CN101219126A - Beta-carotene pellet and method for preparing the same - Google Patents
Beta-carotene pellet and method for preparing the same Download PDFInfo
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- CN101219126A CN101219126A CNA2007101986997A CN200710198699A CN101219126A CN 101219126 A CN101219126 A CN 101219126A CN A2007101986997 A CNA2007101986997 A CN A2007101986997A CN 200710198699 A CN200710198699 A CN 200710198699A CN 101219126 A CN101219126 A CN 101219126A
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Abstract
The invention provides a beta-carotene micro-pill prepared from beta-carotene and medicinal adjuvant, characterized in that the medicinal adjuvant comprises an excipient and a bonding agent; the content of the beta-carotene in the beta-carotene micro-pill is 1-10 weight percent, the excipient 70-95 weight percent and the bonding agent 1-5 weight percent. The beta-carotene micro-pill of the invention has the advantages of high dissolution rate, high bioavailability, easy preparation method and convenient and easy operation.
Description
Technical field:
The present invention relates to the medicine food technical field, be specifically related to micropill that a kind of beta-carotene makes and preparation method thereof.
Background technology:
Beta-carotene, name derive from Latin Radix Dauci Sativae, belong to a member of native chemical thing (for example carotene or carotenoid) family.It exists in plant in large quantities, makes fruits and vegetables have full yellow and orange.The same with other carotenoid, beta-carotene is a kind of polyphenoils.The edible food that is rich in the beta-carotene can prevent a kind of saboteur who is called free radical of Body contact.By the process of an oxidation, free radical can damage by pair cell.If things go on like this, might cause human body to suffer from various chronic diseases.Some studies show that the beta-carotene of taking in capacity from diet may reduce the danger of suffering from two kinds of chronic diseases---heart disease and cancer.Remove in addition, beta-carotene also has the xerosis cutis of preventing, and is coarse; Help to improve body immunity, preventing cold; Promote skeleton and dental health to grow up; Improve the reproduction merit; Help good health purposes such as visual performance.
At present, be subjected to consumers in general's favor deeply about the product of beta-carotene, these products are common tablet and capsule substantially, above-mentioned dosage form exist disintegration time long; A certain position point disintegrate in vivo has certain zest to gastric mucosa; Shortcomings such as bioavailability 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 discharge micro-pill type product controlled and that bioavailability is high in vivo.
Generally to add pharmaceutic adjuvants such as excipient, binding agent, porogen, disintegrating agent, plasticizer [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc. in the preparation process of pellet preparations, Chinese Medicine science and technology publishing house, 2006,257-258], in the research process of micropill, need carry out deep research to formulation preparation, just can prepare qualified micropill product.
Summary of the invention:
For these reasons, we carry out deep analysis by physics and chemical property to beta-carotene, with the dissolution is index, test by science, determine that pharmaceutic adjuvant is excipient and binding agent, and excipient and binding agent are carried out determining of weight percentage: " pharmaceutic adjuvant is excipient and binding agent; the beta-carotene weight percentage is 1～10% in its pellet preparations; the weight percentage of excipient is 70～95%, and the weight percentage of binding agent is 1～5% "; By this complete technical scheme, those skilled in the art just can prepare satisfactory pellet preparations according to the preparation method of the micropill of prior art; Above-mentioned pellet preparations can be prepared into satisfactory slow releasing preparation or enteric coated preparation, help user's compliance.We have carried out sufficient pulverizing with beta-carotene and excipient, be that micronization is pulverized, make beta-carotene be distributed in the excipient well, make particle diameter reach micro powder grade, make micropill with such material, in vivo in the process of Shi Fanging, main constituent can discharge rapidly along with the dissolving of excipient, and this product is made up of the little micropill unit of hundreds of grain, disperse area big in vivo, the organ contacted specific surface area is also big with absorbing, so onset is rapid after making this product take, and the bioavailability height.
The objective of the invention is provides a kind of novel formulation-pellet preparations of beta-carotene in order to overcome the problems of the prior art.
Another object of the present invention is to provide a kind of preparation method of beta-carotene pellet preparation, this method is simple, convenient, easy operating.
Beta-carotene of the present invention can be an extract, also can be effective ingredient, prepares according to existing literature method or patented method.
The objective of the invention is to be achieved through the following technical solutions:
A kind of beta-carotene pellet preparation, be prepared from by beta-carotene, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, the beta-carotene weight percentage is 1～10% in its pellet preparations, the weight percentage of excipient is 70～95%, and the weight percentage of binding agent is 1～5%.
The slow release formulation of above-mentioned beta-carotene pellet formulation preparation.
Or the enteric dosage form of above-mentioned beta-carotene pellet formulation preparation.
Wherein said excipient is one or more the mixture that is selected from sucrose, dextrin, starch, microcrystalline Cellulose, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and the gelatin.
Wherein said binding agent is one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, saccharide, the animal acid.
Pellet preparations of the present invention can be according to technique scheme, is prepared with the preparation method of prior art pellet preparations, also can be prepared according to following method:
(1) gets beta-carotene, add excipient, be crushed to micronized rank, mixing;
(2) a kind of in the water-soluble or ethanol with binding agent, or in two kinds of solution that is mixed in proportion;
(3) adopt the micropill forming technique to make micropill.
Wherein said micropill forming technique comprises agitation procedure, method of extruding and kneading to pellets or the centrifugal fluidized granulation method of being selected from.
In the conventional art, the degree of grinding of medical material or extract is coarse powder (in take, particle diameter 850um ± 70um, cross 24 mesh sieves), middle powder (in take, particle diameter 250um ± 9.9um, cross 65 mesh sieves), fine powder (wound usefulness, particle diameter 150um ± 6.6um, cross 100 mesh sieves), fine powder (eye dripping usefulness, 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 beta-carotene is ground into micropowder, its mean diameter is generally less than 10um, mainly is distributed in 1～20um.Method of micronization can adopt method of the prior art: physical pulverization method, for example mechanical impact crusher, jet mill, ball mill, vibromill, stirring mill, Raymond mill, high-pressure micronizer machine etc.; The physical chemistry synthetic method comprises spray drying, original position micronization and supercritical fluid technology etc.Compare with traditional crushing technology, the main advantage of this technology is: increase the effective ingredient absorbance, improve bioavailability.The dissolution rate of effective ingredient is directly proportional with its specific grain surface is long-pending, and specific surface area and particle diameter are inversely proportional to.Therefore, the particle diameter of effective ingredient is thin more, and then its specific surface area is big more, helps the stripping of effective ingredient more.According to the study, the intestines and stomach is about 15um to the optimal absorption granularity of material grains, and the granule of micron composition has just reached this optimal absorption fineness level; Because the micron order effective ingredient obviously increases at the gastrointestinal dissolubility, thereby increases its bioavailability, has accelerated its onset time.
Micropill forming technique among the present invention can adopt any micropill forming technique of the prior art, and these technology include but not limited to: agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method etc.
Beneficial effect of the present invention is:
At first, we have carried out sufficient pulverizing with beta-carotene and excipient, make beta-carotene be distributed in the excipient well, and particle diameter has reached micro powder grade, make micropill with such material, in vivo in the process of Shi Fanging, main constituent 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 area big in vivo, also big with the gastric juice contacted specific surface area, admittedly onset is rapid after making this product take, the bioavailability height.
The micropill that micropill of the present invention can be made rapid release or discharge 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 be made positioned releasing micropills such as stomach dissolution type, enteric solubility.This micropill can encapsulatedly be made capsule, or tabletting makes tablet, or makes other various packaged forms.Micropill of the present invention is compared with single dose dosage form (as tablet), and supplementary product consumption is few, and steady quality has curative effect repeatability preferably, and adverse reaction rate is low; This product micropill increases at the area of gastrointestinal tract surface distributed, bioavailability is improved and local excitation is less or eliminate, and selects for consumers in general provide more consumption.
We have carried out release in vitro contrast test (experimental technique is according to Pharmacopoeia of People's Republic of China version dissolution in 2005 check and analysis method) with this product and commercially available tablet and conventional capsule agent, and the result is as follows:
The conventional capsule agent (Beijing manufacturer production, lot number: 070403) 30 minutes dissolution rates are 58% in gastric juice;
Tablet (Beijing manufacturer production, lot number: 061206) 30 minutes dissolution rates are 62% in gastric juice;
And this product 30 minutes dissolution rates in gastric juice promptly reach 90%.
Simultaneously, we can also by different coating materials, make product become the product of different sizes such as slow release, controlled release, enteric by micropill being carried out the technology of coating.
Therefore after we make slow-release micro-pill with this product, have 12 hours slow-release function, can effectively control the burst size of beta-carotene, safety, effectiveness are better; Slow-release micro-pill can make that concentration reaches curative effect concentration rapidly on the blood, and keep steadily, valid density for a long time, blood concentration fluctuation is little; This product has reduced the accumulated dose of taking than common dosage form simultaneously, has reduced the number of times of taking of consumer.We find that by the release in vitro simulation test its release profiles is obvious with this product, and when 2h, release is more than 30%; During 5h, release is more than 55%; During 8h, release is more than 75%; During 12h, release is more than 90%.
There is the consumer of stomach illness for some, for fear of the influence of product to stomach, this product is absorbed by the body better, we can also make enteric coated preparation with this product, promptly, make product reach the purpose of enteric by micropill is carried out enteric coated technology.We carry out the release in vitro simulation test with this enteric coated micropill and find, micropill in simulated gastric fluid 2 hours without any stripping, outward appearance is also without any variation, and when we were put into its taking-up in the simulated intestinal fluid dissolution test, its 25 minutes releases had just reached more than 90%.
The specific embodiment
Embodiment 1
Get the raw material for standby of following prescription
| Beta-carotene | (1.5g in pure product) |
| Starch | 94g |
| Hydroxypropyl emthylcellulose | 4.5g |
Prepare pellet preparations in accordance with the following methods:
(1) beta-carotene of getting above-mentioned formula ratio adds starch, is crushed to micronization rank, mixing with ball mill;
(2) hydroxypropyl emthylcellulose is dissolved in 75% alcoholic solution;
(3) adopt method of extruding and kneading to pellets to make micropill.
Embodiment 2
Get the raw material for standby of following prescription
| Beta-carotene | 5g (in pure product) |
| Starch | 90g |
| Polyvinylpyrrolidone | 5g |
Prepare pellet preparations in accordance with the following methods:
(1) beta-carotene of getting above-mentioned formula ratio adds starch, is crushed to micronization rank, mixing with ball mill;
(2) polyvinyl pyrrolidone is soluble in water;
(3) adopt agitation procedure to make micropill.
Embodiment 3
Get the raw material for standby of following prescription
| Beta-carotene | 8g (in pure product) |
| Celluloasun Microcrystallisatum | 88.5g |
| Hydroxypropyl emthylcellulose | 3.5g |
Prepare pellet preparations in accordance with the following methods:
(1) beta-carotene of getting above-mentioned formula ratio adds Celluloasun Microcrystallisatum, is crushed to micronization rank, mixing with ball mill;
(2) hydroxypropyl emthylcellulose is dissolved in an amount of 70% ethanol;
(3) adopt the centrifugal fluidized granulation method to make micropill.
Claims (7)
1. beta-carotene pellet preparation, be prepared from by bata-carotene, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, the beta-carotene weight percentage is 1～10% in its pellet preparations, the weight percentage of excipient is 70～95%, and the weight percentage of binding agent is 1～5%.
2. the slow release formulation of a kind of bata-carotene pellet preparations preparation according to claim 1.
3. the enteric dosage form of a kind of beta-carotene pellet formulation preparation according to claim 1.
4. a kind of beta-carotene pellet preparation according to claim 1, wherein said excipient are one or more the mixture that is selected from sucrose, dextrin, starch, microcrystalline Cellulose, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and the gelatin.
5. a kind of beta-carotene pellet preparation according to claim 1, wherein said binding agent are one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, saccharide, the animal acid.
6. according to the preparation method of each described a kind of beta-carotene pellet preparation of claim 1～5, the steps include:
(1) gets beta-carotene, add excipient, be crushed to micronized rank, mixing;
(2) in the solution of binding agent is water-soluble, dehydrated alcohol or aquiferous ethanol;
(3) adopt the micropill forming technique to make micropill.
7. preparation method according to claim 6, wherein said micropill forming technique comprise agitation procedure, method of extruding and kneading to pellets or the centrifugal fluidized granulation method of being selected from.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101986997A CN101219126A (en) | 2007-12-27 | 2007-12-27 | Beta-carotene pellet and method for preparing the same |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101986997A CN101219126A (en) | 2007-12-27 | 2007-12-27 | Beta-carotene pellet and method for preparing the same |
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| CN101219126A true CN101219126A (en) | 2008-07-16 |
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| CNA2007101986997A Pending CN101219126A (en) | 2007-12-27 | 2007-12-27 | Beta-carotene pellet and method for preparing the same |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106617227A (en) * | 2016-09-09 | 2017-05-10 | 江南大学 | Method for preparing beta-carotene microcapsule |
| CN108294297A (en) * | 2017-02-24 | 2018-07-20 | 南通励成生物工程有限公司 | A kind of preparation method of lutein nutrition fortifier |
-
2007
- 2007-12-27 CN CNA2007101986997A patent/CN101219126A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106617227A (en) * | 2016-09-09 | 2017-05-10 | 江南大学 | Method for preparing beta-carotene microcapsule |
| CN106617227B (en) * | 2016-09-09 | 2018-09-18 | 江南大学 | A method of preparing beta carotene microcapsules |
| CN108294297A (en) * | 2017-02-24 | 2018-07-20 | 南通励成生物工程有限公司 | A kind of preparation method of lutein nutrition fortifier |
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Open date: 20080716 |