Compositions and methods for inhibiting alpha-glucosidase

Abstract

A composition for administration to a subject is disclosed. The composition comprises at least one plant active component. The plant active component is present in the composition in an amount effective to inhibit alpha-glucosidase in the subject. The plant active component comprises at least one extract of Lysidice rhodostegia. The composition can be in the form of an oral composition, for example for ingestion. The composition can also be in the form of a topical composition, for example for topical administration. A method of inhibiting alpha-glucosidase in a subject is also provided. The method comprises administering to the subject an effective amount of the composition.

Description

Invention Field

[0001] This invention generally relates to compositions and methods for inhibiting α-glucosidase, and more specifically, to compositions containing plant extracts for inhibiting α-glucosidase in a subject. Related methods are also provided. Background of the Invention

[0002] Alpha-glucosidase is an enzyme that catalyzes the breaking of glycosidic bonds in oligosaccharides or glycoconjugates to break down starches and disaccharides into glucose. Alpha-glucosidase is located at the brush border of the small intestine and is responsible for metabolizing oligosaccharides and disaccharides into monosaccharides. High levels of glucose in the blood are called hyperglycemia. Postprandial hyperglycemia remains a problem in the management of type 2 diabetes. Postprandial hyperglycemia significantly promotes the development of chronic diabetic complications, particularly cardiovascular disease and microvascular complications of diabetes. Of all available antidiabetic drugs, alpha-glucosidase inhibitors appear to be the most effective in reducing postprandial hyperglycemia.

[0003] Given the above, there remains an opportunity to provide new and useful α-glucosidase inhibitors. Such α-glucosidase inhibitors could provide potential preventative and therapeutic methods for reducing the risk of hyperglycemia, diabetes, or other pathogenic complications caused by α-glucosidase. Therefore, there also remains an opportunity to provide new and useful compositions and methods for inhibiting α-glucosidase. Invention Overview

[0004] A composition is provided for administration to a subject. The composition comprises at least one plant-active ingredient. The plant-active ingredient is typically present in the composition in an amount that effectively inhibits α-glucosidase in the subject. The plant-active ingredient comprises at least one herbaceous herb (…). Anisochilus carnosus Extracts of ).

[0005] In various embodiments, the composition is preferably an oral composition formulated for oral administration to a subject. In other embodiments, the composition may be a topical composition formulated for topical administration to a subject.

[0006] The composition can be used to inhibit α-glucosidase in a subject. A method of inhibiting α-glucosidase in a subject includes administering an effective amount of the composition to the subject. Brief description of the attached diagram

[0007] Figure 1 This is a graph showing the α-glucosidase inhibition rate using the herb extract;

[0008] Figure 2 This is a graph showing the α-glucosidase inhibition rate using the 70% ethanol extract of *Platycodon grandiflorus*.

[0009] Detailed description of the current embodiments

[0010] A composition for administration to a subject is disclosed. The composition comprises at least one botanical active ingredient. The composition is described below, followed by related uses and methods.

[0011] As will be appreciated in light of the present disclosure, the composition is not particularly limited except for the botanical active ingredient, particularly extracts thereof, and related components and methods. Thus, the composition can be formulated, for example, as a topical composition (e.g., a cosmetic composition), or as an oral composition or a pharmaceutical, and can be used as the sole and independent therapeutic agent or in combination with other therapeutics that are compatible therewith.

[0012] The composition can be used to treat, prevent, and / or ameliorate a variety of conditions, such as those associated with alpha-glucosidase activity. In particular, as will be appreciated in light of the following description and examples, it is believed that the compositions of the present embodiments are capable of inhibiting alpha-glucosidase, and more particularly, inhibiting alpha-glucosidase in a subject.

[0013] Thus, the composition can be used to treat (i.e., slow, prevent, reverse, etc.) conditions generally associated with alpha-glucosidase activity, such as complications associated with hyperglycemia, diabetes, and other health disorders.

[0014] As introduced above, the composition comprises a botanical active ingredient. More particularly, the botanical active ingredient comprises at least one extract of Syzygium aromaticum, optionally consists essentially of at least one extract of Syzygium aromaticum, or optionally consists of at least one extract of Syzygium aromaticum. Each extract can be simply referred to as a "botanical extract" or collectively as "botanical extracts," and are described below.

[0015] The term "extract" is used herein in its conventional sense to refer to a composition obtained by fluid extraction from a source material. Thus, the term "botanical extract" is understood to be a composition obtained by fluid extraction (e.g., solvent extraction, gas extraction, CO2 extraction, etc.) from a botanical source (i.e., plant material). Botanical extracts suitable for use in the composition can be obtained by any extraction method known in the art or combinations of these methods, including water extraction, steam extraction, solvent extraction, etc. Exemplary extraction techniques are described below. However, botanical extracts are not generally limited to a particular extraction method, or additional / supplemental techniques used to obtain botanical extracts, but can vary according to the parameters described herein. In addition, the extraction step is not necessary to prepare the botanical active ingredient and / or the composition, as suitable extracts (e.g., standardized extracts) can be readily obtained from many commercial suppliers.

[0016] Plant extracts suitable for use in or as a plant active ingredient include those obtained by solvent extraction, such as by using polar solvents such as alcohols (e.g., methanol, ethanol, butylene glycol, etc.), ethers (e.g., diethyl ether, methyl tert-butyl ether, etc.), ketones (e.g., acetone), esters (e.g., ethyl acetate), phenols, water, etc., non-polar solvents such as benzene, xylene, toluene, etc., and derivatives, modifications, and combinations thereof (e.g., solvent-water blends, including alcohol-water, acetone-water, etc.). Additional and alternative extraction techniques include sequential fractionations, total hydro-ethanolic extractions, lump-sum extractions, supercritical fluid extraction (e.g., with CO2), etc., as well as those utilizing secondary or further extractions from a first extract (e.g., non-polar solvent extraction of a plant extract obtained from a polar solvent extraction) or other processing techniques, such as filtration, purification, distillation, dehydration, evaporation, concentration, drying, etc. Specific examples of suitable extraction methods are described in U.S. Patent No. 7,897,184, which is incorporated herein by reference.

[0017] As understood in the art, various parts or portions of a plant can be used to obtain essential oils and extracts, such as bark, berry, flower, fruit, leaf, peel, resin, rhizome, root, seed, and / or wood. Essential oils can be obtained by a number of methods, such as by distillation (e.g., using steam), pressing, solvent extraction, absolute oil extraction, resin tapping, and / or cold pressing.

[0018] In various embodiments, the solvent used to obtain a plant extract suitable for use in the present disclosure is a solvent in which the resulting plant extract and / or its subsequent form (e.g., plant extract powder) is suitable for ingestion. For example, the solvent is water or ethanol.

[0019] In one example, a plant extract can be obtained using an organic solvent extraction technique. In another example, a plant extract can be obtained using solvent sequential fractionation. Total hydro-ethanolic extraction techniques can also be used to obtain a plant extract. Generally, this is referred to as lump-sum extraction. In this method, a plant extract is generated that contains a wide variety of phytochemicals present in the extracted material, including both lipid-soluble and water-soluble phytochemicals. After the plant extract solution is collected, the solvent is evaporated to yield the plant extract.

[0020] Total ethanol extraction can also be used. This technique uses ethanol as the solvent. This extraction technique can result in a plant extract that can include liposoluble and / or lipophilic compounds in addition to water-soluble compounds. Total methanol extraction can also be used in a similar manner with similar results.

[0021] Another example of an extraction technique that can be used to obtain a plant extract is supercritical fluid carbon dioxide extraction (SFE). In this extraction procedure, the material to be extracted is not exposed to any organic solvents. Rather, the extraction solvent is carbon dioxide (C02) under supercritical conditions (e.g., > 31.3 °C and > 73.8 bar), with or without a modifier. Those skilled in the art will recognize that the temperature and pressure conditions can be varied to obtain optimal yields of the plant extract. Similar to the total hexane and ethyl acetate extraction techniques that can also be used, this technique results in a plant extract of liposoluble and / or lipophilic compounds.

[0022] Each of the above extraction methods can also include and / or be used in conjunction with one or more additional processing steps as understood in the art. For example, the plant material can be comminuted, broken, milled, etc. There can also be one or more filtration steps to remove, for example, cellulosic / fibrous material or other solid material. There can also be one or more purification steps to remove, for example, certain components and / or contaminants. Such purification can be achieved, for example, by distillation, evaporation, centrifugation, etc. There can also be one or more concentration and / or drying steps to remove water and / or other volatiles, such as alcohols, lighter compounds, VOCs, etc. In addition, acids and / or bases can be added to adjust the pH or neutralize. Depending on the desired form of the final / finished plant extract, various additional steps as understood in the art can also be used, such as sieving, pressing, milling, grinding, mixing, dispersing, etc. It will be recognized that these additional processing steps are contemplated in combinations of repetitions and / or in different orders.

[0023] Anisochilus carnosus

[0024] In some embodiments, the plant active component and thus the composition, comprises an extract of P. lanceolata, i.e., an extract comprising, optionally consisting essentially of, material from the plant species P. lanceolata, such as stems and / or roots. The P. lanceolata extract is not particularly limited and can comprise or be any stem extract, root extract, or combination of stem and / or root extract from a P. lanceolata plant suitable for use in the embodiments herein. More specifically, exemplary P. lanceolata stem and / or root extracts include those capable of inhibiting alpha-glucosidase or eliciting / exhibiting any other such activity described herein as part of the plant active component.

[0025] P. lanceolata has been reported to contain various bioactive components, such as phenolic acids, flavonoids, flavanols, flavones, organic acids, fatty acids, triterpenoids, and other compounds. P. lanceolata can be referred to simply as A. carnosus , or various other names such as Anisochilus carnosus P. lanceolata (L.f.) Benth. Et Wall., "Xiang Pai Cao", Xiang Pai Cao, "Pai Cao Xiang", Pai Cao Xiang, or Pai Xiang Cao.

[0026] Specific examples of P. lanceolata extracts are known in the art. Thus, P. lanceolata extracts can be purchased or otherwise commercially obtained from various sources, prepared (e.g., using any conventional extraction technique known in the art, such as any of those described herein, or a combination thereof), or combinations thereof. In certain embodiments, extracts of P. lanceolata are obtained by water extraction (or aqueous extraction) of plant material of P. lanceolata. In further or additional embodiments, extracts of P. lanceolata are obtained by alcohol extraction (e.g., ethanol extraction) of plant material of P. lanceolata.

[0027] As will be appreciated by those skilled in the art, P. lanceolata is cultivated primarily for its plant material, including but not limited to its stems and roots. Thus, in various embodiments, extracts of P. lanceolata are extracts of P. lanceolata stems and roots. Suitable extractions include those noted above, such as aqueous and ethanol extraction of stems and roots. The stems and roots can be from one or more plants, and can be fresh, dried, or otherwise aged.

[0028] For example, certain extracts can be obtained in which P. lanceolata (e.g., stems and roots) are pulverized to a uniform size in a mill. Next, the resulting powder is extracted with water or an ethanol solution. The solution is then filtered, and the filtrate can be concentrated under reduced pressure to obtain a syrup. The syrup can then be freeze-dried to dryness to obtain the extract.

[0029] In various embodiments, the plant active components consist of extracts of P. lanceolata stems and roots. In further or additional embodiments, the composition is substantially to completely free of components obtained from non-stem-based plant material and / or non-root-based plant material of P. lanceolata. In these embodiments, the non-stem-based plant material and non-root-based plant material of P. lanceolata can be, for example, flowers, leaves, buds, seeds, and / or fruits of P. lanceolata plants. Without being bound to any particular theory, it is believed that stems and / or roots of P. lanceolata are most effective for alpha-glucosidase inhibition; whereas other parts of P. lanceolata are not (as illustrated in the Examples section below).

[0030] In other embodiments, the R. drupacea extract can comprise material from any part or combination of parts of the plant and is not limited to stem and / or root extracts. For example, the R. drupacea extract can comprise material extracted from one or more parts of the R. drupacea plant, including its flowers, leaves, shoots, seeds, and / or fruits. Further, such extracts can be further processed (e.g., defatted, partially defatted, ground, dried, precipitated, washed, filtered, sieved, extracted, distilled, concentrated, etc.) to obtain the R. drupacea extract. Likewise, the R. drupacea plant can be extracted in its raw form, or processed prior to extraction of the R. drupacea extract (e.g., used in its raw form, suspended form, dehydrated form, concentrated form, etc.). In certain embodiments, the plant active component comprises a R. drupacea extract comprising material obtained (i.e., extracted) from the whole plant of R. drupacea.

[0031] The amount of R. drupacea extract used in the plant active component can vary and is selected based on the number and type of components used in the plant active component. In certain embodiments, the plant active component comprises 1 to 2000 mg of R. drupacea extract, such as 1 to 1000 mg, optionally 2 to 800 mg, optionally 20 to 750 mg, or optionally 50 to 500 mg. However, amounts outside of these ranges can also be used. For example, in certain embodiments, the plant active component includes R. drupacea extract in an amount of at least 1 mg, optionally at least about 20 mg, optionally at least about 50 mg, optionally at least 100 mg, optionally at least 250 mg, optionally at least 500 mg, optionally at least 1000 mg, or optionally at least 1500 mg. In these or other embodiments, the upper limit can be selected such that the plant active component comprises R. drupacea extract in an amount of < 100, < 250, < 500, < 750, < 1000, < 2000, < 5000 mg. In various embodiments, the plant active component can include R. drupacea extract in an amount of optionally greater than 1, optionally greater than 5, optionally greater than 10, optionally greater than 25, optionally greater than 50, optionally greater than 75, optionally greater than 80, or optionally greater than 95% by weight, based on the total weight of the plant active component. In such embodiments, the upper limit can be selected to be typically < 10, < 20, < 30, < 40, < 50, < 60, < 70, < 80, < 90, and < 99% by weight, respectively, based on the total weight of the plant active component.

[0032] In certain embodiments, the plant active component comprises more than one R. drupacea extract, such as 2, 3, 4, or more R. drupacea extracts. In such embodiments, each R. drupacea extract is independently selected, can be the same as or different from any other R. drupacea extract, and is each used in an amount as described above.

[0033] The extract of P. odoratum can be used in any form, such as neat (i.e., in the absence of a solvent, carrier vehicle, diluent, etc.), or in a carrier vehicle, such as a solvent or dispersant. If present, the carrier vehicle can comprise an aqueous solvent (e.g., water), an organic solvent, a fluid or oil, etc., or combinations thereof. When used, the carrier vehicle should be selected based on the plant active component and / or the particular components of the composition, such as the particular extract of P. odoratum used. It is recognized that if a carrier vehicle is used, the extract of P. odoratum can be combined with the carrier vehicle before, during, or after combination with the plant active component and / or any other components of the composition.

[0034] Definitions

[0035] To provide a clear and consistent understanding of the specification and claims, the following definitions are provided.

[0036] The term "composition" or "formulation" refers to a product that treats, ameliorates, promotes, increases, manages, controls, maintains, optimizes, modifies, reduces, inhibits, or prevents a particular condition associated with a natural state, biological process, or disease or disorder. For example, the composition or formulation ameliorates, minimizes, inhibits, or prevents at least one of hyperglycemia and diabetes. The terms composition and formulation include, but are not limited to, a medicinal product (i.e., a drug), an over-the-counter drug (OTC), a cosmetic, which includes an effective amount of the extract, at least one component of the extract, or a mixture thereof. Exemplary compositions and / or formulations include a cream, a cosmetic lotion, a pack, or a powder, or as an emulsion, a lotion, a liniment foam, a tablet, a plaster, a granule, or an ointment. Preferred compositions are formulated for topical application / administration and for oral administration / intake.

[0037] As used herein, the term "effective amount" or "therapeutically effective amount" of a purified compound, composition, extract, extract mixture, component of an extract, and / or active agent or ingredient or combination thereof refers to an amount effective, at dosages and for periods of time necessary, to achieve the desired result. For example, an "effective amount" or "therapeutically effective amount" refers to the amount of a purified compound, composition, extract, plant extract, extract mixture, plant extract mixture, component of an extract, and / or active agent or ingredient of the present application or combination thereof that, when administered to a subject (e.g., a mammal, such as a human), is

[0038] The term "pharmaceutically acceptable" means those drugs, medicaments, extracts or inert ingredients that are suitable for use with human and lower animals' tissues without undue toxicity, incompatibility, instability, irritation, and the like, commensurate with a reasonable benefit / risk ratio, as well as the salts, solvates, and clathrates of the active compounds.

[0039] The terms "administering" and "administration" are defined as providing a composition to a subject by routes known in the art, including, but not limited to, topical, intravenous, intraarterial, oral, parenteral, buccal, transdermal, rectal, intramuscular, subcutaneous, intraosseous, transmucosal, or intraperitoneal routes of administration. In preferred embodiments, topical and / or oral routes of administration of the composition are suitable.

[0040] The terms "minimize," "reduce," "prevent," "decrease," and / or "inhibit" refer to a reduction or mitigation of hyperglycemia and / or its downstream effects by inhibiting alpha-glucosidase in the presence of a plant ingredient or plant extract as described herein, as compared to alpha-glucosidase activity in the absence of the plant ingredient or plant extract, as in a control sample. The extent to which hyperglycemia and / or its downstream effects are reduced by inhibiting alpha-glucosidase will vary depending on the nature and amount of plant ingredient or plant extract present, but is appreciably seen, for example, as a detectable decrease in alpha-glucosidase activity; the extent of the decrease is desirably greater than about 5%, about 10%, about 15%, about 20%, about 25%, about 50%, about 75%, about 90%, about 95%, or about 99% (or any decrease in the range of about 5% to about 99%) as compared to alpha-glucosidase activity in the absence of the plant ingredient or plant extract. For example, a composition comprising a plant ingredient or plant extract of Lysimachia foenum-gracum can minimize or decrease alpha-glucosidase activity.

[0041] The term "subject" or "individual" as used herein includes mammals to which a composition can be administered. Non-limiting examples of mammals include humans, non-human primates, rodents (including transgenic and non-transgenic mice), and the like. In some embodiments, the subject is a mammal, and in some embodiments, the subject is a human.

[0042] Compositions (or formulations)

[0043] The composition can include any amount of the plant active ingredient, selected based on the number and type of ingredients used in the overall composition. Generally, the plant active ingredient is present in the composition in an amount effective to inhibit alpha-glucosidase in a subject.

[0044] In certain embodiments, the composition comprises the plant active ingredient in an amount of 1 to 5000, optionally 2 to 2000 mg, optionally 5 to 1750, optionally 10 to 1500, optionally 15 to 1250, optionally 20 to 1000, optionally 25 to 750, optionally 30 to 500, optionally 35 to 500, optionally 40 to 500, optionally 45 to 450, optionally 50 to 450, or optionally 50 to 400 mg. However, amounts outside of and / or overlapping with these ranges can also be used. For example, it is recognized that the ranges described above with respect to the amount of each plant extract in the plant active ingredient can equally apply to the amount of each plant extract in the overall composition, as when the plant active ingredient consists of only one plant extract.

[0045] In some embodiments of the composition, the formulation comprises an extract of Lysimachia foenum-gracum.

[0046] Flavoring essences and / or sugar substitutes can be included in the composition and can be any type of conventional component understood in the art, e.g., flavoring agents. The plant extracts can each be as described above. Examples of suitable flavoring agents are further described below.

[0047] In general, the composition is not limited in formulation, peripheral ingredients, form, number of functions, etc., except for including the plant active component and its plant extract. Rather, the composition can vary and can be formulated in any manner consistent with the present disclosure.

[0048] Generally, the composition is formulated or otherwise adapted for suitable administration to a mammalian subject, e.g., a human. For example, in various embodiments, the composition is adapted for topical administration or consumption and / or oral administration to a human subject.

[0049] In certain embodiments, the composition is further defined as a topical composition formulated for topical administration to a subject. In such embodiments, the composition can also be referred to as a cosmetic composition, and generally includes at least one cosmetically acceptable carrier in addition to the biologically active agent composition. In specific embodiments, the cosmetically acceptable carrier is not naturally occurring. In other words, the carrier is not a natural product in these specific embodiments. In other embodiments, the carrier is selected from conventional carriers understood in the art, and can be used in conventional amounts.

[0050] In other embodiments, the composition is further defined as an oral composition formulated for oral administration to a subject. In such embodiments, the composition can also be referred to as an ingestible composition, and generally includes at least one pharmaceutically acceptable additive in addition to the biologically active agent composition. In specific embodiments, the pharmaceutically acceptable additive is not naturally occurring. In other words, the pharmaceutically acceptable additive is not a natural product in these specific embodiments. In other embodiments, the pharmaceutically acceptable additive is selected from conventional additives understood in the art, and can be used in conventional amounts.

[0051] Accordingly, it should be recognized that the particular additives, carriers, adjuvants, fillers, and the like that are present in or combined with the composition can vary. Further, the physical form of the composition is not limited and will be selected based on the particular components of the composition, the intended use of the composition, and the like. Thus, as will be appreciated in light of the description herein, the composition can be formulated as a liquid, a dry powder, a suspension, an emulsion, a gel, a paste, and the like, and combinations thereof. In certain embodiments, the composition is formulated as a sterile, pyrogen-free liquid solution or suspension, a coated capsule, a suppository, a lyophilized powder, a transdermal patch, a soft gel capsule, or other known form. Other examples of suitable forms include a solid, a gel, a liquid, a cream, a lotion, a pomade, a mousse, a powder, a foam, a spray, an ointment, or other such formulation in which the plant active ingredient is placed in an appropriate carrier vehicle, such as any of those described herein.

[0052] The composition can be prepared using various methods. For example, the actives (e.g., plant extract) of the composition and optionally one or more inactives (e.g., one or more conventional components, additives, excipients, and the like) can be mixed or blended and compressed or compounded using various techniques understood in the art. The composition of the present disclosure is not limited to a particular order of preparation steps or method of preparation.

[0053] In various embodiments, the composition is administered orally by being ingested by a subject. The subject is typically a human and can include males and females of various ages. The methods / compositions of the present disclosure are not limited to a particular subject.

[0054] The composition can be in various forms. Examples of suitable forms include solids, gels, and liquids. For example, the composition can be formulated to be applied as a gel, a cream, a lotion, a pomade, a mousse, a powder, or a foam to be applied to the skin of a subject. In another example, the composition can be formulated to be applied as a spray onto the skin of a subject. The composition can be formulated to be sprayed as an aerosol spray or a pump spray. In yet another example, the composition can be formulated to be applied using a pre-moistened wipe. In another example, the composition can be formulated as a solid to be rubbed onto the skin of a subject. In another example, the composition is formulated to be delivered by a patch that adheres to the skin of a subject.

[0055] In addition to the plant active component (i.e., the "active" or "active ingredient"), the composition can also include pharmaceutically acceptable additives that are inactive (or "inactive ingredients"), including, but not limited to, excipients, such as diluents and binders; granulating agents; glidants (or flow aids); fillers; lubricants; preservatives; stabilizers; coating agents; disintegrants; fragrances; and pigments. The active ingredient and the pharmaceutically acceptable additives can be combined or compounded as desired to form an individual dose that, when applied topically, provides a desired amount of the active ingredient to a human subject.

[0056] Optionally, the composition can include one or more additional components, such as additives. Suitable additives include those understood in the art, including, but not limited to, moisturizers, emollients, emulsifiers, surfactants, oils, extracts, skin protectants, antiseptics, preservatives, drugs and drug substances, analgesic compounds, antineuralgic compounds, antioxidants, blood circulation promoters, anti-depressant compounds, anti-anxiety compounds, anti-stress compounds, sunscreens, insect repellents, preservatives, exfoliants, fragrances, colorants, fillers, solvents, vehicles, carriers, other types of additives known to those skilled in the art, and combinations thereof. These additives can be used alone or in combination. Generally, the optional additives can be any type used in personal care products and cosmetics.

[0057] Excipients can be further classified into other components. Specifically, excipients for oral solid dosage forms have been classified into the following groups based on their function: diluents, disintegrants, binders, compression aids, granulating agents, glidants, lubricants, controlled release polymers, stabilizers (such as antioxidants, chelating agents, and pH modifiers), film coating polymers, coating agents, vehicles, plasticizers, surfactants, colorants, sweeteners, and flavors.

[0058] In various embodiments, the composition comprises at least one component selected from the group consisting of a binder, a lubricant, a glidant, and combinations thereof. In certain embodiments, the composition includes one or more compounds, including, but not limited to, methylcellulose, hydroxypropyl methylcellulose, ethylcellulose, cellulose acetate phthalate, gum arabic, gums, waxes, glycerol monostearate, acrylic acid polymers and copolymers, methacrylic acid, methyl acrylate, ethyl acrylate, methyl methacrylate, ethyl methacrylate, lactose, calcium sulfate, dibasic calcium phosphate, sugars, microcrystalline cellulose (MCC), starch, sodium starch glycolate, polyvinyl pyrrolidone, polyethylene glycol, and magnesium stearate. Combinations of these components can be used, and these components and other components used in conventional tablets are understood in the art.

[0059] "Diluents" as used herein can be inert substances added to increase the bulk of the composition to bring the tablets to a practical size for compression. Thus, they can also be referred to as fillers. Commonly used diluents include, but are not limited to, microcrystalline cellulose (MCC), wood cellulose, corn starch, modified corn starch, (tri) calcium phosphate, calcium sulfate, lactose, kaolin, mannitol, sodium chloride, dry starch, (powdered) sugar, dextrose, mannitol, sorbitol, and the like. Diluents / fillers can be used alone or in various mixtures and in any amount known in the art for use in oral compositions.

[0060] "Flavorants" as used herein are compounds which are intended to impart a more palatable taste to the composition. Flavorants vary widely in their chemical structure, from simple esters, alcohols and aldehydes to carbohydrates and complex volatile oils. Synthetic flavorants of almost any desired type are now available and are well known in the art. If the astringent, sour or bitter taste derived from the starting material can be inhibited by flavoring or perfuming, then an acidulant (e.g., citric, tartaric, malic, ascorbic acid, etc.), a sweetener (e.g., sodium saccharin, dipotassium glycyrrhizinate, aspartame, stevia, thaumatin, etc.), or a flavorant (e.g., various fruit flavors containing lemon, orange or strawberry oils, and yogurt, mint, menthol, etc.) can be included in the composition. Flavorants can be used alone or in various mixtures and in any amount known in the art for use in oral compositions.

[0061] As used herein, "lubricants" are materials that perform a number of functions in relation to the composition. In certain embodiments, such as tablet manufacture, lubricants perform one or more functions such as improving the rate of flow of the tablet granulation, preventing the tablet material from adhering to the surfaces of the die and punch, reducing interparticulate friction, and facilitating the ejection of the tablet from the die cavity. Examples of suitable lubricants include, but are not limited to, zinc stearate, acacia powder, cocoa butter, carnauba wax, carboxymethylcellulose calcium, carboxymethylcellulose sodium, caropeptide, colloidal silicon dioxide, dry aluminum hydroxide gel, glycerin, magnesium silicate, light anhydrous silicic acid, light liquid petrolatum, crystalline cellulose, hardened oil, synthetic aluminum silicate, sesame oil, flour starch, white beeswax, magnesium oxide, dimethicone, potassium sodium tartrate, sucrose fatty acid ester, glycerin fatty acid ester, silicone, aluminum hydroxide gel, stearyl alcohol, stearic acid, aluminum stearate, calcium stearate, polyoxyl stearate, magnesium stearate, cetyl alcohol, gelatin, talc, magnesium carbonate, precipitated calcium carbonate, corn starch, lactose, hard fat, sucrose, potato starch, hydroxypropyl cellulose, fumaric acid, sodium stearyl fumarate, polyethylene glycol, polyoxyethylene polyoxypropylene glycol, polysorbate, beeswax, magnesium aluminometasilicate, methyl cellulose, Japan wax, glyceryl monostearate, sodium lauryl sulfate, calcium sulfate, magnesium sulfate, liquid petrolatum, phosphoric acid, palmitic acid, and hydrogenated vegetable oil and fat. Lubricants can be used alone or in various mixtures, and in any amount known in the art for use in oral compositions.

[0062] As used herein, "binders" are agents used to impart cohesiveness to powdered materials. Binders, or sometimes called "granulating agents," impart cohesiveness to tablet formulations, which ensures that the tablet remains intact after compression, as well as improve the free-flowing properties by formulating granules of the desired hardness and size. Materials commonly used as binders include starches, such as corn starch and pregelatinized starch; gelatin; sugars, such as sucrose, dextrose, dextran, molasses, and lactose; natural and synthetic gums, such as acacia, sodium alginate, blua moss extract, panwar gum, gum

[0063] As used herein, "coloring agents" are agents that impart a more pleasing appearance to the composition, in addition to aiding the manufacturer in controlling the product during its manufacture and aiding the user in identifying the product. Any approved certified water-soluble FD&C colors, mixtures thereof, or their corresponding lakes can be used to color the tablets. Lakes are groups obtained by adsorbing a water-soluble dye on a hydrated oxide of a heavy metal, thereby obtaining an insoluble form of the dye. The coloring agents can be used alone or in various mixtures and in any amounts known in the art for use in oral compositions.

[0064] Other conventional ingredients that can optionally be present in the composition include preservatives, stabilizers, anti-tacking agents or silicon dioxide flow regulators or glidants, such as silicon dioxide. These ingredients can be used alone or in various mixtures and in any amounts known in the art for use in oral compositions.

[0065] It is recognized that certain components or additives can be categorized under different technical terms and that their classification under a term does not mean that they are limited to that function. If used, one or more additives can be present in the composition in various amounts. Additional ingredients optionally used in the composition are described in U.S. Patent Nos. 5,747,006; 5,980,904; 6,994,874; 7,060,304; 7,247,321; 7,348,034; 7,364,759; 7,700,110; 7,722,904; 8,202,556; 8,916,212; 9,445,975; 9,801,809; 10,307,366; 10,532,024; and 10,537,516; and U.S. Publication Nos. 2006 / 0257509; 2007 / 0224154; 2008 / 0081082; 2008 / 0124409; 2013 / 0302265; 2017 / 0252293; 2017 / 0281666; 2018 / 0200285; 2019 / 0083566; 2019 / 0160117; 2020 / 0171117; 2020 / 0383898; 2021 / 0017240; and 2021 / 0212926; the disclosures of which are incorporated herein in their entirety.

[0066] Methods of administration

[0067] The composition can be administered or applied as desired, daily, several times daily, or in any suitable regimen, to achieve the desired result. In the methods of the present disclosure, the frequency of administration (e.g., oral ingestion) can depend on several factors, including the level of alpha-glucosidase inhibition desired. Typically, the regimen includes ingestion of the composition once or twice daily, including administration in the morning and / or administration in the evening. The amount and / or frequency of administration of the composition can depend on several factors, including the level of desired result and the particular composition.

[0068] The formulations of the present application can be administered topically, internally, or some combination thereof, to achieve improved alpha-glucosidase inhibition. Preferably, the formulations of the present application are administered with an acceptable carrier. For example, the formulations of the present application can be administered topically with an acceptable carrier in the form of a gel, lotion, cream, tonic, emulsion, and the like. As a further example, the formulations of the present application can be administered internally with an acceptable carrier in the form of a pill, tablet, powder, bar, beverage, and the like. Thus, the formulations described herein can be used in a wide variety of finished products, including pharmaceutical products. Preferably, the product is useful for providing alpha-glucosidase inhibition to a mammal.

[0069] When the formulations of the present application are administered orally in liquid form, the liquid can be water-based, milk-based, tea-based, juice-based, or some combination thereof. The solid and liquid formulations for internal administration according to the present application can further comprise a thickening agent, including xanthan gum, carboxymethylcellulose, carboxyethylcellulose, hydroxypropylcellulose, methylcellulose, microcrystalline cellulose, starch, dextrin, fermented whey, soy, maltodextrin, polyols, including sugar alcohols (e.g., sorbitol and mannitol), carbohydrates (e.g., lactose), propylene glycol alginate, gellan gum, guar gum, pectin, tragacanth gum, acacia gum, locust bean gum, gum arabic, gelatin, and mixtures of these thickening agents. These thickening agents are typically included in the formulations of the present application in a content of up to about 0.1%, depending on the particular thickening agent involved and the viscosity effect desired.

[0070] The solid and liquid formulations of the present application can contain and typically contain an effective amount of one or more sweeteners, including carbohydrate sweeteners and natural and / or artificial non-caloric / low-caloric sweeteners. The amount of sweetener used in the formulations of the present application varies, but is typically dependent on the type of sweetener used and the sweetness intensity desired.

[0071] In another example, the formulations of the present application are administered topically in the form of a solution, gel, lotion, cream, ointment, oil-in-water emulsion, water-in-oil emulsion, stick, spray, paste, mousse, tonic, foundation, or other cosmetic and topically suitable form.

[0072] Preferably, the formulations of the present application suitable for topical administration are mixed with an acceptable carrier. The acceptable carrier can variously function to solubilize, carry, dilute, or disperse the ingredients of the composition, and allow for uniform application to the skin surface at an appropriate dilution. The acceptable carrier can also facilitate penetration of the composition into the skin.

[0073] In one example of a formulation for topical application, the acceptable carrier comprises from about 70% to about 99.99% by weight of the total composition. In other examples, the acceptable carrier comprises from about 85% to 99.99% by weight of the total composition. The acceptable carrier can also comprise from about 90% to about 99.99% by weight of the total composition; or from about 99.95% to about 99.999% by weight of the total composition. The acceptable carrier can comprise the balance of the composition in the absence of other cosmetic adjuvants or additives.

[0074] The various ingredients used to practice the present application can or can not be soluble in the acceptable carrier. If all of the ingredients of the formulation are soluble in the acceptable carrier, the vehicle functions as a solvent. However, if all or some of the ingredients of the formulation are not soluble in the acceptable carrier, these ingredients are dispersed in the vehicle by means of, for example, a suspension, emulsion, gel, cream, or paste.

[0075] Thus, it will be apparent to those skilled in the art that the range of possible acceptable carriers is quite broad. For example, the acceptable carrier can be an emulsion, lotion, cream, or tonic. The acceptable carrier can include water, ethanol, butylene glycol, or other various solvents that aid in skin penetration. Some examples of suitable vehicles are described in U.S. Patent Nos. 6,184,247 and 6,579,516, the entire contents of which are hereby incorporated by reference.

[0076] Preferably, the acceptable carrier used to practice the present application comprises water and ethanol. Optionally, the acceptable carrier also contains butylene glycol. For example, the acceptable carrier can comprise 2-5% butylene glycol by weight of the composition. In the practice of the present application, such an acceptable carrier is preferably mixed with 2% by weight of the total composition of the formulation of the present application. In other examples, the acceptable carrier is mixed with 0.001% to 30% by weight of the total composition; 1% to 5% by weight of the total composition; 0.01% to 15% by weight of the total composition; or 0.5% to 1.0% by weight of the total composition of the formulation of the present application.

[0077] However, in general, acceptable carriers according to the present application can include, but are not limited to, any one of the following examples: water; castor oil; ethylene glycol monobutyl ether; diethylene glycol monoethyl ether; corn oil; dimethyl sulfoxide; ethylene glycol; isopropyl alcohol; soybean oil; glycerin; soluble collagen; safflower seed oil; meadowfoam seed oil; mineral oil; squalene; shea butter; borage oil; or rice bran oil; polyquaternium-10; methyl paraben; PEG-8; disodium lauroamphodipropionate; sodium trideceth sulfate; hexylene glycol; sodium methyl cocoyl taurate; lauryl alcohol sulfate TEA salt; lauryl betaine; sodium myristoyl sarcosinate; PEG-150 distearate; anhydrous citric acid; sodium citrate-dihydrate; diazolidinyl urea; disodium EDTA; propyl paraben; polysorbate 60; isopropyl palmitate; octyl palmitate; C12-15 alkyl benzoate; dipropylene glycol dibenzoate; PPG-15 stearyl ether benzoate; isododecane; isoeicosane; squalane; jojoba oil; dimethicone; glyceryl stearate; PEG-100 stearate; cetyl alcohol; butylene glycol; chlorphenesin; fragrance; polyacrylamide; C13-14 isoparaffin; laureth-7; aloe powder; aloe gel, hydroxyethyl acrylate; sodium acryloyldimethyl taurate copolymer; behenyl alcohol; tocopheryl acetate; isodecyl neopentanoate; glyceryl trioctanoate; cetearyl alcohol; cetearyl glucoside; mother-of-pearl extract; biosaccharide gum-1; pentadecalactone; dipropylene glycol; cyclomethicone; PEG / PPG-18 / 18 dimethicone; cyclopentasiloxane; disteardimonium hectorite; SD alcohol 40; phenoxyethanol; ethyl paraben; trimethylsiloxysilicate; triethoxycaprylylsilane; micronized titanium dioxide; titanium dioxide; zinc oxide; iron oxides (yellow; red; black; etc.); octylsilane; sodium chloride; diisopropyl dimer dilinoleate; aluminum hydroxide; stearic acid; polyethelene beads; C12-15 alkyl benzoate; acrylates / C10-30 alkyl acrylate; xanthan gum; sorbitan laurate; panthenol; petrolatum; isopropyl isostearate; dimethicone; arginine; phenoxyethanol; acryloyldimethyltaurate copolymer; isohexadecane; polysorbate 80; hydroxyethyl acrylate; sodium acryloyldimethyl taurate copolymer; octinoxate (octyl methoxycinnamate); oxybenzone; dicaprylyl ether; isodecyl neopentanoate; cetearyl alcohol; cetearyl glucoside; benzyl alcohol; HDI / trimethylhexyllactone crosspolymer; silica; isodecyl neopentanoate; cocoglycoside; C20-22 alkyl phosphate; C20-22 alcohol; palmitoyl proline; palmitoyl magnesium glutamate; sodium palmitoyl sarcosinate; C30-45 alkyl cetearyl crosspolymer; polyacrylate 13; polyisobutene; polysorbate 20; iodopropynyl butylcarbamate;Sodium Magnesium Silicate; Methyl Gluceth-20; Isosorbide Dimethyl Ether; Silica; SD Alcohol 40-B; Salicylic Acid; Cetyl Alcohol Polymyx-20; Fragrance; or Hamamelis.

[0078] Additionally, acceptable carriers for use in the present application can optionally comprise one or more humectants including, but not limited to: dibutyl phthalate; soluble collagen; sorbitol; or sodium 2-pyrrolidone-5-carboxylate. Other examples of humectants useful in the practice of the present application can be found in the CFTA Cosmetic Ingredient Handbook, relevant portions of which are incorporated herein by reference.

[0079] Additionally, acceptable carriers in the present application can optionally comprise one or more emollients including, but not limited to: butane-1,3-diol; cetyl palmitate; dimethicone; glyceryl monoricinoleate; glyceryl monostearate; isobutyl palmitate; isocetyl stearate; isopropyl palmitate; isopropyl stearate; butyl stearate; isopropyl laurate; hexyl laurate; decyl oleate; isopropyl myristate; lauryl lactate; octadecan-2-ol; capryl triglyceride; capric triglyceride; polyethylene glycol; propane-1,2-diol; triethylene glycol; sesame oil; coconut oil; safflower oil; isopentyl laurate; nonoxynol-9; panthenol; hydrogenated vegetable oil; tocopheryl acetate; tocopheryl linoleate; allantoin; propylene glycol; peanut oil; castor oil; isostearic acid; palmitic acid; isopropyl linoleate; lauryl lactate; myristyl lactate; decyl oleate; or myristyl myristate. Other examples of emollients useful in the practice of the present application can be found in the CFTA Cosmetic Ingredient Handbook, relevant portions of which are incorporated herein by reference.

[0080] Additionally, acceptable carriers for use in the present application can optionally comprise one or more penetration enhancers including, but not limited to: pyrrolidones, such as 2-pyrrolidone; alcohols, such as ethanol; alkanols, such as decanol; diols, such as propylene glycol, dipropylene glycol, butylene glycol; surfactants; or terpenes.

[0081] Other acceptable carriers useful in the practice of the present application will be apparent to those skilled in the art and are included within the scope of the present application.

[0082] For example, the acceptable carrier can be a lotion for topical application. The lotion can comprise carbomer 981, water, glycerin, isopropyl myristate, mineral oil, shea butter, stearic acid, ethylene glycol stearate, cetyl alcohol, dimethicone, preservatives, tea, and various ingredients of the formulation of the present application.

[0083] The formulations of the present application can also contain various known and conventional cosmetic adjuvants, so long as they do not deleteriously affect the desired improvements provided by the formulation. For example, the formulations of the present application can further include one or more additives or other optional ingredients well known in the art, which can include, but are not limited to, fillers (e.g., solids, semi-solids, liquids, etc.); carriers; diluents; thickening agents; gelling agents; vitamins, retinoids, and retinols (e.g., vitamin B3, vitamin A, etc.); pigments; fragrances; chemical sunscreens and physical sunblocks; antioxidants and free radical scavengers; organic hydroxy acids; exfoliants; skin conditioners; moisturizers; ceramides, pseudoceramides, phospholipids, sphingolipids, cholesterol, glucosamine, pharmaceutically acceptable penetrants (e.g., n-decylmethylsulfoxide, lecithin organogel, tyrosine, lysine, etc.); preservatives; antimicrobials; amino acids, such as proline, pyrrolidone carboxylic acid, its derivatives and salts, saccharide isomerate, panthenol, buffers with bases such as triethanolamine or sodium hydroxide; waxes, such as beeswax, ozocerite, paraffin wax; plant extracts, such as aloe vera, cornflower, witch hazel, elderflower, or cucumber, and combinations thereof. Other suitable additives and / or adjuvants are described in U.S. Patent No. 6,184,247, the entire contents of which are hereby incorporated by reference.

[0084] The formulations can include additional inactive ingredients, including but not limited to surfactants, cosolvents, and excipients. Surfactants, such as hydrophilic and hydrophobic surfactants, can be included in the formulation. Specific surfactants can be used based on the overall composition of the formulation and the intended delivery of the formulation. Useful surfactants include polyethoxylated (PEG) fatty acids, PEG-fatty acid diesters, PEG-fatty acid monoesters and diester mixtures, polyethylene glycol glycerol fatty acid esters, alcohol-oil transesterification products, polyglycerolated fatty acids, propylene glycol fatty acid esters, mixtures of propylene glycol ester-glycerol esters, glycerol monoesters and diesters, sterols and sterol derivatives, polyethylene glycol sorbitan fatty acid esters, polyethylene glycol alkyl ethers, polysaccharide esters, polyethylene glycol alkyl phenols, polyoxyethylene-polyoxypropylene block copolymers, sorbitan fatty acid esters, lower alcohol fatty acid esters, ionic surfactants, and mixtures thereof.

[0085] The formulations can also include cosolvents, such as alcohols and polyols, polyethylene glycol ethers, amides, esters, other suitable cosolvents, and mixtures thereof. The formulations can also include excipients or additives, such as sweeteners, flavorings, colorants, antioxidants, preservatives, chelating agents, viscosity modifiers, tonicifiers, odorants, opacifiers, suspending agents, binders, and mixtures thereof.

[0086] Generally, the formulations of the present application are applied topically or orally at least once daily for a period of time sufficient to bring about the desired level of improvement in alpha-glucosidase inhibition. Topical or oral application of the formulations of the present application can continue for any suitable period of time. More particularly, within hours to days of the initial application or ingestion, the user can notice an improvement in the symptoms of hyperglycemia or diabetes. It will be appreciated that the frequency of application or ingestion of the formulations of the present application will vary depending on the desired level of improvement. In particular, the degree of relief of symptoms will vary directly with the total amount of composition used.

[0087] Useful dosage forms can be prepared by methods and techniques well understood by those skilled in the art, and can include the use of additional ingredients in the production of tablets, capsules, or liquid dosage forms.

[0088] Industrial applicability

[0089] The present disclosure provides new and useful advanced alpha-glucosidase inhibitors, which include the plant extracts described herein. Such alpha-glucosidase inhibitors can provide potential prophylactic and therapeutic methods for reducing the risk of hyperglycemia, diabetes, or other pathogenic complications resulting from alpha-glucosidase activity. Accordingly, the compositions and methods described herein can be used to inhibit alpha-glucosidase.

[0090] The general series of compositions and products provided by the present disclosure relate to personal care, nutritional, skin care, and nutricosmetic products that utilize such alpha-glucosidase inhibitors, and specific examples include pills and liquids that utilize such alpha-glucosidase inhibitors.

[0091] Alpha-glucosidases are metabolic pathways that break down carbohydrates (oligosaccharides and disaccharides) into monosaccharides and thus absorb glucose. Elevated levels of glucose in the blood (hyperglycemia) is a complication of individuals with type 2 diabetes and can lead to or exacerbate other medical conditions, such as cardiovascular disease. Hyperglycemia can also lead to ketoacidosis. The compositions and methods of the present disclosure provide potential prophylactic and therapeutic methods for reducing the risk of hyperglycemia, diabetes, or other pathogenic complications resulting from alpha-glucosidase.

[0092] The following examples, which illustrate the compositions and methods of the present disclosure, are intended to be exemplary and not limiting of the present disclosure. Example

[0093] Plant water and ethanol extracts were evaluated for their inhibitory effect on alpha-glucosidase. Specifically, two extracts of Lysimachia foenum-gracum were evaluated for their potential to inhibit alpha-glucosidase. As shown in the following table and in the accompanying figures, both extracts exhibited inhibition. The extracts were prepared in the laboratory, but are also commercially available.

[0094] Inhibition of alpha-glucosidase

[0095] To 40 μΐ^of the test substance (extract) was added 40 μΐ^of α-glucosidase solution (0.1 U / mL in PBS) and mixed for 5 minutes. Next, 20 μΐ^of PNPG (2.5 mmol / L) was added to the mixture as a substrate for α-glucosidase and incubated at 37°C for 15 minutes. Then, the reaction was terminated using 100 μΐ^of sodium carbonate solution (0.1 mol / L). Acarbose was used as a control. The absorbance at 405 nm was measured and the inhibitory activity was calculated as follows.

[0096] Determination of inhibition rate

[0097] The absorbance of the incubated solution was measured. The inhibition rate of α-glucosidase was calculated by the following equation:

[0098] Inhibition rate (%)

[0099] where A1 is the absorbance of the mixture of the sample and α-glucosidase, A2 is the absorbance of the mixture of the sample and buffer, A3 is the absorbance of the mixture of the buffer and α-glucosidase, and A4 is the absorbance of the buffer.

[0100] The results are shown in the following table. The average inhibition rate can also be understood with reference to the attached figure.

[0101] Table 1:

[0102]

[0103] * See also Figure 1 (where the X axis is concentration and the Y axis is % inhibition).

[0104] Table 2:

[0105]

[0106] * See also Figure 2 Figure 1 (where the X axis is concentration and the Y axis is % inhibition).

[0107] As shown in the above table, at lower concentrations, the water extract of Cyrtomium fortunei showed higher α-glucosidase inhibition than the 70% ethanol extract, while at higher concentrations, the water extract and the 70% ethanol extract showed similar α-glucosidase inhibition.

[0108] The terms "comprise" (and any grammatical variations thereof such as "comprises" and "comprising"), "have" (and any grammatical variations thereof such as "has" and "having"), "include" (and any grammatical variations thereof such as "includes" and "including") and "contain" (and any grammatical variations thereof such as "contains" and "containing") are open-ended linking verbs. They do not mean "consist" or "consist essentially of." As used herein, the singular forms "a", "an" and "the" include plural referents unless the context clearly dictates otherwise. "Approximately" as used herein is used to reasonably encompass or describe slight variations in a value that are measured by an instrument or caused by sample handling. Such slight variations can be ±0-10, ±0-5, or ±0-2.5% of the value. In addition, the term "approximately" applies to both values when associated with a range of values. Furthermore, the term "approximately" can apply to a value even if not expressly stated, even on an individual basis.

[0109] Generally, as used herein, the hyphenated- or en-dash "to" or "–" is used to indicate a range or a continuum of values. The terms "greater than" and "greater than or equal to" are used interchangeably with the symbol ">" and the symbol ">=" respectively. The terms "less than" and "less than or equal to" are used interchangeably with the symbol "<" and the symbol "<=" respectively. Each of the aforementioned patent applications, patents, and / or patent application publications are herein incorporated by reference in their entirety for all purposes.

[0110] It is to be understood that the following claims are not limited to the specific compounds, compositions or methods described in the detailed description, which can vary somewhat as falling within the scope of the claims. With respect to any Markush groups relied upon herein, it is intended that only the members individually identified in the specification are presented as separately provided. It is also intended each member of such groups be individually identified as the minimum disclosure of the specific embodiments required by 35 U.S.C. § 112, paragraph 6. It is further intended that all combinations of the members of these groups be specifically recited, for example, X1is A, B or C; X2is D, E or F; and X3is G, H or I. It is specifically intended that the claims not be limited to the embodiments and dependencies specifically described in the specification.

[0111] It is also to be understood that any range or sub-range described herein independently and collectively falls within the scope of the appended claims and is understood to describe and cover all sub-ranges included therein, even if not explicitly written out. It is readily apparent to one skilled in the art that the recited ranges and sub-ranges are sufficient to describe and enable various embodiments of the present application, and that such ranges and sub-ranges can be further delineated into related 1 / 2, 1 / 3, 1 / 4, 1 / 5, and so on. By way of example only, the range "0.1 to 0.9" can be further delineated into the lower 1 / 3, i.e., 0.1 to 0.3, the middle 1 / 3, i.e., 0.4 to 0.6, and the upper 1 / 3, i.e., 0.7 to 0.9, each of which independently and collectively falls within the scope of the appended claims and can independently and / or collectively rely on the recited ranges to provide adequate support for specific embodiments within the scope of the appended claims. Moreover, words such as "at least," "greater than," "less than," "not greater than," and the like, in reference to a range or sub-range, are to be understood as including the sub-range and / or upper or lower limit. By way of further example, the range "at least 10" inherently includes the sub-range of at least 10 to 35, the sub-range of at least 10 to 25, the sub-range of 25 to 35, and so on, each of which independently and collectively falls within the scope of the appended claims and can independently and / or collectively rely on the recited ranges to provide adequate support for specific embodiments within the scope of the appended claims. Finally, individual values within a disclosed range can be relied upon and provide adequate support for specific embodiments within the scope of the appended claims. For example, the range "1 to 9" includes individual integers such as 3, as well as individual values (or fractions) containing a decimal point, such as 4.1, each of which can be relied upon and provide adequate support for specific embodiments within the scope of the appended claims.

[0112] The present application has been described in an illustrative manner, and it is to be understood that the terminology used is intended to be in the nature of words of description rather than limitation. Many modifications and variations of the present application are possible in light of the above teachings. The application can be practiced otherwise than as specifically described within the scope of the appended claims. The subject matter of all combinations of the elements from any two or more of the claims below are expressly included in the scope of the claims.

Claims

1. Use of an extract of Saururus chinensis as the sole active ingredient in the manufacture of a medicament for the prevention and / or treatment of diabetes in a subject, wherein the extract of Saururus chinensis consists of one or both of an extract of the root of Saururus chinensis and an extract of the stem of Saururus chinensis, and wherein the extract of Saururus chinensis is obtained by water extraction or alcohol extraction of one or more of the stem and root of Saururus chinensis.

2. Use of an extract of Saururus chinensis as the sole active ingredient in the manufacture of a medicament for the prevention and / or treatment of hyperglycemia in a subject, wherein the extract of Saururus chinensis consists of one or both of an extract of the root of Saururus chinensis and an extract of the stem of Saururus chinensis, and wherein the extract of Saururus chinensis is obtained by water extraction or alcohol extraction of one or more of the stem and root of Saururus chinensis.

3. The use according to claim 1 or 2, wherein the extract of Saururus chinensis is obtained by water extraction of one or more of the stem and root of Saururus chinensis.

4. The use according to claim 1 or 2, wherein the extract of Saururus chinensis is obtained by alcohol extraction of one or more of the stem and root of Saururus chinensis.

5. The use according to claim 4, wherein the extract of Saururus chinensis is obtained by ethanol extraction of one or more of the stem and root of Saururus chinensis.

6. The use according to claim 1 or 2, wherein the extract of Saururus chinensis is completely free of components obtained from non-stem-based plant material and non-root-based plant material of Saururus chinensis.

7. The use according to claim 1 or 2, wherein the medicament is further defined as an oral medicament formulated for oral administration to a subject.

8. The use according to claim 7, wherein the medicament further comprises a pharmaceutically acceptable additive.

9. The use according to claim 8, wherein the pharmaceutically acceptable additive is not naturally occurring.

10. The use according to claim 1 or 2, wherein the medicament is further defined as a topical medicament formulated for topical administration to a subject.

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