Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ortho-hydroxybenzoic acid or derivative doai
Reexamination Certificate
2000-12-19
2001-06-19
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ortho-hydroxybenzoic acid or derivative doai
Reexamination Certificate
active
06248731
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to using potassium hydroxide, KOH, to stabilize acetylsalicylic acid, ASA, salicylic acid, SA, and any other related composition and ascorbic acid for oral and topical use.
2. Discussion of the Related Art
U.S. Pat. No. 1,349,207 to Galat discloses the use of alkaline solvents to stabilize aspirin compositions in solution and describes salicylic acid and acetic acid as undesirable byproducts of the breakdown of acetylsalicylic acid (ASA). To avoid this breakdown of ASA, anionic exchange materials are used. Galat articulates the general assumption that, in order to stabilize aspirin, one must begin with ASA.
Salicylic acid (SA) is closely related to salicin, the earliest form of aspirin found in white willow bark, meadowsweet and other botanicals. American Indian tribes used it in therapeutic baths and teas, as did early Americans. The botanicals are still sold in certain health food stores and used in the same way.
Potassium Hydroxide (KOH) has been used as a stabilizer for Aspirin in Solution. In one patent, KOH was used as a catalyst in the processing of Aspirin. In U.S. Pat. No. 3,279,990 to Rose et al., U.S. Pat. No. 1,217,862, to Gerngross, U.S. Pat. No. 4,228,162, to Luzzi et al., and U.S. Pat. No. 4,885,287, to Hussain et al., sodium hydroxide is used to stabilize an aspirin in solution; however, the high sodium content was, and is, undesirable. In the patent to Luzzi et al., it is noted that the stability of aspirin in a solution increases with increasing concentration of the drug. Using dimethyl isosorbate as a solvent, the patent achieves a concentration of 280 mg of ASA/ml.
In the past, KOH was used to restore electrolytes in animals in veterinary practice. It also is used in solution to saponify vegetable oils in the making of castile soap.
Examination of the properties of ascorbic acid and salicylic acid suggests that the therapeutic action, acidity, antiseptic quality, historical range of uses, and even side effects when separated from its original plant source, as well as the manner in which it deteriorates by esterification, of salicylic acid resembles vitamin C. Also, vitamin C is a detoxifier.
Earlier cultures have used whole plant forms of salicin as a remedy for food poisoning and dysentery, suggesting a possible detoxifying role for SA. Although aspirin, as we know it, may injure the gastrointestinal tract, teas from plants containing salicin were used for healing it.
Studies at Cornell University about how plants create SA which prevents microbes from causing disease in them suggest a unique role for SA, other than as a drug. If SA functions as an agent which combines with excess wastes or undesirable substances, including microbes in the body, and carries them off through circulation without leaving toxic traces of its own, then like ascorbic acid, SA may qualify as a detoxifier. If it is not simply a drug but a detoxifier, its role in health could become therapeutic or healing rather than simply medicinal.
A problem persists, however, in stabilizing solutions of ASA or SA which would allow effective oral and/or topical application of such drugs for either medicinal or therapeutic uses. When mixed in water, such substances rapidly biodegrade and become unsuitable for use.
In view of the foregoing, there remains a need to prolong the stability of an aspirin or aspirin-like product, ASA and SA, in a soluable state in a water base solution for purposes of obtaining a medicinal drug, and possibly a therapeutic detoxifer, which can be administered both orally and topically and which will exhibit a commercially and medically acceptable shelf life.
SUMMARY OF THE INVENTION
Salicylic acid, SA, and Acetylsalicylic Acid, ASA, are dissolved in solutions of potassium hydroxide, KOH, to form potassium salicylic acid (KSA) and potassium acetylsalicyclic acid (KASA). In some embodiments, dehydration shortly after mixing in solution and while the liquid is still hot from its own chemical reaction reduces the biodegradation which sometimes occurs when water is present with SA and ASA.
The more concentrated the KOH solution is, the more SA or ASA that dissolves and the less the chance for degradation. A solution at or close to its saturation point for SA and ASA remains liquid upon cooling. On the other hand, a supersaturated solution remains liquid only while it is still hot and lends itself to rapid dehydration immediately after the solids are thoroughly dissolved. This manner of facilitating the drying process overcomes the problem of SA's and ASA's resistance to giving up moisture in dehydration.
Making a preferably alkaline formula of KSA and KASA at maximum concentration, limited by a desired pH, is desirable and the resultant formula is diluted for use. The pH values should be within optimal range and are related to the body's physiological well-being or the preference or need of different body systems, e.g., the GI tract, the skin.
The pH of an oral formula should be in the range of 8-10. This pH counteracts excess acidity and soothes the gastrointestinal(GI), tract.
Finding a high dose aspirin without GI side effects is probably the main reason why a new more gentle form of aspirin has been sought for nearly a century. The alkaline formulas of the present invention permit higher doses and have powerful yet soothing systemic effects. The importance of this is that many small doses do not achieve the same result as one large dose.
In the preferred embodiment for oral alkaline formulas, approximately two parts by weight SA or ASA is dissolved with one part KOH in a water base KOH solution. The solution chemically reacts until the substances are fully soluabilized as potassium KSA or KASA. A resultant pH of about 12-13 is achieved. For administration, the pH is lowered by diluting the KSA or KASA in water to a pH of between 8 and 10.
In a preferred embodiment for topical application, a water based, preferably aloe vera gel, lotion or cream is mixed and combined with dehydrated KSA. The pH of the resultant topical lotion is approximately 4.62.
In some embodiments the liquid KSA and KASA formulations are rapidly dehydrated by heating before the liquid formulation cools from the initial mixing to thereby reduce biodegration of the resultant anhydrous KSA or KASA. The anhydrous KSA or KASA can subsequently be dissolved in water for oral administration or mixed with a carrier for topical applications.
It is a primary object of the present invention to prolong the stability of an aspirin or aspirin-like product, which stabilized product can be taken orally or applied topically when mixed with a suitable carrier.
It is another primary object of the present invention to provide an aspirin formulation which can be used to permit higher doses of SA and ASA to be administered orally for substantially all known uses of aspirin without the adverse side affects currently present in aspirin products.
It is also an object of the present invention to provide aspirin formulations which may be applied topically to provide treatment and relief from insect bites, bee stings, sores, burns, rashes, itching from poisonous botanicals, funges and the like.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The present invention is directed to methods of stabilizing aspirin and aspirin-like compounds, ASA and SA, for oral and topical medicinal and therapeutic uses wherein greater doses of ASA and SA can be safely administered for both human as well as animal treatment. In order to prevent degradation of the ASA, SA, it has been determined that these compounds can be chemically reacted with potassium hydroxide, KOH, in proper proportions and under conditions which result in an alkaline pH in the range of 8 to 10 for oral administration and an acid pH between 4-5 for topical administration.
Through testing it has been determined that the concentration of KOH in solution should be as high as possible while still obtaining a complete chemical reaction to convert all ASA or SA to KASA or KSA. A solution which is at o
Dowell & Dowell
Henley III Raymond
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