CN102462744A - Cortex moutan extract pellet and preparation method thereof - Google Patents
Cortex moutan extract pellet and preparation method thereof Download PDFInfo
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- CN102462744A CN102462744A CN2010105495144A CN201010549514A CN102462744A CN 102462744 A CN102462744 A CN 102462744A CN 2010105495144 A CN2010105495144 A CN 2010105495144A CN 201010549514 A CN201010549514 A CN 201010549514A CN 102462744 A CN102462744 A CN 102462744A
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- cortex moutan
- moutan extract
- excipient
- pellet preparations
- binding agent
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Abstract
The invention provides a cortex moutan extract pellet preparation which is prepared from a cortex moutan extract and a pharmaceutical adjuvant material and is characterized in that the pharmaceutical adjuvant material contains an excipient and an adhesive; in the pellet, the weight percent of the cortex moutan extract is from 1% to 45%; the weight percent of the excipient is from 50% to 98%; and the weight percent of the adhesive is from 1% to 5%. The pellet can be prepared into a slow-release preparation or an enteric preparation as required. Indicated by a pharmaceutical experiment, the pellet provided by the invention has the functions of analgesia, antibiosis, anti-inflammation and the like.
Description
Technical field
The present invention relates to the medicine food technical field, be specifically related to micropill that a kind of Cortex Moutan extract processes and preparation method thereof.
Background technology
Cortex Moutan extract is a ranunculaceae peony dry root peel extract.Its main component is a paeonol.Originate in ground such as Anhui, Shandong.Cortex Moutan has multiple pharmacological effect such as analgesia, hemostasis, antiinflammatory, antibiotic, blood pressure lowering; Paeonol is external to have the obvious suppression effect to multiple human pathogen.
The product of Cortex Moutan extract is approved by consumers in general progressively that these products are common tablet and capsule basically, 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 Cortex Moutan 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 Cortex Moutan extract weight percentage is 1%-45% in the pellet preparations; the excipient weight percentage is 50%-98%, and the percentage composition of binding agent is 1%-5% "; 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 Cortex Moutan extract pellet preparations method for preparing on the basis of existing technology, and unexpected the discovery carried out sufficient pulverizing with Cortex Moutan extract and excipient; Be that micronization is pulverized, Cortex Moutan 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 Cortex Moutan 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 Cortex Moutan extract pellet preparations, this method is simple, convenient, easy operating.
Cortex Moutan 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 Cortex Moutan extract pellet preparations; It is to be prepared from Cortex Moutan extract and pharmaceutic adjuvant; It is characterized in that pharmaceutic adjuvant is excipient and binding agent; Wherein the Cortex Moutan extract weight percentage is 1-45% in the pellet preparations, and the excipient weight percentage is 50-98%, and the percentage composition of binding agent is 1-5%.
The slow release formulation of above-mentioned Cortex Moutan extract pellet preparations preparation.
Or the enteric dosage form of above-mentioned Cortex Moutan 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 Cortex Moutan extract pellet preparations the steps include:
(1) gets Cortex Moutan 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 Cortex Moutan 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 Cortex Moutan extract to be prepared into the technology of pellet preparations, we are through carrying out deep analysis to Cortex Moutan 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 Cortex Moutan extract weight percentage is 1-45% in the pellet preparations, and the excipient weight percentage is 50-98%, and the percentage composition of binding agent is 1-5% "; 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 Cortex Moutan 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 Cortex Moutan extract pellet preparations method for preparing on the basis of existing technology, and unexpected the discovery carried out sufficient pulverizing with Cortex Moutan extract and excipient; Be that micronization is pulverized, Cortex Moutan 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 (the Shandong manufacturer production, lot number: 20100302) 30 minutes dissolution rates are 47% in gastric juice;
Tablet (Liaoning manufacturer production, lot number: 091109) 30 minutes dissolution rates are 59% 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 Cortex Moutan 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 70%; 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 Cortex Moutan 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 Cortex Moutan extract weight percentage is 1% in the pellet preparations, and the excipient weight percentage is 98%, and the percentage composition of binding agent is 1%.
2, the Cortex Moutan extract weight percentage is 45% in the pellet preparations, and the excipient weight percentage is 50%, and the percentage composition of binding agent is 5%.
3, the Cortex Moutan extract weight percentage is 5% in the pellet preparations, and the excipient weight percentage is 92%, and the percentage composition of binding agent is 3%.
4, the Cortex Moutan extract weight percentage is 25% in the pellet preparations, and the excipient weight percentage is 71%, and the percentage composition of binding agent is 4%.
5, the Cortex Moutan extract weight percentage is 40% in the pellet preparations, and the excipient weight percentage is 58%, and the percentage composition of binding agent is 2%.
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 Cortex Moutan extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Cortex Moutan extract weight percentage is 1% in the pellet preparations, and the excipient weight percentage is 98%, and the percentage composition of binding agent is 1%, prepares qualified pellet preparations.
Embodiment 2
A kind of Cortex Moutan extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Cortex Moutan extract weight percentage is 45% in the pellet preparations, and the excipient weight percentage is 50%, and the percentage composition of binding agent is 5%.
Embodiment 3
A kind of Cortex Moutan extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Cortex Moutan extract weight percentage is 9% in the pellet preparations, and the excipient weight percentage is 89.5%, and the percentage composition of binding agent is 1.5%.
Embodiment 4
A kind of Cortex Moutan extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Cortex Moutan extract weight percentage is 22% in the pellet preparations, and the excipient weight percentage is 75%, and the percentage composition of binding agent is 3%.
Embodiment 5
A kind of Cortex Moutan extract pellet preparations, pharmaceutic adjuvant are excipient and binding agent, and wherein the Cortex Moutan extract weight percentage is 40% in the pellet preparations, and the excipient weight percentage is 56%, 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: Cortex Moutan extract 1 gram (1%), microcrystalline Cellulose 98 grams (98%), hydroxypropyl emthylcellulose 1 gram (1%);
Embodiment 7
Get the raw material for standby of following prescription: Cortex Moutan extract 45 grams (45%), sucrose, dextrin, starch, Celluloasun Microcrystallisatum, lactose and methylcellulose be totally 50 grams (50%), polyvinylpyrrolidone 5 grams (5%);
Embodiment 8
Get the raw material for standby of following prescription: Cortex Moutan extract 12 grams (12%), sucrose 85 grams (85%), cellulose family, resinae and saccharide be totally 3 grams (3%);
Embodiment 9
Get the raw material for standby of following prescription: Cortex Moutan extract 20 grams (20%), sodium carboxymethyl cellulose, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin be totally 78 grams (78%), resinae 2 grams (2%);
Embodiment 10
Get the raw material for standby of following prescription: Cortex Moutan extract 28 grams (28%), starch is totally 68 grams (68%), and cellulose family, resinae and saccharide be totally 4 grams (4%);
Embodiment 11
Get the raw material for standby of following prescription: Cortex Moutan extract 34g (34%), sucrose 64g (64%), polyvinylpyrrolidone 2g (2%);
Embodiment 12
Get the raw material for standby of following prescription: Cortex Moutan extract 40g (40%), starch 57.5g (57.5%), polyvinylpyrrolidone 2.5g (2.5%)
The foregoing description 1-12 can also can prepare according to following method according to the art methods preparation:
Embodiment 13
(1) Cortex Moutan 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) Cortex Moutan 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) Cortex Moutan 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. Cortex Moutan extract pellet preparations; It is to be prepared from Cortex Moutan extract and pharmaceutic adjuvant; It is characterized in that pharmaceutic adjuvant is excipient and binding agent; Wherein the Cortex Moutan extract weight percentage is 1-45% in the pellet preparations, and the excipient weight percentage is 50-98%, and the percentage composition of binding agent is 1-5%.
2. the slow release formulation of Cortex Moutan extract pellet preparations preparation according to claim 1.
3. the enteric dosage form of a kind of Cortex Moutan extract pellet preparations preparation according to claim 1.
4. according to described a kind of Cortex Moutan 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 Cortex Moutan 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 Cortex Moutan extract pellet preparations of claim 1-5, the steps include:
(1) gets Cortex Moutan 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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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109464477A (en) * | 2018-11-15 | 2019-03-15 | 罗莱生活科技股份有限公司 | A kind of pomegranate rind extract pellet preparations and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109464477A (en) * | 2018-11-15 | 2019-03-15 | 罗莱生活科技股份有限公司 | A kind of pomegranate rind extract pellet preparations and preparation method thereof |
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Application publication date: 20120523 |