United States Patent (19) 11 Patent Number: 5,385,734 Friedman (45) Date of Patent: Jan
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US005385734A United States Patent (19) 11 Patent Number: 5,385,734 Friedman (45) Date of Patent: Jan. 31, 1995 54 HORSERADISH PREPARATION FOR THE (56. References Cited TREATMENT OF NASAL AND SINUS DYSFUNCTION U.S. PATENT DOCUMENTS 4,782,023 ii/1988 Anawis et al. ...................... 435/188 75 Inventor: William H. Friedman, St. Louis, Mo. 5,114,969 5/1992 Chung et al. ....................... 514/514 OTHER PUBLICATIONS (73) Assignee: Horseradish Spray, Inc., St. Louis, Mo. Fan-Yung et al., "Dispersion Characteristics of Vegeta ble Juices', Izvestiya Vysshikh Uchebnykh Zavedenii, Pishcheyaya Tekhnologiya 1980, No. 2, 138-139, Ab 21) Appl. No.: 68,998 stract only. 22) Filed: May 27, 1993 Primary Examiner-Thurman K. Page Assistant Examiner-Carlos Azpuru Related U.S. Application Data Attorney, Agent, or Firm-Bryan Cave 62) Division of Ser. No. 844,107, Mar. 2, 1992, Pat. No. 57 ABSTRACT 5,248,504. Amethod of treatment for nasal and sinus dysfunction is disclosed comprising topically applying a horseradish, (51) Int. Cl. ..................... A01N 65/00; A61K 35/78; sinigrin or allyl isothiocyanate preparation to affected A61K 9/14 mucosa. Preparations for the treatment of nasal and (52) U.S. Cl. ................................. 424/434; 424/195.1; sinus dysfunction are also disclosed, including prepara 424/489; 514/951 tions of horseradish, sinigrin and allyl isothiocyanate. (58) Field of Search ..................... 424/195.1, 434, 489; 514/951; 426/615 10 Claims, No Drawings 5,385,734 1. 2 No. 98,875, relates to a medical compound for alleviat HORSERADISH PREPARATION FOR THE ing and curing asthma, coughs and colds. The com TREATMENT OF NASAL AND SINUS pound includes pulverized horseradish. Diets, U.S. Pat. DYSFUNCTION No. 74,205, discloses a medical compound containing horseradish for the cure of consumption. These oral CROSS-REFERENCE TO RELATED horseradish remedies include substances, such as apple APPLICATION cider, ground ivy, and red beets, that are not suitable for This application is a division of U.S. application Ser. topical applications. No. 07/844,107, filed Mar. 2, 1992, now U.S. Patent No. Other natural oral remedies are known in the art. 5,248,504, granted Sep. 28, 1993. 10 Reeves, U.S. Pat. No. 28,904, relates to a treatment for inflammatory diseases of the pulmonary organ that FIELD OF THE INVENTION includes the use of capsaicin or African cayenne pepper. This invention relates to a method of treatment for Greene, U.S. Pat. No. 378,504, relates to a catarrh treat nasal and sinus dysfunction comprising topically apply ment which includes red pepper (capsaicin). ing a horseradish, sinigrin or allyl isothiocyanate prepa 15 However, none of the above-cited prior art provides ration to affected mucosa. The invention also relates to a topical therapy or a preparation which is consistently preparations for the treatment of nasal and sinus dys safe and effective in the treatment of most nasal and function, including preparations of horseradish, sinigrin and allyl isothiocyanate. sinus dysfunctions. 20 SUMMARY OF THE INVENTION BACKGROUND OF THE INVENTION This invention provides a formulation for the topical Many people suffer from nasal and sinus dysfunction. treatment of nasal or sinus dysfunction, comprising an Examples of nasal and sinus dysfunction include allergic aqueous dispersion of a therapeutic amount of horserad and vasomotor inflammatory conditions of nasal mu ish particles, sinigrin or allyl isothiocyanate in a dilute cous membranes, sinugenic headaches, post nasal dis 25 charge, and the like. suspension or solution, e.g., in an aqueous saline suspen Nasal sprays have been used in the treatment of such sion or solution. nasal and sinus dysfunctions, but are not without draw Another aspect of the present invention relates to a backs. For instance, common nasal sprays containing method of making a horseradish dispersion useful in the sympatho-mimetic compounds, and over-the-counter 30 treatment of nasal or sinus dysfunction. The method remedies containing phenylephrine hydrochloride, ox comprises (a) reducing the size of the horseradish to ymetazoline hydrochloride, or xylometazoline are gen form horseradish particles of about 100-1000 microns; erally considered to be harmful when used over long (b) dispersing the horseradish particles in a sodium chlo periods of time because they cause damage to nasal ride solution; (c) filtering the dispersion to obtain a mucosal ciliary function, and they cause rebound muco 35 filtrate comprising horseradish particles with a mean sal thickening leading to nasal congestion. The manu particle diameter from 20-90 microns dispersed in the facturers of certain over-the-counter remedies warn sodium chloride solution; and (d) ultrafiltering the fil that their products should not be used for more than trate to obtain a horseradish dispersion comprising three days. Also, the use or abuse of these drugs has horseradish particles having a mean particle diameter resulted in anosmia, prolonged nasal obstruction, and not greater than 20 microns; wherein the horseradish habituation of the medications. dispersion comprises from about 0.01-10.0 weight per Other nasal sprays in the art include saline nasal cent horseradish. sprays and topical steroid sprays. It is thought that the DETALED DESCRIPTION OF THE anti-inflammatory effect of steroid sprays produces a INVENTION beneficial reaction in the nasal and sinus mucosa. How 45 ever, such sprays can produce mucosal atrophy in post The present invention is useful in the treatment of a surgical states, and are generally effective only in reduc wide range of nasal and sinus dysfunctions. Such dys ing inflammation. They generally have inconsequential functions may occur prior or subsequent to surgery of decongestant or physiological mucosal effects in mobi the paranasal sinuses. Nasal and sinus dysfunctions may lizing secretions or stimulating cells to evacuate secre 50 accompany allergic and vasomotor inflammatory con tionS. ditions of the nasal mucous membrane. Certain mucous Another drawback of the prior art preparations is membrane disorders are associated with sinugenic head that a significant segment of the population is reluctant aches, post nasal discharge, and mucous membrane to apply artificial compositions to their nasal mucosa. disorders presumably related to an immotile cilia condi As a result, topical therapy for nasal and sinus dysfunc 55 tion. The latter condition results when the cilia of the tion in this segment of the population is largely nonexis mucous membranes lining the nose (pseudo-stratified tent. ciliated columnar epithelium) appear to perform their Attempts have been made to produce natural reme mucous clearance and secretional mobilization activities dies for certain ailments. For instance, Stammberger has in a sluggish or incomplete fashion. Immotile cilia con administered capsaicin P (trans-8-methyl-N-vanillyl-6- ditions are frequently found in patients with chronic nonenamide), the pungent extract of red pepper, to sinusitis, allergy, asthma, and other systemic conditions patients with headaches. However, the capsaicin has in which the nose and sinuses play a major role. been found to produce only profound vasodilation, Nasal and sinus dysfunctions are sometimes a result of sneezing, and either vasomotor or cholinergic secretory limited mucosal contact within the nose, resulting from episodes. Also, the capsaicin is known to destroy unmy 65 nasal septal deviations, middle turbinate "squeeze' syn elinated C fibers of sensory and vagal afferent neurons. dromes, and other "trigger” type situations that pro Attempts have also been made to provide oral horse duce long-standing headaches, often projecting to re radish remedies for certain ailments. Mays, U.S. Pat. mote dermatromes of the head and neck. 5,385,734 3 4. Other types of nasal and sinus dysfunctions that may be treated according to the present invention include Although the mode of operation of the present inven nasal congestion from allergic, vasomotor, or infectious tion is not fully understood, it is believed that the benefi etiologies, and crusting or atrophic rhinitides associated cial effect of the preparations of the present invention with infection or surgery. may result from stimulating a focal physiological cellu The preparations of the present invention may vary lar response in mucosa. A natural antibiotic effect may widely in composition, however they will typically result when either sinigrin or allyl isothiocyanate, per comprise horseradish, sinigrin, allyl isothiocyanate, or haps in combination with ascorbic acid (vitamin C), is mixtures thereof, in a saline solution. applied to affected mucosa. Vitamin C is present in Topical applications may be performed by a number 10 large concentrations in horseradish. of techniques. A preparation may be sprayed onto the The concentration of horseradish in the dispersion affected mucosa, or the nasal mucosa may be bathed may vary. The concentration should be such that the with drops of the preparation. A preparation may be user's mucosa do not become irritated, and generally is applied by loading the preparation onto a swab and from about 0.01-10.0 weight percent horseradish. A dabbing the swab on affected mucosao A preparation 15 preferred concentration is from about 3.0-10.0 weight may also be applied as a nasal douche. percent, and a more preferred concentration is from The preparations of the present invention preferably about 8.0-10.0 weight percent horseradish. are derived from natural sources, although chemical The mean particle diameter of the horseradish should synthesis of the active ingredients may also be em be small enough so that the user's mucosa do not be ployed. Horseradish (raphanus rusticanus) is the root of 20 come irritated. typically not in excess of 20 microns. A radicula armoracia. It contains ascorbic acid and sini preferred mean particle diameter is from about 2-10 grin. Black mustard (also referred to as brown mustard microns. and red mustard) is derived from dried ripe seeds of The concentration of sinigrin in the sinigrin solution brassica nigra. Its constituents include sinigrin, myosin, may vary.