CN104664397A - Micro-pills containing apple polyphenol, and preparation method of micro-pills - Google Patents
Micro-pills containing apple polyphenol, and preparation method of micro-pills Download PDFInfo
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- CN104664397A CN104664397A CN201310635633.5A CN201310635633A CN104664397A CN 104664397 A CN104664397 A CN 104664397A CN 201310635633 A CN201310635633 A CN 201310635633A CN 104664397 A CN104664397 A CN 104664397A
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- apple polyphenol
- pellet preparations
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- excipient
- micropill
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Abstract
The invention provides a micro-pill preparation containing apple polyphenol. The micro-pill preparation is prepared from apple polyphenol and pharmaceutical adjuvants, and is characterized in that the pharmaceutical adjuvants comprise an excipient and a bonding agent. The micro-pill preparation comprises 5-20% of apple polyphenol, 70-85% of excipient and 1-5% of a bonding agent by weight percent. The micro-pill preparation is high in dissolution rate and bioavailability, and a preparation method of the micro-pill preparation is simple, convenient and easy to operate.
Description
technical field:
The present invention relates to medicine food technical field, be specifically related to micropill that a kind of apple polyphenol makes and preparation method thereof.
background technology:
At present, about the product of apple polyphenol deeply by the accreditation of consumers in general, these products are common Tablet and Capsula agent substantially, 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, in order to overcome the problems of the prior art, to provide a kind of novel formulation of apple polyphenol---pellet preparations.
Another object of the present invention is to the preparation method that a kind of apple polyphenol pellet preparations is provided, the method is simple, convenient, be easy to operation.
The object of the invention is to be achieved through the following technical solutions:
A kind of apple polyphenol pellet preparations, be prepared from by apple polyphenol, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, apple polyphenol weight percentage is 5 ~ 20%, the weight percentage of excipient is 70 ~ 85%, and the weight percentage of adhesive is 1 ~ 5%.
Slow release formulation prepared by above-mentioned apple polyphenol pellet preparations.
Or enteric formulation prepared by above-mentioned apple polyphenol pellet preparations.
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 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 compound gingkgo leaf 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, apple polyphenol and excipient have been carried out sufficient pulverizing by us, apple polyphenol has been distributed in excipient well, and particle diameter reach 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
| Apple polyphenol | 15g |
| Celluloasun Microcrystallisatum | 80g |
| Hydroxypropyl methylcellulose | 4g |
Prepare pellet preparations in accordance with the following methods:
(1) get the apple polyphenol of above-mentioned formula ratio, add Celluloasun Microcrystallisatum, be 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
| Apple polyphenol | 10g |
| Starch | 82g |
| Polyvinylpyrrolidone | 5g |
Prepare pellet preparations in accordance with the following methods:
(1) get the apple polyphenol of above-mentioned formula ratio, add starch, be 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
| Apple polyphenol | 8g |
| Sucrose | 49g |
| Starch | 34g |
| Polyvinylpyrrolidone | 4g |
Prepare pellet preparations in accordance with the following methods:
(1) get the apple polyphenol of above-mentioned formula ratio, add sugarcane sugar and starch, be 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. an apple polyphenol pellet preparations, be prepared from by apple polyphenol, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and adhesive, in its pellet preparations, apple polyphenol weight percentage is 5 ~ 20%, the weight percentage of excipient is 70 ~ 85%, and the weight percentage of adhesive is 1 ~ 5%.
2. the slow release formulation prepared of a kind of apple polyphenol pellet preparations according to claim 1.
3. the enteric formulation prepared of a kind of apple polyphenol pellet preparations according to claim 1.
4. a kind of apple polyphenol pellet preparations 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 apple polyphenol pellet preparations 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 apple polyphenol pellet preparations according to any one of Claims 1 to 5, the steps include:
(1) get 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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310635633.5A CN104664397A (en) | 2013-12-03 | 2013-12-03 | Micro-pills containing apple polyphenol, and preparation method of micro-pills |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310635633.5A CN104664397A (en) | 2013-12-03 | 2013-12-03 | Micro-pills containing apple polyphenol, and preparation method of micro-pills |
Publications (1)
| Publication Number | Publication Date |
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| CN104664397A true CN104664397A (en) | 2015-06-03 |
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| CN201310635633.5A Pending CN104664397A (en) | 2013-12-03 | 2013-12-03 | Micro-pills containing apple polyphenol, and preparation method of micro-pills |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105995987A (en) * | 2016-05-25 | 2016-10-12 | 吴立超 | Apple dietary fiber pill and preparation method thereof |
-
2013
- 2013-12-03 CN CN201310635633.5A patent/CN104664397A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105995987A (en) * | 2016-05-25 | 2016-10-12 | 吴立超 | Apple dietary fiber pill and preparation method thereof |
| CN105995987B (en) * | 2016-05-25 | 2019-03-08 | 吴立超 | Apple dietary fiber ball and preparation method thereof |
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Application publication date: 20150603 |