Fat-burning oral liquid with body shaping function and preparation process

Abstract

The invention discloses a fat-burning oral liquid with a body-shaping function and a preparation process thereof, the oral liquid is a nano-emulsion, and is prepared from the following raw materials: a first active component (immature bitter orange extract), a second active component (L-carnitine), an auxiliary body-shaping component (such as globe artichoke extract and fennel fruit extract) and phospholipid. The key step of the preparation process is that an oil phase and a water phase containing active components are prepared into a stable nano-emulsion with the average particle size of 20-200 nanometers through high-pressure homogenization treatment. Compared with the prior art, the technical pain points that the core fat-burning component is low in bioavailability, poor in formula stability and obvious in side effect are solved, the stability, the absorptivity and the user experience of the product are remarkably improved through the synergistic composition and the innovative nano preparation process, and the composition has important application value.

Description

Technical Field

[0001] The present invention relates to the technical field of functional foods and medical health care, in particular to a fat burning oral liquid with body shaping function and a preparation process thereof. Background Art

[0002] With the changing lifestyles of modern society, obesity and its related metabolic diseases have become global public health issues. Consequently, market demand for weight management and body fat control is growing, leading to the emergence of a wide variety of dietary supplements and functional foods claiming to have fat-burning and body-slimming properties. Existing products in this category generally rely on several core active ingredients, such as caffeine and tea polyphenols (particularly EGCG) from green tea and coffee; L-carnitine, which acts as a fatty acid transporter; and alkaloids (such as synephrine) derived from specific plants (e.g., Citrus Aurantium), which stimulate thermogenesis by mimicking the effects of adrenaline. Furthermore, to achieve a more comprehensive "body-slimming" effect, some products also incorporate ingredients with diuretic, detoxifying, or digestive benefits, such as artichoke extract and fennel extract.

[0003] Products in the existing technology have problems such as low bioavailability of core ingredients, poor formula stability, easy to cause side effects such as palpitations, and backward production technology leading to product homogeneity.

[0004] For example, the oral absorption rates of core active ingredients such as EGCG and synephrine are not ideal, and multiple ingredients with different water and oil properties (such as plant extracts, functional oils, etc.) are prone to stratification and precipitation after simple mixing, which seriously affects product quality and effect.

[0005] Therefore, developing an innovative product that can efficiently deliver multiple effective ingredients and allow them to coexist stably is a technical problem that needs to be urgently solved in this field. Summary of the Invention

[0006] The present invention provides a synergistic fat burning composition, a fat burning oral liquid with body shaping function prepared from the composition, and a preparation process of the oral liquid, in order to solve the problems raised by the above background technology.

[0007] To achieve the above-mentioned object, the present invention provides the following technical solution: a fat-burning oral liquid with body-slimming function, wherein the oral liquid is a nanoemulsion prepared from raw materials containing the following components: (a) a first active ingredient, which is an extract of Citrus aurantium; (b) a second active ingredient, which is L-carnitine, a pharmaceutically acceptable salt thereof, or a derivative thereof; (c) an auxiliary body-slimming component selected from at least one of artichoke extract and fennel fruit extract; and (d) Phospholipids, which serve as nanocarrier building agents.

[0008] As a preferred technical solution of the present invention, the first active component further comprises at least one of green tea extract, caffeine or guarana extract.

[0009] As a preferred technical solution of the present invention, the raw material further comprises piperine, which serves as an absorption enhancer.

[0010] As a preferred technical solution of the present invention, the raw material further contains L-theanine.

[0011] As a preferred technical solution of the present invention, the phospholipid is one or more of soybean lecithin, sunflower seed lecithin or egg yolk lecithin.

[0012] As a preferred technical solution of the present invention, the average particle size of the dispersed phase of the nanoemulsion is between 20 nanometers and 200 nanometers.

[0013] The preparation process of the fat burning oral liquid with body shaping function comprises the following steps: (a) dissolving a water-soluble raw material in water to form an aqueous phase raw material; (b) mixing a fat-soluble or poorly water-soluble raw material with a phospholipid to form an oil phase raw material; (c) mixing the oil phase raw material and the water phase raw material, and performing high pressure homogenization treatment to form a nanoemulsion.

[0014] As a preferred technical solution of the present invention, the aqueous phase raw material comprises L-carnitine or a pharmaceutically acceptable salt thereof, and optionally artichoke extract or fennel fruit extract.

[0015] As a preferred technical solution of the present invention, the oil phase raw material comprises an extract of Citrus aurantium and optionally piperine.

[0016] As a preferred technical solution of the present invention, the pressure of the high-pressure homogenization treatment is between 80 MPa and 200 MPa, and the treatment is circulated 2 to 8 times; Before the high-pressure homogenization treatment in step (c), the method further includes subjecting the oil phase raw material and the water phase raw material to high-speed shear pre-emulsification, wherein the rotation speed of the high-speed shear is 3000-10000 rpm.

[0017] Compared with the prior art, the present invention has the following beneficial effects: The present invention significantly improves the oral bioavailability of hydrophobic or low-permeability active ingredients in the composition by constructing an oil / water nanoemulsion delivery system; In the prior art, core active ingredients such as synephrine in Citrus aurantium extract and EGCG in green tea extract have limited solubility and / or permeability in the gastrointestinal tract due to their physical and chemical properties, resulting in low oral absorption efficiency.

[0018] 1. The present invention utilizes a high-pressure homogenization process to encapsulate the active ingredient in nanoscale oil droplets made with phospholipids as carriers, forming a nanoemulsion with an average particle size of 20-200 nanometers. This dosage form overcomes absorption barriers through the following mechanisms: (a) Nanoparticle size greatly increases the dispersibility and effective specific surface area of ​​the active substance in the gastrointestinal fluid, which directly increases its dissolution rate according to the Noyes-Whitney equation; (b) Phospholipid carriers have good biocompatibility and mucosal adsorption, which can prolong the retention time of the preparation in the intestinal absorption site; (c) Nanocarriers can enter the systemic circulation through paracellular and transcellular pathways (including phagocytosis by M cells), partially bypassing the first-pass effect in the liver. This is particularly critical for active ingredients that are easily metabolized. As demonstrated in subsequent efficacy verification experiments, the formulation of this invention can increase the transmembrane permeability of the core active ingredient by 7-9 times, resolving the problem of low absorption efficiency in existing technologies and ensuring that the active ingredient reaches its target at a higher concentration.

[0019] 2. The nanoemulsion prepared by the present invention has excellent physical and chemical stability, which solves the technical problems of easy delamination, precipitation and degradation of active ingredients in the composite liquid preparations in the prior art; Stably formulating plant extracts and active ingredients from multiple sources and with different physicochemical properties into a single liquid phase system is a major challenge in existing technologies.

[0020] The present invention imparts a high degree of dynamic stability to the nanoemulsion system through a high-pressure homogenization process. On the one hand, the surface of the formed nano-droplets has a high surface charge due to the directional arrangement of phospholipid molecules, and the absolute value of its zeta potential can reach above 30mV. The electrostatic repulsion between the droplets is sufficient to resist the van der Waals attraction, effectively preventing flocculation and aggregation caused by Brownian motion. On the other hand, the uniform nanoscale particle size distribution effectively suppresses the Ostwald ripening phenomenon caused by particle size differences; In addition, active ingredients that are sensitive to oxygen, light or pH (such as EGCG) are encapsulated in the inner core of the nano-oil droplet and physically isolated by the phospholipid layer, which significantly reduces their oxidative or hydrolytic degradation rate during storage. Therefore, the product of the present invention can maintain a uniform appearance, no stratification, and no precipitation under long-term and accelerated storage conditions, thereby ensuring the quality and shelf life of the product.

[0021] 3. The present invention provides a technology platform that can stably encapsulate multiple active ingredients in a single system, thereby achieving synergistic effects between the components in pharmacology and pharmacokinetics; The creativity of this invention is not only reflected in the dosage form process, but also in the scientific compounding and pharmacology achieved based on this process; The present invention combines a thermogenic agent that promotes fat mobilization (such as Citrus aurantium extract) with L-carnitine, which is responsible for fatty acid transport, to act on different key links in fat metabolism, producing a pathway synergistic effect; In terms of pharmacokinetics, the present invention combines the physical absorption promotion mechanism of nanocarriers with the biochemical mechanism of piperine inhibiting metabolic enzymes and efflux pumps such as cytochrome P450 (CYP3A4) and P-glycoprotein, forming a dual strategy of "promoting absorption" and "inhibiting clearance"; In terms of functional integration, the nanoemulsion technology platform of the present invention can stably dissolve water-soluble auxiliary body-slimming components (such as artichoke and fennel fruit extracts) in the aqueous phase, while stably encapsulating the fat-soluble core fat-burning components in the oil phase, thus achieving the unification of multi-dimensional body-slimming functions such as "fat burning", "diuresis" and "digestion aid".

[0022] 4. The present invention improves the sensory properties of the product and reduces the risk of adverse reactions through the compounding of specific components and the advantages of dosage form, thereby improving the product's tolerance and compliance; Synephrine and other thermogenic components in Citrus aurantium extract may cause central nervous system excitation, leading to adverse reactions such as palpitations and anxiety. This invention introduces L-theanine, which can cross the blood-brain barrier, promote the generation of alpha brain waves, and antagonize the side effects of caffeine / synephrine. This significantly improves product safety and user comfort without sacrificing fat-burning effects. In addition, the core-shell structure of the nanoemulsion can effectively mask the unpleasant flavors (such as bitterness and astringency) of some plant extracts, give the product a smooth taste, and improve the palatability of the product; more importantly, due to the improved bioavailability, the product of the present invention can achieve the same or even better effects as traditional high-dose products at a lower dose, which is in line with the "high efficiency and low toxicity" principle of the development of drugs and functional foods, and reduces the potential safety risks of long-term use. DETAILED DESCRIPTION

[0023] Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making any creative work shall fall within the scope of protection of the present invention.

[0024] The present invention provides a technical solution: a fat burning oral liquid with body shaping function, wherein the oral liquid is a nanoemulsion prepared from raw materials containing the following components: (a) a first active ingredient, which is an extract of Citrus aurantium; (b) a second active ingredient, which is L-carnitine, a pharmaceutically acceptable salt thereof, or a derivative thereof; (c) an auxiliary body-slimming component selected from at least one of artichoke extract and fennel fruit extract; and (d) Phospholipids, which serve as nanocarrier building agents.

[0025] In a preferred embodiment, the first active component further comprises at least one of green tea extract, caffeine or guarana extract.

[0026] In a preferred embodiment, the raw material further comprises piperine, which serves as an absorption enhancer.

[0027] In a preferred embodiment, the raw material further comprises L-theanine.

[0028] In a preferred embodiment, the phospholipid is one or more of soybean lecithin, sunflower seed lecithin or egg yolk lecithin.

[0029] In a preferred embodiment, the average particle size of the dispersed phase of the nanoemulsion is between 20 nanometers and 200 nanometers.

[0030] The preparation process of the fat burning oral liquid with body shaping function comprises the following steps: (a) dissolving a water-soluble raw material in water to form an aqueous phase raw material; (b) mixing a fat-soluble or poorly water-soluble raw material with a phospholipid to form an oil phase raw material; (c) The oil phase raw material and the water phase raw material are mixed and subjected to high pressure homogenization to form a nanoemulsion.

[0031] In a preferred embodiment, the aqueous phase raw material comprises L-carnitine or a pharmaceutically acceptable salt thereof, and optionally artichoke extract or fennel fruit extract.

[0032] In a preferred embodiment, the oil phase raw material comprises an extract of Citrus aurantium and optionally piperine.

[0033] In a preferred embodiment, the pressure of the high-pressure homogenization treatment is between 80 MPa and 200 MPa, and the treatment is circulated 2 to 8 times; Before the high-pressure homogenization treatment in step (c), the method further includes subjecting the oil phase raw material and the water phase raw material to high-speed shear pre-emulsification, wherein the rotation speed of the high-speed shear is 3000-10000 rpm.

[0034] Example 1: Preparation of fat burning oral liquid with Citrus aurantium extract as the core This embodiment provides a fat burning oral liquid with an extract of Citrus aurantium immaturum (containing p-synephrine) as the main thermogenic component.

[0035] 1.1 Raw material formula (based on preparation of 1000L): Citrus Aurantium Extract (6% p-synephrine): 25.0kg L-carnitine tartrate: 20.0kg Black pepper extract (piperine content ≥98%): 0.2kg Soy lecithin (PC content ≥80%): 7.0kg L-theanine: 2.0kg Concentrated pineapple juice: 50.0kg Concentrated apple juice: 30.0kg Citric acid (food grade): 1.2kg Potassium sorbate: 1.0kg Purified water: add to 1000L 1.2 Preparation process: (1) Preparation of aqueous phase (phase A) raw materials: Dissolve L-carnitine tartrate, L-theanine, concentrated pineapple juice, concentrated apple juice, citric acid and potassium sorbate in about 800 L of purified water.

[0036] (2) Preparation of oil phase (Phase B) raw materials: Mix the Citrus aurantium extract and black pepper extract with the hydrated phospholipids.

[0037] (3) Pre-emulsification: Under high-speed shearing, phase B is pumped into phase A to form a primary emulsion.

[0038] (4) High-pressure homogenization: The primary emulsion was subjected to high-pressure homogenization at a pressure of 130 MPa for 4 cycles.

[0039] (5) Post-processing: The obtained nanoemulsion is cooled, matured, and inspected for quality before aseptic filling to obtain the finished product. The final product has an average particle size of 95 nm and a PDI of 0.20.

[0040] Example 2: Preparation of Multifunctional Body Slimming, Drainage and Fat Burning Oral Liquid This embodiment provides a multifunctional compound formula oral liquid that integrates "fat burning", "detoxification (diuresis)" and "digestion improvement".

[0041] 2.1 Raw material formula (based on preparation of 1000L): Citrus aurantium extract (p-synephrine content 6%): 15.0kg Artichoke extract (Cynarascolymus L.): 60.0kg Fennel fruit extract (Foeniculum vulgare Mill.): 20.0kg L-carnitine tartrate: 15.0kg Soy lecithin (PC content ≥80%): 8.0kg Black pepper extract (piperine content ≥98%): 0.2kg Citric acid: 1.5kg Xanthan gum: 0.5kg Potassium sorbate: 1.0kg Purified water: add to 1000L 2.2 Preparation process: (1) Preparation of aqueous phase (Phase A) raw materials: Dissolve artichoke extract, fennel fruit extract, L-carnitine tartrate, citric acid, xanthan gum and potassium sorbate in about 800 L of purified water, heat to 80 °C and stir for 30 minutes to ensure that the extract and thickener are completely dissolved and hydrated.

[0042] (2) Preparation of oil phase (Phase B) raw materials: Mix the Citrus aurantium extract and black pepper extract with the hydrated phospholipids.

[0043] (3) The remaining steps (pre-emulsification, high-pressure homogenization, cooling and filling) are the same as those in Example 1.

[0044] The final nanoemulsion had an average particle size of 130 nm, a PDI of 0.24, a dark brown appearance, and good fluidity.

[0045] Example 3: Preparation of Citrus aurantium and green tea synergistic fat burning oral solution This embodiment provides an oral liquid that combines an extract of Citrus aurantium and an extract of green tea to achieve a synergistic fat burning effect.

[0046] 3.1 Raw material formula (based on preparation of 1000L): Citrus aurantium extract (p-synephrine content 6%): 10.0kg Green tea extract (EGCG content ≥95%): 1.5kg L-carnitine tartrate: 20.0kg Sunflower seed lecithin (PC content ≥75%): 7.5kg Black pepper extract (piperine content ≥98%): 0.2kg L-theanine: 1.5kg Citric acid: 1.2 kg Potassium sorbate: 1.0kg Purified water: add to 1000L 3.2 Preparation process: The basic process was the same as in Example 1, except that both Citrus aurantium extract and green tea extract were added to the oil phase, and sunflower seed lecithin was used as an emulsifier. The high-pressure homogenization pressure was increased to 150 MPa, and the mixture was cycled five times. The resulting nanoemulsion had an average particle size of 115 nm and a PDI of 0.21.

[0047] Comparative Examples and Effect Verification Experiments In order to demonstrate the superiority of the fat burning oral liquid and its preparation process of the present invention, the following comparative examples were set up and effect verification experiments were conducted.

[0048] Comparative Example 1: The same raw material formula as in Example 1 was used, but the high-pressure homogenization process was not used, and only high-speed shear mixing was performed for 60 minutes.

[0049] Comparative Example 2: The same raw material formula as Example 2 was used, but the high-pressure homogenization process was not used, and only high-speed shear mixing was performed for 60 minutes.

[0050] Comparative Example 3: The same raw material formula as Example 3 was used, but the high-pressure homogenization process was not used, and only high-speed shear mixing was performed for 60 minutes.

[0051] Comparative Example 4: The same preparation process as Example 3 was used, but the black pepper extract was not included in the formula, to verify the synergistic effect of the absorption enhancer.

[0052] Experiment 1: Physical and chemical stability test of the product Method: The samples prepared in Examples 1, 2, and 3 and Comparative Examples 1, 2, and 3 were placed under accelerated conditions of 40°C / 75% RH for 6 months. The appearance and properties of the samples were observed, and the average particle size and retention rate of the key active ingredient (synephrine or EGCG) were measured.

[0053] result: Conclusion: The results clearly demonstrate that the nanoemulsion process employed in this invention can produce products with highly stable physical and chemical properties, regardless of the formulation combination, a feat completely unattainable with traditional physical mixing processes. This demonstrates the broad applicability and significant superiority of the process.

[0054] Experiment 2: In vitro permeability study of Caco-2 cell model Methods: A mature Caco-2 cell monolayer model was used to simulate the human small intestinal epithelial cell barrier, and the transmembrane permeability coefficients (Papp) of the key active ingredients synephrine and EGCG in the samples of Example 3, Comparative Example 3 and Comparative Example 4 were compared.

[0055] result: Conclusion: The data show that: (1) Compared with Comparative Example 3, the absorption of Comparative Example 4 using the nanotechnology process has been significantly improved by 4-5 times. (2) Compared with Comparative Example 4 (without piperine), the absorption of Example 3 containing piperine is further improved by about 1.7 times, demonstrating the synergistic effect of piperine as an absorption enhancer in the composition of the present invention. Overall, the absorption efficiency of the core ingredient has been improved by 7-9 times.

[0056] It should be noted that, in this document, relational terms such as first and second, etc., are used only to distinguish one entity or operation from another entity or operation, and do not necessarily require or imply any actual relationship or order between these entities or operations. Moreover, the terms "comprises," "comprising," or any other variations thereof are intended to cover non-exclusive inclusion, such that a process, method, article, or apparatus that includes a list of elements includes not only those elements but also other elements not explicitly listed, or elements inherent to such process, method, article, or apparatus.

[0057] While embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions, and variations may be made to these embodiments without departing from the principles and spirit of the invention, and that the scope of the invention is defined by the appended claims and their equivalents.

Claims

1. A fat burning oral liquid with body shaping function, characterized in that: The oral liquid is a nanoemulsion prepared from raw materials comprising the following components: (a) a first active ingredient, which is an extract of Citrus aurantium; (b) a second active ingredient, which is L-carnitine, a pharmaceutically acceptable salt thereof, or a derivative thereof; (c) an auxiliary body-slimming component selected from at least one of artichoke extract and fennel fruit extract; and (d) Phospholipids, which serve as nanocarrier building agents.

2. The fat burning oral liquid with body shaping function according to claim 1, characterized in that The first active ingredient further comprises at least one of green tea extract, caffeine or guarana extract.

3. The fat burning oral liquid with body shaping function according to claim 2, characterized in that The raw material also contains piperine, which acts as an absorption enhancer.

4. The fat burning oral liquid with body shaping function according to claim 3, characterized in that The raw material also contains L-theanine.

5. The fat burning oral liquid with body shaping function according to claim 1, characterized in that The phospholipid is one or more of soybean lecithin, sunflower seed lecithin or egg yolk lecithin.

6. The fat burning oral liquid with body shaping function according to claim 1, characterized in that The average particle size of the dispersed phase of the nanoemulsion is between 20 nanometers and 200 nanometers.

7. The preparation process of the fat burning oral liquid with body shaping function according to claim 4, characterized in that: The following steps are involved: (a) dissolving a water-soluble raw material in water to form an aqueous phase raw material; (b) mixing a fat-soluble or poorly water-soluble raw material with a phospholipid to form an oil phase raw material; (c) mixing the oil phase raw material and the water phase raw material, and performing high pressure homogenization treatment to form a nanoemulsion.

8. The process for preparing the fat burning oral liquid with body shaping function according to claim 7, characterized in that: The aqueous phase raw material comprises L-carnitine or a pharmaceutically acceptable salt thereof, and optionally artichoke extract or fennel fruit extract.

9. The process for preparing the fat burning oral medicinal liquid with body shaping function according to claim 7, characterized in that: The oil phase raw material comprises an extract of Citrus aurantium and optionally piperine.

10. The process for preparing the fat burning oral liquid with body shaping function according to claim 7, characterized in that: The pressure of the high-pressure homogenization treatment is between 80 MPa and 200 MPa, and the treatment is circulated 2 to 8 times; Before the high-pressure homogenization treatment in step (c), the method further includes subjecting the oil phase raw material and the water phase raw material to high-speed shear pre-emulsification, wherein the rotation speed of the high-speed shear is 3000-10000 rpm.

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