Title:  Plantago majorand piper methysticum compound for use in treating a tobacco or nicotine habit

United States Patent:  6,303,647

Appl. No.:  525931

A composition containing the herbs Plantago major and Piper methysticum is presented. Use of the composition, of the present invention, in a form adapted to be orally ingested produces a diminished desire for tobacco (i.e., nicotine) without the use of nicotine itself and advantageously provides anti-depressive and anti-anxiety effects without sedative or hypnotic effects.

DESCRIPTION OF THE PREFERRED EMBODIMENT

The composition of the present invention comprises a Plantago major component and a Piper methysticum component and serves as an aid in smoking cessation. The herbs used in the present invention may by prepared for use either by a drying method or by an extraction method.

When a drying method is preferred, the herbs Plantago major and Piper methysticum are prepared by drying the herbs by suitable methods known in the art. After the herbs have been effectively dried, the entire plant or a portion thereof may be used in the composition of the present invention. When dried herbs are used in the present composition, the Plantago major component comprises from about 5% to about 95 % by weight of the total composition and the Piper methysticum component comprises from about 95% to about 5% by weight of the total composition, wherein the dried Piper methysticum is standardized to comprise at least 30% by weight of kava lactones, which are the active constituents in Piper methysticum. The kava lactones are generally found in the lipid-soluble portion of the herb's root and have shown anxiolytic, analgesic, muscle-relaxing and anticonvulsant effects. Dried Plantago major and Piper methysticum are commercially available from Natures Value, Bayshore, New York. Alternatively, the Plantago major and Piper methysticum for use in the composition of the present invention may be prepared as liquid extracts of the herbs by extraction methods known in the art. The herbs may be extracted in either alcohol and water or by a glycerin and water based extraction method. One preferred extraction method comprises preparing the extracts of the herbs by a maceration process involving an alcohol (ethanol, ethyl alcohol, and not methanol) treatment, as is known in the art. Alternatively, the glycerin and water extraction process is particularly useful because glycerin may be used as a solvent in a liquid core of a capsule. Liquid filtrate which is obtained in a conventional extraction process after filtering the extractant liquid may then be further refined by removing any solvents with sufficiently low boiling points such as an alcohol by using standard evaporation techniques until the composition is substantially free from such solvents. Stabilizers and preservatives are typically added during the extraction method. When the Plantago major and Piper methysticum are prepared using extraction methods, the composition of the present invention comprises Plantago major extract in the amount from about 0.05% to about 40% by volume of the total composition and Piper methysticum extract in the amount from about 0.05% to about 40% by volume of the total composition, wherein the Piper methysticum extract is standardized to comprise at least 30% kava lactones. Plantago major and Piper methysticum extracts are commercially available from Botanical Laboratories, Inc., Ferndale, Wash.

In accordance with the present invention, once the Plantago major and Piper methysticum components have been prepared for use in the composition of the present invention by either a drying process or by an extraction process, the Plantago major and Piper methysticum components may be used in a composition which is intended to be orally ingested. Suitable compositional forms which may be administered orally include but are not limited to soft and hard gelatin capsules, pills, coated pills, tablets, dragees, and other forms known in the art.

When the Plantago major and Piper methysticum composition is to be administered in a soft or hard gelatin capsule form, a liquid core component is prepared and then encapsulated in a soft or hard gelatin shell in accordance with the present invention. As is known in the art, preselected amounts of pharmaceutical or herbal compositions can be encapsulated within soft or hard gelatin shells. When using soft gelatin shells, the soft gelatin shells typically comprise gelatin, plasticizers, water and other compositions. Gelatin is an essential component of the soft gelatin shells and conventionally one or more plasticizers are incorporated to produce a soft gelatin shell. The soft gelatin thus obtained has the required flexibility characteristics for use as an encapsulating agent. Useful plasticizers include glycerin, sorbitan, sorbitol, or similar low molecular weight polyols, and mixtures thereof. A preferred plasticizer is glycerin. The soft gelatin shells also comprise water. Without being limited to theory, water is believed to aid in the rapid dissolution or rupture of the soft gelatin shell upon contact with the gastrointestinal fluids encountered in the body. The shell may contain still other usual accessory substances, such as preservatives or coloring substances and pigments.

As is generally known in the art, the production of soft gelatin capsules comprises a first operation by which a wet capsule is formed and which is thereafter dried. Accordingly, the gelatin used for making the shell of the capsule contains at the time of manufacture a considerable proportion of water. During drying of the capsules, the water contained in the walls of the wet capsule normally does not completely vaporize. A small proportion of the water passes into the liquid core.

The liquid core of the soft gelatin capsules for use in the present invention comprises the Plantago major component and the Piper methysticum component along with conventional stabilizers, preservatives and other components known in the art. The liquid core has a sufficient quantity of solvent to act as a carrier of the Plantago major component and Piper methysticum component. In accordance with the present invention, the Plantago major component and Piper methysticum component may be added to the liquid core in either a dried state or as an extract. The upper limit of the addition of the Plantago major and Piper methysticum to the liquid core lies in the solubility of the herbs in the solvent. Conventional liquid core solvents include but are not limited to polyethylene glycols, polyvinylpyrrolidone, propylene glycol, and glycerol. The liquid core may also comprise a mixture of ethanol and one or more partial glycerides of fatty acids having from 6-18 carbon atoms. The partial glycerides useful in the liquid core include monoglycerides or diglycerides as well as mixtures thereof, e.g., See U.S. Pat. No. 4,888,239 to Brox, which is incorporated by reference herein in its entirety. Other components which can be incorporated into the liquid core include colorings, flavorings, preservatives, lubricants, flow-enhancers, filling aids, anti-oxidants, essences, and other aesthetically pleasing components. A preferred preservative for use in the liquid core of the present invention is citric acid.

When a soft gelatin capsule is the preferred means of administering the Plantago major and Piper methysticum composition of the present invention, the Plantago major and Piper methysticum components are preferably prepared as liquid extracts for use in the liquid core of a capsule. As hereinbefore recited, standard extraction methods, including alcohol and water or glycerin and water, may be used to prepare extracts of Plantago major and Piper methysticum.

Any suitable soft gelatin capsule known in the art may be used with the Plantago major and Piper methysticum composition of the present invention. For example, soft gelatin capsules are disclosed in U.S. Pat. No. 4,744,988; U.S. Pat. No. 5,431,916; and U.S. Pat. No. 5,641,512, all of which have hereinbefore been incorporated by reference in their entirety. Suitable soft gelatin capsules for use in the present invention are soluble in water and in gastrointestinal fluids. Upon swallowing the capsule, the gelatin shell rapidly dissolves or ruptures in the gastrointestinal tract thereby introducing the Plantago major and Piper methysticum composition from the liquid core into the physiological system.

In accordance with the present invention, the Plantago major and Piper methysticum composition may be orally ingested in a pill form. Conventional pelletizing methods may be used to manufacture the Plantago major and Piper methysticum composition in pill form. As is known in the pharmaceutical arts and in other arts, the components may be weighed, blended and pelletized to form a solid pill form. In addition, tablets may be prepared according to a dry or wet granulating procedure as is known in the art. These solid forms, e.g., pill, may be orally ingested and upon swallowing, they rapidly dissolves in the gastrointestinal tract thereby introducing the active material within the pill into the physiological system. In accordance with the present invention, the Plantago major and Piper methysticum herbs may be incorporated and pelletized in a dried state or a liquid extract of the herbs may be prepared before the extract solvent is evaporated using conventional techniques thereby leaving a solid extract residue. This solid extract residue may then by weighed and blended into a pill form along with suitable solid carrier materials. When dried herbs are used as a material to be pelletized into a pill, the entire dried plant or a portion thereof may be used. Preferably, the Plantago major comprises between about 5% to about 95% by weight of the total composition and the Piper methysticum also comprises between about 95% to about 5% by weight of the total composition, wherein the Piper methysticum is standardized to comprise at least 30% by weight Kava lactones.

The Plantago major and Piper methysticum composition of the present invention offers significant advantages over prior art tobacco cessation products. The composition of the present invention is easily orally ingested in either a capsule form or a pill form. The composition of the present invention combines the desirable properties of Plantago major and Piper methysticum in one product for aiding in the cessation of tobacco use. Plantago major is an all natural herb which creates an aversion to tobacco and eases anxiety. Therefore, the danger of increasing the nicotine addiction inherent in the use of nicotine patches is avoided with this invention. Piper methysticum is an all natural herb which has anti-depressive and anti-anxiety properties and advantageously has very few side effects, unlike the pharmaceutical composition bupropion which is often dispensed as an anti-depressive to help with the depressive effects of nicotine withdrawal. Because the depressive effects associated with nicotine withdrawal are an important factor in nicotine addiction, the use of the herb Piper methysticum in the composition aids in diminishing the desire for tobacco products. Furthermore, Piper methysticum is noted for promoting relaxation without causing a decrease in mental sharpness, making it particularly useful for the management of daytime anxiety associated with a nicotine withdrawal. It also facilitates normal, restful sleep and acts as a relaxant for skeletal muscles, all of which aid a person in their attempt to cease consuming nicotine products. Importantly, Piper methysticum does not significantly lose its effectiveness over a prolonged period of time and therefore, the same level of does continues to produce the same desirable properties over this prolonged period of time. A tolerance for Piper methysticum does not appreciably develop over time and thus, the effectiveness of the herb is advantageously maintained.

While preferred embodiments have been shown and described, various modifications and substitutions may be made thereto without departing from the spirit and scope of the invention. Accordingly, it is to be understood that the present invention has been described by way of illustration and not limitation.

Claim 1 of 10 Claims

What is claimed is:

1. A method for aiding an individual in the cessation of tobacco use, comprising:

administering to said individual a composition containing a Plantago major component and a Piper methysticum component,

wherein said Plantago major component is prepared by a process comprising either drying a Plantago major plant to form a dried Plantago major plant, said dried Plantago major plant is at a concentration of about 5% to about 95% by weight based on said composition, or extracting said Plantago major plant to form a Plantago major extract, said Plantago major extract is at a concentration of about 0.05% to about 40% by volume based on said composition, and

wherein said Piper methysticum component is prepared by a process comprising either drying a Piper methysticum plant to form a dried Piper methysticum plant, said dried Piper methysticum plant is at a concentration of about 5% to about 95% by weight based on said composition and said dried Piper methysticum plant comprises at least 30% by weight of kava lactones, or extracting said Piper methysticum plant to form a Piper methysticum extract, said Piper methysticum extract is at a concentration of about 0.05% to about 40% by volume based on said composition and said Piper methysticum extract comprises at least 30% by volume of kava lactones,

said composition being administered in an amount effective to cause an aversion to tobacco.

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