WO2006029189A2

WO2006029189A2 - Topical medicament

Info

Publication number: WO2006029189A2
Application number: PCT/US2005/031819
Authority: WO
Inventors: Clyde Morgan
Original assignee: Clyde Morgan
Priority date: 2004-09-08
Filing date: 2005-09-07
Publication date: 2006-03-16
Also published as: AU2005282502A1; US7704522B2; US20060051432A1; GB2432314A; CA2579338C; GB2432314B; US8541034B2; GB0704141D0; AU2005282502B2; US20080069903A1; US20090017138A1; CA2579338A1; US8048447B2; WO2006029189A3

Abstract

New topical medicaments are provided. The medicaments comprise menthol and camphor, preferably provided as part of a base gel, supplemented with potassium and a source of oxygen. The most preferred base gel is sold under the name SOMBRA, while the most preferred source of oxygen is a chlorite (e.g., sodium chlorite) and/or spirulina. The medicaments provide high metabolic activities and sustain those activities over prolonged periods of time, thus being useful for treating a large variety of aliments, including diabetic neuropathy, post hepatic neuralgia, sclerodema, psoriasis, strain, spasticity, headaches, neuropathy secondary to drugs, peripheral neuropathy, leg pain, muscle cramps, muscle aches and pains, bruise, sinusitis, sprain, arthritis, joint pain (arthralgia), and edema.

Description

TOPICAL MEDICAMENT

BACKGROUND OF THE INVENTION Related Applications This application claims the priority benefit of U.S. Provisional Patent Application

No. 60/608,136, filed September 8, 2004, incorporated by reference herein.

Field of the Invention

The present invention is broadly concerned with improved topical medicaments in forms of creams or lotions which are useful in the treatment of a variety of conditions that are ameliorated by increased cell metabolism, circulation, and nerve function. More particularly, the invention is concerned with such medicaments having a gel base with menthol and camphor, and supplemented with potassium and an oxygen source such as an alkali metal chlorite.

Description of the Prior Art

A variety of topically applied creams and lotions have been developed in the past for treatment of conditions such as arthritis and muscle pains. One such product is commercialized under the designation SOMBRA. This product contains 3% menthol and 3% camphor, in a gel base, and is used for the temporary relief of minor aches and pains of muscles and joints associated with simple backaches, arthritis, strains, bruises, and sprains.

However, many prior art creams and lotions do not adequately treat these conditions in most people. Furthermore, even those that are successful do not sustain metabolic activity for extended periods of time, thus making any relief experienced rather temporary. There is a need for new treatments that provide relief for a wide variety of conditions and for extended periods of time.

SUMMARY OF THE INVENTION

The present invention overcomes these problems by broadly providing novel topical medicaments having improved metabolic activity. In more detail, the inventive medicaments comprise menthol, camphor, potassium, and a source of oxygen. The menthol and camphor can be individually added to the composition, or they can be added via a base composition including menthol and camphor. One preferred base composition is a gel sold under the name SOMBRA. Regardless of the delivery source, the menthol is preferably present in the medicament at a level of at least about 0.5% by weight, more preferably from about 2-20% by weight, and even more preferably from about 2-4% by weight, based upon the total weight of the medicament taken as 100% by weight. Furthermore, the camphor is preferably present in the medicament at a level of at least about 0.5% by weight, more preferably from about 2-20% by weight, and even more preferably from about 2-4% by weight, based upon the total weight of the medicament taken as 100% by weight.

The potassium is preferably provided in powder form, and it can be obtained from dietary supplements, for example. One preferred source of potassium is Potassium Chelate (99 mg potency) sold by Nature's Way. Potassium Chelate is provided in the form of a capsule including powder potassium and minor amounts of ground millet. The capsule can simply be opened, and the powder from the capsule used in the present invention. Potassium is preferably present in the medicament at a level of at least about 0.02% by weight, more preferably from about 0.04-0.5% by weight, and even more preferably from about 0.09-0.2% by weight, based upon the total weight of the medicament taken as 100% by weight. When Potassium Chelate or a similar product is used, preferably from about 1-20 capsules, more preferably from about 1-15 capsules, and even more preferably from about 8-13 capsules are used.

The source of oxygen can be any source that is capable of delivering the appropriate levels of oxygen to the medicament. Suitable oxygen sources include those selected from the group consisting of chlorites (and preferably alkali metal chlorites such sodium chlorite and magnesium chlorite), spirulina, and mixtures of the foregoing. The most preferred oxygen source is sold under the name AEROBIC 07, which contains deionized water, sodium chlorite, carbonates, and bicarbonates.

The oxygen source is preferably present in the medicament in sufficient quantities to provide oxygen levels of at least about 0.016% by weight, more preferably from about 0.10-0.85% by weight, and even more preferably from about 0.17-0.25% by weight, based upon the total weight of the medicament taken as 100% by weight. When AEROBIC 07 or a similar product is used, it is preferably added at levels of from about 1-13 drops, more preferably from about 1-10 drops, and even more preferably about 4 drops.

In one alternative embodiment, the medicament also includes a source of chlorine ions. If sodium chlorite is used as the source of oxygen, it will also functions as a source of chlorine ions. Other suitable sources of chlorine ions include any chlorite (e.g., sodium hypochlorite) such as those found in commercially available bleaching agents (e.g., CLOROX, CALIBEX). In these embodiments, the source of chlorine is included in sufficient quantities to provide chlorine ion levels of from about 0.10-10% by weight, and more preferably from about 0.16-0.85% by weight, based upon the total weight of the medicament taken as 100% by weight.

The inventive medicaments can also include a number of optional ingredients, depending upon the final use. Some suitable ingredients include those selected from the group consisting of aloe vera extract, capsaicin, carbomer, decyl plyglucose, deionized water, grapefruit seed extract, green tea extract, orange peel extract, queen of the prairie extract, rose water, silica, sodium hydroxymethyl glycinate, vegetable glycerin, witch hazel, yucca extract, carbonates, bicarbonates, and mixtures of the foregoing. The preferred quantities of these ingredients are set forth in Table 1. These ingredients can be added individually or in a group as part of another composition (e.g., in abase composition such as SOMBRA).

Table 1

^A The percentages by weight are based upon the total weight of the topical medicament taken as 100% by weight.

The inventive medicaments are formed by simply mixing the above ingredients together, preferably in some type of carrier. If SOMBRA is used, then the carrier is provided by that product.

In a particularly preferred preparation method, a precursor composition containing the camphor and menthol is provided. The precursor composition should comprise: from about 1-10% by weight menthol, preferably from about 1-5% menthol, and even more preferably about 3% by weight menthol; and from about 1-10% by weight camphor, preferably from about 1-5% camphor, and even more preferably about 3% by weight camphor, based upon the total weight of the medicament taken as 100% by weight.

The precursor composition can also include some or all of the optional ingredients discussed above. A quantity of the precursor composition is added to a container, along with a portion of the potassium. Further respective quantities of the precursor composition and potassium are then added in alternating steps until the desired quantity as been obtained. The precursor composition and potassium within the container are preferably then mixed until substantially homogeneous (e.g., from about 1-3 minutes, and preferably about 2 minutes). Mixing can be carried out by hand or mechanical mixing means (e.g., mixer, shearing in industrial equipment). The source of oxygen is then added to the resulting mixture and further mixing is carried out. Any optional ingredients that were not already added can then be added to the mixture to yield the final medicament.

The inventive topical medicament is used to treat a portion of the body (human or animal) afflicted with an ailment by simply contacting the medicament with the afflicted portion of the body. The medicament is then preferably rubbed into the skin until it is no longer visible. It will be appreciated that the medicament can be used to treat numerous conditions, including diabetic neuropathy, post hepatic neuralgia, scleroderma, psoriasis, strain, spasticity, headaches, neuropathy secondary to drugs, peripheral neuropathy, leg pain, muscle cramps, muscle aches and pains, bruise, sinusitis, sprain, arthritis, joint pain

(arthralgia), and edema. •

The inventive medicament offers a particularly significant advantage in that it achieves high metabolic activity and maintains that activity over extended periods of time.

"Metabolic activity" as used herein refers to energy (in mV) that is created by the potassium ions in the medicament. That energy is then transferred to the patient at the medicament location on the skin. Though not wishing to be bound by theory, it is believed that the energy excites and thus opens the sodium-potassium pumps in the cells. This stimulates the nervous system and better allows active ingredients to enter the cells.

Metabolic activity is determined by mixing 1 g of a medicament with 0.1 g of a commercially available electrolyte material (e.g., one sold under the name ORAL REHYDRATION SALTS, available from Jianas Bros. Packaging Co.). The mixture is then placed onto an electrogel pad, which is "sandwiched" between two ECG patches connected to a voltmeter. Readings in mV are taken over regular intervals (e.g., 5-minute intervals).

When using the medicaments of the invention, a peak (i.e., highest or maximum) metabolic activity of at least about 2.5 mV, preferably at least about 4 mV, and more preferably from about 4-20 mV is achieved. This peak is preferably achieved within about 30 minutes, and more preferably within about 15 minutes, of application to the afflicted area.

The inventive medicaments also possess the property of having a retained metabolic activity of at least about 20%, preferably at least about 30%, and even more preferably from about 50-100% over a 45-minute time period. Furthermore, the inventive medicaments possess the property of having a retained metabolic activity of at least about 5%, preferably at least about 20%, and even more preferably from about 25-100% over an 8-hour time period. As used herein, "retained metabolic activity" is determined as follows :

metabolic activity after 45 minutes or 8 hours

Retained Metabolic Activity = x 100 peak metabolic activity

BRIEF DESCRIPTION OF THE DRAWINGS

Figure Ia is a graph depicting the metabolic activity of a prior art product over a 45-minute time period; Fig. Ib is a graph depicting the metabolic activity of another prior art product over a 45 -minute time period;

Fib. 1 c is a graph depicting the metabolic activity of the inventive medicament over a 45-minute time period; and Fig. 1 d is a graph depicting the metabolic activity of the inventive medicament over an 8-hour time period.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

EXAMPLES

The following examples set forth preferred methods in accordance with the invention. It is to be understood, however, that these examples are provided by way of illustration and nothing therein should be taken as a limitation upon the overall scope of the invention.

EXAMPLE 1

Preparation of Topical Medicament

A 1 -gallon plastic jug was tared on a Sunbeam Model SP5 top balance (no shield, small pan balance). The jug was then charged with 5.7 oz of SOMBRA Natural Pain Relieving Gel (available from Sombra Inc., Albuquerque, NM).

Thirteen potassium amino acid chelate capsules (99 mg potassium with millet filler; available from Nature's Way, Springville, UT) were emptied three at a time. The filled capsule weight was 0.78 g, the emptied powder weight was 0.67 g, and the empty capsule weight was 0.67 g (n=l). The level of elemental potassium in the capsule was not given on the label.

The powder emptied from the capsules was then added to the SOMBRA in the plastic jug as follows:

(1) The jug was charged with SOMBRA to a weight of 12.1 oz., and the powder from three empty capsules was added; (2) The jug was charged with SOMBRA to a weight of 1 Ib. 6.1 oz., and the powder from three empty capsules was added;

(3) The jug was charged with SOMBRA to a weight of 2 Ib. 3.9 oz., and the powder from the remaining empty capsules was added; and (4) The jug was charged to a final weight of 3 Ib. 1 oz. with SOMBRA.

A cap was placed on the jug, and the jug was shaken by hand for about 2 minutes to substantially evenly distribute the powder. The gel did not adhere to the plastic jug after the potassium amino acid chelate was added.

AEROBIC 07 (a dietary supplement including deionized water, sodium chlorite, carbonates, and bicarbonates; available from Aerobic Live, Phoenix, AZ) was used as a stabilized source of oxygen. Thirteen drops of the Aerobic 07 were added to the plastic jug containing the SOMBRA-potassium amino acid chelate mixture. The jug was again capped and shaken by hand for about 2 minutes to yield the final topical medicament. The final medicament was more viscous than the SOMBRA gel. When comparing a quantity of each, the compounded medicament did not separate or flow as compared to the

SOMBRA gel, which showed some physical separation.

EXAMPLE 2 Treatment of Patient A 1. Patient History

The topical medicament prepared in Example 1 was used to treat a patient (hereinafter referred to as "Patient A"). Patient A was a Caucasian female in her 60s, and she was 57" and approximately 220 Ib. Patient A exhibited neuropathy of the legs and feet, with the left leg being worse than the right. Patient A's big toe on her right foot and second toe on her left foot were amputated within the preceding 3 years due to diabetes.

She had received angioplasty about 9 months prior, and the angioplasty improved blood flow to her lower extremities.

Both legs below the knees presented open sores about half-way between the knee caps and ankles. The sores were worse on the right leg than the left. She had used Bactroban and Betadine to treat the topical sores for infection. Patient A also had an ulcer on the bottom of her right foot. She had begun a second, 2-3 week treatment course of Regranex, applying at bedtime. Previous use of Regranex had worked, but the ulcer recurred, so she then had surgery. She began to use Etherex, which she stated is a generic medicine for Regranex and Bactroban. Her daily medications are shown in Table A-B.

Table A

Table B

Patient A also reported using Walitin (generic for Claritin) and Nasonex as needed for allergies.

2. Treatment with Inventive Topical Medicament

The ambient temperature during treatment ranged from 74-78°F according to measurements from four different Stress Thermometers used "as is" (Dr. Lowenstein's Model SC911 accuracy +/- 1.8°F, 10 ft. lead with fast temperature sensor).

Patient A was recumbent on a treatment table with a triangular pillow positioned behind both knees so that the knees were bent upward to rise above the ankles. A temperature probe was strapped on each upper ventral thigh and on the inside of each ankle. The probes were covered, and no medicament was applied to the probes. Equilibration time was approximately 10 minutes after the patient reclined in the prone position. After equilibration time was reached, the temperatures were recorded as shown in Table C.

Table C

The inventive medicament was applied to the top and bottom of each thigh and later (as shown in Table D) to the top and bottom of each calf, ankle, and foot. The product was massaged into the skin until nearly invisible to the eye. The dosage level was 0.3 oz. on each thigh and each ankle for a total per leg dosage of 0.6 oz.

Temperature readings were taken at intervals, beginning 5 minutes after application to Patient A's legs. These readings are set forth in Table D.

Table D

Five minutes after application to left calf and lower thigh (0 time).

Patient A rose from the table at 78 minutes, and the thigh probes were removed. Patient A held the readout portion of the thermometers in her hand while the probes were still attached to the ankles to allow her to walk to the restroom and take a further readout of her ankles after 5 minutes elapsed. However, at 82 minutes the left ankle probe came loose so no reading was taken. The right ankle probe gave a reading of 81.1⁰F at 82 minutes. Patient A reported that her left side (neuropathic side) felt soothed.

EXAMPLE 3 Treatment of Patient B

1. Patient History

The topical medicament prepared in Example 1 was used to treat a second patient

(hereinafter referred to as "Patient B"). Patient B was a 60-year old, 57", Caucasian female. She was a non-insulin dependent diabetic and had sensory neuropathy that was worse in her right leg. She did not have any visible wounds. Her daily oral medications were Glucophage (1 in the evening), Toprol, Diovan, and Lipitor (1 in the evening). 2. Treatment with Inventive Topical Medicament

The ambient temperature during treatment ranged from 74-75⁰F according to measurements from the four different Stress Thermometers as described in Part 2 of Example 2. The probes were applied as described in Part 2 of Example 2. The initial readings are shown in Table E.

Table E

^A Temperature prior to medicament application.

^B The probe came loose from the right thigh, thus resulting in the 79°F reading. ^c Temperature at 4 minutes after temperature reading in middle column.

Temperature readings were taken as described in Part 2 of Example 2. These readings and the times of medicament application to Patient B's legs are set forth in Table F.

Table F

^A Five minutes after first temperature reading in Table E.

The probes were removed after 70 minutes. EXAMPLE 4

Determination of Metabolic Activity

The topical medicament prepared in Example 1 was applied to the left inner forearm (below the elbow) of a patient. The treated area was then swabbed with a glass slide that was subsequently sandwiched between two ECG patches attached to leads to a Radio Shack digital, multi-meter. The initial reading (time = 0) was 0.0 mV. Subsequent readings were taken at different intervals, and those results are reported in Table G.

Table G

This test was carried out to show that oxygen activation from the compounded medicament occurs following the application to human skin with or without sweat.

This test was repeated using medicament that had been swabbed from another patient's back. However, the cream turned green in color and did not reproduce similar results with the ECG patches. It also took about 6 hours and 20 minutes for this person to notice the heat activation in the location where the medicament had been applied to the back. EXAMPLE 5

Metabolic Activity Comparison

In this test, the metabolic activity of the topical medicament prepared in Example 1 was determined following the steps set forth in Example 4. The same steps were followed to determine the metabolic activity of two prior art products. Fig. Ia shows the metabolic activity of one prior art product (non-modified SOMBRA) over a 45-minute time period. Fig. Ib shows the metabolic activity of another prior art product (non- modified BIO-FREEZE) over a 45-minute time period. Fig. Ic shows the inventive medicament's metabolic activity over a 45-minute time period. A comparison of these figures shows that metabolic activity of the prior art peaks and then drops substantially over the 45-minute time period while the inventive medicament's metabolic activity maintains very high levels even after peaking. Fig. Id shows the inventive medicament's metabolic activity over an 8-hour time period. This graph shows that this activity drops slowly over the 8-hour time period, thus providing prolonged treatment periods as compared to prior art products.

EXAMPLE 6

Treatment of Patient with Inventive Topical Medicament The patient in this example (hereinafter referred to as "Patient C") was a Caucasian female in her late 50s. Patient C was suffering from neuropathy in her feet, with symptoms including sharp, stabbing pains and contractures due to over-stimulation of muscles. The condition had caused Patient C to take disability from work.

The topical medicament prepared in Example 1 was applied to Patient Cs feet.

Within 10 minutes, the contractures in her feet started to release, and she reported that her feet felt 90% better. Also, the sharp, stabbing pain was relieved for 6 hours after treatment.

Claims

I Claim:

1. In a topical medicament comprising menthol and camphor, the improvement being that said medicament further comprises potassium and a source of oxygen.

2. The medicament of claim 1 , wherein said medicament is in the form of a gel.

3. The medicament of claim 1 , wherein said source of oxygen is selected from the group consisting of chlorites, spirulina, and mixtures of the foregoing.

4. The medicament of claim 3, wherein said source of oxygen is an alkali metal chlorite.

5. The medicament of claim 1 , wherein said medicament comprises: at least about 0.5% by weight menthol; at least about 0.5% by weight camphor; at least about 0.02% by weight potassium; and sufficient quantities of said oxygen source to provide at least about 0.016% by weight oxygen, based upon the total weight of the medicament taken as

100% by weight.

6. The medicament of claim 1 , wherein said medicament further comprises an ingredient selected from the group consisting of aloe vera extract, capsaicin, carbomer, decyl plyglucose, deionized water, grapefruit seed extract, green tea extract, orange peel extract, queen of the prairie extract, rose water, silica, sodium hydroxymethyl glycinate, vegetable glycerin, witch hazel, yucca extract, carbonates, bicarbonates, and mixtures of the foregoing.

7. The medicament of claim 1, wherein said medicament has a retained metabolic activity of at least about 20% over a 45-minute time period.

8. The medicament of claim 1, wherein said medicament has a retained metabolic activity of at least about 5% over an 8-hour time period.

9. A method of treating a portion of a body afflicted with an ailment, said method comprising the step of contacting a medicament with the portion of the body afflicted with the ailment, said medicament comprising menthol, camphor, potassium, and a source of oxygen.

10. The method of claim 9, wherein said contacting step comprises rubbing said medicament into the portion of the body afflicted with the ailment.

11. The method of claim 9, wherein said medicament is in the form of a gel.

12. The method of claim 9, wherein said source of oxygen is selected from the group consisting of chlorites, spirulina, and mixtures of the foregoing.

13. The method of claim 12, wherein said source of oxygen is an alkali metal chlorite.

14. The method of claim 9, wherein said medicament comprises: at least about 0.5% by weight menthol; at least about 0.5% by weight camphor; at least about 0.02% by weight potassium; and sufficient quantities of said oxygen source to provide at least about 0.016% by weight oxygen, based upon the total weight of the medicament taken as 100% by weight.

15. The method of claim 9, wherein said medicament further comprises an ingredient selected from the group consisting of aloe vera extract, capsaicin, carbomer, decyl plyglucose, deionized water, grapefruit seed extract, green tea extract, orange peel extract, queen of the prairie extract, rose water, silica, sodium hydroxymethyl glycinate, vegetable glycerin, witch hazel, yucca extract, and mixtures of the foregoing.

16. The method of claim 9, wherein said medicament has a retained metabolic activity of at least about 20% 45 minutes after said contacting step

17. The method of claim 9, wherein said medicament has a retained metabolic activity of at least about 5% 8 hours after said contacting step.

18. A method of preparing a topical medicament, said method comprising the step of mixing together menthol, camphor, potassium, and a source of oxygen.

19. The method of claim 18, wherein said method further comprises the steps of:

(a) providing a precursor composition comprising said menthol and camphor;

(b) adding said potassium to a quantity of said precursor composition to yield a first intermediate composition;

(c) alternately adding further quantities of said precursor composition and said potassium to said first intermediate composition to form a second intermediate composition; and

(d) adding said source of oxygen to said second intermediate composition to yield the topical medicament.

20. The method of claim 19, further comprising the step of mixing said second intermediate composition prior to adding step (d).