CN103948621A - Lentinan oral preparation and preparation method thereof - Google Patents
Lentinan oral preparation and preparation method thereof Download PDFInfo
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- CN103948621A CN103948621A CN201410169024.XA CN201410169024A CN103948621A CN 103948621 A CN103948621 A CN 103948621A CN 201410169024 A CN201410169024 A CN 201410169024A CN 103948621 A CN103948621 A CN 103948621A
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- lentinan
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- peroral dosage
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- 229920001491 Lentinan Polymers 0.000 title claims abstract description 170
- 229940115286 lentinan Drugs 0.000 title claims abstract description 170
- 238000002360 preparation method Methods 0.000 title claims abstract description 30
- 238000004519 manufacturing process Methods 0.000 claims abstract description 11
- 239000002552 dosage form Substances 0.000 claims description 42
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 19
- 239000007788 liquid Substances 0.000 claims description 14
- 238000002156 mixing Methods 0.000 claims description 14
- 238000003756 stirring Methods 0.000 claims description 14
- 239000008187 granular material Substances 0.000 claims description 13
- 238000010521 absorption reaction Methods 0.000 claims description 11
- IQFVPQOLBLOTPF-HKXUKFGYSA-L congo red Chemical compound [Na+].[Na+].C1=CC=CC2=C(N)C(/N=N/C3=CC=C(C=C3)C3=CC=C(C=C3)/N=N/C3=C(C4=CC=CC=C4C(=C3)S([O-])(=O)=O)N)=CC(S([O-])(=O)=O)=C21 IQFVPQOLBLOTPF-HKXUKFGYSA-L 0.000 claims description 10
- 240000000599 Lentinula edodes Species 0.000 claims description 8
- 239000002775 capsule Substances 0.000 claims description 8
- 239000002994 raw material Substances 0.000 claims description 7
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 6
- 238000013019 agitation Methods 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 239000008103 glucose Substances 0.000 claims description 6
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 5
- 229930195725 Mannitol Natural products 0.000 claims description 5
- 239000000594 mannitol Substances 0.000 claims description 5
- 235000010355 mannitol Nutrition 0.000 claims description 5
- 239000004375 Dextrin Substances 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- 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 4
- 229930006000 Sucrose Natural products 0.000 claims description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 4
- 235000019425 dextrin Nutrition 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000000945 filler Substances 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 239000007909 solid dosage form Substances 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 239000005720 sucrose Substances 0.000 claims description 4
- 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 3
- 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 3
- 229910002092 carbon dioxide Inorganic materials 0.000 claims description 3
- 239000001569 carbon dioxide Substances 0.000 claims description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 3
- 239000008101 lactose Substances 0.000 claims description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 3
- 239000003826 tablet Substances 0.000 claims description 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 239000000796 flavoring agent Substances 0.000 claims description 2
- 235000013355 food flavoring agent Nutrition 0.000 claims description 2
- 235000001727 glucose Nutrition 0.000 claims description 2
- 238000010438 heat treatment Methods 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 235000010356 sorbitol Nutrition 0.000 claims description 2
- 239000007924 injection Substances 0.000 abstract description 27
- 238000002347 injection Methods 0.000 abstract description 27
- 206010028980 Neoplasm Diseases 0.000 abstract description 13
- 230000000694 effects Effects 0.000 abstract description 13
- 230000002708 enhancing effect Effects 0.000 abstract description 2
- 230000002519 immonomodulatory effect Effects 0.000 abstract description 2
- 239000003814 drug Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 8
- 230000003442 weekly effect Effects 0.000 description 8
- 241000699670 Mus sp. Species 0.000 description 7
- 230000000259 anti-tumor effect Effects 0.000 description 7
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 6
- 230000035622 drinking Effects 0.000 description 6
- 230000003203 everyday effect Effects 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000002245 particle Substances 0.000 description 6
- 235000013361 beverage Nutrition 0.000 description 5
- 230000000857 drug effect Effects 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 230000000968 intestinal effect Effects 0.000 description 3
- 238000011068 loading method Methods 0.000 description 3
- 229940100691 oral capsule Drugs 0.000 description 3
- 239000007935 oral tablet Substances 0.000 description 3
- 229940096978 oral tablet Drugs 0.000 description 3
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 3
- 235000017557 sodium bicarbonate Nutrition 0.000 description 3
- UIIMBOGNXHQVGW-UHFFFAOYSA-N sodium;hydron;carbonate Chemical compound [Na+].OC(O)=O UIIMBOGNXHQVGW-UHFFFAOYSA-N 0.000 description 3
- 230000001954 sterilising effect Effects 0.000 description 3
- 235000001674 Agaricus brunnescens Nutrition 0.000 description 2
- 235000001715 Lentinula edodes Nutrition 0.000 description 2
- 238000002512 chemotherapy Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 238000011049 filling Methods 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 239000002955 immunomodulating agent Substances 0.000 description 2
- 229940121354 immunomodulator Drugs 0.000 description 2
- 230000002584 immunomodulator Effects 0.000 description 2
- 230000007365 immunoregulation Effects 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000012856 packing Methods 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 238000001959 radiotherapy Methods 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- 230000002588 toxic effect Effects 0.000 description 2
- 206010003445 Ascites Diseases 0.000 description 1
- 102000005853 Clathrin Human genes 0.000 description 1
- 108010019874 Clathrin Proteins 0.000 description 1
- 238000012449 Kunming mouse Methods 0.000 description 1
- 239000005434 MCC/mannitol excipient Substances 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 230000000118 anti-neoplastic effect Effects 0.000 description 1
- 238000000149 argon plasma sintering Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229930193282 clathrin Natural products 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 238000000151 deposition Methods 0.000 description 1
- 210000002249 digestive system Anatomy 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000000686 essence Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000005243 fluidization Methods 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 238000000892 gravimetry Methods 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 238000009863 impact test Methods 0.000 description 1
- 238000002329 infrared spectrum Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 210000005075 mammary gland Anatomy 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a lentinan oral preparation, which is characterized by comprising lentinan, wherein the lentinan is a pure beta triple helix-forming single lentinan with specific infrared features, weight-average molecular weight of 400,000-800,000 and lentinan content of more than 94wt%. The lentinan oral preparation has effects on resisting tumors and enhancing immunomodulatory, being the same as a lentinan injection preparation, and the preparation method of the oral preparation is simpler and more convenient, shorter in production cycle, lower in cost and wider in application than that of the injection preparation.
Description
Technical field
The present invention relates to peroral dosage form of a kind of lentinan and preparation method thereof, it belongs to field of biology, also belongs to pharmacy dosage form research.
Background technology
As everyone knows, pure β, triple helical configuration, single lentinan are to be widely used in the radiotherapy of tumor and a kind of immunomodulator of chemotherapy.For tumors such as digestive system and lung, mammary gland, have and heighten the effect of a treatment significantly and reduce toxic and side effects.Lentinan injection (lentinan) preparation process is complicated, cycle is tediously long, and manufacturing cost is high, and especially injection is unique route of administration, it is had the tumor patient of various diseases (as heart, liver, kidney) to bring Operative risk and trouble, has also increased treatment cost.
Lentinan (C
6h
10o
5)
npure β, triple helical configuration, the single polysaccharide extracting from mushroom fruiting body.At present, it is that everybody generally admits: effective medicine with antitumor, enhancing immunoloregulation function, but in route of administration, there is different cognitions, a kind of viewpoint is to think to form β, triple helical configuration lentinan, its molecular weight is excessive, can not is absorbed by the body and be arrived whole body everywhere by human body intestinal canal cell.What can be passed through by human body intestinal canal Cell uptake is that molecular weight is little, can not form the lentinan of β, triple helical configuration, therefore, does not also possess activity and forms drug effect.Only have weight average molecular weight is controlled to 40～800,000 lentinan makes injection, by injection, with blood, reach whole body everywhere, just form drug effect.And now, along with many scientists study discovery: many Chinese herbal medicine extracting polysaccharide out, likely by Clathrin albumen by the complete absorption of human body, this oral absorption and drug effect that is found to be lentinan provides new scientific basis.Chinese patent CN101244093 has proposed a kind of oral liquid that contains lentinan, the lentinan molecular weight ranges that it contains is 2-100 ten thousand dalton, although this shiitake fungus polyoses oral liquid produces effect, but its oral utilization ratio is not high, reach the dose that satisfied therapeutic effect needs larger.
Summary of the invention
The object of this invention is to provide peroral dosage form of a kind of lentinan with high oral utilization rate and preparation method thereof, the lentinan injection of itself and anti-tumor activity has equal effect.
In order to achieve the above object, the peroral dosage form that the invention provides a kind of lentinan, is characterized in that, containing weight average molecular weight is 400,000～800,000 pure β, the lentinan of triple helical configuration, its purity is > 96wt%, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.
Indication lentinan molecular formula of the present invention is suc as formula shown in (1):
Preferably, the Congo red of described lentinan reacts be positive (+).
The present invention also provides the preparation method of the peroral dosage form of above-mentioned lentinan, it is characterized in that, concrete steps comprise: in proportion that binding agent 100 weight portions are soluble in water, under agitation join in filler or diluent 99-99.9 weight portion, stir, make solid dosage forms, wherein, described binding agent comprises lentinan 1-0.1 weight portion again.
Preferably, described solid dosage forms is tablet, capsule or granule.
Preferably, described filler or diluent are one or more in starch, dextrin, lactose, microcrystalline Cellulose, mannitol, glucose, sorbitol, sucrose (Icing Sugar) and micropowder silica gel.
Preferably, described binding agent also comprises one or more in glucose, sucrose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, starch and dextrin.
The present invention also provides the preparation method of the peroral dosage form of another kind of above-mentioned lentinan, it is characterized in that, concrete steps comprise: by lentinan heating for dissolving in pure water, obtaining lentinan content is the lentinan raw materials for production liquid of 2-3%, and pure water is delivered to mixing kettle, opens mix and blend, add lentinan raw materials for production liquid, continue to stir, the mixed liquor of gained is carried out to fill, obtain shiitake fungus polyoses oral liquid.
Preferably, before fill, the shiitake fungus polyoses oral liquid in mixing kettle adds sodium bicarbonate, and the weight content of lentinan is 2-500PPM.
Preferably, before fill, in lentinan solution, add at least one in sodium bicarbonate, essence and flavoring agent, during fill, add carbon dioxide.
Preferably, in the oral liquid of described lentinan, the weight content of lentinan is 2PPM～10PPM.
Preferably, the pH of described shiitake fungus polyoses oral liquid is 7～9.
Lentinan in peroral dosage form of the present invention is to extract from mushroom fruiting body, processes the pure β, the single lentinan of triple helical configuration (lentinan) that obtain.After this lentinan is oral, by intestinal, be absorbed by the body, reach the immunomodulator effect being applied to after antineoplastic chemotherapy, radiotherapy, have and heighten the effect of a treatment significantly and reduce toxic and side effects.With this lentinan, make various medicines and the health product of peroral dosage form, possessed antitumor, strengthened immunoregulation effect, possess same effect with lentinan injection.
Compared with prior art, the invention has the beneficial effects as follows:
1, the present invention has possessed antitumor, has strengthened immunoregulation effect, possess same effect, and the preparation method of peroral dosage form is more simple and convenient than injection, the manufacturing cycle is short, cost is low, application is more extensive with lentinan injection.
2, the present invention adopts pure β, triple helical Cortex Seu Radix Wikstroemiae Micranthae type, single and have the lentinan of specific infrared signature, can improve greatly the bioavailability of lentinan peroral dosage form raw material, reduces day to take dosage, easy to use, and improves patient's compliance.
3, the present invention utilizes lentinan more stable various effective configurations of maintenance of energy under alkalescence (pH is 7～9) environment, therefore lentinan is made to soda pop, both demand had suited public tastesplay to the gallery, the function that keeps again lentinan, a kind of novel functional health beverage of can yet be regarded as.
The specific embodiment
Below in conjunction with embodiment, illustrate the present invention.It is that the method separation and purification of recording in the method > > embodiment of CN101161112, the patent No. Chinese patent < < separating and purifying lentinan that is ZL200610116956.3 obtains that lentinan of the present invention adopts publication number.Other auxiliary material is all from Chemical Reagent Co., Ltd., Sinopharm Group.Wherein the weight average molecular weight of lentinan is measured with light scattering method; Lentinan purity is measured with sulfuric acid-phynol method; Lentinan configuration is measured with infrared spectrum and Congo red reaction method.
Embodiment 1
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%,, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan, concrete steps are: in high-speed mixing granulating machine, add mannitol 99.7g; above-mentioned lentinan 0.1g is dissolved in 50mL water, under agitation joins in mannitol, with 15 hertz of rotating speeds, stir 12 minutes; cross 20 mesh sieves, granule processed.Granule drying case is dried, add magnesium stearate 0.2g, after mix homogeneously, be transferred to tabletting on tablet machine, tab is heavily 0.1g, makes 1000, obtains lentinan oral tablet.The lentinan oral tablet smooth surface of gained, mouthfeel is good, the bioavailability of lentinan improves greatly, can every day a slice, greatly reduce medication dose.
Embodiment 2
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan; concrete steps are: in high-speed mixing granulating machine; add microcrystalline Cellulose 40g and mannitol 57.9g; above-mentioned lentinan 0.1g and glucose 2g are dissolved in 50mL water; under agitation join in microcrystalline Cellulose and mannitol; with 15 hertz of rotating speeds, stir 15 minutes, cross 20 mesh sieves, granule processed.Granule drying case is dried, through 20 mesh sieve granulate, after mix homogeneously, the granule after granulate is proceeded in capsule filling machine, every capsules is loaded 0.1g, can obtain 1000 lentinan oral capsules.The stripping of gained capsule is fast, and bioavailability is high, can greatly reduce medication dose.
Embodiment 3
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%,, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan, concrete steps are: in fluid bed granulator, add microcrystalline Cellulose 2700g, open compressed air, make powder fluidisation; Above-mentioned lentinan 1g and glucose 299g are dissolved in 500mL water; under agitation pump in fluid bed granulator, top spray adds, boiling granulating 30 minutes; air outlet is controlled 70 ℃; dry 5 minutes, material is crossed to 40 mesh sieve granule processed, proceed in particles packing machine; divide packing; every bag 3g, makes 1000 bags, obtains lentinan granule.Gained even particle size, stripping is fast, and the bioavailability of lentinan peroral dosage form raw material improves greatly, can wrap every day one, greatly reduces medication dose.
Embodiment 4
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%., and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan; concrete steps are: lactose 295g is put into high-speed mixing granulating machine; above-mentioned lentinan 1g and sodium carboxymethyl cellulose 4.8g are dissolved in 500mL water; under agitation join in high-speed mixing granulating machine; with 15 hertz of speed, stir 14 minutes; be transferred in oscillating granulator, cross 18 mesh sieves, granulate.Gained granule, through 70 ℃ of dry half an hour of baking oven, is transferred in V-type blender, adds magnesium stearate 0.2g, and mix homogeneously, is transferred in capsule filling machine, and adjustment loading amount is 0.3g, makes 1000, obtains lentinan oral capsule.Gained even particle size, capsule stripping is fast, and the bioavailability of lentinan peroral dosage form raw material improves greatly, can every day one, greatly reduce medication dose.
Embodiment 5
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan, concrete steps are: take above-mentioned lentinan 5g, 90 ℃ of heated and stirred, be dissolved in 2.5L pure water, all dissolve and have no not after dissolved particles, continue heated and stirred 30 minutes, guarantee all to dissolve, be uniformly distributed, obtain lentinan content and be 2% lentinan solution, press drinking pure water standard, the drinking pure water of producing is 997.5L through metering, inject batching mixing kettle, open mix and blend, the 2.5L lentinan solution being uniformly dissolved is injected to batching mixing kettle, and add sodium bicarbonate 700g, regulating PH is 7.5, stir 30 minutes, stop stirring, by automatic loading production line, filter, sterilizing, by 200ml/, have to 498 Lentinus Edodes beverages of trial production fill, wherein, the weight content of lentinan is 5PPM, pH is 7.5.
Embodiment 6
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%,, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan, concrete steps are: take above-mentioned lentinan 3g, 90 ℃ of heated and stirred, be dissolved in 1.5L pure water, all dissolve and have no not after dissolved particles, continue heated and stirred 30 minutes, guarantee whole dissolvings, be uniformly distributed, obtain lentinan content and be 2% lentinan solution, press drinking pure water standard, the drinking pure water of producing, through metering, be 28.5L, drop in 50L batching mixing kettle, open mix and blend, the lentinan solution being uniformly dissolved is injected to mixing kettle and adds sodium bicarbonate 21g, regulating pH is 7.5, stir 30 minutes, stop stirring, delivered solution fill is after filtering to oral liquid bottle, every 10ml/ bottle is again through sterilizing, gland, pack to such an extent that 2962 bottlenecks take lentinan health beverage, wherein, the weight content of lentinan is 100PPM, pH is 7.5.
Embodiment 7
A peroral dosage form for lentinan, contains weight average molecular weight and is 400,000～800,000 the lentinan suc as formula the pure β shown in (1), triple helical configuration, and its purity is 96.1wt%,, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.The Congo red of lentinan reacts be positive (+).The preparation method of the peroral dosage form of above-mentioned lentinan, concrete steps are: take above-mentioned lentinan 10g, 90 ℃ of heated and stirred, be dissolved in 5L pure water, all dissolve and have no not after dissolved particles, continue heated and stirred 30 minutes, guarantee all to dissolve, be uniformly distributed, obtain lentinan content and be 2% lentinan solution, press drinking pure water standard, the drinking pure water of producing is 2795L through metering, inject batching mixing kettle, open mix and blend, add again 3kg sodium bicarbonate stirring and dissolving 10 minutes, the 5L lentinan solution being uniformly dissolved is injected to batching mixing kettle, stir 30 minutes, stop stirring, pass through automatic loading production line, filter, sterilizing, only press 280ml/, add carbon dioxide, 9982 Lentinus Edodes soda water beverages of trial production fill, wherein, the weight content of lentinan is 3.6PPM, pH is 8.2.
Lentinan anti-tumor experiment:
Lentinan peroral dosage form classification for experiment:
| Title | Dosage form |
| Embodiment 1 | Lentinan content is 0.1mg/100mg oral tablet |
| Embodiment 2 | Lentinan content is 0.1mg/100mg oral capsule |
| Embodiment 3 | Lentinan content is 1mg/3g bag oral granular formulation |
| Embodiment 4 | Lentinan content is 1mg/0.3g oral capsule |
| Embodiment 5 | Lentinan content is 1mg/200ml oral liquid |
| Embodiment 6 | Lentinan content is 1mg/10ml health beverage |
| Embodiment 7 | Lentinan content is 1mg/280ml soda water |
Lentinan peroral dosage form anti-tumor experiment consumption
| Title | Every day dosage form consumption | The medication cycle |
| Lentinan for injection injection | 0.025mg/0.1ml | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 1 | 0.025mg/25mg | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 2 | 0.025mg/25mg | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 3 | 0.025mg/75mg | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 4 | 0.025mg/7.5mg | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 5 | 0.025mg/5ml | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 6 | 0.025mg/0.25ml | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
| Embodiment 7 | 0.025mg/7ml | Drug withdrawal 2 days after 5 days weekly, is used in conjunction 3 weeks |
Get body weight 25g ± 1g female, without pregnant ICR healthy mice.
Take after mouse subcutaneous transplanting S180 ascites cell, by measuring after administration, the data statistics of administration group and blank group, illustrates the anti-tumor activity of lentinan types of formulation.
With lentinan injection add aquesterilisa be mixed with every 1ml containing lentinan 0.25mg solution as injection for medicine.
By Mouse Weight order, be divided at random 6 groups, 10 every group.
From mouse subcutaneous transplanting S180 tumor cell second day, start for medicine every day to medication group, dosage is that in all kinds of preparations of lentinan for injection injection 0.1ml (0.025mg lentinan), lentinan peroral dosage form, contained lentinan is 0.025mg, after tumour transplatation 25 days, kill whole mices, take out tumor, gravimetry.
Meter mark is respectively organized the exemplary embodiment lock of mice: blank group (WC), administration group (WT)
According to following formula, ask the suppression ratio of tumor:
Tumor control rate (%)=(WC-WT)/WC*100%
The comparison on tumor control rate impact of lentinan oral formulations and lentinan injection
| Mice medication group | Take out the average weight of tumor | Tumor control rate | Effective order |
| Blank group | 9.2g | ? | ? |
| Lentinan for injection injection | 0.8g | 91％ | 1 |
| Embodiment 1 | 1.29g | 86％ | 8 |
| Embodiment 2 | 1.05g | 89％ | 4 |
| Embodiment 3 | 1.17g | 87％ | 7 |
| Embodiment 4 | 1.1g | 88％ | 6 |
| Embodiment 5 | 0.96g | 90％ | 3 |
| Embodiment 6 | 0.88g | 90％ | 2 |
| Embodiment 7 | 1.03g | 89％ | 5 |
Lentinan oral formulations and lentinan injection drug effect are examined and determine life span impact test:
Get Kunming mouse in 4～5 week age, male and female dual-purpose, divides 6 groups at random, and 12 every group, it is 5*10 that S180 tumor liquid is become to cell concentration with normal saline dilution
6the cell suspension of/0.2ml, ip injects.
With lentinan injection add aquesterilisa be mixed with every 1ml containing lentinan 0.25mg solution as lentinan injection.
Give respectively each test group injected in mice 0.1ml (containing 0.025mg lentinan) lentinan injection, other each medication group is taken contained lentinan in peroral dosage form and is 0.025mg, every day 1 time, is used in conjunction 3 weeks, observes the impact of all kinds of preparations on tumor-bearing mice life span.
Lentinan oral formulations and the impact of lentinan injection drug effect on life span
| Mice medication group | On average in the time of depositing | Existence order time delay |
| Blank group | 30.5 | ? |
| Lentinan for injection injection | 66.2 | 1 |
| Embodiment 1 | 61.5 | 5 |
| Embodiment 2 | 59.2 | 8 |
| Embodiment 3 | 60.4 | 6 |
| Embodiment 4 | 61.8 | 4 |
| Embodiment 5 | 60 | 7 |
| Embodiment 6 | 63.5 | 2 |
| Embodiment 7 | 62 | 3 |
Result shows: blank group and medicinal group differ significantly, and oral formulations and injection differ DeGrain.
Claims (9)
1. a peroral dosage form for lentinan, is characterized in that, containing weight average molecular weight is 400,000～800,000 pure β, the lentinan of triple helical configuration, and its purity is > 96wt%, and this lentinan is at 3500～3300cm
-1, 2920-2800cm
-1, 1100-1000cm
-1, 890cm
-1there is INFRARED ABSORPTION.
2. the peroral dosage form of lentinan as claimed in claim 1, is characterized in that, the molecular formula of described lentinan is:
。
3. the peroral dosage form of lentinan as claimed in claim 1, is characterized in that, the Congo red of described lentinan reacts be positive (+).
4. the preparation method of the peroral dosage form of the lentinan described in claim 1, it is characterized in that, concrete steps comprise: in proportion that binding agent 100 weight portions are soluble in water, under agitation join in filler or diluent 99-99.9 weight portion, stir, make solid dosage forms, wherein, described binding agent comprises pure β, triple helical configuration, single lentinan 1-0.1 weight portion again.
5. the preparation method of the peroral dosage form of lentinan as claimed in claim 4, is characterized in that, described solid dosage forms is tablet, capsule or granule.
6. the preparation method of the peroral dosage form of lentinan as claimed in claim 4, it is characterized in that, described filler or diluent are one or more in starch, dextrin, lactose, microcrystalline Cellulose, mannitol, glucose, sorbitol, sucrose and micropowder silica gel.
7. the preparation method of the peroral dosage form of lentinan as claimed in claim 4, is characterized in that, described binding agent also comprises one or more in glucose, sucrose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, starch and dextrin.
8. the preparation method of the peroral dosage form of lentinan claimed in claim 1, it is characterized in that, concrete steps comprise: by lentinan heating for dissolving in pure water, obtaining lentinan content is the lentinan raw materials for production liquid of 2-3%, and pure water is delivered to mixing kettle, opens mix and blend, add lentinan raw materials for production and sodium bicarbonate, continue to stir, the mixed liquor of gained is carried out to fill, the weight content that obtains shiitake fungus polyoses oral liquid lentinan is 2PPM～500PPM.
9. the preparation method of the peroral dosage form of lentinan as claimed in claim 8, is characterized in that, before fill, also adds sodium bicarbonate, at least one in essence and flavoring agent in mixing kettle.During fill, add carbon dioxide, in shiitake fungus polyoses oral liquid, the weight content of lentinan is 2-10PPM.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107468655A (en) * | 2017-08-21 | 2017-12-15 | 无限极（中国）有限公司 | A kind of lentinan particle and preparation method thereof |
| CN108066302A (en) * | 2017-12-28 | 2018-05-25 | 无限极（中国）有限公司 | A kind of preparation method of fast dispersion solid medicine and the fast dispersion solid medicine of preparation |
| CN108107010A (en) * | 2017-12-21 | 2018-06-01 | 无限极（中国）有限公司 | A kind of method for detecting lentinan content |
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| CN101244093A (en) * | 2008-02-22 | 2008-08-20 | 上海慈瑞医药科技有限公司 | Method of preparing shiitake fungus polyoses oral liquid |
| CN102190739A (en) * | 2010-03-12 | 2011-09-21 | 南京易亨制药有限公司 | Process for extracting lentinan and method for measuring molecular weight distribution of lentinan |
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| CN101244093A (en) * | 2008-02-22 | 2008-08-20 | 上海慈瑞医药科技有限公司 | Method of preparing shiitake fungus polyoses oral liquid |
| CN102190739A (en) * | 2010-03-12 | 2011-09-21 | 南京易亨制药有限公司 | Process for extracting lentinan and method for measuring molecular weight distribution of lentinan |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107468655A (en) * | 2017-08-21 | 2017-12-15 | 无限极（中国）有限公司 | A kind of lentinan particle and preparation method thereof |
| CN107468655B (en) * | 2017-08-21 | 2020-02-18 | 无限极（中国）有限公司 | Lentinan particles and preparation method thereof |
| CN108107010A (en) * | 2017-12-21 | 2018-06-01 | 无限极（中国）有限公司 | A kind of method for detecting lentinan content |
| CN108066302A (en) * | 2017-12-28 | 2018-05-25 | 无限极（中国）有限公司 | A kind of preparation method of fast dispersion solid medicine and the fast dispersion solid medicine of preparation |
| CN108066302B (en) * | 2017-12-28 | 2020-09-11 | 无限极（中国）有限公司 | Preparation method of fast-dispersing solid preparation and fast-dispersing solid preparation prepared by same |
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| CN103948621B (en) | 2017-05-17 |
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