Injection composition for lipolysis

Abstract

The present invention relates to an injection composition for lipolysis, which is safe and effective, and more specifically, to an injection composition for lipolysis, which comprises: one or more compounds selected from the group consisting of hyaluronidase and pentoxifylline, and one or more compounds selected from the group consisting of hyaluronidase, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline, pentoxifylline and pentoxifylline. 5 to 10% (v / v) of carnitine (Carnitine); and lidocaine (Lidocaine); and normal saline. As a composition having both safety and efficacy, the injection composition for lipolysis of the present invention has an excellent lipolysis effect, does not cause a yo-yo phenomenon over time, and thus has a characteristic of not causing side effects such as skin depression.

Description

Technical Field

[0001] This invention relates to an injectable composition for lipolysis that combines safety and efficacy, and more specifically, to an injectable composition for lipolysis comprising: one or more compounds selected from hyaluronidase and pentoxifylline; 5-10% (v / v) of carnitine; lidocaine; and physiological saline. Background Technology

[0002] According to a report by the World Health Organization (WHO), since 1975, obesity rates have increased dramatically, primarily in high-income countries, and South Korea has shown a similar trend. With South Korea's rapid economic development and improved living standards, dietary habits have changed accordingly. However, simultaneously, due to reduced physical activity and increased consumption of high-calorie foods, the obesity rate has continued to rise. This increase in the obese population has transcended a simple physical problem, bringing economic, social, and cultural burdens. As a result, the treatment costs for various obesity-related diseases have increased significantly. Currently, the economic burden associated with obesity treatment is estimated to be in the billions of dollars, and experts predict that these costs will continue to rise in the future (Global Pipeline Analysis, Competitive Landscape, and Market Forecasts).

[0003] In the past, liposuction or fat reduction surgery was the primary methods used to treat obesity. However, these existing surgical methods not only cause pain for patients but also lead to side effects such as adhesion between the surgical site and the dermis, hematoma formation, and infection. In particular, some early surgeries have been reported to involve the use of potentially carcinogenic substances, posing a risk of serious health problems. To address these issues, the medical system is continuously researching new treatment methods that maximize fat reduction while minimizing pain and side effects. This research is moving towards shortening postoperative recovery time and reducing the risk of local tissue necrosis or infection through minimally invasive surgical techniques.

[0004] With modern society placing greater emphasis on body shape, the demand for aesthetic improvements and body management has surpassed simple obesity treatments, showing a growing trend. Consequently, the development of more effective and safer lipolysis injectable compositions with minimal side effects has emerged as an important research topic. In particular, with the increasing number of consumers seeking to improve their appearance through lipolysis, such compositions must combine safety and efficacy to meet consumer needs. Current research reflects this market demand.

[0005] Therefore, modern compositions for fat breakdown should not only meet economic and social needs, but should also be developed in a safe manner that improves user satisfaction. In conclusion, it is hoped that such compositions will become a highly reliable solution in obesity treatment and body shape management, and that their development will continue in the future.

[0006] Existing technical documents

[0007] Patent documents

[0008] Patent Document 1: Korean Patent No. 10-2517928

[0009] Patent Document 2: Korean Patent No. 10-2627595. Summary of the Invention

[0010] Technical issues

[0011] The purpose of this invention is to provide an injectable composition for fat decomposition, comprising: one or more compounds selected from hyaluronidase and pentoxifylline; 5-10% (v / v) carnitine; 0.1-1.0% (v / v) lidocaine; and physiological saline.

[0012] Technical solution

[0013] To achieve the aforementioned objective, the present invention provides an injectable composition for lipolysis, comprising: one or more compounds selected from hyaluronidase and pentoxifylline; 5-10% (v / v) carnitine; 0.1-1.0% (v / v) lidocaine; and physiological saline.

[0014] When the injectable composition for fat breakdown contains hyaluronidase, the content of hyaluronidase may be from 600 IU to 900 IU.

[0015] When the injectable composition for lipolysis contains pentoxifylline, the content of pentoxifylline may be 8-12% (v / v).

[0016] The injectable composition may further include one or more additives selected from the group consisting of excipients, penetration enhancers, dispersants, disintegrants, lubricants, wetting agents, emulsifiers, suspending agents, diluents, binders, lubricants, preservatives, stabilizers, anti-sticking agents, fluidizing agents, colorants, or preservatives.

[0017] The single injection dose of the injectable composition can be from 1.0 cc to 15.0 cc.

[0018] The injectable composition can be administered at injection point intervals of 1.5 cm to 2.5 cm.

[0019] The injectable composition for lipolysis may not cause skin pitting as a side effect.

[0020] The effects of the invention

[0021] As a composition that combines safety and efficacy, the injectable composition for lipolysis of the present invention has excellent lipolysis effect, does not cause the yo-yo effect over time, and also has the characteristic of not causing side effects such as skin pitting. Detailed Implementation

[0022] The present invention will now be described in more detail through embodiments. However, it will be apparent to those skilled in the art that these embodiments are merely for illustrating the invention more specifically, and the scope of the invention is not limited to these embodiments according to the spirit of the invention.

[0023] The present invention provides an injectable composition for lipolysis, comprising: one or more compounds selected from hyaluronidase and pentoxifylline; 5-10% (v / v) carnitine; 0.1-1.0% (v / v) lidocaine; and physiological saline.

[0024] In this invention, the injectable composition for fat breakdown may contain hyaluronidase.

[0025] As an enzyme that breaks down hyaluronic acid, the hyaluronidase is equivalent to a component that provides functions such as reducing edema, breaking down fat, and rapid absorption when injected with drugs.

[0026] In this invention, when the injectable composition for lipolysis contains hyaluronidase, it may contain 600 IU to 900 IU of hyaluronidase. In this case, if the hyaluronidase content is less than 600 IU, the yo-yo effect will occur due to insufficient lipolysis, resulting in a reduced waist circumference reduction. If the hyaluronidase content is greater than 900 IU, not only will the yo-yo effect occur, but side effects such as skin pitting may also occur. Therefore, when the injectable composition for lipolysis contains hyaluronidase, containing 600 IU to 900 IU of hyaluronidase can simultaneously achieve excellent lipolysis effect and stability.

[0027] In this invention, the injectable composition for fat breakdown may contain pentoxifylline.

[0028] As an ingredient that helps supply more oxygen to tissues by reducing blood viscosity and improving blood circulation, the pentoxifylline provides a fat-decomposing effect by activating the metabolism of fat cells and improving blood circulation.

[0029] In this invention, when the injectable composition for fat decomposition contains pentoxifylline, it may contain 8-12% (v / v) of pentoxifylline based on the total volume of the injectable composition. In this case, if the content of pentoxifylline is less than 8% (v / v), the waist circumference reduction effect will be reduced, and the yo-yo effect will be significantly increased. If the content of pentoxifylline is greater than 12% (v / v), side effects such as urticaria, dizziness, and nausea will occur. Conversely, when it contains 8-12% (v / v) of pentoxifylline, the waist circumference reduction effect will be improved, and the yo-yo effect will be reduced.

[0030] In this invention, the injectable composition for fat breakdown may contain carnitine.

[0031] The carnitine may be selected from, but is not limited to, L-carnitine, acetyl-L-carnitine (ALCAR), propionyl-L-carnitine, D-carnitine, L-carnitine tartrate, glycine-propionyl-L-carnitine (GPLC), and combinations thereof.

[0032] Carnitine, as an amino acid derivative required by the body to convert fat into energy, is equivalent to a component that helps burn fat, generate energy, reduce body fat, and improve athletic performance.

[0033] In this invention, the injectable composition for lipolysis may contain 5-10% (v / v) of the carnitine, based on the total volume of the injectable composition. In this case, if the carnitine content is less than 5% (v / v), the lipolysis effect will not be sufficiently demonstrated; if the carnitine content is greater than 10% (v / v), side effects such as skin pitting and excessive yo-yoing may occur.

[0034] In this invention, the injectable composition for lipolysis comprises lidocaine.

[0035] The lidocaine is used as a local anesthetic component to relieve pain when injecting the injectable composition.

[0036] In this invention, the injectable composition for lipolysis may contain 0.1 to 1.0% (v / v) of lidocaine, based on the total volume of the injectable composition. In this case, if the lidocaine content is less than 0.1% (v / v), pain or discomfort may be induced, and the injectable composition may not be effectively applied to the injection site. If the lidocaine content is greater than 1%, various side effects such as cardiovascular side effects and skin irritation may occur.

[0037] In this invention, the composition may further comprise suitable carriers, excipients, penetration enhancers, dispersants, disintegrants, lubricants, wetting agents, emulsifiers, suspending agents, diluents, binders, lubricants, preservatives, stabilizers, anti-sticking agents, fluidizing agents, colorants, or preservatives commonly used in the preparation of injectable compositions. The carriers, excipients, and diluents that may be included include lactose, glucose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum arabic, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, physiological saline, methylparaben, propylparaben, talc, magnesium stearate, and mineral oil, etc. When formulating the composition, commonly used fillers, extenders, binders, wetting agents, disintegrants, surfactants, and other diluents or excipients can be used.

[0038] In this invention, the term "administration" as used herein refers to the delivery of the prescribed composition of the invention to an individual or patient by injection, which may be a subcutaneous injection, intradermal injection, intravenous injection, intramuscular injection, intraperitoneal injection, subcutaneous transplantation, transplantation injection, or administration via ointment or patch, preferably by injection into the skin layer and subcutaneous layer.

[0039] Furthermore, the injectable composition for lipolysis can be administered using an infusion pump. In particular, when overdose of the injectable composition for lipolysis is administered, using an infusion pump is more appropriate than using a syringe.

[0040] In this invention, the injectable composition for lipolysis can be administered to the site where the lipolysis effect is desired, such as the forearm, abdomen, thigh, face, buttocks, etc.

[0041] In this invention, the preferred dosage of the injectable composition for lipolysis can be selected based on the individual, the patient's condition and weight, the presence or absence of disease, the severity of disease, the route of administration, and the duration of administration, and can also be appropriately selected by relevant practitioners. For optimal results, the injectable composition of this invention can be administered in a single dose of 1.0 cc to 15.0 cc, once a day, or divided into several doses.

[0042] In this invention, the injection sites of the injectable composition for lipolysis can be injected at intervals of 1.5 cm to 2.5 cm, but are not limited thereto.

[0043] In this invention, the injectable composition for lipolysis is characterized in that it not only has a lipolysis effect, but also, after one month of administration, the yo-yo effect is minimal and no side effects such as skin depression occur.

[0044] The present invention will now be described in detail through embodiments. However, the following embodiments are merely illustrative of the invention, and the scope of the invention is not limited to these embodiments.

[0045] Example 1

[0046] The injectable composition for lipolysis of Example 1 was prepared by uniformly mixing hyaluronidase (purchased from Daehan Nupharm), carnitine (purchased from Dong Kwang Pharmaceutical Co., Ltd.), and lidocaine (purchased from Daehan Nupharm) in the amounts shown in Table 1 below and dissolving them in physiological saline.

[0047] Table 1

[0048]

[0049]

[0050] Example 2

[0051] The injectable composition for lipolysis of Example 2 was prepared by uniformly mixing pentoxifylline (purchased from Huons), carnitine (purchased from DongKwang Pharmaceutical Company), and lidocaine (purchased from Daehan Nupharm Company) according to the contents of Table 2 below and dissolving it in physiological saline.

[0052] Table 2

[0053] Element Example 2 Theobromine 10% (v / v) L-carnitine 10% (v / v) Lidocaine 0.6% (v / v) physiological saline Remaining amount

[0054] Example 3

[0055] Hyaluronidase (purchased from Daehan Nupharm), pentoxifylline (purchased from Huons), carnitine (purchased from Dong Kwang Pharmaceutical Co.), and lidocaine (purchased from Daehan Nupharm) were uniformly mixed according to the contents shown in Table 3 below, and dissolved in physiological saline to prepare the injectable composition for lipolysis of Example 3.

[0056] Table 3

[0057] Element Example 2 Hyaluronidase 700IU Theobromine 10% (v / v) L-carnitine 10% (v / v) Lidocaine 0.6% (v / v) physiological saline Remaining amount

[0058] Comparative Example 1

[0059] Compared to the injectable composition for lipolysis in Example 1, the injectable composition for lipolysis in Comparative Example 1 was prepared with the same composition and content, except that 500 IU of hyaluronidase was used instead of 700 IU of hyaluronidase.

[0060] Comparative Example 2

[0061] Compared to the injectable composition for lipolysis in Example 1, the injectable composition for lipolysis in Comparative Example 2 was prepared with the same composition and content, except that 1000 IU of hyaluronidase was used instead of 700 IU of hyaluronidase.

[0062] Comparative Example 3

[0063] Compared to the injectable composition for lipolysis in Example 2, the injectable composition for lipolysis in Comparative Example 3 was prepared with the same composition and content, except that 5% (v / v) of pentoxifylline was used instead of 10% (v / v) of pentoxifylline.

[0064] Comparative Example 4

[0065] Compared to the injectable composition for lipolysis in Example 2, the injectable composition for lipolysis in Comparative Example 4 was prepared with the same composition and content, except that 15% (v / v) of pentoxifylline was used instead of 10% (v / v) of pentoxifylline.

[0066] Comparative Example 5

[0067] Compared with the injectable composition for lipolysis in Example 3, the injectable composition for lipolysis in Comparative Example 5 was prepared with the same composition and content, except that 5% (v / v) of pentoxifylline was used instead of 10% (v / v) of pentoxifylline.

[0068] Comparative Example 6

[0069] Compared with the injectable composition for lipolysis in Example 3, the injectable composition for lipolysis in Comparative Example 6 was prepared with the same composition and content, except that it contained 1000 IU of hyaluronidase instead of 700 IU of hyaluronidase and 5% (v / v) of pentoxifylline instead of 10% (v / v) of pentoxifylline.

[0070] Comparative Example 7

[0071] Compared to the injectable composition for lipolysis in Example 3, the injectable composition for lipolysis in Comparative Example 7 was prepared with the same composition and content, except that 15% (v / v) of pentoxifylline was used instead of 10% (v / v) of pentoxifylline.

[0072] The composition and content of the injectable compositions of Examples 1 to 3 and Comparative Examples 1 to 7 are summarized in Table 4 below.

[0073] Table 4

[0074] distinguish Hyaluronidase Theobromine L-carnitine Lidocaine physiological saline Example 1 700IU - 10% (v / v) 0.6% (v / v) Remaining amount Example 2 - 10% (v / v) 10% (v / v) 0.6% (v / v) Example 3 700IU 10% (v / v) 10% (v / v) 0.6% (v / v) Comparative Example 1 500 IU - 10% (v / v) 0.6% (v / v) Comparative Example 2 1000 IU - 10% (v / v) 0.6% (v / v) Comparative Example 3 - 5% (v / v) 10% (v / v) 0.6% (v / v) Comparative Example 4 - 15% (v / v) 10% (v / v) 0.6% (v / v) Comparative Example 5 700IU 5% (v / v) 10% (v / v) 0.6% (v / v) Comparative Example 6 1000 IU 5% (v / v) 10% (v / v) 0.6% (v / v) Comparative Example 7 700IU 15% (v / v) 10% (v / v) 0.6% (v / v)

[0075] Experimental Example 1. Clinical Trial

[0076] To confirm the lipolysis effect of the injectable compositions for lipolysis described in Examples 1 to 3 and Comparative Examples 1 to 7, a clinical trial was conducted on 10 obese patients with a BMI of 25 or higher from admitted adult men and women aged 20 years and older. After administering 10 cc of the injectable composition for lipolysis to the abdomen of each subject at 2 cm intervals, the thickness (mm) of abdominal fat was measured on the third day and at the first month after administration. The results are shown in Table 5 below. In this case, the waist circumference difference after one month of administration represents the change in waist circumference measured on the third day of administration.

[0077] On the other hand, the statistical analysis and testing methods used SPSS statistical software to obtain the distribution of the measured values. In order to observe the effect of different experimental injections on the reduction of abdominal waist circumference, the paired t-test was used to analyze the reliability and the test interval was determined to be within 95%.

[0078] Table 5

[0079]

[0080] Clinical trials confirmed the fat-decomposing effect, demonstrating that the injectable compositions for fat decomposition in Examples 1 to 3 of this invention not only have excellent waist circumference reduction effects but also do not cause side effects such as skin pitting, urticaria, or dizziness. In particular, the injectable compositions for fat decomposition in Examples 2 and 3 showed no yo-yo effect up to one month after administration, exhibiting a sustained fat-decomposing effect.

[0081] Conversely, the injectable composition for lipolysis in Comparative Example 1, containing 500 IU of hyaluronidase, not only failed to show a significant waist circumference reduction effect after 3 days of administration, but also exhibited a yo-yo effect after one month of administration, showing almost no lipolysis effect. The injectable composition for lipolysis in Comparative Example 2, containing 1000 IU of hyaluronidase, not only caused the yo-yo effect but also resulted in minor skin pitting due to excessive hyaluronidase dosage. In other words, when confirming the difference in waist circumference with varying hyaluronidase content, it was confirmed that a hyaluronidase content below 500 IU could not adequately demonstrate a lipolysis effect, while a hyaluronidase content above 1000 IU resulted in minor pitting, confirming the possibility of minor side effects.

[0082] Furthermore, in the case of the injectable composition for lipolysis in Example 2, which contained 10% (v / v) pentoxifylline as a lipolysis compound, compared with the injectable composition of Comparative Example 3 containing 5% (v / v) pentoxifylline, it not only exhibited excellent lipolysis effect but also maintained the lipolysis effect for one month, demonstrating more sustained efficacy. Meanwhile, it was confirmed that compared with the injectable composition for lipolysis in Example 2, which contained 10% (v / v) pentoxifylline as a lipolysis compound, the injectable composition for lipolysis in Comparative Example 4, which contained 15% (v / v) pentoxifylline, caused side effects such as nausea or dizziness, and urticaria. That is, when the content of pentoxifylline is 5% or less, the lipolysis effect exhibits a yo-yo effect, resulting in a decrease in lipolysis efficacy; when the content of pentoxifylline is 15% or more, side effects such as urticaria, dizziness, and nausea occur.

[0083] On the other hand, in Comparative Examples 5 to 7, which simultaneously contain hyaluronic acid and pentoxifylline as lipolysis compounds, Comparative Example 5 did not exhibit the yo-yo effect, but due to insufficient pentoxifylline content, the waist circumference reduction effect after one month of administration was negligible. That is, the injectable composition of Comparative Example 5 showed insufficient persistence of lipolysis effect. Although the injectable composition of Comparative Example 6 showed a significant reduction in waist circumference after 3 days of administration, after one month, it was confirmed that the waist circumference was almost the same as the pre-operative waist circumference, and the yo-yo effect was severe. This was confirmed to be a temporary reduction in edema or swelling caused by excessive hyaluronidase content. Meanwhile, the injectable composition of Comparative Example 7 contained an excessive amount of pentoxifylline, and side effects such as urticaria, dizziness, and nausea were observed. That is, it was confirmed that when hyaluronidase and pentoxifylline are both contained as lipolytic compounds, the hyaluronidase content is 700 IU and the pentoxifylline content is 10% (v / v), which has excellent lipolytic effect and stability as a lipolytic injection composition.

Claims

1. An injectable composition for lipolysis, characterized in that, Include: One or more compounds from hyaluronidase and pentoxifylline; 5-10% v / v carnitine; 0.1–1.0% v / v lidocaine; and Physiological saline solution.

2. The injectable composition for lipolysis according to claim 1, characterized in that, When the injectable composition for fat breakdown contains hyaluronidase, the content of hyaluronidase is 600 IU to 900 IU.

3. The injectable composition for lipolysis according to claim 1, characterized in that, In the case where the injectable composition for fat breakdown contains pentoxifylline, the content of pentoxifylline is 8-12% v / v.

4. The injectable composition for lipolysis according to claim 1, characterized in that, The injectable composition further comprises one or more additives selected from the group consisting of excipients, penetration enhancers, dispersants, disintegrants, lubricants, wetting agents, emulsifiers, suspending agents, diluents, binders, lubricants, preservatives, stabilizers, anti-adhesion agents, fluidizing agents, colorants, or preservatives.

5. The injectable composition for lipolysis according to claim 1, characterized in that, The single injection dose of the injectable composition is 15cc.

6. The injectable composition for lipolysis according to claim 1, characterized in that, The injectable composition is administered at injection point intervals of 1.5 cm to 2.5 cm.

7. The injectable composition for lipolysis according to claim 1, characterized in that, The injectable composition for lipolysis does not cause skin pitting as a side effect.

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