Patent Application
20080058421
In accordance with the invention, there is provided a class of chemical agents that can be used to prepare biologically active antimicrobial, sanitizing and/or disinfecting solutions or creams for cleaning nasal and/or sinus passages, as well as disinfecting nasal and/or sinus cavities of inhaled pollens, dust and chemical pollution particles, viruses, molds, fungi, bacteria and other allergic and infectious agents. The preparations can also be used to clean and disinfect other inanimate surfaces.
The biologically active composition may include other compatible ingredients, which do not reduce or interfere with the cleaning and disinfecting properties. The composition may additionally carry an emollient, a coloring agent, antioxidants, natural or synthetic medicinal ingredients, fragrances, vitamins, and moisturizing agents.
The biologically active sanitizing liquid spray/inhaler composition is based on (a) cleaning, surface active properties of anionic or surface active agent or agents, (b) microbicidal properties of either anionic surface active agent under acidic conditions or a mixture of organic acids, (b) the organic/inorganic acids as acidifying agents or their mixture as microbicidal agents (c) water or suitable solubilizing agent such nontoxic alcohols, glycols or a mixture. Additional ingredients can be incorporated to fortify the microbicidal properties these include tuberculocidal and cysticidal activities of esters of fatty acids; and/or (e) fungicidal properties of benzoic acid and its salts or esters.
The anionic surface-active agent is selected from either free acid or salt forms the following classes of compounds:
The anionic agent used in the nasal and sinus cleaning and disinfecting composition is preferably sodium dodecyl sulfate, sodium dioctyl sulfosuccinate, sodium decyl lactylate, sodium dodecylbenzene sulfonate, and sodium alpha-olefin sulfonate and a mixture thereof. The concentration of anionic agent/agents preferably is between 0.0010% w/v to 15.0% w/v. As used herein, a 1% solution would have 1 gram of solute dissolved in a final volume of 100 milliliters of solution. In this disclosure, such units are labeled as weight/volume (w/v) percentage solution.
The acidifying agent is used to lower the pH below 7.0, preferably at or around pH 3.0. The acidifying agent used to lower the pH must be compatible with the anionic surface-active agent. The acidifying agent is one or more of adipic acid, ascorbic acid, citric acid, dehydroacetic acid, erythorbic acid, fumaric acid, glutaric acid, gluconic acid, hyaluronic acid, hydroxyacetic acid, lactic acid, malic acid, succinic acid, tannic acid, tartaric acid, adipic acidpimelic acid, suberic acid. azelaic acid. sebacic acid, carboxylic acid polymers, homo- or hetero-polymerized carboxylic acid such as poly lactic acid or poly lactic- glycolic acid; or mixtures thereof.
The preferred acidifying agent is one or more selected from citric acid, benzoic acid, sorbic acid, adipic acid, or lactic acid or a mixture thereof used at concentrations of 0.01% w/v to 10% w/v.
The solubilizing agents can be selected water and/or non-toxic alcohols and glycols. The preferred solubilizer used is deionized or distilled water to complete 100% w/v of the composition.
The composition optionally contains sodium chloride at 0.5% w/v to 5% w/v. The other optional ingredients could include color and fragrances. The emollient agent used is the powdered extract of aloe vera used at concentrations between 0.05% w/v to 2% w/v.
The cleaning and disinfecting solution optionally contains natural antimicrobial and medicinal herbs and their ingredients, extracts and/or oils and vitamins such A, C, D and E, tea tree oil fatty alcohols, fatty alcohol esters, sphingolipids, thyme, menthol, ginger, turmeric, eugenol, rosemary, eucalyptol, thymol, coriander, fenugreek, tulsi, basil, lemongrass alone or mixture thereof at concentrations of 0.01% w/v to 5.0% w/v.
The cleaning and disinfecting solution optionally contains antiviral agents such as derivatives or analogs of n-aceryl neuraminic acid, Amantadine, Arbidol, Oseltamivir, Peramivir, Rimantadine, Zanamivir, Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Zalcitabine, Zidovudine, Tenofovir, Efavirenz, Delavirdine, Nevirapine, Loviride Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir, Enfuvirtide, Adefovir, Fomivirsen, Imiquimod, Inosine, Interferon, Podophyllotoxin, Ribavirin, Viramidine, alone or mixture thereof at concentrations of 0.0001% w/v to 5.0% w/v.
The cleaning and disinfecting solution optionally contains decongestant such as Ephedrine, Oxymetazoline, Phenylephrine, Pseudoephedrine, Tramazoline, Xylometazoline alone or mixture thereof at concentrations of 0.0001% w/v to 5.0% w/v.
The cleaning and disinfecting composition optionally contains antihistaminic and antiallergic compounds to control allergic conditions.
The cleaning and disinfecting composition optionally contains gums and polymers for slow release of the disinfecting properties. The gums and the polymers are at concentrations from 0.001% w/v to 10.0% w/v.
The cleaning and disinfecting composition for nasal and sinus cavities is be prepared either as solution spray for instillation or as cream for coating nostrils prepared using thickening and solidifying agents.
The examples in Table 1 show the preparation of wipe sanitizers using anionic surface-active agent and an acidifying agent. The compositions are prepared to a final 100% w/v with deionized water.
To ascertain the sanitizing efficacy and microbicidal spectrum against bacteria, three sanitizers were first evaluated by the sanitizer and germicidal detergent test specified by the Association of Analytical Chemists (A.O.A.C.), 1984, using Escherichia coli ATCC 11229 and Staphylococcus aureus ATCC 6538. The bacterial cultures were purchased from the American Type Culture Collection (ATCC), (Bethesda, Md.). Escherichia coli and Staphylococcus aureus are used to represent both gram-negative and gram-positive bacterial classes. This test is used by the US EPA for to determine compliance for a product to be used as a sanitizing agent. A product that reduces population density of both types of bacteria in 30 seconds by 99.999% satisfies the requirement as a sanitizing agent. Fifty ppm hypochlorite meets the criterion of a sanitizer in this test against Escherichia coli and Staphylococcus aureus and was used as a positive control.
The efficacy of the sanitizers in Examples 1, 2 and 3 was further evaluated with 50 of hypochlorite as controls against Salmonella typhimurium, Listeria monocytogenes, Aeromonas hydrophila, and Pseudomonas aeruginosa essentially by the modified detergent and germicidal sanitizer test of the A.O.A.C. (Lopes, 1986) as shown in Table 2. The sanitizers were tested against both natural isolates and the antibiotic resistant strains of Listeria monocytogenes and Salmonella typhimurium. Each of the antibiotic resistant strains was used separately as well as in a composite strain prepared by mixing equal numbers of five different antibiotic resistant strains of Listeria monocytogenes or those of Salmonella typhimurium, respectively.
Staph.
aureus
E. coli
To be more useful in environment where mycobacteria might be present, the nasal and sinus cleaning and disinfecting composition can also be prepared with tuberculocidal activity. Decyl lactylate was incorporated in the sanitizing and microbicidal wipe composition to impart tuberculocidal activity. An aqueous solution of 300 ppm of decyl lactylate and 8800 ppm of lactic acid (pH ≦3.0) exhibited higher tuberculocidal activity than 100 ppm of hypochlorite when examined essentially by the AOAC germicidal and detergent sanitizer test (Table 2). The tests were carried out in 500 ppm of hard water prepared according to the AOAC procedure (AOAC, 1990). The neutralizing solution used consisted of lecithin with polysorbate 80 prepared in phosphate buffer pH 7.2. In case of hypochlorite 0.1 ml of 10% thiosulfate was added to each tube of the neutralizer solution.
The culture was prepared according to the AOAC procedure for testing tuberculocidal activity of disinfectants (AOAC, 1990). Mycobacterium tuberculosis H37 Ra was maintained on Middlebrook 7H9 agar consisting of 4.7 g Middlebrook 7H9 broth (Difco), 2 ml of glycerol (Sigma) and 15 g Bacto-Agar in 900 ml of deionized water and 100 ml of Middlebrook ADC enrichment (Difco). The same medium was used for surface plating during the test. To provide aerobic conditions for Mycobacterium tuberculosis surface plating was used on pre-poured plates. Pre-poured plates were dried by storing at room temperature for one week prior to use. The culture from a 20-day-old slant was inoculated into modified Proskauer-Beck broth and incubated undisturbed at 37° C. for 25 days. The culture from a single tube was homogenized to a smooth suspension free of visible clumps with 1 ml of 0.1% Tween 80 in 0.9% NaCl. The culture was diluted to give 20% transmission at 650 nm and used in the test.
A germicidal and detergent sanitizer test (AOAC, 1990) was essentially employed for evaluating tuberculocidal of decyl lactylate. Ninety-nine ml of the test sanitizer solution contained 300 ppm of decyl lactylate and 8800 ppm of lactic acid. The test was carried out by rapidly mixing 1 ml of the test suspension into 99 ml of the sanitizer solution. After contact period of 30 seconds, 60 seconds, and 5 minutes, one ml of the test mixture was removed and added to 9 ml of the neutralizer. Clorox at 100 ppm was used as positive control. One ml of the neutralized test mixture was plated on Middlebrook 7H9 agar. The culture was diluted ten fold with 0.02% Tween 80 and plated to estimate the number of bacteria used in the test. The plates were replaced in the original plastic plate bags, which were sealed with adhesive tape to prevent drying and incubated at 37° 2 C. for three weeks. The colonies were counted and reduction in colony count compared to controls was used to calculate efficacy of the sanitizers.
The examples show microbicidal efficacy of sanitizing wipe compositions against gram positive, gram negative as well as tuberculosis bacteria. The tests show that the sanitizing composition has a broad-spectrum lethal activity against microorganisms. Thus the lethal activity of the nasal and sinus cleaning and disinfecting composition can be used to disinfect mucosal surfaces contaminated with bacteria, fungi, protozoa and viruses.
The examples presented above are merely illustrative and should not be read as limiting the scope of the invention as it is defined in the appended claims.
While embodiments of the invention have been illustrated and described, it is not intended that these embodiments illustrate and describe all possible forms of the invention. Rather, the words used in the specification are words of description rather than limitation, and it is understood that various changes may be made without departing from the spirit and scope of the invention.
This application claims the benefit of U.S. provisional application Ser. No. 60/841,962 filed on Sep. 5, 2006.
| Number | Date | Country | |
|---|---|---|---|
| 60841962 | Sep 2006 | US |
