CN102462796A - Aloe extract pellet and preparation method thereof - Google Patents
Aloe extract pellet and preparation method thereof Download PDFInfo
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- CN102462796A CN102462796A CN2010105497012A CN201010549701A CN102462796A CN 102462796 A CN102462796 A CN 102462796A CN 2010105497012 A CN2010105497012 A CN 2010105497012A CN 201010549701 A CN201010549701 A CN 201010549701A CN 102462796 A CN102462796 A CN 102462796A
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- aloe extract
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- excipient
- binding agent
- micropill
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Abstract
The invention provides an aloe extract pellet preparation, which is prepared with aloe extracts and pharmaceutical excipients. The aloe extract pellet preparation is characterized in that the pharmaceutical excipients adopt excipients and adhesives, the weight percentage of the aloe extracts in the pellet preparation is 2-70 percent, the weight percentage of the excipients is 29-90 percent, and the weight percentage of the adhesives is 1-8 percents. The pellet preparation can be made into sustained-release or enteric-coated preparations in accordance with requirements. Pharmacological experiments show that the pellet has good effects of sterilizing, diminishing inflammation, invigorating the stomach, facilitating the bowels, wetting and beautifying.
Description
Technical field
The present invention relates to the medicine food technical field, be specifically related to micropill that a kind of Aloe extract processes and preparation method thereof.
Background technology
Aloe extract is that liliaceous plant Aloe vulgaris Aloe barbadensis Miller, Aloe ferox Miller Aloe ferox Miller or other belong to the dry product of concentrated juice of kindred plant leaf together.Its pharmacological action is: 1. antibacterial, antiinflammation: aloetic Main Ingredients and Appearance tinctura aloes (Aloetin) is the very strong material of antibiotic property, has direct bactericidal action.All can suppress the growth breeding of pathogen to fungus, mycete, antibacterial, virus, and eliminate it, pathogenic bacterias such as dialogue carcinoma of the throat, tetanolysin, pulmonitis strain, escherichia coli also can play antibacterial, antibacterial action.Aloetic slow ground state enzyme and vasotonia combine can unite the opposing inflammation.Especially aloetic polysaccharide can be given resistance of human body, strengthens the resistivity and the anti-inflammation and sterilization of health.2. defecating feces excretion is good for the stomach: Aloe contains aloin (aloin), aloe-emodin active ingredients such as (emochin).Have the stomach of reinforcement function, appetite stimulator is kept the effect of body fluid alkalescence, thereby is improved body constitution, and physical strength reinforcing keeps full of vitality.The aloin composition can increase the secretion of big intestinal juice simultaneously, increases the activity that refers to the fat enzyme, stimulates the large intestine autonomic nerve of imbalance, therefore is to treat the most effectively medicine of constipation at all times, reaches the catharsis and toxin expelling effect.3. immunity is regenerated and antitumor action: Aloin A; Wound hormone and lance glycopeptide manna (KS-2) etc. have disease-resistant plain the infection; Curdlan and 1-decene-1 are united and are had the wound healing activity; Therefore Aloe also is a kind of desirable medicine of treating various skin injuries, wound is cured fully and does not stay scar.Thick substances polysaccharide in the Aloe has and improves immunity and very strong inhibition or destroy paracytic growth, thereby has antitumor action.4. moistening beautification function: Aloe polysaccharide and vitamin to human body skin limb good nutrition arranged, moisten, whitening effect.Especially teen-age acne treatment had good effect.Anthraquinone glycoside materials such as aloe-emodin can make hair soft and glossy, easily pleasant, the effect of anti-dandruff.
At present, receive consumers in general's approval deeply about the product of Aloe extract, except that the cosmetics external, Orally taken product is common tablet and capsule mostly, but above-mentioned dosage form exists disintegration time long; A certain site 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 rapidly that the micropill technology is incorporated into field of food at field of medicaments, these article processed discharge micro-pill type product controlled and that bioavailability is high in vivo, to satisfy consumers in general's demand better.
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 to Aloe extract physics and chemical property, are index with the dissolution; Test through science; Confirm that pharmaceutic adjuvant is excipient and binding agent, and excipient and binding agent are carried out confirming of weight percentage: " pharmaceutic adjuvant is excipient and binding agent, and wherein the Aloe extract weight percentage is 2%-70% in the pellet preparations; the excipient weight percentage is 29%-90%, and the percentage composition of binding agent is 1%-8% "; Through this complete technical scheme, those skilled in the art just can prepare satisfactory pellet preparations according to the method for preparing 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 carry out deep research to Aloe extract pellet preparations method for preparing on the basis of existing technology, and unexpected the discovery carried out sufficient pulverizing with Aloe extract and excipient; Be that micronization is pulverized, Aloe extract has been distributed in the excipient well, make particle diameter reach micro powder grade; Material with such is processed micropill, and in the process that discharges in vivo, main constituent can discharge rapidly along with the dissolving of excipient; And these article are made up of the little micropill unit of hundreds of grain, disperse area big in vivo, and the organ contacted specific surface area is also big with absorbing; Admittedly onset was rapid after these article of making were taken, bioavailability is high.
The objective of the invention is provides a kind of novel formulation of Aloe extract---pellet preparations in order to overcome the problems of the prior art.
Another object of the present invention is to provide a kind of method for preparing of Aloe extract pellet preparations, this method is simple, convenient, easy operating.
Aloe extract of the present invention prepares according to existing literature method or patented method.
The objective of the invention is to realize through following technical scheme:
A kind of Aloe extract pellet preparations; It is to be prepared from Aloe extract and pharmaceutic adjuvant; It is characterized in that pharmaceutic adjuvant is excipient and binding agent; Wherein the Aloe extract weight percentage is 2-70% in the pellet preparations, and the excipient weight percentage is 29-90%, and the percentage composition of binding agent is 1-8%.
The slow release formulation of above-mentioned Aloe extract pellet preparations preparation.
Or the enteric dosage form of above-mentioned Aloe extract pellet preparations 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, prepares with the method for preparing of prior art pellet preparations, also can prepare according to following method:
A kind of method for preparing of Aloe extract pellet preparations the steps include:
(1) gets Aloe extract, add excipient, be crushed to micronized rank, mixing;
(2) in the solution in binding agent is water-soluble, dehydrated alcohol or the aquiferous ethanol;
(3) adopt the micropill forming technique to process 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 Aloe extract 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 research, 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:
(1) in the prior art, do not have Aloe extract to be prepared into the technology of pellet preparations, we are through carrying out deep analysis to Aloe extract physics and chemical property; With the dissolution is index; Through the test of science, confirm that pharmaceutic adjuvant is excipient and binding agent, and do not have other pharmaceutic adjuvant; And excipient and binding agent are carried out confirming of weight percentage: " pharmaceutic adjuvant is excipient and binding agent; wherein the Aloe extract weight percentage is 2-70% in the pellet preparations, and the excipient weight percentage is 29-90%, and the percentage composition of binding agent is 1-8% "; Through this complete technical scheme, those skilled in the art just can prepare satisfactory pellet preparations according to the method for preparing 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.Micropill of the present invention and prior art Aloe extract compared with techniques, 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 that absorbs the organ surface distributed, bioavailability is improved and local excitation is less or eliminate, and selects for consumers in general provide more consumption.
(2) we carry out deep research to Aloe extract pellet preparations method for preparing on the basis of existing technology, and unexpected the discovery carried out sufficient pulverizing with Aloe extract and excipient; Be that micronization is pulverized, Aloe extract has been distributed in the excipient well, make particle diameter reach micro powder grade; Material with such is processed micropill, and in the process that discharges in vivo, main constituent can discharge rapidly along with the dissolving of excipient; And these article are made up of the little micropill unit of hundreds of grain, disperse area big in vivo, and the organ contacted specific surface area is also big with absorbing; Admittedly onset was rapid after these article of making were taken, bioavailability is high.
One, dissolution contrast experiment:
The micropill that micropill of the present invention can be processed rapid release or discharge at a slow speed through 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 processed positioned releasing micropills such as stomach dissolution type, enteric solubility.This micropill can encapsulatedly be processed capsule, or tabletting processes tablet, or makes other various packaged forms.We have carried out release in vitro contrast test (experimental technique is according to Pharmacopoeia of People's Republic of China version dissolution in 2010 check and analysis method) with these article and commercially available tablet and conventional capsule agent, and the result is following:
The conventional capsule agent (Hainan manufacturer production, lot number: 20091112) 30 minutes dissolution rates are 61% in gastric juice;
Tablet (Lianyun Harbour manufacturer production, lot number: 20100202) 30 minutes dissolution rates are 49% in gastric juice;
And these article 30 minutes dissolution rates in gastric juice promptly reach 90%.
Simultaneously, we can also through different coating materials, make product become the product of different sizes such as slow release, controlled release, enteric through micropill being carried out the technology of coating.
Therefore after we process slow-release micro-pill with these article, have 12 hours slow-release function, can effectively control the burst size of aloe saponin, safety, effectiveness are better; Slow-release micro-pill can make blood drug level reach curative effect concentration rapidly, and keeps steady, long valid density, and blood concentration fluctuation is little; These article have reduced the accumulated dose of taking than common dosage form simultaneously, have reduced the number of times of taking of consumer.We find that through the release in vitro simulation test its release profiles is obvious with these article, and when 2h, the release degree is more than 30%; During 5h, the release degree is more than 50%; During 8h, the release degree is more than 75%; During 12h, the release degree is more than 90%.
Have the consumer of stomach illness for some, for fear of the influence of product to stomach, these article are absorbed by the body better, we can also process enteric coated preparation with these article, promptly through micropill is carried out enteric coated technology, make product reach the purpose of enteric.We carry out the release in vitro simulation test with this enteric coated micropill and find; The micropill stripping that 2 hours have no in simulated gastric fluid; Outward appearance also has no variation, and when we were put into its taking-up in the simulated intestinal fluid dissolution test, its 30 minutes release degree had just reached more than 85%.
Two, pellet preparations research process:
Get Aloe extract, according to method [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc., the Chinese Medicine science and technology publishing house of existing document micropill preparation; 2006; 257-258] prepare, can not prepare qualified pellet preparations, therefore; We further study, and experimentize through following experimental technique:
1, the Aloe extract weight percentage is 2% in the pellet preparations, and the excipient weight percentage is 90%, and the percentage composition of binding agent is 8%.
2, the Aloe extract weight percentage is 70% in the pellet preparations, and the excipient weight percentage is 29%, and the percentage composition of binding agent is 1%.
3, the Aloe extract weight percentage is 50% in the pellet preparations, and the excipient weight percentage is 47%, and the percentage composition of binding agent is 3%.
4, the Aloe extract weight percentage is 60% in the pellet preparations, and the excipient weight percentage is 36%, and the percentage composition of binding agent is 4%.
5, the Aloe extract weight percentage is 10% in the pellet preparations, and the excipient weight percentage is 85%, and the percentage composition of binding agent is 5%.
Get the micropill of above-mentioned different experiments scheme,, detect according to the Pharmacopoeia of the People's Republic of China (version in 2010) appendix dissolution detection method.
Experimental result: the micropill of above-mentioned different schemes reaches more than 85% at 30 minutes dissolution, proves absolutely that the pellet preparations that the present invention prepares has scientific meaning.
Three, preparation embodiment:
Embodiment 1
A kind of Aloe extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Aloe extract weight percentage is 2% in the pellet preparations, and the excipient weight percentage is 90%, and the percentage composition of binding agent is 8%, prepares qualified pellet preparations.
Embodiment 2
A kind of Aloe extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Aloe extract weight percentage is 70% in the pellet preparations, and the excipient weight percentage is 29%, and the percentage composition of binding agent is 1%.
Embodiment 3
A kind of Aloe extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Aloe extract weight percentage is 10% in the pellet preparations, and the excipient weight percentage is 85.5%, and the percentage composition of binding agent is 4.5%.
Embodiment 4
A kind of Aloe extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Aloe extract weight percentage is 35% in the pellet preparations, and the excipient weight percentage is 62%, and the percentage composition of binding agent is 3%.
Embodiment 5
A kind of Aloe extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Aloe extract weight percentage is 20% in the pellet preparations, and the excipient weight percentage is 76%, and the percentage composition of binding agent is 4%.
Pellet preparations among the foregoing description 1-5 can be prepared into slow releasing preparation or enteric coated preparation according to demands of different.
The pellet preparations binding agent among the foregoing description 1-5 and the selection of excipient are selected to get final product according to the conventional adjuvant of pharmaceutics pellet preparations.
The method for preparing of micropill gets final product according to the method for preparing of existing document micropill among the foregoing description 1-5.
Embodiment 6
Get the raw material for standby of following prescription: Aloe extract 2 grams (2%), microcrystalline Cellulose 90 grams (90%), hydroxypropyl emthylcellulose 8 grams (8%);
Embodiment 7
Get the raw material for standby of following prescription: Aloe extract 70 grams (80%), sucrose, dextrin, starch, Celluloasun Microcrystallisatum, lactose and methylcellulose be totally 29 grams (29%), polyvinylpyrrolidone 1 gram (1%);
Embodiment 8
Get the raw material for standby of following prescription: Aloe extract 35 grams (35%), sucrose 60 grams (60%), cellulose family, resinae and saccharide be totally 5 grams (5%);
Embodiment 9
Get the raw material for standby of following prescription: Aloe extract 10 grams (10%), sodium carboxymethyl cellulose, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin be totally 85 grams (85%), resinae 5 grams (5%);
Embodiment 10
Get the raw material for standby of following prescription: Aloe extract 60 grams (60%), starch is totally 36 grams (36%), and cellulose family, resinae and saccharide be totally 4 grams (4%);
Embodiment 11
Get the raw material for standby of following prescription: Aloe extract 50g (50%), sucrose 48g (48%), polyvinylpyrrolidone 2g (2%);
Embodiment 12
Get the raw material for standby of following prescription: Aloe extract 65g (65%), starch 31.5g (31.5%), polyvinylpyrrolidone 3.5g (3.5%)
The foregoing description 1-12 can also can prepare according to following method according to the art methods preparation:
Embodiment 13
(1) Aloe extract of getting above-mentioned formula ratio adds excipient, is crushed to micronization rank, mixing with ball mill;
(2) binding agent is dissolved in 75% alcoholic solution;
(3) adopt method of extruding and kneading to pellets to process micropill.
Embodiment 14
(1) Aloe extract of getting above-mentioned formula ratio adds excipient, is crushed to micronization rank, mixing with ball mill;
(2) binding agent is soluble in water;
(3) adopt agitation procedure to process micropill.
Embodiment 15
(1) Aloe extract of getting above-mentioned formula ratio adds excipient, is crushed to micronization rank, mixing with ball mill;
(2) binding agent is dissolved in the dehydrated alcohol;
(3) adopt the centrifugal fluidized granulation method to process micropill.
Annotate: the present invention's concrete technical scheme required for protection is not limited to the concrete combination of the expressed technical scheme of the foregoing description.
Claims (7)
1. Aloe extract pellet preparations; It is to be prepared from Aloe extract and pharmaceutic adjuvant; It is characterized in that pharmaceutic adjuvant is excipient and binding agent; Wherein the Aloe extract weight percentage is 2-70% in the pellet preparations, and the excipient weight percentage is 29-90%, and the percentage composition of binding agent is 1-8%.
2. the slow release formulation of Aloe extract pellet preparations preparation according to claim 1.
3. the enteric dosage form of a kind of Aloe extract pellet preparations preparation according to claim 1.
4. according to described a kind of Aloe extract pellet preparations of claim 1, wherein said excipient is one or more the mixture that is selected from sucrose, dextrin, starch, Celluloasun Microcrystallisatum, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and the gelatin.
5. a kind of Aloe extract pellet preparations 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 method for preparing of each described a kind of Aloe extract pellet preparations of claim 1-5, the steps include:
(1) gets Aloe extract, add excipient, be crushed to micronized rank, mixing;
(2) in the solution in binding agent is water-soluble, dehydrated alcohol or the aquiferous ethanol;
(3) adopt the micropill forming technique to process micropill.
7. method for preparing 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.
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| CN2010105497012A CN102462796A (en) | 2010-11-19 | 2010-11-19 | Aloe extract pellet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2010105497012A CN102462796A (en) | 2010-11-19 | 2010-11-19 | Aloe extract pellet and preparation method thereof |
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| CN102462796A true CN102462796A (en) | 2012-05-23 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103054028A (en) * | 2013-01-11 | 2013-04-24 | 太原市澳意医药生物科技有限公司 | Aloe-dietary fibre convenient granules |
-
2010
- 2010-11-19 CN CN2010105497012A patent/CN102462796A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103054028A (en) * | 2013-01-11 | 2013-04-24 | 太原市澳意医药生物科技有限公司 | Aloe-dietary fibre convenient granules |
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Application publication date: 20120523 |