5-(3,4,
5-)Softoxypendyl)-pyrimidine or also known as Syraprim. For example, The Merck Index
Index) *10th edition.

Please refer to page 1387. Preferably the amount of trimethoprim present is about 0.125% by weight of the total composition and the amount of benzyl alcohol present is about 2.0% by weight of the total composition.

In order to further enhance the disinfecting properties of the compositions of the present invention, ethylenediaminetetraacetic acid or its equivalent with disinfecting properties is preferably used in an amount effective to increase the germicidal factor of the D value with respect to bacterial, fungal, yeast and/or viral microorganisms. A water soluble salt is present in the composition. A preferred salt of EDTA is the disodium salt (disodium nibtate). Other salts of EDTA that can be used are, for example, mono-, di-, tri- and tetra-alkali metal salts. Generally, an effective amount of EDTA or its salt will be from about 0.025 to about 0.5 of the total composition.
Weight%. Preferably, the amount of disodium nibtate present is about 0.25% by weight of the total composition.

The compositions of the present invention preferably contain about 0% of the total composition of the aqueous composition.
．． Contains one or more approximately neutral water-soluble compatible salts having a tonicity equivalent to 8 to about 1.8 weight percent thorium chloride. That is, preferred compositions of the invention have tonicities approximately equal to or slightly higher than normal human tear fluid. Hypertonic solutions are preferred so that the osmolality of the solution is higher than the osmolarity of the tear fluid of contact lens wearers, but soluble salts or mixtures thereof that are compatible with the ocular tissue may be optionally added to provide the desired osmolality. Can be used. Preferably, sodium chloride, potassium chloride or mixtures thereof are used to provide the desired tonicity.

However, if tonicity adjustment is necessary, all or a portion of the sodium chloride or potassium chloride in the solutions of the invention may be replaced with one or more approximately neutral water-soluble alkali metal salts or alkaline earth metal salts. May be replaced. Preferably, sodium chloride and potassium chloride are used in a weight ratio of about 2:1 to about 7:3.

Preferably the composition contains one or more buffers. Suitable buffers are known in the art and include, for example, sodium bicarbonate buffers. The preferred combination of buffers is present in an amount sufficient to provide and maintain the desired pH.

The composition may optionally contain propylene glycol. The amount of propylene glycol present generally ranges from about 0.2 to about 2.5 weight percent, preferably about 1.0 weight percent of the total composition of the aqueous composition. Propylene glycol acts as a wetting agent, preservative and fungal growth inhibitor.

The remainder of the composition is U', S, P, and pure water.

According to one embodiment of the method of the present invention, a method for sterilizing contact lenses is provided. According to this method, lenses are stored in an aqueous solution containing simultaneously effective bactericidal concentrations of trimethoprim and benzyl alcohol. It is possible to use any of the solutions of the invention. A lens is contacted with an aqueous composition of the invention and this contact is maintained for a sufficient period of time to cause the composition to kill at least a portion of the bacteria bound to the contact lens. For example, a lens typically undergoes a proper cleaning procedure before being introduced into a container containing a sufficient amount of the solution of the invention to completely immerse the lens. The container is then closed and the contact lenses maintained in the solution for a period sufficient to disinfect them. Since no row heat source is applied, the lenses are stored at room temperature. Generally, storing lenses in the solution of the present invention for about 6 hours disinfects and sterilizes contact lenses to the extent that they can be worn. Therefore, it is an ideal method for storing contact lenses overnight or outside of the wearing period. However, it is anticipated that some solutions of the present invention may be stored for less than 6 hours.

According to the method of the invention, no heating of the solution or lens is required. Accordingly, the solutions and methods of the present invention allow lenses to be disinfected at room temperature without the risk of adverse effects due to heating.

The aqueous compositions of the present invention are preferably utilized as part of a wearer's maintenance routine for soft, silicone, and silicone copolymer contact lenses. That is, one or more effective cleaning steps are an important part of an effective maintenance procedure for soft and hard lenses. Because there is a separate lens cleaning step, there is no chance of too much organic or inorganic deposits and contaminants depleting the disinfecting properties of the aqueous compositions of the present invention.

An example of a particularly preferred bath for washing and low-temperature quenching is shown below.

Claims (10)

[Claims] (1) (a) Contacting a contact lens with an aqueous composition in which trimethoprim and benzyl alcohol coexist in water in an effective sterilizing amount; (b) contacting the contact lens with the aqueous composition to ensure sufficient sterilization. A contact lens sterilization method characterized by maintaining the sterilization over a period of time. 2. The method of claim 1, wherein the lens is completely immersed in the composition for about 6 hours. (3) the amount of trimethoprim present is from about 0.01 to about 4.0% by weight of the total composition of the aqueous composition, and the amount of benzyl alcohol present is from about 0.10 to about 5.0% by weight; A method according to claim 1, characterized in: (4) The concentration of the trimethoprim compound is about 0.125% by weight of the total composition of the aqueous composition, and the concentration of benzyl alcohol is about 2.0% by weight. Method described. (5) The method according to claim 1, wherein the aqueous composition further contains ethylenediaminetetraacetic acid or a water-soluble salt thereof. (6) An aqueous composition for normal temperature disinfection of soft contact lenses, which contains both trimethoprim and benzyl alcohol in effective bactericidal amounts and is compatible with soft contact lenses. (7) The amount of trimethoprim in the total composition is about 0.01~
7. The composition of claim 6, wherein the amount of benzyl alcohol is about 4.0% by weight and the amount of benzyl alcohol present is from about 0.1 to about 5.0% by weight of the total composition. (8) The composition according to claim 6, further comprising ethylenediaminetetraacetic acid or a water-soluble salt thereof. (9) The composition according to claim 6, further comprising at least one type of buffer compound. (10) The composition contains about 0.125% by weight of trimethoprim, about 2.0% by weight of benzyl alcohol, and about 0.25% by weight of disodium salt of ethylenediaminetetraacetic acid, and about 0.10% by weight of the composition. of sodium bicarbonate, about 0.03% by weight of sodium phosphate, about 0.03% by weight of sodium dihydrogen phosphate, and about 0.7% by weight of sodium phosphate.
9% by weight sodium chloride, about 0.368% by weight potassium chloride, about 0.05% by weight sodium bisulfite, and about 1.0% by weight propylene glycol. Composition according to paragraph 9.