US3856942A

US3856942A - Appetite control composition

Info

Publication number: US3856942A
Application number: US00359056A
Authority: US
Inventors: P Murphy
Original assignee: Individual
Current assignee: Individual
Priority date: 1973-05-10
Filing date: 1973-05-10
Publication date: 1974-12-24
Anticipated expiration: 1991-12-24

Abstract

An appetite control composition is provided, comprised of a flavor or taste modifier and safe mild stimulant such as caffeine, a local anesthetic such as benzocaine or benzyl alcohol, and a carbohydrate base such as sucrose or glucose or a combination thereof. A process for reducing weight is also provided, which includes the periodic administration of this appetite control composition.

Description

nited States Patent [191 urphy Dec. 24, 1974 APPE'llllTE CONTROL COMPOSITION [76] Inventor: Paul L. Murphy, 831 Massachusetts Ave., Cambridge, Mass. 02139 [22] Filed: May 10, 1973 [21] Appl. No.: 359,056

[52] US. Cl. 424/180 [51] Int. Cl. A01n 9/00, AOln 9/28 [58] Field of Search 424/180 [56] References Cited UNITED STATES PATENTS 2,714,083 7/1955 Ferguson, Jr. 167/55 2,935,447 5/1960 Miller et al. 424/180 Primary Examiner-Elbert L. Roberts [5 7] ABSTRACT An appetite control composition is provided, comprised of a flavor or taste modifier and safe mild stimulant such as caffeine, a local anesthetic such as benzocaine or benzyl alcohol, and a carbohydrate base such as sucrose or glucose or a combination thereof. A process for reducing weight is also provided, which includes the periodic administration of this appetite control composition.

28 Claims, N0 Drawings APPETITE CONTROL COMPOSITION Large numbers of people are obese simply because they eat too much. Their overweight is not necessarily the result of eating large meals. It may arise from skipping meals, such as breakfast, but constantly snacking, nibbling or cheating" between meals, or when tired, depressed or bored. Many people will consume large quantities of food and beverages while watching television, or participating in some other passive activity. Their overeating is not necessarily a result of their feeling hungry, but rather a result of their wanting to have something in their mouth. While there are some people who are overweight because of glandular imbalance, endocrine conditions, disease, or other metabolic disorders, it appears that a major proportion of overweight people are overweight because of overeating.

Overweight people who fall in this category are particularly difficult to treat so that they will actually lose weight. A variety of treatments have been proposed, based on restricted diets, plus something added to be sure the patient keeps to the prescribed diet. This something is usually either willpower, or a drug, neither of which is fully satisfactory.

People on a willpower regime may lose weight while on the regime, but as soon as the regime is ended they quickly regain weight, mostly because their longestablished habits of eating and drinking are so in grained that they lack the sustained willpower needed to accept radical changes in these habits except for brief periods of time, such as while they are on the regime. Moreover, in many cases people on a willpower regime are subjected to a crash diet, which may be too restrictive, and whose prolonged use could result in nutritional deficiencies, resulting in a quick return to normal habits when the diet is ended.

The drug type of regime relies upon the administration of some drug to reduce the appetite, and thus reduce the caloric intake. Amphetamines are widely used for this purpose. However, many people cannot continue to use amphetamines for the time required to lose significant amounts of weight, because of severe side reactions. Moreover, it frequently happens that even upon protracted treatment with this drug, weight losses are not maintained. Side reactions are also reported for other appetite suppressant drugs. The leading proprietary appetite suppressant is essentially caramel candy sold under the trademark AYDS.

Mayer OVERWEIGHT: Causes, Cost, and Control, Prentice-Hall, Inc. (1968), page 18, has pointed out that lowering blood glucose levels through injections of insulin leads to gastric contractions and hunger. He postulated that there are in the hypothalmus receptors with a special affinity for glucose, which are activated by this blood component in the measure that they utilize it. Mayer with Van ltallie have verified this theory by demonstrating in man a correlation between utilization of glucose by the body and the state of hunger or satiety. Gastric hunger contractions appear when glucose utilization is low. When the satiety centers are destroyed, glucagon no longer inhibits the stomach contractions of a hungry animal, from which Mayer and Van ltallie concluded that the satiety center did control gastric motility.

In accordance with the invention, an appetite control composition is provided, based on a carbohydrate such as sucrose and/or glucose to obtain the effect of carbohydrate on hunger, as noted by Mayer and Van ltallie, in combination with a nontoxic local anesthetic such as an ester of p-aminobenzoic acid, an alkaloid stimulant such as caffeine, and nutrients if desired to control the appetite and supplement nutrient intake. These ingredients, which are the essential ingredients, can be combined in any suitable form for oral administration, so that the composition is readily ingested by a person desiring to control his or her weight. Because of the carbohydrate content, a candy or sweet is a practical form of composition, but the composition can be in any solid or liquid form, as desired. Additional ingredients can be added, including coloring agents and flavoring agents, to render the composition more palatable, and more attractive to the eye.

The composition is normally prepared in dosage unit form, in which the proportions of the essential ingredients are selected for the desired effect. These dosage unit forms can be within the range from about 1 to about 12 g. in weight, per unit.

Any carbohydrate can be used. Good results have been obtained with sucrose, glucose (dextrose), maltose, fructose. These are conveniently used in naturallyoccurring forms such as corn syrup, cane sugar, and beet sugar. A mixture of sugars such as glucose and sucrose may be advantageously used because the mixture produces an ideal plastic mass.

The purpose of the carbohydrate is to elevate blood sugar level to a high level, preferably a high-normal level, and consequently the amount of carbohydrate per unit dose is sufficient to maintain blood sugar at this level. The amount is within the range from about 1000 to about 12,000 parts by weight, preferably from about 2000 to about 3000 parts by weight. For a normal size dosage unit, these parts are taken in milligrams.

A local anesthetic when placed on the tongue reduces sensation safely and effectively but temporarily on the epithelial end organs in the papillae on the surface of the tongue, the socalled taste buds. Consequently, the effect in the appetite control composition is to reduce the craving of the consumer for food and beverages.

The amount of local anesthetic is within the range from about 3 to about 20 parts by weight. For a normal size dosage unit, these parts are taken in milligrams.

To obtain an immediate effect to 30 minutes, each dosage unit form of the composition of the invention should contain an amount within the range from about 3 to about 10 mg of anesthetic. An amount less than 3 mg may be ineffective in one dosage unit, requiring two or more dosage units for the desired effect. An amount in excess of 10 mg may be undesirable if the consumer ingests a large number of dosage units per day, but of course if the number of dosage units ingested is reduced, even this amount can be used. The maximum imposed for optimum effect is approximately 5 mg per dosage unit, and when this amount is used, the average number of dosage units per day is from 10 to 20.

The topical anesthetic can be any local anesthetic which is sparingly soluble in water and therefore too slowly absorbed to be toxic. The lower alkyl esters of para-amino benzoic acid that lack a secondary or tertiary amino group are one class, of which benzocaine (ethyl aminobenzoate), butyl aminobenzoate, butacaine sulfate, and orthoform are exemplary. Also useful are aromatic alcohols such as benzyl alcohol and saligenin, certain alkyl halides such as chloroform, and quinine.

Lower alkyl esters of aminobenzoic acid hydrolyze in the stomach to yield aminobenzoic acid and the corresponding alkyl alcohol, which are both water-soluble, and are excreted by the kidneys, specifically as glycine, to form aminohippuric acid, and both the alcohol and aminohippuric acid are excreted in the urine. This mechanism is a specific detoxifying reaction for these esters.

The alkaloid stimulant is caffeine or a caffeinerelated alkaloid, such as theobromine. Caffeine is added to modify the flavor of the composition. It also tends to reduce the sweet taste of the composition. At the same time, it also imparts the well-known stimulating effect, relieving fatigue, and thereby helping to suppress the desire of the consumer to eat, since fatigue frequently stimulates hunger and eating.

The amount of caffeine is within the range from about to about 80 parts by weight, preferably from about 30 to about 40 parts by weight. For a normal size dosage unit, these parts are taken in milligrams.

In order to obtain the effect of caffeine on palatability, at least about 25 mg per dosage unit should be used. The maximum unit amount is imposed according to the number of dosage units ingested daily. At a lower level per dosage unit the product may be taken somewhat more freely than if at a higher level.

It is known that caffeine forms a stabilizing complex with esters of aminobenzoic acid (Higuchi and Lachman, J. Am. Pharm. Assoc. XLIV 52l-6 [1955]) which is resistant to hydrolysis by water. This effect can be advantageous in the compositions of the invention, and therefore such combinations are preferred.

In order to supplement a restricted daily caloric intake, nutrients such as vitamins can be added to the composition, but these are not essential, and can be omitted. The vitamins can include any one or several vitamins, according to the diet that is prescribed. Vitamins A, B complex, C, D and E can be added, and the amounts are selected to provide a useful vitamin supplementation to the diet. The vitamin content may accordingly vary widely, within recognized limits, and is in no way critical. Thus, the amount of vitamins can vary from a fraction of USRDA to several times the USRDA, preferably from about 25% to about 100% of USRDA. USRDA is the United States Recommended Dietary Allowance as established by the Food and Drug Administration.

The physical form of the composition can be either a liquid or a solid, as desired. For maximum effect on appetite control per dosage unit, however, the dosage unit should be long-lasting in the mouth. Thus, the consumer can slowly dissolve a single dosage unit for quite some time, if it dissolves very slowly in the mouth, and this automatically reduces the number of dosage units taken per day. For this reason, the composition preferably is in a slowly-dissolving form such as hard candy, or compressed tablets.

lf slow dissolution is not desired, the composition can take a number of forms, such as gum drops, soft candy of other types, such as chocolate bars and drops, or cotton candy, liquid solutions such as beverages, and gelled solutions such as gelatin desserts.

The usual flavoring components are compatible with the essential ingredients of the composition, and if desired can be used in the usual manner. Both artificial and natural flavorings can be used, such as cherry,

strawberry, orange, lemon, lime, raspberry, blackberry, currant, coffee, peppermint, apple, apricot, peach and grape. Artifical colorings can also be added, such as red, orange, green, yellow, or brown, to improve the appearance of the composition.

Quinine and its salts, if added, add a bitter flavor which reduces sweetness. Niacinamide also adds a bitter flavor that reduces sweetness. Gentian is another bitter flavoring that can be used. Caffeine also adds a bitter taste.

The amount of flavoring if used will depend upon the taste per unit dose, and will normally be within the range from about 0 to about 60 parts, preferably from about 20 to about 30 parts, measured in milligrams for a normal size dosage unit. Similar amounts can be used of the coloring agents.

The candy compositions of the invention can be prepared by the following procedure:

An aqueous carbohydrate solution is prepared by adding water to the carbohydrate, or a natural syrup such as corn syrup or cane sugar syrup can be used. The syrup is then heated, preferably under vacuum, to a cooking temperature, usually 295F, although either a higher or lower temperature can be used. Heating is continued until the syrup has been reduced to a viscous mass of the desired water content. The concentrated sugar syrup is then transferred to a suitable blender or mixing slab. A uniform blend of alkaloid such as caffeine and anesthetic such as benzocaine is added, and blended thoroughly. A suitable blending temperature of the plastic mass is between about 240 and about 275F. Next is added the vitamin premix, and flavors and colors, as desired. The plastic mass can then be rolled and formed into discs, using ordinary hard candy compression machines, and allowed to harden at a reduced temperature, such as room temperature.

The following Examples, in the opinion of the inventor, represent preferred embodiments of the invention.

EXAMPLE 1 An active ingredient premix is prepared by mixing 630 grams of anhydrous caffeine, U.S.P. with 90 grams of benzocaine, N.F.

A vitamin blend is formed containing all essential vitamins for inclusion in the finished product.

The flavor is a wild cherry flavor, manufactured for use in high boiled confections.

The coloring to be used is FD and C Red, Number 40, which is used in a 10% solution for incorporation in high boiled confections.

A candy base is prepared by the mixing of ll5.7 pounds of 67% liquid sucrose and 51.7 pounds of high maltose corn syrup. This mixture is then heated to a temperature of 235 to 245 F in a precooker. After attaining the temperature, the mixture is pumped to the vacuum cooker where the temperature is raised to 250 to 270 F under 25 30 inches of vacuum.

This cooking removes water from the mass, so that the moisture level of the mass upon completion of cooking will be between 0.5 and 1%, and the total final weight of the mass will be about 1 19 pounds of sucrose and high maltose corn syrup solids.

The cooked mass is then placed in the premixer, where the premixed active ingredients are added. The first ingredient to be added is the caffeine and benzocaine premix. The next ingredients added are the vitamin premix, color, and flavor. After being mixed completely, the mass is transferred to the mixer cooling table. The mass is worked on this table automatically for a period of 4 to 6 minutes. During this period the mass will obtain a plastic consistency and the temperature will be lowered to between 170 and 190F. The mass is completely homogeneous.

The mass is then placed into forming equipment and run into discs or tablets that weigh three grams apiece. The discs or tablets are then placed on a cooling belt where the temperature is brought from 170F to 80- 90F in a period of 6 minutes. The finished candy product is then packaged for shipment.

EXAMPLE 2 The following is the formulation of a tablet, per tablet unit:

Amount Ingredient (mg) Caffeine 35 Benzocaine 5 Vitamin mixture l5 Flavoring 3O Dextrose, hydrous 2893 (compressible grade) Magnesium stearate 22 This mix can be compressed and tabletted using conventional tabletting equipment.

CLINICAL TEST Three hundred and eight obese subjects each at least pounds overweight were then separated into five paired groups, and subjected to a clinical test. Five paired groups of males and females were used in the test, each with a different regime.

Group I was assigned the amphetamine regime.

Group ll was assigned the AYDS regime.

Group II] was assigned the willpower regime, with a 35 bling, and cheating between meals, except for the product, and that they could use the product before meals or between meals whenever they had the desire to eat. They were further instructed to do no crash dieting, but merely to cut down on the sizes of their three meals. They were also allowed to drink alcoholic beverages.

A complete medical history was taken on each subject undertaking the regime. A general examination was made, including blood pressure determinations. The patients on each regime were weighed at the beginning of the regime, and at weekly intervals during the trial. The subjects were required to return once weekly to be weighed, to report the progress of the regime, and to report the presence or absence of side reactions.

Only subjects whose obesity was caused solely by improper eating habits were registered in the study. Patients with untreated glandular imbalance, endocrine conditions, disease, or other factors or reasons were excluded. To determine the cause of obesity in all cases,

each subject was carefully interviewed to ascertain all of his eating and drinking habits.

Each subject in the study was required to remain on the regime through a period of four weeks. The doubleblind procedure was employed for Groups IV and V, so

that the identity of the active appetite control product and the control product were unknown both to the patient and'to the doctor, and remained so until the conclusion of the trial. The control" product used was the product containing glucose and flavoring only. Supplies of all products were given to the patients on a weekly basis, to ensure their return to the clinic. Prescriptions for the amphetamines were issued weekly, as well.

Patients who failed to return for reexamination were considered dropouts. Those who advised in advance of their inability to return for reexamination for a valid reason were given an extra supply of the product, to

hold them until the next examination. Every effort was made to determine the reason or reasons why each subjected dropped out of the study. All followup data were recorded on case record forms, including reasons why the subject failed to cooperate and the reasons why they became dropouts.

The results of all five regimes are shown in Table i.

TABLE I.--RESULTS Group and regime No. of patients inducted into trial No. of patients who completed trial No. of patients who lost weight during entire triaL. No. of lbs. lost by patients who completed trial, lbs. No. of patients who lost Weight 1st week No. 01' lbs. lost 1st week, lbs Average weight loss 1st week, lbs. Minimum weight loss 1st week, 1bs Maximum weight loss 1st week, lbs Average weight loss during entire trial, lbs N0. of patients who gained Weight 1st week No. of lbs. gained 1st week, lbs No. 01' patients who remained at same weight 1st week Minimum weight loss during entire trial, lbs Maximum weight loss during entire trial, lbs, Average weekly weight loss during entire trial, lbs. N0. of patients who gained upon completion of trial No. of lbs. gained by patients who completed entire trial, lbs No. of patients who remained at same weight upon completion of entire trial No. of dropouts 1st week... No. of dropouts 2nd week No. 01 dropouts 3rd week. N o. of dropouts 4th week.

Total No. of dropouts I II III IV V Ampheta- O-T-C willpower mine proprietary (800-1, 200 Appetite (Dexedrine suppressant calorie control of 10 mg.) (AYBS) daily diet) Control invention Total 62 62 60 62 25 ll] U 32 24 16 9 27 206. G9. 25 40. 25 125. 00 31 36 41 199.50 80.00 06.75 111.50 4. 07 2.58 2. 6'.) 2. 72 0. 50 0. 50 0. 50 0. 25 13.00 6.00 6.25 7.75 8. 4. 33 l. 47 4. 63 1 11 3 (i 3. 25 14. 00 1. 50 16. 4 8 7 7 1. 25 1.00 0. 50 0.75 21.00 10.00 11.50 7.00 2.15 1.08 1.12 1.16 1 3 0 l 0. 50 3.00 (l (i. 50

0 0 (l 1 0 1 8 12 1-1 8 0 42 13 13 16 0 z 53 J 10 8 J 3 30 7 8 13 4 4 36 37 43 51 30 U Fifty-three patients out of a population of 62 on the Group V appetite control regime completed the trial, as compared with significantly fewer patients on the other regimes: Group I, amphetamines (25 of 62),

as compared with 79% of the patients in Group l, 5871 of those in Group III and 50% of Group II. It is to be further noted that 66% of the subjects in Group IV lost weight the first week, significantly more in number Group ll, OTC suppressant (19 of 62) and Group III th th e in Gr u s II or III willpo er 0f ignifican ly, Ore patients on The dropout population by the end of the trial for Group IV, control (32 of 62) completed the trial than Groups I to III was customarily high; amphetamines, those on any of the first three regimes. 60%; OTC suppressant, 69%; willpower, 85%. The

Subjects h Group V Q Completed the 9 dropout population for Group V is very low 14%). Sigmol'e that) twlee as fhueh Welght y the end the trial nificantly fewer patients in Group IV (48%) dropped as all sub ects combined who completed the trial on the f m h i l h those on any f h traditiemd first three regimes. Although both the Group IV and i S T bl N I Group V regimes offered oral gratification, neverthe- Th dropout population d i th fi d ond e those who eompleted the me] on Group V 10st v weeks of the trial also further demonstrates the ineffectimes more weight than those who completed the trial 15 tiveness f the regimes f Groups I to 1] h On Y P I mines, 34%; OTC suppressant, willpower, The number of h l Group v who lost welght Only two patients in Group V (3%) had dropped by the end ofthe trial (53) was more than double those by the end f the Second week The number who Q Group I on amphetamines (24) more than three dropped out of Group IV during this period was 27%, tlmes as y as those of P P H, on the OTC 20 again fewer than those on any of the first three regimes. Suppressant h nearly SIX as y as these The main reasons for patients dropping out were failf Group 011 PQ There Were nearly twlee ure to lose weight, side reactions, or dissatisfaction with as many who lost weight in Group V (53) as those in h regime to hi h h were i d Group IV (27). The presence or absence of side reactions is shown All 62 patients in Group V lost weight the first week, 25 i T bl N II,

TABLE H W Nugber of Tim as Rgportad 1nln'ita- Hyper Head 512- Dry Nervous Er Flam" Consfi' are m m use mmmswm wmww. 1% I Ampm- 5 a a 4 a a 7 14 '1 5 8 0 6 5 72 amine H OTC Propriell 888'- an? o o o 1 2 o o o o 0 0 1 2 14 1 O 21 m willpower o o o o o o 0 o o o 0 0 0 0 IV Control 0 0 0 0 0 0 1 0 0 0 0 0 0 0 1 0 0 2 v Appetite Controlol Invenfion 1 o 0 o 1 0 2 o 0' 0 o o 0 0 0 4 Side effects were most frequent and most severe, by far, among the amphetamine Group I. Tremor, nervousness, insomnia, nausea, constipation, palpitations, vertigo, drowsiness, dryness of the mouth and hyperactivity were fairly frequent reactions reported by those on the amphetamine regime. Several subjects on amphetamines denied side-effects in spite of overt evidence of their presence, or were reluctant to admit their occurrence for fear that the medication might be discontinued.

Constipation was a fairly frequent side effect, especially among subjects on the OTC suppressant Group ll regime; diarrhea, bloating, excessive gas, nausea and headache were also reported as side reactions caused by the OTC suppressant. Many subjects also complained that the suppressant (carmel candy) was uncomfortable in the mouth, causing dentures, caps and fillings to loosen or to fall out. Dryness of the mouth on occasion was reported by some subjects of Groups W and V. One subject said that the control product (hard candy) caused canker; one subject of Group V complained of insomnia, and one reported nausea.

At the conclusion of the 4 week test period, the weight reduction program for all Groups was continued for those patients who still were overweight. in this extended test. Group W was maintained to determine whether there would be a significant difference between the effectiveness of the appetitie control of the invention and the control. The results for all five Groups at the end of the 2 1 st week of the extended test are shown in Table lll.

Table Il Number of Patients on Protracted Study at End of 21st Week; Their Average Weekly Weight Loss; and Number of Patients Who Reduced to Normal Weight Table Il-Continued Number of Patients on Protracted Study at End of 21st Week; Their Average Weekly Weight Loss; and Number of Patients Who Reduced to Normal Weight Average Number of I Patient on Control- Regime Showed a net gain of 1.75 pounds.

The Table shows that the subjects of Group V on the appetite control composition of the invention lost significantly greater amounts of weight than those on any of the other four regimes, and they were continuing to lose an average of 2.2 lbs per week at the end of the fifth month of the test. Patients on the other four regimes during the protracted study continued to demonstrate unsatisfactory results, especially with regard to the number of dropouts.

The effect of the appetite control composition of the invention as an oral pacifier is considered to be a significant factor in aiding patients on this composition to lose more weight in larger numbers in less time than any of those on the other weight reduction regimes. In fact, a review of the literature over a 30 year period has shown that with the exception of Feinstein, Dole and Schwartz, The use of a formula diet for weight reduction of obese out-patients, Ann. Intern Med. 48 330-343, (1959), no author has published even a 20 lb weight loss in more than 29% of his patients. The percent of patients losing 40 lbs is far smaller. Thus, the results of this regime are quite remarkable, as compared to previously reported weight reduction regimes. in fact, the literature does not show a single successful long-term study using a diet regimen by itself or in combination with drugs, psychologic treatment, or exercise.

No patient on any of the four regimes except the appetite control regime of the invention successfully reduced to his normal weight during the 21 week study, despite the fact that each of the five regimes was equally divided as to the range of pounds overweight per patient. The average weekly weight loss of 2.2 lbs. by 43 patients on the appetite control composition of the invention is considered quite satisfactory, since this rate of loss allows for a gradual change in eating habits, and a gradual adjustment to an altered body image.

It has been found that weight loss decreases during protracted weight reduction programs. A considerable loss of body water (initial dehydration) is known to occur when obese patients start treatment with reducing diets. This may be due to changes in the diet which include reductions in the high intake of carbohydrates to a regime on which the patient depends in large measure on fat for much of his energy requirements. This mechanism might account for the decrease in the average weekly weight loss between the initial trial and the subsequent protracted study.

A weight maintenance program was also undertaken for test purposes with those patients participating who had attained their normal or desired weight, in order to ascertain whether this weight was maintained. Histories of maintenance of weight loss show even less success than histories of weight reduction (Fellows Am J M Sc 181 301-312, 1931 Mc Cann and Trulsonl Am DietetA 31 1108-1 110 (1955);Osserman and Dolger Ann Intern Med 34 72-79, (1951); Dole, Schwartz and Thaysen Am J Clin Nutr 2 381-390, (1954) The majority of patients regain all previous weight loss or even exceed previous weight losses. This is especially true of patients on amphetamines, and those attending diet clinics.

The patients on this weight maintenance program were quite similar in their histories. Prior to joining the clinical trial, they had been on and off diets for years, often under treatment with pharmacologic agents. None reported that they could maintain their weight loss, even though it was considerable in some cases, for any protracted period after reducing to their desired weight. All blamed their failures on traditional dieting methods, i.e., diets that prohibited eating and drinking most of the foods and beverages they desired or reducing by means of pharmacologic agents. Consequently, in the past, once their goal had been achieved, the impulse was to revert to indulging in foods and beverages, which their tastes demanded, in unrestricted amounts. They had not been adequately conditioned to do otherwise. Thorn and Bondy, (Obesity, in Principles of Internal Medicine, edited by Harrison TR, Adams, Bennett et a1, 5th ed. New York, McGraw-Hill Book Co., 1966, p 398 in evaluating the pharmacological treatment of obesity also have found that as soon as the pharmacologic effect wears off, or the medication is discontinued, appetite will return, and weight gain will recur, unless the patient 5 inherent capacity to control his food intake has been altered fundamentally.

A major requirement of the weight maintenance program was to test the effect that all desired foods and beverages had on individual metabolism. Patients began the program by ingesting small portions of whatever foods or beverages they wished, including desserts and alcoholic beverages. They recorded on a meal-bymeal, day-by-day basis the exact size of all portions of foods and beverages ingested. If, by the end of each week, they had not gained weight, they then knew the size of the portions they could eat or drink. If they had gained weight, they were advised to correspondingly reduce the amounts ingested. If they continued to lose weight, they were told to proportionately increase their portions. After a few weeks on the program while ingesting a wide variety of foods and beverages, they were able to adequately adjust, through habit, to the proper portions of both food and beverage without the need of calorie counting, which so many patients find difficult, inconvenient and impractical.

The entire population on the weight maintenance program (13 patients) had been on Group V, the appetite control regime. The subjects maintained their normal weight with the appetite control composition of the invention without fluctuating more than 1 or 2 pounds, plus or minus. When a pound or two was gained, they were trained to eliminate the gain the next week by adequate dieting.

Of great importance to these patients was the reeducation of eating customs which they had originally acquired while on the Group V appetite control regime. They had been instructed to ingest foods and beverages that they enjoyed, but in gradually reduced amounts each week. Consequently, when placed upon the weight maintenance program and permitted increased amounts of these pleasurable foods and beverages because no further weight losses were necessary, they felt rewarded; more importantly, they reported never being unduly hungry. The oral syndrome which previously resulted in snacking, nibbling and cheating was eliminated by the oral gratification provided by the appetite control composition of the invention.

Having regard to the foregoing disclosure, the following is claimed as the inventive and patentable embodiments thereof:

1. An appetite control composition for oral administration to a human subject to aid him in controlling his weight, comprising, in combination, a carbohydrate in an amount to obtain the effect ofcarbohydrate on hunger, and a nontoxic local anesthetic and an alkaloid stimulant in amounts to control the appetite.

2. An appetite control composition in accordance with claim 1, comprising at least one vitamin in an amount to supplement the vitamin intake of the user.

3. An appetite control composition in accordance with claim 1, in which the vitamins are selected from the group consisting of Vitamins A, B complex, C, D and E and mixtures thereof.

4. An appetite control composition in accordance with claim 1, in which the carbohydrate is selected from the group consisting of sucrose, glucose, maltose, fructose and dextrose and mixtures thereof.

5. An appetite control composition in accordance with claim 1, in which the carbohydrate is selected from the group consisting of corn syrup, cane sugar, and beet sugar.

6. An appetite control composition in accordance with claim 1 in which the nontoxic local anesthetic is a lower alkyl ester of para-amino benzoic acid lacking a secondary or tertiary amino group.

7. An appetite control composition in accordance with claim 6 in which the ester is selected from the group consisting of ethyl aminobenzoate, butyl aminobenzoate, butacaine sulfate, and orthoform.

8. An appetite control composition in accordance with claim 1, in which the alkaloid stimulant is caffeine or a caffeinerelated alkaloid.

9. An appetite control composition in accordance with claim 1, in the form of a candy or sweet.

10. An appetite control composition in accordance with claim 1, in the form of a solid.

11. An appetite control composition in accordance with claim 1, in the form of a liquid.

12. An appetite control composition in accordance with claim 1, comprising a flavoring agent to render the composition more palatable.

13. An appetite control composition in accordance with claim 1, comprising a coloring agent to render the composition more attractive.

14. An appetite control composition in accordance with claim 1, in a dosage unit form, in which the proportions of the essential ingredients are selected for an appetite control effect per dosage unit.

15. An appetite control composition in accordance with claim 14, in which the dosage unit form is within the range from about 1 to about l2 g. in weight.

16. An appetite control composition in accordance with claim 14, in which the amount of carbohydrate is sufficient to maintain blood sugar at a high normal level and is within the range from about 1000 to about 6000 mg. per unit dosage.

17. An appetite control composition in accordance with claim 15, in which the amount of anesthetic is within the range from about 3 to about 20 mg.

18. An appetite control composition in accordance with claim 14, in which the amount of alkaloid stimulant is within the range from about 10 to about mg.

19. An appetite control composition in accordance with claim 14, comprising at least one vitamin in an amount within the range from about 0.1 USRDA to about 5 USRDA.

20. An appetite control composition in accordance with claim 1, in which the amount of carbohydrate is within the range from about 1000 to about 6000 parts by weight.

21. An appetite control composition in accordance with claim 1, in which the amount of anesthetic is within the range from about 3 to about 20 parts by weight.

22. An appetite control composition in accordance with claim 1, in which the amount of alkaloid stimulant is within the range from about 10 to about 80 parts by weight.

23. An appetite control composition in accordance with claim 1, comprising at least one vitamin in an amount within the range from about 0.1 USRDA to about 5 USRDA.

24. An appetite control composition in accordance with claim 1, in a dosage unit form that is long-lasting in the mouth of the user.

25. An appetite control composition in accordance with claim 1, in which the carbohydrate is in the form of a solid matrix in which the other ingredients are dispersed.

26. A process for controlling weight of patients which comprises administering orally a composition in accordance with claim 1 and limiting the intake of foods by control of appetite therewith.

27. A process for controlling weight of'patients in accordance with claim 26, in which the appetite control composition is in dosage unit form.

28. A process for controlling weight of patients in accordance with claim 27, in which the dosage unit form is a candy or a sweet.

Claims

1. AN APPETITE CONTROL COMPOSITION FOR ORAL ADMINISTRATION TO A HYMAN SUBJECT TO AID HIM IN CONTROLLING HIS WEIGHT, COMPRISING, IN COMBINATION, A CARBOHYDRATE IN AN AMOUNT TO OBTAIN THE EFFECT OF CARBOHYDRATE ON HUNGER, AND A NONTOXIC LOCAL ANESTHETIC AND AN ALKALOID STIMULTANT IN AMOUNTS TO CONTROL THE APPETITE.

15. An appetite control composition in accordance with claim 14, in which the dosage unit form is within the range from about 1 to about 12 g. in weight.

18. An appetite control composition in accordance with claim 14, in which the amount of alkaloid stimulant is within the range from about 10 to about 80 mg.

27. A process for controlling weight of patients in accordance with claim 26, in which the appetite control composition is in dosage unit form.