Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-12-04
2002-05-21
Geist, Gary (Department: 1623)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S570000
Reexamination Certificate
active
06391886
ABSTRACT:
TECHNICAL FIELD
The present invention is for oral compositions containing therapeutic agents that generally have undesirable consumer aesthetics. Such compositions include compositions in a variety forms including liquids and solids comprising pharmaceutical actives. The liquid compositions include, but are not necessarily limited to elixirs, syrups, liquid-filled chewable capsules, suspensions, sprays, and suspensions.
BACKGROUND OF THE INVENTION
Stimulation of the nerves in the mouth takes place when flavors or chemical substances are readily available to stimulate these nerves. Oral compositions containing therapeutic agents such as pharmaceutical actives frequently contain disagreeable tasting or unpalatable components. These compositions are taken by mouth and frequently are designed to deliver the agent into the blood through the mucosa of the intestinal tract. These formulations are not intended to deliver their therapeutic agents through the mucosa of the mouth and esophagus. Such compositions are made to taste as good as possible in order to improve the patient compliance. This is usually done by using a sufficient level of sugar/syrup and, or sweeteners, and flavors to mask negative product taste. The medicines may optionally be administered in a volume wherein the therapeutic agent is diluted sufficiently to avoid the poor taste of such.
It is possible, however, to prepare formulations that are intended to deliver substantial portions of the therapeutic agent through the intra-oral mucosa. One problem associated with doing this is that the therapeutic agents can cause very strong negative sensory perceptions in the mouth due to their delivery through the mucosa. These perceptions are undesirable and are often so objectionable that a patient stops taking the medicine that might otherwise give them a desired health benefit. In such cases, the use of conventional sweetener/flavor approach is not sufficient to mask or hide these negative perceptions.
Sweeteners and coolants, both are sufficiently well known for use in medicines for improving consumer acceptance. For example, U.S. Pat. Nos. 4,822,597 and 4,853,212, both to Faust, issued 4/18/89 and 8/1/89 respectively, disclose chewing gums delivering anesthetics to numb irritated areas of the throat; incorporated herein by reference. These patents disclose peppermint and menthol and water-soluble sweeteners, extractable sweeteners and, or artificial sweeteners. U.S. Pat. Nos. 5,725,865 and 5,843,466, both to Mane, issued 3/10/98 and 12/1/98 respectively, disclose coolant compositions comprising mono menthyl succinate and its salts intended to mitigate bitterness attributable to known coolant compounds. Such compositions utilize flavoring syrups containing the natural sugar sorbitol; incorporated herein by reference. U.S. Pat. No. 5,009,893, Cherukuri et al, issued 4/23/91 discloses using menthol in combination with N-substituted p-methanecarboxamide compounds as coolant compositions in edible products; incorporated herein by reference. U.S. Pat. No. 5,451,404, Furman, issued Sep. 19, 1995 discloses coolant compositions comprising a ketal and a secondary coolant that are useful in toiletry foodstuffs, beverages or tobacco compositions; incorporated herein by reference.
Compositions containing therapeutic agents that are formulated to be absorbed through the oral mucosal tissue can produce strong irritation. Irritation as discussed in this application is defined as a singular or combined perceived sensations produced upon the therapeutic agent in sufficient concentration contacting the oral mucosal tissues. These sensations include prickling of the tissue similar to that experienced when the tongue comes into contact with sharp flavors or highly carbonated liquids such as club soda. Additionally irritation as used herein includes the non-thermally generated burning sensation upon contacting mucosal tissue. An example of the burning sensation is the sensation upon eating hot peppers or consuming liquors containing a high level of alcohol. Finally as used herein, irritation includes a tissue-numbing sensation. By tissue-numbing, or simply “numbing”, it is meant that there is an absence of feeling much like that when oil of cloves is applied to a sore area of the mouth.
The levels of sweetener and coolant as normally used in the art will not generally provide enough relief of bitterness associated with the agent and the objectionable irritation mentioned above. When used in levels high enough to combat the bitterness attributed to such agents, the sweeteners themselves impart a bitter, metallic or other objectionable taste to the composition. If the coolant level is raised to levels high enough to combat the irritation caused by the agent, a burning sensation often results. There remains a need then to develop formulations that while delivering actives for oral mucosal absorption strong negative local effects are significantly reduced.
SUMMARY OF THE INVENTION
The present invention is for oral compositions comprising therapeutic agents, particularly those intended to be primarily delivered through oral mucosal tissue. These compositions comprise a combination of sweeteners and coolants wherein the irritation association with the composition's therapeutic agent or agents contacting mucosal tissue is substantially mitigated. Surprisingly it has been discovered that through there is a synergistic effect using high levels of both sweetening agents or sweeteners and cooling agents or coolants, both being undesirable when used alone at the levels attributed to the combination of the present invention. Mitigating irritation attributed with the therapeutic agent while creating compositions that taste good improves patient or user compliance to prescribed or recommended therapies that include consumption of such therapeutic agents.
DETAILED DESCRIPTION OF THE INVENTION
It is known to those skilled in the art that sweeteners, particularly artificial sweeteners used at high levels result in the composition having a bitter, metallic or other objectionable. Likewise coolants at high levels high result in the composition producing other forms of irritation such as burning, or headaches similar to those when eating frozen dessert such as ice cream or consuming highly iced beverages such as shushes. One skilled in the art would expect that using high levels of both coolant and sweeteners to mitigate the negatives associated with therapeutic agents would not produce a consumer-desirable composition. Surprisingly, however, when these components are combined in a composition containing therapeutic agents, there is a dramatic improvement in terms of the consumer-noticeable aspects of such a composition. The irritation of the mucosal tissue due primarily to the therapeutic agent including burning, prickly feel, numbing and other penetrating effects are dramatically reduced to a point wherein the consumer does not find such a composition objectionable. There is very little or no perceptible bitter, metallic or other objectionable taste associated with the sweetener and, or coolants.
Therapeutic Agents
Without being restricted to theory, the applicants believe that at high concentrations, the therapeutic agents delivered to the oral mucosal membranes lead to activation of a number of non-specific afferent neural pathways leading to the brain. Inducing histamine release from mast cells within the mucosal membranes are thought to induces sensations that include burning, prickling and itching of the oral tissue in the mouth. These histamines and other neurotransmitters, or the therapeutic agent itself may cause a large stimulation of the nerve fibers called nociceptors (or pain receptors) within the mucosal membranes. This results in chemical burning pain. Nociceptors and pain sensation are described in
Principles of Neuroscience
, E. R. Kandel, J. H. Schwartz, T. M. Jessel editors, p. 442, McGraw Hill, 4
th
edition, 2000; herein incorporated by reference. The bitter nature of the therapeutic agents in compositions of the present invention in
Clark Karen F.
Cunningham Joan B.
Geist Gary
Howell John M.
The Procter & Gamble & Company
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