CN105497220A - Lemon peel pellet and preparation method thereof - Google Patents
Lemon peel pellet and preparation method thereof Download PDFInfo
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- CN105497220A CN105497220A CN201410501035.3A CN201410501035A CN105497220A CN 105497220 A CN105497220 A CN 105497220A CN 201410501035 A CN201410501035 A CN 201410501035A CN 105497220 A CN105497220 A CN 105497220A
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- citri limoniae
- fericarpium citri
- pellet preparations
- excipient
- micropill
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Abstract
The invention provides a lemon peel extract pellet preparation. The lemon peel extract pellet preparation is prepared from lemon peel extract and pharmaceutical adjuvant and is characterized in that the pharmaceutical adjuvant is composed of an excipient and an adhesive and the weight percentages of the lemon peel extract, the excipient and the adhesive are 10 to 30%, 65 to 85% and 1 to 5%, respectively. The pellet preparation provided by the invention has a high dissolution rate and high bioavailability; and the preparation method for the pellet preparation is simple, convenient and easily practicable.
Description
technical field:
The present invention relates to medicine food technical field, be specifically related to a kind of Fericarpium Citri Limoniae micropill and preparation method thereof.
background technology:
At present, about the product of Fericarpium Citri Limoniae deeply by the accreditation of consumers in general, be substantially common Tablet and Capsula agent, but above-mentioned dosage form to there is disintegration time long; A certain position point disintegrate in vivo, has certain zest to gastric mucosa; The 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 and discharge the controlled and compound recipe micro-pill type product that bioavailability is high in vivo, to meet the demand of consumers in general better.
The pharmaceutic adjuvants such as excipient, binding agent, porogen, disintegrating agent, 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 Fericarpium Citri Limoniae is provided.
Another object of the present invention is to the preparation method that a kind of Fericarpium Citri Limoniae 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 Fericarpium Citri Limoniae pellet preparations, be prepared from by Fericarpium Citri Limoniae, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, in its pellet preparations, Fericarpium Citri Limoniae weight percentage is 5 ~ 30%, the weight percentage of excipient is 75 ~ 90%, and the weight percentage of binding agent is 1 ~ 5%.
Slow release formulation prepared by above-mentioned Fericarpium Citri Limoniae pellet preparations.
Or enteric dosage form prepared by above-mentioned Fericarpium Citri Limoniae pellet preparations.
Wherein said excipient is the mixture of one or more be selected from sucrose, dextrin, starch, microcrystalline Cellulose, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin.
Wherein said binding agent is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, saccharide, 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 Fericarpium Citri Limoniae, add excipient, be crushed to micronized rank, mixing;
(2) in the solution in binding agent is water-soluble, dehydrated alcohol or aquiferous ethanol;
(3) micropill forming technique is adopted to make micropill.
Wherein said micropill forming technique comprises and is selected from agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method.
In conventional art, the degree of grinding of medical material or extract is coarse powder (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 dripping 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 ganoderma extract is ground into micropowder, its mean diameter is generally less than 10um, is mainly distributed in 1 ~ 20um.Method of micronization can adopt method of the prior art: physical pulverization method, such as mechanical impact crusher, jet mill, ball mill, vibromill, Ball-stirring mill, Raymond mill, high-pressure pulverizer etc.; Physical chemistry synthetic method, comprises spraying dry, original position micronization and supercritical fluid technology etc.Compared with conventional size reduction technology, this technique main advantage is: increase effective ingredient absorbance, improves bioavailability.The dissolution rate of effective ingredient is directly proportional to 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 thinner, then its specific surface area is larger, more contributes to the stripping of effective ingredient.According to the study, the optimal absorption granularity of the intestines and stomach to material grains is about 15um, and the granule of micron composition just reaches this optimal absorption fineness level; Because micron order effective ingredient obviously increases at gastrointestinal dissolubility, thus increase its bioavailability, 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: agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method etc.
Beneficial effect of the present invention is:
First, Fericarpium Citri Limoniae and excipient have been carried out sufficient pulverizing by us, Fericarpium Citri Limoniae 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, main constituent 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 surface area contacted with gastric juice is also large, admittedly make this product take rear onset rapidly, bioavailability 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 tabletting, 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 repeatability, adverse reaction rate is low; This product micropill increases at the area of gastrointestinal tract surface distributed, makes bioavailability 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 coating to micropill, by different coating materials, make product become the product of the different sizes such as slow release, 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 preparation by us simultaneously, namely by carrying out enteric coated technology to micropill, makes product reach the object of enteric.This enteric coated micropill is carried out the discovery of release in vitro simulation 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
Lemon peel extract 10g
Microcrystalline Cellulose 82g
Hydroxypropyl emthylcellulose 4g
Prepare pellet preparations in accordance with the following methods:
(1) get the Fericarpium Citri Limoniae of above-mentioned formula ratio, add microcrystalline Cellulose, be crushed to micronization rank with ball mill, mixing;
(2) hydroxypropyl emthylcellulose is dissolved in 75% alcoholic solution;
(3) method of extruding and kneading to pellets is adopted to make micropill.
embodiment 2
Get the raw material for standby of following formula
Lemon peel extract 15g
Starch 85g
Polyvinylpyrrolidone 5g
Prepare pellet preparations in accordance with the following methods:
(1) get the Fericarpium Citri Limoniae of above-mentioned formula ratio, add starch, be crushed to micronization rank with ball mill, mixing;
(2) polyvinyl pyrrolidone is soluble in water;
(3) agitation procedure is adopted to make micropill.
embodiment 3
Get the raw material for standby of following formula
Lemon peel extract 8g
Sucrose 49g
Starch 34g
Polyvinylpyrrolidone 4g
Prepare pellet preparations in accordance with the following methods:
(1) get the Fericarpium Citri Limoniae of above-mentioned formula ratio, add sugarcane sugar and starch, be crushed to micronization rank with ball mill, mixing;
(2) polyvinylpyrrolidone is dissolved in suitable quantity of water;
(3) centrifugal fluidized granulation method is adopted to make micropill.
Claims (7)
1. one kind is prepared from by lemon peel extract, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, in its pellet preparations, lemon peel extract weight percentage is 10 ~ 30%, the weight percentage of excipient is 65 ~ 85%, and the weight percentage of binding agent is 1 ~ 5%.
2. the slow release formulation prepared of a kind of Fericarpium Citri Limoniae pellet preparations according to claim 1.
3. the enteric dosage form prepared of a kind of Fericarpium Citri Limoniae pellet preparations according to claim 1.
4. a kind of Fericarpium Citri Limoniae 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 carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin.
5. a kind of Fericarpium Citri Limoniae pellet preparations according to claim 1, wherein said binding agent is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, saccharide, animal acid.
6. the preparation method of a kind of Fericarpium Citri Limoniae pellet preparations according to any one of Claims 1 to 5, the steps include:
(1) get Fericarpium Citri Limoniae, add excipient, be crushed to micronized rank, mixing;
(2) in the solution of binding agent is water-soluble, dehydrated alcohol or aquiferous 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 agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410501035.3A CN105497220A (en) | 2014-09-26 | 2014-09-26 | Lemon peel pellet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410501035.3A CN105497220A (en) | 2014-09-26 | 2014-09-26 | Lemon peel pellet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
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| CN105497220A true CN105497220A (en) | 2016-04-20 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410501035.3A Pending CN105497220A (en) | 2014-09-26 | 2014-09-26 | Lemon peel pellet and preparation method thereof |
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| CN (1) | CN105497220A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110907604A (en) * | 2019-12-06 | 2020-03-24 | 浙江华康药业股份有限公司 | Method for improving sensory attributes of sugar alcohol substances and application thereof |
-
2014
- 2014-09-26 CN CN201410501035.3A patent/CN105497220A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110907604A (en) * | 2019-12-06 | 2020-03-24 | 浙江华康药业股份有限公司 | Method for improving sensory attributes of sugar alcohol substances and application thereof |
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Application publication date: 20160420 |