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WO2020172840A1 - Drug based on agriophyllum squarrosum alcohol extract - Google Patents

Drug based on agriophyllum squarrosum alcohol extract Download PDF

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Publication number
WO2020172840A1
WO2020172840A1 PCT/CN2019/076435 CN2019076435W WO2020172840A1 WO 2020172840 A1 WO2020172840 A1 WO 2020172840A1 CN 2019076435 W CN2019076435 W CN 2019076435W WO 2020172840 A1 WO2020172840 A1 WO 2020172840A1
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parts
alcohol extract
gardenia
extract
filtrate
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Chinese (zh)
Inventor
马小飞
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Ma Shirui Biotechnology Jiangsu Co Ltd
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Ma Shirui Biotechnology Jiangsu Co Ltd
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Priority to PCT/CN2019/076435 priority Critical patent/WO2020172840A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/488Pueraria (kudzu)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/537Salvia (sage)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/72Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/74Rubiaceae (Madder family)
    • A61K36/744Gardenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics

Definitions

  • the invention relates to the technical field of biomedicine, in particular to a medicine based on an alcohol extract of saponin.
  • the purpose of the present invention is to provide a medicine based on an alcohol extract of saponin, which solves one or more of the above-mentioned existing technical problems.
  • a medicine based on the alcohol extract of sapin comprising the following components in percentages by mass: 5-10 parts of geniposide, 10-20 parts of saponin alcohol extract, 3-5 parts of kudzu root, 1- 5 parts of Salvia and 8-10 parts of Hovenia dulcis.
  • the following components are included in percentages by mass: 8 parts of geniposide, 15 parts of alcohol extract of sapin, 4 parts of Pueraria lobata, 2 parts of Salvia miltiorrhiza, and 9 parts of Hovenia dulcis.
  • the preparation method of the alcohol extract of saponin includes the following steps:
  • A1 Crush the saponine through a 60-mesh sieve, mix the material-liquid ratio with the alcohol solution in a certain proportion, heat and reflux for 2 times, 2 hours each time, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and vacuum dry to obtain saponol Extract.
  • the alcohol solution is one or more of absolute ethanol, methanol, or glycerol.
  • the alcohol solution is absolute ethanol.
  • the ratio of material to liquid is 1:5-1:10.
  • the extraction method of geniposide further includes the following steps:
  • the pretreatment method includes the following steps:
  • Shelling Put the classified gardenia seeds into the shelling machine for shelling;
  • Drying Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;
  • C4. Crushing Use a crusher to crush the gardenia seeds, and pass through a 20-60 mesh sieve to obtain the gardenia powder.
  • Each component of the medicine of the embodiment of the application can be obtained by pure natural purification, and can effectively reduce total cholesterol.
  • a medicine ⁇ based on the alcohol extract of sapin comprising the following components in percentage by mass: 5 parts of geniposide, 10 parts of the alcohol extract of sapin, 3 parts of Pueraria lobata, 1 part of Salvia miltiorrhiza and 8 parts Hovenia dulcis.
  • the preparation method of the alcohol extract of Sapin includes the following steps:
  • the extraction method of geniposide includes the following steps:
  • Shelling Put the classified gardenia seeds into the shelling machine for shelling;
  • Drying Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;
  • Crushing use a crusher to crush the gardenia seeds and pass a 20-mesh sieve to obtain the gardenia powder.
  • a drug ⁇ based on the alcohol extract of sapin comprising the following components in percentages by mass: 10 parts of geniposide, 20 parts of the alcohol extract of sapin, 5 parts of Pueraria lobata root, 5 parts of Salvia miltiorrhiza and 10 parts Hovenia dulcis.
  • the preparation method of the alcohol extract of Sapin includes the following steps:
  • the extraction method of geniposide includes the following steps:
  • Shelling Put the classified gardenia seeds into the shelling machine for shelling;
  • Drying Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;
  • Crushing use a crusher to crush the gardenia seeds, and pass through a 60-mesh sieve to obtain the gardenia powder.
  • a medicine ⁇ based on the alcohol extract of sapin comprising the following components in percentages by mass: 8 parts of geniposide, 15 parts of saponin alcohol extract, 4 parts of Pueraria lobata root, 2 parts of Danshen and 9 parts Hovenia dulcis.
  • the preparation method of the alcohol extract of Sapin includes the following steps:
  • the extraction method of geniposide includes the following steps:
  • Shelling Put the classified gardenia seeds into the shelling machine for shelling;
  • Drying Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;
  • Crushing Use a crusher to crush the gardenia seeds and pass a 40-mesh sieve to obtain the gardenia powder.
  • Wistar rats were randomly divided into cages for 5 days to adapt to the environment and fed with basic feed. Randomly divided into 5 groups according to body weight: normal group, high fat group, ⁇ group, ⁇ group and ⁇ group.
  • Animals in each group are kept in separate cages.
  • the animal room is well ventilated and light.
  • the light and dark cycle is 12h
  • the room temperature is 22°C
  • the relative humidity is 40-50%. Clean drinking water and feeding are given once a day.
  • the weight of the rats was measured and recorded every day, and the gavage was calculated according to the weight in the afternoon.
  • the ⁇ group, the ⁇ group and the ⁇ group were given the above-mentioned drugs for 15 days.
  • the normal group was fed with basic feed, and the remaining 4 groups were fed with high-fat feed.
  • High fat feed formula sodium cholate 0.5%, cholesterol 3%, lard 10%, basic feed 86.5%.
  • Cholesterol and sodium cholate are evenly mixed, the lard is evenly rubbed in the above-mentioned evenly mixed feed powder, and then water is fully kneaded and pressed into a fixed shape, dried, and set aside.
  • Serum total cholesterol content is measured by COD-PAP colorimetric method
  • serum triglyceride content is measured by GPO-PAP colorimetric method
  • serum low-density lipoprotein cholesterol content is measured by polyvinyl sulfate precipitation method
  • serum high-density lipoprotein cholesterol material is phosphotungsten Determination by acid-magnesium precipitation method.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • Mycology (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

A drug based on an Agriophyllum squarrosum alcohol extract, comprising the following components: 5-10 parts of geniposide, 10-20 parts of an Agriophyllum squarrosum alcohol extract, 3-5 parts of Radix Puerariae, 1-5 parts of Salvia miltiorrhiza, and 8-10 parts of Hovenia dulcis Thunb. The drug can effectively lower cholesterol levels.

Description

一种基于沙蓬醇提物的药物A medicine based on alcohol extract of sapin 技术领域Technical field

本发明涉及生物药物的技术领域,特别涉及一种基于沙蓬醇提物的药物。The invention relates to the technical field of biomedicine, in particular to a medicine based on an alcohol extract of saponin.

背景技术Background technique

现有技术中,没有一种能有效的降胆固醇中药,因此,需要开发一种无毒副作用的能有效的降低胆固醇的中药。In the prior art, there is no traditional Chinese medicine that can effectively lower cholesterol. Therefore, there is a need to develop a traditional Chinese medicine that can effectively lower cholesterol without toxic side effects.

发明内容Summary of the invention

本发明的目的是提供一种基于沙蓬醇提物的药物,解决上述现有技术问题中的一个或者多个。The purpose of the present invention is to provide a medicine based on an alcohol extract of saponin, which solves one or more of the above-mentioned existing technical problems.

一种基于沙蓬醇提物的药物,按质量百份数包括以下组分:5-10份的栀子苷、10-20份的沙蓬醇提物、3-5份的葛根、1-5份的丹参以及8-10份的枳椇子。A medicine based on the alcohol extract of sapin, comprising the following components in percentages by mass: 5-10 parts of geniposide, 10-20 parts of saponin alcohol extract, 3-5 parts of kudzu root, 1- 5 parts of Salvia and 8-10 parts of Hovenia dulcis.

在一些实施方式中,按质量百份数包括以下组分:8份的栀子苷、15份的沙蓬醇提物、4份的葛根、2份的丹参以及9份的枳椇子。In some embodiments, the following components are included in percentages by mass: 8 parts of geniposide, 15 parts of alcohol extract of sapin, 4 parts of Pueraria lobata, 2 parts of Salvia miltiorrhiza, and 9 parts of Hovenia dulcis.

在一些实施方式中,沙蓬醇提物的制备方法包括以下步骤:In some embodiments, the preparation method of the alcohol extract of saponin includes the following steps:

A1、粉碎沙蓬过60目筛,料液比按一定的比例加醇溶液混合,加热回流2次,每次2小时,合并滤液,真空抽滤,滤液减压浓缩,真空干燥得到沙蓬醇提取物。A1. Crush the saponine through a 60-mesh sieve, mix the material-liquid ratio with the alcohol solution in a certain proportion, heat and reflux for 2 times, 2 hours each time, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and vacuum dry to obtain saponol Extract.

在一些实施方式中,醇溶液为无水乙醇、甲醇或者丙三醇中的一种或多种。In some embodiments, the alcohol solution is one or more of absolute ethanol, methanol, or glycerol.

在一些实施方式中,醇溶液为无水乙醇。In some embodiments, the alcohol solution is absolute ethanol.

在一些实施方式中,料液比为1:5-1:10。In some embodiments, the ratio of material to liquid is 1:5-1:10.

在一些实施方式中,栀子苷的提取方法还包括以下步骤:In some embodiments, the extraction method of geniposide further includes the following steps:

B1、称取经过预处理的栀子粉末,加入乙醚溶液回流1-2h,其中栀子粉末与乙醚溶液的固液比为1:5-1:30,抽滤,收取滤液;B1. Weigh the pretreated gardenia powder, add ether solution and reflux for 1-2h, wherein the solid-liquid ratio of gardenia powder to ether solution is 1:5-1:30, filter with suction, and collect the filtrate;

B2、往滤渣中加入含量为5-10%的乙醚再回流,抽滤,收取滤液,合并滤液,蒸馏去除乙醚,然后加入含量为20-30%的乙醇,过滤,减压蒸馏,然后用水溶解,抽滤,得到栀子粉粗提取液;B2. Add 5-10% diethyl ether to the filter residue and reflux, filter with suction, collect the filtrate, combine the filtrate, distill off diethyl ether, then add 20-30% ethanol, filter, distill under reduced pressure, and then dissolve in water , Suction filtration to obtain a crude extract of gardenia powder;

B3、将栀子粉粗提取液用大孔吸附树脂柱进行吸附分离,其中母液与大孔吸附树脂体积比为1:10-1:20,使用质量分数为5-20的乙醇水溶液进行洗脱,洗脱剂量为2-3倍的柱体积,得到洗脱液,将洗脱液进行真空干燥,得到所述的栀子苷。B3. Adsorb and separate the crude gardenia powder extract with a macroporous adsorption resin column, in which the volume ratio of mother liquor to macroporous adsorption resin is 1:10-1:20, and the mass fraction of ethanol is 5-20 for elution. The elution dose is 2-3 times the column volume to obtain the eluate, and the eluate is vacuum dried to obtain the gardenoside.

在一些实施方式中,预处理方法包括以下步骤:In some embodiments, the pretreatment method includes the following steps:

C1、筛分:通过滚筒分级筛对栀子籽的大小进行分级;C1. Screening: Classify the size of gardenia seeds through a drum grading screen;

C2、脱壳:将经过分级处理的栀子籽,加入脱壳机进行脱壳;C2. Shelling: Put the classified gardenia seeds into the shelling machine for shelling;

C3、烘干:使用微波烘干设备将栀子进行烘干,使得栀子籽中的水分汽化蒸发;C3. Drying: Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;

C4、粉碎:使用粉碎机将栀子籽粉碎,过20-60目筛,得到所述栀子粉末。C4. Crushing: Use a crusher to crush the gardenia seeds, and pass through a 20-60 mesh sieve to obtain the gardenia powder.

有益效果:Benefits:

本申请实施例的药物的各组分可通过纯天然提纯得到,且能有效的降低总胆固醇。Each component of the medicine of the embodiment of the application can be obtained by pure natural purification, and can effectively reduce total cholesterol.

具体实施方式detailed description

下面的实施案例,对本发明进行进一步详细的说明。The following implementation cases illustrate the present invention in further detail.

实施案例1:Implementation case 1:

一种基于沙蓬醇提物的药物α,按质量百份数包括以下组分:5份的栀子苷、10份的沙蓬醇提物、3份的葛根、1份的丹参以及8份的枳椇子。A medicine α based on the alcohol extract of sapin, comprising the following components in percentage by mass: 5 parts of geniposide, 10 parts of the alcohol extract of sapin, 3 parts of Pueraria lobata, 1 part of Salvia miltiorrhiza and 8 parts Hovenia dulcis.

其中,沙蓬醇提物的制备方法包括以下步骤:Wherein, the preparation method of the alcohol extract of Sapin includes the following steps:

α1、粉碎沙蓬过60目筛,料液比按1:5的比例加无水乙醇混合,加热回流2次,每次2小时,合并滤液,真空抽滤,滤液减压浓缩,真空干燥得到沙蓬醇提取物。α1. Crush the sapphire through a 60-mesh sieve, mix the material-liquid ratio with anhydrous ethanol at a ratio of 1:5, heat and reflux twice for 2 hours each time, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and dry under vacuum. Saponin alcohol extract.

栀子苷的提取方法包括以下步骤:The extraction method of geniposide includes the following steps:

α2、筛分:通过滚筒分级筛对栀子籽的大小进行分级;α2, sieving: the size of gardenia seeds is classified through a drum grading screen;

α3、脱壳:将经过分级处理的栀子籽,加入脱壳机进行脱壳;α3. Shelling: Put the classified gardenia seeds into the shelling machine for shelling;

α4、烘干:使用微波烘干设备将栀子进行烘干,使得栀子籽中的水分汽化蒸发;α4. Drying: Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;

α5、粉碎:使用粉碎机将栀子籽粉碎,过20目筛,得到所述栀子粉末。α5. Crushing: use a crusher to crush the gardenia seeds and pass a 20-mesh sieve to obtain the gardenia powder.

α6、称取经过预处理的栀子粉末,加入乙醚溶液回流1h,其中栀子粉末与乙醚溶液的固液比为1:5,抽滤,收取滤液;α6. Weigh the pretreated gardenia powder, add the ether solution and reflux for 1 hour, where the solid-liquid ratio of the gardenia powder to the ether solution is 1:5, suction filter, and collect the filtrate;

α7、往滤渣中加入含量为5%的乙醚再回流,抽滤,收取滤液,合并滤液,蒸馏去除乙醚,然后加入含量为20%的乙醇,过滤,减压蒸馏,然后用水溶解,抽滤,得到栀子粉粗提取液;α7. Add 5% ether to the filter residue and reflux, filter with suction, collect the filtrate, combine the filtrate, distill to remove the ether, then add 20% ethanol, filter, distill under reduced pressure, and then dissolve with water and filter with suction. To obtain a crude extract of gardenia powder;

α8、将栀子粉粗提取液用大孔吸附树脂柱进行吸附分离,其中母液与大孔吸附树脂体积比为1:10,使用质量分数为5的乙醇水溶液进行洗脱,洗脱剂量为2倍的柱体积,得到洗脱液,将洗脱液进行真空干燥,得到所述的栀子苷。α8. Adsorb and separate the crude gardenia powder extract with a macroporous adsorption resin column, where the volume ratio of mother liquor to macroporous adsorption resin is 1:10, and elution is carried out with an ethanol aqueous solution with a mass fraction of 5, and the elution dose is 2 Times the column volume to obtain the eluent, which is vacuum dried to obtain the gardenoside.

实施案例2:Implementation case 2:

一种基于沙蓬醇提物的药物β,按质量百份数包括以下组分:10份的栀子苷、20份的沙蓬醇提物、5份的葛根、5份的丹参以及10份的枳椇子。A drug β based on the alcohol extract of sapin, comprising the following components in percentages by mass: 10 parts of geniposide, 20 parts of the alcohol extract of sapin, 5 parts of Pueraria lobata root, 5 parts of Salvia miltiorrhiza and 10 parts Hovenia dulcis.

其中,沙蓬醇提物的制备方法包括以下步骤:Wherein, the preparation method of the alcohol extract of Sapin includes the following steps:

β1、粉碎沙蓬过60目筛,料液比按1:10的比例加甲醇混合,加热回流2次,每次2小时,合并滤液,真空抽滤,滤液减压浓缩,真空干燥得到沙蓬醇提取物。β1. Crush the sapphire through a 60-mesh sieve, mix with methanol at a ratio of 1:10 to the material-liquid ratio, heat and reflux twice for 2 hours each, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and vacuum dry to obtain sapphire Alcohol extract.

栀子苷的提取方法包括以下步骤:The extraction method of geniposide includes the following steps:

β2、筛分:通过滚筒分级筛对栀子籽的大小进行分级;β2, sieving: grading the size of gardenia seeds through a roller grading screen;

β3、脱壳:将经过分级处理的栀子籽,加入脱壳机进行脱壳;β3. Shelling: Put the classified gardenia seeds into the shelling machine for shelling;

β4、烘干:使用微波烘干设备将栀子进行烘干,使得栀子籽中的水分汽化蒸发;β4. Drying: Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;

β5、粉碎:使用粉碎机将栀子籽粉碎,过60目筛,得到所述栀子粉末。β5. Crushing: use a crusher to crush the gardenia seeds, and pass through a 60-mesh sieve to obtain the gardenia powder.

β6、称取经过预处理的栀子粉末,加入乙醚溶液回流2h,其中栀子粉末与乙醚溶液的固液比为1:30,抽滤,收取滤液;β6. Weigh the pretreated gardenia powder, add ether solution and reflux for 2h, in which the solid-liquid ratio of gardenia powder to ether solution is 1:30, suction filter, and collect the filtrate;

β7、往滤渣中加入含量为10%的乙醚再回流,抽滤,收取滤液,合并滤液,蒸馏去除乙醚,然后加入含量为30%的乙醇,过滤,减压蒸馏,然后用水溶解,抽滤,得到栀子粉粗提取液;β7. Add 10% ether to the filter residue and reflux, filter with suction, collect the filtrate, combine the filtrate, distill to remove the ether, then add 30% ethanol, filter, distill under reduced pressure, and then dissolve in water and filter with suction. To obtain a crude extract of gardenia powder;

β8、将栀子粉粗提取液用大孔吸附树脂柱进行吸附分离,其中母液与大孔吸附树脂体积比为1:20,使用质量分数为20的乙醇水溶液进行洗脱,洗脱剂量为3倍的柱体积,得到洗脱液,将洗脱液进行真空干燥,得到所述的栀子苷。β8. Adsorb and separate the crude gardenia powder extract with a macroporous adsorption resin column, where the volume ratio of mother liquor to macroporous adsorption resin is 1:20, and eluted with an ethanol aqueous solution with a mass fraction of 20, and the elution dose is 3 Times the column volume to obtain the eluent, which is vacuum dried to obtain the gardenoside.

实施案例3:Implementation case 3:

一种基于沙蓬醇提物的药物γ,按质量百份数包括以下组分:8份的栀子苷、15份的沙蓬醇提物、4份的葛根、2份的丹参以及9份的枳椇子。A medicine γ based on the alcohol extract of sapin, comprising the following components in percentages by mass: 8 parts of geniposide, 15 parts of saponin alcohol extract, 4 parts of Pueraria lobata root, 2 parts of Danshen and 9 parts Hovenia dulcis.

其中,沙蓬醇提物的制备方法包括以下步骤:Wherein, the preparation method of the alcohol extract of Sapin includes the following steps:

γ1、粉碎沙蓬过60目筛,料液比按1:8的比例加丙三醇溶液混合,加热回流2次,每次2小时,合并滤液,真空抽滤,滤液减压浓缩,真空干燥得到沙蓬醇提取物。γ1. Crush the sarcophagus through a 60-mesh sieve, add the glycerin solution to the ratio of 1:8, heat and reflux for 2 times, 2 hours each time, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and dry under vacuum An alcohol extract of saponin was obtained.

栀子苷的提取方法包括以下步骤:The extraction method of geniposide includes the following steps:

γ2、筛分:通过滚筒分级筛对栀子籽的大小进行分级;γ2, sieving: grading the size of gardenia seeds through a drum grading screen;

γ3、脱壳:将经过分级处理的栀子籽,加入脱壳机进行脱壳;γ3. Shelling: Put the classified gardenia seeds into the shelling machine for shelling;

γ4、烘干:使用微波烘干设备将栀子进行烘干,使得栀子籽中的水分汽化蒸发;γ4. Drying: Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated;

γ5、粉碎:使用粉碎机将栀子籽粉碎,过40目筛,得到所述栀子粉末。γ5. Crushing: Use a crusher to crush the gardenia seeds and pass a 40-mesh sieve to obtain the gardenia powder.

γ6、称取经过预处理的栀子粉末,加入乙醚溶液回流1.5h,其中栀子粉末与乙醚溶液的固液比为1:10,抽滤,收取滤液;γ6. Weigh the pretreated gardenia powder, add ether solution and reflux for 1.5h, in which the solid-liquid ratio of gardenia powder to ether solution is 1:10, suction filter, and collect the filtrate;

γ7、往滤渣中加入含量为8%的乙醚再回流,抽滤,收取滤液,合并滤液,蒸馏去除乙醚,然后加入含量为25%的乙醇,过滤,减压蒸馏,然后用水溶解,抽滤,得到栀子粉粗提取液;γ7. Add 8% ether to the filter residue and reflux, filter with suction, collect the filtrate, combine the filtrate, distill the ether, then add 25% ethanol, filter, distill under reduced pressure, and then dissolve with water and filter with suction. To obtain a crude extract of gardenia powder;

γ8、将栀子粉粗提取液用大孔吸附树脂柱进行吸附分离,其中母液与大孔吸附树脂体积比为1:15,使用质量分数为10的乙醇水溶液进行洗脱,洗脱剂量为2.5倍的柱体积,得到洗脱液,将洗脱液进行真空干燥,得到所述的栀子苷。γ8. Adsorb and separate the crude gardenia powder extract with a macroporous adsorption resin column, where the volume ratio of mother liquor to macroporous adsorption resin is 1:15, and elution is performed with an ethanol aqueous solution with a mass fraction of 10, and the elution dose is 2.5 Times the column volume to obtain the eluent, which is vacuum dried to obtain the gardenoside.

对实施案例中的药物α、β、γ进行测试:Test the drugs α, β, and γ in the implementation case:

将Wistar大鼠随机分笼饲养5天适应环境,喂饲基础饲料。按体重随机分成5组:正常组,高脂组,α组,β组以及γ组。Wistar rats were randomly divided into cages for 5 days to adapt to the environment and fed with basic feed. Randomly divided into 5 groups according to body weight: normal group, high fat group, α group, β group and γ group.

各组动物分笼饲养。动物房通风光照良好,明暗周期12h,室温22℃,相对湿度40-50%,每日给予洁净饮水并投食1次。每日测量并记录大白鼠体重,每天下午按体重换算出灌胃量,α组,β组以及γ组给药上述药品15天。正常组用基础饲料喂养,其余4组用高脂饲料喂养。Animals in each group are kept in separate cages. The animal room is well ventilated and light. The light and dark cycle is 12h, the room temperature is 22℃, and the relative humidity is 40-50%. Clean drinking water and feeding are given once a day. The weight of the rats was measured and recorded every day, and the gavage was calculated according to the weight in the afternoon. The α group, the β group and the γ group were given the above-mentioned drugs for 15 days. The normal group was fed with basic feed, and the remaining 4 groups were fed with high-fat feed.

高脂饲料配方:胆酸钠0.5%,胆固醇3%,猪油10%,基础饲料86.5%。High fat feed formula: sodium cholate 0.5%, cholesterol 3%, lard 10%, basic feed 86.5%.

胆固醇、胆酸钠均匀混合,将猪油均匀搓在上述均匀混合的饲料粉中,再加水充分揉搓后压成固定形状,晒干,备用。Cholesterol and sodium cholate are evenly mixed, the lard is evenly rubbed in the above-mentioned evenly mixed feed powder, and then water is fully kneaded and pressed into a fixed shape, dried, and set aside.

在第15天禁食自由饮水16小时后,从股动脉取血,将血液放置凝血30min后离心15分钟。离心速度为3000r/min。血清总胆固醇含量采用COD-PAP比色法测定,血清甘油三酯含量采用GPO-PAP比色法,血清低密度脂蛋白胆固醇含量采用聚乙烯硫酸沉淀法测定,血清高密度脂蛋白胆 固醇材料磷钨酸-镁沉淀法测定。After fasting and drinking water for 16 hours on the 15th day, blood was taken from the femoral artery, and the blood was left to clot for 30 minutes and centrifuged for 15 minutes. The centrifugal speed is 3000r/min. Serum total cholesterol content is measured by COD-PAP colorimetric method, serum triglyceride content is measured by GPO-PAP colorimetric method, serum low-density lipoprotein cholesterol content is measured by polyvinyl sulfate precipitation method, serum high-density lipoprotein cholesterol material is phosphotungsten Determination by acid-magnesium precipitation method.

测试结果如下:The test results are as follows:

Figure PCTCN2019076435-appb-000001
Figure PCTCN2019076435-appb-000001

从上表可知,实施例的药物α组,β组以及γ组均能有效的降低胆固醇。It can be seen from the above table that the drugs α group, β group and γ group of the examples can effectively lower cholesterol.

以上表述仅为本发明的优选方式,应当指出,对本领域的普通技术人员来说,在不脱离本发明创造构思的前提下,还可以做出若干变形和改进,这些也应视为发明的保护范围之内。The above expressions are only the preferred modes of the present invention. It should be pointed out that for those of ordinary skill in the art, without departing from the inventive concept of the present invention, several modifications and improvements can be made. These should also be regarded as the protection of the invention. Within range.

Claims (8)

一种基于沙蓬醇提物的药物,其特征在于,按质量百份数包括以下组分:5-10份的栀子苷、10-20份的沙蓬醇提物、3-5份的葛根、1-5份的丹参以及8-10份的枳椇子。A medicament based on alcohol extract of sapin, which is characterized in that it comprises the following components in percentage by mass: 5-10 parts of geniposide, 10-20 parts of saponin alcohol extract, 3-5 parts of Pueraria lobata, 1-5 parts of salvia and 8-10 parts of Hovenia dulcis. 根据权利要求1所述的一种基于沙蓬醇提物的药物,其特征在于,按质量百份数包括以下组分:8份的栀子苷、15份的沙蓬醇提物、4份的葛根、2份的丹参以及9份的枳椇子。The medicament based on the alcohol extract of Sapin according to claim 1, characterized in that it comprises the following components in percentage by mass: 8 parts of geniposide, 15 parts of alcohol extract of Sabon, 4 parts Pueraria lobata root, 2 salvia miltiorrhiza and 9 Hovenia dulcis. 根据权利要求1或2所述的一种基于沙蓬醇提物的药物,其特征在于,所述沙蓬醇提物的制备方法包括以下步骤:A medicine based on an alcohol extract of saponin according to claim 1 or 2, wherein the preparation method of the alcohol extract of saponin comprises the following steps: A1、粉碎沙蓬过60目筛,料液比按一定的比例加醇溶液混合,加热回流2次,每次2小时,合并滤液,真空抽滤,滤液减压浓缩,真空干燥得到沙蓬醇提取物。A1. Crush the saponine through a 60-mesh sieve, mix the material-liquid ratio with the alcohol solution in a certain proportion, heat and reflux for 2 times, 2 hours each time, combine the filtrate, vacuum filter, concentrate the filtrate under reduced pressure, and vacuum dry to obtain saponol Extract. 根据权利要3所述的一种基于沙蓬醇提物的药物,其特征在于,所述醇溶液为无水乙醇、甲醇或者丙三醇中的一种或多种。The medicine based on the alcohol extract of saponin according to claim 3, wherein the alcohol solution is one or more of absolute ethanol, methanol or glycerol. 根据权利要4所述的一种基于沙蓬醇提物的药物,其特征在于,所述醇溶液为无水乙醇。The medicine based on the alcohol extract of saponin according to claim 4, wherein the alcohol solution is absolute ethanol. 根据权利要3所述的一种基于沙蓬醇提物的药物,其特征在于,所述料液比为1:5-1:10。The medicine based on the alcohol extract of saponin according to claim 3, characterized in that the ratio of material to liquid is 1:5-1:10. 根据权利要求1或2所述的一种基于沙蓬醇提物的药物,其特征在于,所述栀子苷的提取方法还包括以下步骤:The medicine based on the alcohol extract of sapin according to claim 1 or 2, wherein the method for extracting geniposide further comprises the following steps: B1、称取经过预处理的栀子粉末,加入乙醚溶液回流1-2h,其中栀子粉末与乙醚溶液的固液比为1:5-1:30,抽滤,收取滤液;B1. Weigh the pretreated gardenia powder, add ether solution and reflux for 1-2h, wherein the solid-liquid ratio of gardenia powder to ether solution is 1:5-1:30, filter with suction, and collect the filtrate; B2、往滤渣中加入含量为5-10%的乙醚再回流,抽滤,收取滤液,合并滤液,蒸馏去除乙醚,然后加入含量为20-30%的乙醇,过滤,减压蒸馏,然后用水溶解,抽滤,得到栀子粉粗提取液;B2. Add 5-10% diethyl ether to the filter residue and reflux, filter with suction, collect the filtrate, combine the filtrate, distill off diethyl ether, then add 20-30% ethanol, filter, distill under reduced pressure, and then dissolve in water , Suction filtration to obtain a crude extract of gardenia powder; B3、将栀子粉粗提取液用大孔吸附树脂柱进行吸附分离,其中母液与 大孔吸附树脂体积比为1:10-1:20,使用质量分数为5-20的乙醇水溶液进行洗脱,洗脱剂量为2-3倍的柱体积,得到洗脱液,将洗脱液进行真空干燥,得到所述的栀子苷。B3. Adsorb and separate the crude gardenia powder extract with a macroporous adsorption resin column, in which the volume ratio of mother liquor to macroporous adsorption resin is 1:10-1:20, and the mass fraction of ethanol is 5-20 for elution. The elution dose is 2-3 times the column volume to obtain the eluate, and the eluate is vacuum dried to obtain the gardenoside. 根据权利要7所述的一种基于沙蓬醇提物的药物,其特征在于,所述预处理方法包括以下步骤:A medicine based on the alcohol extract of saponin according to claim 7, wherein the pretreatment method comprises the following steps: C1、筛分:通过滚筒分级筛对栀子籽的大小进行分级;C1. Screening: Classify the size of gardenia seeds through a drum grading screen; C2、脱壳:将经过分级处理的栀子籽,加入脱壳机进行脱壳;C2. Shelling: Put the classified gardenia seeds into the shelling machine for shelling; C3、烘干:使用微波烘干设备将栀子进行烘干,使得栀子籽中的水分汽化蒸发;C3. Drying: Use microwave drying equipment to dry the gardenia, so that the water in the gardenia seeds is vaporized and evaporated; C4、粉碎:使用粉碎机将栀子籽粉碎,过20-60目筛,得到所述栀子粉末。C4. Crushing: Use a crusher to crush the gardenia seeds, and pass through a 20-60 mesh sieve to obtain the gardenia powder.
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