JP2002511777A - 調放性粒子の埋包およびカプセル化 - Google Patents
調放性粒子の埋包およびカプセル化Info
- Publication number
- JP2002511777A JP2002511777A JP52055898A JP52055898A JP2002511777A JP 2002511777 A JP2002511777 A JP 2002511777A JP 52055898 A JP52055898 A JP 52055898A JP 52055898 A JP52055898 A JP 52055898A JP 2002511777 A JP2002511777 A JP 2002511777A
- Authority
- JP
- Japan
- Prior art keywords
- hydrochloride
- sodium
- acid
- starch
- barrel
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000002245 particle Substances 0.000 title abstract description 41
- 238000005538 encapsulation Methods 0.000 title description 15
- 238000013270 controlled release Methods 0.000 title description 12
- 239000011159 matrix material Substances 0.000 claims abstract description 138
- 239000008393 encapsulating agent Substances 0.000 claims abstract description 117
- 239000000203 mixture Substances 0.000 claims abstract description 92
- 229920002472 Starch Polymers 0.000 claims abstract description 91
- 239000008107 starch Substances 0.000 claims abstract description 91
- 235000019698 starch Nutrition 0.000 claims abstract description 91
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 84
- 239000000463 material Substances 0.000 claims abstract description 64
- 238000002156 mixing Methods 0.000 claims abstract description 39
- 239000000126 substance Substances 0.000 claims abstract description 33
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 20
- 239000004014 plasticizer Substances 0.000 claims abstract description 19
- 230000002209 hydrophobic effect Effects 0.000 claims abstract description 13
- 230000006378 damage Effects 0.000 claims abstract description 12
- 230000002829 reductive effect Effects 0.000 claims abstract description 12
- -1 amcinoid Chemical compound 0.000 claims description 163
- 239000000047 product Substances 0.000 claims description 78
- 238000000034 method Methods 0.000 claims description 54
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 44
- 239000004615 ingredient Substances 0.000 claims description 35
- 238000010438 heat treatment Methods 0.000 claims description 22
- 239000002253 acid Substances 0.000 claims description 20
- 239000011734 sodium Substances 0.000 claims description 14
- 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 13
- 229940083542 sodium Drugs 0.000 claims description 13
- 229910052708 sodium Inorganic materials 0.000 claims description 13
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- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 9
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 9
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 8
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims description 8
- 239000006185 dispersion Substances 0.000 claims description 8
- LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 claims description 8
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 8
- 239000003921 oil Substances 0.000 claims description 8
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- 235000018102 proteins Nutrition 0.000 claims description 8
- 102000004169 proteins and genes Human genes 0.000 claims description 8
- 108090000623 proteins and genes Proteins 0.000 claims description 8
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 8
- 229940095064 tartrate Drugs 0.000 claims description 8
- 239000002775 capsule Substances 0.000 claims description 7
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- 150000002632 lipids Chemical class 0.000 claims description 7
- 235000016709 nutrition Nutrition 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 6
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 claims description 6
- MJVAVZPDRWSRRC-UHFFFAOYSA-N Menadione Chemical compound C1=CC=C2C(=O)C(C)=CC(=O)C2=C1 MJVAVZPDRWSRRC-UHFFFAOYSA-N 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 6
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 6
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims description 6
- 235000007264 Triticum durum Nutrition 0.000 claims description 6
- 241000700605 Viruses Species 0.000 claims description 6
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- 230000009477 glass transition Effects 0.000 claims description 6
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- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims description 6
- 229920003133 pregelled starch Polymers 0.000 claims description 6
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims description 6
- FZKWRPSUNUOXKJ-CVHRZJFOSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide;hydrate Chemical compound O.C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O FZKWRPSUNUOXKJ-CVHRZJFOSA-N 0.000 claims description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 5
- XUIIKFGFIJCVMT-LBPRGKRZSA-N L-thyroxine Chemical compound IC1=CC(C[C@H]([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-LBPRGKRZSA-N 0.000 claims description 5
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 5
- 241000209143 Triticum turgidum subsp. durum Species 0.000 claims description 5
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- 229960003722 doxycycline Drugs 0.000 claims description 5
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims description 5
- 239000002917 insecticide Substances 0.000 claims description 5
- NXFQHRVNIOXGAQ-YCRREMRBSA-N nitrofurantoin Chemical compound O1C([N+](=O)[O-])=CC=C1\C=N\N1C(=O)NC(=O)C1 NXFQHRVNIOXGAQ-YCRREMRBSA-N 0.000 claims description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 5
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 5
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- 229940088594 vitamin Drugs 0.000 claims description 5
- 229930003231 vitamin Natural products 0.000 claims description 5
- 235000013343 vitamin Nutrition 0.000 claims description 5
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- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims description 4
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims description 4
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims description 4
- YKFCISHFRZHKHY-NGQGLHOPSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid;trihydrate Chemical compound O.O.O.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1 YKFCISHFRZHKHY-NGQGLHOPSA-N 0.000 claims description 4
- DIWRORZWFLOCLC-HNNXBMFYSA-N (3s)-7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one Chemical compound N([C@H](C(NC1=CC=C(Cl)C=C11)=O)O)=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-HNNXBMFYSA-N 0.000 claims description 4
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims description 4
- GIKNHHRFLCDOEU-UHFFFAOYSA-N 4-(2-aminopropyl)phenol Chemical compound CC(N)CC1=CC=C(O)C=C1 GIKNHHRFLCDOEU-UHFFFAOYSA-N 0.000 claims description 4
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 claims description 4
- KHOITXIGCFIULA-UHFFFAOYSA-N Alophen Chemical compound C1=CC(OC(=O)C)=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OC(C)=O)C=C1 KHOITXIGCFIULA-UHFFFAOYSA-N 0.000 claims description 4
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims description 4
- KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 claims description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 4
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 claims description 4
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- WDJUZGPOPHTGOT-OAXVISGBSA-N Digitoxin Natural products O([C@H]1[C@@H](C)O[C@@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@@](C)([C@H](C6=CC(=O)OC6)CC5)CC4)CC3)CC2)C[C@H]1O)[C@H]1O[C@@H](C)[C@H](O[C@H]2O[C@@H](C)[C@@H](O)[C@@H](O)C2)[C@@H](O)C1 WDJUZGPOPHTGOT-OAXVISGBSA-N 0.000 claims description 4
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- LJCNRYVRMXRIQR-OLXYHTOASA-L potassium sodium L-tartrate Chemical compound [Na+].[K+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O LJCNRYVRMXRIQR-OLXYHTOASA-L 0.000 description 1
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- 230000002028 premature Effects 0.000 description 1
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- 235000012434 pretzels Nutrition 0.000 description 1
- WIKYUJGCLQQFNW-UHFFFAOYSA-N prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 description 1
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- 230000001737 promoting effect Effects 0.000 description 1
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- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- BALXUFOVQVENIU-KXNXZCPBSA-N pseudoephedrine hydrochloride Chemical compound [H+].[Cl-].CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-KXNXZCPBSA-N 0.000 description 1
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- YSAUAVHXTIETRK-AATRIKPKSA-N pyrantel Chemical compound CN1CCCN=C1\C=C\C1=CC=CS1 YSAUAVHXTIETRK-AATRIKPKSA-N 0.000 description 1
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- NHDHVHZZCFYRSB-UHFFFAOYSA-N pyriproxyfen Chemical compound C=1C=CC=NC=1OC(C)COC(C=C1)=CC=C1OC1=CC=CC=C1 NHDHVHZZCFYRSB-UHFFFAOYSA-N 0.000 description 1
- 229960002778 pyrvinium Drugs 0.000 description 1
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- 238000011084 recovery Methods 0.000 description 1
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- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 1
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- 150000004671 saturated fatty acids Chemical class 0.000 description 1
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- 238000007493 shaping process Methods 0.000 description 1
- 238000004904 shortening Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- 235000010288 sodium nitrite Nutrition 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 229960003339 sodium phosphate Drugs 0.000 description 1
- GOZDTZWAMGHLDY-UHFFFAOYSA-L sodium picosulfate Chemical compound [Na+].[Na+].C1=CC(OS(=O)(=O)[O-])=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS([O-])(=O)=O)C=C1 GOZDTZWAMGHLDY-UHFFFAOYSA-L 0.000 description 1
- 229960005077 sodium picosulfate Drugs 0.000 description 1
- 239000001476 sodium potassium tartrate Substances 0.000 description 1
- 235000011006 sodium potassium tartrate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229940001941 soy protein Drugs 0.000 description 1
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- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 1
- 229960002256 spironolactone Drugs 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
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- 150000003431 steroids Chemical class 0.000 description 1
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- 150000008163 sugars Chemical class 0.000 description 1
- 229960002673 sulfacetamide Drugs 0.000 description 1
- SKIVFJLNDNKQPD-UHFFFAOYSA-N sulfacetamide Chemical compound CC(=O)NS(=O)(=O)C1=CC=C(N)C=C1 SKIVFJLNDNKQPD-UHFFFAOYSA-N 0.000 description 1
- 229960002597 sulfamerazine Drugs 0.000 description 1
- QPPBRPIAZZHUNT-UHFFFAOYSA-N sulfamerazine Chemical compound CC1=CC=NC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 QPPBRPIAZZHUNT-UHFFFAOYSA-N 0.000 description 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 description 1
- 229960001544 sulfathiazole Drugs 0.000 description 1
- JNMRHUJNCSQMMB-UHFFFAOYSA-N sulfathiazole Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=NC=CS1 JNMRHUJNCSQMMB-UHFFFAOYSA-N 0.000 description 1
- 238000004381 surface treatment Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- 229960000351 terfenadine Drugs 0.000 description 1
- QIWDGSYHBCMXSI-UHFFFAOYSA-J tetrasodium;(2-methyl-4-phosphonatooxynaphthalen-1-yl) phosphate;hexahydrate Chemical compound O.O.O.O.O.O.[Na+].[Na+].[Na+].[Na+].C1=CC=CC2=C(OP([O-])([O-])=O)C(C)=CC(OP([O-])([O-])=O)=C21 QIWDGSYHBCMXSI-UHFFFAOYSA-J 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
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- MDMUQRJQFHEVFG-UHFFFAOYSA-J thorium(iv) iodide Chemical compound [I-].[I-].[I-].[I-].[Th+4] MDMUQRJQFHEVFG-UHFFFAOYSA-J 0.000 description 1
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- 230000005068 transpiration Effects 0.000 description 1
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- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
- 229960004479 trihexyphenidyl hydrochloride Drugs 0.000 description 1
- QDWJJTJNXAKQKD-UHFFFAOYSA-N trihexyphenidyl hydrochloride Chemical compound Cl.C1CCCCC1C(C=1C=CC=CC=1)(O)CCN1CCCCC1 QDWJJTJNXAKQKD-UHFFFAOYSA-N 0.000 description 1
- 229960002575 trimethobenzamide hydrochloride Drugs 0.000 description 1
- FMHHVULEAZTJMA-UHFFFAOYSA-N trioxsalen Chemical compound CC1=CC(=O)OC2=C1C=C1C=C(C)OC1=C2C FMHHVULEAZTJMA-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
- 229960001572 vancomycin hydrochloride Drugs 0.000 description 1
- LCTORFDMHNKUSG-XTTLPDOESA-N vancomycin monohydrochloride Chemical compound Cl.O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)[C@H](O)[C@H](C)O1 LCTORFDMHNKUSG-XTTLPDOESA-N 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
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- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
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- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
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- 239000003039 volatile agent Substances 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
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- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
- A23L27/70—Fixation, conservation, or encapsulation of flavouring agents
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- A—HUMAN NECESSITIES
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- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
- A23L29/212—Starch; Modified starch; Starch derivatives, e.g. esters or ethers
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
- A23P10/00—Shaping or working of foodstuffs characterised by the products
- A23P10/20—Agglomerating; Granulating; Tabletting
- A23P10/25—Agglomeration or granulation by extrusion or by pressing, e.g. through small holes, through sieves or between surfaces
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
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- B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
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- B29B7/30—Mixing; Kneading continuous, with mechanical mixing or kneading devices
- B29B7/34—Mixing; Kneading continuous, with mechanical mixing or kneading devices with movable mixing or kneading devices
- B29B7/38—Mixing; Kneading continuous, with mechanical mixing or kneading devices with movable mixing or kneading devices rotary
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- B29B7/42—Mixing; Kneading continuous, with mechanical mixing or kneading devices with movable mixing or kneading devices rotary with single shaft with screw or helix
- B29B7/421—Mixing; Kneading continuous, with mechanical mixing or kneading devices with movable mixing or kneading devices rotary with single shaft with screw or helix with screw and additionally other mixing elements on the same shaft, e.g. paddles, discs, bearings, rotor blades of the Banbury type
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- B—PERFORMING OPERATIONS; TRANSPORTING
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- B29B7/482—Mixing; Kneading continuous, with mechanical mixing or kneading devices with movable mixing or kneading devices rotary with more than one shaft with intermeshing devices, e.g. screws provided with screw parts in addition to other mixing parts, e.g. paddles, gears, discs
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- B29B7/72—Measuring, controlling or regulating
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- B29B7/86—Component parts, details or accessories; Auxiliary operations for working at sub- or superatmospheric pressure
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- B29C48/00—Extrusion moulding, i.e. expressing the moulding material through a die or nozzle which imparts the desired form; Apparatus therefor
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- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Mechanical Engineering (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Medicinal Preparation (AREA)
- Manufacturing Of Micro-Capsules (AREA)
- General Preparation And Processing Of Foods (AREA)
- Lubricants (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Formation And Processing Of Food Products (AREA)
- Fodder In General (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
- Extrusion Moulding Of Plastics Or The Like (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. a.少なくとも1種類の可塑化可能なマトリックス材料を少なくとも1種類の 可塑剤とカプセル化剤の放出速度を調節するための少なくとも1種類の成分と混 合し、当該混合を低剪断条件下で行ない、可塑化可能なマトリックス材料を前記 少なくとも1種類の可塑化材料を実質的に破壊することなく可塑化し、かつ実質 的に均質な可塑化物質を得る、 b.前記可塑化物質中の可塑剤の含有量を減らし、 c.可塑化物質の温度を下げ、冷却された可塑化物質を得る、 d.成形可能な混合部を得るため、少なくとも1種類のカプセル化剤を前記冷却さ れた可塑化物質と混合し、当該混合を前記少なくとも1種類のカプセル化剤の実 質的な熱的破壊を防止する可塑化物質温度で低剪断条件下で行ない、 e.前記成形可能混合物を金型を通して押出して押出し物を得、 f.前記押出し物を切断して部片(ピース)にする、 ことを含む、マトリックス中に成分を連続的にカプセル化または埋包する方法。 2.前記可塑化可能な物質と前記可塑剤を混合し、当該可塑化可能な物質の溶融 またはガラス転移温度以上に加熱した後、前記少なくとも1種類の放出速度調節 成分と混合する、請求項1記載の方法。 3.前記可塑化可能な物質、前記可塑剤、および前記少なくとも1種類の放出速 度調節成分を混合し、その後可塑化可能な物質の溶融またはガラス転移温度以上 に加熱することを特徴とする請求項1記載の方法。 4.前記カプセル化剤が前記冷却された可塑化物質と混合される前にフィルム形 成物質で被覆される、請求項1記載の方法。 5.前記ピースがフィルム形成物質で被覆される、請求項1記載の方法。 6.前記ピースがフィルム形成物質で被覆される、請求項4記載の方法。 7.前記可塑化可能なマトリックス材料がでん粉からなり、前記可塑剤が水から なり、かつ実質的に均質な可塑化物質を得るための前記混合を、前記でん粉 を少なくとも実質的にゲル化するために加熱しながら行う、請求項1記載の方法 。 8.前記少なくとも1種類の放出速度調節成分が疎水性成分である、請求項7記載 の方法。 9.前記疎水性成分が、脂肪、油、ワックス、脂肪酸、乳化剤、ポリオレフィン 、ポリウレタン、ポリ塩化ビニル、パラフィン、ポリ酢酸ビニル、および変性で ん粉からなる群から選ばれた少なくとも1つである、請求項8記載の方法。 10.前記少なくとも1種類の放出速度調節成分が水結合能力の高い成分である ことを特徴とする請求項7記載の方法。 11.前記水結合能力の高い成分が、蛋白質および親水コロイドからなる群から 選ばれる、請求項10記載の方法。 12.前記少なくとも1種類の放出速度調節剤の量が、前記でん粉の重量に対し て約10重量%から約35重量%である、請求項7記載の方法。 13.前記ピースのでん粉含有量が当該ピースの重量に対して少なくとも約40重 量%である、請求項12記載の方法。 14.可塑化物質の水分含有量を少なくとも約10重量%現象させる、請求項7記 載の方法。 15.前記可塑化可能なマトリクス材料が予備ゲル化でん粉またはデュラム小麦 粉からなり、かつ前記可塑剤が水である、請求項1記載の方法。 16.前記カプセル化剤を全長約3-10 1/dの分散型混合スクリュ部分で混合し、 添加される成分をマトリクス中に充分に混合、分散および埋包させる、請求項7 記載の方法。 17.押出し物をカッター、ペレタイザー、回転式ナイフまたは窪んだ型を有す る対向回転型成形ドラムを用いて、0.5から10の長さ対直径比を有するピース分 離する、請求項1記載の方法。 18.前記カプセル化剤が熱感受性薬理学的成分、栄養治療学的成分、栄養学的 成分、着香成分、香料成分、分散剤または界面活性成分、あるいは生物学的活性 成分の少なくとも1種類である、請求項1記載の方法により得られるカプセ ル化製品。 19.請求項1記載の方法により得られるカプセル化製品を含む組成物。 20.前記カプセル化剤が、アセプロマジン、アセトアミノフェン、アセトヘキ サミド、アセトヒドロキサム酸、アセチルコリン、アセチルシステインアシクロ ビール、アルベンダゾール、ジプロピオン酸アルクロメタゾン、アロプリノール 、アルプラゾラム、アルプロスタジル、アムシノイド、アマンタジン、アムジノ シリン、アミカシンアミロライド、アミノカプロン酸、アミノフィリン、アミノ サリチル酸塩、アミノサリチル酸、アミトリプチリン塩酸塩、塩化アンモニウム 、アモバルビタール、アモジアキン塩酸塩、アモキサピン、アモキシリン、硫酸 アンフェタミン、アンホテリシン、アンピシリンアンプロリウム、アセタゾール 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ィリン、チアベンダゾール、チアミン塩酸塩、チアミン、チアミラル、チエチル ペラジンシメロサル、チオグアニン、チオリダジン塩酸塩、チストレプトン、チ オテパ、チオチキセン、トレオニン、チロイド、チカルシリン、チモロール、チ オコナゾール、二酸化チタン、トラザアミド、トルブタミド、トルメチン、トル ナフテート、トラゾドン塩酸塩、トレチノイン、トリアセチン、トリアムシノロ ン、トリアムテレン、トリアゾラム、トリコールフォン、トリクロルメチアジド 、トリエンチン塩酸塩、トリフルオペラジン塩酸塩、トリフルプロマジン、トリ ヘキシフェニジル塩酸塩、酒石酸トリメプラジン、トリメタジオン、トリメトベ ンズアミド塩酸塩、トリメトプリム、トリオキサレン、トリペレナミン、トリプ ロリジン、トリスルファピリミジン、トロピカミド、トリプシン、トリプトファ ン、ツベルクリン、チロキサポール、チロパノエートナトリウム、チロシン、チ ロトリシン、チロスリシンベタメタゾン、チオクト酸、ソタロール、サルブタモ ール、ノルフェネフリン、シリマリン、ジヒドロエルゴタミン、ブフロメジル、 エトフィブレート、インドメタシン、尿素、バリン、バルプロイン酸、バンコマ イシン塩酸塩、バソプレシン、ベラプラミル、ビダラビン、ビンブラスチン、ビ ンクリスチン、ビタミン、ワルファリン、黄熱病ワクチン、酢酸亜鉛、炭酸亜鉛 、塩化亜鉛、グルコン酸亜鉛、ベータアセチルジゴキシン、ピロキシカム、ハロ ペリドール、ISMN、アミトリプチリン、ジクロフェナック、ニフェジピン、ベラ パミル、ピリチノール、ニトレンジピン、ドキシサイクリン、ブロムヘキシン、 メチルプルドニソロン、クロニジン、フェノフィブレート、アロプリノール、ピ レニエピン、レボチロキシン、タモキシフェン、メチルジゴキシン、o−(ベー タ−ヒドロキシエチル)−ルトシド、プロピシリン、アシクロビールモノ硝酸塩 、パラセタモール、ナフチドロフリル、ペントキシフィリン、プロパフェノン、 アセブトロール、 L−チロキシン、トラマドール、ブロモクリプチン、ロペラミド、ケトチフェン 、フェノテロール、カドベリセート、プロパノロール、マレイン酸エナラプリル ハイドロジェン、ベザフェブレート、ISDN、ガロパミル、ニコチン酸キサンチノ ール、ジギトキシン、フルニトラゼパム、ベンシクラン、デキサパンテノール、 ピンドロール、ロラゼパム、ジルチアゼム、ピラセタム、フェノキシメチルペニ シリン、フロセミド、ブロマゼパム、フルナリジン、エリスロマイシン、メトク ロプラミド、アセメタシン、ラニチジン、ビペリデン、メタミゾール、ドキセピ ン、クロロアゼピン酸二カリウム、テトラゼパム、燐酸エストラムスチン、テル ブタリン、カプトプリル、マプロチリン、プロゾシン、アテノロール、グリベン クラミド、セファクロール、エチルフリン、シメチジン、テオフィリン、ヒドロ モルフォン、イブプロフェン、プリミドン、クロバザム、オキサセプロール、メ ドロキシプロゲステロン、フレカイニド、グルタミン酸ピリドキサル5燐酸塩、 ヒメクロモン、エトフィリンクロフィブレート、ビンカミン、シナリジン、ジア ゼパム、ケトプロフェン、フルペンチキソール、モルシミン、グリボルヌリド、 ジメチンデン、メルペロン、ソキノロール、ジヒドロコデイン、クロメチアゾー ル、クレマスチン、グリソキセピド、カリジノゲナーゼ、オキシフェドリン、バ クロフェン、カルボキシメチルシステイン、チオリダジン、ベタヒスチン、L− トリプトファン、ムルトール、ブロメライン、プレニラミン、サラゾスルファピ リジン、アステミゾール、スルピリド、ベンゼラジド、ジベンゼピン、アセチル サリチル酸、ミコナゾール、ナイスタチン、ケトコナゾール、ナトリウムピコス ルフェート、コルチラミン、ゲンフィブロシル、リファムピシン、フルオコルト ロン、メキシレチン、アモキシリン、テルフエナドリン、ムコ多糖体多硫酸エス テル、トリアゾラム、ミアンセリン、チアプロフェン酸、アメジニウムメチルス ルフェート、メフロキン、プロブコール、キニジン、カルバマゼピン、L−アス パルチン酸塩、ペンブトロール、ピレタニド、エスキンアミトリプチリン、シプ ロテロン、バルプロイン酸ナトリウム、メベベリン、ビサコジル、5−アミノサ リチル酸、ジヒドララジン、マガルドレート、フェンプロクモン、アマンタジン 、ナプロキセン、 カルテオロール、ファモチジン、メチルドーパ、オーラノフィン、エストリオー ル、ナドロール、レボメプロマジン、ドキソルビシン、メドフェノキセート、ア ザチオプリン、フルタミド、ノルフロキサシン、フェンジリン、酒石酸プラジマ リウム、ホスホナチドの脂質誘導体、両親媒性ポリマー、アデノシン誘導体、硫 化タンニン、モノクローナル抗体、および水溶性テキサチリンの金属複合体、か らなる群から選ばれる少なくとも1員である、請求項1記載の方法により得られる カプセル化製品。 21.前記カプセル化物が、抗酸化剤、植物化学品、ホルモン、ビタミン、プロ ビタミン、ミネラル、微生物、生物学的前駆物質(prebiotics)、生物学的親和 性物質(probiotics)、微量成分、必須および/または高度不飽和脂肪酸、抗生 物質、栄養補助品、酵素、ジドブジン含有処方品、巨大分子ポリペプチド、抗ウ イルスおよび抗腫瘍剤として有用な芳香族ニトロおよびニトロソ化合物およびそ れらの代謝物、HIVプロテアーゼ阻害剤、抗生物質、ウイルス、色素、ステロイ ド、オリゴペプチド、ジペプチド、アミノ酸、着香成分、香料成分、分散剤およ び界面活性成分、ホスファナチドの脂質誘導体、両親媒性ポリマー、アデノシン 誘導体、硫酸化タンニン、モノクローナル抗体、および水溶性テキサチリン殻な る群から選ばれる少なくとも1員である、請求項1記載の方法により得られるカプ セル化製品。 22.前記カプセル化剤が、除草剤、病害虫防除剤、殺虫剤、殺鼠剤、及び殺菌 剤からなる群から選ばれる少なくとも1員である、請求項1記載の方法により得ら れるカプセル化製品。 23.即席朝食用シリアル類、デザート・ミックス、ベーキング・ミックス、ベ ーキング粉、ディナー・ミックス、ヨーグルト、フルーツ・スナック、電子レン ジ用ポップコーン、および穀類スナックからなる群から選ばれるものであること を特徴とする請求項19記載の組成物。 24.前記可塑化可能なマトリクス物質が、でん粉、シクロデキストリン、デキ ストリン、単糖、二糖、ポリビニルピロリドン、N−ビニルピロリドンと酢酸ビ ニルのコポリマー、ポリビニルアルコール、セルロースエステル、セルロ ースエーテルおよびポリエチレングリコールからなる群から選ばれる少なくとも 1員である、請求項1記載の方法により得られるカプセル化製品。
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PCT/US1997/018984 WO1998018610A1 (en) | 1996-10-28 | 1997-10-27 | Embedding and encapsulation of controlled release particles |
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JP52055898A Pending JP2002511777A (ja) | 1996-10-28 | 1997-10-27 | 調放性粒子の埋包およびカプセル化 |
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US (1) | US6190591B1 (ja) |
EP (1) | EP0935523B1 (ja) |
JP (1) | JP2002511777A (ja) |
AT (1) | ATE277739T1 (ja) |
AU (1) | AU744156B2 (ja) |
CA (1) | CA2269806C (ja) |
DE (1) | DE69730982T2 (ja) |
ES (1) | ES2565163T3 (ja) |
NO (1) | NO992036L (ja) |
PL (1) | PL191399B1 (ja) |
WO (1) | WO1998018610A1 (ja) |
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Also Published As
Publication number | Publication date |
---|---|
NO992036D0 (no) | 1999-04-28 |
EP0935523A4 (en) | 1999-12-29 |
DE69730982D1 (de) | 2004-11-04 |
DE69730982T2 (de) | 2005-09-01 |
US6190591B1 (en) | 2001-02-20 |
CA2269806A1 (en) | 1998-05-07 |
AU744156B2 (en) | 2002-02-14 |
NO992036L (no) | 1999-04-28 |
PL191399B1 (pl) | 2006-05-31 |
ES2565163T3 (es) | 2016-03-31 |
EP0935523A1 (en) | 1999-08-18 |
ATE277739T1 (de) | 2004-10-15 |
WO1998018610A1 (en) | 1998-05-07 |
CA2269806C (en) | 2006-01-24 |
AU4991597A (en) | 1998-05-22 |
EP0935523B1 (en) | 2004-09-29 |
PL333095A1 (en) | 1999-11-08 |
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