KR102024813B1 - Composition for fat dissolution - Google Patents

Abstract

According to an aspect of the present invention, as a composition for lipolysis, provided is the composition for lipolysis in which every 100 ml of the composition for lipolysis, 500 to 750 IU of hyaluronidase, 250 to 500 mg of aminophylline, and 200 to 600 mg of the Melilotus extract are contained.

Description

Composition for fat decomposition {Composition for fat dissolution}

The present invention relates to a composition for lipolysis, and more particularly, to a composition for lipolysis that is effective in decomposing topical subcutaneous fat or cellulite to reduce weight and improve body shape.

Mesotherapy is a compound word of 'meso', which means middle, and 'therapy,' which means treatment, and is a combination of proven drugs, plant extracts, vitamins, minerals, and other nutritional ingredients. Refers to a procedure administered to the interlayer of skin such as intradermal or subcutaneous using a syringe or the like. This method was invented by Dr. Michel Pistor, a French doctor in 1952, and has been used to treat blood circulation, chronic pain, and sports damage. It is also widely used in the field of beauty such as anti-aging, hair loss prevention.

The composition used for mesotherapy may include a component that degrades fat, and examples thereof include hyaluronidase. Hyaluronidase is a component found in venom and leech venom. In mesotherapy, a method of injecting a composition containing hyaluronidase into subcutaneous fat, cellulite, and the like is widely used. Hyaluronidase injected into the human body can break down fat cells and correct their body shape.

However, side effects such as hypersensitivity reactions, dizziness, pain, swelling, itching, erythema, etc. often occur in a patient to which hyaluronidase has been administered, and especially when a high dose of hyaluronidase is administered to the skin of the patient. There are also serious side effects such as local depression, sagging skin and wrinkles.

In addition, inflammation or edema often occurs during the procedure using a conventional lipolytic composition.

Thus, the present inventors in the lipolysis composition containing hyaluronidase through the present specification, the effect of weight loss, body shape, and the like to ensure the same or more, but caused by the use of the conventional lipolysis composition It proposes a composition for lipolysis that can minimize side effects.

Korea Patent Registration No. 10-1706549 (2017.02.08)

The present invention has an object to solve the above problems of the prior art.

It is another object of the present invention to provide a composition for lipolysis that increases the lipolysis effect and minimizes the side effects.

Representative configuration of the present invention for achieving the above object is as follows.

According to an aspect of the present invention, as a composition for lipolysis, hyaluronidase 500 IU to 750 IU, aminophylline 250 mg to 500 mg, and melilotusx 200 mg to every 100 ml of the composition for lipolysis. There is provided a composition for lipolysis comprising 600 mg.

According to the present invention, it is possible to provide a composition for lipolysis that increases the lipolysis effect but minimizes side effects.

1 is a view showing a change in lipolysis effect according to the change in the content of each component in each lipolysis composition according to the experimental examples of the present invention.
Figure 2 is a table showing the change in the lipolysis effect according to the change in the content of each component in each lipolysis composition according to the experimental examples of the present invention in a specific numerical value.
Figure 3 is a table showing the evaluation of the drug adverse reaction of the subject according to the change in the content of each component in each fat decomposition composition according to the experimental examples of the present invention as a specific value.

DETAILED DESCRIPTION The following detailed description of the invention refers to the accompanying drawings that show, by way of illustration, specific embodiments in which the invention may be practiced. These embodiments are described in sufficient detail to enable those skilled in the art to practice the invention. It should be understood that the various embodiments of the present invention are different but need not be mutually exclusive. For example, certain shapes, structures, components, and characteristics described herein may be embodied by changing from one embodiment to another without departing from the spirit and scope of the invention. In addition, it is to be understood that the environment or order in which each component is positioned or disposed in each embodiment, or a mixture, reaction, or the like between the individual components may be changed without departing from the spirit and scope of the present invention. Accordingly, the following detailed description is not to be taken in a limiting sense, and the scope of the present invention should be taken as encompassing the scope of the claims of the claims and all equivalents thereto. Like reference numerals in the drawings indicate the same or similar elements throughout the several aspects.

Hereinafter, various preferred embodiments of the present invention will be described in detail with reference to the accompanying drawings so that those skilled in the art can easily implement the present invention.

Composition of the composition for lipolysis according to the present invention

Composition for lipolysis according to an embodiment of the present invention is at least a part of physiological saline, hyaluronidase, aminophylline (aminophylline), L-carnitine (L-carnitine), pheniramine and melilotus extract (melilotus extract) It may include. In the following, it is assumed that the total amount of the lipolytic composition administered to the patient is 100 ml, and the dose of each component included in every 100 ml of the composition will be exemplified.

According to one embodiment of the present invention, in the composition for lipolysis, saline may be used as a solvent. Physiological saline has a salt concentration of 0.9% that is the same as that of human blood, and unlike ordinary water, physiological saline does not cause osmotic pressure changes even when directly injected into blood vessels. It is a well-known substance used.

Hyaluronidase according to an embodiment of the present invention may act to break down the fibrous tissue band formed between the fat lobule of cellulite. More specifically, it is possible to hydrolyze the binding of D-gluronic acid and N-acetyl-D-glucosamine present in hyaluronic acid, chondroitin and chondroitin sulfate. Through this, hyaluronidase can reduce the degree of cell binding and increase the permeability of connective tissue, thereby promoting the diffusion of the injection solution or topical exudate administered together.

However, in the case of hyaluronidase, increasing the dosage to increase the lipolytic effect, antibodies that neutralize it may occur, and dimples that often change the surface of the skin unevenly occur. have.

Therefore, in the present invention, in order to enhance the lipolysis effect, instead of the method of administering a single component of hyaluronidase in a high dose (1500 IU; based on 100 ml of the composition), the monolithic hyaluronidase is increased while the lipolysis effect is increased. In order to minimize the above side effects that may occur in the course of administration, the method of limiting the dose of hyaluronidase per 100 ml of the composition to 500 IU ~ 750 IU and devised a method of additionally using other ingredients.

The composition for lipolysis according to one embodiment of the present invention may include aminophylline as described above. Aminophylline is understood to be able to inhibit PDE (PhosphoDiEsterase) to increase cyclic Adenosine MonoPhosphate (cAMP) and to promote lipolysis by inhibiting R-site adenosine receptor. However, even in the case of aminophylline may cause side effects such as pain, itching, heat, redness, etc., in the lipolysis composition according to an embodiment of the present invention, the amount of aminophylline per 100 ml of the composition is limited to 250 mg to 500 mg At the same time, it is possible to minimize the side effects by adding peniramine and / or melillotus extract as described below.

Lipid decomposition composition according to an embodiment of the present invention may include L-carnitine as described above. L-carnitine can function as a transporter that introduces fatty acids into the mitochondria (which play a role in energy production in the cell), which means that when L-carnitine attaches to the mitochondria, it produces ATP, which is an energy source. Becomes Thus, L-carnitine may promote the energization of fatty acids to reduce body fat. However, when L-carnitine is administered at a predetermined dose or more, it may cause side effects such as nausea, vomiting and diarrhea. Therefore, in order to minimize such side effects, the dose of L-carnitine should be 1000 mg per 100 ml of the composition. It may be desirable.

According to one embodiment of the invention, the composition for lipolysis may further comprise choline alfoscerate. Choline alfoscerate may act to promote lipolysis, ie this may eliminate the side effects of conventional Phosphhatidyl Choline (PPC) and may aid in the degradation of cellulite. For reference, choline alfoscerate acts on dopamine receptors as a drug used in secondary symptoms caused by cerebrovascular defects and degenerative or degenerative cerebral stromal mental syndrome. Choline alfoscerate may be adjusted according to the content ratio of the components constituting the composition for lipolysis, but preferably 1000 mg per 100 ml of the composition may be appropriate.

As described above, the composition for lipolysis according to an embodiment of the present invention may include aminophylline, L-carnitine and choline alfoscerate in addition to hyaluronidase, thereby ensuring a lipolytic effect, but not including hyaluronidase. High doses of a single agent may reduce the frequency and extent of side effects that may occur.

However, the present inventors have side effects such as inflammation, edema, etc., which may still occur even if a procedure for lipolysis is performed using the lipolysis composition consisting of the aforementioned components, namely, hyaluronidase, aminophylline, L-carnitine, and the like. To minimize this, it has been found that pheniramine and / or melilotusx can be added to the composition.

According to one embodiment of the present invention, pheniramine is an antihistamine preparation having an anticholinergic effect and can be used to alleviate the reaction of allergy or inflammation. In the present embodiment, antihistamines containing peniramine may be adjusted according to the content ratio of the components constituting the composition for lipolysis, but preferably 1 mg per 100 ml of the composition may be appropriate.

According to one embodiment of the present invention, melilotox extract contains coumarin, flavonoids, etc. as an extract of the legumes, with the effect of anti-inflammatory action, increased peripheral blood circulation, promoting lymphatic drainage Edema reduction.

However, the present inventors have newly discovered that the lipolytic composition including melilothex is superior to the lipolytic composition not containing the same by a sufficiently significant difference in terms of the lipolytic effect. In other words, melillotus X contained in the composition for lipolysis seems to not only relieve side effects but also contribute to maximizing lipolysis effect.

Hereinafter, the frequency of the effects of lipolysis according to the change in the content of each component in the lipolysis composition according to an embodiment of the present invention described above will be described in detail.

Confirmation regarding the effects of the present invention

1 and 2 is a view showing a change in lipolysis effect according to the change in the content of each component in the composition for lipolysis according to the experimental examples of the present invention and a table showing this as a specific value. Figure 3 is a table showing the evaluation of the drug adverse reaction of the subject according to the change in the content of each component in each fat decomposition composition according to the experimental examples of the present invention as a specific value.

Experimental Examples 1 to 15 of the present invention was conducted in 75 abdominal obesity patients with BMI 25 kg / m ² or more of adult men and women 19 years or older. In the test method, five subjects were assigned to each experimental group, and the subjects in each group were administered a total of four times at a weekly interval of 100 ml to the abdomen for the lipolysis composition of each experimental example shown in FIG. 2.

The lipolytic effect of FIG. 2 was confirmed by measuring the abdominal circumference of the subject. Here, the abdominal circumference of the subject was measured before administration of the composition for lipolysis and when 1 week, 2 weeks, and 4 weeks had elapsed since the end of four administrations. The change in abdominal circumference was described as the mean and standard deviation at each measurement time point.For the statistical analysis and verification method, the non-parametric method Wilcoxon rank sum test was applied using R, the statistical software, and the verification interval for reliability was 95%. Decided. Evaluation of the adverse drug reaction shown in FIG. 3 relates to the frequency of adverse reactions confirmed by questionnaire and examination of the subject after administration of the lipolytic composition to the subject.

A description with reference to FIGS. 1 to 3. Looking at the various experimental examples, the increase in the dose of hyaluronidase in the lipolysis composition improved the decrease in the abdominal circumference to a significant extent. Specifically, in Experiments 4 to 6, the abdominal circumference was measured while changing the dose of hyaluronidase while maintaining the dose of melilotusx at 0 mg and the dose of aminophylline at 500 mg. As a result, Experimental Example 4 (for administration of 500 IU of hyaluronidase) and Experimental Example 5 (for administration of Hyaluronidase 750 IU) and Experimental Example 5 (for administration of Hyaluronidase 750 IU) And the average difference in abdominal circumferential decrease in Experimental Example 6 (for hyaluronidase 1500 IU administration) was 1.8 cm and 2.2 cm, respectively, and their nonparametric tests showed p-values of [0.007937] and [0.007937]. Here, the average difference in abdominal circumference decrease is calculated by comparing the values measured at the time of 4 weeks. Therefore, below, we will look at the average difference with the measured value at the time of 4 weeks.

In Experiments 7 to 9, only the dose of hyaluronidase was changed while maintaining the dose of melilotusx at 200 mg and the amount of aminophylline at 500 mg. As a result, the seventh example (Halu) In case of administration of 500 mg of IU) and Experimental Example 8 (in case of administration of hyaluronidase 750 IU) and Experimental Example 8 (in case of administration of hyaluronidase 750 IU) and Experimental Example 9 (hyaluronidase) The mean difference in abdominal circumferential reduction in the case of 1500 IU administration) was 1.5 cm and 2.1 cm, respectively, and their nonparametric tests showed p-values of [0.007937] and [0.007937], respectively.

Experimental Examples 1 to 3 (Experiments of 400 mg and 500 mg of melolotosex and aminophylline respectively) and Examples 10 to 12 (Experiments of melolotusx and aminophylline respectively) In the experimental examples set at 600 mg and 500 mg), as the dose of hyaluronidase was increased, the abdominal circumferential decrease was significantly improved.

However, in the case of hyaluronidase, a serious side effect such as skin depression may occur when the subject is administered a predetermined dose or more. Referring to FIG. 3, in the experimental examples (third, sixth, ninth, and twelfth experiments) in which the dose of hyaluronidase was 1500 IU, the frequency of skin depression was considerably high. . In contrast, in the remaining experiments (experiments where the dose of hyaluronidase was 750 IU or less), the incidence of skin depression was much lower. Thus, in order to minimize serious side effects, it may be necessary to limit the dose of hyaluronidase, and specifically, it may be desirable to limit the dose of hyaluronidase to 750 IU or less.

In Examples 13, 14, 2, and 15, the lipolytic effect also increased as the dose of aminophylline increased. Specifically, in these experimental examples, only the dose of aminophylline was changed while the doses of melillotusx and hyaluronidase were maintained at 400 mg and 750 IU, respectively. Experimental results: Experimental Example 13 (for 0 mg aminophylline) and Experimental Example 14 (for 250 mg aminophylline), Experimental Example 14 (for 250 mg aminophylline) and Experiment 2 (500 mg aminophylline) Dosing), and the mean difference in abdominal circumferential reduction in Experiment 2 (for 500 mg aminophylline) and Example 15 (for 750 mg aminophylline) was 1.6 cm, 2 cm and 0.2 cm, respectively. The p-values were [0.007937], [0.007937] and [0.6905]. In other words, as the dose of aminophylline was increased, the lipolytic effect of the lipolytic composition also increased. In the third case, however, the statistical significance could not be secured.

However, in the fifteenth experimental example with a dose of aminophylline of 750 mg, the frequency of pain of VAS 3 or more was significantly higher than that of other experimental examples. Thus, as with hyaluronidase, it may be necessary to limit the content of aminophylline in order to minimize side effects, and it may be desirable to limit the dose of aminophylline to 500 mg or less.

As described above, in the case of hyaluronidase and aminophylline, as the dose is increased, the effect of lipolysis increases, but there is a problem that side effects become serious. Thus, as described above, the present inventors have invented a composition for lipolysis that can maximize the lipolysis effect while minimizing side effects by including melillotus x in the composition for lipolysis.

According to the experimental results and a description thereof, which will be described later, it can be proved that melilotusx increases the lipolytic effect of the lipolytic composition. Specifically, in the fourth experimental example, the seventh experimental example, the first experimental example, and the tenth experimental example, only the dose of melilotusx was changed while the doses of hyaluronidase and aminophylline were maintained at 500 IU and 500 mg, respectively. . As a result, the average difference in abdominal circumferential decrease between the fourth experimental example (in the case of the administration of melilotusx 0 mg) and the seventh example (in the case of the administration of melilotusx 200 mg) was 1.8 cm, and Wilcoxon rank sum The test showed a significant difference (p-value = [0.007937]). In addition, the average difference in abdominal circumferential decrease between Experimental Example 7 (for 200 mg of Melillotus X) and Experimental Example 1 (for 400 mg of Melillotus X) was 1.5 cm (p-value = [0.01587]), the average difference between the abdominal circumferential reduction of Experimental Example 1 (for 400 mg of Melillotus X) and Experimental Example 10 (for 600 mg of Mellotus X) was 1.3 cm (p- value = [0.007937]).

In Examples 5, 8, 2, and 11, only the dose of melilotusx was changed while maintaining the doses of hyaluronidase and aminophylline at 750 IU and 500 mg, respectively. As a result, the fifth experimental example (in the case of the administration of melilotusx 0 mg) and the eighth experiment (in the case of the administration of melilotusx 200 mg), and the eighth experiment (in the case of the administration of melilotusx 200 mg) and the second In the experimental example (in the case of melillotusx 400 mg administration), the average difference in abdominal circumferential reduction was 1.5 cm and 2 cm, respectively, and the non-parametric test showed that all p-values were [0.007937], which means the above difference. It was a difference. However, the average difference in abdominal circumferential decrease was not large in Experimental Example 2 (for 400 mg of mellitus extract) and Experimental Example 11 (for 600 mg of mellitus extract).

In Experiments 6, 9, 3, and 12, only the dose of melilotusx was changed while maintaining the doses of hyaluronidase and aminophylline at 1500 IU and 500 mg, respectively. Experimental Example 6 (in the case of administration of melilotus extract 0 mg) and Experimental Example 9 (in the case of administration of melilotus extract 200 mg), Experimental Example 9 (in the case of administration of melilotus extract 200 mg) and Experimental Example 3 ( In the case of the administration of melilotusx 400 mg), and in the third experimental example (for 400 mg of melilotusx) and the 12th experimental example (for 600 mg of melilotusx), the average difference in abdominal circumference was 1.4, respectively. cm, 2.2 cm and 2.1 cm, and their assay p-values were [0.1508], [0.007937] and [0.03175], respectively.

As can be seen from the above experimental results, that is, the experimental results of the experimental examples in which only the dose of melillotus extract is changed, the meliolysis extract contained in the lipolytic composition directly or indirectly affects the lipolytic effect of lipolytic effect. It seems clear that it raises significantly. In addition, in the experimental examples including melittoxx, the frequency of side effects such as redness, itching, edema, etc. was relatively lower than in the experimental examples without the same (the fourth to sixth experimental examples).

Therefore, the composition for lipolysis according to one embodiment of the present invention includes less than 750 IU of hyaluronidase and less than 500 mg of aminophylline per 100 ml in order to minimize side effects. Minimize side effects while maximizing effectiveness. In particular, as can be seen in the first to third experimental examples and the seventh to fifteenth experimental example, it may be preferable to include meliloth extract to 200 mg to 600 mg per 100 ml of the composition.

Claims (4)

As a composition for lipolysis,
Every 100 ml of the dose of the lipolysis composition,
Hyaluronidase 500 IU ~ 750 IU,
Aminophylline 250 mg to 500 mg,
Melillotus X 200 mg to 600 mg to reduce the side effects due to the hyaluronidase and the aminophylline while increasing the lipolytic effect of the lipolytic composition
Lipolysis composition comprising a. The method of claim 1,
Using saline as a solvent
Lipolytic composition. The method of claim 1,
Further comprising at least one of L-carnitine 1000 mg and choline alfoscerate 1000 mg
Lipolytic composition. The method of claim 1,
Further comprising 1 mg of antihistamines containing pheniramine
Lipolytic composition.

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