U.S. patent number 3,705,239 [Application Number 05/081,555] was granted by the patent office on 1972-12-05 for pain removing compositions and methods.
Invention is credited to Roy B. Gregory.
United States Patent |
3,705,239 |
Gregory |
* December 5, 1972 |
PAIN REMOVING COMPOSITIONS AND METHODS
Abstract
Pain removing compositions for external use on warm blooded
animals. A pain removing composition is made from acetic acid,
urea, ammonium hydroxide, glycerol, and water and may be used with
plastiquinone A in a solvent. A binder may be used to tie the
components together. A binder contains lanolin, stearic acid,
water, triethanolamine and mineral oil. When rubbed on an external
part of an affected area of a warm blooded animal, pain is removed
in a short period of time.
Inventors: |
Gregory; Roy B. (Lafayette,
IN) |
[*] Notice: |
The portion of the term of this patent
subsequent to December 7, 1988 has been disclaimed. |
Family
ID: |
22164910 |
Appl.
No.: |
05/081,555 |
Filed: |
October 16, 1970 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
Issue Date |
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820311 |
Apr 29, 1969 |
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Current U.S.
Class: |
424/719 |
Current CPC
Class: |
A61K
33/02 (20130101); A61K 33/02 (20130101); A61K
9/0014 (20130101); A61K 33/02 (20130101); A61K
31/047 (20130101); A61K 31/19 (20130101); A61K
2300/00 (20130101); A61K 31/17 (20130101) |
Current International
Class: |
A61K
33/02 (20060101); A61K 47/00 (20060101); A61k
027/00 () |
Field of
Search: |
;424/195,332,322,168,317,166 |
Other References
Chem. Abst., 55 21276G (1961)..
|
Primary Examiner: Friedman; Stanley J.
Parent Case Text
CROSS REFERENCES TO RELATED APPLICATIONS
This application is a continuation-in-part of application Ser. No.
820,311 Filed Apr. 29, 1969 by Roy Gregory with title PAIN REMOVING
COMPOSITION AND METHODS.
Claims
What is claimed is:
1. A process for the manufacture of a pain removing composition
which comprises with percentage by volume diluting from 2.9 to 4
percent of acetic acid with a small amount of water to allow
ionization, adding to the acetic acid from 3.75 to 5 percent of
urea, after the urea has dissolved, adding from 4.5 to 6 percent of
26 percent ammonium hydroxide, to the dissolved urea, then adding
from 3 to 6 percent of glycerol and adding water to make 100
percent.
2. A pain removing composition as is produced by the method of
claim 1.
3. A process for making a pain removing composition comprising
making a binder by mixing together at about 180.degree. to
212.degree. F by volume 14 to 18 percent lanolin, about 3 to 6
percent water and about 1 to 2 percent triethanol amine, upon
cooling 9 to 12 percent mineral oil is added along with sufficient
water to make 100 percent, mixing 1 to 20 percent of this binder
with 3 to 90 percent of 5 percent plastiquinone A in heptane and
with 8 to 96 percent of the composition produced by the method of
claim 1.
4. A method for treating pain which comprises external application
to a patient of the composition produced by the process of claim 1.
Description
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention is concerned with medicinal products of the pain
remover type. More specifically this invention is concerned with
external pain removers for use on warm blooded animals. The pain
removers of this invention are particularly suited for use on
humans.
2. Description of the Prior Art
Pain removing compositions for external use are generally known in
the prior art. Most of the prior art compositions contain
ingredients which when applied to the surface of a warm blooded
animal causes the area to feel hot or cold. These compositions
generally change the flow rate of blood to the affected area.
Common components in these prior art compositions are capsicum,
chloroform, menthol, methyl salicylate, turpentine, camphor, oil of
mustard, aspirin, narcotics, etc.
While the compositions and methods of the subject invention are
similar to the above described prior art in that they are applied
externally, their action is totally different because they do not
draw more blood to the area in question or change the flow rate of
blood in any manner.
Other prior art methods include massage, light rays, swirl baths,
ultra sonic sound waves, etc. While these additional prior art
methods bring some relief, they are disadvantageous in that they
are time consuming and they are expensive.
Generally, it could be said that the prior art compositions and
methods are slow to act and are only capable of rendering temporary
relief. In contrast the present invention functions in a short
period of time and it is capable of rendering relief which lasts
for an extended period of time. It may be of interest to note that
this invention also removes the pain and swelling due to injury or
pain due to bursitis without any sensation that the pain and
swelling is being removed.
SUMMARY OF THE INVENTION
The invention is concerned with pain removing compositions for
external use on warm blooded animals, methods of removing pain, and
methods for the manufacture of the compositions. A pain removing
composition is made from acetic acid, urea, ammonium hydroxide,
glycerol and water. Plastiquinone A in a solvent may also be used
in conjunction with the composition for prolonging the pain
removing effect. A perfume can be added to cover the medicinal odor
of the pain removing composition.
DESCRIPTION OF THE PREFERRED EMBODIMENT
The pain remover of this invention is for external use on warm
blooded animals. The compositions of this invention are
specifically meant to be a pain remover and not a cure. This
invention is for pain in muscle due to injury or contusions of
external origin and pain in muscle caused by bursitis.
In contrast this invention is not for pain due to disease or pain
due to internal disorder of vital parts of the body.
The subject composition generally has a composition in accordance
with the percentages by volume as are specified in Table I.
TABLE I
Acetic Acid (100%) 2.90 - 4% Urea (U.S.P.) 3.75 - 5% Ammonium
Hydroxide (26%) 4.5 - 6% Glycerol (U.S.P.) 3 - 6l % Water
Balance
A preferred composition in accordance with this invention is set
forth in Table II.
TABLE II
Acetic Acid (100%) 3. 33 % Urea (U.S.P.) 4. 18 % Ammonium Hydroxide
(26%) 5. 00 % Glycerol &U.S.P) 3. 33 % Water 84. 16 % 100. 00
%
The composition of this invention is generally prepared by diluting
the acetic acid component with a small amount of water. To this
diluted acetic acid is added the urea, which dissolves after
shaking for a short period of time. The ammonium hydroxide is then
added and then the glycerol. The glycerol disperses with vigorous
agitation. The remainder of the water is added to produce a
composite system. This composite system alone is effective in
reducing pain.
It has been found that pain from some causes is only temporarily
relieved with the composite system but may be permanently relieved
with the additional use of plastiquinone A. The plastiquinone A may
be produced by extracting finely divided fresh spinach chloroplast
with a solvent for plastiquinone A for 12 hours. Heptane is the
preferred solvent; however methanol, ethanol, acetone and petroleum
ether are known solvents for plastiquinone A. Obviously the solvent
chosen would have to be one which would not be harmful when applied
externally.
The various solvents used would extract other compounds from the
spinach but the other compounds would not be harmful or interfere
with the pain reliever and may merely be left in the solvent. When
heptane is used as a solvent with moist spinach leaves, a yield of
5 percent plastiquinone A by weight in the Heptane is obtained.
This is what is used in this invention. If the spinach is first
freeze dried, the yield increases to 10 percent by weight. These
spinach extracts work just as effectively as do similar percentages
of pure plastiquinone A in pure heptane and are less expensive.
For best results the plastiquinone A is either applied concurrently
with or after application of the composite system. While any
non-harmful solvent may be used to apply plastiquinone A after the
pain reliever (composite system) has been applied, certain problems
may occur in applying the two simultaneously. When heptane is the
solvent, the heptane and the composite system are immiscible and
thus must be vigorously shaken before use.
Binders may be added to slow down or prevent the separation of the
two immiscible mixtures. A binder for use in this invention is
preferably prepared by mixing together at about 200.degree.F by
volume about 16 percent lanolin, about 4 percent stearic acid,
about 4 percent water and about 1 percent triethanolamine, upon
cooling about 11 percent mineral oil is added along with sufficient
water to make 100 percent.
The binder may be prepared by mixing together at about 180.degree.
to 212.degree. F by volume about 14 to 18 percent lanolin, about
31/2 to 5 percent stearic acid, about 3 to 6 percent water and
about 1 to 2 percent triethanol amine, upon cooling 9 to 12 percent
mineral oil is added along with sufficient water to make 100
percent.
Acceptable ranges of ingredients are by volume 5% plastiquinone A
in heptane 3-90 percent, binder 1-20 percent, and composite system
8-96 percent. Preferred percentages are by volume 5 percent
plastiquinone A in heptane 4 percent, binder 2 percent, and
composite system 94 percent.
When a binder is not used, mineral oil may be added to the heptane
to prevent rapid drying on the surface of the skin. The amount used
is not at all critical but generally about 3 percent mineral oil by
volume is preferred. When a lanolin base hand or facial cream is
added (about 10 to 50 percent volume) to the plastiquinone A in
heptane a similar result is achieved.
The invention has a high concentration of each component in a small
amount of solvent. This arrangement is advantageous because it does
not allow each component to combine with other components
completely, leaving some of each in a free or uncombined state. The
free or uncombined molecules are necessary to react with the
organic acids in the pain affected muscles to change these organic
acids into products which the natural body metabolism can
assimilate.
In addition to removing pain the subject composition is useful as a
means of locating the exact point of injury. For example, when an
entire arm and shoulder area hurts, a doctor cannot find the exact
point of injury. Using this invention, a doctor can pin-point the
exact point of injury in 45 minutes. The point of injury itself
will remain tender to the touch. The doctor can then proceed with
proper treatment to a speedy recovery. This is to be contrasted
with the present methods employed by doctors which is to immobilize
the arm and shoulder in a plaster cast and administer pain pills
for relief. Sprains are immobilized and are soaked in hot packs or
ice packs to reduce pain and swelling. The present invention makes
these procedures unnecessary.
The composition of this invention functions by aiding in the rapid
assimilation of the organic acids which are concentrated in the
affected area and are responsible for the sensation of pain.
Pain caused by injury is due mainly to a high concentration of
oxalic, lactic and amino acids that radiate outward from point of
injury. This invention will act on and react with these pain
causing acids in the muscle changing these acids into non-harmful,
non-painful products which the body metabolism can assimilate and
move out very quickly. The oxalic and lactic acids are quickly
changed by the subject composition into amines and are eliminated
with this group.
Likewise, the composition of this invention causes an amino acid to
inhibit the activity of one of the early enzymes in its pathway. It
quickly releases this inhibitor, restricts an oversupply of amino
acids, unblocks their biosynthetic pathway and regulates their
accumulation.
Finally, the subject composition increases protein synthesis
allowing these acids to move out of affected area by natural body
metabolism.
Injury due to accidents causes a build up of organic acids in
muscles which slows down protein synthesis causing a surplus of the
19 other amino acids each of which shuts off its own biosynthetic
pathway and thus contributes to a build up of intermediary
catabolites which are corepressors of catabolic enzymes. Amino
acids have the ability to inhibit the activity of one of the early
enzymes in its biosynthetic pathway. Reduce the supply of amino
acids by a factor or two, this reduction quickly releases this
inhibition. Beginning 5 to 10 minutes after the shift down in amino
acid supply, a marked depression of the enzyme concerned with the
biosynthesis of the restricted amino acid occurs as a result of a
reduced intracellular concentration of a repressing derivative of
the amino acid. A near total repression of many catabolic enzymes
begins within a few minutes of the amino acid shift down. The
rapidity of response indicates this occurs independently of any
long term affect of amino acid restriction such as reduced enzyme
level. Protein synthesis and biosynthetic enzyme repression require
the interaction of the amino acid with the same specific aminoacyl
synthetase.
This invention has the ability to reduce an amino acid supply,
inhibit an enzyme, unblock their biosynthetic pathway, regulate
their accumulation. Increase protein synthesis cause these acids to
be removed by natural body metabolism. Observation has shown that
active acetate identified now as acetyl coenzyme A is involved in
synthesis of fatty acids. Coenzyme A acts as a carrier not only for
acetyl but for other acyl groups. The urea molecule reacts with
these various acids with the help of ammonia and acetyl to change
these acids into amines. The glycerol acts as a hydrogen and
hydroxyl acceptor. Plastiquinone A activates coenzyme Q.
Coenzyme Q is located within the lipoprotein membrane of system of
cells. Its activity is necessary for proper functioning of cells.
Pain due to injury or irritation in muscle due to bursitis causes
this enzyme to become dormant. The activity and function of
coenzyme Q is necessary in the stringent cells to return these
cells to normal structure and function. Plastiquinone A will
activate coenzyme Q and keep it working. Plastiquinone A acts as an
electron transport system to transport energy through the cells
farther away than next to or adjacent to each cell. There is a pool
of quinone between the two sites to transfer energy from the site
where electron flow occurs to the site where energy is used.
Plastiquinone A undergoes rapid oridation and reduction during the
electron transport process. Coenzyme Q undergoes rapid oxidation
and reduction to account for the main unilateral electron transfer
of protons and hydroxyl ions. As a result of this additional action
pain and swelling does not return.
The following examples will illustrate the subject invention. These
examples are given for the purpose of illustration and not for
purposes of limiting this invention. The data for Examples 1 to 49
is listed in Table III. In these examples the dosage was rubbed
externally on the affected area of the body. It can be seen from
these examples that in a short period of time the pain in the
affected area was removed and the relief lasted for an extended
period. In the table under the Dosage column the letter P
represents the use of the composite system (formed from acetic
acid, urea, ammonium hydroxide and glycerol). The letter Q
represents the use of 5 percent Plastiquinone A containing spinach
extract with heptane as the solvent. The letter B indicates the use
of a binder and the "+" separates ingredients when a two solution
form was used. "m" represents the use of mineral oil and "1"
represents the use of a lanolin base face cream. ##SPC1## ##SPC2##
##SPC3## ##SPC4## ##SPC5## ##SPC6##
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