CN103845293A - Lutein pellet and preparation method thereof - Google Patents
Lutein pellet and preparation method thereof Download PDFInfo
- Publication number
- CN103845293A CN103845293A CN201210519053.5A CN201210519053A CN103845293A CN 103845293 A CN103845293 A CN 103845293A CN 201210519053 A CN201210519053 A CN 201210519053A CN 103845293 A CN103845293 A CN 103845293A
- Authority
- CN
- China
- Prior art keywords
- lutein
- preparation
- excipient
- micropill
- micropills
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 38
- 239000008188 pellet Substances 0.000 title claims abstract description 21
- KBPHJBAIARWVSC-XQIHNALSSA-N trans-lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C KBPHJBAIARWVSC-XQIHNALSSA-N 0.000 title claims abstract description 21
- 235000012680 lutein Nutrition 0.000 title claims abstract description 20
- 239000001656 lutein Substances 0.000 title claims abstract description 20
- KBPHJBAIARWVSC-RGZFRNHPSA-N lutein Chemical compound C([C@H](O)CC=1C)C(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\[C@H]1C(C)=C[C@H](O)CC1(C)C KBPHJBAIARWVSC-RGZFRNHPSA-N 0.000 title claims abstract description 20
- 229960005375 lutein Drugs 0.000 title claims abstract description 20
- ORAKUVXRZWMARG-WZLJTJAWSA-N lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C ORAKUVXRZWMARG-WZLJTJAWSA-N 0.000 title claims abstract description 20
- FJHBOVDFOQMZRV-XQIHNALSSA-N xanthophyll Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C=C(C)C(O)CC2(C)C FJHBOVDFOQMZRV-XQIHNALSSA-N 0.000 title claims abstract description 20
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 30
- 238000000034 method Methods 0.000 claims description 35
- 239000011230 binding agent Substances 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 10
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 8
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- 239000002552 dosage form Substances 0.000 claims description 5
- 238000013019 agitation Methods 0.000 claims description 4
- 238000005469 granulation Methods 0.000 claims description 4
- 230000003179 granulation Effects 0.000 claims description 4
- -1 hydroxypropyl Chemical group 0.000 claims description 4
- 238000004898 kneading Methods 0.000 claims description 4
- 229930006000 Sucrose Natural products 0.000 claims description 3
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 3
- 239000005720 sucrose Substances 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- 239000004925 Acrylic resin Substances 0.000 claims description 2
- 229920000178 Acrylic resin Polymers 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
- 239000004375 Dextrin Substances 0.000 claims description 2
- 229920001353 Dextrin Polymers 0.000 claims description 2
- 239000001856 Ethyl cellulose Substances 0.000 claims description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- 241001465754 Metazoa Species 0.000 claims description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 150000001720 carbohydrates Chemical class 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 235000010980 cellulose Nutrition 0.000 claims description 2
- 229960000935 dehydrated alcohol Drugs 0.000 claims description 2
- 235000019425 dextrin Nutrition 0.000 claims description 2
- 229960004756 ethanol Drugs 0.000 claims description 2
- 229920001249 ethyl cellulose Polymers 0.000 claims description 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 2
- 239000003232 water-soluble binding agent Substances 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 abstract description 8
- 239000000853 adhesive Substances 0.000 abstract 2
- 230000001070 adhesive effect Effects 0.000 abstract 2
- 239000000047 product Substances 0.000 description 22
- 238000005516 engineering process Methods 0.000 description 9
- 239000002245 particle Substances 0.000 description 9
- 239000000843 powder Substances 0.000 description 7
- 238000001727 in vivo Methods 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 239000002775 capsule Substances 0.000 description 4
- 210000004051 gastric juice Anatomy 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 239000006187 pill Substances 0.000 description 3
- 238000010298 pulverizing process Methods 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- 210000002784 stomach Anatomy 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000000470 constituent Substances 0.000 description 2
- 239000003405 delayed action preparation Substances 0.000 description 2
- 238000007599 discharging Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000049 pigment Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 210000001525 retina Anatomy 0.000 description 2
- 238000004088 simulation Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- JKQXZKUSFCKOGQ-JLGXGRJMSA-N (3R,3'R)-beta,beta-carotene-3,3'-diol Chemical compound C([C@H](O)CC=1C)C(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)C[C@@H](O)CC1(C)C JKQXZKUSFCKOGQ-JLGXGRJMSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 241000459479 Capsula Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 240000000111 Saccharum officinarum Species 0.000 description 1
- 235000007201 Saccharum officinarum Nutrition 0.000 description 1
- 208000034189 Sclerosis Diseases 0.000 description 1
- JKQXZKUSFCKOGQ-LQFQNGICSA-N Z-zeaxanthin Natural products C([C@H](O)CC=1C)C(C)(C)C=1C=CC(C)=CC=CC(C)=CC=CC=C(C)C=CC=C(C)C=CC1=C(C)C[C@@H](O)CC1(C)C JKQXZKUSFCKOGQ-LQFQNGICSA-N 0.000 description 1
- QOPRSMDTRDMBNK-RNUUUQFGSA-N Zeaxanthin Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCC(O)C1(C)C)C=CC=C(/C)C=CC2=C(C)CC(O)CC2(C)C QOPRSMDTRDMBNK-RNUUUQFGSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- JKQXZKUSFCKOGQ-LOFNIBRQSA-N all-trans-Zeaxanthin Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2=C(C)CC(O)CC2(C)C JKQXZKUSFCKOGQ-LOFNIBRQSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000001156 gastric mucosa Anatomy 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 210000002189 macula lutea Anatomy 0.000 description 1
- 239000012567 medical material Substances 0.000 description 1
- 230000004089 microcirculation Effects 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 239000003361 porogen Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000009978 visual deterioration Effects 0.000 description 1
- 235000010930 zeaxanthin Nutrition 0.000 description 1
- 239000001775 zeaxanthin Substances 0.000 description 1
- 229940043269 zeaxanthin Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention provides a lutein pellet, which is prepared from lutein and a pharmaceutic adjuvant. The lutein pellet is characterized in that the pharmaceutic adjuvant is an excipient and an adhesive, wherein the pellet preparation contains 5-20% of lutein, 70-85% of excipient and 1-5% of adhesive. The lutein pellet disclosed by the invention is high in dissolution rate, and high in bioavailability, and the preparation method 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 phylloxanthin makes and preparation method thereof.
Background technology
Phylloxanthin and zeaxanthin are the key components that forms the plant pigment such as vegetable, fruit, flowers, are also the main pigments that forms human eye retina's macular region.The phylloxanthin that the mankind's eyes contain a large amount, this element is that human body cannot be manufactured, and must supplement by taking in phylloxanthin, if lack this element, eyes will be blind.Foreign study shows: phylloxanthin can prevent eyes photic damage, prevent because phylloxanthin lacks the visual deterioration and the blind disease that cause, and because of body aging cause cardiovascula sclerosis, coronary heart disease and tumor disease.It is the chief component material that eye retina, macula lutea can not lack; Prevent physiological structure and the function variation of eyes; Be a kind of potent antioxidant, absorb ultraviolet, blue light, dissolve eyes light poisoning at all; There is vasodilation function, improve optical fundus blood microcirculation, promote nutrient substance supply.
At present, be deeply subject to consumers in general's approval about the product of phylloxanthin, these products are common Tablet and Capsula agent substantially, but above-mentioned dosage form exists 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 discharged in vivo micro-pill type product controlled and that bioavailability is high, to meet better consumers in general's demand.
In the preparation process of pellet preparations, generally to add 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., Chinese Medicine science and technology publishing house, 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
For these reasons, we carry out deep analysis by the physics and chemistry character to phylloxanthin, take dissolution as index, by the test of science, determine that pharmaceutic adjuvant is excipient and binding agent, and excipient and binding agent are carried out to determining of weight percentage: " pharmaceutic adjuvant is excipient and binding agent, and its pellet preparations Lutein weight percentage is 5～20%; the weight percentage of excipient is 70～85%, and the weight percentage of binding agent is 1～5% "; By this complete technical scheme, those skilled in the art, according to the preparation method of the micropill of prior art, just can prepare satisfactory pellet preparations; Above-mentioned pellet preparations can be prepared into satisfactory slow releasing preparation or enteric coated preparation, be conducive to user's compliance.Phylloxanthin and excipient have been carried out sufficient pulverizing by we, be that micronization is pulverized, phylloxanthin has been distributed in excipient well, make particle diameter reach micro powder grade, make micropill with such material, in the process discharging in vivo, 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 in vivo area large, the specific surface area that contacts of organ is also large with absorbing, therefore it is rapid to make this product take rear onset, bioavailability is high.
The object of the invention is, in order to overcome the problems of the prior art, provides a kind of novel formulation of phylloxanthin---pellet preparations.
Another object of the present invention is to provide a kind of preparation method of lutein micropills preparation, the method is simple, convenient, easy operating.
Phylloxanthin of the present invention can be extract, can be also effective ingredient, prepares according to existing literature method or patented method.
The object of the invention is to be achieved through the following technical solutions:
A kind of lutein micropills preparation, be prepared from by phylloxanthin, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, its pellet preparations Lutein weight percentage is 5～20%, the weight percentage of excipient is 70～85%, and the weight percentage of binding agent is 1～5%.
Slow release formulation prepared by above-mentioned lutein micropills preparation.
Or the enteric dosage form prepared of above-mentioned lutein micropills preparation.
Wherein said excipient is one or more the mixture being 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 one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, saccharide, animal acid.
Pellet preparations of the present invention can, according to technique scheme, be prepared with the preparation method of prior art pellet preparations, also can be prepared by the following method:
(1) get phylloxanthin, add excipient, be crushed to micronized rank, mix;
(2) by the solution in water-soluble binding agent, dehydrated alcohol or aquiferous ethanol;
(3) adopt 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 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), 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 adopts micronization technology that phylloxanthin 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, stirring mill, Raymond mill, high-pressure pulverizer etc.; Physical chemistry synthetic method, comprising that spraying is dry, original position micronization and supercritical fluid technology etc.Compared with traditional crushing technology, this technique main advantage is: increase effective ingredient absorbance, improve 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, and its specific surface area is larger, more contributes to the stripping of effective ingredient.According to the study, the intestines and stomach is 15um left and right to the optimal absorption granularity of material grains, and the granule of micron composition has just reached this optimal absorption fineness level; Because micron order effective ingredient obviously increases at gastrointestinal dissolubility, thereby increase its bioavailability, accelerated 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, phylloxanthin and excipient have been carried out sufficient pulverizing by we, phylloxanthin has been distributed in excipient well, and particle diameter reached micro powder grade, make micropill with such material, in the process discharging 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 little micropill unit of hundreds of grain, disperse in vivo area large, the specific surface area contacting with gastric juice is also large, admittedly it is rapid to make this product take rear onset, bioavailability is high.
The micropill that micropill of the present invention can be made quick release or be discharged 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 is made to the 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 good curative effect repeatability, 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.
This product and commercially available tablet and conventional capsule agent have been carried out release in vitro contrast test (experimental technique is according to Pharmacopoeia of People's Republic of China version dissolution determination method in 2005) by we, and result is as follows:
Conventional capsule agent (Xi'an manufacturer production, lot number: 100203) 30 minutes dissolution rates are 62% in gastric juice;
Tablet (Guangzhou manufacturer production, lot number: 110205) 30 minutes dissolution rates are 60% in gastric juice;
And this product 25 minutes dissolution rates in gastric juice reach 92%.
Meanwhile, we can also, by micropill being carried out to the technology of coating, by different coating materials, make product become the product of the different sizes such as slow release, controlled release, enteric.
We make this product after slow-release micro-pill, have the slow-release function of 12 hours, therefore can effectively control the burst size of phylloxanthin, and safety, effectiveness are better; Slow-release micro-pill can make blood drug level reach rapidly curative effect concentration, and maintains steady, long valid density, and 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 this product by release in vitro simulation test, its release profiles is obvious, and in the time of 2h, release is more than 25%; When 5h, release is more than 50%; When 8h, release is more than 75%; When 12h, release is more than 95%.
The consumer that has gastric lesions for some, the impact for fear of product on stomach makes this product be absorbed by the body better simultaneously, and we can also make enteric coated preparation by this product, by micropill is carried out to enteric coated technology, make product reach the object of enteric.This enteric coated micropill is carried out the discovery of release in vitro simulation test by we, micropill in simulated gastric fluid 2 hours without any stripping, outward appearance is also without any variation, and in the time that we are put into its taking-up in simulated intestinal fluid dissolution test, its 30 minutes releases have just reached more than 90%.
The specific embodiment
embodiment 1
Get the raw material for standby of following formula
| Phylloxanthin | 15g(is in sterling) |
| Celluloasun Microcrystallisatum | 81 |
| Hydroxypropyl emthylcellulose | 4g |
Prepare in accordance with the following methods pellet preparations:
(1) phylloxanthin of getting above-mentioned formula ratio adds Celluloasun Microcrystallisatum, is crushed to micronization rank with ball mill, mixes;
(2) hydroxypropyl emthylcellulose is dissolved in to 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 formula
| Phylloxanthin | 10g(is in sterling) |
| Starch | 85g |
| Polyvinylpyrrolidone | 5g |
Prepare in accordance with the following methods pellet preparations:
(1) phylloxanthin of getting above-mentioned formula ratio adds starch, is crushed to micronization rank with ball mill, mixes;
(2) polyvinyl pyrrolidone is soluble in water;
(3) adopt agitation procedure to make micropill.
embodiment 3
Get the raw material for standby of following formula
| Phylloxanthin | 8g(is in sterling) |
| Sucrose | 54 |
| Starch | 34g |
| Polyvinylpyrrolidone | 4g |
Prepare in accordance with the following methods pellet preparations:
(1) phylloxanthin of getting above-mentioned formula ratio adds sugarcane sugar and starch, is crushed to micronization rank with ball mill, mixes;
(2) polyvinylpyrrolidone is dissolved in suitable quantity of water;
(3) adopt centrifugal fluidized granulation method to make micropill.
Claims (7)
1. a lutein micropills preparation, be prepared from by phylloxanthin, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, its pellet preparations Lutein weight percentage is 5～20%, the weight percentage of excipient is 70～85%, and the weight percentage of binding agent is 1～5%.
2. the slow release formulation that prepared by a kind of lutein micropills preparation according to claim 1.
3. the enteric dosage form that prepared by a kind of lutein micropills preparation according to claim 1.
4. a kind of lutein micropills preparation according to claim 1, wherein said excipient is one or more the mixture being 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 lutein micropills preparation according to claim 1, wherein said binding agent is one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, saccharide, animal acid.
6. according to the preparation method of a kind of lutein micropills preparation described in claim 1～5 any one, the steps include:
(1) get phylloxanthin, add excipient, be crushed to micronized rank, mix;
(2) by the solution of water-soluble binding agent, dehydrated alcohol or aquiferous ethanol;
(3) adopt micropill forming technique to make micropill.
7. preparation method according to claim 6, 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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210519053.5A CN103845293A (en) | 2012-12-06 | 2012-12-06 | Lutein pellet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210519053.5A CN103845293A (en) | 2012-12-06 | 2012-12-06 | Lutein pellet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103845293A true CN103845293A (en) | 2014-06-11 |
Family
ID=50853702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210519053.5A Pending CN103845293A (en) | 2012-12-06 | 2012-12-06 | Lutein pellet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103845293A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN114957072A (en) * | 2021-02-25 | 2022-08-30 | 内蒙古昶辉生物科技股份有限公司 | Method for preparing zeaxanthin and zeaxanthin pellet from marigold ointment |
-
2012
- 2012-12-06 CN CN201210519053.5A patent/CN103845293A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN114957072A (en) * | 2021-02-25 | 2022-08-30 | 内蒙古昶辉生物科技股份有限公司 | Method for preparing zeaxanthin and zeaxanthin pellet from marigold ointment |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101703540A (en) | Celeryseed extract pellets and preparation method thereof | |
| CN103845293A (en) | Lutein pellet and preparation method thereof | |
| CN101214322A (en) | Grape seed extract micropills and preparation thereof | |
| CN101444489A (en) | Astragalus polyose pellet and preparation method thereof | |
| CN101444558A (en) | Desertliving cistanche herb extract pellet and preparation method thereof | |
| CN101703475A (en) | Chondroitin sulfate pellet and preparation method thereof | |
| CN105435144A (en) | Raw ginger micro-pill and preparation method thereof | |
| CN105560603A (en) | Novel tea polyphenol spherical particles | |
| CN101703532A (en) | Ganoderan polysaccharide pellet and preparation method thereof | |
| CN101219126A (en) | Beta-carotene pellet and method for preparing the same | |
| CN101214232A (en) | Lutein micropills and preparation thereof | |
| CN104666367A (en) | Compound lucid ganoderma extract pellets and preparation method thereof | |
| CN101455679A (en) | Donkey-hide gelatin micro-pills and preparation method thereof | |
| CN104666355A (en) | Propolis pellets and preparation method thereof | |
| CN104666486A (en) | Compound seabuckthorn extract pellets and preparation method thereof | |
| CN102462717A (en) | American ginseng extract pellet and preparation method thereof | |
| CN105497220A (en) | Lemon peel pellet and preparation method thereof | |
| CN103859384A (en) | Compound grape seed extract pellets and preparation method thereof | |
| CN101703477A (en) | Coenzyme Q10 mini-pill and preparation method thereof | |
| CN101444547A (en) | Sea buckthorn extract pellet and preparation method thereof | |
| CN101703476A (en) | Zeaxanthin pellets and preparation method thereof | |
| CN104664399A (en) | Compound hyaluronic acid pellet and preparation method thereof | |
| CN105434570A (en) | Compound spina date seed extract-containing micro-pill and preparing method thereof | |
| CN104664397A (en) | Micro-pills containing apple polyphenol, and preparation method of micro-pills | |
| CN105520966A (en) | Hericium erinaceus micro-pills and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20140611 |