KR20160050143A - Pharmaceutical composition comprising extract of lysimachia foenum-graecum hance for the prevettion or treatment of obesity - Google Patents

Abstract

The present invention relates to a pharmaceutical composition for treating obesity, containing a Lysimachiae Foenum-graeci Herba extract, sugar, or sugar alcohol. More specifically, disclosed is a pharmaceutical composition which does not contain a surfactant.

Description

FIELD OF THE INVENTION The present invention relates to a composition for treating obesity,

The present invention relates to a composition for the treatment of obesity, which comprises an extract of Youngran Scent as an active ingredient. More particularly, the present invention relates to a composition for treating obesity, which comprises an ethanol extract of Yeongran Flavor. The present invention relates to a pharmaceutical composition optimized for the effect of treating obesity.

Lysimachia foenum-graecum Hance refers to a biennial plant belonging to the primulaceae, which is also called an influenza, a poison, a herb, or an influenza. It can be divided into stems and leaves, and the stems grow to about 40 to 70 cm. The leaves are folded to about 4 to 6 cm, And a long petiole.

This Korean spirit scent has been used as a pest repellent because of its strong fragrance. It has been used as a remedy for colds and headaches because it has been known as a pesticide eliminating agent, Salt, toothache, diarrhea, or oil well.

The present inventor's patent application No. 10-2014-33833 discloses that, in addition to inhibiting adipocyte differentiation induced by Youngran's aroma, adipocyte B is also excellent in obesity-induced rats As a result of the follow-up study by the inventor of the present invention, it has been found that a composition containing the extract of Youngran Scent as an active ingredient and having the prescription and content as defined in the present invention, The effect is optimized, leading to the present invention.

Korean Patent Application No. 10-2014-33833

It is an object of the present invention to provide a pharmaceutical composition containing an extract of Youngran Scent as an active ingredient and exhibiting an anti-obesity effect at the maximum.

Disclosed is a pharmaceutical composition for treating obesity, which comprises an extract of Youngran Scent as an active ingredient and contains a sugar alcohol, but does not contain a surfactant.

According to the present invention, it is possible to provide a pharmaceutical composition for treating obesity in which the effect of treating obesity is maximized.

The terms and abbreviations used herein have the meanings given below.

The term "treatment" is defined to include prevention, reduction, interruption, or reversal of the progression or severity of the symptom or symptom being treated. Thus, the present invention suitably includes both medical and / or prophylactic administration.

The term "effective amount" means the amount of the pharmaceutical preparation effective in the treatment of the desired condition or symptom. An effective amount of a Korean herb extract for treating or preventing obesity means an amount sufficient to stop the progression of the obesity of the patient and to maintain it.

The term "lubricating" means a pharmaceutically acceptable formulation commonly used in the art as a lubricant or lubricant in the manufacture of solid pharmaceutical preparations. Nonlimiting examples of such lubricants include but are not limited to talc, magnesium stearate, calcium stearate, stearic acid, colloidal silicon dioxide, calcium silicate, starch, mineral oil, wax, glyceryl behenate, polyethylene glycol, sodium benzoate, sodium acetate, Sodium aryl fumarate, and hydrogenated vegetable oil. The lubricant is preferably selected from the group consisting of magnesium stearate, sodium stearyl fumarate and stearic acid. The lubricant is most preferably magnesium stearate.

The term " solid oral dosage form "is used in its ordinary sense to refer to a solid pharmaceutical product to be administered orally. Solid oral dosage forms will be understood by those skilled in the art to include formulations such as tablets and capsules.

The term "diluent" means a compound commonly used in pharmaceutical preparations to render it bulky for the production of tablets of actual size. Non-limiting examples of water-soluble diluents include sugars such as lactose, sucrose and dextrose, polysaccharides such as dextrates and maltodextrins, polyols such as mannitol, xylitol and sorbitol and cyclodextrins, In the invention, sugar or sugar alcohol is used as a diluent.

The composition containing a single component as an active ingredient and the composition containing the natural extract as an active ingredient differ from each other in consideration of actual formulation. In general, in the case of a single component, its physicochemical properties can be assessed on a uniform basis, for example, whether it is soluble, water soluble, stable at a certain pH, and furthermore, depending on the excipient, It is easy to understand whether it changes or not.

However, in the case of a natural product extract, a mixture of single components having different physicochemical properties is often used, and the placenta among them is often an unknown compound which is not identified. Therefore, unexpected disadvantage .

In the case of Youngran Scent Extract, since it is insoluble in water itself, means for solubilizing it are required. For example, Korean Patent Application No. 10-2014-33833 discloses the use of anionic, cationic or amphoteric surfactant .

However, according to the study of the present inventors, it has been found that when a surfactant is used in a pharmaceutical composition containing Youngryung scent as an active ingredient, the gastric barrier may be damaged, and in particular, The inventors of the present invention have found that it is preferable not to use a surfactant as much as possible and that the effect of treating the obesity treatment of the Yeongran extract is maximized. Therefore, it has been found that, when the formulation means including the specific sugar or sugar alcohols are added, the solubilization of the Korean spirit flavor becomes possible and the effect of treating obesity can be maximized without adding a surfactant . Hereinafter, the composition according to the present invention will be described in detail.

In order to prepare the Yeongran scent extract used in the present invention, it is necessary to dry Yeongran scent. The drying method of the Korean scent incense is not particularly limited, but the drying can be performed in the shade so that native compounds contained in the Korean scent are not denatured by an external strong light source. The dried Youngran Scent is crushed into an appropriate form for maximizing the extraction efficiency and the degree of crushing, that is, the size of the Youngran Scent, is independent of the change in the chemical properties of the extract. The drying may be performed at room temperature, and the drying period is not particularly limited, but is preferably about several days.

The aliphatic alcohol having 1 to 6 carbon atoms can be used for the extraction from the dried Korean marble incense, and more preferably, methanol or ethanol can be used. The extraction can be carried out using any method. However, the high temperature extraction method such as hot water extraction may cause denaturation or destruction of the compound contained in the leaves of Youngryung scent, and it may be preferable to extract at low temperature. The filtration can be performed by any method, for example, a filter paper, a vacuum filtration, a syringe filter, or the like can be used. Concentration after filtration can be carried out by any method. For example, a method of concentration under reduced pressure at a temperature of 40 ° C or lower can be used.

In preparing the pharmaceutical composition using the extract of Yeongran Flavor prepared as described above as an active ingredient, conventional formulation means can be used, but in the present invention, those containing sugar or sugar alcohol and containing no surfactant .

That is, the diluent used in the present invention provides a suitable volume for the formulation and is present in the formulation in an amount sufficient to effect tablet preparation, and preferred examples of the aqueous diluent include about 50 to about 85 wt%, more preferably about 50 ≪ / RTI > to about 75% by weight of the composition. The sugar or sugar alcohol used in the present invention may be selected from the group consisting of xylitol, mannitol, isomalt, sorbitol, maltitol, refined sugar, lactose, inositol, erythritol, fructose, trehalose, ribitol, arabitol, galactitol, lactitol and maltotritol ≪ / RTI > Particularly, xylitol is preferable, and when xylitol is used, the solubilization and bioavailability of Korean herb extract are increased, and the effect of treating obesity is maximized.

A binder may be used in the composition of the present invention. The binder is provided in an amount sufficient to act to support the extract and the excipient together in the tablet. In the case of powder formulations, the binder facilitates powder preparation and handling and enhances the stability of the active compound.

Preferred binders usable in the present invention are, for example, cellulose derivatives, including hydroxypropyl cellulose and hydroxypropyl methylcellulose. Non-limiting examples of other cellulose derivatives include hydroxyethylcellulose and hydroxybutylmethylcellulose. Other non-limiting binding agents include povidone. The amount of binder present in the formulation is preferably present in an amount of from about 1 to about 5 weight percent based on the weight of the formulation.

A disintegrant may be used in the composition of the present invention. Croscarmellose sodium and crospovidone promote disintegration of formulations, especially tablet dosage forms, after administration and upon contact with water. Croscarmellose sodium and crospovidone are particularly advantageous when used in an amount of about 3 to about 15% by weight, preferably about 3 to about 10% by weight, based on the weight of the formulation.

In the present invention, a lubricant (or a lubricant) may be used. The lubricant is provided in an amount sufficient to reduce die wall frictional force when compressing the formulation into tablet. Preferably, the lubricant is magnesium stearate present in an amount of about 0.25 to about 2.0 weight percent based on the weight of the formulation. Lubricants also facilitate handling of dry powder formulations of the formulation.

On the other hand, the present invention does not use a surfactant. According to research conducted by the present inventors, it has been found that when a surfactant is used, it is helpful to solubilize a Korean spirit flavor. However, there is a fear that gastrointestinal side effects may occur And it was found that the treatment effect of obesity could be lowered. In addition, in the present invention, the optional additional ingredients, such as coloring agents or flavoring agents, can be incorporated into the formulation in an amount sufficient to perform the intended function without adversely affecting the tablet or powder formulation prepared using the formulation.

In a preferred embodiment, the relative proportions (% by weight) of the formulation components are as follows.

Yeongran Scent Extract 0.1 to 30% Xylitol 30 to 80% Binder 1 to 5% Croscarmellose sodium 1 to 5% Magnesium stearate 0.5 to 2% Microcrystalline cellulose 1 to 5%

In addition to this, the composition of the present invention may include other medicinally acceptable carriers, including surfactant extracts, sugars or sugar alcohols, and not including surfactants.

The composition of the present invention can be used as a composition for preventing and treating obesity, a medicine, a food or a food additive, and can be administered orally or parenterally when it is used as a medicine. The formulation of the composition can be variously determined in consideration of the method of use and effectiveness.

Hereinafter, a composition including the extract of Yeongran Flavor according to an embodiment of the present invention will be described with reference to specific examples. However, the technical idea of the present invention is not limited by the following embodiments.

Production Example 1_ Preparation of Youngran Scent Extract

800 g of pH 3 ethanol, 800 ml of pH 8 ethanol and 800 ml of ethanol of pH 11 were added to 100 g of Lysimachia foenum-graecum pulverized powder, respectively, and they were completely immersed in each extraction solvent and extracted with reflux at room temperature. Each of the Korean herb extracts prepared by the above extraction method was concentrated under reduced pressure using a vacuum concentrator to obtain dry powders of Youngran Scent Extract.

EXAMPLES 1 TO 4 Preparation of Pharmaceutical Compositions Containing Extracts of Youngran Scent

A pharmaceutical composition comprising the Youngran Scent Extract having the prescription set forth in Table 2 below was prepared. Purified water, USP, was used for the preparation of tablets. Water was removed during the process and a minimum amount remained in the final product. Tablets were prepared using a wet granulation method. A step-by-step description of the process follows. After extracting the Korean herb extract and the excipient, the Korean herb extract was dry-mixed with xylitol (or mannitol, lactose, erythritol), hydroxypropylmethylcellulose, and croscarmellose sodium. The resulting powder mixture was granulated with an aqueous solution of hydroxypropyl methylcellulose using Powrex or other high shear granulator. Additional water can be added to reach the desired end point. The mill was used to break up the wet granulate mass and promote drying. The wet granulation was dried using a fluid bed dryer or a drying oven. After drying these materials, they can be sorted by size to remove large aggregates. After mixing magnesium stearate, the mixed granules were compressed into tablets using a rotary compressor. If necessary, the core tablets were film coated with an aqueous suspension of the appropriate color mixture in a coating pan (e.g., Accela Cota). The coated tablets were lightly dusted with talc to improve tablet handling properties.

Example 1 Example 2 Example 3 Example 4 Yeongran scent extract 100mg Yeongran scent extract 100mg Yeongran scent extract 100mg Yeongran scent extract 100mg Xylitol 200mg Mannitol 200 mg Lactose 200mg Erythritol 200 mg HPMC 10 mg HPMC 10 mg HPMC 10 mg HPMC 10 mg Croscarmellose sodium 5mg Croscarmellose sodium 5mg Croscarmellose sodium 5mg Croscarmellose sodium
5 mg Magnesium stearate 2 mg Magnesium stearate 2 mg Magnesium stearate 2 mg Magnesium stearate 2 mg

Preparation of Comparative Examples 1 to 4

Except that the microcrystalline cellulose was used instead of the sugar or the sugar alcohol, and various surfactants were used. The prescription is shown in Table 3 below.

Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Yeongran scent extract 100mg Yeongran scent extract 100mg Yeongran scent extract 100mg Yeongran scent extract 100mg Microcrystalline Cellulose 200 mg Microcrystalline Cellulose 200 mg Microcrystalline Cellulose 200 mg Microcrystalline Cellulose 200 mg HPMC 10 mg HPMC 10 mg HPMC 10 mg HPMC 10 mg Croscarmellose sodium 5mg Croscarmellose sodium 5mg Croscarmellose sodium 5mg Croscarmellose sodium
5 mg Magnesium stearate 2 mg Magnesium stearate 2 mg Magnesium stearate 2 mg Magnesium stearate 2 mg Sodium lauryl sulfate 10 mg Docusate sodium 10 mg Poloxamer 10 mg

Modifications and variations of the above embodiments are within the scope of the present patent, unless they depart from the spirit of the present invention.

A preferred pharmaceutical composition is provided which contains an extract of Longran fragrance as an active ingredient.

Claims (3)

A pharmaceutical composition for the treatment of obesity, which comprises a Korean herb extract, a sugar or sugar alcohols, and which does not contain a surfactant. 2. The pharmaceutical composition according to claim 1, wherein the sugar or sugar alcohol is selected from the group consisting of xylitol, mannitol, lactose and erythritol. 3. The pharmaceutical composition according to claim 1 or 2, wherein the pharmaceutical composition comprises a scent extract, xylitol, sodium croscarmellose and magnesium stearate.