CN110693898A - 一种含有人参皂苷的药物组合物 - Google Patents
一种含有人参皂苷的药物组合物 Download PDFInfo
- Publication number
- CN110693898A CN110693898A CN201911160358.XA CN201911160358A CN110693898A CN 110693898 A CN110693898 A CN 110693898A CN 201911160358 A CN201911160358 A CN 201911160358A CN 110693898 A CN110693898 A CN 110693898A
- Authority
- CN
- China
- Prior art keywords
- ginsenoside
- cordycepin
- ethanol
- pharmaceutical composition
- ethyl acetate
- 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
- 229930182494 ginsenoside Natural products 0.000 title claims abstract description 36
- 229940089161 ginsenoside Drugs 0.000 title claims abstract description 30
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 23
- KQLDDLUWUFBQHP-UHFFFAOYSA-N Cordycepin Natural products C1=NC=2C(N)=NC=NC=2N1C1OCC(CO)C1O KQLDDLUWUFBQHP-UHFFFAOYSA-N 0.000 claims abstract description 26
- OFEZSBMBBKLLBJ-BAJZRUMYSA-N cordycepin Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)C[C@H]1O OFEZSBMBBKLLBJ-BAJZRUMYSA-N 0.000 claims abstract description 26
- OFEZSBMBBKLLBJ-UHFFFAOYSA-N cordycepine Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(CO)CC1O OFEZSBMBBKLLBJ-UHFFFAOYSA-N 0.000 claims abstract description 26
- 150000004676 glycans Chemical class 0.000 claims abstract description 23
- 229920001282 polysaccharide Polymers 0.000 claims abstract description 23
- 239000005017 polysaccharide Substances 0.000 claims abstract description 23
- CKUVNOCSBYYHIS-UHFFFAOYSA-N (20R)-ginsenoside Rg3 Natural products CC(C)=CCCC(C)(O)C1CCC(C2(CCC3C4(C)C)C)(C)C1C(O)CC2C3(C)CCC4OC1OC(CO)C(O)C(O)C1O CKUVNOCSBYYHIS-UHFFFAOYSA-N 0.000 claims abstract description 16
- CKUVNOCSBYYHIS-IRFFNABBSA-N (20S)-ginsenoside Rh2 Chemical compound O([C@H]1CC[C@]2(C)[C@H]3C[C@@H](O)[C@H]4[C@@]([C@@]3(CC[C@H]2C1(C)C)C)(C)CC[C@@H]4[C@@](C)(O)CCC=C(C)C)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O CKUVNOCSBYYHIS-IRFFNABBSA-N 0.000 claims abstract description 16
- CKUVNOCSBYYHIS-LGYUXIIVSA-N 20(R)-Ginsenoside Rh2 Natural products O([C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1)[C@@H]1C(C)(C)[C@H]2[C@@](C)([C@H]3[C@](C)([C@@]4(C)[C@H]([C@H](O)C3)[C@@H]([C@](O)(CC/C=C(\C)/C)C)CC4)CC2)CC1 CKUVNOCSBYYHIS-LGYUXIIVSA-N 0.000 claims abstract description 16
- 239000004475 Arginine Substances 0.000 claims abstract description 12
- 241001523681 Dendrobium Species 0.000 claims abstract description 12
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims abstract description 12
- HGHDGOQXDUNVGT-UHFFFAOYSA-N Ophiopogonin B Natural products CC1CCC2(OC1)OC3CC4C5CC=C6CCCC(OC7OC(C)C(O)C(O)C7OC8OC(C)C(O)C(O)C8O)C6(C)C5CCC4(C)C3C2C HGHDGOQXDUNVGT-UHFFFAOYSA-N 0.000 claims abstract description 11
- OWGURJWJHWYCIQ-AKYREZHBSA-N Ophiopogonin B Chemical compound O([C@@H]1[C@@H](O)[C@@H](O)[C@@H](C)O[C@H]1O[C@@H]1C[C@H](O)CC2=CC[C@H]3[C@@H]4C[C@H]5[C@@H]([C@]4(CC[C@@H]3[C@]21C)C)[C@@H]([C@]1(OC[C@H](C)CC1)O5)C)[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O OWGURJWJHWYCIQ-AKYREZHBSA-N 0.000 claims abstract description 11
- 239000004480 active ingredient Substances 0.000 claims abstract description 8
- 239000003381 stabilizer Substances 0.000 claims abstract description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 38
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 38
- 238000003756 stirring Methods 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 18
- 239000013078 crystal Substances 0.000 claims description 16
- 238000001914 filtration Methods 0.000 claims description 14
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 12
- 239000006228 supernatant Substances 0.000 claims description 12
- 238000002360 preparation method Methods 0.000 claims description 9
- 239000000047 product Substances 0.000 claims description 7
- 238000010438 heat treatment Methods 0.000 claims description 6
- 239000007788 liquid Substances 0.000 claims description 6
- 229930190017 ophiopogonin Natural products 0.000 claims description 6
- 238000005303 weighing Methods 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 4
- 239000002244 precipitate Substances 0.000 claims description 4
- 238000001556 precipitation Methods 0.000 claims description 4
- 238000010298 pulverizing process Methods 0.000 claims description 3
- 241001264174 Cordyceps militaris Species 0.000 claims description 2
- 239000005909 Kieselgur Substances 0.000 claims description 2
- 230000002378 acidificating effect Effects 0.000 claims description 2
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 claims description 2
- BFNBIHQBYMNNAN-UHFFFAOYSA-N ammonium sulfate Chemical compound N.N.OS(O)(=O)=O BFNBIHQBYMNNAN-UHFFFAOYSA-N 0.000 claims description 2
- 229910052921 ammonium sulfate Inorganic materials 0.000 claims description 2
- 235000011130 ammonium sulphate Nutrition 0.000 claims description 2
- 239000012043 crude product Substances 0.000 claims description 2
- 238000012258 culturing Methods 0.000 claims description 2
- 238000005520 cutting process Methods 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 claims description 2
- 239000012153 distilled water Substances 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 239000003480 eluent Substances 0.000 claims description 2
- 239000012535 impurity Substances 0.000 claims description 2
- 238000011068 loading method Methods 0.000 claims description 2
- 239000000463 material Substances 0.000 claims description 2
- 239000003960 organic solvent Substances 0.000 claims description 2
- 238000000643 oven drying Methods 0.000 claims description 2
- 239000002994 raw material Substances 0.000 claims description 2
- 238000010992 reflux Methods 0.000 claims description 2
- 239000011347 resin Substances 0.000 claims description 2
- 229920005989 resin Polymers 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 238000001179 sorption measurement Methods 0.000 claims description 2
- 238000005406 washing Methods 0.000 claims description 2
- 238000002386 leaching Methods 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract description 14
- 201000011510 cancer Diseases 0.000 abstract description 9
- 239000003814 drug Substances 0.000 abstract description 8
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 6
- 231100000419 toxicity Toxicity 0.000 abstract description 5
- 230000001988 toxicity Effects 0.000 abstract description 5
- 230000005764 inhibitory process Effects 0.000 abstract description 4
- 239000000203 mixture Substances 0.000 abstract description 3
- 230000028993 immune response Effects 0.000 abstract description 2
- 238000005316 response function Methods 0.000 abstract description 2
- 210000004027 cell Anatomy 0.000 description 21
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 12
- 235000008434 ginseng Nutrition 0.000 description 12
- 241000208340 Araliaceae Species 0.000 description 10
- 235000005035 Panax pseudoginseng ssp. pseudoginseng Nutrition 0.000 description 10
- 235000003140 Panax quinquefolius Nutrition 0.000 description 10
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 8
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 8
- 210000004881 tumor cell Anatomy 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- 239000012528 membrane Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 4
- 239000000706 filtrate Substances 0.000 description 4
- 238000007873 sieving Methods 0.000 description 4
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 235000002789 Panax ginseng Nutrition 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000012091 fetal bovine serum Substances 0.000 description 3
- 238000000227 grinding Methods 0.000 description 3
- 210000003292 kidney cell Anatomy 0.000 description 3
- 239000013641 positive control Substances 0.000 description 3
- 230000035755 proliferation Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 230000001954 sterilising effect Effects 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 229930189092 Notoginsenoside Natural products 0.000 description 2
- 240000004371 Panax ginseng Species 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- 238000004806 packaging method and process Methods 0.000 description 2
- 210000000952 spleen Anatomy 0.000 description 2
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 108010059892 Cellulase Proteins 0.000 description 1
- 241001076416 Dendrobium tosaense Species 0.000 description 1
- 208000001382 Experimental Melanoma Diseases 0.000 description 1
- 206010019695 Hepatic neoplasm Diseases 0.000 description 1
- 101000573199 Homo sapiens Protein PML Proteins 0.000 description 1
- 238000012449 Kunming mouse Methods 0.000 description 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 1
- 229930182816 L-glutamine Natural products 0.000 description 1
- WSMYVTOQOOLQHP-UHFFFAOYSA-N Malondialdehyde Chemical compound O=CCC=O WSMYVTOQOOLQHP-UHFFFAOYSA-N 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 244000111146 Sonchus arvensis Species 0.000 description 1
- 235000006731 Sonchus arvensis Nutrition 0.000 description 1
- 102000019197 Superoxide Dismutase Human genes 0.000 description 1
- 108010012715 Superoxide dismutase Proteins 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 239000006143 cell culture medium Substances 0.000 description 1
- 229940106157 cellulase Drugs 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 230000001085 cytostatic effect Effects 0.000 description 1
- 230000003013 cytotoxicity Effects 0.000 description 1
- 231100000135 cytotoxicity Toxicity 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 1
- 231100000086 high toxicity Toxicity 0.000 description 1
- 102000054896 human PML Human genes 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000003859 lipid peroxidation Effects 0.000 description 1
- 208000014018 liver neoplasm Diseases 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 238000003672 processing method Methods 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000010025 steaming Methods 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 230000035922 thirst Effects 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明涉及医药技术领域，具体为一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和稳定剂；其中人参皂苷Rh2 20‑25重量份、麦冬皂苷B 5‑10重量份、石斛多糖5‑10重量份、虫草素1‑3重量份和稳定剂65‑70重量份，通过人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸组成的药物组合物，能够增强机体免疫应答功能，提高对癌细胞的抑制性，同时通过石斛多糖能够修复被人参皂苷Rh2、麦冬皂苷B的毒性损伤的细胞，从而减少细胞的损伤。
Description
技术领域
本发明涉及医药技术领域，具体为一种含有人参皂苷的药物组合物。
背景技术
癌症是常见病、多发病，对人们生命和健康有着严重威胁，对国民经济建设的影响也是巨大的。全世界和我国的癌症发病率在逐年明显增加。我国每年新患癌症约160万人、死于癌症者约130万人。现在我国癌症死亡的水平，全国每1分钟就有2个人死于癌症，每天将有2800多人被癌症夺走生命，1年将相当于一个有百万人口的城市被毁灭。
人参属上等名贵中药，主要功效为：“大补元气，补脾益肺，生津止渴，安神增智”。人参不仅能治疗和预防许多疾病，也是养生保健之佳品。依据人参产地及炮制方法可分为野山参、园参、吉林参、朝鲜参，生晒参、白参、红参等。红参是人参经蒸制加工而成。
1983年，北川勋首次从朝鲜红参中分离出人参皂苷Rh2。通过大量的研究，现已经证实人参皂苷Rh2可以通过诱导分化或凋亡，抑制多种肿瘤细胞的增殖和生长，并证明对正常细胞毒性作用较低；以及人参皂苷Rh2有较好的缓解体力疲劳的作用。
目前，专利申请号为2015101818483的一项中国专利公开了一种含有人参皂苷的药物组合物，按重量百分含量包括活性成分人参皂苷Rg320％～70％、人参皂苷Rh2 10％～40％、三七皂苷ft1 20％～50％。同时还提供了组合物在预和治疗癌症及抗癌辅助药物及提高机体免疫力的药品或保健品中的应用。该药物组合物能够有效的抑制肿瘤细胞，但该药物组合物的对正常细胞毒性作用较高，使得正常细胞也会受损，为此，提出一种能够有效的抑制肿瘤细胞且对正常细胞损坏较低的含有人参皂苷的药物组合物。
发明内容
为了解决上述的问题，本发明提供一种含有人参皂苷的药物组合物。
本发明解决其技术问题采用以下实施例来实现：
一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和稳定剂；其中人参皂苷Rh2 20-25重量份、麦冬皂苷B 5-10重量份、石斛多糖5-10重量份、虫草素1-3重量份和稳定剂65-70重量份。
优选的，所述稳定剂采用精氨酸。
优选的，所述人参皂苷Rh2的制备方法:在搅拌条件下向乙酸乙酯中先加入硅藻土，再加入人参皂苷提取物，于78-85℃加热回流0.5-1.5小时，过滤，浓缩；加入硅藻土的量为人参皂苷提取物重量的0.8-1.2倍，乙酸乙酯与人参皂苷提取物的液固比为15-20ml/g；再加入蒸馏水除杂，分出乙酸乙酯层，乙酸乙酯层过酸性氧化铝柱，用水饱和乙酸乙酯洗脱，收集洗脱液；洗脱液减压浓缩至无乙酸乙酯味，加乙醇使之溶解，再加水至使含醇量为60-70％，静置，使析出粗结晶，过滤，取粗结晶，烘干；粗结晶依次用乙醇和乙酸乙酯重结晶，即得。
优选的，所述石斛多糖的制备方法：取石斛药材,切成0.5cm长的饮片,各称取100g,提取液浓缩至1:1ml/g,加3倍量乙醇使沉淀,放置,倾出上清液,沉淀加水溶解,加稀乙醇使沉淀；放置离心，取其上清液继续加乙醇使含醇量达70％以上,放置,倾出上清液；沉淀依次用乙醇、无水乙醇洗涤,减压过滤,低温干燥.即得多糖粗品。
优选的，所述石斛药材采用铁皮石斛。
优选的，以培养蛹虫草子座剩余的基质为原料,将基质粉碎后以有机溶剂进行浸提，离心收集上清液；利用大孔树脂吸附色谱柱对离心后的粗液进行纯化；将将纯化后的上清液采用乙醇、硫酸铵组成的双水相体系进行富集并收集样品；装层析柱，甲醇溶液洗脱，洗脱液减压蒸馏浓缩，浓缩的洗脱液甲醇洗脱,洗脱液结晶得到虫草素晶体，虫草素晶体粉碎后获得虫草素。
优选的，所述虫草素晶体粉碎后获得虫草素需要再经过200目的筛网筛选。
与现有技术相比，本发明的有益效果是：本发明所述的一种含有人参皂苷的药物组合物，通过人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸组成的药物组合物，能够增强机体免疫应答功能，提高对癌细胞的抑制性，同时通过石斛多糖能够修复被人参皂苷Rh2、麦冬皂苷B的毒性损伤的细胞，从而减少细胞的损伤，同时石斛多糖也能显著抑制S180实体瘤的增殖，水溶性多糖能够有效抑制小鼠肉瘤S180瘤体生长和离体肝肿瘤细胞生长，有效提高荷瘤小鼠胸腺指数和脾脏指数，提高超氧化物歧化酶活性和降低膜脂过氧化产物丙二醛含量，促进神经母瘤细胞凋亡；在体外则对人早幼粒白血病细胞增殖表现出较强的抗性。
具体实施方式
下面将结合本发明实施方式中的实施例进行清楚、完整地描述，显然，所描述的实施例仅仅是本发明一部分实施方式，而不是全部的实施方式。基于本发明中的实施例，本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例，都属于本发明保护的范围。
实施例1
一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸；称取精氨酸65g、等质量的水，搅拌均匀，加入人参皂苷Rh220g、麦冬皂苷B5g、石斛多糖5g、虫草素1g，加热至45℃，搅拌溶解，用含3％盐酸的水溶液调pH值至5.6，加水至全量，搅拌均匀；再加入配液量0.l％(g/ml)的活性炭，搅拌25分钟，粗滤脱炭；过0.22μm滤膜，得精滤液；121℃高压灭菌30分钟，析出结晶，通过研磨机粉碎，再通过200目筛网筛分，获得干燥粉末，检验，包装，入库。
实施例2
一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸；称取精氨酸70g、等质量的水，搅拌均匀，加入人参皂苷Rh2 25g、麦冬皂苷B8g、石斛多糖5g、虫草素1g，加热至45℃，搅拌溶解，用含3％盐酸的水溶液调pH值至5.6，加水至全量，搅拌均匀；再加入配液量0.l％(g/ml)的活性炭，搅拌25分钟，粗滤脱炭；过0.22μm滤膜，得精滤液；121℃高压灭菌30分钟，析出结晶，通过研磨机粉碎，再通过200目筛网筛分，获得干燥粉末，检验，包装，入库。
实施例3
一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸；称取精氨酸70g、等质量的水，搅拌均匀，加入人参皂苷Rh2 25g、麦冬皂苷B8g、石斛多糖5g、虫草素1g，加热至45℃，搅拌溶解，用含3％盐酸的水溶液调pH值至5.6，加水至全量，搅拌均匀；再加入配液量0.l％(g/ml)的活性炭，搅拌25分钟，粗滤脱炭；过0.22μm滤膜，得精滤液；121℃高压灭菌30分钟，析出结晶，通过研磨机粉碎，再通过200目筛网筛分，获得干燥粉末，将干燥的粉末压片得到片剂。
实施例4
一种含有人参皂苷的药物组合物，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和精氨酸；称取精氨酸70g、等质量的水，搅拌均匀，加入人参皂苷Rh2 25g、麦冬皂苷B8g、石斛多糖5g、虫草素1g，加热至45℃，搅拌溶解，用含3％盐酸的水溶液调pH值至5.6，加水至全量，搅拌均匀；再加入配液量0.l％(g/ml)的活性炭，搅拌25分钟，粗滤脱炭；过0.22μm滤膜，得精滤液；121℃高压灭菌30分钟，析出结晶，通过研磨机粉碎，再通过200目筛网筛分，获得干燥粉末，将干燥的粉末溶解到生理盐水中，即获得注射液。
实验例1
试验动物：动物2-3月龄，昆明种雄性健康小鼠，体重(25±3)g。
细胞：B16黑色素瘤细胞(B16melanomacell)和人肝癌细胞(HepG2)
培养基：细胞培养用DMEM液培养(FBS；HyClone,Logan,UT,USA)，培养液添加10％胎牛血清(FBS；HyClone,Logan,UT,USA)，0.03％L–谷氨酰胺,100U/L青酶素，100mg/L链霉素，5％NaCO2调pH至6.8–7.0。
样品：实验组1：实施例1制取的产品；实验组2：实施例2制取的产品；实验组3：人参皂苷Rg370％，人参皂苷Rh215％，三七皂苷ft115％。组合物用20μl二甲基亚砜(DMSO)溶解，用于配置不同浓度的DMEM细胞培养基。
试验方法：原代培养的正常昆明鼠肾细胞，B16细胞以及HepG2细胞以细胞密度为1×104/ml接种于96孔板中培养24小时后，把普通DMEM培养基换为含有终浓度为0μg，25μg，50μg，75μg，100μg不同组化合的DMEM培养基，每个浓度设3个孔，并在24小时之后用MTT法检测细胞的活性，细胞抑制活性用抑制浓度IC50(medianinhibitoryconcentration)表示。抑制浓度(IC50)为细胞活性抑制率为50％时的药物浓度，计算方法为IC50＝(A细胞对照组-A供试样品组)/A细胞对照组-A空白组)×100％。
MTT法：根据Mosmann建立的MTT法检测药物的细胞毒性。具体方法是：向吸去上清的细胞孔中加入0.4mg/mLMTT，0.1mL/孔，37℃5％CO2培养4h，去上清，每孔加入0.1mL二甲基亚砜(DMSO)，孵育10min，在酶标仪上测定溶液在570nm下的吸光度值。
表1对肿瘤细胞的半数抑制浓度IC50(μg/mL)。
实验结果如表1所示，阳性对照组(TAX，PPD)以及三个实验组均对B16和HepG2细胞有抑制作用。对两种肿瘤细胞的半数抑制浓度IC50均在40μg/ml以下。通过细胞计数法对原代鼠肾细胞数量进行计数，能够得知，实验组1和实验组2的原代鼠肾细胞数量明显高于阳性对照组(TAX，PPD)以及实验组3，表面实验组1和实验组2的毒性小于阳性对照组(TAX，PPD)以及实验组3，实验组1和实验组2的样品相对于实验组3的样品，具有更高的肿瘤抑制效果，且毒性更小。
虽然在上文中已经参考实施例对本发明进行了描述，然而在不脱离本发明的范围的情况下，可以对其进行各种改进并且可以用等效物替换其中的部件。尤其是，只要不存在结构冲突，本发明所披露的实施例中的各项特征均可通过任意方式相互结合起来使用，在本说明书中未对这些组合的情况进行穷举性的描述仅仅是出于省略篇幅和节约资源的考虑。因此，本发明并不局限于文中公开的特定实施例，而是包括落入权利要求的范围内的所有实施例。
Claims (7)
1.一种含有人参皂苷的药物组合物，其特征在于，包括药物组合物活性成分为：人参皂苷Rh2、麦冬皂苷B、石斛多糖、虫草素和稳定剂；其中人参皂苷Rh2 20-25重量份、麦冬皂苷B5-10重量份、石斛多糖5-10重量份、虫草素1-3重量份和稳定剂65-70重量份。
2.根据权利要求1所述的一种含有人参皂苷的药物组合物，其特征在于：所述稳定剂采用精氨酸。
3.根据权利要求1所述的一种含有人参皂苷的药物组合物，其特征在于：所述人参皂苷Rh2的制备方法:在搅拌条件下向乙酸乙酯中先加入硅藻土，再加入人参皂苷提取物，于78-85℃加热回流0.5-1.5小时，过滤，浓缩；加入硅藻土的量为人参皂苷提取物重量的0.8-1.2倍，乙酸乙酯与人参皂苷提取物的液固比为15-20ml/g；再加入蒸馏水除杂，分出乙酸乙酯层，乙酸乙酯层过酸性氧化铝柱，用水饱和乙酸乙酯洗脱，收集洗脱液；洗脱液减压浓缩至无乙酸乙酯味，加乙醇使之溶解，再加水至使含醇量为60-70％，静置，使析出粗结晶，过滤，取粗结晶，烘干；粗结晶依次用乙醇和乙酸乙酯重结晶，即得。
4.根据权利要求1所述的一种含有人参皂苷的药物组合物，其特征在于：所述石斛多糖的制备方法：取石斛药材,切成0.5cm长的饮片,各称取100g,提取液浓缩至1:1ml/g,加3倍量乙醇使沉淀,放置,倾出上清液,沉淀加水溶解,加稀乙醇使沉淀；放置离心，取其上清液继续加乙醇使含醇量达70％以上,放置,倾出上清液；沉淀依次用乙醇、无水乙醇洗涤,减压过滤,低温干燥.即得多糖粗品。
5.根据权利要求4所述的一种含有人参皂苷的药物组合物，其特征在于：所述石斛药材采用铁皮石斛。
6.根据权利要求1所述的一种含有人参皂苷的药物组合物，其特征在于：所述虫草素的制备方法：以培养蛹虫草子座剩余的基质为原料,将基质粉碎后以有机溶剂进行浸提，离心收集上清液；利用大孔树脂吸附色谱柱对离心后的粗液进行纯化；将将纯化后的上清液采用乙醇、硫酸铵组成的双水相体系进行富集并收集样品；装层析柱，甲醇溶液洗脱，洗脱液减压蒸馏浓缩，浓缩的洗脱液甲醇洗脱,洗脱液结晶得到虫草素晶体，虫草素晶体粉碎后获得虫草素。
7.根据权利要求6所述的一种含有人参皂苷的药物组合物，其特征在于：所述虫草素晶体粉碎后获得虫草素需要再经过200目的筛网筛选。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911160358.XA CN110693898A (zh) | 2019-11-23 | 2019-11-23 | 一种含有人参皂苷的药物组合物 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911160358.XA CN110693898A (zh) | 2019-11-23 | 2019-11-23 | 一种含有人参皂苷的药物组合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110693898A true CN110693898A (zh) | 2020-01-17 |
Family
ID=69206615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201911160358.XA Pending CN110693898A (zh) | 2019-11-23 | 2019-11-23 | 一种含有人参皂苷的药物组合物 |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110693898A (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116370367A (zh) * | 2023-01-31 | 2023-07-04 | 西安绿天生物技术有限公司 | 一种化妆品用植物提取物及其制备方法和应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101015649A (zh) * | 2006-11-23 | 2007-08-15 | 天津市轩宏医药技术有限公司 | 一种铁皮石斛多糖提取物、其药物组合物和其制备方法及其应用 |
| CN103877112A (zh) * | 2014-04-06 | 2014-06-25 | 吴静 | 一种含有人参皂苷Rh2、麦冬皂苷B的药物组合物 |
| CN104327139A (zh) * | 2014-09-28 | 2015-02-04 | 西北农林科技大学 | 虫草素晶体的制备方法 |
| CN106109953A (zh) * | 2016-07-11 | 2016-11-16 | 吕其镁 | 肿瘤防治中药制剂及其制备方法 |
-
2019
- 2019-11-23 CN CN201911160358.XA patent/CN110693898A/zh active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101015649A (zh) * | 2006-11-23 | 2007-08-15 | 天津市轩宏医药技术有限公司 | 一种铁皮石斛多糖提取物、其药物组合物和其制备方法及其应用 |
| CN103877112A (zh) * | 2014-04-06 | 2014-06-25 | 吴静 | 一种含有人参皂苷Rh2、麦冬皂苷B的药物组合物 |
| CN104327139A (zh) * | 2014-09-28 | 2015-02-04 | 西北农林科技大学 | 虫草素晶体的制备方法 |
| CN106109953A (zh) * | 2016-07-11 | 2016-11-16 | 吕其镁 | 肿瘤防治中药制剂及其制备方法 |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116370367A (zh) * | 2023-01-31 | 2023-07-04 | 西安绿天生物技术有限公司 | 一种化妆品用植物提取物及其制备方法和应用 |
| CN116370367B (zh) * | 2023-01-31 | 2024-05-17 | 西安绿天生物技术有限公司 | 一种化妆品用植物提取物及其制备方法和应用 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101242850A (zh) | 文冠果的提取物和从提取物分离出的化合物的组成，功能和应用，以及它们的制备方法 | |
| CN102138966B (zh) | 藏茵陈提取物及其制备方法、药物组合物和用途 | |
| CN110051726A (zh) | 一种青钱柳叶中总黄酮和总多糖的制备方法及应用 | |
| CN105777924B (zh) | 一种桑黄子实体抗癌活性多糖pbpp及其制备方法 | |
| CN101584718A (zh) | 对萼猕猴桃叶提取物及其制备方法和用途 | |
| CN111961022B (zh) | 一种具有神经保护作用的双黄酮类化合物及其提取分离方法 | |
| CN101229335A (zh) | 酶法制备黑刺菝葜总皂苷提取物的方法 | |
| CN103505480A (zh) | 石榴皮抗肿瘤多酚有效部位及其制备方法和应用 | |
| CN112159451A (zh) | 一种绞股蓝皂苷提取物及其制备方法 | |
| CN106883306A (zh) | 一种具有抗肿瘤活性的向日葵茎芯多糖的提取分离方法 | |
| CN110693898A (zh) | 一种含有人参皂苷的药物组合物 | |
| CN107496490B (zh) | 一种淫羊藿红景天制剂及其制备方法 | |
| CN105198943B (zh) | 一种名为茶山奈苷a的酰化黄酮糖苷及其制备方法和应用 | |
| Park et al. | The neuroprotective and neurotrophic effects of Tremella fuciformis in PC12h cells | |
| CN115894735B (zh) | 一种老鹰茶酸性多糖及其提取纯化方法和抗癌应用 | |
| CN110507749A (zh) | 一种蒙古韭抗肿瘤提取物及其制备方法和用途 | |
| CN102293251B (zh) | 山茱萸果奶 | |
| CN110194754A (zh) | 一种蹄叶橐吾脂溶性提取物及其制备方法和用途 | |
| CN112851621B (zh) | 牛白藤总环烯醚萜提取物、提取纯化方法及其应用 | |
| CN104857245A (zh) | 紫萼玉簪花总皂苷的制备方法和应用 | |
| CN101732377A (zh) | 具有抗癌作用的刺人参叶总皂苷提取物的制备方法 | |
| CN108434171A (zh) | 一种预防化学性肝损伤的慈姑多糖组合物及其制备方法 | |
| CN102579869A (zh) | 一种治疗肝病的藏药组合物的制备方法 | |
| CN113368156A (zh) | 一种连翘叶活性成分及其在制备抗阿尔茨海默症药物中的应用 | |
| CN101863945B (zh) | 西洋参皂苷f6及其提取方法及其医药用途 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20200117 |