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(12) Patent Application Publication (10) Pub. No.: US 2011/0223150 A1 HOLLOWAY (43) Pub US 201102231.50A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0223150 A1 HOLLOWAY (43) Pub. Date: Sep. 15, 2011 (54) NEUTRACEUTICAL-BASED TOPICAL Publication Classification ANXOLYTICAGENT AND METHOD OF USE (51) Int. Cl. A638/48 (2006.01) (76) I t Garrett Blake HOLLOWAY A6IP 25/22 (2006.01) VO Kerrville,ae TXK (US) s (52) U.S. Cl. ..................................................... 424/94.64 (57) ABSTRACT (21) Appl. No.: 12/949,746 topicalA nutraceutical-based application is a anxiolvticSE. T agentR.S. (composition) R. fora combination of active ingredients directed to up-regulate the parasympathetic nervous system and calming Vagal nerve (22) Filed: Nov. 18, 2010 enervation and its resultant stress symptomatology. The active ingredients in the topical composition include GABA (gamma-aminobutyric acid), L-theanine, Phenibut (beta-phe Related U.S. Application Data nyl-gamma-aminobutyric acid), and casein tryptic hydrolysase. The active ingredients are dissolved in a lecithin (60) Provisional application No. 61/262.534, filed on Nov. organogel carrier Such as Lipoderm or Phloderm to provide a 18, 2009. Superior transdermal delivery system. Patent Application Publication Sep. 15, 2011 US 2011/0223150 A1 Combine GABAA, L-Theanine, Phenibut, and Casein Tryptic Hydrolysase to form Base Dissolve Base in Methyl Alcohol 100% and Propylene Glycol to form Solution Combine Solution with Transdermal (Lipoderm for Example) Add Water (with Preservatives) to Solution to Improve Suspension, Smoothness, and Shelf Life Divide Resultant Cream into Individual Doses Fig. 1 Provide GABAA, L-Theanine, Phenibut, and Casein Tryptic Hydrolysase Based Transdermal Cream Apply Divided Dose of Transdermal Cream, Half to Each Side of the Neck Over the Carotid Arteries Apply Excess of Transdermal Cream in Each Ear over the Arnold’s Branch (Auricular) of the Vagus Nerve Fig. 2 US 2011/0223 150 A1 Sep. 15, 2011 NEUTRACEUTICAL-BASED TOPCAL and non-agitative delivery. The formulation has a rapid ANXOLYTICAGENT AND METHOD OF USE response rate, low incidence of side effects, and low to no potential for development of dependency or tolerance. The CROSS REFERENCE TO RELATED resulting topical agent has application across a wide spectrum APPLICATIONS of anxiety based symptoms with relatively modest require 0001. This application claims the benefit under Title 35 ment for modification of the basic formulation for optimal United States Code S 119(e) of U.S. Provisional Patent Appli application to a particular condition or symptom. cation Ser. No. 61/262,534 filed Nov. 18, 2009, the full dis closure of which is incorporated herein by reference. BRIEF DESCRIPTION OF THE DRAWINGS BACKGROUND OF THE INVENTION 0010 FIG. 1 is a flowchart of the method steps associated with the formulation of the anxiolytic agent for topical appli 0002 1. Field of the Invention 0003. The present invention relates generally to topical cation of the present invention. preparations for providing relief from Symptoms of stress in 0011 FIG. 2 is a flowchart of the method steps associated individuals suffering from anxiety. The present invention with the use of the anxiolytic agent for topical application of relates more specifically to an improved nutraceutical trans the present invention. dermal topical agent for the amelioration and management of the physiological symptoms of anxiety. DETAILED DESCRIPTION OF THE PREFERRED 0004 2. Description of the Related Art EMBODIMENT 0005. It is well known in the medical and dental fields to provide a variety of palliative agents to patients to reduce the 0012. As indicated above, the present invention relates generalized anxiety responses experienced by many individu primarily to a combination of several neutraceutical-based als both before and during medical and dental procedures. anxiolytic agents dissolved in a Lecithin organogel transder Currently, such anxiety is addressed primarily by controlled mal delivery system. This topical application is useful in the class prescription medications. These commonly include amelioration and management of the physiological Symp sedatives, hypnotics, and antipsychotics which are adminis toms of anxiety. The agent can be effective in relieving stress tered orally or parenterally. symptoms resulting from many conditions including gener 0006 Less frequently, topical preparations are given for alized anxiety disorder, social anxiety disorder, post-trau anxiety. The known topicals, however, tend to be less potent matic stress disorder, medical and dental phobias, health pro than the parenterals, have slower response times, shorter cedure phobias, and panic disorders. durations, and less precise dosage titration. Many of these 0013. In one preferred embodiment of the present inven drugs produce undesirable side effects and have the potential tion, a preferred quantity (by mass) of the active ingredients may be as follows: GABA A 200 mg. L-Theanine 200 mg. for tolerance and dependency. In many cases, these drugs are Phenibut 400 mg, and Casein Tryptic Hydrolysase 400 mg. not well tolerated or produce excessive sedation. The preferred topical carrier may be from the Lecithin orga 0007. It would therefore be beneficial to provide a nutra nogels, e.g., Lipoderm or Phloderm. ceutical-based topical agent Suitable for use in the manage 0014 Reference is made to FIG. 1 wherein the laboratory, ment of the physiological symptoms of anxiety. It would be an effective compounded formula may be formulated as fol helpful if Such an agent would have a Superior transdermal lows: GABAA 10 g, L-Theanine 10 g, Phenibut 20 g, and delivery system. It would further be beneficial if such an agent Casein Tryptic Hydrolysase 20 g combined (Step 102) and was easy to use and apply Such that it could be dispensed in a dissolved (Step 104) in 50 ml (40 ml ethyl alcohol 100% and metered dose pen or unit dose packets. 10 ml propylene glycol) to yield 1.2 g/ml. The transdermal SUMMARY OF THE INVENTION may preferably have 3.5 g base per 35 g transdermal (Lipo derm) (Step 106). Water may be added to improve the sus 0008. In fulfillment of the above and other objectives the pension and smoothness of the compound (Step 108). Preser present invention provides a nutraceutical-based anxiolytic vative may also be included to enhance the shelf life of the agent for topical application. The novel formulation utilizes a compound. The oral dose 100%-1200 mg of active ingredi combination of active ingredients directed to up-regulate the ents. The transdermal bioavailability requires only 8%-10% parasympathetic nervous system and calming Vagal nerve of the oral dose=96 mg or 0.096 g (120 mg or 0.12 g). The enervation and its resultant stress symptomatology. The transdermal dose is equivalent if not greater than oral deliv active ingredients in the topical composition include GABA ery. The resultant cream may then be divided into individual (gamma-aminobutyric acid), L-Theanine, Phenibut (beta doses (Step 110) for dispensing. phenyl-gamma-aminobutyric acid), and Casein Tryptic 0015 The compound may be delivered in a number of Hydrolysase. The active ingredients are dissolved in a lecithin ways, a typical example of which is described in FIG. 2. organogel carrier Such as Lipoderm or Phloderm to provide a Essentially the cream (Step 202) is dispensed to the neck over Superior transdermal delivery system. the left and right carotid arteries (Step 204) and also applied 0009. The resulting topical agent has many advantages in the ear over the Arnold's Branch of the vagus nerve (Step over drugs currently used to reduce anxiety, especially during 206). For example, the compound may be delivered by a dose medical and dental procedures. The composition of the metering pen wherein one click of the pen dispenses 0.05 g. present invention is easily stored and packaged, has easy Otheringredients may be added Such as myoinositol, glycine, dosage titration and application, and provides non-invasive and N-acetyl L-tyrosine. Depending on the application and US 2011/0223 150 A1 Sep. 15, 2011 known interactions, the formula may be adjusted to include GABA is frequently given to produce a tranquilizing effect other ingredients for other applications such as lowering and to Successfully treat patients suffering from anxiety or blood pressure, PTSD, and Smoking cessation. depression. 0016. The pathways of action are the brain and the vagus 0021 L-Theanine is a unique anxiety reducer and mood nerve. The agent is applied topically to the area of the neck enhancer. Many studies have shown the health benefits of over the carotid arteries and to the area in each ear over green tea, but what makes it the most consumed beverage in Arnold's branch (auricular branch) of the vagus nerve. The the world after water is its pleasant taste and relaxation effect. application of the transdermal formula is preferably 1.2 g/ml Both of these qualities can be traced to L-theanine (gamma which is applied in a divided dose, half to each side of the neck ethylamino-L-glutamic acid), a unique, neurologically-active with the excess applied into each ear over Arnold's branch. amino acid. L-theanine is a free (non-protein) amino acid Up to 50% more may be used for individuals weighing over found almost exclusively in tea plants (Camelia sp.), consti 180 pounds. The agent may be delivered by a metered dose tuting between 1% and 2% of the dry weight of tea leaves. It pen, unit dose packets, vial and non-needle Syringe, or other is the predominant amino acid in green tea leaves. Isolating convenient dosing method. L-theanine, with its physical and neurological benefits, from 0017. The initial onset of effect is within three minutes. tea leaves was once difficult, expensive, and inefficient. Eco The duration of effect is approximately 1/2-2 hours. The nomically feasible methods of producing the identical desired effect reported is a sense of relaxation, calm, and L-theanine now exist and do not require large quantities of tea greatly diminished anxiety.
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