CN117771318A - Medicinal polysaccharide functional explosive bead composition and preparation method thereof - Google Patents
Medicinal polysaccharide functional explosive bead composition and preparation method thereof Download PDFInfo
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- CN117771318A CN117771318A CN202410217548.5A CN202410217548A CN117771318A CN 117771318 A CN117771318 A CN 117771318A CN 202410217548 A CN202410217548 A CN 202410217548A CN 117771318 A CN117771318 A CN 117771318A
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- polysaccharide
- betel nut
- bead composition
- polyphenol
- betel
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- 229920001282 polysaccharide Polymers 0.000 title claims abstract description 102
- 239000005017 polysaccharide Substances 0.000 title claims abstract description 102
- 239000000203 mixture Substances 0.000 title claims abstract description 63
- 150000004676 glycans Chemical class 0.000 title claims abstract description 48
- 239000011324 bead Substances 0.000 title claims abstract description 44
- 239000002360 explosive Substances 0.000 title claims abstract description 34
- 238000002360 preparation method Methods 0.000 title claims abstract description 24
- 235000006226 Areca catechu Nutrition 0.000 claims abstract description 73
- 244000080767 Areca catechu Species 0.000 claims abstract description 73
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 69
- 235000013824 polyphenols Nutrition 0.000 claims abstract description 61
- -1 polysaccharide polyphenol Chemical class 0.000 claims abstract description 55
- 239000002775 capsule Substances 0.000 claims abstract description 32
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 28
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims abstract description 14
- 241000416162 Astragalus gummifer Species 0.000 claims abstract description 13
- 229920001353 Dextrin Polymers 0.000 claims abstract description 13
- 239000004375 Dextrin Substances 0.000 claims abstract description 13
- 108010010803 Gelatin Proteins 0.000 claims abstract description 13
- 229920002907 Guar gum Polymers 0.000 claims abstract description 13
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- CBMPTFJVXNIWHP-UHFFFAOYSA-L disodium;hydrogen phosphate;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound [Na+].[Na+].OP([O-])([O-])=O.OC(=O)CC(O)(C(O)=O)CC(O)=O CBMPTFJVXNIWHP-UHFFFAOYSA-L 0.000 claims description 11
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- HXMWJLVXIHYART-UHFFFAOYSA-M sodium;2-hydroxypropane-1,2,3-tricarboxylic acid;hydroxide;hydrochloride Chemical compound [OH-].[Na+].Cl.OC(=O)CC(O)(C(O)=O)CC(O)=O HXMWJLVXIHYART-UHFFFAOYSA-M 0.000 claims description 3
- XPFJYKARVSSRHE-UHFFFAOYSA-K trisodium;2-hydroxypropane-1,2,3-tricarboxylate;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound [Na+].[Na+].[Na+].OC(=O)CC(O)(C(O)=O)CC(O)=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O XPFJYKARVSSRHE-UHFFFAOYSA-K 0.000 claims description 3
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- 238000002156 mixing Methods 0.000 description 5
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- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 4
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- 239000000843 powder Substances 0.000 description 3
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- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
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- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
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- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
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- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a medicinal polysaccharide functional explosive bead composition and a preparation method thereof, belonging to the technical field of antidiabetic medicinal preparations. The explosive bead composition consists of a capsule shell and a content, wherein the content consists of the following components: 0.1-5.0% of betel nut polysaccharide polyphenol, 0.05-0.3% of mint essential oil, 0.05-2.5% of histidine and the balance of glycerol; the capsule shell consists of the following components: 1-5% of tragacanth, 1-2% of gelatin, 1-3% of guar gum, 5-10% of glycerol, 1-5% of dextrin and the balance of water. The medicinal polysaccharide functional explosive bead composition comprises betel nut polysaccharide polyphenol, histidine and other components, and the betel nut polysaccharide polyphenol extraction preparation method is optimized, so that the betel nut alkali content is reduced, and the medication safety is improved.
Description
Technical Field
The invention belongs to the technical field of antidiabetic pharmaceutical preparations, and particularly relates to a medicinal polysaccharide functional explosive bead composition and a preparation method thereof.
Background
The disclosure of this background section is only intended to increase the understanding of the general background of the invention and is not necessarily to be construed as an admission or any form of suggestion that this information forms the prior art already known to those of ordinary skill in the art.
The betel nut polysaccharide polyphenol is light yellow to tan powder, has slightly astringent taste, is a natural compound extracted from betel nut fruits after being cleaned, crushed, extracted, filtered, concentrated and dried, not only maintains partial taste of betel nuts, but also removes most of harmful components such as alkaloid and the like in betel nut fruits, wherein the betel nut polysaccharide polyphenol mainly comprises betel nut polysaccharide and betel nut polyphenol, the betel nut polysaccharide mainly comprises glucose, fructose, arabinose and the like, the polyphenol compounds in the betel nut polysaccharide polyphenol mainly comprise flavonoids, catechins, anthocyanin and the like, and have various biological activities, and the betel nut polysaccharide polyphenol has various pharmacological effects such as antioxidation, anti-inflammatory, antibacterial, antitumor and the like, and is widely studied and applied to the fields of medicines, foods, health products and the like.
Diabetes is a chronic disease, commonly associated with high blood glucose levels, also known as adult-type diabetes, caused by insulin deficiency or resistance of cells to insulin, a hormone produced by the pancreas that helps the body convert glucose in the blood to energy. Diabetics may often develop hyperglycemic conditions that may negatively impact the various systems and organs of the body. Symptoms of type II diabetes are early in the process, and some common symptoms include frequent urination, thirst, fatigue, weight loss, blurred vision, and susceptibility to infection. If not controlled in time, type II diabetes may lead to a range of complications such as cardiovascular disease, neuropathy, kidney disease, eye disease and foot problems.
Chinese patent publication No. CN107375806A discloses a pharmaceutical composition for treating diabetes, which comprises medicines such as betel nuts and the like, is prepared into granules or powder, has the efficacy of balancing blood sugar, and has a certain repairing effect on pancreatic tissue injury. However, since betel nuts contain a large amount of alkaloids, tannins and other chemical substances, the betel nuts can be directly used as a medicine and can be taken for a long time to generate various damages, for example: (1) risk of carcinogenesis: betulin is a carcinogen, and long-term consumption increases the risk of oral cancer. (2) addiction: betel nuts have addiction, and long-term eating can lead to dependence and addiction. (3) digestive system problems: betel nut may adversely affect the digestive system, resulting in symptoms such as stomach discomfort and diarrhea. (4) oral problem: the long-term eating of betel nut may cause oral problems such as dental ulcer and gingivitis.
Song Fei et al report on the inhibition kinetics of the activity of alpha-glucosidase by betel nut polyphenol extract, found that betel nut polyphenol has an inhibition effect on alpha-glucosidase and has a prospect in the development and application of high-efficiency hypoglycemic drugs (Song Fei, chen Kaijian, tang Minmin, etc.. Betel nut polyphenol extract has an inhibition kinetics study on the activity of alpha-glucosidase [ J ]. Tropical crop theory, 2021,42 (05): 1455-1461). But it was found that: (1) The betel nut polyphenol extract is not good in effect of reducing blood sugar when being singly used; (2) Betel nut polyphenol also contains partial betel nut alkali, and has medication risk.
Disclosure of Invention
In order to overcome the defects in the prior art, the invention provides a medicinal polysaccharide functional explosive bead composition with high safety, which can effectively reduce blood sugar level.
Specifically, the technical scheme of the invention is as follows:
the first aim of the invention is to provide a preparation method of betel nut polysaccharide polyphenol, which comprises four steps of betel nut pretreatment, detoxification treatment, extraction and purification, and specifically comprises the following steps:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of buffer solution with pH of 4.0-5.5, standing for 1-2 h, adding beta-glucosidase with the dosage of 0.01 times of betel nut, performing crude extraction, and performing enzymolysis at 70-85 ℃ for 1-2 h;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting in a water bath at 45-55 ℃ for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Purifying: washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
In various embodiments, the enzymolysis temperature in the step (2) is 80 ℃, the buffer solution in the step (2) is selected from one of disodium hydrogen phosphate-citric acid buffer solution, citric acid-sodium citrate buffer solution and citric acid-sodium hydroxide-hydrochloric acid buffer solution, and the water bath temperature in the step (3) is 50 ℃.
The second object of the invention is to provide a medicinal polysaccharide functional explosive bead composition, which consists of a capsule shell and contents, wherein the contents consist of the following components: 0.1-5.0% of betel nut polysaccharide polyphenol, 0.05-0.3% of mint essential oil, 0.05-2.5% of histidine and the balance of glycerol; the capsule shell consists of the following components: 1-5% of tragacanth, 1-2% of gelatin, 1-3% of guar gum, 5-10% of glycerol, 1-5% of dextrin and the balance of water.
In a preferred embodiment, the contents consist of the following components: 2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of histidine and the balance of glycerin; the capsule shell consists of the following components: 2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Wherein the percentage ratio of betel polysaccharide polyphenol to histidine is 2:1.
A third object of the present invention is to provide the use of the above-mentioned pharmaceutical polysaccharide functional explosive bead composition for the preparation of a medicament for treating diabetes, which is type 2 diabetes.
Compared with the prior art, the invention has the technical effects that:
the invention optimizes the extraction and preparation method of betel polysaccharide polyphenol, reduces betel alkali content and improves medication safety. The betel nut polysaccharide polyphenol is prepared into the explosive beads, so that the betel nut polysaccharide polyphenol is convenient to take orally, and the betel nut polysaccharide polyphenol is applied to the aspect of treating diabetes.
Drawings
FIG. 1 shows the betulin content of the pharmaceutical polysaccharide functional explosive composition according to the various embodiments.
Figure 2 is a graph showing fasting blood glucose levels before and after dosing of each group of rats.
Detailed Description
The present invention will be further described with reference to examples for the purpose of making the objects and technical aspects of the present invention more apparent, but the scope of the present invention is not limited to these examples, which are only for explaining the present invention. It will be understood by those skilled in the art that variations or equivalent substitutions that do not depart from the spirit of the invention are intended to be included within the scope of the invention.
EXAMPLE 1 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of disodium hydrogen phosphate-citric acid buffer solution with pH of 4.8, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of that of betel nut, performing enzymolysis for 1-2 h at 80 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 50 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of histidine and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
EXAMPLE 2 pharmaceutical polysaccharide functional burst compositions
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of citric acid-sodium citrate buffer solution with pH of 4.0, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of the betel nut, performing crude extraction, and performing enzymolysis at 70 ℃ for 1-2 h;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting in a water bath at 40 ℃ for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
0.1% of betel nut polysaccharide polyphenol, 0.05% of mint essential oil, 0.05% of histidine and the balance of glycerin;
capsule shell composition:
1.0% of tragacanth, 1.0% of gelatin, 1.0% of guar gum, 5.0% of glycerol, 1.0% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
EXAMPLE 3 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of citric acid-sodium hydroxide-hydrochloric acid buffer solution with pH of 5.5, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of the betel nut, performing enzymolysis for 1-2 h at 85 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 55 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
5.0% of betel nut polysaccharide polyphenol, 0.3% of mint essential oil, 2.5% of histidine and the balance of glycerol;
capsule shell composition:
5.0% of tragacanth, 2.0% of gelatin, 3.0% of guar gum, 10.0% of glycerol, 5.0% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Comparative example 1 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of disodium hydrogen phosphate-citric acid buffer solution with pH of 4.8, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of that of betel nut, performing enzymolysis for 1-2 h at 80 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 50 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of peppermint essential oil and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Comparative example 2 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of disodium hydrogen phosphate-citric acid buffer solution with pH of 4.8, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of that of betel nut, performing enzymolysis for 1-2 h at 80 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 50 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of lysine and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Comparative example 3 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of disodium hydrogen phosphate-citric acid buffer solution with pH of 4.8, standing for 1-2 h, adding beta-glucosidase with weight of 0.01 times of that of betel nut, performing enzymolysis for 1-2 h at 80 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 50 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 4.0% of histidine and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Comparative example 4 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of disodium hydrogen phosphate-citric acid buffer solution with pH of 4.8, standing for 1-2 h, adding cellulase with weight of 0.01 times of that of betel nut, and performing enzymolysis at 80 ℃ for 1-2 h;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting at the temperature of 50 ℃ in water bath, repeating for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of histidine and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Comparative example 5 pharmaceutical polysaccharide functional burst bead composition
Extracting betel nut polysaccharide polyphenol:
(1) Squeezing and extracting: sorting, cleaning and crushing fresh betel nuts, squeezing by a physical method to obtain juice, and processing the juice to obtain clear juice; mixing the residues of Arecae semen, and standing.
(2) Removing tannins: adding edible ethanol into the clarified juice, mixing until the final concentration of the ethanol is 45% -85%, standing overnight, and taking the supernatant to obtain a juice solution.
(3) Removing part of alkaloids: concentrating the juice solution at low temperature under reduced pressure to remove ethanol, passing the concentrated juice solution through a solid phase column, and collecting all the liquid to obtain juice extract. The solid phase column is filled with betulin molecule branding polymer as stationary phase.
(5) Extracting residues: adding 3-10 times of water and cellulase into the betel nut residue for biological pyrolysis, mixing, adjusting the pH value to 3-6 by citric acid, ultrasonically extracting for 1-6 hours, and centrifuging at 6000-12000 rpm to obtain residue extract, wherein the final concentration of the cellulase is 0.01% -0.8%.
(6) Mixing the juice extract and the residue extract, concentrating under reduced pressure at low temperature, dehydrating to obtain solid, pulverizing with 30-120 mesh sieve, and inspecting to obtain Arecae semen polysaccharide polyphenol.
Preparation of a medicinal polysaccharide functional explosive bead composition:
the composition of the content is as follows:
2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of histidine and the balance of glycerin;
capsule shell composition:
2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
Preparing the capsule shell and the sol of the content according to the prescription, dripping, and wrapping the content in the capsule shell to obtain the medicinal polysaccharide functional explosive bead composition.
Betulin content determination
Betulin is a main addictive substance of betel nut, has the function of stimulating central nervous system and respiratory system, and can cause various health hazards for long-term and excessive use. Betulin content is determined according to high performance liquid chromatography (general rule 0512) of Chinese pharmacopoeia 2020 edition, chromatographic conditions and system applicability test: strong cation exchange bonded silica gel is used as a filler (SCX-strong cation exchange resin column); acetonitrile-phosphoric acid solution (2-1000, concentrated ammonia solution to adjust pH value to 3.8) (55:45) is used as mobile phase; the detection wavelength was 215nm. The number of theoretical plates should be not less than 3000 calculated according to arecoline peak. Preparation of a control solution: taking a proper amount of arecoline hydrobromide reference substance, precisely weighing, adding mobile phase to prepare a solution containing 0.1mg per 1ml, and obtaining (arecoline weight=arecoline hydrobromide weight/1.5214). Preparation of test solution: taking about 0.3g of the powder (sieving with a fifth sieve), precisely weighing, placing into a conical flask with a plug, adding 50ml of diethyl ether, adding carbonate buffer solution (1.91 g of sodium carbonate and 0.56g of sodium bicarbonate, adding water to dissolve into 100ml, and standing for 30 min, and shaking constantly; heating and refluxing for 30 minutes, separating diethyl ether solution, and adding the diethyl ether solution into an evaporation dish containing 1ml of phosphoric acid solution (5-1000); extracting the residue with diethyl ether under reflux for 2 times (30 ml, 20 ml) each for 15 min, mixing diethyl ether solutions, placing in the same evaporating dish, volatilizing diethyl ether, dissolving the residue with 50% acetonitrile solution, transferring to 25ml measuring flask, and adding 50% acetonitrile to scale; shaking, filtering, and collecting filtrate. Assay: respectively precisely sucking 10 μl of the reference solution and the sample solution, and injecting into a liquid chromatograph for measurement.
As shown in fig. 1, the existing extraction method of betel polysaccharide polyphenol is used in comparative example 5, wherein the removal degree of betel alkali harmful to human body is poor, the betel alkali component content in the prepared betel polysaccharide polyphenol is high, and the conventional enzymolysis enzyme is used in comparative example 4, but the betel alkali removal effect is poor, and the betel alkali content in the betel polysaccharide polyphenol prepared in examples 1-3 of the invention is low, so that toxic substances are removed to the maximum extent, and the medication safety is ensured.
Optimization of betel nut polysaccharide polyphenol preparation method by single factor test
The preparation method of betel nut polysaccharide polyphenol is optimized, the selection of buffer solution in detoxification treatment, the pH of the buffer solution, the dosage of beta-glucosidase, the enzymolysis temperature and the like are optimized, and various test conditions are tried, and the following typical single-factor tests and results are listed.
The single factor variables are as follows, and the other conditions are the same as those for the preparation of betel polysaccharide polyphenol in example 1.
A: the addition amount of beta-glucosidase is 0.005 times of that of betel nut
B: the addition amount of beta-glucosidase is 0.02 times of betel nut
C: the addition amount of beta-glucosidase is 0.04 times of betel nut
D: the buffer solution is disodium hydrogen phosphate-citric acid buffer solution with pH=4.0
E: the buffer solution is disodium hydrogen phosphate-citric acid buffer solution with pH=5.5
F: the buffer solution is acetic acid-sodium acetate buffer solution with pH=5.0
G: the buffer solution is disodium hydrogen phosphate-citric acid buffer solution with pH=3.0
H: the buffer solution is disodium hydrogen phosphate-citric acid buffer solution with pH=6.5
I: the enzymolysis temperature is 65 DEG C
J: the enzymolysis temperature is 90 DEG C
Table 1 determination of betulin content in betel polysaccharide polyphenols
| Betulin content (%) | |
| A | 0.13 |
| B | 0.16 |
| C | 0.18 |
| D | 0.07 |
| E | 0.05 |
| F | 0.15 |
| G | 0.12 |
| H | 0.17 |
| I | 0.19 |
| J | 0.14 |
Table 1 shows that the addition of beta-glucosidase, the selection of buffer solution and the selection of pH of buffer solution have a critical influence on the extraction effect, and the betulin content in betel nut polysaccharide polyphenol is affected to a certain extent.
Polysaccharide functional bursting bead composition for treating type 2 diabetes
Alpha-glucosidase activity inhibition rate assay
The inhibition rate of the polysaccharide functional bursting bead composition of each embodiment with the same betel nut polysaccharide polyphenol concentration on the activity of alpha-glucosidase is respectively measured by adopting a method in a literature cited in the background technology.
TABLE 2 inhibition of alpha-glucosidase Activity
| Inhibition of alpha-glucosidase activity (%) | |
| Example 1 | 96.44 |
| Example 2 | 92.95 |
| Example 3 | 95.10 |
| Comparative example 1 | 83.37 |
| Comparative example 2 | 80.40 |
| Comparative example 3 | 86.21 |
| Comparative example 4 | 90.52 |
| Comparative example 5 | 88.47 |
Table 2 shows that the polysaccharide functional explosive bead composition phenol in the embodiments 1-3 has better inhibition effect on alpha-glucosidase, and can delay the generation and absorption of glucose, thereby delaying postprandial hyperglycemia of diabetics and obviously reducing blood sugar fluctuation.
Experimental animals: SD rats, SPF grade, weight 180-220 g, male and female halves, were adapted to 1 week under standard conditions prior to the experiment.
Establishment of hyperglycemic rat model
Rats were fasted for 24 hours, were given a dose of 120mg/kg of tetraoxypyrimidine by intraperitoneal injection, and after 24 hours, were given 100mg/kg of tetraoxypyrimidine by intraperitoneal injection again, and 2.5 hours and 5 hours after injection of tetraoxypyrimidine were given a dose of 25% glucose 1ml/100g, and 72 hours after the last administration, and fasting blood glucose was examined, and a dose of higher than 11.1mmol/L was considered successful molding.
Grouping and administration of laboratory animals
Rats successfully molded were divided into model group, example 1 group, example 2 group, example 3 group, comparative example 1 group, comparative example 2 group, comparative example 3 group, comparative example 4 group, comparative example 5 group, 10 rats each, and gastric lavage of the corresponding drug. The model group was given equal amount of distilled water, and 10 normal rats selected from the blank group were not subjected to molding treatment, and only equal amount of distilled water was given. The administration was 1 time daily for 7 consecutive days.
Statistical treatment
Statistical analysis of the obtained data using SPSS22.0 software for metering the dataThe comparison between the groups adopts single-factor analysis of variance, and the analysis between the two groups adopts independent sample T test mode. To be used forP<A difference of 0.05 is statistically significant.
Rat blood glucose assay
Blood was taken from the tail vein of each rat 6 hours after the last administration, and fasting blood glucose was measured. FIG. 2 shows fasting blood glucose levels before and after administration of rats in each group, and there was no significant difference in blood glucose between rats in each of model group, example 1 group, example 2 group, example 3 group, comparative example 1 group, comparative example 2 group, comparative example 3 group, comparative example 4 group, and comparative example 5 group before administration, and rats in each of example 1 group, example 2 group, and example 3 group after administration were compared with blood glucose levels of rats in the model group,P<0.01, with significant differences. The polysaccharide functional bursting bead composition of the embodiments 1-3 can reduce the blood sugar level of rats.
Claims (10)
1. The medicinal polysaccharide functional explosive bead composition is characterized by comprising a capsule shell and contents, wherein the contents comprise the following components: 0.1-5.0% of betel nut polysaccharide polyphenol, 0.05-0.3% of mint essential oil, 0.05-2.5% of histidine and the balance of glycerol; the capsule shell consists of the following components: 1-5% of tragacanth, 1-2% of gelatin, 1-3% of guar gum, 5-10% of glycerol, 1-5% of dextrin and the balance of water;
the preparation method of the betel nut polysaccharide polyphenol comprises the following steps:
(1) Pretreatment of betel nuts: cleaning Arecae semen, crushing, squeezing, and filtering to obtain Arecae semen juice;
(2) Detoxification treatment: adding 2-5 times of buffer solution with the pH of 4.0-5.5, standing for 1-2 hours, adding beta-glucosidase, performing crude extraction, and performing enzymolysis for 1-2 hours at 70-85 ℃;
(3) Extracting: adding 2-3 times of 75% ethanol in volume into the solution subjected to the detoxification treatment in the step (2), carrying out ultrasonic treatment, extracting in a water bath at 45-55 ℃ for 2 times, carrying out suction filtration, merging filtrate, and carrying out reduced pressure distillation to remove ethanol solvent to obtain a concentrated product;
(4) Washing and freeze-drying the concentrated product of the step (3) to obtain betel nut polysaccharide polyphenol.
2. The pharmaceutical polysaccharide functional explosive bead composition of claim 1, wherein the contents consist of: 2.0% of betel nut polysaccharide polyphenol, 0.15% of mint essential oil, 1.0% of histidine and the balance of glycerin.
3. The pharmaceutical polysaccharide functional burst bead composition of claim 1, wherein the capsule shell consists of: 2.0% of tragacanth, 1.5% of gelatin, 1.5% of guar gum, 7.5% of glycerol, 3.5% of dextrin and the balance of water.
4. The pharmaceutical polysaccharide functional explosive bead composition according to claim 1, wherein the percentage ratio of betel polysaccharide polyphenol to histidine is 2:1.
5. The pharmaceutical polysaccharide functional burst composition of claim 1, wherein the enzymatic hydrolysis temperature in step (2) is 80 ℃.
6. The pharmaceutical polysaccharide functional explosive bead composition according to claim 1, wherein the buffer solution in step (2) is selected from one of disodium hydrogen phosphate-citric acid buffer solution, citric acid-sodium citrate buffer solution, and citric acid-sodium hydroxide-hydrochloric acid buffer solution.
7. The pharmaceutical polysaccharide functional explosive bead composition according to claim 1, wherein the beta-glucosidase added in the step (2) is 0.01 times of the weight of betel nuts.
8. The pharmaceutical polysaccharide functional burst composition of claim 1, wherein the water bath temperature in step (3) is 50 ℃.
9. Use of the pharmaceutical polysaccharide functional explosive bead composition of claim 1 in the preparation of a medicament for treating diabetes.
10. The use according to claim 9, wherein the diabetes is type 2 diabetes.
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| 宋菲;陈开健;唐敏敏;陈华;李永东: "槟榔多酚提取物对α-葡萄糖苷酶活性的抑制动力学研究", 热带作物学报, no. 005, 31 December 2021 (2021-12-31), pages 1455 - 1461 * |
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