Title:  Edible herbal compositions for relieving nicotine craving

United States Patent:   6,534,527

Issued:  March 18, 2003

Inventors:  Wolfson; Philip (San Anselmo, CA); Jacobs, III; Payton (Lafayette, CA); Shulgin; Alexander T. (Lafayette, CA)

Assignee:  Phytos, Inc. (San Anselmo, CA)

Appl. No.:  871693

Filed:  June 4, 2001

Compositions useful in relieving craving in nicotine habituated patients are provided that include an herbal component. The herbal component provides multiple nicotine agonists, one of which is anabasine. The compositions are preferably in the form of chewing gum, tablets, capsules, or lozenge.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

Broadly, compositions of this invention are edible, that is to say, they are suitably formulated for oral use (e.g., chewing gum, tablets, lozenges, capsules, and the like). Regardless of the particular form, the compositions consist essentially of an herbal component that is derived from a plant or mixtures of plants having a quantity of anabasine and at least one other nicotine agonist, but with little or no nicotine. Among the plants from which the herbal component may be obtained are, for example, Medicago sativa, Lupinus formosus, Solanum carolinense, Aniba coto, Zinnia elegans, Sophora pachycarpa, Verbascum songaricum, Priestleya elliptica, Priestleya tomentosa, Haloxylon persicum, Haloxylon salicornicum, and Nicotiana glauca. Some species include quantities of both anabasine and nicotine, such as N. glauca and N. debneyi (with anabasine predominating).

A particularly preferred plant for obtaining the herbal component is N. glauca (sometimes commonly called "tree tobacco"). This is a very wide-spread plant in the United States and grows at diverse places. It has been medicinally used as an analgesic poultice applied externally. Anabasine is the dominant alkaloid in N. glauca leaves.

The herbal component of this invention will usually be provided by (or derived from) plant foliage (leaves and stems), although plant roots can also be used also, since the concentrations of anabasine in some plants are higher in roots than in leaves. The herbal component can be incorporated as dried plant parts or an extract therefrom. Herbal extracts are extracts of plant materials, such as a tincture of botanical materials, which typically are prepared by contacting botanical material with a solvent (British Herbal Pharmacopeia, Peter R. Bradley, Ed., British Herbal Medicine Association, 1983; and British Herbal Compendium, Peter R. Bradley, ed., British Herbal Medicine Association, 1992). The solvent, for example, can be aqueous or organic, or a combination thereof. Acceptable organic solvents include, but are not limited to, glycerin, propylene glycol or alcohol, or a combination thereof. The most preferred solvents are hydroalcoholic solvents as defined in British Herbal Pharmacopeia and Compendium.

Since a smoking cessation program may begin by gradual cessation of nicotine, followed by more complete, or by complete cessation of nicotine, inventive compositions may be formulated that have some nicotine (albeit in quantities substantially less than the anabasine amount) in which case there are an expanded number of plant sources suitable as the precursor for the herb or herbal extract. It is believed that use of an herbal component with multiple agonists to provide the essential anabasine component results in surprisingly improved properties and results over the prior attempts to use pure anabasine hydrochloride in gums or tablets. We do not presently know why the use of an herb or an herbal extract with multiple nicotine agonists provides the surprisingly improved properties and results for treating patients in a smoking reduction or cessation program. Without being limited by theory, it may be that the essential anabasine component serves as primary agonist and the one or more additional agonists, particularly such as the preferred anatabine, even when present in relatively small amounts, serves or serve as a co-agonist or co-agonists. Alternatively, it may be that there are multiple binding sites on the receptor.

In any event, use of herbs or herbal extracts in accordance with this invention provides a mixture of complex ingredients. Since an agonist stimulates the receptor by stabilizing an active confirmation, and this stabilization can be achieved in many different ways depending upon the chemical nature of the ligand and on the structure of the receptor, the combination of agonists provided from a source of complex ingredients, such as the suitable herbs or herbal extracts of this invention, may achieve a stabilizing function through multiple interactions at different parts of the target receptor.

In compositions of this invention, the anabasine content per recommended dose is in the range of between about 0.5 mg to about 10 mg, more preferably from about 2 mg to about 4 mg. Thus, for example, if a recommended daily dose is 8 tablets (as in chewing gum), then a patient could be receiving about 1-80 mg/day, more preferably 4-32 mg/day, of anabasine.

Compositions of the invention preferably have from only small, or trace, amounts of nicotine or no nicotine at all. Thus, the amount of nicotine per recommended dose will be from 0 wt. % to trace levels.

When formulated as tablets, lozenges, capsules, or chewing gum, it is contemplated that the herbal component will be present in an amount from about 200 mg to about 600 mg dry weight, or about 50 mg to 400 mg liquid extract of the dry plant material. Such compositions will typically also include additional components such as a binder, a humectant, and flavoring agents such as sweeteners, artificial or natural fruit flavors, oils, and the like. Coloring may also be included.

Thus, in one embodiment, the composition is included in a chewing gum formulation. The formulations of chewing gum are conventional, and well known to those skilled in the art. For example, a carrier may be provided that may be mixed with the herbal component. Suitable carriers, particularly in formulating chewing gums, comprise arabic, guar, and natural rubber gums. Other typical components are sweeteners (sugar, saccharin, sorbitol, aspartame), flavoring agents (e.g., mints, fruits, spices), coloring agents, and the like.

For example, the chewing gum or solid carrier may be composed, in its basic formula, of ingredients such as sucrose, corn syrup, gum base, coloring and flavoring. Ingredients such as HSH (hydrogenated starch hydrolysate), sorbitol, xylitol, and/or isomalt can replace sucrose and corn syrup at different ratios. As an example of preparation, to a hot water jacketed stainless steel gum mixer equipped with sigma tangential blades rotating at 9-12 rpm with a 1:2 rotating ratio, molten gum base may be added at approximately 55-55^oC., and corn syrup or HSH, added at room temperature in the desired amounts, and mixed until fully dispersed. When a homogeneous mix is obtained, sucrose or sorbitol, xylitol, or isomalt may be added, all in powder form, and mixed until fully dispersed. During the process of the addition of the powder material, the herbal component may be added. Color, flavoring, and any other ingredient deemed necessary for the particular formula may be added. The gummy mass is then discharged from the gum mixer and conveyed to the gum forming equipment.

Thus, for example, the solid portion or chewing gum used as a carrier for the herbal component may be composed of sucrose (10-80%, preferably 15-50%), corn syrup (5-60%, preferably 10-30%), gum base (10-90%, preferably 20-80%), sorbitol (10-60%, preferably 20-50%), hydrogenated starch hydrolysate (HSH) (5-60%, preferably 10-30%), hydrolyzed proteins (1-8%, preferably 1.5-3.0%), isomalt (10-80%, preferably 15-50%), xylitol (10-80%, preferably 15-50%), artificial sweeteners (0.2-2.0%, preferably 0.5-1.0%), natural sweeteners, coloring, and flavor ingredients--to appearance and taste. Additional ingredients may include other botanical extracts, gelatin, glycerin, starch and modified starches (1-7%, preferably 1.5-5.0%), these being used for the purpose of modifying texture and chewing properties of the gum as well as to enhance the release of nicotine agonists from the gum matrix. The texture and physical properties of the finished product are affected by the final form of the chewing gum, which can also be in sugar or sugar-free form. Such a chewing gum formulation may also include a liquid center in the gum. In such case, the herbal component, preferably in the form of an herbal extract in suitable solvent, may be incorporated into or serve as the liquid center.

In another embodiment, the herb or herbal extract component of this invention is included in a tablet, capsule, or a lozenge for oral administration of the medication with local effects on the mouth and throat. Known tableting agents, binders, and the like as carriers may be used in such formulations.

Further, liquid preparations (where the carrier is a liquid) and emulsions are also contemplated for the inventive compositions.

It is to be understood that while the invention has been described above in conjunction with preferred specific embodiments, the description and examples are intended to illustrate and not limit the scope of the invention.

Claim 1 of 16 Claims

We claim:

1. A composition useful in relieving craving in a nicotine habituated patient who is abstaining from or reducing nicotine intake, comprising:

an herb or an herbal extract providing a plurality of nicotine agonists, at least one of the nicotine agonists being anabasine in an amount of at least about 0.2 weight percent of the herb or herbal extract, the herb or herbal extract having from about 0 weight percent nicotine to a trace amount, wherein said trace amount is less than the amount of anabasine; and

an edible carrier for the herb or herbal extract.
 

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