US 2600700 A
Description (OCR text may contain errors)
Patented June 17, 1952 COMPOSITION FOR ALLEVIATION OF THE TOBACCO HABIT Colburn J. Smith, Lemoore, Calif.
No Drawing. Application March 8, 1949, Serial No. 80,318
1 Claim. 1
The present invention relates to pharmaceutical compositions and more particularly to a palliative preparation and method of alleviating habits involving the use of tobacco.
Individuals using tobacco frequently desire to terminate its use for health, social, or economic reasons. It is well known that the smoking, chewing, or snufiing of tobacco for protracted periods makes the termination of its use difficult and in some instances almost impossible. The sedative effect on the nervous system approaches a requirement when relied upon for any considerable length of time.
Many preparations have been devised to combat tobacco habits. These prior efforts have generally been directed to the concurrent use of tobacco and an emetic or other substance causing nausea or ill feeling to the end of building up a psychological response to tobacco that makes the same undesirable through its continued association with an undesirable. Not only have such preparations proved unpopular because of the lack of desire on the part of the individual deliberately to make himself ill to cure the habit but has proved ineffective in many instances even when faithfully employed.
An object of the present invention is, therefore, to provide a new and improved preparation directed to the alleviation and/or termination of tobacco habits in all of their forms.
Another object is to provide. a pharmaceutical preparation which combats the tobacco habit without imparting nausea or other ill effects to the user and which is of itself a source of healthful food values when taken internally.
Another object is to provide a composition of the type described which is available in liquid or solid form at the convenience of the user.
Another object is to provide a composition of the character described which is substantially tasteless and may be taken internally by application to tobacco being smoked, chewed, or snuffed without any objectionable flavor to the user and even without the user being conscious of the employment of the composition.
' come apparent in the subsequent description in Another object is to provide a composition'consulf ate.
The composition includes a plurality of ingredients mixed in proportions obtaining a fluid mixture that is pleasant to the taste, that contains health promoting vitamins, and which diminishes or obviates the desire to use tobacco. The liquid preparation in preferred form contains a plurality of vitamins, glucose for sweetening, aromatics or other flavoring, and lobelinesulfate. As will subsequently be described, the vitamins have an important effect in addition to their health-giving properties and with the lobeline sulfate comprise the active ingredients of the composition of the present invention. As an example, each fluid ounce of a successful embodiment of the present invention contains the following ingredients in the amounts indicated:
Thiamine hydrochloride (vit. B1) 7.5 mg. Riboflavin (vit. B2) 7.5 mg. Nicotinamide 18.75 mg. Pyridoxine hydrochloride (vit. Bs) 18.75 mg. Lobeline sulfate 4.2 mg. Glucose 10.5 mg. Aromatics Sufficient quantity for flavoring The ingredients listed are readily dissolved in water in the quantities set forth and remain in solution in the water indefinitely under normal room temperatures. The quantity and type of aromatics or flavoring employed and the amount of glucose, can, of course be varied to suit individual taste preferences. For example, small quantities of peppermint with the glucose can readily hide the bitter taste of the lobeline In the preparation of commercial forms of the subject invention the materials listed above are dissolved in a quantity of water sufficient to form one fluid ounce. The vitamins employed are preferably first dissolved in the water and the lobeline sulfate subsequently dissolved in the aqueous vitamin solution. The lucose and aromatics are added at am time desired. Only a simple mixing operation is required to dissolve the ingredients in the quantities suggested in water.
It is well known that the habit-forming and health-deterring factor in tobacco is the nicotine CHl4N2. The precise chemical or physiological effect of nicotine is not known. Its general effect is that of a strong sedative. The lobeline sulfate (C22H2702N)2.H2SO4 of the above composition is employed as a counterirritant. When taken into the mouth and throat it acts upon taste buds normallysubject to tobacco influence and imparts a substitute sensation thereto leaving the taste buds non-responsivetothe alkaloidal nicotine taken into the system by smoking, chewing, or snuflmg. Theseffe'ct of: the lobeline sulfate is apparently restricted=toportions given above are recommended for averagev use. With the taste budspreconditionedso as to be non responsive'to nicotine, the desire to use tobacco is minimized and its use is entirely unsatisfactory because of the lack of flavor expected. This effect lasts for several hours after the use. of lobeline sulfate.
The thiamine hydrochloride (vitamin B1); riboflavin (vitamin. B nicotinamide; and.p ridoxine hydrochloride sources of highly desirable vitamins of-healthful significance and when dissolvedingwater the aqueous solutions thereof constitute useful solvents for lobeline sulfate, glucose, and aromatics but the utility of the vitamins in the subject compositions is of greater significance:
The reaction of an alkali and; thiamine-hy drochloride is well known. If; for example, sodium, hydroxide is added tothiamine h-ydrochloride, the sodium hydroxideliberates the hydrochloride resulting in'a neutral monochloride. Further addition of the sodium hydroxide begins to liberate the strong quaternary base which goes over rapidly into the neutral pseudobase or carbinol. In alkaline. solution, quaternary thiazoles such as this undergo ring-opening forming an acidic sulfhydryl group which. is then neutralized by the alkali forming a-sodium compound. It is known that the objectionable material in tobacco is alkaloidal nicotine. The thiamine hydrochloride in the composition of the present invention reacts with the alkaloidal nicotine in a similar manner. It is believed that the alkaloidal nicotine neutralizes the thiamine hydrochloride forming a thiaminemonochloride. Further, the alkaloidal nicotine is believed. to
produce hydroxyl ionsso that the. reaction with the thiamine hydrochloride may go through the quaternary base to the. neutral pseudo-base or. carbinol.
The alkaline hydrolysis of riboflavin is known to yield urea. of the alkaloidal nicotine results in urea; on con.- tact with riboflavin withinthe human. system. Thus riboflavin like thiamine;hydrochloride-has a destructive effect upon thealkaloidal nicotine.
(vitamin B6) provide It is believed-that'the alkalinity.
Alkaloidal nicotine has a similar reaction on pyridoxin hydrochloride as upon thiamine hydrochloride effecting a neutralization of the pyridoxin hydrochloride and a release of the pyridoxin. Pyridoxin is known to oxidize nicotine in the body but is perhaps less effective in this regard than riboflavin which decomposes nicotine by oxidation, very rapidly. Strong oxidizing agents oxidize nicotine to nicotinic acid. Weak oxidizing agents oxidize nicotine to form nicotyrine.
The effects of the vitamins in the composition of .the present invention upon alkaloidal nicotine residually present in the system or because of concurrent use of tobacco may be briefly summarized as. follows:
1. Alkaloidal nicotine is changed to nicotine hydrochloride by the thiamine hydrochloride.
2. Alkaloidal nicotine: is changed to nicotine hydrochloride by pyridoxin hydrochloride.
3; Alkaloidal nicotine is oxidized by riboflavin to eitheror both nicotyrine or nicotinic acid.
4. Alkaloidal nicotine is oxidized by pyridoxin to. either or both nicotyrine or nicotinic acid.
The effects of alkaloidal nicotine on the vitamins may be summarizedas follows:
1. Thiamine hydrochloride is changed to neutral; thiamine monochloride and perhaps .by further alkalization due to the. alkaloidal nicotine to carbinol.
2. Pyridoxin hydrochloride is changed to pyridoxin.
3. Riboflavin is believed to form, urea by the action of alkaloidal nicotine.
The resultant forms. of the nicotineafter the action ofthe vitamins thereon are neither harm.- fulgto. the human system in the. quantities formed nor, do they have the sedative effect of the alkaloidal nicotine. Further, the materialsformed of the vitamins are neither harmful'nor present in large amounts after the interactionwiththe alkaloidal nicotine. Obviously it is desirable to employ the vitamins in excess so thatthe alkaloidal nicotine will be combinedwith the vita: mins to the point. ofexhaustion thereof. Any excessof thevitamins is of.course of beneficial effect on thehuman system.
Thecomposition .of the present invention has.
a pH value of approximately 4.4. Ithas been found that approximately grams of the liquid composition are sufficient toneutralize .248 gram ,ofalkaloidal nicotine to aneutral point of p I-I.'7 .0.. Inasmuch as .the actual quantities of alkaloidal nicotine in the system are-quite. small it is apparent that relatively small quantities of they composition are. adequate. for. the purpose.
It hasbeen found in actual use,-for.example,-that,
position on the tobaccobeing employed sothat.
it is passed into the mouth; The lobeline sulfate immediately acts upon the taste buds as set forth aboveand they areso conditionedthat-the influence of nicotine thereon is not noticed and thus the patient does not achieve the taste experience he expects and desires. 'I'he-smoking-or chewingof .tobaccoto. which a few drops ofthe composition have beenapplied thus is an acceptthe composition of the present invention accords with the results achieved, it is to be understood that the present invention is not to be limited to such explanation. In actual case tests covering many months of experience, patients having used large quantities of tobacco for years have been cured of the tobacco habit almost immediately. The initial administration of the composition terminates the taste for tobacco for a period of several hours and each subsequent administration of the composition tends to continue this effect. The action of the vitamins removes the alkaloidal nicotine from the system and preeludes the accumulation of additional quantities thereof thus removing a source of sedative effect tending to make the patient nervous between periods of smoking.
As set forth, the composition is conveniently available in liquid form and may be taken independently or, if the patient desires, concurrently with the use of tobacco. The liquid is readily incorporated in tablet or lozenge form as is well known in medicaments.
Although the present invention has been described in a practical and possibly preferred form, it is to be understood that departures may be made therefrom within the scope of the-present invention which is not to be limited to the details disclosed herein, but is to be accorded the full scope of the claim so as to embrace any and all equivalent compositions and methods.
Having described my invention, what I claim as new and desire to secure by Letters Patent is:
A tobacco habit treating composition comprising a liquid mixture including substantially about 4.2 milligrams of lobeline sulfate, 7.5 milligrams of thiamine hydrochloride, 7.5 milligrams of riboflavin, 18.75 milligrams of nicotinamide, 18.75 milligrams of pyridoxine hydrochloride, and a quantity of water sufficient to form one fluid ounce.
COLBURN J. SMITH.
REFERENCES CITED The following references are of record in the file of this patent:
UNITED STATES PATENTS Number Name Date 154,635 Behrend Sept. 1, 1874 1,842,266 Hicks Jan. 19, 1932 2,198,188 Viscardi Apr. 23, 1940 2,407,624 Bird Sept. 17, 1946 OTHER REFERENCES Rosenberg: Chemistry and Physiology of Vitamins (1942), pages 219, 522.
Wright: Journal of the American Medical Association, volume 109, August 28, 1937, pages 649 to 654.
U. S. Dispensatory, 23rd edition (1943), pages 652, 653.
Gutman: Modern Drug Encyclopedia, 3rd edition (1946), page 83.