CN1903181A - Enteric quick-dissolving tablets contg. aconitine, and its prepn. method - Google Patents
Enteric quick-dissolving tablets contg. aconitine, and its prepn. method Download PDFInfo
- Publication number
- CN1903181A CN1903181A CNA2006100486072A CN200610048607A CN1903181A CN 1903181 A CN1903181 A CN 1903181A CN A2006100486072 A CNA2006100486072 A CN A2006100486072A CN 200610048607 A CN200610048607 A CN 200610048607A CN 1903181 A CN1903181 A CN 1903181A
- Authority
- CN
- China
- Prior art keywords
- enteric
- aconitine
- quick releasing
- coated quick
- acid
- 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
- XFSBVAOIAHNAPC-XTHSEXKGSA-N 16-Ethyl-1alpha,6alpha,19beta-trimethoxy-4-(methoxymethyl)-aconitane-3alpha,8,10alpha,11,18alpha-pentol, 8-acetate 10-benzoate Chemical compound O([C@H]1[C@]2(O)C[C@H]3[C@@]45C6[C@@H]([C@@]([C@H]31)(OC(C)=O)[C@@H](O)[C@@H]2OC)[C@H](OC)[C@@H]4[C@]([C@@H](C[C@@H]5OC)O)(COC)CN6CC)C(=O)C1=CC=CC=C1 XFSBVAOIAHNAPC-XTHSEXKGSA-N 0.000 title claims abstract description 25
- XFSBVAOIAHNAPC-UHFFFAOYSA-N Aconitin Natural products CCN1CC(C(CC2OC)O)(COC)C3C(OC)C(C(C45)(OC(C)=O)C(O)C6OC)C1C32C4CC6(O)C5OC(=O)C1=CC=CC=C1 XFSBVAOIAHNAPC-UHFFFAOYSA-N 0.000 title claims abstract description 25
- 229940039750 aconitine Drugs 0.000 title claims abstract description 25
- STDXGNLCJACLFY-UHFFFAOYSA-N aconitine Natural products CCN1CC2(COC)C(O)CC(O)C34C5CC6(O)C(OC)C(O)C(OC(=O)C)(C5C6OC(=O)c7ccccc7)C(C(OC)C23)C14 STDXGNLCJACLFY-UHFFFAOYSA-N 0.000 title claims abstract description 25
- 238000000034 method Methods 0.000 title claims description 6
- 239000003814 drug Substances 0.000 claims abstract description 20
- 239000002904 solvent Substances 0.000 claims abstract description 8
- 238000002156 mixing Methods 0.000 claims abstract description 7
- 229920000642 polymer Polymers 0.000 claims abstract description 5
- 239000004014 plasticizer Substances 0.000 claims abstract description 3
- 238000002360 preparation method Methods 0.000 claims description 11
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 239000002671 adjuvant Substances 0.000 claims description 9
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 9
- -1 polyethylene phthalate Polymers 0.000 claims description 8
- 239000004925 Acrylic resin Substances 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 239000000463 material Substances 0.000 claims description 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 5
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 5
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 5
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 5
- 229920000623 Cellulose acetate phthalate Polymers 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
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims description 4
- 238000005303 weighing Methods 0.000 claims description 4
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 3
- 229920000858 Cyclodextrin Polymers 0.000 claims description 3
- 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 description 3
- 229920002472 Starch Polymers 0.000 claims description 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 3
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 3
- 238000007907 direct compression Methods 0.000 claims description 3
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 3
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- 229910052708 sodium Inorganic materials 0.000 claims description 3
- 239000008107 starch Substances 0.000 claims description 3
- 235000019698 starch Nutrition 0.000 claims description 3
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 claims description 2
- 235000016623 Fragaria vesca Nutrition 0.000 claims description 2
- 240000009088 Fragaria x ananassa Species 0.000 claims description 2
- 235000011363 Fragaria x ananassa Nutrition 0.000 claims description 2
- 108010036781 Fumarate Hydratase Proteins 0.000 claims description 2
- 102100036160 Fumarate hydratase, mitochondrial Human genes 0.000 claims description 2
- 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 2
- XINCECQTMHSORG-UHFFFAOYSA-N Isoamyl isovalerate Chemical compound CC(C)CCOC(=O)CC(C)C XINCECQTMHSORG-UHFFFAOYSA-N 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims description 2
- 229920002301 cellulose acetate Polymers 0.000 claims description 2
- 239000007888 film coating Substances 0.000 claims description 2
- 238000009501 film coating Methods 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- 229960003943 hypromellose Drugs 0.000 claims description 2
- 229940116298 l- malic acid Drugs 0.000 claims description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 2
- 239000011976 maleic acid Substances 0.000 claims description 2
- 229940117841 methacrylic acid copolymer Drugs 0.000 claims description 2
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- 238000000576 coating method Methods 0.000 abstract description 8
- 239000011248 coating agent Substances 0.000 abstract description 5
- 239000000654 additive Substances 0.000 abstract 1
- 230000000996 additive effect Effects 0.000 abstract 1
- 238000010298 pulverizing process Methods 0.000 abstract 1
- YRECILNLFWZVRM-XTNYDWJGSA-N bulleyaconitine a Chemical compound O=C([C@H]1[C@]2(O)C[C@H]3[C@]45[C@H](OC)CC[C@@]6(COC)CN([C@@H]5[C@H]([C@H](OC)[C@H]64)[C@](C[C@@H]2OC)(OC(C)=O)[C@H]31)CC)C1=CC=C(OC)C=C1 YRECILNLFWZVRM-XTNYDWJGSA-N 0.000 description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 15
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 description 12
- 239000007941 film coated tablet Substances 0.000 description 12
- 238000006243 chemical reaction Methods 0.000 description 11
- 239000000047 product Substances 0.000 description 9
- 239000003826 tablet Substances 0.000 description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- 238000009505 enteric coating Methods 0.000 description 6
- 239000002702 enteric coating Substances 0.000 description 6
- 210000001035 gastrointestinal tract Anatomy 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- RIPYIJVYDYCPKW-UHFFFAOYSA-N 3-Acetylaconitine Natural products CCN1CC(C(CC2OC)OC(C)=O)(COC)C3C(OC)C(C(C45)(OC(C)=O)C(O)C6OC)C1C32C4CC6(O)C5OC(=O)C1=CC=CC=C1 RIPYIJVYDYCPKW-UHFFFAOYSA-N 0.000 description 5
- 230000000968 intestinal effect Effects 0.000 description 5
- 230000000638 stimulation Effects 0.000 description 5
- RIPYIJVYDYCPKW-UOGIXDCTSA-N x1071 Chemical compound O([C@H]1[C@]2(O)C[C@H]3[C@@]45C6[C@@H]([C@@]([C@H]31)(OC(C)=O)[C@@H](O)[C@@H]2OC)[C@H](OC)[C@@H]4[C@]([C@@H](C[C@@H]5OC)OC(C)=O)(COC)CN6CC)C(=O)C1=CC=CC=C1 RIPYIJVYDYCPKW-UOGIXDCTSA-N 0.000 description 5
- 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 4
- QUSPUZQKMRMVFL-UHFFFAOYSA-N 2-(benzenesulfonamido)-4-methylsulfanylbutanoic acid Chemical compound CSCCC(C(O)=O)NS(=O)(=O)C1=CC=CC=C1 QUSPUZQKMRMVFL-UHFFFAOYSA-N 0.000 description 4
- 230000008859 change Effects 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 230000002496 gastric effect Effects 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 230000036407 pain Effects 0.000 description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 4
- 229920000053 polysorbate 80 Polymers 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 230000003110 anti-inflammatory effect Effects 0.000 description 3
- 230000033228 biological regulation Effects 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 230000003467 diminishing effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 3
- 210000004211 gastric acid Anatomy 0.000 description 3
- 210000004051 gastric juice Anatomy 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 239000002085 irritant Substances 0.000 description 3
- 231100000021 irritant Toxicity 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- 241000227129 Aconitum Species 0.000 description 2
- 241000701413 Aconitum kusnezoffii Species 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 2
- 102000011759 adducin Human genes 0.000 description 2
- 108010076723 adducin Proteins 0.000 description 2
- 229930013930 alkaloid Natural products 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 239000000835 fiber Substances 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 230000007062 hydrolysis Effects 0.000 description 2
- 238000006460 hydrolysis reaction Methods 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000007689 inspection Methods 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical group O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 2
- 239000011347 resin Substances 0.000 description 2
- 229920005989 resin Polymers 0.000 description 2
- 229920002545 silicone oil Polymers 0.000 description 2
- 239000007901 soft capsule Substances 0.000 description 2
- 230000004936 stimulating effect Effects 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- NWBWCXBPKTTZNQ-UHFFFAOYSA-N (16S)-4-(N-Acetyl-anthraniloyloxy)-20-aethyl-1alpha,14alpha,16-trimethoxy-aconitan-8,9-diol Natural products C1CC(OC)C2(C3C4)C5CC(C(C6)OC)C(OC)C5(O)C6(O)C4C2N(CC)CC31OC(=O)C1=CC=CC=C1NC(C)=O NWBWCXBPKTTZNQ-UHFFFAOYSA-N 0.000 description 1
- HFVMEOPYDLEHBR-UHFFFAOYSA-N (2-fluorophenyl)-phenylmethanol Chemical compound C=1C=CC=C(F)C=1C(O)C1=CC=CC=C1 HFVMEOPYDLEHBR-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- 241000173529 Aconitum napellus Species 0.000 description 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010020565 Hyperaemia Diseases 0.000 description 1
- 206010022061 Injection site erythema Diseases 0.000 description 1
- 241000581650 Ivesia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229960001138 acetylsalicylic acid Drugs 0.000 description 1
- 229940023019 aconite Drugs 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 210000003567 ascitic fluid Anatomy 0.000 description 1
- 238000001354 calcination Methods 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229940121657 clinical drug Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000000593 degrading effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000002662 enteric coated tablet Substances 0.000 description 1
- XTLNYNMNUCLWEZ-UHFFFAOYSA-N ethanol;propan-2-one Chemical compound CCO.CC(C)=O XTLNYNMNUCLWEZ-UHFFFAOYSA-N 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 239000007948 fast release tablet Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000007661 gastrointestinal function Effects 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Substances [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 239000004531 microgranule Substances 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 239000007935 oral tablet Substances 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000035484 reaction time Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 210000000697 sensory organ Anatomy 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- NWBWCXBPKTTZNQ-QOQRDJBUSA-N y4m5974f7z Chemical compound O([C@]12CN([C@@H]3[C@H]4[C@]5(O)[C@@]6(O)[C@@H](OC)[C@@H]([C@H](C5)OC)C[C@H]6[C@@]3([C@@H]1C4)[C@@H](OC)CC2)CC)C(=O)C1=CC=CC=C1N=C(C)O NWBWCXBPKTTZNQ-QOQRDJBUSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
Disintegrating agent, label adjuvant | Enteric-coating material, solvent | ||||||||||
Embodiment | Bulleyaconitine A | Cross-linked carboxymethyl cellulose sodium | Magnesium stearate | Microcrystalline cellulose | Lactose | Mannitol | The cellulose acetate phthalate ester | Lac | Acetone | Ethanol | The phthalic acid diethylester |
1 | 0.2g | 5g | 4g | 100g | 12g | 20g | 4g | 3g | 15ml | 17ml | 0.6g |
2 | 0.4g | 4g | 4g | 40g | 12g | 20g | 3g | 2g | 12ml | 12ml | 0.5g |
Disintegrating agent, label adjuvant | Enteric-coating material, solvent | |||||||||||
Embodiment | 3-acetylaconitine | Cyclodextrin/crosslinked carboxymethylstach sodium | Carmethose | Microcrystalline cellulose | Polyethylene Glycol-6000 | Mannitol | Flavoring orange essence | Polyacrylic resin III number | Tween 80 | 95% ethanol | The phthalic acid diethylester | Oleum Ricini |
3 | 0.3g | 6g | 9g | 40g | 2g | 40g | 0.1g | 1.3g | 0.3ml | 18ml | 0.2g | 0.2ml |
4 | 1g | 3g | 9g | 48g | 2g | 55g | 0.1g | 1.8g | 0.3ml | 21ml | 0.2g | 0.2ml |
Disintegrating agent, label adjuvant | Enteric-coating material, solvent | |||||||||||||
Embodiment | Lappaconitine hydrobromide (crossing 1000 orders) | Soluble starch | Microcrystalline cellulose (100 order) | Lactose (120 order) | Low-substituted hydroxypropyl cellulose (80 order) | Beta-schardinger dextrin-(80 order) | Polyethylene Glycol-6000 | Citric acid/succinic acid | Polyacrylic resin II number | Tween 80 | 95% ethanol | The phthalic acid diethylester | Oleum Ricini | Silicone oil |
5 | 6g | 10g | 16g | 5g | 4g | 2g | 0.8g | 0.25g | 1.6g | 0.2ml | 20ml | 0.1g | 0.1ml | 0.15ml |
6 | 10g | 18g | 21g | 5g | 4g | 0.9g | 0.2g | 1.9g | 0.2ml | 20ml | 0.1g | 0.1ml | 0.16ml |
Group | Body weight | Dosage (mg/Kg) | Turn round the body number of times | Suppression ratio |
Blank group | 20±1.0 | Equal-volume | 30.7±7.88 | |
The morphine group | 20±1.3 | 10 | 2.4±1.50 | 92.5% |
The bulleyaconitine A sheet | 20±1.1 | 0.2 | 10.5±3.42 | 76.04% |
The enteric-coated quick releasing sheet | 20±1.2 | 0.2 | 7.5±3.00 | 87.2% |
Group | Body weight | Dosage (mg/Kg) | Optical density value | Suppression ratio |
Blank group | 20±1.12 | Equal-volume | 0.28±0.05 | |
Aspirin | 20±1.13 | 200 | 0.13±0.03 | 62.5% |
The bulleyaconitine A sheet | 20±1.12 | 0.2 | 0.10±0.02 | 71.4% |
The enteric-coated quick releasing sheet | 20±1.1 | 0.2 | 0.09±0.002 | 79.5% |
Order of reaction | Irritant reaction |
0 | No change |
1 | No significant change |
2 | The mild hyperaemia point is arranged |
3 | The congested point of moderate is arranged |
4 | The congested point of severe is arranged, change with the small size position |
Sample | January | February | March | June | December | 24 months |
Example 1 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Example 2 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Example 3 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Example 4 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Example 5 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Example 6 | Qualified | Qualified | Qualified | Qualified | Qualified | Qualified |
Claims (6)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2006100486072A CN100518721C (en) | 2006-08-08 | 2006-08-08 | Enteric quick-dissolving tablets containing aconitine, and preparation method thereof |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2006100486072A CN100518721C (en) | 2006-08-08 | 2006-08-08 | Enteric quick-dissolving tablets containing aconitine, and preparation method thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1903181A true CN1903181A (en) | 2007-01-31 |
CN100518721C CN100518721C (en) | 2009-07-29 |
Family
ID=37672641
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2006100486072A Active CN100518721C (en) | 2006-08-08 | 2006-08-08 | Enteric quick-dissolving tablets containing aconitine, and preparation method thereof |
Country Status (1)
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CN102178658A (en) * | 2011-05-03 | 2011-09-14 | 中国人民解放军第三军医大学第二附属医院 | Lappaconitine hydrobromide orally disintegrating tablets and preparation method thereof |
CN102406640A (en) * | 2010-09-26 | 2012-04-11 | 上海泰因生物技术有限公司 | Analgesic and antiphlogistic medicines and micro-needle transdermal administration method for same |
CN102526233A (en) * | 2010-12-24 | 2012-07-04 | 无锡济民可信山禾药业股份有限公司 | Multi-unit enteric-coated preparation containing aconitine and preparation method thereof |
Family Cites Families (7)
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CN1038473C (en) * | 1993-10-23 | 1998-05-27 | 云南省弥勒县制药厂 | Bulleyaconitine A oral preparation |
CN1069519C (en) * | 1998-03-17 | 2001-08-15 | 昆明制药股份有限公司 | Bulleyaconitine A soft capsule and its production method |
CN1535684A (en) * | 2003-04-09 | 2004-10-13 | 王 锦 | Aconitum kusnezoffii methylsine powder injection preparation and its preparation method |
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CN1297271C (en) * | 2003-09-30 | 2007-01-31 | 昆明紫健生物技术有限公司 | Fat emulsion injection of bulleyaconitine A and its manufacturing method |
CN1778299A (en) * | 2004-11-19 | 2006-05-31 | 昆明五和堂药物研制有限公司 | Cavitas nasisal cavity medicine-supply preparation with radix aconiti agrestis methyl |
CN100406012C (en) * | 2005-04-19 | 2008-07-30 | 北京正大绿洲医药科技有限公司 | Hydrobromic acid high tortoiseshell component drip pill and its preparation method |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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CN102406640A (en) * | 2010-09-26 | 2012-04-11 | 上海泰因生物技术有限公司 | Analgesic and antiphlogistic medicines and micro-needle transdermal administration method for same |
CN102526233A (en) * | 2010-12-24 | 2012-07-04 | 无锡济民可信山禾药业股份有限公司 | Multi-unit enteric-coated preparation containing aconitine and preparation method thereof |
CN102526233B (en) * | 2010-12-24 | 2016-01-27 | 无锡济民可信山禾药业股份有限公司 | A kind of multiple-unit enteric coated preparation containing aconitine and preparation method thereof |
CN102178658A (en) * | 2011-05-03 | 2011-09-14 | 中国人民解放军第三军医大学第二附属医院 | Lappaconitine hydrobromide orally disintegrating tablets and preparation method thereof |
CN102178658B (en) * | 2011-05-03 | 2013-04-10 | 中国人民解放军第三军医大学第二附属医院 | Lappaconitine hydrobromide orally disintegrating tablets and preparation method thereof |
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CN100518721C (en) | 2009-07-29 |
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