CN112353837B - Flos puerariae extract and its use - Google Patents

Flos puerariae extract and its use Download PDF

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Publication number
CN112353837B
CN112353837B CN202011391358.3A CN202011391358A CN112353837B CN 112353837 B CN112353837 B CN 112353837B CN 202011391358 A CN202011391358 A CN 202011391358A CN 112353837 B CN112353837 B CN 112353837B
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vitamin
extract
composition
flos puerariae
flower extract
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CN112353837A (en
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庄瑞宾
侯龙辉
王建智
陈旭
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Yijia Yuanpin Industrial Xiamen Co ltd
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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)
    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/5939,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals

Abstract

The invention relates to a pueraria flower extract and application thereof. Specifically, the invention provides application of a pueraria flower extract in preparing a composition for promoting oral absorption of vitamin D. The pueraria flower extract can be used for promoting the oral absorption of vitamin D, so that the treatment effect of the vitamin D3 on vitamin D3 deficiency is improved.

Description

Flos puerariae lobatae extract and its use
Technical Field
The invention relates to the field of medicines, in particular to a pueraria flower extract and application thereof.
Background
Vitamin D deficiency is also called nutritional vitamin D deficiency rickets, and the vitamin D deficiency of growing bones causes systemic calcium and phosphorus metabolism disorder, and calcium salt can not be normally deposited in the osteogenesis process, so that the chronic nutritional disease of the whole body is characterized by skeletal deformity. Among them, Vitamin D3(Vitamin D3, CAS: 67-97-0) is an important active ingredient of Vitamin D group.
In the case of vitamin D3 deficiency, it is required to rapidly improve the absorption of vitamin D3 for therapeutic purposes, in the prior art, the absorption of vitamin D3 is often improved by improving the dosage of vitamin D3, however, in the prior art, vitamin D3 is often administered in the form of soft capsules or tablets, and increasing the dosage of vitamin D3 means increasing the number of the soft capsules or tablets taken, which leads to the decrease of patient compliance, especially for infants or children who are not taking medicine, and further increasing the vitamin resistance of the infants or children by increasing the number of the soft capsules or tablets taken or tablets, and furthermore, increasing the dosage of D3 also increases the medicine cost. Although the vitamin D3 can rapidly increase the blood concentration of vitamin D3 by injection administration, the compliance of the patient subjected to injection administration is poorer, the cost of injection administration is higher, and the injection administration is not suitable for long-term administration. In the prior art, medicines for promoting the oral absorption of vitamin D3 are lacked, so that the vitamin D3 is limited to play a role in quickly treating the deficiency of vitamin D3 after oral administration.
Therefore, there is a need in the art to develop a drug that promotes oral absorption of vitamin D3, thereby improving the therapeutic effect of vitamin D3 on vitamin D3 deficiency.
Disclosure of Invention
The invention aims to provide a medicament for promoting the oral absorption of vitamin D3, thereby improving the treatment effect of vitamin D3 on vitamin D3 deficiency.
In a first aspect, the present invention provides the use of a pueraria flower extract for the preparation of a composition for promoting the oral absorption of vitamin D.
Preferably, the composition is a pharmaceutical composition, a food composition or a health care composition.
Preferably, the composition further comprises a pharmaceutically, food or nutraceutical acceptable carrier.
Preferably, the composition is in a solid or liquid form.
Preferably, the composition is in the form of oral preparation or injection preparation.
Preferably, the composition is in the form of emulsion, tablet, capsule, oral liquid, granule, powder or syrup.
Preferably, the composition is an oral liquid.
Preferably, the oral liquid comprises pueraria flower extract, vitamin D and water.
Preferably, said vitamin D comprises vitamin D3.
Preferably, the pueraria flower extract is selected from the group consisting of: C1-C4 lower alcohol extract, water extract, C1-C4 lower alcohol water extract, or combinations thereof.
Preferably, the pueraria flower extract comprises a dry extract.
Preferably, the pueraria flower extract is a dry extract.
Preferably, the pueraria flower extract is prepared by solvent extraction selected from the group consisting of: water, C1-C4 lower alcohol, C1-C4 lower alcohol in water, or combinations thereof.
Preferably, the pueraria flower extract is prepared by the following method:
extracting flos Puerariae Lobatae with solvent, filtering, concentrating the filtrate, and drying to obtain flos Puerariae Lobatae extract.
Preferably, the extraction solvent is selected from the group consisting of: water, C1-C4 lower alcohol, C1-C4 lower alcohol in water, or combinations thereof.
Preferably, the pueraria flower extract is prepared by the following method:
adding 90-98% (v/v) ethanol 4-6 times the weight of flos Puerariae Lobatae, heating and reflux extracting for 8-12 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain the flos Puerariae Lobatae ethanol extract.
Preferably, the C1-C4 lower alcohol comprises one or more of methanol, ethanol, propanol and butanol.
Preferably, the volume fraction of the C1-C4 lower alcohol in the aqueous solution of the C1-C4 lower alcohol is 80-98%, preferably 85-98% (v/v), more preferably 90-98% (v/v).
Preferably, the composition further comprises xylitol.
In a second aspect, the present invention provides a composition comprising a pueraria flower extract and vitamin D.
Preferably, the pueraria flower extract is selected from the group consisting of: C1-C4 lower alcohol extract, water extract, C1-C4 lower alcohol water extract, or combinations thereof.
Preferably, the C1-C4 lower alcohol comprises one or more of methanol, ethanol, propanol and butanol.
Preferably, the pueraria flower extract is prepared by the following method:
adding 90-98% (v/v) ethanol 4-6 times the weight of flos Puerariae Lobatae, heating and reflux extracting for 8-12 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain the flos Puerariae Lobatae ethanol extract.
Preferably, the C1-C4 lower alcohol comprises one or more of methanol, ethanol, propanol and butanol.
Preferably, the volume fraction of the C1-C4 lower alcohol in the aqueous solution of the C1-C4 lower alcohol is 80-98%, preferably 85-98% (v/v), more preferably 90-98% (v/v).
Preferably, the pueraria flower extract is as described in the first aspect of the present invention.
Preferably, said vitamin D comprises vitamin D3.
Preferably, the composition is a pharmaceutical composition, a food composition or a health-care product composition.
Preferably, the composition further comprises a pharmaceutically, food or nutraceutical acceptable carrier.
Preferably, the composition is in a solid or liquid form.
Preferably, the composition is in the form of oral preparation or injection preparation.
Preferably, the composition is in the form of emulsion, tablet, capsule, oral liquid, granule, powder or syrup.
Preferably, the composition is an oral liquid.
Preferably, the oral liquid comprises pueraria flower extract, vitamin D and water.
Preferably, the composition further comprises xylitol.
Preferably, the ratio (mg: IU) of the pueraria flower extract to the vitamin D is (1-40): (0.02-5), preferably (5-20): (0.05-1), more preferably (5-15): (0.05-0.5), more preferably (8-12): (0.08-0.2).
Preferably, the content of the pueraria flower extract is 1-99 wt%, preferably 10-90 wt%, more preferably 20-80 wt%, based on the total weight of the composition.
Preferably, the vitamin D is present in an amount of 1 to 99 wt%, preferably 10 to 90 wt%, more preferably 20 to 80 wt%, based on the total weight of the composition.
In a third aspect, the present invention provides the use of a composition according to the second aspect of the invention for the preparation of a medicament for (a) the prevention and/or treatment of vitamin D deficiency; (b) treating diseases associated with vitamin D deficiency.
Preferably, the vitamin D comprises vitamin D in blood.
Preferably, the disease related to vitamin D deficiency is one or more of rickets and osteoporosis.
It is to be understood that within the scope of the present invention, the above-described features of the present invention and those specifically described below (e.g., in the examples) may be combined with each other to form new or preferred embodiments.
Detailed Description
The invention discovers that the pueraria flower extract can be used for promoting the oral absorption of vitamin D, thereby improving the treatment effect of the vitamin D3 on vitamin D3 deficiency.
Term(s)
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.
As used herein, the terms "comprising," "including," and "containing" are used interchangeably and include not only open-ended definitions, but also semi-closed and closed-ended definitions. In other words, the term includes "consisting of … …", "consisting essentially of … …".
As used herein, the "flower of kudzu" is a flower of the leguminous plant kudzu vine lobata (Willd.) Ohwi, kudzu p.
As used herein, the term "IU" is an international unit.
As used herein, the term "95% (v/v) ethanol" refers to an aqueous ethanol solution having a volume fraction of ethanol of 95%, e.g., 95% ethanol is formulated from 95ml absolute ethanol +5ml water.
Use of
The invention provides application of a pueraria flower extract to promoting oral absorption of vitamin D.
Typically, the vitamin D includes vitamin D3.
In a preferred embodiment of the invention, the pueraria flower extract is C1-C4 lower alcohol extract, water extract or C1-C4 lower alcohol water extract. Preferably, the pueraria flower extract is C1-C4 lower alcohol extract.
In a preferred embodiment of the present invention, the pueraria flower extract comprises a dry extract.
In a preferred embodiment of the present invention, the pueraria flower extract is prepared by extracting with a solvent selected from the group consisting of: water, C1-C4 lower alcohol, C1-C4 lower alcohol in water, or combinations thereof.
Typically, the pueraria flower extract is prepared by the following method:
extracting flos Puerariae Lobatae with solvent, filtering, concentrating the filtrate, and drying to obtain flos Puerariae Lobatae extract.
Preferably, the extraction solvent is selected from the group consisting of: water, C1-C4 lower alcohol, C1-C4 lower alcohol aqueous solution, or a combination thereof.
In a preferred embodiment of the present invention, the pueraria flower extract is prepared by the following method:
adding 90-98% (v/v) ethanol 4-6 times the weight of flos Puerariae Lobatae, heating and reflux extracting for 8-12 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain the flos Puerariae Lobatae ethanol extract.
In a preferred embodiment of the invention, the C1-C4 lower alcohol comprises one or more of methanol, ethanol, propanol and butanol.
In a preferred embodiment of the present invention, the volume fraction of the C1-C4 lower alcohol in the aqueous solution of the C1-C4 lower alcohol is 80-98%, preferably 85-98% (v/v), more preferably 90-98% (v/v).
Composition comprising a metal oxide and a metal oxide
The invention also provides a composition which can be a pharmaceutical composition, a food composition or a health-care product composition.
The composition also comprises a carrier acceptable in pharmacy, food or health care products.
As used herein, the term "pharmaceutically, comestibly or nutraceutically acceptable carrier" refers to: one or more compatible solid, semi-solid, liquid or gel fillers suitable for human or animal use and of sufficient purity and sufficiently low toxicity.
It is to be understood that, in the present invention, the carrier is not particularly limited, and may be prepared using materials commonly used in the art, or by a conventional method, or may be commercially available. Examples of the pharmaceutically acceptable carrier moiety are cellulose and its derivatives (e.g., methylcellulose, ethylcellulose, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, etc.), gelatin, talc, solid lubricants (e.g., stearic acid, magnesium stearate), calcium sulfate, vegetable oils (e.g., soybean oil, sesame oil, etc.), polyols (e.g., propylene glycol, glycerin, sorbitol, etc.), emulsifiers (e.g., tween), wetting agents (e.g., sodium laurylsulfate), buffers, chelating agents, thickeners, pH adjusters, transdermal enhancers, colorants, flavors, stabilizers, antioxidants, preservatives, bacteriostats, pyrogen-free water, etc.
In the present invention, the dosage form of the pharmaceutical composition includes, but is not limited to, oral preparations or injectable preparations.
Typically, the composition is in the form of emulsion, tablet, capsule, oral liquid, granule, powder or syrup. Preferably, the composition is an oral liquid.
In a preferred embodiment of the invention, the composition comprises pueraria flower extract and vitamin D.
Preferably, said vitamin D comprises vitamin D3.
Preferably, the composition further comprises xylitol. When the composition is orally administered, xylitol can improve taste and improve oral administration compliance.
In a preferred embodiment, the ratio (mg: IU) of the pueraria flower extract to the vitamin D is (1-40): (0.02-5), preferably (5-20): (0.05-1), more preferably (5-15): (0.05-0.5), more preferably (8-12): (0.08-0.2).
The present invention also provides a use of a composition containing pueraria flower extract and vitamin D for (a) preventing and/or treating vitamin D deficiency; (b) treating diseases associated with vitamin D deficiency.
Preferably, the vitamin D comprises vitamin D in blood.
Preferably, the disease related to vitamin D deficiency is one or more of rickets and osteoporosis.
The main technical effects of the invention comprise:
1. the invention discovers that the pueraria lobata flower extract can obviously improve the oral absorption of vitamin D (such as vitamin D3), so that the pueraria lobata flower extract can obviously improve the treatment effect of oral administration of vitamin D3 on vitamin D3 deficiency.
2. The flos Puerariae Lobatae extract can improve oral absorption of vitamin D (such as vitamin D3), reduce oral dosage of vitamin D (such as vitamin D3), and reduce administration cost.
The invention will be further illustrated with reference to the following specific examples. It should be understood that these examples are for illustrative purposes only and are not intended to limit the scope of the present invention.
Example 1
1. Preparation method of flos Puerariae Lobatae alcohol extract
Pulverizing flos Puerariae Lobatae, adding 5 weight times of 95% (v/v) ethanol, heating and reflux extracting for 10 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain dry extract, i.e. flos Puerariae Lobatae ethanol extract.
2. Preparation of water extract of flos Puerariae Lobatae
Pulverizing flos Puerariae Lobatae, adding 5 weight times of water, heating and extracting at 70 deg.C for 10 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain dry extract, i.e. flos Puerariae Lobatae water extract.
3. Investigating the inducing effect of the pueraria flower extract on vitamin D3
Vitamin D3 (V)D3) MeasuringDetermining: the vitamin D3 content in mouse serum was determined using a vitamin D3 enzyme linked immunosorbent assay (ELISA) kit.
Statistical analysis: the measurement adopts M +/-SD, SPSS software is adopted for data analysis, two-two comparison adopts t test, and p is less than 0.05, so that the statistical significance is achieved.
The experimental method comprises the following steps:
dividing normal healthy male ICR mice into experiment group 1, experiment group 2, experiment group 3, experiment group 4 and control group, wherein each group comprises 8 mice, wherein the mice in experiment group 1 are intragastrically administered with normal saline (the dosage of the intragastrically administered flos puerariae extract is 10mg/kg body weight), the mice in experiment group 2 are intragastrically administered with normal saline with vitamin D3 (the dosage of the intragastrically administered vitamin D3 is 0.1IU/kg body weight), the mice in experiment group 3 are intragastrically administered with normal saline with flos puerariae alcohol extract and vitamin D3 (the dosage of the intragastrically administered flos puerariae extract is 10mg/kg body weight and the dosage of the vitamin D3 is 0.1IU/kg body weight), the mice in experiment group 4 are intragastrically administered with normal saline with flos puerariae water extract and vitamin D3 (the dosage of the aqueous flos puerariae extract is 10mg/kg body weight and the dosage of the vitamin D3 is 0.1IU/kg body weight), the control group of mice was gavage with normal saline, the mice of different groups were gavage at the frequency of once every 2 days for 21 consecutive days, and the vitamin D3 content in the serum of the mice was measured by vitamin D3 enzyme-linked immunosorbent assay (ELISA) kit on 7 days, 14 days and 21 days, respectively, during the experiment, the mice of each group were fed with normal feed.
V in serum of mice of each group at different time pointsD3The contents of (A) are shown in Table 1:
TABLE 1V in serum of groups of miceD3Content of (ng/ml, M + -SD, n ═ 8)
Figure BDA0002811032180000071
P <0.05, compared to control.
As can be seen from table 1, the pueraria lobata flower extract can improve the absorption of vitamin D3, particularly the pueraria lobata flower alcohol extract, has a significant promoting effect on the oral absorption of vitamin D3, thereby significantly improving the oral availability of vitamin D3 and enhancing the therapeutic effect of vitamin D3 on vitamin D3 deficiency (such as osteoporosis and rickets).
The above description is only a preferred embodiment of the present application and is not intended to limit the present application, and various modifications and changes may be made by those skilled in the art. Any modification, equivalent replacement, improvement and the like made within the spirit and principle of the present application shall be included in the protection scope of the present application.

Claims (2)

1. A composition for promoting the oral absorption of vitamin D3, wherein the composition comprises a flower of Pueraria lobata extract and vitamin D3;
the pueraria flower extract is prepared by the following method:
pulverizing flos Puerariae Lobatae, adding 95% ethanol 5 times by weight, heating under reflux for 10 hr, filtering, concentrating the filtrate under reduced pressure, and drying to obtain dry extract, i.e. flos Puerariae Lobatae ethanol extract;
the ratio mg: IU of the pueraria flower extract to the vitamin D3 is 10: 0.1.
2. the composition of claim 1, wherein the composition is in the form of an emulsion, a tablet, a capsule, an oral liquid, a granule, a powder, or a syrup.
CN202011391358.3A 2020-12-01 2020-12-01 Flos puerariae extract and its use Active CN112353837B (en)

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CN101444523A (en) * 2005-07-04 2009-06-03 山东省医学科学院药物研究所 Application of pueraria flower glucoside in preparation of medical compound for remedying osteoporosis
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JP2017197461A (en) * 2016-04-26 2017-11-02 株式会社東洋新薬 Calcium absorption promoting composition
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CN101444523A (en) * 2005-07-04 2009-06-03 山东省医学科学院药物研究所 Application of pueraria flower glucoside in preparation of medical compound for remedying osteoporosis
CN101569638A (en) * 2009-06-02 2009-11-04 香港理工大学深圳研究院 New application of fructus ligustri lucidi in preparing medicines for adjusting human body vitamin D3 metabolism and medicines for promoting calcium absorption and medicinal preparation thereof
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