CN105475735A - Compound mulberry extract product pellets and preparation method thereof - Google Patents

Compound mulberry extract product pellets and preparation method thereof Download PDF

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Publication number
CN105475735A
CN105475735A CN201410496505.1A CN201410496505A CN105475735A CN 105475735 A CN105475735 A CN 105475735A CN 201410496505 A CN201410496505 A CN 201410496505A CN 105475735 A CN105475735 A CN 105475735A
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CN
China
Prior art keywords
micropill
mulberry extract
preparation
weight percentage
excipient
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Pending
Application number
CN201410496505.1A
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Chinese (zh)
Inventor
魏洪君
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JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd
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JF-PHARMALAND TECHNOLOGY DEVELOPMENT Co Ltd
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Priority to CN201410496505.1A priority Critical patent/CN105475735A/en
Publication of CN105475735A publication Critical patent/CN105475735A/en
Pending legal-status Critical Current

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Abstract

The invention provides compound mulberry extract product pellets, which can be prepared by an mulberry extract product, apple polyphenol and a pharmaceutic adjuvant. The compound mulberry extract product pellets are characterized in that the pharmaceutic adjuvant is an excipient and an adhesive, the weight percentage of the mulberry extract product in the compound mulberry extract product pellets accounts for 10-30%, the weight percentage of the apple polyphenol in the compound mulberry extract product pellets accounts for 5-10%, the weight percentage of the excipient accounts for 50-80%, and the weight percentage of the adhesive accounts for 5-10%. The compound mulberry extract product pellets have the advantages that leaching rate is high, bioavailability is high, preparation method is simple and convenient, and operation is easy.

Description

A kind of mulberry 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 mulberry extract makes and preparation method thereof.
background technology:
The various folk prescription health products of mulberries extract and apple polyphenol are more, but the compound preparation about the two has no report, at present, about the product of mulberries extract and apple polyphenol deeply by the accreditation of consumers in general, these products are except for except single preparations of ephedrine, substantially be common Tablet and Capsula agent, but above-mentioned formulation to there is 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 discharge the controlled and compound micro-pill type product that bioavilability is high in vivo, to meet the demand of consumers in general better.
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. generally will be added in the preparation process of pellet preparations, China Medical Science Press, 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 to overcome the problems of the prior art, a kind of novel formulation---pellet preparations of mulberry extract is provided.
Another object of the present invention is to the preparation method that a kind of mulberry extract micropill preparation is provided, the method is simple, convenient, be easy to operation.
Mulberry extract of the present invention can be extract, also can be active ingredient, prepare 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 mulberry extract micropill preparation, be prepared from by mulberries extract, apple polyphenol, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, mulberries extract weight percentage composition is 10 ~ 30%, the weight percentage of apple polyphenol is 5 ~ 10%, the weight percentage of excipient is 50 ~ 80%, and the weight percentage of adhesive is 5 ~ 10%.
Slow release formulation prepared by above-mentioned mulberry extract micropill preparation.
Or enteric formulation prepared by above-mentioned mulberry extract micropill preparation.
Wherein said excipient is the mixture of one or more be selected from sucrose, dextrin, starch, microcrystalline cellulose, lactose, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl methylcellulose and gelatin.
Wherein said adhesive is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, carbohydrate, animal acid.
Pellet preparations of the present invention according to technique scheme, can be prepared with the preparation method of prior art pellet preparations, also can be prepared by the following method:
(1) get mulberries extract, apple polyphenol, add excipient, be crushed to micronized rank, mixing;
(2) in the solution in adhesive is water-soluble, absolute ethyl alcohol or hydrous ethanol;
(3) micropill forming technique is adopted to make micropill.
Wherein said micropill forming technique comprises and is selected from general ball method, extruding-round as a ball one-tenth ball method or centrifugal-fluidisation and 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), most 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 then adopts micronization technology that mulberry 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, Ball-stirring mill, Raymond mill, high-pressure pulverizer etc.; Physical chemistry synthetic method, comprises spraying dry, original position micronizing and supercritical fluid technique etc.Compared with conventional size reduction technology, this technique main advantage is: increase active ingredient absorptivity, improves 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, then its specific area is larger, more contributes to the stripping of active ingredient.According to the study, the optimal absorption granularity of stomach to material grains is about 15um, and the particle of micron composition just reaches this optimal absorption fineness level; Because micron order active ingredient obviously increases in GI solubility, thus increase its bioavilability, accelerate 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 make ball method etc.
Beneficial effect of the present invention is:
First, mulberries extract, apple polyphenol and excipient have been carried out sufficient pulverizing by us, mulberries extract and apple polyphenol is made to be distributed in excipient well, and particle diameter reaches micro powder grade, micropill is made with such material, in the process discharged 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 micropill unit that hundreds of grain is little, diffusional area is large in vivo, the specific area contacted with gastric juice is also large, admittedly make this product take rear onset rapidly, bioavilability is high.
Micropill of the present invention as required by the micropill that different prescription is made release fast or discharged at a slow speed, can belong to multiple agent type, can be made up of the micropill of different drug release rate.Also by packaging technique, micropill is made the positioned releasing micropills such as stomach dissolution type, enteric solubility.This micropill encapsulatedly can make capsule, or tablet made by compressing tablet, or makes other various packaged forms.Micropill of the present invention is compared with Single unit dosage forms (as tablet), and supplementary product consumption is few, steady quality, and have good curative effect reappearance, adverse reaction rate is low; This product micropill increases at the area of intestines and stomach surface distributed, makes bioavilability raising and local excitation is less or eliminate, for consumers in general provide more consumption choice.
Meanwhile, we can also, by carrying out the technology of dressing to micropill, by different coating materials, make product become the product of the different sizes such as slowly-releasing, controlled release, enteric.
Some are existed to the consumer of gastric lesions, in order to avoid product is on the impact of stomach, make this product be absorbed by the body better, this product can also be made enteric coated preparations by us simultaneously, namely by carrying out enteric coated technology to micropill, makes product reach the object of enteric.This enteric-coated micro-pill is carried out the discovery of release in vitro simulated test by us, micropill in simulated gastric fluid 2 hours without any stripping, outward appearance also without any change, when we taken out be put into dissolution test in simulated intestinal fluid time, its 30 minutes releases just reach more than 90%.
Detailed description of the invention
embodiment 1
Get the raw material for standby of following formula
Mulberries extract 10g(is in sterling)
Apple polyphenol 5g
Celluloasun Microcrystallisatum 80g
Hydroxypropyl methylcellulose 5g
Prepare pellet preparations in accordance with the following methods:
(1) mulberries extract, the apple polyphenol of getting above-mentioned formula ratio add Celluloasun Microcrystallisatum, are crushed to micronizing rank with ball mill, mixing;
(2) hydroxypropyl methylcellulose is dissolved in 75% ethanolic solution;
(3) extruding-round as a ball one-tenth ball method is adopted to make micropill.
embodiment 2
Get the raw material for standby of following formula
Mulberries extract 20g(is in sterling)
Apple polyphenol 8g
Celluloasun Microcrystallisatum 65g
Hydroxypropyl methylcellulose 7g
Prepare pellet preparations in accordance with the following methods:
(1) mulberries extract, the apple polyphenol of getting above-mentioned formula ratio add starch, are crushed to micronizing rank with ball mill, mixing;
(2) polyvinyl pyrrolidone is soluble in water;
(3) general ball method is adopted to make micropill.
embodiment 3
Get the raw material for standby of following formula
Mulberries extract 30g(is in sterling)
Apple polyphenol 10g
Sucrose 45g
Starch 10g
Polyvinylpyrrolidone 5g
Prepare pellet preparations in accordance with the following methods:
(1) mulberries extract, the apple polyphenol of getting above-mentioned formula ratio add sugarcane sugar and starch, are crushed to micronizing rank with ball mill, mixing;
(2) polyvinylpyrrolidone is dissolved in suitable quantity of water;
(3) adopt centrifugal-fluidisation to make ball method and make micropill.

Claims (7)

1. a mulberry extract micropill preparation, be prepared from by mulberries extract, apple polyphenol, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, mulberries extract weight percentage composition is 10 ~ 30%, the weight percentage of apple polyphenol is 5 ~ 10%, the weight percentage of excipient is 50 ~ 80%, and the weight percentage of adhesive is 5 ~ 10%.
2. the slow release formulation prepared of a kind of mulberry extract micropill preparation according to claim 1.
3. the enteric formulation prepared of a kind of mulberry extract micropill preparation according to claim 1.
4. a kind of mulberry extract micropill preparation according to claim 1, wherein said excipient is the mixture of one or more be selected from sucrose, dextrin, starch, microcrystalline cellulose, lactose, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl methylcellulose and gelatin.
5. a kind of mulberry extract micropill preparation according to claim 1, wherein said adhesive is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, carbohydrate, animal acid.
6. the preparation method of a kind of mulberry extract micropill preparation according to any one of Claims 1 to 5, the steps include:
(1) get mulberries extract, apple polyphenol, add excipient, be crushed to micronized rank, mixing;
(2) in the solution of adhesive is water-soluble, absolute ethyl alcohol or hydrous ethanol;
(3) micropill forming technique is adopted to make micropill.
7. preparation method according to claim 6, wherein said micropill forming technique comprises and is selected from general ball method, extruding-round as a ball one-tenth ball method or centrifugal-fluidisation and makes ball method.
CN201410496505.1A 2014-09-25 2014-09-25 Compound mulberry extract product pellets and preparation method thereof Pending CN105475735A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201410496505.1A CN105475735A (en) 2014-09-25 2014-09-25 Compound mulberry extract product pellets and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201410496505.1A CN105475735A (en) 2014-09-25 2014-09-25 Compound mulberry extract product pellets and preparation method thereof

Publications (1)

Publication Number Publication Date
CN105475735A true CN105475735A (en) 2016-04-13

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107519245A (en) * 2017-09-25 2017-12-29 广东省农业科学院蚕业与农产品加工研究所 A kind of preparation method with the mulberry fruit fine powder for improving gastrointestinal function

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107519245A (en) * 2017-09-25 2017-12-29 广东省农业科学院蚕业与农产品加工研究所 A kind of preparation method with the mulberry fruit fine powder for improving gastrointestinal function

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Application publication date: 20160413