US 2427887 A
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Patented Sept. 23, 1947 2,427,883] ANALGESIC coMrosrnoN Theodore B. Wallace, Plymouth Meeting, Pa., as-
signor to Smith, Kline & French Laboratories, Philadelphia, Pa., a corporation of Pennsylvania No Drawing. Application October 23,
Serial No. 507,455
This invention relates to an analgesic composition and, more particularly, to an analgesic composition of the antipyretic type having no narcotic effect.
The composition according to this invention has been found to be of great eflicacy in relievin pain in cases such as headache, toothache, neuralgia, and the like, where analgesics of the antipyretic type having no narcotic effect, as, for example, aspirin and the like, are indicated,
The composition according to this invention involves the combination of an analgesic of the antipyretic type having no narcotic efiect with a sympathomimetic amine, effective to stimulate the sympathetic and central nervous systems, having a structure within the following formula, optical isomers and non-toxic salts thereof:
cm-cn-cm I NHR wherein R is a member of the group consisting of H and CH3.
The sympathomimetic amines of the group indicated, the optical isomers and non-toxic salts thereof have been long well known and widely used. However, they have not heretofore been suggested or used for analgesic effect, However, despite their lack of any recognized analgesic effect and their well known capacity to stimulate the sympathetic central nervous systems, when administered in admixture with a given dose of an analgesic of the antipyretic type having no narcotic effect, they markedly increase the anal-.
As illustrative of aromatic sympathomimetic amines contemplatedas an ingredient of compositions according to this invention, for example, l-phenyl-Z-aminopropane, phenylisopropylmeth- 6 Claims. (Cl. 167-65) 2 ylamine, optical isomers and non-toxic salts thereof, as sulfates, hydrochlorides, and the like, may be used.
The essential ingredients of the composition according to this invention may be included inwidely Varying proportion. For administration the composition may be made up in various forms, as, for example, in a tablet, a solution, a powder or other suitable form.
As will be obvious, the essential ingredients may be extended with any desired excipient, as, for example, sugar or milk, starch, water, or the like, and if desired other ingredients may be included, such, for example, as an effervescent, as sodium bicarbonate and citric acid, or the like where it is desirable to administer the composition in the form of an effervescent drink.
Generally speaking, and for practical purposes, the essential ingredients of the composition in accordance with this invention will be combined in proportions within about the broad range:
More specifically with reference to a composition including acetylsalicylic acid and phenylisopropylamine sulfate (amphetamine sulfate),-
the essential component may be present within about the range:
Acetylsalicylic acid gm .31.0 Phenylisopropylamine sulfate mgm 5-10 and generally a highly eflicient composition may be made up on any of the following formulae:
Example 1 Acetylsalicylic acid gm 0.5 Amphetamine sulfate "mgm 5 I Example 2 Aminopyrine cm 0,3 d-Phenylisopropylamine sulfate mgm- 2.5
Example 3 Acetophenetidin ..gm 0.3 d-Phenylisopropylmethylamine sulfate v i A mgm 2.5 Example 4 Aminopyrine m 0.3 rl-(p-hydroxyphenyl) -2-aminopropane hydrobromide g 20 variously the dosage and form of the composition for administration according to this invention will vary for the individual case and it will be understood that the specific examples given above are not limiting, but are given as illustrative of practical procedure.
In making up compositions in accordance with this invention using the essential ingredients in proportions within the range indicated, the essential ingredients in powdered form will be admixed, an excipient, as sugar of milk, added and the composition tableted. Again, the ingredients may remain in powdered form or be put in solution for administration. As has been indicated, an effervescent may be added to the end that the composition may be administered in water with efiervescence.
What I claim and desire to protect by Letters Patent is:
1. An analgesic composition comprising in admixture an analgesic of the antipyretic type having no narcotic effect and a component to substantially increase the eflectiveness of the analgesic, said component comprising a non-toxic salt of a sympathomimetic amine having the following formula:
cm-cn-cm NHR wherein R is a member of the group consisting of H and CH1.
2. An analgesic composition according to claim 1, characterized by the fact that the analgesic and the non-toxic salt of a sympathomimetic amine are in proportion on the basis of 0.1-1.0 gm. of analgesic to 25-10 mg. of non-toxic salt of asympathomimetic amine.
3. An analgesic composition according to claim 1, characterized by the fact that phenylisopropylamine sulfate comprises the non-toxic salt of a sympathomimetic amine.
4. An analgesic composition according to claim 1. characterized by the fact that phenylisopropylmethylamine sulfate comprises the non-toxic salt of a sympathomimetic amine.
a sympathomimetic amine, th acetylsalicylic and phenylisopropylamine sulfate being in proportion on the basis of 0.1-1.0 gm, of acetylsalicylic acid to 25-10 mg. of amine.
THEODORE B. WALLACE.
REFERENCES CITED The following references are of record in the flle of this patent:
UNITED STATES PATENTS Number Name Date 2,350,318 Shonle et al May 30, 1944 OTHER REFERENCES Gutman, Modem Drug Encyc., 2d ed., N. Y., 1941, pp. 56, 205, .228, 349, 507.
Pharmaceutical Abstracts. 1942, p. 98.
Extra Pharmacopoeia-Martindale, 22d ed.
I (1941) in ,2 vols., vol I, pp. 499 to 502.
Sollmann, Manual Pharmacology, 8th ed., 1942, pp. 613, 615, 621, 622, 626, 830.