A GABA-vitamin D neuroprotective composition and method of making same

Abstract

This application relates to the field of functional composition technology, and in particular to a GABA-vitamin D neuroprotective composition and its preparation method, comprising medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend. This application utilizes the low interfacial tension and strong amphiphilic compatibility of medium-chain triglycerides and modified phospholipids, enabling them to be miscible with the blend, thus improving the characteristics of GABA and vitamin D being easily degraded and oxidatively inactivated under complex physiological environments, and solving the problems of poor stability and asynchronous absorption. In the preparation method, the preferred component mass ratio is (0.6–1.5):1:(1–1.6), and mixing is carried out at 50–80°C for 10–60 min. The resulting system features high encapsulation efficiency, uniform particle size distribution, and high bioavailability. After treatment in simulated gastric fluid (pH 1.2) for 2 hours, the average GABA retention rate is ≥88% (optimal up to 94.3%), and the average vitamin D retention rate is ≥94% (optimal up to 96.8%). After treatment in simulated intestinal fluid (pH 6.8) for 4 hours, the simultaneous release rate of GABA and vitamin D is ≥90%, achieving precise intestinal delivery and making it suitable for industrial production.

Description

Technical Field

[0001] This invention belongs to the field of biomedical technology, specifically relating to a GABA-vitamin D neuroprotective composition and its preparation method. Background Technology

[0002] Gamma-aminobutyric acid (GABA), an important inhibitory neurotransmitter in the central nervous system, plays a role in improving sleep, relieving anxiety, and preventing neurodegenerative diseases. Healthy regulation of the nervous system typically requires the synergistic participation of multiple nutrients, among which vitamin D (VD) has significant neuroimmunomodulatory functions, and it exhibits remarkable synergistic potential with GABA in maintaining neuronal homeostasis and protecting nerve cells. With the deepening of research in the field of neurohealth, higher demands are placed on the stability and synergistic absorption of functional compositions under different physiological environments.

[0003] The physicochemical properties of a composition are among the most important characteristics affecting its bioavailability, and are crucial factors in determining the retention rate of the active ingredient in the gastrointestinal tract and the efficiency of transmembrane transport. Furthermore, stability is also a significant factor affecting the storage and efficacy of the composition. For most bioactive substances, GABA is easily degraded in the acidic environment of the stomach and exhibits a significant first-pass effect, leading to a reduction in the effective dose entering the circulatory system. Vitamin D, on the other hand, is a highly lipid-soluble substance, extremely sensitive to light, heat, and oxygen, and readily precipitates in aqueous systems, resulting in poor flowability and limited bioavailability. To improve the stability of components, researchers have attempted to adjust their state through physical mixing or the preparation of simple emulsions. However, due to differences in polarity and stability requirements between components, their ability to withstand physiological environments and maintain activity has been weakened.

[0004] GABA and vitamin D are commonly used active ingredients in the field of neuroprotection. GABA is highly hydrophilic, but it is easily destroyed by the acidic environment when passing through the digestive tract; while vitamin D exhibits strong lipid solubility and is easily oxidized and degraded when exposed to moisture or air. These characteristics have made the combined application of the two attractive in functional foods and pharmaceutical preparations. However, conventional physical mixing or simple emulsion systems cannot guarantee the physicochemical stability of the two in the same microenvironment, and with changes in environmental conditions, component separation or degradation and inactivation are very likely to occur, which greatly limits their application in neuroprotection and precise delivery.

[0005] Studies have found that adding traditional surfactants or stabilizers to compositions can adjust the dispersion of GABA and vitamin D, but this can easily affect their synchronous release characteristics and synergistic bioavailability at the intestinal absorption site. Therefore, finding a suitable method to address the poor stability and asynchronous absorption of GABA and vitamin D in complex systems holds great promise for future applications. Summary of the Invention

[0006] This application provides a GABA-vitamin D neuroprotective composition and its preparation method, aiming to solve the problems of poor stability and asynchronous absorption of GABA and vitamin D in complex systems.

[0007] The first aspect of this application provides a GABA-vitamin D neuroprotective composition comprising a medium-chain triglyceride, a modified phospholipid, and a GABA-vitamin D blend.

[0008] The medium-chain triglycerides and modified phospholipids in the GABA-vitamin D neuroprotective composition described in this application have low interfacial tension and strong amphiphilic compatibility, which can be miscible with GABA-vitamin D blends and improve their easy degradation and oxidative inactivation characteristics under complex physiological environments.

[0009] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the medium-chain triglycerides include one or more of caprylic acid glyceride, caprylic / capric acid glyceride, caprylic / capric acid glyceride, laurate glyceride, and myristate glyceride.

[0010] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the medium-chain triglyceride is one or more of caprylic glyceride, capric glyceride, and caprylic / capric glyceride.

[0011] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the modified phospholipid includes one or more of hydroxylated soybean phospholipids, acetylated soybean phospholipids, enzymatically hydrolyzed soybean phospholipids, and hydrogenated soybean phospholipids.

[0012] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the modified phospholipid is one or more of hydroxylated soybean phospholipid, acetylated soybean phospholipid, and enzymatically hydrolyzed soybean phospholipid.

[0013] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the mass ratio of the medium-chain triglyceride, the modified phospholipid, and the GABA-vitamin D blend is (1−5):(0−3):(0−9).

[0014] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the mass ratio of the medium-chain triglyceride, the modified phospholipid, and the GABA-vitamin D blend is (0.6−1.5):1:(1−1.6).

[0015] According to some embodiments of the GABA-vitamin D neuroprotective composition described in this application, the polydispersity index (PDI) of the GABA-vitamin D neuroprotective composition in the dispersion system is 0.15–0.55.

[0016] A second aspect of this application provides a method for preparing the GABA-vitamin D neuroprotective composition described in the first aspect of this application, comprising the following steps: mixing medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend to obtain the GABA-vitamin D neuroprotective composition.

[0017] The mixed system prepared by the method of this application has the characteristics of high encapsulation rate, uniform particle size distribution and high bioavailability, and is suitable for industrial production.

[0018] According to some embodiments of the preparation method of the GABA-vitamin D neuroprotective composition described in this application, the mixing temperature is 50–80 °C and the mixing time is 10–60 min. Attached Figure Description

[0019] Figure 1 This is a flowchart illustrating the preparation method of the GABA-vitamin D neuroprotective composition for this invention application;

[0020] Figure 2 This invention application provides a structural block diagram of the GABA-vitamin D neuroprotective composition. Detailed Implementation

[0021] The embodiments of the present invention are described in detail below. These embodiments are exemplary and intended to explain the present invention, and should not be construed as limiting the present invention.

[0022] In this invention, the terms "an embodiment," "some embodiments," "example," "specific example," or "some examples," etc., refer to a specific feature, structure, material, or characteristic described in connection with that embodiment or example, which is included in at least one embodiment or example of the invention. In this specification, the illustrative expressions of the above terms do not necessarily refer to the same embodiment or example. Furthermore, the specific features, structures, materials, or characteristics described may be combined in any suitable manner in one or more embodiments or examples. Moreover, without contradiction, those skilled in the art can combine and integrate the different embodiments or examples described in this specification, as well as the features of different embodiments or examples.

[0023] This application provides a GABA-vitamin D neuroprotective composition comprising medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend. The medium-chain triglycerides and modified phospholipids in the GABA-vitamin D neuroprotective composition of this application possess low interfacial tension and strong amphiphilic compatibility, allowing them to be miscible with the GABA-vitamin D blend and improving its susceptibility to degradation and oxidative inactivation under complex physiological conditions.

[0024] In some embodiments of this application, the medium-chain triglycerides include one or more of caprylic acid glyceride, caprylic / capric acid glyceride, caprylic / capric acid glyceride, laurate glyceride, and myristate glyceride.

[0025] In some embodiments of this application, the medium-chain triglyceride is one or more of caprylic acid glyceride, caprylic acid glyceride, and caprylic / capric acid glyceride. Caprylic acid glyceride, due to its shorter carbon chain structure, exhibits weaker intermolecular forces and is miscible with fat-soluble vitamins and modified phospholipids. It also possesses excellent metabolic stability, good dispersibility, hydrophobicity, and low surface tension, thus making it an excellent base oil for materials such as carriers and solubilizers of fat-soluble active substances.

[0026] In some embodiments of this application, the modified phospholipids include one or more of hydroxylated soybean phospholipids, acetylated soybean phospholipids, enzymatically hydrolyzed soybean phospholipids, and hydrogenated soybean phospholipids.

[0027] In some embodiments of this application, the modified phospholipid is one or more of hydroxylated soybean phospholipid, acetylated soybean phospholipid, and enzymatically hydrolyzed soybean phospholipid. Hydroxylated soybean phospholipid is produced by introducing hydroxyl functional groups into the phospholipid molecule. Physically, it presents as a pale yellow to brown viscous liquid or powder, and its hydrophilic-lipophilic balance (HLB) varies with the degree of hydroxylation. With increasing hydroxyl content, its dispersibility and emulsifying ability in aqueous systems are enhanced, significantly reducing oil-water interfacial tension. It also exhibits excellent antioxidant and thermal stability, effectively protecting the encapsulated active components in complex gastrointestinal environments.

[0028] In some embodiments of this application, the mass ratio of the medium-chain triglyceride, the modified phospholipid, and the GABA-vitamin D blend is (1−5):(0−3):(0−9).

[0029] In some embodiments of this application, the mass ratio of the medium-chain triglycerides, the modified phospholipids, and the GABA-vitamin D blend is (0.6–1.5):1:(1–1.6), for example, 0.6:1:1, 0.8:1:1, 1:1:1, 1.2:1:1.2, 1.5:1:1.5, 1.5:1:1.6, etc. The neuroprotective composition obtained within this ratio range exhibits optimal stability and component release synchronization in a simulated gastrointestinal fluid environment, showing a trend of consistency between particle size stability and bioavailability, thus constructing a stable and precise intestinal delivery system.

[0030] In some embodiments of this application, the polydispersity index (PDI) of the GABA-vitamin D neuroprotective composition in the dispersion system is 0.15–0.55, for example, 0.15, 0.20, 0.25, 0.30, 0.36, 0.38, 0.43, 0.45, 0.5, 0.52, 0.55, etc. The polydispersity index (PDI) is a key factor affecting the composition's distribution in vivo, physical stability, and transmembrane absorption efficiency. The smaller the PDI, the more uniform the particle distribution in the system. The larger the PDI, the greater the risk of Austronesian ripening or aggregation and precipitation during storage or digestion, and the longer the time required for the active ingredient to reach the absorption site. This can easily lead to component separation, resulting in GABA degradation or vitamin D oxidation, thereby reducing the synergistic neuroprotective effect. The composition of this application has a PDI of 0.15–0.55, indicating good dispersion uniformity, which solves the problems of poor stability and asynchronous absorption of GABA and vitamin D in complex systems.

[0031] This application also provides a method for preparing the GABA-vitamin D neuroprotective composition described in the first aspect of this application, comprising the following steps: mixing medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend to obtain the GABA-vitamin D neuroprotective composition. The mixed system obtained by the preparation method of this application has the characteristics of high encapsulation rate, uniform particle size distribution, and high bioavailability, making it suitable for industrial production.

[0032] In some embodiments of this application, the mixing temperature is 50–80 °C, such as 50 °C, 60 °C, 70 °C, 80 °C, etc., and the mixing time is 10–60 min, such as 10 min, 20 min, 30 min, 40 min, 50 min, 60 min, etc.

[0033] The technical solution of this application will be further explained below with reference to specific implementation cases.

[0034] Example 1

[0035] A GABA-vitamin D neuroprotective composition comprises 3g caprylic / capric triglyceride, 3g hydroxylated soybean lecithin, and 3g GABA-vitamin D blend. The preparation method of the GABA-vitamin D neuroprotective composition includes the following steps: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol; specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g caprylic acid glyceride, 3g hydroxylated soybean lecithin and 3g GABA-vitamin D blend at a mass ratio of 1:1:1, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0036] Example 2

[0037] The difference between Example 2 and Example 1 is that the GABA-vitamin D neuroprotective composition in Example 2 includes 3g caprylic acid glyceride, 2g hydroxylated soybean lecithin, and 5g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g caprylic acid glyceride, 2g hydroxylated soybean lecithin and 5g GABA-vitamin D blend in a mass ratio of 3:2:5, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at 20kHz for 30min, and then place in an oil bath at 60℃ for 30min to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0038] Example 3

[0039] The difference between Example 3 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 3 includes 3g caprylic acid glyceride, 3g hydroxylated soybean lecithin, and 4g GABA-vitamin D blend. Specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of caprylic acid glyceride, 3g of hydroxylated soybean lecithin and 4g of GABA-vitamin D blend in a mass ratio of 3:3:4, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0040] Example 4

[0041] The only difference between Example 4 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 4 includes 2g caprylic acid glyceride, 3g hydroxylated soybean lecithin, and 5g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 2g of caprylic glyceride, 3g of hydroxylated soybean lecithin and 5g of GABA-vitamin D blend at a mass ratio of 2:3:5, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0042] Example 5

[0043] The difference between Example 5 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 5 includes 3g of decanoic acid glyceride, 3g of hydroxylated soybean lecithin, and 3g of GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of decanoic acid glyceride, 3g of hydroxylated soybean lecithin and 3g of GABA-vitamin D blend in a mass ratio of 3:3:3, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0044] Example 6

[0045] The difference between Example 6 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 6 includes 3g caprylic acid glyceride, 3g acetylated soybean lecithin, and 3g GABA-vitamin D blend. Specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in a 60°C oven and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of caprylic glyceride, 3g of acetylated soybean lecithin and 3g of GABA-vitamin D blend in a mass ratio of 3:3:3, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at 20kHz for 30 minutes, and then place in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0046] Example 7

[0047] The only difference between Example 7 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 7 includes 3g caprylic / capric triglyceride, 3g enzymatically hydrolyzed soybean lecithin, and 3g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of caprylic / capric triglyceride, 3g of enzymatically hydrolyzed soybean lecithin and 3g of GABA-vitamin D blend at a mass ratio of 1:1:1, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0048] Example 8

[0049] The difference between Example 8 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 8 includes 3g caprylic acid glyceride, 3g hydrogenated soybean lecithin, and 3g GABA-vitamin D blend. Specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of caprylic glyceride, 3g of hydrogenated soybean lecithin and 3g of GABA-vitamin D blend in a mass ratio of 1:1:1, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0050] Example 9

[0051] The difference between Example 9 and Example 1 is only that the GABA-vitamin D neuroprotective composition described in Example 9 includes 3g caprylic / capric triglyceride, 3g caprylic / capric triglyceride, and 3g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 3g of caprylic / capric triglyceride, 3g of caprylic / capric triglyceride and 3g of GABA-vitamin D blend in a mass ratio of 1:1:1, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0052] Example 10

[0053] The only difference between Example 10 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 10 includes 2g caprylic acid glyceride, 2g hydroxylated soybean lecithin, and 6g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 2g of caprylic glyceride, 2g of hydroxylated soybean lecithin and 6g of GABA-vitamin D blend at a mass ratio of 1:1:3, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0054] Example 11

[0055] The only difference between Example 11 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 11 comprises 1g caprylic acid glyceride, 2g hydroxylated soybean lecithin, and 7g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 1g caprylic acid glyceride, 2g hydroxylated soybean lecithin and 7g GABA-vitamin D blend at a mass ratio of 1:2:7, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0056] Example 12

[0057] The only difference between Example 12 and Example 1 is that the GABA-vitamin D neuroprotective composition described in Example 12 comprises 1g caprylic acid glyceride, 1g hydroxylated soybean lecithin, and 8g GABA-vitamin D blend. The specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, the beaker is ultrasonically cleaned with deionized water for 15 minutes, followed by ultrasonic cleaning with acetone for 15 minutes, and then ultrasonic cleaning with anhydrous ethanol for 15 minutes. The beaker is then placed in an oven at 60°C and dried for 12 hours for later use. Step 2: Compound composition: Weigh 1g caprylic acid glyceride, 1g hydroxylated soybean lecithin and 8g GABA-vitamin D blend at a mass ratio of 1:1:8, with an accuracy of 0.001g. Mix them in the beaker dried in Step 1, sonicate at a frequency of 20kHz for 30 minutes, and then place them in an oil bath at 60℃ for 30 minutes to fully dissolve them, finally obtaining a GABA-vitamin D neuroprotective composition with excellent stability.

[0058] Comparative Example 1

[0059] The only difference between Comparative Example 1 and Example 1 is that the GABA-vitamin D neuroprotective composition in Comparative Example 1 uses soybean oil instead of caprylic / capric triglycerides and hydroxylated soybean phospholipids. The specific steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then dried in a 60°C oven for 12 hours. Step 2: Compounding: 6g of soybean oil and 3g of GABA-vitamin D blend are weighed at a mass ratio of 2:1 (accuracy 0.001g). They are mixed in the dried beaker from Step 1 and ultrasonically sonicated at 20kHz for 30 minutes. The mixture is then placed in an oil bath at 60°C for 30 minutes to fully dissolve the GABA-vitamin D neuroprotective composition, ultimately obtaining a stable GABA-vitamin D neuroprotective composition.

[0060] Comparative Example 2

[0061] The only difference between Comparative Example 2 and Example 1 is that the GABA-vitamin D neuroprotective composition in Comparative Example 2 uses Tween-80 instead of hydroxylated soybean lecithin. The specific steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then dried in a 60°C oven for 12 hours. Step 2: Compounding: 3g of caprylic / capric triglyceride, 3g of Tween-80, and 3g of GABA-vitamin D blend are weighed in a mass ratio of 1:1:1, with an accuracy of 0.001g. These are mixed in the dried beaker from Step 1 and ultrasonically sonicated at 20kHz for 30 minutes. The mixture is then placed in an oil bath at 60°C for 30 minutes to fully dissolve the GABA-vitamin D neuroprotective composition, ultimately obtaining a stable GABA-vitamin D neuroprotective composition.

[0062] Comparative Example 3

[0063] The only difference between Comparative Example 3 and Example 1 is that the GABA-vitamin D neuroprotective composition in Comparative Example 3 uses magnesium stearate instead of glyceryl caprylate. The specific steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then dried in a 60°C oven for 12 hours. Step 2: Compounding: 3g of magnesium stearate, 3g of hydroxylated soybean lecithin, and 3g of GABA-vitamin D blend are weighed at a mass ratio of 1:1:1, with an accuracy of 0.001g. These are mixed in the dried beaker from Step 1, ultrasonicated at 20kHz for 30 minutes, and then placed in an oil bath at 60°C for 30 minutes to fully dissolve the mixture, ultimately obtaining a stable GABA-vitamin D neuroprotective composition.

[0064] Comparative Example 4

[0065] The only difference between Comparative Example 4 and Example 1 is that the composition of Comparative Example 4 does not contain hydroxylated soybean lecithin. Specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then dried in a 60°C oven for 12 hours. Step 2: Compounding: 3g of caprylic / capric glyceride and 3g of GABA-vitamin D blend are weighed at a mass ratio of 1:1, with an accuracy of 0.001g. They are mixed in the dried beaker from Step 1, ultrasonicated at 20kHz for 30 minutes, and then placed in an oil bath at 60°C for 30 minutes to fully dissolve the mixture, ultimately obtaining a stable GABA-vitamin D neuroprotective composition.

[0066] Comparative Example 5

[0067] The only difference between Comparative Example 5 and Example 1 is that the composition of Comparative Example 5 does not contain the raw materials hydroxylated soybean lecithin and caprylic acid glyceride.

[0068] Comparative Example 6

[0069] The only difference between Comparative Example 6 and Example 1 is that the composition of Comparative Example 6 does not contain the raw material caprylic / capric triglyceride. Specific operating steps include: Step 1: Pretreatment: The beaker is ultrasonically cleaned sequentially with deionized water, acetone, and anhydrous ethanol. Specifically, it is ultrasonically cleaned with deionized water for 15 minutes, then with acetone for 15 minutes, and then with anhydrous ethanol for 15 minutes. The beaker is then dried in a 60°C oven for 12 hours. Step 2: Compounding: 3g of hydroxylated soybean lecithin and 3g of GABA-vitamin D blend are weighed at a mass ratio of 1:1, with an accuracy of 0.001g. They are mixed in the dried beaker described in Step 1, ultrasonicated at 20kHz for 30 minutes, and then placed in an oil bath at 60°C for 30 minutes to fully dissolve, ultimately obtaining a stable GABA-vitamin D neuroprotective composition.

[0070] The dispersibility of the GABA-vitamin D neuroprotective compositions described in Examples 1-12 and Comparative Examples 1-6 of this application was tested using a laser particle size analyzer to determine the polydispersity index (PDI) of the composition dispersion system. Specifically, the composition sample was first added to deionized water and stirred at 100 rpm for 15 minutes at 37 °C. Then, a sample was placed in a measuring cell, and the refractive index and viscosity parameters were set. Each sample was measured three times, and the average value was taken. Simultaneously, the retention rate of the active ingredient after treatment with simulated gastric fluid (pH 1.2) for 2 hours was tested. The test results are shown in Table 1.

[0071]

[0072] As can be seen from Table 1, the combination of modified phospholipids and medium-chain triglycerides can effectively improve the dispersion uniformity of the composition system and achieve effective protection of GABA and vitamin D under complex environments.

[0073] Although the above embodiments have been shown and described, it is understood that the above embodiments are exemplary and should not be construed as limiting the present invention. Any changes, modifications, substitutions and variations made to the above embodiments by those skilled in the art are within the protection scope of the present invention.

Claims

1. A GABA-vitamin D neuroprotective composition, characterized in that, The mixture comprises medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend; the medium-chain triglycerides include one or more of caprylic glyceride, caprylic glyceride, caprylic-caprylic glyceride, laurate glyceride, and myristate glyceride; the modified phospholipids include one or more of hydroxylated soybean phospholipids, acetylated soybean phospholipids, enzymatically hydrolyzed soybean phospholipids, and hydrogenated soybean phospholipids; the mass ratio of the medium-chain triglycerides, the modified phospholipids, and the GABA-vitamin D blend is (0.6–1.5):1:(1–1.6).

2. The GABA-vitamin D neuroprotective composition according to claim 1, characterized in that, The modified phospholipid is one or more of hydroxylated soybean phospholipid, acetylated soybean phospholipid, and enzymatically hydrolyzed soybean phospholipid.

3. The GABA-vitamin D neuroprotective composition according to any one of claims 1-2, characterized in that, The polydispersity index (PDI) of the GABA-vitamin D neuroprotective composition in the dispersion system is 0.15–0.

55.

4. The GABA-vitamin D neuroprotective composition according to claim 1, characterized in that, The medium-chain triglycerides are one or more of caprylic glyceride, caprylic glyceride, and caprylic / capric glyceride.

5. The GABA-vitamin D neuroprotective composition according to claim 1, characterized in that, The mass ratio of the medium-chain triglyceride, the modified phospholipid, and the GABA-vitamin D blend is (1−5):(0−3):(0−9).

6. A method for preparing the GABA-vitamin D neuroprotective composition according to any one of claims 1-5, characterized in that, The method includes the following steps: mixing medium-chain triglycerides, modified phospholipids, and a GABA-vitamin D blend to obtain the GABA-vitamin D neuroprotective composition; the medium-chain triglycerides include one or more of caprylic glyceride, caprylic glyceride, caprylic-caprylic glyceride, laurate glyceride, and myristate glyceride; the modified phospholipids include one or more of hydroxylated soybean phospholipids, acetylated soybean phospholipids, enzymatically hydrolyzed soybean phospholipids, and hydrogenated soybean phospholipids.

7. The method for preparing the GABA-vitamin D neuroprotective composition according to claim 6, characterized in that, The mixing temperature is 50–80 °C, and the mixing time is 10–60 min.

8. The method for preparing the GABA-vitamin D neuroprotective composition according to claim 6, characterized in that, Prior to the mixing step, a pretreatment step is included, which involves ultrasonic cleaning with deionized water, acetone and anhydrous ethanol in sequence, followed by drying at 60 °C for 12 h.

9. The method for preparing the GABA-vitamin D neuroprotective composition according to claim 6, characterized in that, The mixing process is accompanied by ultrasonic treatment, the frequency of which is 20 kHz and the duration of which is 30 min.

10. The method for preparing the GABA-vitamin D neuroprotective composition according to claim 6, characterized in that, The mixture was fully dissolved in an oil bath at 60 °C for 30 min.

Images