US2881113A - Therapeutically active compositions containing amphetamines - Google Patents
Therapeutically active compositions containing amphetamines Download PDFInfo
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- US2881113A US2881113A US636866A US63686657A US2881113A US 2881113 A US2881113 A US 2881113A US 636866 A US636866 A US 636866A US 63686657 A US63686657 A US 63686657A US 2881113 A US2881113 A US 2881113A
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- United States
- Prior art keywords
- mgm
- amphetamine
- amphetamines
- aluminum hydroxide
- magnesium trisilicate
- Prior art date
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- Expired - Lifetime
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- 239000000203 mixture Substances 0.000 title claims description 26
- GXGAKHNRMVGRPK-UHFFFAOYSA-N dimagnesium;dioxido-bis[[oxido(oxo)silyl]oxy]silane Chemical compound [Mg+2].[Mg+2].[O-][Si](=O)O[Si]([O-])([O-])O[Si]([O-])=O GXGAKHNRMVGRPK-UHFFFAOYSA-N 0.000 claims description 12
- 239000000391 magnesium silicate Substances 0.000 claims description 12
- 229940099273 magnesium trisilicate Drugs 0.000 claims description 12
- 229910000386 magnesium trisilicate Inorganic materials 0.000 claims description 12
- 235000019793 magnesium trisilicate Nutrition 0.000 claims description 12
- 208000008589 Obesity Diseases 0.000 claims description 7
- VIROVYVQCGLCII-UHFFFAOYSA-N amobarbital Chemical compound CC(C)CCC1(CC)C(=O)NC(=O)NC1=O VIROVYVQCGLCII-UHFFFAOYSA-N 0.000 claims description 7
- 235000020824 obesity Nutrition 0.000 claims description 7
- -1 DEXTROAMPHETAMINE COMPOUND Chemical class 0.000 claims description 5
- TWXDDNPPQUTEOV-FVGYRXGTSA-N methamphetamine hydrochloride Chemical compound Cl.CN[C@@H](C)CC1=CC=CC=C1 TWXDDNPPQUTEOV-FVGYRXGTSA-N 0.000 claims description 5
- 229960000632 dexamfetamine Drugs 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical class C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 description 15
- 229940069428 antacid Drugs 0.000 description 13
- 239000003159 antacid agent Substances 0.000 description 13
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 12
- 239000003826 tablet Substances 0.000 description 9
- 229940025084 amphetamine Drugs 0.000 description 7
- 238000011282 treatment Methods 0.000 description 6
- PYHRZPFZZDCOPH-QXGOIDDHSA-N (S)-amphetamine sulfate Chemical compound [H+].[H+].[O-]S([O-])(=O)=O.C[C@H](N)CC1=CC=CC=C1.C[C@H](N)CC1=CC=CC=C1 PYHRZPFZZDCOPH-QXGOIDDHSA-N 0.000 description 5
- LCWAOCHOPBSGMU-UHFFFAOYSA-J aluminum;magnesium;sodium;hydrogen carbonate;oxygen(2-);silicon;trihydroxide Chemical compound [OH-].[OH-].[OH-].[O-2].[Na+].[Mg+2].[Al+3].[Si].OC([O-])=O LCWAOCHOPBSGMU-UHFFFAOYSA-J 0.000 description 5
- 229940119751 dextroamphetamine sulfate Drugs 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 239000007937 lozenge Substances 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 108010010803 Gelatin Proteins 0.000 description 4
- BWZOPYPOZJBVLQ-UHFFFAOYSA-K aluminium glycinate Chemical compound O[Al+]O.NCC([O-])=O BWZOPYPOZJBVLQ-UHFFFAOYSA-K 0.000 description 4
- 230000001458 anti-acid effect Effects 0.000 description 4
- 230000036528 appetite Effects 0.000 description 4
- 235000019789 appetite Nutrition 0.000 description 4
- 229940015826 dihydroxyaluminum aminoacetate Drugs 0.000 description 4
- 201000006549 dyspepsia Diseases 0.000 description 4
- 229920000159 gelatin Polymers 0.000 description 4
- 239000008273 gelatin Substances 0.000 description 4
- 235000019322 gelatine Nutrition 0.000 description 4
- 235000011852 gelatine desserts Nutrition 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 229940024545 aluminum hydroxide Drugs 0.000 description 3
- PYHRZPFZZDCOPH-UHFFFAOYSA-N amphetamine sulfate Chemical compound OS(O)(=O)=O.CC(N)CC1=CC=CC=C1.CC(N)CC1=CC=CC=C1 PYHRZPFZZDCOPH-UHFFFAOYSA-N 0.000 description 3
- 229940098184 amytal Drugs 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 208000024798 heartburn Diseases 0.000 description 3
- 229960002532 methamphetamine hydrochloride Drugs 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- SEVKYLYIYIKRSW-UHFFFAOYSA-N 1-phenylpropan-2-ylazanium;chloride Chemical compound Cl.CC(N)CC1=CC=CC=C1 SEVKYLYIYIKRSW-UHFFFAOYSA-N 0.000 description 2
- FTOAOBMCPZCFFF-UHFFFAOYSA-N 5,5-diethylbarbituric acid Chemical compound CCC1(CC)C(=O)NC(=O)NC1=O FTOAOBMCPZCFFF-UHFFFAOYSA-N 0.000 description 2
- 206010012735 Diarrhoea Diseases 0.000 description 2
- 206010028813 Nausea Diseases 0.000 description 2
- 206010033307 Overweight Diseases 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 230000002891 anorexigenic effect Effects 0.000 description 2
- 239000002830 appetite depressant Substances 0.000 description 2
- 229960002319 barbital Drugs 0.000 description 2
- 229940125717 barbiturate Drugs 0.000 description 2
- 230000003139 buffering effect Effects 0.000 description 2
- 230000000881 depressing effect Effects 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 235000012054 meals Nutrition 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 230000008693 nausea Effects 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 230000008673 vomiting Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 208000020401 Depressive disease Diseases 0.000 description 1
- 240000006927 Foeniculum vulgare Species 0.000 description 1
- 235000004204 Foeniculum vulgare Nutrition 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 206010024264 Lethargy Diseases 0.000 description 1
- 244000246386 Mentha pulegium Species 0.000 description 1
- 235000016257 Mentha pulegium Nutrition 0.000 description 1
- 235000004357 Mentha x piperita Nutrition 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229940008238 amphetamine sulfate Drugs 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 235000001050 hortel pimenta Nutrition 0.000 description 1
- 235000003642 hunger Nutrition 0.000 description 1
- 239000008141 laxative Substances 0.000 description 1
- 230000002475 laxative effect Effects 0.000 description 1
- 201000003102 mental depression Diseases 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 201000003631 narcolepsy Diseases 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- DDBREPKUVSBGFI-UHFFFAOYSA-N phenobarbital Chemical compound C=1C=CC=CC=1C1(CC)C(=O)NC(=O)NC1=O DDBREPKUVSBGFI-UHFFFAOYSA-N 0.000 description 1
- 229960002695 phenobarbital Drugs 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 238000009491 slugging Methods 0.000 description 1
- 239000000021 stimulant Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
Definitions
- This invention relates to new and improved compositions consisting of amphetamine compounds and has particular relation to a new and useful therapeutic agent containing the aforementioned compounds. More specifically, the present invention relates to amphetamine compounds such as dl-amphetamine sulfate, dl-amphetamine hydrochloride, dextroamphetamine sulfate, and methamphetamine hydrochloride, combined with critical amounts of an amphoteric antacid such as aluminum hydroxide, magnesium trisilicate, or dihydroxy aluminum aminoacetate.
- the compositions of my invention are appetite satients effective for the treatment of obesity.
- amphetamines are used not infrequently in the treatment of mental depression, narcolepsy, lethargy and several other conditions. Their most common use, however, is as appetite depressants in the treatment of overweight and obesity.
- amphetamine compounds such as amphetamine sulfate and hydrochloride, dextroamphetamine sulfate, methamphetamine hydrochloride, etc., act as stimulants for the central nervous system and are capable of exerting valuable effects in the treatment of obesity.
- amphetamine compounds have also certain undesirable gastrointestinal effects, such as heartburn, nausea, vomiting, and diarrhea. These symptoms are not infrequently observed in patients receiving amphetamine compounds.
- Another object of the present invention is to provide a therapeutic agent, the anorexigenic or appetite-depressant effects of which are higher than those of the amphetamines alone.
- Still another object of this invention is to reduce the undesirable side effects such as epigastric distress and heartburn which are occasionally encountered with the amphetamines alone.
- the novel appetite satient composition of the present invention includes, in addition to the amphetamine compound or mixture of amphetamine compounds, at least 8 milli-equivalents of a mixture of aluminum hy- 2 dioxide, magnesium trisilicate, and dihydroxyaluminum aminoacetate.
- the amphetamine compound which I have found effective in my compositions is dextroamphetamine (dextro-l-phenyl-2-aminopropane). It is known that this compound is more effective when mixed with the dlamphetamine.
- a sedative such as amytal (5-ethy1-5- isoamyl barbituric acid), barbital. (5,5'-diethyl barbituric acid), or phenobarbital 5-ethyl-5'-phenyl barbituric acid) in variable doses.
- compositions prepared according to this invention contain about two or three parts by weight of magnesium trisilicate to one part by weight of aluminum hydroxide.
- Dihydroxy aluminum amino'acetate may be substituted in whole or in part for the aluminum hydroxide.
- My compositions may more conveniently be used i171 the form of tablets of lozenges (pleasant tasting).
- tablets may be prepared by mixing the active'ingredients (amphetamine compounds, barbiturates, magnesium trisilicate, and aluminum hydroxide) with excipients (sugar, talc, corn starch and binders) and flavoring oils (oil of peppermint, oil of fennel and methyl salicylate).
- the tablet may be prepared by processes well known in the pharmaceutical line, such as by slugging or by a wet granulation process.
- Lozenges containing similar dosage of active ingredients may also be prepared by known methods. It is an advantage of the lozenges that they' may be chewed and swallowed without the aid of water.
- the lozenges are a most convenient dosage form.
- EXAMPLE II Ingredient: Per tablet, mgm. A. Dextroamphetamine sulfate 3.5 Methamphetamine hydrochloride 1.5 Amytal 20.0 Aluminum hydroxide 110.0 Magnesium trisilicate 350.0
- amphetamines were in the same dosage as noted for group I.
- the 10 patients in group III were a control group. These patients received antacids (aluminum hydroxide and magnesium trisilicate) alone.
- EXAMPLE IV Ingredient: Per tablet, mgm. AJBextroamphetamine sulfate 3.0 dl-Amphetamine sulfate 3.0 Amytal 30.0 Aluminum hydroxide 110.0 Magnesium trisilicate 600.0 Dixhydroxy aluminum aminoacetate 300.0 E. Sucrose 1000.0
- the proportions of the various ingredients of my composition may be varied widely.
- the amphetamine comperiod may vary from about 3 to about 6 mgm. per dosage unit.
- the barbiturate may be eliminated entirely or may be present in an amount up to approximately mgm.
- the lower limit of the amphoteric antacid is critical as too small an amount is not effective. I have found that at least 4 milli-equivalents of aluminum hydroxide (104 mgm.) in combination with at least 4 mini-equivalents of magnesium trisilicate (350 mgm.) is required to synergize the appetite depressing action of amphetamines. An equivalent amount of dihydroxy aluminum aminoacetate may be substituted for the aluminum hydroxide. Since the amphoteric antacids employed are non-toxic, the upper limit of the amount of antacid present is not critical.
- An obesity control composition suitable for oral administration comprising in the following relative proportions, 3-4 mgm. of a dextroamphetamine compound, 1-2 mgm. of d-methamphetamine hydrochloride, 0-20 mgm. of S-ethyl-S-isoamyl barbituric acid, 4 milli-equivalents of aluminum hydroxide, and 4 milli-equivalents of magnesium trisilicate.
- An obesity control composition suitable for oral administration comprising in the following relative pro-. portions, 3 mgm. of dextroamphctamine sulfate, 3 mgm. of dl-amphetamine hydrochloride, 20 mgm. of S-ethyl-S- isoamyl barbituric acid, 350 mgm. of aluminum hydroxide, and 800 mgm. of magnesium trisilicate.
- An obesity control composition suitable for oral of a mixture of amphetamine compounds and at least 8 milli-equivalents of a mixture of aluminum hydroxide and magnesium trisilicate.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
United States Patent THERAPEUTICALLY ACTIVE COMPOSITIONS CONTAINING AMPHETAMINES Max Millman, Springfield, Mass, assignor 'to' Ortho lyharmaceutical Corporation, a corporation of New ersey N0 Drawing. Application January 29, 1957 Serial No. 636,866
3 Claims. (Cl. 167-55) This invention relates to new and improved compositions consisting of amphetamine compounds and has particular relation to a new and useful therapeutic agent containing the aforementioned compounds. More specifically, the present invention relates to amphetamine compounds such as dl-amphetamine sulfate, dl-amphetamine hydrochloride, dextroamphetamine sulfate, and methamphetamine hydrochloride, combined with critical amounts of an amphoteric antacid such as aluminum hydroxide, magnesium trisilicate, or dihydroxy aluminum aminoacetate. The compositions of my invention are appetite satients effective for the treatment of obesity.
The amphetamines are used not infrequently in the treatment of mental depression, narcolepsy, lethargy and several other conditions. Their most common use, however, is as appetite depressants in the treatment of overweight and obesity.
It is well known that amphetamine compounds such as amphetamine sulfate and hydrochloride, dextroamphetamine sulfate, methamphetamine hydrochloride, etc., act as stimulants for the central nervous system and are capable of exerting valuable effects in the treatment of obesity. However, said compounds have also certain undesirable gastrointestinal effects, such as heartburn, nausea, vomiting, and diarrhea. These symptoms are not infrequently observed in patients receiving amphetamine compounds.
It is the main object of the present invention to provide an amphetamine composition, the beneficial eifects of which are greater and the undesirable side eflfects of which are less than known amphetamine compositions.
It is another object of the present invention to improve the action of amphetamine compounds by buffering or combining them with critical amounts of amphoteric antacids such as aluminum hydroxide, magnesium trisilicate, and dihydroxy aluminum aminoacetate.
Another object of the present invention is to provide a therapeutic agent, the anorexigenic or appetite-depressant effects of which are higher than those of the amphetamines alone.
Still another object of this invention is to reduce the undesirable side effects such as epigastric distress and heartburn which are occasionally encountered with the amphetamines alone.
Other objects and advantages of the invention will be apparent from the appended claims and the following specification which describes by way of example some embodiments of the invention.
I have now discovered that the appetite depressing action of amphetamines may be synergized and the undesirable side efiects of amphetamine compounds reduced by combining or buffering them with critical amounts of certain amphoteric antacids. More specifically, the novel appetite satient composition of the present invention includes, in addition to the amphetamine compound or mixture of amphetamine compounds, at least 8 milli-equivalents of a mixture of aluminum hy- 2 dioxide, magnesium trisilicate, and dihydroxyaluminum aminoacetate.
The amphetamine compound which I have found effective in my compositions is dextroamphetamine (dextro-l-phenyl-2-aminopropane). It is known that this compound is more effective when mixed with the dlamphetamine. I prefer to use in a single dosage unit approximately 3 mgm. of an amphetamine compound such as dextroamphetamine sulfate together with 3 mgm. of dl-amphetamine sulfate. To this I add at least .8- milliequivalents of a mixture of aluminum hydroxide and magnesium trisilicate. To minimize the occasional undesirable stimulation of the nervous system caused by administering amphetamine compounds, I may. add to my composition a sedative such as amytal (5-ethy1-5- isoamyl barbituric acid), barbital. (5,5'-diethyl barbituric acid), or phenobarbital 5-ethyl-5'-phenyl barbituric acid) in variable doses.
Because of their amphoteric character, there is no critical limitation on the maximum amount of antacid that is present in my compositions. As magnesium trisilicate is a laxative and large amounts of aluminum hydroxide would cause constipation, it is desirable 'to combine these two antacids. Satisfactory compositions prepared according to this invention contain about two or three parts by weight of magnesium trisilicate to one part by weight of aluminum hydroxide. Dihydroxy= aluminum amino'acetate may be substituted in whole or in part for the aluminum hydroxide.
My compositions may more conveniently be used i171 the form of tablets of lozenges (pleasant tasting). The
tablets may be prepared by mixing the active'ingredients (amphetamine compounds, barbiturates, magnesium trisilicate, and aluminum hydroxide) with excipients (sugar, talc, corn starch and binders) and flavoring oils (oil of peppermint, oil of fennel and methyl salicylate). The tablet may be prepared by processes well known in the pharmaceutical line, such as by slugging or by a wet granulation process. Lozenges containing similar dosage of active ingredients may also be prepared by known methods. It is an advantage of the lozenges that they' may be chewed and swallowed without the aid of water.
As the amphetamines are most effective when taken about one-half to one hour before meals when water is not always readily available for administration, the lozenges are a most convenient dosage form.
Granulate part A with 10% gelatin solution and dry at 50 C. Regranulate and mix with B. Compress into tablets weighing 1183.5 mgm.
EXAMPLE II Ingredient: Per tablet, mgm. A. Dextroamphetamine sulfate 3.5 Methamphetamine hydrochloride 1.5 Amytal 20.0 Aluminum hydroxide 110.0 Magnesium trisilicate 350.0
B. Starch 4.25 Magnesium stearate 4.25
Granulate part A with 10% gelatin solution. Dry at Compress .into
with the exception that the aluminum hydroxide and magnesium trisilicate were omitted. The amphetamines were in the same dosage as noted for group I.
The 10 patients in group III were a control group. These patients received antacids (aluminum hydroxide and magnesium trisilicate) alone.
The clinical results are tabulated in Table I.
Table 1 Average Number Total lbs. lost Group of Treatment lbs. lost, per
patients 8 wks. patlent per week I 26 Amphetamines and antacids... 479 2. 30 II 26 Amphetamines alone 261 1. III..... 10 Antacids alone 0 It is apparent that there is a significant difference in the degree of weight loss induced by the three treatments. It may be noted that the antacids have no appetite-depressing action. Since, however, upon combination with amphetamines the anorexigenic effect of the latter was enhanced, it may be concluded that the antacids pro- EXAMPLE .111 Ingredient: Per tablet, mgm. A. Dextroamphetamine sulfate up 5.0 Amytal 15.0 Aluminum hydroxide 250.0 Magnesium trisilicate 500.0 B. Starch 4.25 Magnesium stearate 4.25 -Granulate part A with 10% gelatin solution and dry at 50 C. Regranulate and mix with B. Compress into tablets weighing 778.5 mgm.
EXAMPLE IV Ingredient: Per tablet, mgm. AJBextroamphetamine sulfate 3.0 dl-Amphetamine sulfate 3.0 Amytal 30.0 Aluminum hydroxide 110.0 Magnesium trisilicate 600.0 Dixhydroxy aluminum aminoacetate 300.0 E. Sucrose 1000.0
I Granulate part A with 10% gelatin solution and dry at ,50' C. Regranulate and mix with B. Compress into lozenges weighing 2,046 mgm.
"The proportions of the various ingredients of my composition may be varied widely. The amphetamine comperiod may vary from about 3 to about 6 mgm. per dosage unit. The barbiturate may be eliminated entirely or may be present in an amount up to approximately mgm. The lower limit of the amphoteric antacid is critical as too small an amount is not effective. I have found that at least 4 milli-equivalents of aluminum hydroxide (104 mgm.) in combination with at least 4 mini-equivalents of magnesium trisilicate (350 mgm.) is required to synergize the appetite depressing action of amphetamines. An equivalent amount of dihydroxy aluminum aminoacetate may be substituted for the aluminum hydroxide. Since the amphoteric antacids employed are non-toxic, the upper limit of the amount of antacid present is not critical.
"The practical effect of my amphetamine compositions may be appreciated from clinical results on 62 unselected overweight patients ranging in age from 17 to 72 years and in weight from 132 to 291 pounds. These patients were divided into three groups and treated for a period of eight weeks. The 26 patients in group I were treated with tablets prepared according to Example I. Dosage wasthre'e tablets daily about one-half to one hour before meals, yielding a total of 15 mgm. of amphetamines perday.
Group II also consisted of 26 patients similarly treated What is claimed is:
duced a synergistic effect with the amphetamines. Experimental findings in laboratory animals corroborate this observation.
In addition to the better results observed with the use of aluminum hydroxide and magnesium trisilicate, the patients in group I reported less hunger and fewer gastrointestinal side effects such as heartburn, nausea, vomiting and diarrhea.
1. An obesity control composition suitable for oral administration comprising in the following relative proportions, 3-4 mgm. of a dextroamphetamine compound, 1-2 mgm. of d-methamphetamine hydrochloride, 0-20 mgm. of S-ethyl-S-isoamyl barbituric acid, 4 milli-equivalents of aluminum hydroxide, and 4 milli-equivalents of magnesium trisilicate.
2. An obesity control composition suitable for oral administration comprising in the following relative pro-. portions, 3 mgm. of dextroamphctamine sulfate, 3 mgm. of dl-amphetamine hydrochloride, 20 mgm. of S-ethyl-S- isoamyl barbituric acid, 350 mgm. of aluminum hydroxide, and 800 mgm. of magnesium trisilicate.
3. An obesity control composition suitable for oral of a mixture of amphetamine compounds and at least 8 milli-equivalents of a mixture of aluminum hydroxide and magnesium trisilicate.
References Cited in the file of this patent Wilson: The American Drug Index, 1956, Lippincott Co., Philadelphia, Pa., PP. 292 and 337.
Claims (1)
1. AN OBESITY CONTROL COMPOSITION SUITABLE FOR ORAL ADMINISTRATION COMPRISING IN THE FOLLOWING RELATIVE PROPORTIONS, 3-4 MGM. OF A DEXTROAMPHETAMINE COMPOUND, 1-2 MGM. OF D-METHAMPHETAMINE HYDROCHLORIDE, O-20 MGM. OF 5-ETHYL-5-ISOAMYL BARBITURIC ACID, 4 MILLI-EQUIVALENTS OF ALUMIUNM HYDROXIDE, AND 4 MILLI-EQUIVALENTS OF MAGNESIUM TRISILICATE.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US636866A US2881113A (en) | 1957-01-29 | 1957-01-29 | Therapeutically active compositions containing amphetamines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US636866A US2881113A (en) | 1957-01-29 | 1957-01-29 | Therapeutically active compositions containing amphetamines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| US2881113A true US2881113A (en) | 1959-04-07 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US636866A Expired - Lifetime US2881113A (en) | 1957-01-29 | 1957-01-29 | Therapeutically active compositions containing amphetamines |
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| Country | Link |
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| US (1) | US2881113A (en) |
Cited By (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3369967A (en) * | 1962-11-21 | 1968-02-20 | Lab D Analyses Et De Rech S Bi | Compositions for treating obesity and methods of use |
| US4581232A (en) * | 1983-07-20 | 1986-04-08 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates |
| US4632822A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antiasmatics |
| US4632823A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of appetite suppressants |
| US4632821A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of decongestants |
| US4642231A (en) * | 1983-07-20 | 1987-02-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antihistamines |
| US4643892A (en) * | 1983-07-20 | 1987-02-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of analgesics |
| US4643898A (en) * | 1983-07-20 | 1987-02-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of nutritional supplements and laxatives |
| US4647459A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Confectionery compositions containing magnesium trisilicate adsorbates |
| US4647449A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of alkaloids |
| US4647450A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Chewing gum compositions containing magnesium trisilicate absorbates |
| US4649041A (en) * | 1983-07-20 | 1987-03-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants |
| US4650663A (en) * | 1983-07-20 | 1987-03-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antitussives |
| US20040219213A1 (en) * | 1998-10-21 | 2004-11-04 | Burnside Beth A. | Oral pulsed dose drug delivery system |
| US20060127473A1 (en) * | 2004-12-13 | 2006-06-15 | Nichols William M | Compositions and methods for stabilizing active pharmaceutical ingredients |
| US20070264323A1 (en) * | 2006-05-12 | 2007-11-15 | Shire Llc | Controlled dose drug delivery system |
| US20080139653A1 (en) * | 2006-12-11 | 2008-06-12 | Mickle Travis C | Non-standard amino acid conjugates of amphetamine and processes for making and using the same |
| US20080207757A1 (en) * | 2007-02-08 | 2008-08-28 | Mickle Travis C | Polar Hydrophilic Prodrugs of Amphetamine and Other Stimulants and Processes for Making and Using the Same |
-
1957
- 1957-01-29 US US636866A patent/US2881113A/en not_active Expired - Lifetime
Non-Patent Citations (1)
| Title |
|---|
| None * |
Cited By (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3369967A (en) * | 1962-11-21 | 1968-02-20 | Lab D Analyses Et De Rech S Bi | Compositions for treating obesity and methods of use |
| US4650663A (en) * | 1983-07-20 | 1987-03-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antitussives |
| US4632822A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antiasmatics |
| US4632823A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of appetite suppressants |
| US4632821A (en) * | 1983-07-20 | 1986-12-30 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of decongestants |
| US4642231A (en) * | 1983-07-20 | 1987-02-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antihistamines |
| US4643892A (en) * | 1983-07-20 | 1987-02-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of analgesics |
| US4643898A (en) * | 1983-07-20 | 1987-02-17 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of nutritional supplements and laxatives |
| US4647459A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Confectionery compositions containing magnesium trisilicate adsorbates |
| US4647449A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of alkaloids |
| US4647450A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Chewing gum compositions containing magnesium trisilicate absorbates |
| US4649041A (en) * | 1983-07-20 | 1987-03-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants |
| US4581232A (en) * | 1983-07-20 | 1986-04-08 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates |
| USRE42096E1 (en) * | 1998-10-21 | 2011-02-01 | Shire LLC, USA | Oral pulsed dose drug delivery system |
| US20040219213A1 (en) * | 1998-10-21 | 2004-11-04 | Burnside Beth A. | Oral pulsed dose drug delivery system |
| US20060127473A1 (en) * | 2004-12-13 | 2006-06-15 | Nichols William M | Compositions and methods for stabilizing active pharmaceutical ingredients |
| US20070264323A1 (en) * | 2006-05-12 | 2007-11-15 | Shire Llc | Controlled dose drug delivery system |
| US9173857B2 (en) | 2006-05-12 | 2015-11-03 | Shire Llc | Controlled dose drug delivery system |
| US8846100B2 (en) | 2006-05-12 | 2014-09-30 | Shire Llc | Controlled dose drug delivery system |
| WO2008073918A1 (en) * | 2006-12-11 | 2008-06-19 | Kempharm, Inc. | Non-standard amino acid conjugates of amphetamine and processes for making and using the same |
| US7776917B2 (en) | 2006-12-11 | 2010-08-17 | Mickle Travis C | Non-standard amino acid conjugates of amphetamine and processes for making and using the same |
| US20100292336A1 (en) * | 2006-12-11 | 2010-11-18 | Mickle Travis C | Polar Hydrophilic Prodrugs and Non-Standard Amino Acid Conjugates of Amphetamine and Other Stimulants and Processes for Making and Using the Same |
| US8101661B2 (en) | 2006-12-11 | 2012-01-24 | Kempharm, Inc. | Polar hydrophilic prodrugs and non-standard amino acid conjugates of amphetamine and other stimulants and processes for making and using the same |
| US20080139653A1 (en) * | 2006-12-11 | 2008-06-12 | Mickle Travis C | Non-standard amino acid conjugates of amphetamine and processes for making and using the same |
| US20100292337A1 (en) * | 2007-02-08 | 2010-11-18 | Mickle Travis C | Polar Hydrophilic Prodrugs of Amphetamine and Other Stimulants and Processes for Making and Using the Same |
| US20080207757A1 (en) * | 2007-02-08 | 2008-08-28 | Mickle Travis C | Polar Hydrophilic Prodrugs of Amphetamine and Other Stimulants and Processes for Making and Using the Same |
| US7772222B2 (en) | 2007-02-08 | 2010-08-10 | Mickle Travis C | Polar hydrophilic prodrugs of amphetamine and other stimulants and processes for making and using the same |
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