CN111728209A - Composition for enhancing bioavailability of silymarin - Google Patents

Composition for enhancing bioavailability of silymarin Download PDF

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CN111728209A
CN111728209A CN201911264420.XA CN201911264420A CN111728209A CN 111728209 A CN111728209 A CN 111728209A CN 201911264420 A CN201911264420 A CN 201911264420A CN 111728209 A CN111728209 A CN 111728209A
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oil
silymarin
composition
food composition
lecithin
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金志成
朴赞雄
赵源庆
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Amorepacific Corp
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    • A23V2250/00—Food ingredients
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    • A23V2250/184—Emulsifier
    • A23V2250/1842—Lecithin
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    • A23V2250/00—Food ingredients
    • A23V2250/18—Lipids
    • A23V2250/184—Emulsifier
    • A23V2250/1846—Phosphatidyl Choline

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Abstract

The present disclosure relates to a composition for enhancing bioavailability of silymarin, comprising one or more of lecithin and phosphatidylcholine as an effective ingredient, wherein the composition is added to a food composition comprising silymarin and vegetable oil. More specifically, the composition for enhancing the bioavailability of silymarin according to the present disclosure can effectively enhance the bioavailability of silymarin, but does not include a synthetic surfactant. In addition, the food composition comprising the composition for enhancing the bioavailability of silymarin according to the present disclosure has excellent silymarin solubility and bioavailability, but does not use a synthetic surfactant and an organic solvent, and can also prevent side effects caused by the synthetic surfactant or the organic solvent.

Description

Composition for enhancing bioavailability of silymarin
Background
Technical Field
The present disclosure relates to a composition for enhancing the bioavailability of silymarin and a food composition comprising the same.
Description of the Related Art
Silymarin is a component extracted from the eriodictyol of Silybum marianum (Silybum marianum), a medicinal plant belonging to the family Compositae, and is a flavonoid-based compound. The plant is of south europe and north africa and is also grown in the continental americas, and the plant has therefore been cultivated as an ornamental or medicinal plant.
Silymarin is known to stabilize the liver cell membrane, thereby inhibiting the inflow of harmful substances into the cells, and to activate protein synthesis of the liver cells, thereby promoting the regeneration of the liver cells. Therefore, it has been widely used for treating various liver diseases caused by smoking, drinking, overworking, and environmental pollution due to various pollutions.
Preparations containing silymarin as an active ingredient have been widely used clinically for the treatment of liver diseases. However, silymarin, which is an active ingredient thereof, is a water-insoluble substance, which is rarely dissolved in water, and has low absorption when orally administered, and thus, its bioavailability is only about 20-40%. Therefore, enhancing bioavailability by increasing solubility and dissolution rate is considered to be important in the development of silymarin-containing formulations.
In the related art, in order to increase the low solubility and bioavailability of silymarin, a self-emulsifying drug delivery system consisting of a drug, an oil, a surfactant, a co-surfactant, a solvent, and the like has been applied. However, in this case, there is a disadvantage in that a large amount of synthetic surfactant (e.g., polysorbate, etc.) and a large amount of organic solvent (e.g., hexane, etc.) which are not used for food and may cause more irritation (e.g., gastritis and gastric ulcer) to a user having gastrointestinal diseases or cause side effects such as diarrhea, abdominal pain, etc., are used. In addition, the volume of the formulation becomes larger, which is inconvenient for ingestion.
Further, in the case of silymarin as a tablet, there is a demand for soft capsules due to low consumer preference due to specific odor or the like, and in terms of convenience of taking, a technology of containing a high content of functional ingredients in a small size is required.
Reference list
Patent document
Patent document 1: korean patent laid-open No. 10-2005-0075074
Disclosure of Invention
In order to solve the above problems, it is an object of the present disclosure to provide a composition for enhancing the bioavailability of silymarin, which effectively enhances the dissolution and bioavailability of silymarin while exhibiting no side effects because it does not contain a synthetic surfactant, and a food composition exhibiting excellent bioavailability of silymarin.
To achieve the object, in one aspect, the present disclosure provides a composition for enhancing bioavailability of silymarin, comprising one or more of lecithin and phosphatidylcholine as effective ingredients, wherein the composition is added to a food composition comprising silymarin and vegetable oil such that the weight ratio of the silymarin to the one or more of lecithin and phosphatidylcholine is 1: 0.08 or more and is 1: 2.31 or less.
In another aspect, the present disclosure provides a composition for enhancing bioavailability of silymarin, comprising one or more of lecithin and phosphatidylcholine as effective ingredients, wherein the composition is added to a food composition comprising silymarin and vegetable oil, and the food composition has a dissolution concentration of silymarin of 6-31 μ g/mL within 240 minutes when tested for dissolution in purified water according to the paddle method according to the dissolution determination method of the korean pharmacopoeia.
In another aspect, the present disclosure provides the use of one or more of lecithin and phosphatidylcholine in the manufacture of a composition for enhancing the bioavailability of silymarin, wherein the composition is added to a food composition comprising silymarin and vegetable oil.
In another aspect, the present disclosure provides the use of one or more of lecithin and phosphatidylcholine for enhancing the bioavailability of silymarin, wherein the one or more of lecithin and phosphatidylcholine is added to a food composition comprising silymarin and a vegetable oil.
Drawings
Fig. 1 shows the dissolution rate test results according to test example 1.
Fig. 2 shows the results of the disintegration test according to test example 2.
Fig. 3 shows the bioavailability test results according to test example 3.
Detailed Description
Hereinafter, the present disclosure will be explained in detail.
In one aspect, the present disclosure may relate to a composition for enhancing bioavailability of silymarin, which includes one or more of lecithin and phosphatidylcholine as an effective ingredient.
In another aspect, the present disclosure may relate to the use of one or more of lecithin and phosphatidylcholine in the preparation of a composition for enhancing the bioavailability of silymarin.
In a further aspect, the present disclosure may relate to the use of one or more of lecithin and phosphatidylcholine to enhance the bioavailability of silymarin.
The composition for enhancing the bioavailability of silymarin may be added to a food composition comprising silymarin and vegetable oil. In addition, the one or more of lecithin and phosphatidylcholine may be added to a food composition comprising silymarin and vegetable oil.
Silymarin is known to stabilize the liver cell membrane, thereby inhibiting the inflow of harmful substances into the cells, and to activate protein synthesis of the liver cells, thereby promoting the regeneration of the liver cells. Specifically, silymarin is known to have a strong antioxidant action, reduce phospholipid synthesis, prevent hyper-accumulation of neutral lipids, lower serum LDL, and promote recovery of patients suffering from inflammation, cancer, acute viral hepatitis, chronic hepatitis complications, and liver cirrhosis. Thus, silymarin has been widely used to treat various liver diseases caused by smoking, drinking, overworking, and environmental pollution caused by various pollutions.
In addition, the silymarin is an aggregate of flavanlignan in which silibinin (which is a main component), silicristin (which is an isomer of silibinin), silidianin and isosilibinin are mixed.
In one embodiment, the silymarin may be obtained from an extract of milk thistle. Here, "milk thistle" refers to the plant milk thistle, "milk thistle extract" refers to a substance obtained by isolation from milk thistle, and more specifically, the extract refers to a substance obtained by isolation from milk thistle by using a typical extraction solvent known in the art, such as water, C1-C4 alcohols (e.g., methanol, ethanol, butanol, etc.), or a mixed solvent of the alcohols and water.
Further, the milk thistle extract can be obtained by known various extraction methods (e.g., hot water extraction, organic solvent extraction, supercritical extraction, or the like), and can be prepared in a powder form by another method such as distillation under reduced pressure and freeze-drying or spray-drying, or the like.
In one embodiment, the lecithin may be one or more of soybean lecithin and egg yolk lecithin.
The present disclosure may include natural surfactants such as lecithin and phosphatidylcholine, and does not use synthetic surfactants such as polysorbate, thereby not showing side effects caused by a large amount of synthetic surfactants.
In one embodiment, the vegetable oil may be one or more selected from the group consisting of soybean oil, sunflower oil, rapeseed oil, avocado oil, corn oil, palm oil, coconut oil, rice bran oil, cottonseed oil, castor oil, sesame seed oil, linseed oil, olive oil, canola oil (canola oil), grape seed oil, almond oil, peanut oil, hazelnut oil, and walnut oil.
In one embodiment, the composition is added to a food composition such that the ratio of silymarin: the weight ratio of one or more of lecithin and phosphatidylcholine is 1: 0.08 or greater and 1: 2.31 or less.
In another embodiment, in the food composition, the weight ratio of one or more of silymarin lecithin and phosphatidylcholine may be 1: 0.08 or greater, 1: 0.15 or greater, 1: 0.23 or greater, 1: 0.35 or greater, 1: 0.40 or greater, 1: 0.46 or greater, 1: 0.53 or greater, 1: 1 or greater, 1: 1.23 or greater or 1: 1.53 or greater, and further, the weight ratio of one or more of silymarin lecithin and phosphatidylcholine may be 1: 2.31 or less, 1: 2.3 or less, 1: 2 or less, 1: 1.7 or less, 1: 1.53 or less, 1: 1.4 or less, 1: 1.23 or less, 1: 1 or less, 1: 0.7 or less, 1: 0.53 or less, or 1: 0.46 or less. Preferably, the weight ratio of silymarin to one or more of lecithin and phosphatidylcholine in the food composition may be 1: 0.46 to 1: 1.53, and within said range the bioavailability of silymarin may be higher.
In one embodiment, the food composition according to the present disclosure may be a soft capsule formulation. In another embodiment, when preparing a soft capsule formulation, the food composition may be prepared by appropriately selecting ingredients generally used in the related art, in addition to the active ingredient, by those skilled in the art.
In one embodiment, the food composition may have a viscosity of 1800cps or less. Specifically, the viscosity of the food composition may be 1800cps or less, 1600cps or less, 1400cps or less, 1200cps or less, 1000cps or less, 800cps or less, 600cps or less, 400cps or less, 200cps or less, and further, may be 10cps or more, 50cps or more, 100cps or more, 200cps or more, 400cps or more, 600cps or more, 800cps or more, 1000cps or more, 1200cps or more, 1400cps or more, or 1600cps or more.
In one embodiment, when the dissolution rate in purified water is tested according to the paddle method in the dissolution determination method according to the korean pharmacopoeia, the dissolution rate is measured by rotating at a rotation frequency of 150rpm at 37 ℃ using 500mL of purified water as a dissolution solution, and the food composition has a dissolution concentration of silymarin of 6-31 μ g/mL in 240 minutes. In another embodiment, the dissolution concentration of silymarin may be 6. mu.g/mL or more, 6.5. mu.g/mL or more, 7. mu.g/mL or more, 8. mu.g/mL or more, 8.5. mu.g/mL or more, 9. mu.g/mL or more, 9.5. mu.g/mL or more, 15. mu.g/mL or more, 19. mu.g/mL or more, 19.6. mu.g/mL or more, 23. mu.g/mL or more, 24. mu.g/mL or more, 26. mu.g/mL or more, 28. mu.g/mL or more, or 30. mu.g/mL or more. Furthermore, the dissolution concentration of silymarin may be 31. mu.g/mL or less, 28.5. mu.g/mL or less, 25.5. mu.g/mL or less, or 22. mu.g/mL or less. Preferably, the dissolution concentration of silymarin may be 19.6-31 μ g/mL.
According to one embodiment, the food composition according to the present disclosure may be a health functional food composition and may be used to improve liver function.
Herein, "improving" includes treating, alleviating, and preventing symptoms, and in the present disclosure, the term refers to treating, alleviating, or preventing liver function, liver disorder, liver disease, and liver disease.
In the present disclosure, "prevention" refers to inhibiting or delaying all the behavior of liver disease outbreaks by administering a composition according to the present disclosure.
In the present disclosure, "liver disease" includes, but is not limited to, all liver diseases that can be treated, alleviated, or prevented by the composition of the present disclosure, and examples thereof include non-alcoholic fatty liver, hepatitis, cirrhosis, liver cancer, and the like.
The health functional food composition of the present disclosure may include supplementary ingredients for nutrition, and additives for enhancing sensory acceptability and forming a formulation within a range that does not impair the effects of the present disclosure.
Hereinafter, the present disclosure will be explained in more detail with reference to examples and test examples. However, these examples and test examples are provided only for understanding the present disclosure, and the scope of the present disclosure is not limited to the examples and test examples. Any modification, substitution, and insertion, etc. generally known in the related art may be performed, and are also covered by the scope of the present disclosure.
[ examples and comparative examples ]
Examples 1 to 21 and comparative examples 1 to 4, which are compositions having a total content of 600mg, were prepared according to the compositions of Table 1 below (unit: mg).
TABLE 1
Figure BDA0002312445650000061
[ test example 1] evaluation of dissolution of silymarin
The dissolution rates of examples 1-21, comparative examples 1-4 and milk thistle extracts were compared and evaluated. The milk thistle extract is a raw material prepared as follows: separating and extracting from milk thistle (Silybum marianum), filtering, concentrating, purifying, and using milk thistle extract (HONSON) with silymarin content of 50%
Figure BDA0002312445650000062
Canada).
Dissolution evaluation assay was performed by dissolution evaluation assay in accordance with the dissolution assay method of korean pharmacopoeia to evaluate dissolution in vitro, and the amount of silybin, which is a main component of silymarin, was quantified and evaluated by HPLC analysis method. More specifically, according to the Paddle method according to the dissolution determination project of the Korean pharmacopoeia, 3ml of each of examples 1 to 21, comparative examples 1 to 4 and milk thistle extract was taken, and 500ml of purified water was used as a dissolution solution, and the dissolution rate was measured at 37 ℃ at a rotation frequency of 150 rpm. The results are shown in Table 2 below (unit:. mu.g/mL) and in FIG. 1.
TABLE 2
Figure BDA0002312445650000071
The results shown in table 2 and fig. 1 show that examples 1 to 21, which contained one or more of lecithin and phosphatidylcholine, silymarin and soybean oil, exhibited higher dissolution concentrations of silymarin than comparative example 1, which contained only silymarin and soybean oil. Thus, it was confirmed that the dissolution rate of silymarin was increased by including one or more of lecithin and phosphatidylcholine.
Furthermore, it can be confirmed that examples 7 to 21 comprising one or more of lecithin and phosphatidylcholine in a weight ratio of 1: 0.46 to 1: 1.53 have a much higher dissolution concentration of silymarin after 240 minutes of the dissolution test, as compared to the milk thistle extract.
As can be seen from the above, it was confirmed that the health functional food composition comprising the composition for enhancing bioavailability of silymarin according to the present disclosure and silymarin has greatly enhanced bioavailability due to excellent dissolution rate of silymarin.
On the other hand, it was confirmed that comparative examples 2 to 4 had increased dissolution concentration of silymarin because the amount of one or more of lecithin and phosphatidylcholine was increased, but as will be shown in test example 2 below, the measurement results of the degree of disintegration showed that formulation as a soft capsule was not possible.
Test example 2 disintegration measurement of Soft Capsule preparation
A disintegration test was conducted to evaluate whether the compositions of example 11 and comparative example 2 were suitable for production as a soft capsule formulation. The disintegration measurement was performed according to the disintegration measurement method among the general measurement methods in the korean food standard Codex. Specifically, water was used as the measurement solution, and a disintegration tester (J-DTC2,
Figure BDA0002312445650000081
) And (4) carrying out measurement. In the case of the soft capsule, it should be completely disintegrated within 20 minutes, and the auxiliary plate is placed and moved up and down for 20 minutes, and then it is determined that the disintegration is complete if no residue of the corresponding composition remains in the glass tube, or if the residue is a film even though the residue remains.
The results are shown in FIG. 2. From the results of fig. 2, it can be confirmed that the composition according to example 11 of the present disclosure is suitable for production as a soft capsule because it is completely disintegrated within 20 minutes. In contrast, in the case of comparative example 2, it was confirmed that the weight ratio of silymarin to one or more of lecithin and phosphatidylcholine was 1: 2.31, and thus the amounts of lecithin and phosphatidylcholine were too high, so that the viscosity was high and thus not completely disintegrated within 20 minutes. Therefore, the composition is not suitable for the production as a soft capsule.
[ test example 3] evaluation of bioavailability
The pharmacokinetics of each milk thistle extract of test example 1 and the composition of example 11 were examined to evaluate the bioavailability of silibinin, which is the main component of silymarin. Specifically, 200mg/kg of milk thistle extract and the composition of example 11 were orally administered to five SD rats based on the silybin concentration, and then blood samples were taken 11 times in total (0 min, 2 min, 5 min, 10 min, 20 min, 30 min, 45 min, 60 min, 90 min, 120 min, 180 min) over time and analyzed using High Performance Liquid Chromatography (HPLC).
The HPLC analysis conditions were as follows.
-HPLC type: model Prominsence of Shimadzu HPLC-UV system
-analytical column: kientex C18 column (250X 4.6mm)
-a mobile phase: isocratic mode, 10mM ammonium acetate buffer acetonitrile 74: 26
-flow rate: 1.0mL/min
-UV wavelength: 288nm
-sample injection volume: 20 μ L
In the HPLC analysis method, specifically, 120. mu.L of SD rat plasma was taken, 400. mu.L of acetonitrile containing an internal standard substance (phenacetin 3. mu.g/mL) was added, and mixed for 5 minutes to deproteinize. The deproteinized sample was then centrifuged at 15,000 Xg for 10 minutes at 4 ℃ to obtain 400. mu.L of supernatant, which was then dried using a nitrogen concentrator and reconstituted with 60. mu.L of mobile phase. Then 20 μ L of the sample was injected into HPLC for analysis.
The results are shown in the following table and in fig. 3.
TABLE 3
Auclast(μg·min/ml) Cmax(μg/ml)
Milk thistle extract 76.5±19.2 1.02±0.24
Extract 11 207±28 3.13±0.49
(AuclastIs an index for comparing the total blood absorption of test drugs, CmaxIs the highest blood concentration index for the test drug. )
From the results of table 3 and fig. 3, it was verified that in the composition according to example 11 of the present disclosure, the total blood absorption and maximum concentration values of silibinin, which is the main component of silymarin, were greatly increased compared to the milk thistle extract. That is, it was confirmed that in example 11 according to the present disclosure, the bioavailability of silymarin was significantly higher than that of milk thistle extract.
The composition for enhancing the bioavailability of silymarin according to the present disclosure may effectively enhance the bioavailability of silymarin while not including a synthetic surfactant.
Furthermore, the food composition comprising the composition for enhancing the bioavailability of silymarin according to the present disclosure may exhibit excellent silymarin dissolution and bioavailability without using a synthetic surfactant and an organic solvent, and may also prevent side effects caused by the use of a synthetic surfactant or an organic solvent.
While the present disclosure has been described with respect to specific embodiments, it will be apparent to those skilled in the art that various changes and modifications may be made without departing from the spirit and scope of the disclosure as defined in the following claims.

Claims (12)

1. Use of one or more of lecithin and phosphatidylcholine in the manufacture of a composition for enhancing the bioavailability of silymarin, wherein the composition is added to a food composition comprising silymarin and vegetable oil.
2. Use according to claim 1, wherein the composition is added to the food composition such that the silymarin: the weight ratio of one or more of lecithin and phosphatidylcholine is 1: 0.08 or greater and 1: 2.31 or less.
3. The use according to claim 1, wherein the silymarin is obtained from milk thistle extract.
4. The use of claim 1, wherein the lecithin is one or more of soybean lecithin and egg yolk lecithin.
5. Use according to claim 1, wherein the vegetable oil is selected from one or more of the following: soybean oil, sunflower oil, rapeseed oil, avocado oil, corn oil, palm oil, coconut oil, rice bran oil, cottonseed oil, castor oil, sesame seed oil, linseed oil, olive oil, canola oil, grape seed oil, almond oil, peanut oil, hazelnut oil and walnut oil.
6. The use according to claim 1, wherein the silymarin: the weight ratio of one or more of lecithin and phosphatidylcholine is 1: 0.46 to 1: 1.53.
7. The use according to claim 1 wherein the food composition has a viscosity of 1800cps or less.
8. The use according to claim 1, wherein the food composition has a dissolution concentration of silymarin of 6 to 31 μ g/mL within 240 minutes when the dissolution in purified water is determined according to the paddle method in accordance with the dissolution determination method of the korean pharmacopoeia.
9. The use according to claim 1, wherein the silymarin has a dissolution concentration of 19.6 to 31 μ g/mL.
10. Use according to any one of claims 1-9, wherein the food composition is in the form of a soft capsule formulation.
11. A food composition comprising the composition for enhancing the bioavailability of silymarin according to any of claims 1 to 9, silymarin and vegetable oil.
12. The food composition of claim 11, wherein the food composition is in the form of a soft capsule formulation.
CN201911264420.XA 2019-03-25 2019-12-11 Composition for enhancing bioavailability of silymarin Pending CN111728209A (en)

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