Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
1998-06-29
2001-09-18
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
C424S447000, C424S448000, C424S484000, C514S078000
Reexamination Certificate
active
06290986
ABSTRACT:
The present invention is directed to transdermal administration of pharmacologic agents, and in particular to transdermal administration of drugs including antidepressant serotonin specific reuptake inhibitors (as SSRIs) such as fluoxetine, antidepressants such as buproprion and reboxetine, tricyclic antidepressant medications that have neuropathic pain treatment efficacy such as amitriptyline and doxepin, mood stabilizers such as carbamazepine, or valproic acid, Attention Deficit Hyperactivity Disorder (ADHD) medications such as pemoline anti-inflammatory or analgesic medications such as ketoprofen or piroxicam, treatments for impotence such as sildenafil and or anti-convulsants believed to possess neuropathic pain treatment efficacy such as gabapentin, carbamazepine, or combinations thereof such as using a gel matrix, preferably a lecithin organogel and/or a polymer gel.
BACKGROUND INFORMATION
In the past, patients suffering from a wide variety of conditions have been successfully treated by administration of pharmacologic agents. A vast majority of such patients receive doses of these agents orally. Unfortunately, in some situations, oral administration of such agents has been infeasible or ineffective. In some cases, oral administration is associated with side effects, particularly gastrointestinal side effects, sedation, or weight gain which cannot be tolerated well by the patient. In other cases, malabsorption of oral preparation have resulted in subtherapeutic plasma levels. In other cases, the agents have relatively short plasma half-lives, necessitating inconveniently frequent dosing. In general, oral delivery involves a time delay as the pharmaceutical is absorbed via the digestive system before entering the bloodstream. A number of agents which have traditionally been administered orally or by injection have been inappropriate or suboptimal for some patients when so-administered.
There are a number of medications which in at least some patients are not tolerated well when orally administered (e.g. which cause undesirable gastrointestinal or other side effects) and/or which provide undesirably high or low concentrations or delayed concentrations in a target tissue. In some cases, dosages which are appropriate for oral administration, upon being distributed more or less uniformly throughout the body, are undesirably low in a particular tissue to achieve desired results. Oral or injection administration may result in to slow or too rapid increase in blood plasma levels, e.g. may involve an undesirably long time delay as the pharmaceutical is absorbed by the digestive system before entering the bloodstream, or may result in a “spike” in blood plasmal levels followed by an undesirably low level, where a more constant level would be preferable. Some pharmaceuticals are particularly prone to cause or contribute to liver damage when administered orally.
One alternative route of administration for selected pharmaceuticals, has been transdermal delivery. Transdermal delivery has been utilized , e.g., for the treatment of high blood pressure, for ischemic heart disease and for hormone replacement. Transdermal delivery is not necessarily appropriate for all types of pharmaceuticals and, it is believed, has not, in general, previously been successfully used, with full effectiveness, for psychopharmacologic or psychotropic agents. Transdermal delivery is accompanied by its own side effects, including a potential for skin irritation, arising from the gel or other matrix, from the pharmaceutical itself, or from the interaction of the pharmaceutical with the matrix. Furthermore, a transdermal system must be configured such that the combination of the matrix and the pharmaceutical does not react with or modify the pharmaceutical, or otherwise render it ineffective, such that the combination provides sufficient diffusion coefficients, such that the delivery system is not adversely affected by expected temperature variations during normal manufacture, transportation, storage and use, such that the gel or other matrix retain the desired viscosity, and such that the pharmaceutical can be properly dispersed or dissolved in the matrix such that components remain homogenous and do not separate (particularly when more than one pharmaceutical is included) and the like.
Although other forms of delivery of pharmaceuticals agents are known, each has its drawbacks. Parenteral (i.e., intravenously or intramuscularly injected) administration is inconvenient and expensive, and is rarely used outside the hospital. Inhalation is believed to be not feasible with psychopharmacologic agents currently in use or with many other pharmaceuticals.
Accordingly, it would be useful to provide a transdermal delivery system effective to provide good transdermal absorption and acceptable plasma blood levels preferably a system which can be adapted for use with a wide variety of different agents for transdermal delivery of effective amounts of such agents at a desired or controlled rate, while preferably avoiding or reducing undesired effects such as liver damage, gastrointestinal side effects, sedation, and weight gain.
SUMMARY OF THE INVENTION
The present invention provides for transdermal delivery of pharmacologic agents, particularly psychopharmacologic, anti-convulsant, anti-inflammatory, analgesic or other agents, by dissolving or dispersing such agents in a gel, preferably a lecithin organogel. In one embodiment, an agent is delivered using a lecithin gel such as a gel formed using lecithin and an organic solvent such as isopropyl palmitate or isopropyl myristate, alcohol, or ethoxy diglycol. In one embodiment, the gel includes or is formed from a polymer such as that sold under the trade name “Pluronic” available from BASF-Wyandotte Corporation, Parsippany, N.J.
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Murdock Robert W.
Williams C. Donald
Channavajjala Lakshmi
DeConti, Jr. Gjulio A.
Laccotripe Maria C.
Lahive & Cockfield LLP
Page Thurman K.
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