CN1069520C - Breviscapine soft capsule and its production method - Google Patents
Breviscapine soft capsule and its production method Download PDFInfo
- Publication number
- CN1069520C CN1069520C CN98106599A CN98106599A CN1069520C CN 1069520 C CN1069520 C CN 1069520C CN 98106599 A CN98106599 A CN 98106599A CN 98106599 A CN98106599 A CN 98106599A CN 1069520 C CN1069520 C CN 1069520C
- Authority
- CN
- China
- Prior art keywords
- breviscapine
- soft capsule
- gelatin
- acid
- hydroxybenzoate
- 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.)
- Expired - Lifetime
Links
- 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 title claims abstract description 25
- 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 title claims abstract description 25
- 239000007901 soft capsule Substances 0.000 title claims abstract description 24
- 238000004519 manufacturing process Methods 0.000 title claims abstract description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 76
- 229920000159 gelatin Polymers 0.000 claims abstract description 33
- 235000019322 gelatine Nutrition 0.000 claims abstract description 33
- 108010010803 Gelatin Proteins 0.000 claims abstract description 32
- 239000008273 gelatin Substances 0.000 claims abstract description 32
- 235000011852 gelatine desserts Nutrition 0.000 claims abstract description 32
- 235000011187 glycerol Nutrition 0.000 claims abstract description 26
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 12
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 12
- 235000015112 vegetable and seed oil Nutrition 0.000 claims abstract description 12
- 239000008158 vegetable oil Substances 0.000 claims abstract description 12
- 230000002421 anti-septic effect Effects 0.000 claims abstract description 11
- 239000000375 suspending agent Substances 0.000 claims abstract description 11
- 239000003085 diluting agent Substances 0.000 claims abstract description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 238000002156 mixing Methods 0.000 claims abstract description 5
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 21
- 239000007788 liquid Substances 0.000 claims description 17
- 239000007766 cera flava Substances 0.000 claims description 15
- 241000132521 Erigeron Species 0.000 claims description 12
- 235000006708 antioxidants Nutrition 0.000 claims description 10
- 238000003756 stirring Methods 0.000 claims description 10
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 6
- 239000004615 ingredient Substances 0.000 claims description 5
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 4
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000002202 Polyethylene glycol Substances 0.000 claims description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 4
- 238000007872 degassing Methods 0.000 claims description 4
- -1 dibenzylatiooluene Chemical compound 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 229920001223 polyethylene glycol Polymers 0.000 claims description 4
- 238000005303 weighing Methods 0.000 claims description 4
- MOZDKDIOPSPTBH-UHFFFAOYSA-N Benzyl parahydroxybenzoate Chemical compound C1=CC(O)=CC=C1C(=O)OCC1=CC=CC=C1 MOZDKDIOPSPTBH-UHFFFAOYSA-N 0.000 claims description 3
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 claims description 3
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 claims description 3
- 229920000896 Ethulose Polymers 0.000 claims description 3
- 239000001856 Ethyl cellulose Substances 0.000 claims description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 3
- 239000001859 Ethyl hydroxyethyl cellulose Substances 0.000 claims description 3
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
- IMQLKJBTEOYOSI-GPIVLXJGSA-N Inositol-hexakisphosphate Chemical compound OP(O)(=O)O[C@H]1[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@@H]1OP(O)(O)=O IMQLKJBTEOYOSI-GPIVLXJGSA-N 0.000 claims description 3
- IMQLKJBTEOYOSI-UHFFFAOYSA-N Phytic acid Natural products OP(O)(=O)OC1C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C1OP(O)(O)=O IMQLKJBTEOYOSI-UHFFFAOYSA-N 0.000 claims description 3
- 229940087168 alpha tocopherol Drugs 0.000 claims description 3
- 235000010323 ascorbic acid Nutrition 0.000 claims description 3
- 239000011668 ascorbic acid Substances 0.000 claims description 3
- 229960005070 ascorbic acid Drugs 0.000 claims description 3
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 claims description 3
- 229920001249 ethyl cellulose Polymers 0.000 claims description 3
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 3
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 claims description 3
- 235000019326 ethyl hydroxyethyl cellulose Nutrition 0.000 claims description 3
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 claims description 3
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 claims description 3
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 3
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
- 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 claims description 3
- 229960000367 inositol Drugs 0.000 claims description 3
- 229920000609 methyl cellulose Polymers 0.000 claims description 3
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 3
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 3
- 239000001923 methylcellulose Substances 0.000 claims description 3
- 235000010981 methylcellulose Nutrition 0.000 claims description 3
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 3
- 229960002216 methylparaben Drugs 0.000 claims description 3
- GJLNWLVPAHNBQN-UHFFFAOYSA-N phenyl 4-hydroxybenzoate Chemical compound C1=CC(O)=CC=C1C(=O)OC1=CC=CC=C1 GJLNWLVPAHNBQN-UHFFFAOYSA-N 0.000 claims description 3
- 235000002949 phytic acid Nutrition 0.000 claims description 3
- 239000000467 phytic acid Substances 0.000 claims description 3
- 229940068041 phytic acid Drugs 0.000 claims description 3
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 3
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 3
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 3
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 claims description 3
- 229960000984 tocofersolan Drugs 0.000 claims description 3
- 239000002076 α-tocopherol Substances 0.000 claims description 3
- 235000004835 α-tocopherol Nutrition 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- LKAPTZKZHMOIRE-KVTDHHQDSA-N (2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbaldehyde Chemical compound OC[C@H]1O[C@H](C=O)[C@@H](O)[C@@H]1O LKAPTZKZHMOIRE-KVTDHHQDSA-N 0.000 claims description 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 2
- 229920001817 Agar Polymers 0.000 claims description 2
- 239000005711 Benzoic acid Substances 0.000 claims description 2
- ZJJGPUQRMUBVBE-UHFFFAOYSA-N C(CCC)OC(=O)C1=CC=C(O)C=C1.[Ca] Chemical compound C(CCC)OC(=O)C1=CC=C(O)C=C1.[Ca] ZJJGPUQRMUBVBE-UHFFFAOYSA-N 0.000 claims description 2
- 229920002101 Chitin Polymers 0.000 claims description 2
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 claims description 2
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 claims description 2
- 239000004471 Glycine Substances 0.000 claims description 2
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 2
- KWKVAGQCDSHWFK-VNKDHWASSA-N Methyl sorbate Chemical compound COC(=O)\C=C\C=C\C KWKVAGQCDSHWFK-VNKDHWASSA-N 0.000 claims description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 239000008272 agar Substances 0.000 claims description 2
- 235000010419 agar Nutrition 0.000 claims description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 2
- 235000010233 benzoic acid Nutrition 0.000 claims description 2
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 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
- LKAPTZKZHMOIRE-UHFFFAOYSA-N chitose Natural products OCC1OC(C=O)C(O)C1O LKAPTZKZHMOIRE-UHFFFAOYSA-N 0.000 claims description 2
- 229960004106 citric acid Drugs 0.000 claims description 2
- 235000015165 citric acid Nutrition 0.000 claims description 2
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 claims description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 2
- 229960002449 glycine Drugs 0.000 claims description 2
- 229960004337 hydroquinone Drugs 0.000 claims description 2
- 235000010445 lecithin Nutrition 0.000 claims description 2
- 239000000787 lecithin Substances 0.000 claims description 2
- 229940067606 lecithin Drugs 0.000 claims description 2
- 239000001630 malic acid Substances 0.000 claims description 2
- 235000011090 malic acid Nutrition 0.000 claims description 2
- 229940099690 malic acid Drugs 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 235000010446 mineral oil Nutrition 0.000 claims description 2
- 239000002480 mineral oil Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 2
- RWPGFSMJFRPDDP-UHFFFAOYSA-L potassium metabisulfite Chemical compound [K+].[K+].[O-]S(=O)S([O-])(=O)=O RWPGFSMJFRPDDP-UHFFFAOYSA-L 0.000 claims description 2
- 229940043349 potassium metabisulfite Drugs 0.000 claims description 2
- 235000010263 potassium metabisulphite Nutrition 0.000 claims description 2
- 229960004063 propylene glycol Drugs 0.000 claims description 2
- 235000013772 propylene glycol Nutrition 0.000 claims description 2
- 235000010378 sodium ascorbate Nutrition 0.000 claims description 2
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 claims description 2
- 229960005055 sodium ascorbate Drugs 0.000 claims description 2
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 claims description 2
- 235000010262 sodium metabisulphite Nutrition 0.000 claims description 2
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 claims description 2
- PESXGULMKCKJCC-UHFFFAOYSA-M sodium;4-methoxycarbonylphenolate Chemical compound [Na+].COC(=O)C1=CC=C([O-])C=C1 PESXGULMKCKJCC-UHFFFAOYSA-M 0.000 claims description 2
- IXMINYBUNCWGER-UHFFFAOYSA-M sodium;4-propoxycarbonylphenolate Chemical compound [Na+].CCCOC(=O)C1=CC=C([O-])C=C1 IXMINYBUNCWGER-UHFFFAOYSA-M 0.000 claims description 2
- 235000010199 sorbic acid Nutrition 0.000 claims description 2
- 239000004334 sorbic acid Substances 0.000 claims description 2
- 229940075582 sorbic acid Drugs 0.000 claims description 2
- 239000000230 xanthan gum Substances 0.000 claims description 2
- 229920001285 xanthan gum Polymers 0.000 claims description 2
- 235000010493 xanthan gum Nutrition 0.000 claims description 2
- 229940082509 xanthan gum Drugs 0.000 claims description 2
- 239000000811 xylitol Substances 0.000 claims description 2
- 235000010447 xylitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 2
- 229960002675 xylitol Drugs 0.000 claims description 2
- 239000001828 Gelatine Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 abstract description 4
- 230000008901 benefit Effects 0.000 abstract description 2
- 238000000465 moulding Methods 0.000 abstract description 2
- 239000002671 adjuvant Substances 0.000 abstract 1
- 235000013871 bee wax Nutrition 0.000 abstract 1
- 239000012166 beeswax Substances 0.000 abstract 1
- 239000002775 capsule Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003755 preservative agent Substances 0.000 abstract 1
- 230000002335 preservative effect Effects 0.000 abstract 1
- 238000003825 pressing Methods 0.000 abstract 1
- 238000009849 vacuum degassing Methods 0.000 abstract 1
- 239000000047 product Substances 0.000 description 6
- 239000000843 powder Substances 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 238000001035 drying Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000007903 gelatin capsule Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 206010033799 Paralysis Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 150000002333 glycines Chemical class 0.000 description 2
- 238000009413 insulation Methods 0.000 description 2
- 238000012856 packing Methods 0.000 description 2
- 230000000704 physical effect Effects 0.000 description 2
- 210000000582 semen Anatomy 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 description 1
- 206010013786 Dry skin Diseases 0.000 description 1
- 229910000831 Steel Inorganic materials 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 230000000702 anti-platelet effect Effects 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 230000008344 brain blood flow Effects 0.000 description 1
- 230000003727 cerebral blood flow Effects 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 239000003292 glue Substances 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 238000002372 labelling Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000010687 lubricating oil Substances 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 238000012372 quality testing Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000011265 semifinished product Substances 0.000 description 1
- 210000000952 spleen Anatomy 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 239000010959 steel Substances 0.000 description 1
- 230000004206 stomach function Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a soft capsule oral medicine and its production method. Each soft capsule contains breviscapine 10-200 microgram, beeswax and medicinal adjuvants including diluent, antioxidant and suspending agent. The capsule shell contains 10 parts of gelatin, 3.25-3.35 parts of glycerin (by weight) and preservative. The preparation process comprises the following steps: dissolving gelatin in water, adding glycerol and appropriate amount of antiseptic, and vacuum degassing; adding suspending agent into vegetable oil, mixing breviscapine and vegetable oil, and adding antioxidant; molding and pressing the soft capsule. Compared with the existing preparation of breviscapine, the product has the advantages of stable quality, convenient carrying and administration; the effective components are dissolved out quickly.
Description
The present invention relates to contain the soft capsule oral drugs of breviscapine effective dose.
Breviscapine (Breviscapini) is yellow powder, dissolves in aqueous alkali, is slightly soluble in methanol, water insoluble, chloroform etc.Have and more obviously improve the brain blood circulation, the cerebral blood flow increasing amount reduces the effect of vascular resistance and anti-platelet aggregation.Evidence: better to paralysis and the back something lost paralysis curative effect due to the cerebral hemorrhage due to the obliterated cerebral vascular disease.And harmless to the heart, liver, kidney, lung, spleen stomach function regulating function, there is not obvious toxic-side effects yet.
With breviscapine is that " Breviscapini injection ", " Herba Erigerontis tablet " of main effective ingredient reaches " breviscapine frozen dry powder " and produced by administrative department of public health's approval.But injection, freeze-dried powder carry, administration is all inconvenient; Tablet exists the effective ingredient stripping slow, defectives such as onset in time.
The purpose of this invention is to provide a kind of erigeron breviscopus element soft capsule and production method thereof, the product oral form of administration, its steady quality, easy to use, effective.
Product of the present invention is made of medicinal liquid and softgel shell two large divisions, medicinal liquid contains the breviscapine of effective dosage as effective ingredient, and contain pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant comprises diluent, antioxidant, suspending agent, contain 10 parts in gelatin in the softgel shell, glycerol 3.25-3.35 part (weight ratio) and antiseptic, medicinal liquid by weight every contain breviscapine 10-200 microgram, and also contain Cera Flava.
Diluent can be one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil;
Antioxidant can be one or more in ethylenediaminetetraacetic acid, disodium EDTA, dibenzylatiooluene, D-xylose, xylitol, glycine, alpha-tocopherol, α-tocopheryl acetate, inositol, ascorbic acid, sodium ascorbate, lecithin, malic acid, hydroquinone, citric acid, succinic acid, phytic acid, sodium pyrosulfite, the potassium metabisulfite;
Antiseptic can be one or more in Oleum Caryophylli, propylene glycol, sorbic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, ethylparaben, propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, benzyl p-hydroxybenzoate, P-hydroxybenzoic acid phenyl ester, butyl p-hydroxybenzoate calcium, Sodium Methyl Hydroxybenzoate, Sodium Propyl Hydroxybenzoate, benzyl alcohol, the benzoic acid etc.;
Suspending agent can be one or more in ethylhydroxyethylcellulose, chitin, chitose, methylcellulose, ethyl cellulose, agar, xanthan gum, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, the Cera Flava etc.
In the process of research erigeron breviscopus element soft capsule, solved a following main difficult problem:
1, softgel shell prescription (being applicable to the oil-soluble medicinal liquid)
Gelatin, glycerol proportioning are difficult to grasp in the prescription of softgel shell.The amount of glycerol is too many, and softgel shell is softer, than being easier to extrusion; The amount of glycerol very little, softgel shell is harder, crisp, influences the quality stability and the disintegration time of soft capsule.We have carried out detailed experimental study to the gelatin of softgel shell, the proportioning of glycerol, have obtained a proportioning preferably at last.
An amount of gelatin is added in the rustless steel glue pot, add suitable quantity of water again, airtight, 70 ℃ are incubated 3 hours, add glycerol, the antiseptic of test consumption more respectively, stir, vacuumize degassing 2 hours, put into 70 ℃ of insulations of gelatin heat-preserving container standing over night, second day, the moulding ball, drying at room temperature, keep sample and investigate three months, examination softgel shell outward appearance and physical property, the result is as follows:
| Index/content of the test | Gelatin 10kg glycerol 3.0kg | Gelatin 10kg glycerol 3.2kg | Gelatin 10kg glycerol 3.25-3.35kg | Gelatin 10kg glycerol 3.4kg | Gelatin 10kg glycerol 3.6kg |
| Softgel shell outward appearance and physical property | Too firmly, easily crisp | Too firmly, easily crisp | Suitable | Softer, the easy moisture absorption | Softer, the easy moisture absorption |
Illustrate: the softgel shell prescription that is filtered out is applicable to the place of warm moist.
By above test, can reach a conclusion, should contain in the prescription of softgel shell: 10 parts in gelatin, glycerol 3.25-3.35 part (weight ratio).
2, medicinal liquid prescription
The softgel shell of soft capsule has determined that the used diluent of medicinal liquid can not be water, ethanol and the bigger organic solvent of some toxicity, and ideal is oil substances.But because breviscapine is difficult to be dissolved in vegetable oil, therefore, we are by a large amount of tests, selected for use a kind of toxicity less, can be dissolved in the vegetable oil, can well breviscapine be suspended in the vegetable oil, and can for a long time stable material-Cera Flava.
An amount of Cera Flava is dissolved in an amount of vegetable oil, again breviscapine is added wherein, add suitable antioxidant afterwards and to prevent the medicinal liquid in the soft capsule rotten (oxidation) takes place in storage process, every of soft gelatin capsule contains principal agent--and the amount of breviscapine is determined; Consider the size of economic factor and selected every ball easy to prepare, finally can determine the liquid formula of embodiment.
Contain in the optimum formula of product of the present invention:
Component amount (gram/grain)
Breviscapine 0.01-0.2
Diluent 0.07-0.45
Gelatin 0.04-0.25
Glycerol (32.5-33.5% of gelatin amount)
Suspending agent 0.003-0.01
Antioxidant 0.0006-0.001
Antiseptic 0.00003-0.00007
Cera Flava 0.005-0.035
Annotate: optimum formula is only for the present invention is further illustrated, and the scope of product of the present invention is not subjected to the limitation of this optimum formula.
The preparation technology of erigeron breviscopus element soft capsule may further comprise the steps:
Gelatin adds suitable quantity of water under stirring, treat that gelatin dissolves fully after, add glycerol, an amount of antiseptic, stir, be incubated set aside for use after the vacuumize degassing;
Suspending agent is added in the vegetable oil, take by weighing breviscapine, mix with vegetable oil, treat to add antioxidant again behind the complete mixing, stir, room temperature leaves standstill.
The medicinal liquid for preparing is poured in the medicinal liquid bucket, pressed soft capsule with mould.
Erigeron breviscopus element soft capsule reaches existing dosage forms such as " breviscapine frozen dry powders " and compares with " Breviscapini injection ", " Herba Erigerontis tablet ", and advantage is a steady quality, carries, administration is all convenient; The effective ingredient stripping is fast, onset in time.
Product of the present invention prepares as stated above, and its detailed component is provided by the following example, but protection scope of the present invention is not limited to this.
Embodiment 1
Component amount (gram/grain)
Breviscapine 0.05
Oleum Arachidis hypogaeae semen 0.09
Gelatin 0.06
Glycerol 0.02
Ethyl cellulose 0.004
Alpha-tocopherol 0.0008
Ethylparaben 0.00005
Cera Flava 0.008
Embodiment 2
Component amount (gram/grain)
Breviscapine 0.01 Oleum Glycines 0.08 gelatin 0.05 glycerol 0.015 ethylhydroxyethylcellulose 0.005 dibenzylatiooluene 0.0008 methyl parahydroxybenzoate 0.00005 Cera Flava 0.006
Embodiment 3 component amount (gram/grain) breviscapines 0.02 Polyethylene Glycol 0.1 gelatin 0.05 glycerol 0.017 hydroxyethyl-cellulose 0.006 α-tocopheryl acetate 0.0008 butyl p-hydroxybenzoate 0.00005 Cera Flava 0.009
Embodiment 4 component amount (gram/grain) breviscapines 0.01 Oleum Glycines 0.2 propylene glycol 0.1 gelatin 0.12 glycerol 0.04 Cera Flava 0.006 ascorbic acid 0.0008 propyl p-hydroxybenzoate 0.00005 Cera Flava 0.015
Embodiment 5 component amount (gram/grain) breviscapines 0.15 Oleum Arachidis hypogaeae semen 0.3 propylene glycol 0.1
Gelatin 0.15
Glycerol 0.05
Hydroxypropyl cellulose 0.007
Inositol 0.0008
Benzyl p-hydroxybenzoate 0.00005
Cera Flava 0.024
Embodiment 6
Component amount (gram/grain)
Breviscapine 0.2
Polyethylene Glycol 0.16
Propylene glycol 0.14
Gelatin 0.2
Glycerol 0.08
Component amount (gram/grain)
Methylcellulose 0.009
Phytic acid 0.0008
P-hydroxybenzoic acid phenyl ester 0.00005
Cera Flava 0.03
The preparation technology of above embodiment erigeron breviscopus element soft capsule is:
Take by weighing gelatin and add 100L gelatin retort, under stirring, add suitable quantity of water, airtight, treat that gelatin dissolves fully after, add glycerol, an amount of antiseptic again, stir, vacuumize degassing 2 hours is put into the gelatin heat-preserving container, the insulation standing over night is stand-by.
Under room temperature suspending agent is added in the diluent, take by weighing breviscapine, pulverize, sieve, with mixing diluents, treat to add antioxidant again behind the complete mixing, stir, room temperature leaves standstill.
The gelatin heat-preserving container is suspended from certain altitude, the medicinal liquid for preparing is poured in the medicinal liquid bucket, change mould and begin to press soft capsule, adjust the soft capsule device to scope of design, drying at room temperature two days, reject the soft gelatin capsule of presentation quality difference, with soft gelatin capsule washing (removing the lubricating oil in the pelleting process), again in 24 ℃ of dryings two days, the erigeron breviscopus element soft capsule semi-finished product, the qualified back packing of quality testing, labeling, packing promptly get the erigeron breviscopus element soft capsule finished product.
Claims (4)
1, a kind of erigeron breviscopus element soft capsule, constitute by medicinal liquid and softgel shell two large divisions, medicinal liquid contains the breviscapine of effective dosage as effective ingredient, and contain pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant comprises diluent, antioxidant, suspending agent, contain 10 parts in gelatin in the softgel shell, glycerol 3.25-3.35 part (weight ratio) and antiseptic, medicinal liquid by weight every contain breviscapine 10-200 microgram, and also contain Cera Flava.
2, as the said erigeron breviscopus element soft capsule of claim 1, it is characterized in that:
Diluent is one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil,
Antioxidant is one or more in ethylenediaminetetraacetic acid, disodium EDTA, dibenzylatiooluene, D-xylose, xylitol, glycine, alpha-tocopherol, α-tocopheryl acetate, inositol, ascorbic acid, sodium ascorbate, lecithin, malic acid, hydroquinone, citric acid, succinic acid, phytic acid, sodium pyrosulfite, the potassium metabisulfite
Antiseptic is one or more in Oleum Caryophylli, propylene glycol, sorbic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, ethylparaben, propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, benzyl p-hydroxybenzoate, P-hydroxybenzoic acid phenyl ester, butyl p-hydroxybenzoate calcium, Sodium Methyl Hydroxybenzoate, Sodium Propyl Hydroxybenzoate, benzyl alcohol, the benzoic acid etc.
Suspending agent is one or more in ethylhydroxyethylcellulose, chitin, chitose, methylcellulose, ethyl cellulose, agar, xanthan gum, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, the Cera Flava etc.
3,, it is characterized in that containing in the prescription as the said erigeron breviscopus element soft capsule of claim 2:
Component amount (gram/grain)
Breviscapine 0.01-0.2
Diluent 0.07-0.45
Gelatin 0.04-0.25
The 32.5-33.5% of glycerin gelatine amount
Suspending agent 0.003-0.01
Antioxidant 0.0006-0.001
Antiseptic 0.00003-0.00007
Cera Flava 0.005-0.035
4, a kind of erigeron breviscopus element soft capsule and production method thereof is characterized in that may further comprise the steps:
Gelatin adds suitable quantity of water under stirring, treat that gelatin dissolves fully after, add glycerol, an amount of antiseptic, stir, be incubated set aside for use after the vacuumize degassing.
Suspending agent is added in the vegetable oil, take by weighing breviscapine, mix with vegetable oil, treat to add antioxidant again behind the complete mixing, stir, room temperature leaves standstill.
The medicinal liquid for preparing is poured in the medicinal liquid bucket, pressed soft capsule with mould.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98106599A CN1069520C (en) | 1998-03-17 | 1998-03-17 | Breviscapine soft capsule and its production method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98106599A CN1069520C (en) | 1998-03-17 | 1998-03-17 | Breviscapine soft capsule and its production method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1228959A CN1228959A (en) | 1999-09-22 |
| CN1069520C true CN1069520C (en) | 2001-08-15 |
Family
ID=5219035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98106599A Expired - Lifetime CN1069520C (en) | 1998-03-17 | 1998-03-17 | Breviscapine soft capsule and its production method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1069520C (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771949B (en) * | 2005-11-06 | 2011-04-20 | 沈阳药科大学 | Soft nimodipine capsule and its preparation |
| CN101993462B (en) * | 2009-08-11 | 2013-12-11 | 昆明制药集团股份有限公司 | Scutellarin crystal I and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1095934A (en) * | 1993-05-29 | 1994-12-07 | 昆明制药厂 | Breviscapine powder for injection and its preparation method |
| CN1133180A (en) * | 1995-04-10 | 1996-10-16 | 昆明群星制药厂 | Erigeron breviscapus basic element freezed drying preparation for injection and preparation process |
| CN1136446A (en) * | 1995-05-25 | 1996-11-27 | 张仁保 | Soft capsule of gynostemma pentaphylla total glycoside and its preparing technology |
-
1998
- 1998-03-17 CN CN98106599A patent/CN1069520C/en not_active Expired - Lifetime
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1095934A (en) * | 1993-05-29 | 1994-12-07 | 昆明制药厂 | Breviscapine powder for injection and its preparation method |
| CN1133180A (en) * | 1995-04-10 | 1996-10-16 | 昆明群星制药厂 | Erigeron breviscapus basic element freezed drying preparation for injection and preparation process |
| CN1136446A (en) * | 1995-05-25 | 1996-11-27 | 张仁保 | Soft capsule of gynostemma pentaphylla total glycoside and its preparing technology |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1228959A (en) | 1999-09-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1257711C (en) | Butyl benzene phthalein soft capsule and its preparation method | |
| CN1939358A (en) | Sarcandra glaber dispersant tablets | |
| CN1857676A (en) | Zedoary oil microcapsule preparation and its preparing process | |
| CN1568942A (en) | Liquid capsule and production method thereof | |
| CN1069520C (en) | Breviscapine soft capsule and its production method | |
| KR101645535B1 (en) | Composition containing glucosamine with anti-immflammatory and pain repression effect | |
| CN1543942A (en) | Haw leaf general flavone soft capsule and preparation thereof | |
| CN1481883A (en) | Fleabane soft capsule formulation and its preparation method | |
| CN1939423A (en) | Rhizoma corydalis analgetic dispersing tablet | |
| CN1939512A (en) | Infantile overfood dispersing tablets | |
| CN1449765A (en) | Puerarin soft capsule pharmaceutics and preparation process thereof | |
| CN1069519C (en) | Bulleyaconitine A soft capsule and its production method | |
| CN100544707C (en) | panacea grass soft capsule and production method thereof | |
| CN1634428A (en) | Ginkgo leaf soft capsule and preparation technique thereof | |
| CN1481792A (en) | Andrographolide soft capsule formulation and preparation method | |
| CN1742868A (en) | Soft capsule for promoting blood circulation and removing blood stasis and promoting circulation of qi and relieving pain, and preparing method | |
| CN1064258C (en) | Soft capsule of notoginseng extract and its preparing process | |
| CN106619560B (en) | Polyene phosphatidyl choline capsule and preparation process thereof | |
| CN1259038C (en) | Radix bupleuri soft capsule pharmaceutics and preparation process thereof | |
| CN1839854A (en) | Glycyrrhizin soft capsule and its preparation process | |
| CN1742813A (en) | Soft capsule for treating acute and chronic pyelonephritis and prostatitis and preparing method | |
| CN1742791A (en) | Heat-clearing toxifying soft capsule and preparing method | |
| CN1839849A (en) | Cucurbitacin soft capsule and its preparation process | |
| CN1569121A (en) | Medicinal capsule of Chinese clinopodium herb for and its preparing process | |
| CN1284529C (en) | Compound gastrodia elata drop pills |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C56 | Change in the name or address of the patentee |
Owner name: KUNMING MEDICINE GROUP STOCK CO., LTD. Free format text: FORMER NAME OR ADDRESS: KUNMING MEDICINE STOCK CO., LTD. |
|
| CP01 | Change in the name or title of a patent holder |
Patentee after: Kunming Pharmaceutical Industry Group Corp., Ltd. Patentee before: Kunming Pharmaceutical Co., Ltd. |
|
| C56 | Change in the name or address of the patentee |
Owner name: KPC CO., LTD. Free format text: FORMER NAME: KUNMING PHARMACEUTICAL INDUSTRY GROUP CORP., LTD. |
|
| CP03 | Change of name, title or address |
Address after: 650106 Kunming science and Technology Industrial Development Zone, Yunnan Province Road No. 166 Patentee after: Kun Yao Group Plc Address before: 650100, seven kilometers west of Kunming City, Yunnan Province Patentee before: Kunming Pharmaceutical Industry Group Corp., Ltd. |
|
| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20010815 |