CN102755331A - Asiatic acid salt hard capsule and preparation method thereof - Google Patents
Asiatic acid salt hard capsule and preparation method thereof Download PDFInfo
- Publication number
- CN102755331A CN102755331A CN2011101130649A CN201110113064A CN102755331A CN 102755331 A CN102755331 A CN 102755331A CN 2011101130649 A CN2011101130649 A CN 2011101130649A CN 201110113064 A CN201110113064 A CN 201110113064A CN 102755331 A CN102755331 A CN 102755331A
- Authority
- CN
- China
- Prior art keywords
- hard capsule
- hydrochlorate
- herba centellae
- asiatic acid
- lubricant
- 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.)
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Links
- 239000007902 hard capsule Substances 0.000 title claims abstract description 55
- JXSVIVRDWWRQRT-UYDOISQJSA-N asiatic acid Chemical class C1[C@@H](O)[C@H](O)[C@@](C)(CO)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CC[C@@H](C)[C@H](C)[C@H]5C4=CC[C@@H]3[C@]21C JXSVIVRDWWRQRT-UYDOISQJSA-N 0.000 title abstract description 9
- 238000002360 preparation method Methods 0.000 title abstract description 5
- -1 asiatic acid amino butantriol salt Chemical class 0.000 claims abstract description 33
- 229940011658 asiatic acid Drugs 0.000 claims abstract description 21
- LBGFKBYMNRAMFC-PYSQTNCISA-N asiatic acid Natural products C[C@@H]1CC[C@@]2(CC[C@]3(C)C(=CC[C@@H]4[C@@]5(C)C[C@@H](O)[C@H](O)[C@@](C)(CO)[C@@H]5CC[C@@]34C)[C@]2(C)[C@H]1C)C(=O)O LBGFKBYMNRAMFC-PYSQTNCISA-N 0.000 claims abstract description 21
- CLXOLTFMHAXJST-UHFFFAOYSA-N esculentic acid Natural products C12CC=C3C4CC(C)(C(O)=O)CCC4(C(O)=O)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(CO)C CLXOLTFMHAXJST-UHFFFAOYSA-N 0.000 claims abstract description 21
- 239000000945 filler Substances 0.000 claims abstract description 15
- 239000000314 lubricant Substances 0.000 claims abstract description 15
- 239000002994 raw material Substances 0.000 claims abstract description 12
- 238000000034 method Methods 0.000 claims abstract description 10
- 238000002156 mixing Methods 0.000 claims abstract description 9
- 239000011230 binding agent Substances 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 13
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 10
- 239000012467 final product Substances 0.000 claims description 8
- 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 5
- 239000008101 lactose Substances 0.000 claims description 5
- 235000019359 magnesium stearate Nutrition 0.000 claims description 5
- 239000005995 Aluminium silicate Substances 0.000 claims description 4
- 239000001856 Ethyl cellulose Substances 0.000 claims description 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical group CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 235000012211 aluminium silicate Nutrition 0.000 claims description 4
- 229910000323 aluminium silicate Inorganic materials 0.000 claims description 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 4
- 229920001249 ethyl cellulose Polymers 0.000 claims description 4
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- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- WGYFACNYUJGZQO-UHFFFAOYSA-N aminomethanetriol Chemical compound NC(O)(O)O WGYFACNYUJGZQO-UHFFFAOYSA-N 0.000 claims description 3
- 238000012856 packing Methods 0.000 claims description 2
- PZZYQPZGQPZBDN-UHFFFAOYSA-N aluminium silicate Chemical compound O=[Al]O[Si](=O)O[Al]=O PZZYQPZGQPZBDN-UHFFFAOYSA-N 0.000 claims 1
- 239000000853 adhesive Substances 0.000 abstract 1
- 230000001070 adhesive effect Effects 0.000 abstract 1
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- 229920000178 Acrylic resin Polymers 0.000 description 8
- 239000004925 Acrylic resin Substances 0.000 description 8
- 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 description 8
- 229930006000 Sucrose Natural products 0.000 description 8
- 239000005720 sucrose Substances 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- 239000004698 Polyethylene Substances 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
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- 239000002671 adjuvant Substances 0.000 description 5
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 4
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- 239000004373 Pullulan Substances 0.000 description 4
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- 229920000881 Modified starch Polymers 0.000 description 3
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 3
- 229920002301 cellulose acetate Polymers 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
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- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
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- 241000609240 Ambelania acida Species 0.000 description 2
- SOGAXMICEFXMKE-UHFFFAOYSA-N Butylmethacrylate Chemical compound CCCCOC(=O)C(C)=C SOGAXMICEFXMKE-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 2
- 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 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 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
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- 229920003148 Eudragit® E polymer Polymers 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
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- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229920002125 Sokalan® Polymers 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- KGUHOFWIXKIURA-VQXBOQCVSA-N [(2r,3s,4s,5r,6r)-6-[(2s,3s,4s,5r)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]oxy-3,4,5-trihydroxyoxan-2-yl]methyl dodecanoate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)CCCCCCCCCCC)O[C@@H]1O[C@@]1(CO)[C@@H](O)[C@H](O)[C@@H](CO)O1 KGUHOFWIXKIURA-VQXBOQCVSA-N 0.000 description 2
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- 239000001785 acacia senegal l. willd gum Substances 0.000 description 2
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 2
- 229940072056 alginate Drugs 0.000 description 2
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- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 description 2
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- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 2
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- 229910001628 calcium chloride Inorganic materials 0.000 description 2
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- IQDXNHZDRQHKEF-UHFFFAOYSA-N dialuminum;dicalcium;dioxido(oxo)silane Chemical compound [Al+3].[Al+3].[Ca+2].[Ca+2].[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O IQDXNHZDRQHKEF-UHFFFAOYSA-N 0.000 description 2
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- RSWGJHLUYNHPMX-ONCXSQPRSA-N abietic acid Chemical compound C([C@@H]12)CC(C(C)C)=CC1=CC[C@@H]1[C@]2(C)CCC[C@@]1(C)C(O)=O RSWGJHLUYNHPMX-ONCXSQPRSA-N 0.000 description 1
- 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 description 1
- 239000000654 additive Substances 0.000 description 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
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- 239000007900 aqueous suspension Substances 0.000 description 1
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- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 229960002713 calcium chloride Drugs 0.000 description 1
- UHHRFSOMMCWGSO-UHFFFAOYSA-L calcium glycerophosphate Chemical compound [Ca+2].OCC(CO)OP([O-])([O-])=O UHHRFSOMMCWGSO-UHFFFAOYSA-L 0.000 description 1
- 229940095618 calcium glycerophosphate Drugs 0.000 description 1
- 235000019299 calcium glycerylphosphate Nutrition 0.000 description 1
- BRPQOXSCLDDYGP-UHFFFAOYSA-N calcium oxide Chemical compound [O-2].[Ca+2] BRPQOXSCLDDYGP-UHFFFAOYSA-N 0.000 description 1
- 239000000292 calcium oxide Substances 0.000 description 1
- ODINCKMPIJJUCX-UHFFFAOYSA-N calcium oxide Inorganic materials [Ca]=O ODINCKMPIJJUCX-UHFFFAOYSA-N 0.000 description 1
- 235000012241 calcium silicate Nutrition 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
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- 229920001525 carrageenan Polymers 0.000 description 1
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- 239000003086 colorant Substances 0.000 description 1
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- 150000002148 esters Chemical class 0.000 description 1
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- 239000001761 ethyl methyl cellulose Substances 0.000 description 1
- 230000003176 fibrotic effect Effects 0.000 description 1
- 235000021433 fructose syrup Nutrition 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
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- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
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- 238000010438 heat treatment Methods 0.000 description 1
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- 238000006460 hydrolysis reaction Methods 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
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- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 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 description 1
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 1
- 229960000367 inositol Drugs 0.000 description 1
- TWNIBLMWSKIRAT-VFUOTHLCSA-N levoglucosan Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@H]2CO[C@@H]1O2 TWNIBLMWSKIRAT-VFUOTHLCSA-N 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- HGPXWXLYXNVULB-UHFFFAOYSA-M lithium stearate Chemical compound [Li+].CCCCCCCCCCCCCCCCCC([O-])=O HGPXWXLYXNVULB-UHFFFAOYSA-M 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
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- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
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- 239000003595 mist Substances 0.000 description 1
- 235000019426 modified starch Nutrition 0.000 description 1
- 229920003052 natural elastomer Polymers 0.000 description 1
- 229920001194 natural rubber Polymers 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000003605 opacifier Substances 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229960000502 poloxamer Drugs 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920003229 poly(methyl methacrylate) Polymers 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920002857 polybutadiene Polymers 0.000 description 1
- 229920001083 polybutene Polymers 0.000 description 1
- 239000004926 polymethyl methacrylate Substances 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000010408 potassium alginate Nutrition 0.000 description 1
- 239000000737 potassium alginate Substances 0.000 description 1
- MZYRDLHIWXQJCQ-YZOKENDUSA-L potassium alginate Chemical compound [K+].[K+].O1[C@@H](C([O-])=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C([O-])=O)O[C@@H](O)[C@@H](O)[C@H]1O MZYRDLHIWXQJCQ-YZOKENDUSA-L 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- OQZCJRJRGMMSGK-UHFFFAOYSA-M potassium metaphosphate Chemical compound [K+].[O-]P(=O)=O OQZCJRJRGMMSGK-UHFFFAOYSA-M 0.000 description 1
- 229940099402 potassium metaphosphate Drugs 0.000 description 1
- 229940114930 potassium stearate Drugs 0.000 description 1
- ANBFRLKBEIFNQU-UHFFFAOYSA-M potassium;octadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCCCC([O-])=O ANBFRLKBEIFNQU-UHFFFAOYSA-M 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- RUOJZAUFBMNUDX-UHFFFAOYSA-N propylene carbonate Chemical compound CC1COC(=O)O1 RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 description 1
- 229940032159 propylene carbonate Drugs 0.000 description 1
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229940045870 sodium palmitate Drugs 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- GGXKEBACDBNFAF-UHFFFAOYSA-M sodium;hexadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCC([O-])=O GGXKEBACDBNFAF-UHFFFAOYSA-M 0.000 description 1
- HUAUNKAZQWMVFY-UHFFFAOYSA-M sodium;oxocalcium;hydroxide Chemical compound [OH-].[Na+].[Ca]=O HUAUNKAZQWMVFY-UHFFFAOYSA-M 0.000 description 1
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- BAZVSMNPJJMILC-UHFFFAOYSA-N triadimenol Chemical compound C1=NC=NN1C(C(O)C(C)(C)C)OC1=CC=C(Cl)C=C1 BAZVSMNPJJMILC-UHFFFAOYSA-N 0.000 description 1
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
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- LPEBYPDZMWMCLZ-CVBJKYQLSA-L zinc;(z)-octadec-9-enoate Chemical compound [Zn+2].CCCCCCCC\C=C/CCCCCCCC([O-])=O.CCCCCCCC\C=C/CCCCCCCC([O-])=O LPEBYPDZMWMCLZ-CVBJKYQLSA-L 0.000 description 1
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Landscapes
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses an asiatic acid salt hard capsule and a preparation method thereof. An asiatic acid salt hard capsule formula comprises 5-40 percent of an asiatic acid amino butantriol salt, 50-95 percent of a filling agent, 0-10 percent of a lubricating agent and 0-2.0 percent of an adhesive, wherein the percentage refers to the mass percentage of each component in the total amount of asiatic acid salt hard capsule contents. The method comprises the following steps of: uniformly mixing the raw materials according to a formula; and filling into the conventional hard capsule shell. The asiatic acid salt hard capsule disclosed by the invention has high bioavailability.
Description
Technical field
The present invention relates to a kind of Herba Centellae hydrochlorate hard capsule and preparation method thereof.
Background technology
Report asiatic acid and salt thereof can be prevented and treated the fibrotic disease of some internal organs in the prior art, and still, the drug effect of relevant hard capsule is unsatisfactory, and bioavailability is extremely low, effectively utilizes this medicine for maximizing, and this present situation needs to be resolved hurrily.
Summary of the invention
Technical problem to be solved by this invention is that to have overcome the drug effect of existing asiatic acid and salt hard capsule thereof unsatisfactory, and the extremely low defective of bioavailability, and a kind of Herba Centellae hydrochlorate hard capsule with good biological availability and preparation method thereof is provided.
Herba Centellae hydrochlorate hard capsule prescription of the present invention contains 5%～40% asiatic acid tromethane salt, 50%～95% filler, 0%～10% lubricant and 0%～2.0% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
Among the present invention, described asiatic acid tromethane salt is the conventional described asiatic acid tromethane salt in this area, commercially available get or extract by the asiatic acid raw material according to this area conventional method obtain.
Among the present invention; Described filler is the conventional described filler in this area; Can use diluent for water-soluble diluent, water-insoluble diluent or direct compression; Preferable in trihydroxy aminomethane, sorbitol, sorbitol instant, D-xylose, xylitol, propylene carbonate, calcium glycerophosphate, mannitol, the corn starch of can sterilizing, compressible sugar, polyvinylpolypyrrolidone, inositol, Thomas balsam, maltose alcohol, soda-lime, alpha-lactose, lactose, aluminium hydroxide, medicinal sugar, calcium oxide, zinc oxide, prepared teobroma, pregelatinized Starch, Powderd cellulose, colloidality silicon dioxide, aluminium silicate, Aluminum calcium silicate., starch, sodium chloride, calcium chloride, aluminum chloride, calcium sulfate, glucose, Pulvis Talci, microcrystalline Cellulose, bagasse regrowth, carboxymethylcellulose calcium, polyethylene, polyethylene azoxy ketone, polyvinyl butyral resin, polyethylene acetal diethyl acetate ester, calcium carbonate, magnesium carbonate, magnesium oxide, sucrose, spherical sucrose, compressible sugar, sugar,confectioner's, dextrin, white dextrin, calcium phosphate and the sodium starch phosphate one or more, one or more that better is in microcrystalline Cellulose, lactose and the trihydroxy aminomethane.
Among the present invention; Described lubricant is the conventional described lubricant in this area; Be generally kollag; In preferable is hard paraffin, Palmic acid, synthetic wax, zinc oleate, lithium stearate, potassium stearate, calcium stearate, boric acid, calcium silicates, aluminium silicate, Aluminum calcium silicate., magnesium silicate, silicone rubber, liquid paraffin, hard esteramides, stearic palmitamide, stearic acid, isostearic acid, sodium stearate, hard soap, curdled milk soap, sodium stearate, cobaltous octadecanate, zinc stearate, magnesium stearate, Pulvis Talci, sodium palmitate, Oleum Ricini, SHCO, Polyethylene Glycol, sucrose fatty acid ester, sucrose monolaurate, sucrose palmitic acid ester, olive oil and the calcium phosphate one or more, better is magnesium stearate and/or aluminium silicate.
Among the present invention; Described binding agent is the conventional described binding agent in this area, preferable is ethylmethylcellulose, ethyl cellulose, ethyl cellulose aqueous suspension, butadiene-styrene rubber, natural rubber, acrylic acid, butylacrylate, acrylic acid methyl ester., acrylic resin I number, acrylic resin II number, acrylic resin III number, acrylic resin IV number, Eudragit E
30, chitin, chitose, methyl methacrylate, EMA, butyl methacrylate, EUDRAGIT S100, Eudragit E, acrylic resin L, acrylic resin S, acrylic resin RL, acrylic resin RS, metering system-2-ethoxy, methacrylic acid-2-hydroxypropyl acrylate, methylcellulose, glycerol three rosin esters, zein, compressible sugar, sesbania gum, tara gum, Ficus elastica, carbomer, Petropols, Furcellaran, tragacanth, arabic gum, Resina persicae, maltose alcohol, carrageenin, tamarind gum, high fructose syrup, Nulomoline, fructose, Colophonium, loose glue, POLY-karaya, modified starch, poloxamer, medicinal sugar, alginic acid, sodium alginate, potassium alginate, ammonium alginate, calcium alginate, pregelatinized Starch, Powderd cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, xanthan gum, aluminium-magnesium silicate, terpene resin, liquid glucose, starch, sodium starch glycol, potassium metaphosphate, scleroglucan, glucose, glucosan, Pullulan, acetyl group Pullulan, microbial alginate, microcrystalline Cellulose, bagasse regrowth, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, Mel, guaiac gum, polyethylene, polyethylene azoxy ketone, polyvinyl butyral resin, polyethylene acetal diethyl acetate ester, polybutene, polybutadiene, polymethyl methacrylate, gather methyl 2-methylmethacrylate copolymer, gather methyl and gather L-methyl methacrylate, sodium polyacrylate, polyacrylic acid, polyisobutylene, Parleam, polystyrene-maleic anhydride, polyvinyl-maleic anhydride, gather in 2-ethoxy formyl acrylic ester, polyvidone, polyvinyl acetate, sucrose, spherical sucrose, compressible sugar, sugar,confectioner's, sucrose fatty acid ester, sucrose monolaurate, sucrose palmitic acid ester, locust bean gum, dextrin, white dextrin, cellulose acetate, a cellulose acetate, cellulose diacetate, Triafol T, cellulose acetate dibutylamino-hydrox-ypropyl ether and the sodium starch phosphate one or more, better is ethyl cellulose.
Preferable being made up of 5%～40% asiatic acid tromethane salt, 50%～95% filler, 0%～10% lubricant and 0%～2.0% binding agent of Herba Centellae hydrochlorate hard capsule prescription of the present invention, percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
The invention still further relates to the Herba Centellae hydrochlorate hard capsule preferred embodiments of filling a prescription and contain 15%～30% asiatic acid tromethane salt, 65%～85% filler, 2%～5% lubricant and 0%～2.0% binding agent, percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
The invention still further relates to the Herba Centellae hydrochlorate hard capsule another preferred embodiments of filling a prescription and be made up of 15%～30% asiatic acid tromethane salt, 65%～85% filler, 2%～5% lubricant and 0%～2.0% binding agent, percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
The invention still further relates to another preferred embodiments of Herba Centellae hydrochlorate hard capsule prescription and contain 16.64%～37.88% asiatic acid tromethane salt, 60.61%～83.19% filler, 0.12%～1.52% lubricant and 0～4.76% binding agent, percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
Wherein, the kind of described filler, lubricant and binding agent all as previously mentioned.
The invention still further relates to Herba Centellae hydrochlorate hard capsule prescription again a preferred embodiments comprise 16.7% asiatic acid tromethane salt, 81.3% lactose and 2% magnesium stearate, percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
Herba Centellae hydrochlorate hard capsule of the present invention can also contain conventional various other additives that add in this area and other active component, as long as it does not have antagonism or not appreciable impact hard capsule effect of the present invention.
Among the present invention; The capsule shells of described Herba Centellae hydrochlorate hard capsule is the conventional hard capsule case that uses in this area; The gel and the water that generally contain conventional usefulness, and one or more compositions of following substances: plasticizer, thickening agent, opacifier, coloring agent, antiseptic and cosolvent etc.
Wherein, Described gel is that this area routine is used, one or more that preferable is in formalin, glycerol, arabic gum, gelatin, POLY-karaya, alginic acid, sodium alginate, calcium alginate, calcium chloride, Pullulan, acetyl group Pullulan, microbial alginate and the Polyethylene Glycol.
Wherein, described capsule shells generally can be made by following method: under vacuum condition, agitating heating becomes glue with capsule shells raw material uniform mixing, and system capsule mechanism capsule gets final product.
Herba Centellae hydrochlorate hard capsule of the present invention can make by this area conventional method, and preferable method for preparing comprises the steps: that by prescription behind each raw material uniform mixing, the conventional hard capsule case in this area of packing into gets final product.
Wherein, described raw material incapsulates the component of shell by the capsule shells volumeter, and capacity such as 0.15mL, 0.25mL, 0.30mL, 0.40mL, 0.55mL and 0.75mL are generally arranged.
Agents useful for same of the present invention and raw material are all commercially available to be got.
On the basis that meets this area general knowledge, each above-mentioned among the present invention technical characterictic optimum condition can combination in any obtain preferred embodiments.
Positive progressive effect of the present invention is: Herba Centellae hydrochlorate hard capsule of the present invention has the good biological availability, and quality stability is good, is difficult for crisp broken; The disintegrate index is stable; Facile hydrolysis not, long-time placement surface is not sent out the mist jaundice, and extensive market prospects and practical value are arranged.
The specific embodiment
Mode through embodiment further specifies the present invention below, but does not therefore limit the present invention among the described scope of embodiments.
Embodiment 1
Method for preparing: by last table prescription,, be filled in the capsule shells and get final product with medicine and each raw material blending of adjuvant.
Through detecting (rat tail vein injection, visible " Nanfang Medical Univ's journal " 06 phase in 2009), the bioavailability of gained hard capsule asiatic acid tromethane salt is 22.6%.
Embodiment 2
Method for preparing: by last table prescription,, after the granulation, be filled in the capsule shells and get final product with medicine and each raw material blending of adjuvant.
Embodiment 3
Method for preparing: by last table prescription,, be filled in the capsule shells and get final product with medicine and each raw material blending of adjuvant.
Effect embodiment
Measure according to 2010 editions correlation methods of Chinese Pharmacopoeia, the result is following:
The effect measuring of the hard capsule of table 1 embodiment 1～3
| Embodiment | Dissolution (%) | The granule color and luster is even | Disintegration |
| 1 | 90.3 | Satisfied | 7’26” |
| 2 | 79.7 | Better | 15’19” |
| 3 | 69.9 | Generally | 30’12” |
Can know that by last table hard capsule dissolution of the present invention is good, and content granule color and luster is even, good fluidity, and disintegration is shorter.
Comparative Examples 1
Method for preparing: by last table prescription,, be filled in the capsule shells and get final product with medicine and each raw material blending of adjuvant.
Through detecting (rat tail vein injection, visible " Nanfang Medical Univ's journal " 06 phase in 2009), the bioavailability of asiatic acid potassium salt is 16.8% in the gained hard capsule.
Comparative Examples 2
Method for preparing: by last table prescription,, be filled in the capsule shells and get final product with medicine and each raw material blending of adjuvant.
Through detecting (rat tail vein injection, visible " Nanfang Medical Univ's journal " 06 phase in 2009), the bioavailability of asiatic acid arginine salt is 1.1% in the gained hard capsule.
Claims (8)
1. Herba Centellae hydrochlorate hard capsule; Its prescription contains 5%～40% asiatic acid tromethane salt, 50%～95% filler, 0%～10% lubricant and 0%～2.0% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
2. Herba Centellae hydrochlorate hard capsule as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate hard capsule prescription is made up of 5%～40% asiatic acid tromethane salt, 50%～95% filler, 0%～10% lubricant and 0%～2.0% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
3. Herba Centellae hydrochlorate hard capsule as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate hard capsule prescription contains 15%～30% asiatic acid tromethane salt, 65%～85% filler, 2%～5% lubricant and 0%～2.0% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
4. Herba Centellae hydrochlorate hard capsule as claimed in claim 3; It is characterized in that: described Herba Centellae hydrochlorate hard capsule prescription is made up of 15%～30% asiatic acid tromethane salt, 65%～85% filler, 2%～5% lubricant and 0%～2.0% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
5. Herba Centellae hydrochlorate hard capsule as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate hard capsule prescription contains 16.64%～37.88% asiatic acid tromethane salt, 60.61%～83.19% filler, 0.12%～1.52% lubricant and 0～4.76% binding agent, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
6. like each described Herba Centellae hydrochlorate hard capsule of claim 1～5, it is characterized in that: described filler is one or more in microcrystalline Cellulose, lactose and the trihydroxy aminomethane; And/or described lubricant is magnesium stearate and/or aluminium silicate; And/or described binding agent is an ethyl cellulose.
7. Herba Centellae hydrochlorate hard capsule as claimed in claim 1; It is characterized in that: described Herba Centellae hydrochlorate hard capsule prescription comprises 16.7% asiatic acid tromethane salt, 81.3% lactose and 2% magnesium stearate, and percentage ratio accounts for the mass percent of Herba Centellae hydrochlorate hard capsule content total amount for each composition.
8. like the method for preparing of each described Herba Centellae hydrochlorate hard capsule of claim 1～7, it comprises the steps: that by described prescription behind each raw material uniform mixing, the conventional hard capsule case in this area of packing into gets final product.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101969942A (en) * | 2008-01-11 | 2011-02-09 | 上海医药工业研究院 | Therapeutic formulations based on asiatic acid and selected salts thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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