CN103859384A - Compound grape seed extract pellets and preparation method thereof - Google Patents

Compound grape seed extract pellets and preparation method thereof Download PDF

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Publication number
CN103859384A
CN103859384A CN201210535845.1A CN201210535845A CN103859384A CN 103859384 A CN103859384 A CN 103859384A CN 201210535845 A CN201210535845 A CN 201210535845A CN 103859384 A CN103859384 A CN 103859384A
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CN
China
Prior art keywords
seed extract
micropill
grape
preparation
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201210535845.1A
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Chinese (zh)
Inventor
魏洪君
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd
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JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd
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Filing date
Publication date
Application filed by JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd filed Critical JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd
Priority to CN201210535845.1A priority Critical patent/CN103859384A/en
Publication of CN103859384A publication Critical patent/CN103859384A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23PSHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
    • A23P10/00Shaping or working of foodstuffs characterised by the products
    • A23P10/20Agglomerating; Granulating; Tabletting
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs

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  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Mycology (AREA)
  • Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention provides a compound grape seed extract pellet preparation, which is prepared from a grape seed extract, lycopene and a pharmaceutical auxiliary material, and is characterized in that the pharmaceutical auxiliary material is an excipient and a binder, wherein the content of the grape seed extract in the pellet preparation is 5-20 wt%, the content of the lycopene in the pellet preparation is 1-5 wt%, the content of the excipient in the pellet preparation is 70-85 wt%, and the content of the binder in the pellet preparation is 1-5 wt%. According to the present invention, the pellet preparation has characteristics of high dissolution rate and high bioavailability, and the preparation method is simple and convenient, and is easy to operate.

Description

A kind of compound grape-seed extract micropill and preparation method thereof
Technical field
The present invention relates to medicine food technical field, be specifically related to micropill that a kind of compound grape-seed extract makes and preparation method thereof.
Background technology
The various folk prescription health products of grape seed extract and lycopene are more, but the compound preparation about the two has no report, at present, deeply be subject to consumers in general's approval about the product of grape seed extract and lycopene, these products are except being single preparations of ephedrine, substantially be common Tablet and Capsula agent, but above-mentioned formulation exists disintegration time long; A certain position point disintegration in vivo, has certain excitant to gastric mucosa; The shortcomings such as bioavilability is low.Based on the problems referred to above, we will develop micropill technology transfer rapidly to field of food at field of medicaments, this product made and discharged in vivo compound micro-pill type product controlled and that bioavilability is high, to meet better consumers in general's demand.
In the preparation process of pellet preparations, generally to add the pharmaceutic adjuvants such as excipient, adhesive, pore-foaming agent, disintegrant, plasticizer [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc., Chinese Medicine science and technology publishing house, 2006,257-258], in the research process of micropill, need to carry out deep research to preparation preparation, just can prepare qualified micropill product.
Summary of the invention
The object of the invention is, in order to overcome the problems of the prior art, provides a kind of novel formulation of compound grape-seed extract---pellet preparations.
Another object of the present invention is to provide a kind of preparation method of compound grape-seed extract micropill preparation, the method is simple, convenient, easy operating.
Compound grape-seed extract of the present invention can be extract, can be also active ingredient, prepares according to existing literature method or patented method.
The object of the invention is to be achieved through the following technical solutions:
A kind of compound grape-seed extract micropill preparation, be prepared from by grape seed extract, lycopene, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, grape seed extract weight percentage is 5~20%, the weight percentage of lycopene is 1~5%, the weight percentage of excipient is 70~85%, and the weight percentage of adhesive is 1~5%.
Slow release formulation prepared by above-mentioned compound grape-seed extract micropill preparation.
Or the enteric formulation prepared of above-mentioned compound grape-seed extract micropill preparation.
Wherein said excipient is one or more the mixture being selected from sucrose, dextrin, starch, microcrystalline cellulose, lactose, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl methylcellulose and gelatin.
Wherein said adhesive is one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, carbohydrate, animal acid.
Pellet preparations of the present invention can, according to technique scheme, be prepared with the preparation method of prior art pellet preparations, also can be prepared by the following method:
(1) get grape seed extract, lycopene, add excipient, be crushed to micronized rank, mix;
(2) by the solution in water-soluble adhesive, absolute ethyl alcohol or hydrous ethanol;
(3) adopt micropill forming technique to make micropill.
Wherein said micropill forming technique comprises that being selected from general ball method, extruding-round as a ball one-tenth ball method or centrifugal-fluidisation makes ball method.
In conventional art, the degree of grinding of medicinal material or extract is meal (inside take, particle diameter 850um ± 70um, cross 24 mesh sieves), middle powder (inside take, particle diameter 250um ± 9.9um, cross 65 mesh sieves), fine powder (wound use, particle diameter 150um ± 6.6um, cross 100 mesh sieves), fine powder (eye droppings use, particle diameter 125um ± 5.8um, 120 mesh sieves) and impalpable powder (particle diameter 75um ± 4.1um, 200 mesh sieves), the present invention adopts micronization technology that compound grape-seed extract is ground into micro mist, its average grain diameter is generally less than 10um, is mainly distributed in 1~20um.Method of micronization can adopt method of the prior art: physical crushing method, such as mechanical impact crusher, airslide disintegrating mill, ball mill, vibromill, stirring mill, Raymond mill, high-pressure pulverizer etc.; Physical chemistry synthetic method, comprising that spraying is dry, original position micronizing and supercritical fluid technique etc.Compared with traditional crushing technology, this technique main advantage is: increase active ingredient absorptivity, improve bioavilability.The dissolution rate of active ingredient is directly proportional to its specific grain surface is long-pending, and specific area and particle diameter are inversely proportional to.Therefore, the particle diameter of active ingredient is thinner, and its specific area is larger, more contributes to the stripping of active ingredient.According to the study, stomach is 15um left and right to the optimal absorption granularity of material grains, and the particle of micron composition has just reached this optimal absorption fineness level; Because micron order active ingredient obviously increases in GI solubility, thereby increase its bioavilability, accelerated its onset time.
Micropill forming technique in the present invention can adopt any micropill forming technique of the prior art, and these technology include but not limited to: general ball method, extruding-round as a ball one-tenth ball method or centrifugal-fluidisation are made ball method etc.
Beneficial effect of the present invention is:
First, grape seed extract, lycopene and excipient have been carried out sufficient pulverizing by we, grape seed extract and lycopene have been distributed in excipient well, and particle diameter has reached micro powder grade, make micropill with such material, in the process discharging in vivo, principal component can discharge rapidly along with the dissolving of excipient, and the every capsules of this product is made up of the little micropill unit of hundreds of grain, disperse in vivo area large, the specific area contacting with gastric juice is also large, admittedly it is rapid to make this product take rear onset, bioavilability is high.
The micropill that micropill of the present invention can be made quick release or be discharged at a slow speed by different prescriptions as required, belongs to multiple agent type, can be made up of the micropill of different drug release rates.Also can pass through packaging technique, micropill is made to the positioned releasing micropills such as stomach dissolution type, enteric solubility.This micropill can encapsulatedly be made capsule, or compressing tablet makes tablet, or makes other various packaged forms.Micropill of the present invention is compared with single dose formulation (as tablet), and supplementary product consumption is few, and steady quality has good curative effect reappearance, and adverse reaction rate is low; This product micropill increases at the area of intestines and stomach surface distributed, bioavilability is improved and local excitation is less or eliminate, and selects for consumers in general provide more consumption.
Meanwhile, we can also, by micropill being carried out to the technology of dressing, by different coating materials, make product become the product of the different sizes such as slowly-releasing, controlled release, enteric.
The consumer who has gastric lesions for some, the impact for fear of product on stomach makes this product be absorbed by the body better simultaneously, and we can also make enteric coated preparations by this product, by micropill is carried out to enteric coated technology, make product reach the object of enteric.This enteric-coated micro-pill is carried out the discovery of release in vitro simulated test by we, micropill in simulated gastric fluid 2 hours without any stripping, outward appearance is also without any variation, and in the time that we are put into its taking-up in simulated intestinal fluid dissolution test, its 30 minutes releases have just reached more than 90%.
 
The specific embodiment
 
embodiment 1
Get the raw material for standby of following formula
Grape seed extract 15g(is in sterling)
Lycopene 1g
Celluloasun Microcrystallisatum 80g
Hydroxypropyl methylcellulose 4g
Prepare in accordance with the following methods pellet preparations:
(1) grape seed extract, the lycopene of getting above-mentioned formula ratio add Celluloasun Microcrystallisatum, are crushed to micronizing rank with ball mill, mix;
(2) hydroxypropyl methylcellulose is dissolved in to 75% ethanolic solution;
(3) adopt extruding-round as a ball one-tenth ball method to make micropill.
?
embodiment 2
Get the raw material for standby of following formula
Grape seed extract 10g(is in sterling)
Lycopene 3g
Starch 82g
Polyvinylpyrrolidone 5g
Prepare in accordance with the following methods pellet preparations:
(1) grape seed extract, the lycopene of getting above-mentioned formula ratio add starch, are crushed to micronizing rank with ball mill, mix;
(2) polyvinyl pyrrolidone is soluble in water;
(3) adopt general ball method to make micropill.
embodiment 3
Get the raw material for standby of following formula
Grape seed extract 8g(is in sterling)
Lycopene 5g
Sucrose 49g
Starch 34g
Polyvinylpyrrolidone 4g
Prepare in accordance with the following methods pellet preparations:
(1) grape seed extract, the lycopene of getting above-mentioned formula ratio add sugarcane sugar and starch, are crushed to micronizing rank with ball mill, mix;
(2) polyvinylpyrrolidone is dissolved in suitable quantity of water;
(3) adopt centrifugal-fluidisation to make ball method and make micropill.

Claims (7)

1. a compound grape-seed extract micropill preparation, be prepared from by grape seed extract, lycopene, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, grape seed extract weight percentage is 5~20%, the weight percentage of lycopene is 1~5%, the weight percentage of excipient is 70~85%, and the weight percentage of adhesive is 1~5%.
2. the slow release formulation that prepared by a kind of compound grape-seed extract micropill preparation according to claim 1.
3. the enteric formulation that prepared by a kind of compound grape-seed extract micropill preparation according to claim 1.
4. a kind of compound grape-seed extract micropill preparation according to claim 1, wherein said excipient is one or more the mixture being selected from sucrose, dextrin, starch, microcrystalline cellulose, lactose, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl methylcellulose and gelatin.
5. a kind of compound grape-seed extract micropill preparation according to claim 1, wherein said adhesive is one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, carbohydrate, animal acid.
6. according to the preparation method of a kind of compound grape-seed extract micropill preparation described in claim 1~5 any one, the steps include:
(1) get grape seed extract, lycopene, add excipient, be crushed to micronized rank, mix;
(2) by the solution of water-soluble adhesive, absolute ethyl alcohol or hydrous ethanol;
(3) adopt micropill forming technique to make micropill.
7. preparation method according to claim 6, wherein said micropill forming technique comprises that being selected from general ball method, extruding-round as a ball one-tenth ball method or centrifugal-fluidisation makes ball method.
CN201210535845.1A 2012-12-13 2012-12-13 Compound grape seed extract pellets and preparation method thereof Pending CN103859384A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201210535845.1A CN103859384A (en) 2012-12-13 2012-12-13 Compound grape seed extract pellets and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201210535845.1A CN103859384A (en) 2012-12-13 2012-12-13 Compound grape seed extract pellets and preparation method thereof

Publications (1)

Publication Number Publication Date
CN103859384A true CN103859384A (en) 2014-06-18

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Country Status (1)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106262897A (en) * 2016-08-17 2017-01-04 佛山市夕泪饮料有限公司 A kind of beverage

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106262897A (en) * 2016-08-17 2017-01-04 佛山市夕泪饮料有限公司 A kind of beverage

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Application publication date: 20140618