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CN110856715B - Composition, tablet and capsule containing vine tea extract - Google Patents

Composition, tablet and capsule containing vine tea extract Download PDF

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Publication number
CN110856715B
CN110856715B CN201910652720.9A CN201910652720A CN110856715B CN 110856715 B CN110856715 B CN 110856715B CN 201910652720 A CN201910652720 A CN 201910652720A CN 110856715 B CN110856715 B CN 110856715B
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vine tea
composition
chitosan
standard
extract
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CN110856715A (en
Inventor
远藤幸子
福原慎司
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Fancl Corp
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Fancl Corp
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • 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)
    • A61K36/87Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention provides a composition and a tablet or capsule which contain a large amount of vine tea extract and inhibit peculiar smell (odor evaluated as malodor) of vine tea. Specifically, the composition comprises chitosan and Ampelopsis grossedentata extract, wherein each composition comprises 10-35% by mass of chitosan and 5-22% by mass of ampelopsin (ampelopsin), and the composition with the mass ratio of chitosan/ampelopsin of 0.6-3.5 is prepared and prepared into tablets or capsules.

Description

Composition, tablet and capsule containing vine tea extract
Technical Field
The present invention relates to a composition for inhibiting the odor of vine tea extract and a tablet or capsule containing the same.
Background
Ampelopsis grossedentata is a plant of Ampelopsis genus of Vitaceae family, and Chinese name is Ampelopsis grossedentata. The school name is Ampelopsisgrossedentata. Mainly distributed in Guangxi, guangdong, yunnan, guizhou, hunan, hubei, jiangxi and Fujian provinces and autonomous regions in China. People in Guangxi and Hunan provinces or municipalities in China or Yao nationalities often drink beverages made from stems and leaves of the drinks, and the drinks are also used for cold, sore throat and the like.
Various physiological activities have been found in vine tea extracts, and medical uses or health food uses containing vine tea extracts have been proposed. For example, there have been proposed uses for treating liver diseases (patent document 1), lipase inhibition (patent document 2), matrix protease inhibition (patent document 3), antibacterial (patent document 4), perfume deterioration prevention (patent document 5), pigment discoloration prevention (patent document 6), and the like.
Regarding the Ampelopsis grossedentata extract, ampelopsin, a flavonoid compound, was identified as a component responsible for the above-mentioned various actions, and a large amount of extract containing the same was obtained. The material is obtained by extracting stem and leaf of Ampelopsis grossedentata with water or aqueous alcohol, and is commercially available as concentrated paste concentrate or spray-dried or freeze-dried powder.
The vine tea extract is clear that the vine tea extract has a peculiar unpleasant odor (peculiar smell) in a preparation process for preparing capsules or tablets containing the vine tea extract. The shelf life must necessarily be shortened because of the aggravation of long-term storage.
Therefore, a preparation containing a great amount of vine tea extract, which has little off-flavor even after long-term storage and is easy to drink, is sought.
Prior art literature
Patent literature
Patent document 1: japanese patent laid-open No. 2003-026584
Patent document 2: japanese patent laid-open publication No. 2003-012536
Patent document 3: japanese patent laid-open No. 2002-173424
Patent document 4: japanese patent laid-open No. 2002-159566
Patent document 5: japanese patent application laid-open No. 2004-018756
Patent document 6: japanese patent laid-open No. 2002-065201
Disclosure of Invention
The present inventors have studied on the basis of the above-described background art, and have studied on the vine tea extract under various formulation conditions, and have found that the peculiar smell of the vine tea extract can be suppressed when a composition containing chitosan and the vine tea extract is formulated. Based on such findings, the present invention proposes a composition containing chitosan and a vine tea extract, and a tablet or capsule containing the composition.
That is, the present invention aims to provide a composition, tablet or capsule which contains a large amount of vine tea extract and suppresses the peculiar smell (odor evaluated as malodor) of vine tea.
The main constitution of the present invention is as follows.
(1) A composition contains chitosan and Ampelopsis grossedentata extract, wherein each composition contains 10-35% by mass of chitosan and 5-22% by mass of ampelopsin, and the mass ratio of chitosan/ampelopsin is 0.6-3.5.
(2) A tablet comprising the composition of (1).
(3) A capsule comprising the composition of (1).
According to the present invention, there are provided a composition, a tablet and a capsule each of which suppresses the odor of a vine tea extract. In particular, according to the present invention, long-term storage is possible, and generation of an odor from the vine tea extract is suppressed, so that it is possible to obtain a preparation which is free from contact feeling even for the aged or children and is easy to swallow.
Detailed Description
The invention relates to a composition containing chitosan and vine tea extract, and a tablet or capsule containing the composition.
One of the main constituent components of the composition of the present invention is chitosan. The chitosan is a polysaccharide mainly having a structure in which glucosamine is linked through β1,4 bonds, and may contain N-acetylglucosamine as a constituent in addition to glucosamine.
The source of the chitosan used in the present invention is not particularly limited, and for example, a crustacean shell obtained by converting calcium, protein or the like from shrimp, crab or the like; and a substance obtained by deacetylation of chitin obtained by removing cuttlefish bone or the like.
In addition, the degree of deacetylation of the chitosan used in the present invention is not particularly limited. Generally, a material having a degree of deacetylation of 50 to 100% is used. The degree of deacetylation of chitosan was measured by a colloidal titration method.
Further, the average molecular weight of the chitosan used in the present invention is not particularly limited.
The chitosan used in the present invention is preferably a powder which is used as a food material and meets the commercial specifications.
The Ampelopsis grossedentata extract can be any 1 or more than 2 extracts of leaf, stem, flower and root of Ampelopsis grossedentata. Particular preference is given to using extracts of stems or leaves.
The method of extraction from vine tea is not particularly limited. The vine tea may be used as it is or as a dried product thereof in extraction, and the dried product is preferable in terms of extraction efficiency. In addition, the extraction of the active ingredient can be performed with high extraction efficiency in a short time under stable conditions by pulverizing into particles or powder for extraction. The extraction temperature is not particularly limited, and may be appropriately set according to the particle size of the pulverized vine tea, the kind of solvent, and the like.
The kind of the solvent is not particularly limited. Lower alcohols such as water and ethanol or a mixed solvent of these are preferable. The extraction may be performed at normal temperature. It may be carried out under heating (for example, using a heated solvent such as warm water or hot water).
According to the above extraction operation, the active ingredient of the present invention can be extracted from vine tea and dissolved in a solvent. The solvent containing the extract may be used directly. It is preferably used after the usual purification treatment such as sterilization, washing, filtration, decolorization and deodorization is performed as needed. Further, the solvent was completely volatilized to form a solid (dried product). The dried product may be redissolved in an arbitrary solvent, and powdered by an operation such as spray drying. In the present invention, the above-mentioned powder is preferably used.
The extract (extract) of Ampelopsis grossedentata is commercially available from Wan Kabushiki Kaisha. The commercially available ampelopsis grossedentata extract is a powder in which extraction rate is controlled and standardized by using ampelopsin, which is one of flavonoid compounds contained in a large amount in the leaves of ampelopsis grossedentata, as an index, and the powder can be used in the present invention.
In addition, the tendril tea extract causes extremely specific undesirable odor (off-flavor) in the above-mentioned encapsulating and tableting process.
A composition containing chitosan and Ampelopsis grossedentata extract is prepared by uniformly mixing powder of chitosan and Ampelopsis grossedentata extract for inhibiting odor of Ampelopsis grossedentata. The mixing amount and mixing proportion of the powder of chitosan and vine tea extract are very important. Preferably, the chitosan is contained in an amount of 10 to 35 mass% per part of the composition. Further, ampelopsin is preferably contained in a concentration of 5 to 22% by mass per one part of the composition, and the ampelopsis grossedentata extract is preferably contained. The weight ratio of chitosan/ampelopsin is adjusted to 0.6 to 3.5.
In addition, the composition containing chitosan and vine tea extract may be mixed with various excipients such as sugar or starch, etc. for the purpose of tablet formation by a tabletting method, and may be granulated as required. By compression molding the granules or powder according to a conventional method, a tablet with suppressed odor of vine tea extract can be obtained.
When the composition is prepared into capsules, the composition is filled into hard capsules according to a conventional method to prepare the capsules. In this case, various excipients such as sugar or starch may be mixed in the preparation of the capsule, and granulation may be performed as needed to prepare granules. Capsules with suppressed off-flavors of vine tea extracts can be obtained by filling the granule or powder composition into hard capsules following conventional methods.
In the preparation, the excipient used may be cellulose, starch, lactose, maltitol, cyclodextrin, hemicellulose, guar gum, konjac mannan, alginic acid, agar, carrageenan, chitin, carboxymethyl cellulose, or polydextrose. Cellulose or starch is particularly preferred.
Further, as long as the object of the present invention is not impaired, minerals such as edible oil, calcium, iron, sodium, zinc, copper, potassium, phosphorus, magnesium, iodine, manganese, selenium, etc., fat-soluble or water-soluble vitamin groups such as vitamin a, vitamin C, vitamin D, vitamin E, vitamin K, niacin, folic acid, pantothenic acid, etc., glycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, propylene glycol fatty acid ester, phospholipid, gum arabic, xanthan gum, tragacanth gum, locust bean gum, preservative, antioxidant, flavoring agent or flavor, flavoring agent such as sodium chloride, sodium glutamate, glycine, succinic acid, sodium lactate, etc., sour agents such as citric acid, sodium citrate, acetic acid, adipic acid, fumaric acid, malic acid, etc., low-calorie sweeteners such as aspartame, etc., may be formulated.
Examples
< Tablet >
The effect of the present invention will be described below by showing test examples using tablets of examples and comparative examples.
1. Odor assessment method
The nature of the malodour of vine tea extracts is currently not clear and therefore determines the digitisation based on sensory evaluation. Numerical values were determined by a skilled sensory evaluator by 2 comparison methods with standard, giving a score. Regarding the standard, tablets having the composition of table 1 below were prepared as the standard. In addition, the evaluation criteria are explicitly shown outside the columns of the table. The standard tablet was set to a tablet of phi 8mm, 250 mg/granule, and after mixing the raw materials, it was prepared using a single punch (manufactured by okang Tian Jinggong company) with a percussion pressure of 1000 kgf.
TABLE 1
Standard 5 Standard 4 Standard 3 Standard 2 Standard 1
Vine tea extract (30% Baisu) 0.5 5 15 25 30
Crystalline cellulose 88.5 84 74 64 59
Starch 10 10 10 10 10
Calcium stearate 1 1 1 1 1
Totalizing 100 100 100 100 100
Sensory evaluation was carried out with n=3
Sensory evaluation criteria:
5: odor intensity equivalent to 0.5% (standard 5) of Ampelopsis grossedentata extract
4: Odor intensity equivalent to 5% (standard 4) of Ampelopsis grossedentata extract
3: Odor intensity equivalent to 15% (standard 3) of Ampelopsis grossedentata extract
2: Odor intensity equivalent to 25% (standard 2) of Ampelopsis grossedentata extract
1: Odor intensity equivalent to 30% (standard 1) of Ampelopsis grossedentata extract
The odor intensities of criteria 5 to 1 are based on the contents shown in table 1, and correspond to the following expression in terms of sensory perception.
Standard 5: almost no odor was perceived.
Standard 4: some Xu Chouwei were felt.
Standard 3: a strong malodour is perceived but does not affect drinking.
Standard 2: a very strong odor was perceived and a conflict was perceived for drinking.
Standard 1: a bad smell was perceived.
2. Preparation and evaluation of tablets of examples 1 to 6 and comparative examples 1 to 6
According to the formulation of Table 2, the raw materials were mixed and then a tablet having a diameter of 8mm and a diameter of 250 mg/granule was produced by a single punch tablet press (manufactured by Gang Tian Jinggong Co.). After placing the 20 tablets in an aluminum bag and storing them in an oven at 40 ℃ and 75% RH for 2 weeks, the odor generated at the time of unsealing was evaluated by 3 sensory panelists who had been trained in the professionals. In addition, 5 tablets prepared as described above were used as standards, and the identity was judged by 2 comparison methods.
The evaluation is determined, for example, to be 3 if the test article is an unpleasant odor equivalent to standard 3. In addition, the sensory test results were averaged over 3 scores. The results are shown in the last row of table 2.
The unpleasant odor judged to be above the sensory evaluation average value 4 was reduced.
TABLE 2
< Formulation (%) >
The extract of vine tea (30% Baisu): pharmaceutical Co Ltd
Chitosan: "Chitosamine" manufactured by FOOD TECHNO Co., ltd "
Crystalline cellulose: xudi chemical Co., ltd., "CEOLUS UF-F702"
Starch: xudi chemical Co., ltd., "PCS-50"
Calcium stearate: calcium stearate manufactured by Sakai chemical industry Co., ltd "
From the experimental results using the tablets of examples 1 to 6 and comparative examples 1 to 6, it was revealed that the blending of chitosan was effective for suppressing the specific odor derived from the vine tea extract in the tablets containing the vine tea extract. In addition, in the composition before tabletting containing chitosan and vine tea extract, if each composition contains 5-22 mass% of ampelopsin and 10-35 mass% of chitosan, and the mass ratio of chitosan/ampelopsin is adjusted to 0.6-3.5, tablets which can not feel specific odor from vine tea can be obtained.
< Capsule >
The effect of the present invention will be described below by showing test examples using capsules of examples and comparative examples.
1. Odor assessment method
As with the tablet test, scores were given by a expert sensory evaluator judged by 2 comparison methods with the standard. Regarding the standard, capsules having the composition shown in table 3 below were prepared and used as the standard. In addition, the evaluation criteria are explicitly shown outside the columns of the table.
After mixing the raw materials, a hard capsule (capsule shell is manufactured by capsule corporation) of capsule size No.2 was prepared using a hard capsule filler ("Profill 100" manufactured by capsule corporation).
TABLE 3
Standard 5 Standard 4 Standard 3 Standard 2 Standard 1
Vine tea extract (30% Baisu) 0.5 5 15 25 30
Maltitol 98.5 94 84 74 69
Calcium stearate 1 1 1 1 1
Totalizing 100 100 100 100 100
Sensory evaluation was carried out with n=3
Sensory evaluation criteria:
5: odor intensity equivalent to 0.5% (standard 5) of Ampelopsis grossedentata extract
4: Odor intensity equivalent to 5% (standard 4) of Ampelopsis grossedentata extract
3: Odor intensity equivalent to 15% (standard 3) of Ampelopsis grossedentata extract
2: Odor intensity equivalent to 25% (standard 2) of Ampelopsis grossedentata extract
1: Odor intensity equivalent to 30% (standard 1) of Ampelopsis grossedentata extract
The odor intensities of criteria 5 to 1 were set as described in the above table 3, and they were equivalent to the following expression in terms of sensory properties.
Standard 5: almost no odor was perceived.
Standard 4: some Xu Chouwei were felt.
Standard 3: a strong malodour is perceived but does not affect drinking.
Standard 2: a very strong odor was perceived and a conflict was perceived for drinking.
Standard 1: a bad smell was perceived.
2. Preparation and evaluation of capsules of examples 7 to 12 and comparative examples 7 to 12
According to the formulation of table 4, the raw materials were mixed, and a hard capsule (capsule shell, manufactured by capsule corporation) of capsule size No. 2 was prepared using a hard capsule filler ("Profill" manufactured by capsule corporation) in the same manner as the standard. After the capsule 20 pellets were sealed in an aluminum bag and stored in an incubator at 40 ℃ 75% rh for 2 weeks, the odor generated at the time of unsealing was evaluated by 3 sensory panelists who had been subjected to specialized training.
In addition, identity was judged by 2 comparison methods with the 5 standard capsules prepared above.
The evaluation is determined, for example, to be 3 if the test article is an unpleasant odor equivalent to standard 3. In addition, the sensory test results were averaged over 3 scores. The results are shown in the last row of table 4.
The unpleasant odor judged to be above the sensory evaluation average value 4 was reduced.
TABLE 4
< Formulation (%) >
The extract of vine tea (30% Baisu): pharmaceutical Co Ltd
Chitosan: "Chitosamine" manufactured by FOOD TECHNO Co., ltd "
Maltitol: "Amalty MR-50" manufactured by Mitsubishi business FOOD TECHNO Co "
Calcium stearate: calcium stearate manufactured by Sakai chemical industry Co., ltd "
From the experimental results using the capsules of examples 7 to 12 and comparative examples 7 to 12, it was revealed that the blending of chitosan was effective in suppressing the specific odor derived from the vine tea extract in the capsules containing the vine tea extract. In addition, in the composition before filling the capsule containing chitosan and ampelopsin, if each part of the composition contains 5 to 22 mass percent of ampelopsin and 10 to 35 mass percent of chitosan, and the mass ratio of chitosan/ampelopsin is adjusted to be 0.6 to 3.5, the capsule which can not feel the specific odor from the ampelopsin can be obtained.

Claims (3)

1. An oral composition comprising chitosan and a vine tea extract, characterized in that each part of the composition comprises 30-70% by mass of vine tea extract and 10-35% by mass of chitosan; the content of ampelopsin from vine tea extract is 5-22% by mass, and the mass ratio of chitosan/ampelopsin from vine tea extract is 0.6-3.5.
2. A tablet comprising the oral composition of claim 1.
3. A capsule comprising the oral composition of claim 1.
CN201910652720.9A 2018-08-24 2019-07-19 Composition, tablet and capsule containing vine tea extract Active CN110856715B (en)

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JP2018157129A JP7156861B2 (en) 2018-08-24 2018-08-24 Composition, tablet, capsule containing wisteria tea extract
JP2018-157129 2018-08-24

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CN116808115A (en) * 2023-05-31 2023-09-29 姚美华 Application of ampelopsis grossedentata extract in preparation of antibacterial and/or repairing products

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CN102771593A (en) * 2011-05-13 2012-11-14 贵州省生物研究所 Ampelopsis grossedentata preparation for reducing blood sugar, blood lipid and blood pressure and its preparation method

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JP5004314B2 (en) 2001-06-27 2012-08-22 丸善製薬株式会社 Lipase inhibitor
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CN102772586A (en) * 2011-05-13 2012-11-14 贵州省生物研究所 Preparation with hangover alleviating and liver protection functions and preparation method thereof
CN102771593A (en) * 2011-05-13 2012-11-14 贵州省生物研究所 Ampelopsis grossedentata preparation for reducing blood sugar, blood lipid and blood pressure and its preparation method

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