Lac‑phe‑based composition, health care supplement, and use thereof

By using Lac-Phe-based compositions and nebulizers, the side effects and difficulty in adhering to existing obesity treatments have been addressed, achieving highly efficient and safe obesity treatment while improving bioavailability and treatment effectiveness.

WO2026097353A1PCT designated stage Publication Date: 2026-05-15SHENZHEN INST OF ADVANCED TECH
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
SHENZHEN INST OF ADVANCED TECH
Filing Date
2024-11-07
Publication Date
2026-05-15

AI Technical Summary

Technical Problem

Existing treatments for obesity have significant side effects and are difficult to adhere to, making it difficult to effectively reduce the burden on public health systems and improve global health.

Method used

A Lac-Phe-based composition and nebulizer are provided, which, through optimized formulation and administration method, deliver the active pharmaceutical ingredient directly to the lungs via nebulization inhalation, thereby improving bioavailability and therapeutic efficiency.

Benefits of technology

The Lac-Phe composition has no toxic side effects, improves drug absorption and therapeutic effect, reduces pain during the weight loss process, and enhances patients' willingness and comfort in losing weight.

✦ Generated by Eureka AI based on patent content.

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Abstract

A Lac‑Phe‑based composition, a health care supplement, and a use thereof. The composition comprises propylene glycol, glycerol, Lac-Phe and a synergist in a mass ratio of (0.1-100):(0.1-100):(0.1-10):(0.1-2). The solubility of Lac-Phe is improved and the absorption rate of active pharmaceutical molecules in the body is optimized, thereby enhancing the bioavailability and helping to improve the efficacy of Lac-Phe in preventing and treating obesity.
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Description

A Lac-Phe-based composition, health product and its application Technical Field

[0001] This invention relates to the field of drugs for treating metabolic disorders, and more specifically to a Lac-Phe-based composition, health product, and its application. Background Technology

[0002] A Lancet research report indicates that the number of obese adults worldwide has more than tripled since 1990, exceeding 1 billion by 2022, with the number of obese children and adolescents aged 5 to 19 tripling. Furthermore, in 94% of 188 countries globally, the age-standardized prevalence of obesity among women has increased, and obesity is also generally on the rise among men, with only one exception. This demonstrates that obesity is exacerbating the burden on public health systems, increasing healthcare costs, and creating socioeconomic pressures, thus becoming a significant public health challenge.

[0003] For individuals, obesity not only significantly limits mobility and quality of life, causing numerous adverse effects on daily life, but also significantly increases the risk of developing a variety of diseases, including cardiovascular disease, diabetes, asthma, osteoarthritis, reproductive dysfunction, and certain types of cancer. Therefore, effective measures are needed to reduce the multiple negative impacts of obesity.

[0004] Treating obesity typically involves increasing basal metabolic rate, improving cardiorespiratory function, and strengthening muscles through diet control and appropriate physical activity. These methods help maintain a healthy weight in the long term. However, controlling appetite requires strong willpower and endurance to overcome strong cravings and pre-meal hunger. Exercise for weight loss, on the other hand, requires a significant amount of physical activity, is not only time-consuming but also demands long-term patience and perseverance. Therefore, obese individuals often face considerable challenges when implementing these measures.

[0005] When diet control and exercise are ineffective, medication or even bariatric surgery is often necessary. However, traditional drug treatments, such as orlistat, amphetamine, and metformin, frequently cause side effects like diarrhea, headaches, and nausea. Bariatric surgery can lead to complications such as postoperative wound infection. Furthermore, postoperative diet control and moderate exercise are still required to prevent recurrence of obesity.

[0006] In conclusion, while existing obesity treatments are effective to some extent, significant side effects and difficulties in adhering to them necessitate the development of weight-loss products that are more effective and easier for patients to maintain long-term. Only in this way can we more effectively address the global obesity epidemic, alleviate the burden on public health systems, and improve the overall health of the global population.

[0007] Summary of the Invention

[0008] This invention provides a Lac-Phe-based composition, health product, and its application by optimizing the composition formulation and determining a suitable administration route.

[0009] In a first aspect, the present invention provides a Lac-Phe-based composition comprising propylene glycol, glycerol, Lac-Phe, and a synergist in a mass ratio of (0.1-100):(0.1-100):(0.1-10):(0.1-2).

[0010] In some embodiments, the mass ratio of propylene glycol to glycerol is (7-9):(1-2).

[0011] In some embodiments, the synergist includes vitamin B12.

[0012] In a second aspect, the present invention provides a health product comprising the above-described Lac-Phe-based composition and an atomizing device for atomizing the Lac-Phe-based composition.

[0013] In some embodiments, the atomizing device includes an atomizing circuit, a storage chamber and a battery connected to the atomizing circuit; the storage chamber stores the Lac-Phe-based composition to be atomized; the atomizing circuit converts the Lac-Phe-based composition into an aerosol form; and the battery powers the atomizing circuit.

[0014] A third aspect of the present invention provides the use of the above-described Lac-Phe-based composition or the above-described health product in the preparation of products for the prevention or treatment of obesity.

[0015] A fourth aspect of the present invention provides a method for preventing or treating obesity, comprising administering an effective amount of the above-described Lac-Phe-based composition or the above-described health product to a subject in need.

[0016] Compared with the prior art, the beneficial effects of the present invention are:

[0017] (1) The active pharmaceutical ingredient used in this invention is Lac-Phe. As a normal metabolic product of human movement, Lac-Phe has no toxic side effects and has high safety.

[0018] (2) The Lac-Phe-based composition provided by this invention employs appropriate formulation components and corresponding contents, which improves the solubility of Lac-Phe and optimizes the absorption rate of the active drug molecules in vivo, thereby enhancing bioavailability and helping to improve the efficacy of Lac-Phe in reducing appetite or treating obesity. In addition, the designed formulation also expands the administration routes of Lac-Phe, providing more possibilities for future therapeutic research.

[0019] (3) The health product provided by this invention includes a Lac-Phe-based composition and its corresponding nebulizer. This nebulizer can convert the composition into an aerosol form, allowing the active pharmaceutical ingredient to directly enter the lungs through the respiratory tract. On the one hand, this avoids potential loss or denaturation of the drug during gastrointestinal digestion, improving the bioavailability and therapeutic effect. On the other hand, it also enables the active pharmaceutical ingredient to be rapidly absorbed by the body, improving therapeutic efficiency. Simultaneously, the nebulization inhalation method is not limited by time or location and has the advantages of being portable and easy to operate, further reducing the discomfort during weight loss and increasing the willingness and comfort of those in need to lose weight. Attached Figure Description

[0020] Figure 1 is a diagram of an atomizing device in one embodiment, where 1 is a storage compartment, and 2 is an atomizing circuit and a battery;

[0021] Figure 2 shows the trend of weight change of each group of mice at different time points in one embodiment;

[0022] Figure 3 is a cumulative trend graph of the area under the curve of the weight change values ​​of each group of mice in one embodiment over time;

[0023] Figure 4 shows the change in food intake of mice in each group over time in one embodiment;

[0024] Figure 5 shows the change in water intake of mice in each group over time in one embodiment. Detailed Implementation

[0025] The technical solution of this patent will be further described in detail below with reference to specific embodiments. It should be noted that the following detailed descriptions are exemplary and intended to provide further explanation of this application. Unless otherwise specified, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this application pertains.

[0026] This invention provides a Lac-Phe-based composition comprising propylene glycol, glycerol, Lac-Phe, and a synergist in a mass ratio of (0.1-100):(0.1-100):(0.1-10):(0.1-2). In some embodiments, the mass ratio of propylene glycol to glycerol is (7-9):(1-2). In some embodiments, the synergist comprises one or more vitamins, preferably a synergist containing vitamin B12.

[0027] Furthermore, the present invention provides a health product comprising the above-mentioned Lac-Phe-based composition and an atomizing device for atomizing the composition. As shown in Figure 1, this portable atomizing device is generally symmetrical and mainly includes a storage chamber for storing the composition, an atomizing circuit for converting the composition into an aerosol form, and a battery for power supply.

[0028] Furthermore, the present invention provides the use of the above-described Lac-Phe-based compositions or the above-described health products in the preparation of products for the prevention or treatment of obesity. Further, a method for the prevention or treatment of obesity is provided, comprising administering an effective amount of the above-described Lac-Phe-based compositions or the above-described health products to a subject in need.

[0029] Behavioral experiments were conducted using the Lac-Phe-based composition prepared in Example 1. Specifically, obese mice were housed alone and fed water and a high-fat diet from week 16 to week 26. Starting from week 26, all obese mice were weighed daily and placed in an exposure chamber for acclimatization treatment until their weight stabilized, in order to reduce fluctuations in food intake, water intake, and weight caused by stress. Obese mice with comparable weights were randomly divided into a control group and a treatment group, receiving ultrasonic nebulization treatment with saline and Lac-Phe composition aerosol, respectively. Before each exposure, the mice's weight, food intake, and water intake were measured, and the experiment lasted for 8 days.

[0030] Results: Figure 2 shows the trend of body weight change in each group of mice at different time points, where the horizontal axis represents time and the vertical axis represents the change in body weight. Figure 3 shows the cumulative trend of the area under the curve of body weight change in each group of mice over time, where the horizontal axis represents time and the vertical axis represents the area under the curve as a function of body weight. It can be seen that compared with the control group receiving saline nebulization treatment, the mice in the group treated with Lac-Phe aerosol combination showed a more significant decrease in body weight and exhibited a stronger weight loss trend.

[0031] Figure 4 shows the changes in food intake of mice in each group over time, with the horizontal axis representing time and the vertical axis representing food intake. It can be seen that, compared to the control group receiving saline nebulization, the mice in the Lac-Phe aerosol group showed a decrease in food intake, exhibiting a stronger trend of decreased appetite.

[0032] Figure 5 shows the changes in water intake of mice in each group over time, with the horizontal axis representing time and the vertical axis representing water intake. It can be seen that there was no significant difference in water intake between the control group and the treatment group.

[0033] It should be understood that obesity as mentioned in this application includes: ① overweight adults with a body mass index (BM1) greater than or equal to 25 but less than 30; ② obese adults with a BM1 greater than or equal to 30; ③ overweight children aged 5-19 years with a BM1 greater than one standard deviation of the WHO growth reference standard median; ④ obese children aged 5-19 years with a BM1 greater than two standard deviations of the WHO growth reference standard median; ⑤ overweight children under 5 years of age with a BM1 greater than two standard deviations of the WHO child growth reference standard median; and ⑥ obese children under 5 years of age with a BM1 greater than three standard deviations of the WHO child growth reference standard median.

[0034] The above descriptions are merely some embodiments of the present invention. Those skilled in the art can make various modifications and improvements without departing from the inventive concept of the present invention, and these all fall within the scope of protection of the present invention.

Claims

1. A Lac-Phe based composition, characterized in that, It includes propylene glycol, glycerol, Lac-Phe and synergists in a mass ratio of (0.1-100):(0.1-100):(0.1-10):(0.1-2).

2. The Lac-Phe-based composition according to claim 1, characterized in that, The mass ratio of propylene glycol to glycerol is (7-9):(1-2).

3. The Lac-Phe-based composition according to claim 1, characterized in that, The synergist includes vitamin B12.

4. A health product, characterized in that, The invention includes the Lac-Phe-based composition according to any one of claims 1-3, and an atomizing device for atomizing the Lac-Phe-based composition.

5. The health product according to claim 4, characterized in that, The atomizing device includes an atomizing circuit, a storage compartment and a battery connected to the atomizing circuit; The storage chamber stores the Lac-Phe-based composition to be atomized; The atomizing circuit converts the Lac-Phe-based composition into an aerosol form; The battery powers the atomizing circuit.

6. The use of a Lac-Phe-based composition according to any one of claims 1-3 or the health product according to claim 4 or 5 in the preparation of a product for the prevention or treatment of obesity.

7. A method for preventing or treating obesity, characterized in that, This includes administering an effective amount of the Lac-Phe-based composition of any one of claims 1-3 or the health product of claim 4 or 5 to a desired recipient.