CN1556108A - Extraction process, medicinal composition and preparation process of baicalein - Google Patents
Extraction process, medicinal composition and preparation process of baicalein Download PDFInfo
- Publication number
- CN1556108A CN1556108A CNA2003101103384A CN200310110338A CN1556108A CN 1556108 A CN1556108 A CN 1556108A CN A2003101103384 A CNA2003101103384 A CN A2003101103384A CN 200310110338 A CN200310110338 A CN 200310110338A CN 1556108 A CN1556108 A CN 1556108A
- Authority
- CN
- China
- Prior art keywords
- baicalein
- injection
- scutellarin
- oil
- capsule
- 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.)
- Granted
Links
- FXNFHKRTJBSTCS-UHFFFAOYSA-N Baicalein Natural products C=1C(=O)C=2C(O)=C(O)C(O)=CC=2OC=1C1=CC=CC=C1 FXNFHKRTJBSTCS-UHFFFAOYSA-N 0.000 title claims abstract description 30
- UDFLTIRFTXWNJO-UHFFFAOYSA-N baicalein Chemical compound O1C2=CC(=O)C(O)=C(O)C2=C(O)C=C1C1=CC=CC=C1 UDFLTIRFTXWNJO-UHFFFAOYSA-N 0.000 title claims abstract description 23
- 229940015301 baicalein Drugs 0.000 title claims abstract description 23
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000000203 mixture Substances 0.000 title claims description 18
- 238000000605 extraction Methods 0.000 title description 4
- DJSISFGPUUYILV-UHFFFAOYSA-N UNPD161792 Natural products O1C(C(O)=O)C(O)C(O)C(O)C1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC(O)=CC=1)O2 DJSISFGPUUYILV-UHFFFAOYSA-N 0.000 claims abstract description 87
- NPLTVGMLNDMOQE-UHFFFAOYSA-N carthamidin Natural products C1=CC(O)=CC=C1C1OC2=CC(O)=C(O)C(O)=C2C(=O)C1 NPLTVGMLNDMOQE-UHFFFAOYSA-N 0.000 claims abstract description 87
- DJSISFGPUUYILV-ZFORQUDYSA-N scutellarin Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC(O)=CC=1)O2 DJSISFGPUUYILV-ZFORQUDYSA-N 0.000 claims abstract description 87
- 229930190376 scutellarin Natural products 0.000 claims abstract description 87
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 16
- HIMJIPRMECETLJ-UHFFFAOYSA-N Wogonin Natural products COc1cc(O)c(O)c2C(=O)C=C(Oc12)c3ccccc3 HIMJIPRMECETLJ-UHFFFAOYSA-N 0.000 claims abstract description 8
- XLTFNNCXVBYBSX-UHFFFAOYSA-N wogonin Chemical compound COC1=C(O)C=C(O)C(C(C=2)=O)=C1OC=2C1=CC=CC=C1 XLTFNNCXVBYBSX-UHFFFAOYSA-N 0.000 claims abstract description 8
- 230000009385 viral infection Effects 0.000 claims abstract description 6
- 230000001154 acute effect Effects 0.000 claims abstract description 3
- 208000006454 hepatitis Diseases 0.000 claims abstract description 3
- 231100000283 hepatitis Toxicity 0.000 claims abstract description 3
- 230000000241 respiratory effect Effects 0.000 claims abstract description 3
- 208000011580 syndromic disease Diseases 0.000 claims abstract description 3
- 230000003612 virological effect Effects 0.000 claims abstract description 3
- 208000036142 Viral infection Diseases 0.000 claims abstract 3
- 206010022000 influenza Diseases 0.000 claims abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 63
- 239000007924 injection Substances 0.000 claims description 39
- 238000002347 injection Methods 0.000 claims description 39
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 27
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 26
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 26
- 239000002904 solvent Substances 0.000 claims description 26
- 239000003795 chemical substances by application Substances 0.000 claims description 20
- 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 19
- 239000002775 capsule Substances 0.000 claims description 19
- 239000008101 lactose Substances 0.000 claims description 18
- 239000003826 tablet Substances 0.000 claims description 18
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 17
- 229960003943 hypromellose Drugs 0.000 claims description 17
- -1 flavonoid compound Chemical class 0.000 claims description 16
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 15
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 14
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 14
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 14
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 14
- 239000007901 soft capsule Substances 0.000 claims description 13
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 12
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 12
- 229920000053 polysorbate 80 Polymers 0.000 claims description 12
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 11
- 239000007864 aqueous solution Substances 0.000 claims description 11
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 11
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 11
- 239000007787 solid Substances 0.000 claims description 10
- 239000003921 oil Substances 0.000 claims description 9
- 235000019198 oils Nutrition 0.000 claims description 9
- 239000002674 ointment Substances 0.000 claims description 9
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 9
- 229940068968 polysorbate 80 Drugs 0.000 claims description 9
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 8
- 239000003405 delayed action preparation Substances 0.000 claims description 8
- 239000000463 material Substances 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- IPQKDIRUZHOIOM-UHFFFAOYSA-N Oroxin A Natural products OC1C(O)C(O)C(CO)OC1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 IPQKDIRUZHOIOM-UHFFFAOYSA-N 0.000 claims description 7
- IKIIZLYTISPENI-ZFORQUDYSA-N baicalin Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 IKIIZLYTISPENI-ZFORQUDYSA-N 0.000 claims description 7
- 229960003321 baicalin Drugs 0.000 claims description 7
- AQHDANHUMGXSJZ-UHFFFAOYSA-N baicalin Natural products OC1C(O)C(C(O)CO)OC1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC=CC=1)O2 AQHDANHUMGXSJZ-UHFFFAOYSA-N 0.000 claims description 7
- 239000000725 suspension Substances 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- RTIXKCRFFJGDFG-UHFFFAOYSA-N chrysin Chemical class C=1C(O)=CC(O)=C(C(C=2)=O)C=1OC=2C1=CC=CC=C1 RTIXKCRFFJGDFG-UHFFFAOYSA-N 0.000 claims description 5
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 claims description 5
- 229930003935 flavonoid Natural products 0.000 claims description 5
- 235000017173 flavonoids Nutrition 0.000 claims description 5
- 239000000080 wetting agent Substances 0.000 claims description 5
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 4
- 239000004375 Dextrin Substances 0.000 claims description 4
- 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 4
- 235000019483 Peanut oil Nutrition 0.000 claims description 4
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 4
- 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 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
- 239000001506 calcium phosphate Substances 0.000 claims description 4
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 4
- 235000011010 calcium phosphates Nutrition 0.000 claims description 4
- 239000004202 carbamide Substances 0.000 claims description 4
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 4
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 4
- 235000019425 dextrin Nutrition 0.000 claims description 4
- 239000000284 extract Substances 0.000 claims description 4
- 238000001914 filtration Methods 0.000 claims description 4
- 239000000499 gel Substances 0.000 claims description 4
- 239000008103 glucose Substances 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 239000000312 peanut oil Substances 0.000 claims description 4
- 229920001993 poloxamer 188 Polymers 0.000 claims description 4
- 229920000136 polysorbate Polymers 0.000 claims description 4
- 238000010992 reflux Methods 0.000 claims description 4
- 239000008159 sesame oil Substances 0.000 claims description 4
- 235000011803 sesame oil Nutrition 0.000 claims description 4
- 159000000000 sodium salts Chemical class 0.000 claims description 4
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 4
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 3
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims description 3
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 238000000227 grinding Methods 0.000 claims description 3
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 claims description 3
- 239000006187 pill Substances 0.000 claims description 3
- 235000010265 sodium sulphite Nutrition 0.000 claims description 3
- 239000003549 soybean oil Substances 0.000 claims description 3
- 235000012424 soybean oil Nutrition 0.000 claims description 3
- 239000007921 spray Substances 0.000 claims description 3
- 239000000829 suppository Substances 0.000 claims description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 230000003078 antioxidant effect Effects 0.000 claims description 2
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- 239000000945 filler Substances 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 2
- 235000015424 sodium Nutrition 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 240000004534 Scutellaria baicalensis Species 0.000 claims 1
- 235000017089 Scutellaria baicalensis Nutrition 0.000 claims 1
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 235000013877 carbamide Nutrition 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
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- LKOJGSWUMISDOF-UHFFFAOYSA-N oroxylin A Chemical compound C=1C(=O)C2=C(O)C(OC)=C(O)C=C2OC=1C1=CC=CC=C1 LKOJGSWUMISDOF-UHFFFAOYSA-N 0.000 description 8
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- ZEMPKEQAKRGZGQ-AAKVHIHISA-N 2,3-bis[[(z)-12-hydroxyoctadec-9-enoyl]oxy]propyl (z)-12-hydroxyoctadec-9-enoate Chemical compound CCCCCCC(O)C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CC(O)CCCCCC)COC(=O)CCCCCCC\C=C/CC(O)CCCCCC ZEMPKEQAKRGZGQ-AAKVHIHISA-N 0.000 description 6
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Abstract
本发明涉及高纯度的黄芩素、其药物组合物、制备方法和医药用途，该高纯度的黄芩素按重量百分比计算含黄芩素为90％以上，另有汉黄芩素、千层纸素和白杨素等化合物；本发明的黄芩素及其药物组合物临床上用于治疗各种病毒感染的疾病，如肝炎、病毒性感冒、病毒感染引起的急性呼吸道综合症等。The invention relates to high-purity baicalein, its pharmaceutical composition, preparation method and medical application. The high-purity baicalein contains more than 90% of baicalein by weight percentage, and there are other wogonin, scutellarin and poplar Compounds such as baicalein; baicalein of the present invention and its pharmaceutical composition are clinically used to treat various viral infection diseases, such as acute respiratory syndrome caused by hepatitis, viral influenza, and viral infection.
Description
Technical field
The present invention relates to effective ingredient in Chinese, pharmaceutical composition and preparation method and purposes, specifically, the present invention relates to highly purified scutellarin, pharmaceutical composition and extraction process and medicinal use.
Background technology
The root of large-flowered skullcap is a kind of quite ancient Chinese medicine, has used more than one thousand years in China, and is safe and harmless, just is listed in middle product in Shennong's Herbal.Wherein the root of large-flowered skullcap that is used as medicine with root has the Yunnan root of large-flowered skullcap, Sutellaria viscidula, scutellaria rehderiana Diels, the Lijing root of large-flowered skullcap, scutellaria hypericifolia, the big root of large-flowered skullcap etc.The root of large-flowered skullcap has heat-clearing, purging intense heat, detoxifcation, hemostasis, effect such as antiabortive clinically, its mainly act on be anti-oxidant, remove free radical, anti-inflammatory, antitumor, stop calcium channel, suppress aldose reductase, antiviral, antianaphylaxis etc. and all there are provide protection in systems such as immunity, cardiovascular and cerebrovascular, digestion, nerve.
Root of large-flowered skullcap The Chemical Constituents is of long duration, Chinese scholars has been carried out systematic research to its chemical ingredients and pharmacological action, therefrom separate the flavonoid compound that obtains baicalin (baicalin) is arranged, wogonoside (wogonside), scutellarin (baicalein), wogonin (wogonin), qroxylin A (oroxylinA), skullcapflavone I (skullcapflavone I), and skullcapflavone II (skullcapflavone II) etc., mainly contain baicalin in its root, noroxylin, (the resource science research of the medicinal root of large-flowered skullcap of Song's ten thousand will of multiple flavones ingredients such as wogonoside unit.Acta Pharmaceutica Sinica 1981,16 (2): 139～145).
Flavones ingredient in the root of large-flowered skullcap has stronger pharmacologically active.Scutellarin (also claims noroxylin, baicalein) proved conclusively have antibacterial, diuresis, anti-inflammatory resistance attitude activity, scutellarin is antibacterial except that having, the diuresis, spasmolysis, and proof has stronger (the nearest progress of Ceng Guangfang natural flavonoid Shanghai medicine institute of the Chinese Academy of Sciences, 1963) such as antitumous effects.
Scutellarin (baicalein) also is called noroxylin, loses the product of a part glucuronic acid through hydrolysis for baicalin.It is different to practise the scutellarin that claims on this compound and some document, and the latter often refers to the flavonoid glycoside compound without hydrolysis, now claims baicalin (baicalin).
Summary of the invention
One of purpose of the present invention provides a kind of highly purified scutellarin.Highly purified scutellarin of the present invention, flavonoid compound with 5 structure, wherein to count by weight percentage be more than 90% to the content of scutellarin, also contains content and count by weight percentage and be lower than 10% wogonin, oroxylin and chrysin compound.
Two of purpose of the present invention provides a kind of method for preparing above-mentioned highly purified scutellarin.
Three of purpose of the present invention provide above-mentioned highly purified scutellarin and pharmaceutically the acceptable pharmaceutical carrier mix to form pharmaceutical composition, can be used for the disease of the various virus infectiones of clinical treatment.
Four of purpose of the present invention provide above-mentioned highly purified scutellarin with and the medicinal use of pharmaceutical composition.
For realizing above-mentioned goal of the invention, the present invention is by adopting following technical scheme.
A kind of highly purified scutellarin, flavonoid compound with 5 structure, wherein to count by weight percentage be more than 90% to the content of scutellarin, also contains content and count by weight percentage and be lower than 10% wogonin, oroxylin and chrysin compound.
A kind of pharmaceutical composition is mixed to form composition with acceptable pharmaceutical carrier pharmaceutically by above-mentioned described scutellarin; Preferred this pharmaceutical composition is tablet, capsule, soft capsule, sprays, gelifying agent, gel inhalation, oral preparation, suspensoid, electuary, patch, ointment, pill, powder, injection, infusion solution, freeze dried injection, lipidosome injection, target administration injection, suppository, sustained release preparation or controlled release preparation; Described tablet or capsule are preferably the conventional tablet or the capsule of described scutellarin and weighting agent or disintegrating agent assembly; Described sustained release preparation is preferably the slow releasing tablet or the slow releasing capsule of described scutellarin and weighting agent and hypromellose K4M assembly; Described soft capsule is preferably described scutellarin and is scattered in the soft capsule that obtains in the oil phase; Described ointment preferably prepares with the micro mist of described scutellarin.Described injection is preferably injection or the suspension type injection liquid that described scutellarin and solubilizing agent or solubility promoter form; Described freeze dried injection is preferably the freeze-drying injection powder pin of described scutellarin and S-WAT formation.
Above-mentioned weighting agent is preferably lactose, Microcrystalline Cellulose, dextrin, starch or calcium phosphate; Disintegrating agent is preferably hydroxypropylcellulose, sodium starch glycolate, polyvinylpolypyrrolidone or croscarmellose sodium; Optional tackiness agent, wetting agent and the lubricant of adding.
Wherein, described tablet or capsule are formed by following prescription: described scutellarin: lactose or Microcrystalline Cellulose: hydroxypropylcellulose or sodium starch glycolate, by weight calculating is 1: 0.5～2.5: 0.1～1.0, be preferably 1: 1.0～2.0: 0.4～and 0.6; Perhaps be described scutellarin: lactose or Microcrystalline Cellulose: hypromellose K4M is 1: 0.1～0.7: 0.15～0.8 by weight calculating, be preferably 1: 0.2～0.5: 0.4～and 0.8.
Wherein, described soft capsule, used oil phase is preferably soybean oil, poly(oxyethylene glycol) 400, Oleum Gossypii semen, peanut oil, sesame oil, Semen Maydis oil or sweet oil; Also can add solubilizing agent or latent solvent or oxidation inhibitor.
Wherein, described injection, used solubilizing agent are preferably Soxylat A 25-7 Viscotrol C, tween or pluronic F-68; Used solubility promoter is preferably S-WAT, urea, niacinamide, proline(Pro), glucose, Citric Acid or its sodium salt.
Wherein, described suspension type injection liquid, preferred embodiment be with the micro mist of described scutellarin and Polysorbate 80 mix grind after, be dissolved into the aqueous solution of phosphoric acid potassium dihydrogen, dipotassium hydrogen phosphate, nipagin esters and Xylo-Mucine, make through grinding.
Above-mentioned described highly purified scutellarin, be to prepare by following method: radix scutellariae medicinal materials with water-wet after in 20～30 ℃ the insulation 12～24 hours, with solvent 1 refluxing extraction, extracting solution concentrates the back with 70～100% alcohol reflux, make most of extract dissolving, the insoluble yellow solid of leaching, resulting yellow solid promptly obtains scutellarin through solvent 2 recrystallizations, solvent 1 wherein is an ethanol, ethyl acetate, acetone or its combination, solvent 2 is an acetone, chloroform, acetone and alcoholic acid mixed solution, the mixed solution of chloroform and alcoholic acid mixed solution or chloroform and acetone.
Pharmaceutical combination preparation of the present invention can be made various dosage forms, comprise tablet, capsule, soft capsule, sprays, gelifying agent, gel inhalation, oral preparation, suspensoid, electuary, patch, ointment, pill, powder, injection, infusion solution, freeze dried injection, lipidosome injection, target administration injection, suppository, sustained release preparation, controlled release preparation.Preferably tablet, capsule, slow releasing tablet and capsule, soft capsule, injection, freeze dried injection, suspensoid injectio, ointment.
Pharmaceutical composition of the present invention is characterised in that: the conventional tablet or the capsule that can be scutellarin and weighting agent, disintegrating agent assembly; Or the slow releasing tablet or the capsule of scutellarin and weighting agent and hypromellose K4M assembly; Wherein weighting agent can be selected lactose, Microcrystalline Cellulose, dextrin, starch, calcium phosphate etc. for use; Disintegrating agent can be selected hydroxypropylcellulose, sodium starch glycolate, polyvinylpolypyrrolidone, croscarmellose sodium etc. for use; Also optional tackiness agent, wetting agent and the lubricant of adding.
Preparation of pharmaceutical compositions tablet of the present invention or capsule prescription consist of: by weight, and scutellarin 1: lactose or Microcrystalline Cellulose 0.5～2.5: hydroxypropylcellulose or sodium starch glycolate 0.1～1.0; Perhaps, scutellarin 1: lactose or Microcrystalline Cellulose 0.1～0.7: hypromellose K4M 0.15～0.8.
Preferred prescription is: by weight, and scutellarin 1: lactose or Microcrystalline Cellulose 1.0～2.0: hydroxypropylcellulose or sodium starch glycolate 0.4～0.6; Perhaps, scutellarin 1: lactose or Microcrystalline Cellulose 0.2～0.5: hypromellose K4M 0.4～0.8.
Above-mentioned auxiliary material also can be selected for use, and disintegrating agent is as hydroxypropylated starch, hydroxypropylcellulose, sodium starch glycolate, calcium carboxymethylcellulose, polyvinylpolypyrrolidone, croscarmellose sodium etc.; Weighting agent is as lactose, sucrose, N.F,USP MANNITOL, Microcrystalline Cellulose, dextrin, starch, calcium phosphate, secondary calcium phosphate, calcium sulfate, lime carbonate, cyclodextrin, micro mist Mierocrystalline cellulose etc.; Wetting agent and tackiness agent are as pregelatinized Starch, polyvidone, Xylo-Mucine, hypromellose; Lubricant is as talcum powder, stearic acid, Magnesium Stearate, calcium stearate, micropowder silica gel, hydrogenated vegetable oil, Macrogol 4000 and 6000; Wetting agent is as sodium lauryl sulphate, tween 80; Framework material is as hypromellose, ethyl cellulose etc.
Medicinal composition soft capsule of the present invention is characterized in that: will make in scutellarin dispersion and the oil phase.Wherein oil phase can be soybean oil, Oleum Gossypii semen, peanut oil, sesame oil, Semen Maydis oil, olive wet goods; Also can add solubilizing agent or latent solvent and oxidation inhibitor etc.
Soft capsule of the present invention also can be selected following auxiliary material for use: solvent is as poly(oxyethylene glycol) 400, Oleum Gossypii semen, peanut oil, sesame oil, Semen Maydis oil, olive wet goods; Solubilizing agent or latent solvent are as tween 80, Soxylat A 25-7 Viscotrol C, peruscabin, ethyl lactate etc.; Oxidation inhibitor is as Tenox PG, t-butyl phenol (BHT), vitamin-E etc.The ratio of gelatin, glycerine and water can suitably be regulated in the glue shell, is advisable 1: 0.3～0.4: 0.7～1.4 as gelatin/glycerin/water three's ratio, also can add other compositions in the glue shell, as sanitas: P-hydroxybenzoic acid first, second, third, butyl ester etc.; Softening agent such as sorbyl alcohol etc.; Stablizer such as gum arabic etc.; Opalizer is as titanium dioxide, barium sulfate, precipitated calcium carbonate etc.
Drug combination injection of the present invention is characterised in that: with the Injectable solution of scutellarin and solubilizing agent or solubility promoter formation.Solubilizing agent can be selected Soxylat A 25-7 Viscotrol C, tween, pluronic F-68, polyvidone, polyoxyethylene glycol etc. for use; Solubility promoter can be selected S-WAT, potassium primary phosphate, urea, niacinamide, proline(Pro) for use, glucose, Citric Acid and sodium salt thereof etc.
The present invention can also form the injection freeze-dried powder with scutellarin and S-WAT.
Medicinal-composition suspension type injection liquid of the present invention is characterized in that: with scutellarin micro mist and Polysorbate 80 mix grind after, be dissolved into the aqueous solution of phosphoric acid potassium dihydrogen, dipotassium hydrogen phosphate, nipagin esters and Xylo-Mucine, make through grinding.
Injection of the present invention also can be selected following auxiliary material for use: solubilizing agent is as Tweens, pluronic F-68, polyoxyethylene glycol, Soxylat A 25-7 Viscotrol C, polyvidone etc.; Solubility promoter is as sodium bisulfite, yellow soda ash, sodium bicarbonate, potassium primary phosphate, primary ammonium phosphate etc.; Amides such as urea, ethanamide, thiocarbamide, benzamide etc., amino acids such as arginine, aspartic acid, Serine, glycine, methionine(Met), Histidine, L-glutamic acid, Isoleucine, Threonine, halfcystine, Gelucystine, tryptophane, phenylalanine, Methionin, the compound of hydroxyl or carboxyl such as sucrose, glucose, fructose, wood sugar, seminose, Citric Acid and sodium salt thereof, lactic acid, sodium salicylate etc.; Suspending agent is as Xylo-Mucine, polyvidone, HPMC etc.; Sanitas is as: Metagin, second, third and butyl ester; The pH regulator agent is as Citric Acid and citrate, phosphoric acid salt etc.; Oxidation inhibitor is as vitamins C, cysteine hydrochloride etc.; Solvent is as water for injection, injection ethanol, propylene glycol etc.
Pharmaceutical composition ointment of the present invention is characterized in that: prepare ointment with the scutellarin micro mist.
Every or every of medicinal compositions preferred oral formulation of the present invention contains scutellarin 40-120mg, and every of injection contains 20mg.
The amount of application of formula of the present invention (I) medicinal compositions can be according to variations such as the type of route of administration, patient age, body weight, body surface area, the disease of being treated and severity, and its per daily dose can be 40-720mg, preferred 40-240mg.Can use by one or many.
Above-mentioned described high purity scutellarin of the present invention and described pharmaceutical composition can be used for various virus infections, preferably use in the medicine of acute respiratory syndrome that preparation treatment hepatitis, viral cold, virus infection cause etc.
Embodiment
For a better understanding of the present invention, further set forth the present invention, but should not be understood that the present invention is had any restriction below by specific embodiment.
Embodiment 1
Get radix scutellariae medicinal materials 20kg and be ground into meal, add water-wet, and, use alcohol reflux three times in 20～30 ℃ of incubated overnight.Decompression recycling ethanol does not steam to there being ethanol, resistates adds 85% ethanol, heating makes most of dissolving, filters, and gets insolubles (for yellow solid), use acetone recrystallization, filter, get the about 200g of scutellarin, through purity test, be mainly scutellarin (content is greater than 90%), also contain a small amount of wogonin, oroxylin and chrysin compound (content is less than 10%).
Embodiment 2
Get radix scutellariae medicinal materials 20kg and be ground into meal, add water-wet, and, extract three times with ethyl acetate backflow in 20～30 ℃ of incubated overnight.Reclaim under reduced pressure does not steam to there being ethyl acetate, resistates adds 75% ethanol, heating makes most of dissolving, filters, and gets insolubles (for yellow solid), use the chloroform recrystallization, filter, get the about 200g of scutellarin, through purity test, be mainly scutellarin (content is greater than 90%), also contain a small amount of wogonin, oroxylin and chrysin compound (content is less than 10%).
Embodiment 3
The preparation of scutellarin capsule
Prescription: scutellarin 40mg
Lactose 80mg
Hydroxypropylcellulose 20mg
Polysorbate 80 16mg
3% HPMC (E5) aqueous solution is an amount of
Talcum powder 2.5mg
With scutellarin, lactose, hydroxypropylcellulose is crossed 60 mesh sieves and is mixed, and adds an amount of Polysorbate 80, adds 3% HPMC (E5) aqueous solution and makes softwood in right amount, crosses 20 mesh sieves and granulates.40-50 ℃ of baking oven forced air drying.Dried particle is crossed the whole grain of 20 mesh sieves, adds the talcum powder of recipe quantity, mixes.Press No. 1 capsule of recipe quantity can, every contains scutellarin 40mg.Usage: every day three times, each two.
Embodiment 4
The preparation of scutellarin tablet
Prescription: scutellarin 40mg
Lactose 80mg
Hydroxypropylcellulose 20mg
Polysorbate 80 16mg
3% HPMC (E5) aqueous solution is an amount of
Talcum powder 2.5mg
Scutellarin, lactose, hydroxypropylcellulose are crossed 60 mesh sieves be mixed, add an amount of Polysorbate 80, add 3% HPMC (E5) aqueous solution and make softwood in right amount, cross 20 mesh sieves and granulate.40-50 ℃ of baking oven forced air drying.Dried particle is crossed the whole grain of 20 mesh sieves, adds the talcum powder of recipe quantity, mix, and compressing tablet, every contains scutellarin 40mg.Usage: every day three times, each two.
Embodiment 5
The preparation of scutellarin slow releasing capsule
Prescription: scutellarin 120mg
Polyvidone 60mg
Microcrystalline Cellulose 40mg
Hypromellose E15 20mg
Hypromellose K4M 80mg
3% HPMC (E5) aqueous solution is an amount of
Talcum powder 4mg
Scutellarin and polyvidone are dissolved in the ethanol, and reduction vaporization is removed ethanol, and the gained solid is placed on and spends the night in the vacuum drier to eliminate ethanol.Above-mentioned solid and Microcrystalline Cellulose, hypromellose E15, hypromellose K4M are crossed 60 mesh sieves and be mixed, add 3% HPMC (E5) aqueous solution and make softwood in right amount, cross 20 mesh sieves and granulate.40-50 ℃ of baking oven forced air drying.Dried particle is crossed the whole grain of 20 mesh sieves, adds the talcum powder of recipe quantity, mixes.Press recipe quantity can capsule, every contains scutellarin 120mg.Usage: every day secondary, each one.
Embodiment 6
The preparation of scutellarin slow releasing tablet
Prescription: scutellarin 120mg
Polyvidone 60mg
Lactose 40mg
Hypromellose E15 20mg
Hypromellose K4M 80mg
3% HPMC (E5) aqueous solution is an amount of
Talcum powder 4mg
Just scutellarin and polyvidone are dissolved in the ethanol, and reduction vaporization is removed ethanol, and the gained solid is placed on and spends the night in the vacuum drier to eliminate ethanol.Above-mentioned solid and lactose, hypromellose E15, hypromellose K4M are crossed 60 mesh sieves and be mixed, add 3% HPMC (E5) aqueous solution and make softwood in right amount, cross 20 mesh sieves and granulate.40-50 ℃ of baking oven forced air drying.Dried particle is crossed the whole grain of 20 mesh sieves, adds the talcum powder of recipe quantity, mix, and compressing tablet, every contains scutellarin 120mg.Usage: every day secondary, each a slice.
Embodiment 7
The scutellarin soft capsule
Prescription: every of content contains the glue shell
Scutellarin 40mg gelatin 46.00%
PEG400 0.5ml glycerine 17.82%
Water 36.18%
Get scutellarin and be dissolved among the PEG400, this solution is made soft capsule.Every contains scutellarin 40mg.
Embodiment 8
The scutellarin injection
Prescription: scutellarin 20mg
Soxylat A 25-7 Viscotrol C 1.0mg
Water for injection adds to 5.0mL
Scutellarin is dissolved in dehydrated alcohol, add Soxylat A 25-7 Viscotrol C (CremophorELP), mixing, reduction vaporization is removed ethanol, add an amount of water for injection and be mixed into clear solution, through 0.22 μ m filtering with microporous membrane, coating-dividing sealing, in 100 ℃ of flowing steam sterilizations 30 minutes promptly, every contains scutellarin 20mg.
Embodiment 9
The scutellarin injection
Prescription: scutellarin 2.0g
S-WAT 4.0g
Polyvidone 10.0g
Ethanol 50mL
Water for injection adds to 1000mL
Scutellarin is dispersed in the ethanol, and S-WAT is soluble in water, under ultrasonic or agitation condition sodium sulfite solution is added in the scutellarin gradually, makes into clear solution; Add polyvidone, stir and make dissolving, add water for injection to capacity; Through 0.22 μ m filtering with microporous membrane, coating-dividing sealing, in 100 ℃ of flowing steam sterilizations 30 minutes promptly, every contains scutellarin 20mg.
Embodiment 10
Injection scutellarin (powder injection)
Prescription: scutellarin 20mg
S-WAT 40mg
Polyvidone 50mg
N.F,USP MANNITOL 100mg
Scutellarin is dispersed in 15% ethanol, S-WAT is added, ultrasonicly make dissolving, add polyvidone and N.F,USP MANNITOL, stir and make dissolving; Add needle-use activated carbon by 0.1%, stirred 15 minutes, and took off the charcoal suction filtration in the container of cleaning, add water for injection to capacity through the titanium core, solution stirring was made evenly in 5 minutes, again through 0.22 μ m filtering with microporous membrane, the filtrate can in the 7ml cillin bottle, every bottle of 2ml, butyl rubber bung beyond the Great Wall partly then, deliver on the flaggy in the freeze drying box, insert temp probe, close chamber door.Press the freeze-drying curve lyophilize, the final drying temperature is more than 35 ℃ and kept 2 hours.Close plug, venting, outlet rolls lid.Every contains scutellarin 20mg.
Embodiment 11
Scutellarin suspension type injection
Prescription: scutellarin 20mg
Xylo-Mucine 10mg
Polysorbate 80 0.1mg
Ethyl p-hydroxybenzoate 0.5mg
Propylben 0.5mg
Potassium primary phosphate 16.7mg
Dipotassium hydrogen phosphate 1.7mg
Water for injection adds to 2ml
Scutellarin is carried out comminution by gas stream, get the following micro mist of particle diameter 10 μ m.Potassium primary phosphate and dipotassium hydrogen phosphate are dissolved in the water for injection, add ethyl p-hydroxybenzoate and propyl ester, add Xylo-Mucine again, make whole dissolvings under 60 ℃ of conditions.Scutellarin after the micronization is placed container, add Polysorbate 80 and be ground into thin pasty state, above-mentioned solution is added gradually, after stirring, grind 5 to 10 times through colloidal mill.Routinely measuring method measure content qualified after, be divided in the ampoule, in 100 ℃ of flowing steam sterilizations 30 minutes promptly, every contains scutellarin 20mg.
Embodiment 12
Scutellarin ointment
Prescription: scutellarin 50g
Glyceryl monostearate 120g
Paraffin 50g
Beeswax 50g
White vaseline 50g
Whiteruss 250g
Sorbester p17 20g
Tween 80 10g
Ethyl p-hydroxybenzoate 1g
Distilled water adds to 1000g
Scutellarin ground be impalpable powder, prepare O/W type emulsifiable paste by emulsion process.
Claims (10)
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| CN 200310110338 CN1245398C (en) | 2003-12-31 | 2003-12-31 | Extraction process, medicinal composition and preparation process of baicalein |
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Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1313459C (en) * | 2005-06-07 | 2007-05-02 | 山东大学 | Total flavone glycoside extract of Radix scutellariae, Rodix scutellariae monomer flavone glycoside, its preparation and use |
| CN1325048C (en) * | 2005-11-09 | 2007-07-11 | 中国药科大学 | Application of wogonin for preparing medicine to treat or prevent hepatitis B |
| CN103454373A (en) * | 2012-06-01 | 2013-12-18 | 贵州百灵企业集团制药股份有限公司 | Method for detecting medicament for treating dysmenorrhea |
| CN103933002A (en) * | 2014-05-06 | 2014-07-23 | 鲁南制药集团股份有限公司 | Scutellaria baicalensis total flavonoid sustained release tablet and preparation method thereof |
| CN104610401A (en) * | 2015-02-25 | 2015-05-13 | 山东省中医药研究院 | Method for simultaneously extracting baicalin, baicalein and wogonin from scutellaria baicalensis |
| CN104829577A (en) * | 2015-05-07 | 2015-08-12 | 诸城市浩天药业有限公司 | Baicalein gamma crystal form, preparation method, pharmaceutical composition and applications thereof |
| CN106176935A (en) * | 2016-07-16 | 2016-12-07 | 南京正宽医药科技有限公司 | A kind of baicalin aluminium glue capsule and preparation method thereof |
| CN106333943A (en) * | 2016-11-11 | 2017-01-18 | 中国药科大学 | Oroxylin preparation |
| CN107648310A (en) * | 2016-07-24 | 2018-02-02 | 复旦大学 | High-purity Scullcap total-flavonoid and preparation method thereof and its medicinal usage |
| CN111329896A (en) * | 2020-01-19 | 2020-06-26 | 中国药科大学 | Anti-influenza pharmaceutical composition and application thereof |
| CN112675131A (en) * | 2021-02-02 | 2021-04-20 | 中国药科大学 | Oroxylin pharmaceutical composition and application thereof in preparation of liver cancer drugs |
| CN113521127A (en) * | 2021-08-04 | 2021-10-22 | 北京亿睿达科技有限公司 | Preparation method of preparation with baicalein as main medicinal component for animals |
| CN117338717A (en) * | 2023-10-18 | 2024-01-05 | 南京芩领医药科技有限公司 | A kind of external preparation of baicalein and its application in the treatment of atopic dermatitis |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1313459C (en) * | 2005-06-07 | 2007-05-02 | 山东大学 | Total flavone glycoside extract of Radix scutellariae, Rodix scutellariae monomer flavone glycoside, its preparation and use |
| CN1325048C (en) * | 2005-11-09 | 2007-07-11 | 中国药科大学 | Application of wogonin for preparing medicine to treat or prevent hepatitis B |
| CN103454373A (en) * | 2012-06-01 | 2013-12-18 | 贵州百灵企业集团制药股份有限公司 | Method for detecting medicament for treating dysmenorrhea |
| CN103933002A (en) * | 2014-05-06 | 2014-07-23 | 鲁南制药集团股份有限公司 | Scutellaria baicalensis total flavonoid sustained release tablet and preparation method thereof |
| CN104610401B (en) * | 2015-02-25 | 2017-03-15 | 山东省中医药研究院 | A kind of method for extracting baicalin, baicalin and wogonin from Radix Scutellariae simultaneously |
| CN104610401A (en) * | 2015-02-25 | 2015-05-13 | 山东省中医药研究院 | Method for simultaneously extracting baicalin, baicalein and wogonin from scutellaria baicalensis |
| CN104829577A (en) * | 2015-05-07 | 2015-08-12 | 诸城市浩天药业有限公司 | Baicalein gamma crystal form, preparation method, pharmaceutical composition and applications thereof |
| CN106176935A (en) * | 2016-07-16 | 2016-12-07 | 南京正宽医药科技有限公司 | A kind of baicalin aluminium glue capsule and preparation method thereof |
| CN107648310A (en) * | 2016-07-24 | 2018-02-02 | 复旦大学 | High-purity Scullcap total-flavonoid and preparation method thereof and its medicinal usage |
| CN107648310B (en) * | 2016-07-24 | 2021-05-04 | 复旦大学 | High-purity total flavonoids of Scutellaria baicalensis and preparation method and medicinal use thereof |
| CN106333943A (en) * | 2016-11-11 | 2017-01-18 | 中国药科大学 | Oroxylin preparation |
| CN111329896A (en) * | 2020-01-19 | 2020-06-26 | 中国药科大学 | Anti-influenza pharmaceutical composition and application thereof |
| CN112675131A (en) * | 2021-02-02 | 2021-04-20 | 中国药科大学 | Oroxylin pharmaceutical composition and application thereof in preparation of liver cancer drugs |
| CN113521127A (en) * | 2021-08-04 | 2021-10-22 | 北京亿睿达科技有限公司 | Preparation method of preparation with baicalein as main medicinal component for animals |
| CN117338717A (en) * | 2023-10-18 | 2024-01-05 | 南京芩领医药科技有限公司 | A kind of external preparation of baicalein and its application in the treatment of atopic dermatitis |
| CN117338717B (en) * | 2023-10-18 | 2024-12-17 | 南京芩领医药科技有限公司 | A baicalein external preparation and its application in treating atopic dermatitis |
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