JPS6411039B2 - - Google Patents
Info
- Publication number
- JPS6411039B2 JPS6411039B2 JP13528582A JP13528582A JPS6411039B2 JP S6411039 B2 JPS6411039 B2 JP S6411039B2 JP 13528582 A JP13528582 A JP 13528582A JP 13528582 A JP13528582 A JP 13528582A JP S6411039 B2 JPS6411039 B2 JP S6411039B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- acid
- formula
- trihaloacetyl
- hydrogen
- 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
Links
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 93
- 238000000034 method Methods 0.000 claims description 54
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims description 36
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 30
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 30
- 150000001412 amines Chemical class 0.000 claims description 27
- 239000002253 acid Substances 0.000 claims description 25
- 150000001875 compounds Chemical class 0.000 claims description 23
- 238000006243 chemical reaction Methods 0.000 claims description 22
- 150000003431 steroids Chemical class 0.000 claims description 22
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims description 20
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 20
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical group CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims description 18
- 125000006239 protecting group Chemical group 0.000 claims description 18
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 125000004432 carbon atom Chemical group C* 0.000 claims description 13
- 238000005886 esterification reaction Methods 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 claims description 10
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 claims description 9
- 150000007513 acids Chemical class 0.000 claims description 9
- 230000032050 esterification Effects 0.000 claims description 9
- 150000002148 esters Chemical class 0.000 claims description 9
- 230000008569 process Effects 0.000 claims description 9
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 8
- 150000001244 carboxylic acid anhydrides Chemical class 0.000 claims description 8
- 239000000908 ammonium hydroxide Substances 0.000 claims description 7
- 239000003246 corticosteroid Substances 0.000 claims description 7
- 150000002367 halogens Chemical class 0.000 claims description 7
- 150000002431 hydrogen Chemical group 0.000 claims description 7
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 239000000460 chlorine Chemical group 0.000 claims description 6
- 229910052801 chlorine Chemical group 0.000 claims description 6
- 238000003379 elimination reaction Methods 0.000 claims description 6
- 239000011737 fluorine Chemical group 0.000 claims description 6
- 229910052731 fluorine Inorganic materials 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- -1 trifluoroacetoxy group Chemical group 0.000 claims description 6
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims description 5
- 229940092714 benzenesulfonic acid Drugs 0.000 claims description 5
- 230000003197 catalytic effect Effects 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- 125000002252 acyl group Chemical group 0.000 claims description 4
- 125000006165 cyclic alkyl group Chemical group 0.000 claims description 4
- 125000004122 cyclic group Chemical group 0.000 claims description 4
- 239000007789 gas Substances 0.000 claims description 4
- 239000002904 solvent Substances 0.000 claims description 4
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 150000001735 carboxylic acids Chemical class 0.000 claims description 3
- 230000008030 elimination Effects 0.000 claims description 3
- 229910052736 halogen Inorganic materials 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- JJWLVOIRVHMVIS-UHFFFAOYSA-N isopropylamine Chemical compound CC(C)N JJWLVOIRVHMVIS-UHFFFAOYSA-N 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims 2
- QUSNBJAOOMFDIB-UHFFFAOYSA-N Ethylamine Chemical group CCN QUSNBJAOOMFDIB-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 claims 2
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 claims 2
- DMBHHRLKUKUOEG-UHFFFAOYSA-N diphenylamine Chemical compound C=1C=CC=CC=1NC1=CC=CC=C1 DMBHHRLKUKUOEG-UHFFFAOYSA-N 0.000 claims 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- HQABUPZFAYXKJW-UHFFFAOYSA-N butan-1-amine Chemical compound CCCCN HQABUPZFAYXKJW-UHFFFAOYSA-N 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003141 primary amines Chemical group 0.000 claims 1
- 239000012429 reaction media Substances 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
- 150000003335 secondary amines Chemical group 0.000 claims 1
- 150000003512 tertiary amines Chemical group 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 54
- 239000000047 product Substances 0.000 description 53
- 239000000203 mixture Substances 0.000 description 43
- 238000002360 preparation method Methods 0.000 description 24
- 238000003756 stirring Methods 0.000 description 19
- 229940070710 valerate Drugs 0.000 description 19
- 238000001556 precipitation Methods 0.000 description 16
- 238000002844 melting Methods 0.000 description 15
- 230000008018 melting Effects 0.000 description 15
- 239000011541 reaction mixture Substances 0.000 description 14
- 238000005917 acylation reaction Methods 0.000 description 13
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 description 13
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 12
- 239000007787 solid Substances 0.000 description 12
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 11
- 229960002537 betamethasone Drugs 0.000 description 11
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 description 11
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 10
- 229940092705 beclomethasone Drugs 0.000 description 10
- 238000007796 conventional method Methods 0.000 description 10
- 239000000376 reactant Substances 0.000 description 10
- QAEDZJGFFMLHHQ-UHFFFAOYSA-N trifluoroacetic anhydride Chemical compound FC(F)(F)C(=O)OC(=O)C(F)(F)F QAEDZJGFFMLHHQ-UHFFFAOYSA-N 0.000 description 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- DUCKXCGALKOSJF-UHFFFAOYSA-N pentanoyl pentanoate Chemical compound CCCCC(=O)OC(=O)CCCC DUCKXCGALKOSJF-UHFFFAOYSA-N 0.000 description 9
- 239000002994 raw material Substances 0.000 description 9
- 238000001953 recrystallisation Methods 0.000 description 9
- ZHMASVAJFJFFLS-UHFFFAOYSA-N 5-chloropyridin-3-amine Chemical compound NC1=CN=CC(Cl)=C1 ZHMASVAJFJFFLS-UHFFFAOYSA-N 0.000 description 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 8
- 230000010933 acylation Effects 0.000 description 8
- 229910021529 ammonia Inorganic materials 0.000 description 7
- 235000011114 ammonium hydroxide Nutrition 0.000 description 7
- CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 description 7
- 238000002474 experimental method Methods 0.000 description 7
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 6
- WQDUMFSSJAZKTM-UHFFFAOYSA-N Sodium methoxide Chemical compound [Na+].[O-]C WQDUMFSSJAZKTM-UHFFFAOYSA-N 0.000 description 6
- 239000000538 analytical sample Substances 0.000 description 6
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 6
- 229940082500 cetostearyl alcohol Drugs 0.000 description 5
- 238000001914 filtration Methods 0.000 description 5
- 238000002955 isolation Methods 0.000 description 5
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 5
- 239000000523 sample Substances 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 5
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 229960004703 clobetasol propionate Drugs 0.000 description 4
- 229960001334 corticosteroids Drugs 0.000 description 4
- 239000006071 cream Substances 0.000 description 4
- 229960003957 dexamethasone Drugs 0.000 description 4
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 4
- CIWBQSYVNNPZIQ-PKWREOPISA-N dexamethasone dipropionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CIWBQSYVNNPZIQ-PKWREOPISA-N 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000007921 spray Substances 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 238000005406 washing Methods 0.000 description 4
- WFDIJRYMOXRFFG-UHFFFAOYSA-N Acetic anhydride Chemical compound CC(=O)OC(C)=O WFDIJRYMOXRFFG-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 description 3
- 201000004624 Dermatitis Diseases 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- 239000003377 acid catalyst Substances 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- YHASWHZGWUONAO-UHFFFAOYSA-N butanoyl butanoate Chemical compound CCCC(=O)OC(=O)CCC YHASWHZGWUONAO-UHFFFAOYSA-N 0.000 description 3
- 229960002842 clobetasol Drugs 0.000 description 3
- UQEAIHBTYFGYIE-UHFFFAOYSA-N hexamethyldisiloxane Chemical compound C[Si](C)(C)O[Si](C)(C)C UQEAIHBTYFGYIE-UHFFFAOYSA-N 0.000 description 3
- 239000003701 inert diluent Substances 0.000 description 3
- 238000010255 intramuscular injection Methods 0.000 description 3
- 239000007927 intramuscular injection Substances 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 230000003287 optical effect Effects 0.000 description 3
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 3
- WYVAMUWZEOHJOQ-UHFFFAOYSA-N propionic anhydride Chemical compound CCC(=O)OC(=O)CC WYVAMUWZEOHJOQ-UHFFFAOYSA-N 0.000 description 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 3
- 238000003797 solvolysis reaction Methods 0.000 description 3
- 239000007858 starting material Substances 0.000 description 3
- 230000000699 topical effect Effects 0.000 description 3
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- VHRSUDSXCMQTMA-PJHHCJLFSA-N 6alpha-methylprednisolone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 VHRSUDSXCMQTMA-PJHHCJLFSA-N 0.000 description 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 2
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 2
- 229910002651 NO3 Inorganic materials 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 description 2
- QSZKFXMOBKKROF-YCUXZELOSA-N [(8s,9r,10s,11s,13s,14s,16s,17r)-17-(2-acetyloxyacetyl)-9-fluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] pentanoate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(C)=O)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O QSZKFXMOBKKROF-YCUXZELOSA-N 0.000 description 2
- 238000005903 acid hydrolysis reaction Methods 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 125000001931 aliphatic group Chemical group 0.000 description 2
- 229910052783 alkali metal Inorganic materials 0.000 description 2
- 150000001340 alkali metals Chemical class 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 description 2
- 238000009835 boiling Methods 0.000 description 2
- 238000004587 chromatography analysis Methods 0.000 description 2
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 2
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000012154 double-distilled water Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- 125000000524 functional group Chemical group 0.000 description 2
- 238000007429 general method Methods 0.000 description 2
- 239000008240 homogeneous mixture Substances 0.000 description 2
- 229910052740 iodine Inorganic materials 0.000 description 2
- 239000011630 iodine Substances 0.000 description 2
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 2
- 235000020778 linoleic acid Nutrition 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 description 2
- 229960005205 prednisolone Drugs 0.000 description 2
- 239000008159 sesame oil Substances 0.000 description 2
- 235000011803 sesame oil Nutrition 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 238000010561 standard procedure Methods 0.000 description 2
- 238000001256 steam distillation Methods 0.000 description 2
- SYVFBJQHOGXAMY-XUCMERPOSA-N (8s,9s,10r,13s,14s,17s)-10,13-dimethyl-17-propanoyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-one Chemical group C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)CC)[C@@]1(C)CC2 SYVFBJQHOGXAMY-XUCMERPOSA-N 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- LJSMGWBQOFWAPJ-UHFFFAOYSA-N 4-methoxy-3-(naphthalen-1-ylmethyl)-4-oxobutanoic acid Chemical compound C1=CC=C2C(CC(CC(O)=O)C(=O)OC)=CC=CC2=C1 LJSMGWBQOFWAPJ-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- FBRAWBYQGRLCEK-AVVSTMBFSA-N Clobetasone butyrate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CCC)[C@@]1(C)CC2=O FBRAWBYQGRLCEK-AVVSTMBFSA-N 0.000 description 1
- 241001440269 Cutina Species 0.000 description 1
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 description 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 description 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
- 201000009053 Neurodermatitis Diseases 0.000 description 1
- 239000004264 Petrolatum Substances 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010039793 Seborrhoeic dermatitis Diseases 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 150000007933 aliphatic carboxylic acids Chemical class 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 150000001793 charged compounds Chemical class 0.000 description 1
- XXIFVOHLGBURIG-OZCCCYNHSA-N clobetasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)CC2=O XXIFVOHLGBURIG-OZCCCYNHSA-N 0.000 description 1
- 229960005465 clobetasone butyrate Drugs 0.000 description 1
- 238000004440 column chromatography Methods 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 150000001886 cortisols Chemical class 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- SNHRLVCMMWUAJD-OMPPIWKSSA-N dexamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-OMPPIWKSSA-N 0.000 description 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 125000004185 ester group Chemical group 0.000 description 1
- 125000001033 ether group Chemical group 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 230000008570 general process Effects 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 239000012442 inert solvent Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 208000005005 intertrigo Diseases 0.000 description 1
- 235000015110 jellies Nutrition 0.000 description 1
- 239000008274 jelly Substances 0.000 description 1
- 238000001819 mass spectrum Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N nitrate group Chemical group [N+](=O)([O-])[O-] NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 229940066842 petrolatum Drugs 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- DGYSDXLCLKPUBR-SLPNHVECSA-N prednisolone valerate acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(C)=O)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O DGYSDXLCLKPUBR-SLPNHVECSA-N 0.000 description 1
- 229950008480 prednisolone valerate acetate Drugs 0.000 description 1
- 208000008742 seborrheic dermatitis Diseases 0.000 description 1
- 230000001235 sensitizing effect Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- 238000005809 transesterification reaction Methods 0.000 description 1
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
Landscapes
- Steroid Compounds (AREA)
Description
æ¬çºæã¯ã³ã«ãã³ã¹ããã€ããšã¹ãã«ã®æ°èŠè£œ
é æ³ã«é¢ããã ã³ã«ãã³ã¹ããã€ããæçç掻æ§ãæããããš
ã«ã€ããŠã¯å€ãããç¥ãããŠãããã³ã«ãã³ã¹ã
ãã€ãã«ãšã¹ãã«å®èœåºãå°å ¥ããããšã«ããã
ç¹ã«17äœã®ã¿ã«åã¯17äœãš21äœã«ãšã¹ãã«å®èœåº
ãå°å ¥ããããšã«ãããå±æç掻æ§ãããªãå¢é²
ãããããšãåæ§ã«ç¥ãããŠããããããã®ãšã¹
ãã«åããã³ã«ãã³ã¹ããã€ãã¯ãŸãå šèº«ç³»æŽ»æ§
ãæå°ã§ãããšããå©ç¹ããæäŸããã æ¬çºæã¯åŸèšã®åŒïŒïŒã®ååç©ã補é ããæ°
èŠã§æå¹ãªã«ãŒããæäŸãããã®ã§ããã ããæ æ¬çºæã«ãããšã次åŒïŒ ïŒåŒäžïŒžãR1ãR2åã³R3ã¯åŸèšã®æ矩ãæãïŒ
R5ã¯ããããã·ã«åºåã¯R6ã§ãããR6ã¯åŸèšã®
æ矩ãæããïŒã®ååç©ã®17äœã®ã¿åã¯åèšåŒ
ïŒïŒäžã®R5ãããããã·ã«åºã§ããå Žåã«ã¯17
äœåã³21äœããšã¹ãã«åããããšãããªãããã®
éãšã¹ãã«åã¯17äœã«åã¯17äœãš21äœã«å°å ¥ãã¹
ãåºãå«ãã«ã«ãã³é žã®ç¡æ°Žç©ãããªããé ¢é žãš
ïœâãã«ãšã³ã¹ã«ãã³é žãã¡ã¿ã³ã¹ã«ãã³é žãã
ã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é žåã³å¡©é žããéžãã
äžçš®ã®é žãšãããªãäžå¯Ÿã®åŒ·é žãšãšãã«çšããŠè¡
ãªãããšãç¹åŸŽãšãã次åŒïŒ ïœåŒäžâŠã¯äºéçµåãååšãåŸãããšãè¡šããïŒ
ã¯æ°ŽçŽ ãããçŽ åã¯å¡©çŽ ã§ããïŒR1ã¯æ°ŽçŽ ã
ããçŽ ãå¡©çŽ åã¯ã¡ãã«åºã§ãããã€R1ã¯Î±äœ
åã¯Î²äœã«ååšãåŸããã®ã§ããïŒR2ã¯ããã²
ã³ããªããœåã¯ããªããã¢ã»ããã·ïŒãããããª
ããã¢ã»ãã«åºã¯ããããã·ã«ä¿è·åºã§ããïŒåº
ã§ããïŒR3ã¯æ°ŽçŽ ãαâã¡ãã«åã¯Î²âã¡ãã«
åºã§ããïŒR4ã¯åŒRCOïŒãããã¯(i)ïŒã16åã®
ççŽ ååãæããçŽéãåå²éåã¯ç°åŒã¢ã«ãã«
åºã(ii)ïŒãïŒåã®ççŽ ååãæããã¢ã©ã«ãã«åº
åã¯(iii)ããšãã«åºã§ããïŒã®ã¢ã·ã«åºã§ããïŒ
R6ã¯æ°ŽçŽ ãïŒååã¯ïŒåã®ããã²ã³çœ®æåºåã¯
OR7ããããR7ã¯åŒRâ²COïŒåŒäžRâ²ã¯ïŒ²ãšåäžã§ã
ç°ãªã€ãŠãããã(i)ïŒã16åã®ççŽ ååãæãã
çŽéãåå²éåã¯ç°åŒã¢ã«ãã«åºã(ii)ïŒãïŒåã®
ççŽ ååãæããã¢ã©ã«ãã«åºåã¯(iii)ããšãã«åº
ã§ããïŒã®ã¢ã·ã«åºã§ãããã§ããïœã®ã³ã«ãã³
ã¹ããã€ããšã¹ãã«ã®è£œé æ³ãæäŸãããã ããã«æ¬çºæã®å¥ã®äžèŠæšã¯äžèšæ¬çºæã«åŸã
æ¹æ³ã«ãããåŒïŒïŒã«ãããŠR2ãããªããã¢
ã»ããã·åºã§ããååç©ãããªãã¡æ¬¡åŒïŒ ïŒåŒäžããR1ãR3åã³R5ã¯åèšã®æ矩ãæã
ãïŒããåºçºããŠåŒïŒïŒã«ãããŠR2ãããªã
ãã¢ã»ããã·åºã§ããååç©ãããªãã¡æ¬¡åŒïŒ ïŒåŒäžãâŠããR1ãR3ãR4åã³R6ã¯åèšã®æ
矩ãæããïŒã®ååç©ã補é ããã€ãã§åŒïŒâ²ïŒ
ã®ååç©ããäœçŽã¢ã«ã³ãŒã«ã®ååšäžã«ãçªçŽ å
åãè³éŠæç°ã®äžéšãæ§æããææ©ã¢ãã³ä»¥å€ã®
ææ©ã¢ãã³ãç¡æ°Žæº¶å€äžã«æº¶è§£ãããç¡æ°Žã¢ã³ã¢
ãã¢ã¬ã¹ãæ°Žé žåã¢ã³ã¢ããŠã åã¯ããã©ãžã³ãš
åå¿ãããŠ11âããªããã¢ã»ãã«ä¿è·åºãè±é¢ã
ãããããšãããªã次åŒïŒ ïŒåŒäžãâŠããR1ãR3ãR4åã³R6ã¯åèšã®æ
矩ãæããïŒã®ã³ã«ãã³ã¹ããã€ããšã¹ãã«ã®è£œ
é æ³ã«ããã ãããã€ãŠæ¬çºæã¯ãäžã€ã®äžè¬çãªæ¹æ³ã«ã
ã€ãŠãã¿ã¡ã¿ãŸã³ããããµã¡ã¿ãŸã³ããã¯ãã¡ã¿
ãŸã³ãã¯ããã¿ãŸãŒã«ããã¬ãããœãã³ããã€ã
ãã³ã«ããŸã³ãšã¹ãã«é¡ã®è£œé æ³ãåºãå å«ãã
ãã®ã§ããã ãããååç©ã®è£œé ã«å©çšãåŸãæ¢ç¥ã®åŸæ¥æ³
ã¯ã€ãã®äžçŸ€ã«åé¡ãåŸãã 第ïŒã®åŸæ¥æ³ã¯ãäŸãã°11äœãä¿è·åºã§äœãä¿
è·ããããšãªã17âãšã¹ãã«å®èœåºãçŽæ¥åæã¹
ããã€ãã«å°å ¥ãããã®ã§ããããã®åŸæ¥æ³ã¯J.
Amer.Chem.Soc.74ã5394ã96ãïŒ1952ïŒåã³è±
åœç¹èš±ç¬¬737291å·åã³ç¬¬1070751å·æ现æžåã³ç±³
åœç¹èš±ç¬¬3721687å·æ现æžã«äŸç€ºãããŠãããã
ã®ã¢ã·ã«åã¯ïœâãã«ãšã³ã¹ã«ãã³é žã®åŠãåŒ·é ž
觊åªã®ååšäžã«äœçŽèèªæã«ã«ãã³é žã®ç¡æ°Žç©ã
çšããŠè¡ããããããããã·ã«å®èœåºã®ãšã¹ãã«
åã®é äœã¯ç¬¬ïŒçŽããããã·ã«æ¬¡ãã§ç¬¬ïŒçŽãã
ããã·ã«ãæåŸã«ç¬¬ïŒçŽããããã·ã«åºã§ããã®
ã¯åšç¥ã§ãããå³ã¡ã11ïŒ17ïŒ21âããªãããã
ã·ã¹ããã€ãã®å Žåã«ã¯ãçŽæ¥ãšã¹ãã«åãè¡ã
ãšå¹Ÿåç°ãªã€ãçŸåçã§ã®21âã¢ããšã¹ãã«ãš
11ïŒ21âãžãšã¹ãã«ãš11ïŒ17ïŒ21âããªãšã¹ãã«
ãšããæãæ··åç©ãåŸããããåŸã€ãŠãã®æ··åç©
ããæèŠã®çæç©ãåé¢ããããšã¯ãé©åœãªæ¹æ³
ãèŠåºããããšããŠãçµæžçã«ã¯å®æœãåŸãªãã
æŽã«ã¯11ïŒ17ïŒ21âããªãšã¹ãã«äžã®äžæŽ»æ§å11
âãšã¹ãã«ãéžæçã«é€å»ããæ¹æ³ã¯çŸåšç¥ãã
ãŠããªãã 第ïŒã®åŸæ¥æ³ã¯ïŒã€ä»¥äžã®ãšã¹ãã«å®èœåºã®å°
å ¥åã«åæã¹ããã€ãã®å®èœåºãä¿è·ããå·¥çšã
䌎ãªãã11âããããã·ã«å®èœåºçšã®éåžžã®ä¿è·
åºã¯ããªããã¢ã»ããŒããããªã¡ãã«ã·ãªã«ãšãŒ
ãã«ãããã©ããããã©ã³âïŒ2â²ã€ã«ïŒãšãŒãã«
åã³ç¡é žãšã¹ãã«åºã§ããããããã®ä¿è·åºã®ã
ã¡ããªããã¢ã»ããŒãã¯ç±³åœç¹èš±ç¬¬2800489å·æ
现æžã«æåã«èšèŒãããŠãããè±åœç¹èš±ç¬¬
1097165å·åã³ç±³åœç¹èš±ç¬¬4024131å·æ现æžã§çšã
ãããŠãããããªã¡ãã«ã·ãªã«ãšãŒãã«ä¿è·åºã¯
è±åœç¹èš±ç¬¬1227992å·æ现æžã§çšããŠããããã®
調補æ³ã¯æœåºæè¡ïŒåé¿ããã®ã奜ãŸããïŒã䌎
ãªã€ãŠãããããã«ãæããåŸãããåçã¯æ Œå¥
è¯å¥œã§ã¯ãªããããã©ããããã©ã³âïŒ2â²ã€ã«ïŒ
ãšãŒãã«ä¿è·åºã¯ç±³åœç¹èš±ç¬¬4024131å·æ现æžã«
èšèŒãããŠãããåæ§ã«ãã®èª¿è£œæ³ã¯æœåºæè¡ã
䌎ãªããç¡é žãšã¹ãã«ä¿è·åºã¯å ãè±åœç¹èš±ç¬¬
1082573å·æ现æžã«èšèŒãããŠãã次ãã§åã³è±
åœç¹èš±ç¬¬1158492å·æ现æžã«èšèŒãããŠãããåŸ
è ã®è±åœç¹èš±ã«ã¯ããã®ç¡é žãšã¹ãã«ä¿è·åºãçš
ããæè¡ã¯17âç¡é žãšã¹ãã«ã®çæã«ãããå šè¬
çã«ã¯å¿çšãåŸããç¹ã«21âãã¹ãªãã·ã¹ããã€
ãã«ã¯å¿çšãåŸãªããšé瀺ãããŠããã 11âããããã·ã«åºåã³ä»»æã®ä»ã®éææ§åºã
ä¿è·ãããåŸã«ã17âã¢ã·ã«åãè¡ãªãããã®17
âã¢ã·ã«åã«çšããã¹ã第ïŒã®æ¹æ³ã¯è±åœç¹èš±ç¬¬
737291å·æ现æžã«äžããããæ¹æ³ã§ãããïœâã
ã«ãšã³ã¹ã«ãã³é žã®åŠãåŒ·é žè§Šåªã®ååšäžã«äœçŽ
ã«ã«ãã³é žç¡æ°Žç©ãçšãããã®ã§ããããã®æ¹æ³
ã¯æŽã«ãšãããè±åœç¹èš±ç¬¬1158492å·åã³ç¬¬
1227992å·æ现æžã§çšããããŠãããããããªã
ãäžéã«ãããã®æ¹æ³ã¯ãé·æé100âãè¶ãã
枩床ã§17αâããããã·â20âã±ãã¹ããã€ãã
ã«ã«ãã³é žç¡æ°Žç©ãšå ±ã«å ç±ããããšã«ããã¢ã·
ã«åãè¡ãããšããå¿ èŠã§ãããšããæ¬ ç¹ãåã
ãããã®åå¿ã¯çžåœãªå解ãçèµ·ããç¹ã«å€æ°ã®
æäœæ§å®èœåºãå«æããã¹ããã€ãã§ã¯å解ãç
èµ·ããã åŸã€ãŠãã®æ¹æ³ã«åã€ãŠä»£ã€ãŠãç¬åœç¹èš±ç¬¬
1013284å·æ现æžã«èšèŒãããåŠãäžã€ãšããã
è±åœç¹èš±ç¬¬1391712å·åã³ç¬¬1158492å·æ现æžã§äœ¿
çšãããåŠãããªãã«ãªãç¡æ°Žé ¢é žãšå ±ã«èèªæ
åã¯èç°æã«ã«ãã³é žãçšããæ¹æ³ãæããã
ããããããªãããã®æ¹æ³ã§ãå ã®ç¬¬ïŒã®æ¹æ³ã«
æ¯ã¹ãŠããããªæ¹è¯ãäžããã«éããªããäœæ ãª
ãã°ããã®å Žåã«ãåå¿æ··åç©ã80ã90âã«å ç±
ããã®ããªãå¿ èŠã§ããããã§ããã 次ã«è±åœç¹èš±ç¬¬1097165å·æ现æžã¯ãïŒãïŒå
ã®ççŽ ååãå«ãèèªæåã¯èç°æã«ã«ãã³é žäžŠ
ã³ã«ããªãã«ãªãç¡æ°Žé ¢é žåã³ïœâãã«ãšã³ã¹ã«
ãã³é žã®åŠãåŒ·é žè§ŠåªãçšããŠææã®ã¢ã·ã«åã
è¡ãªãç¹ã§åºæ¬çã«ã¯åèšã®ïŒã€ã®æ¹æ³ã®çµåã
ã§ããæ¹æ³ãèšèŒããŠããããã®æ··åç©ã¯å®€æž©ã§
äœçšãããããã€ãŠãã®åœæã®åŸæ¥æè¡ãããå©
çšäŸ¡å€ãé«ããšãããŠãããããããªããäžéã«
ãããã®æ¹æ³ã§ã¯ãå¿ èŠãªåå¿å€ã®éã¯ããããŠ
å€ããäŸãã°åæã¹ããã€ãã®ïŒïœåœã10mlã®ã«
ã«ãã³é žãšïŒmlã®ããªãã«ãªãç¡æ°Žé ¢é žãšãå¿ èŠ
ã§ãããããã¯è©²æ¹æ³ãé«äŸ¡ãšããã®ã¿ãªããæ
æã®çæç©ãçŽç²ãªç¶æ ã§åé¢ããã®ãå°é£ãšã
ãªããåŸã€ãŠåå¿æ··åç©ãã¹ããŒã èžçããŠå€§é
å°ã®é žãé€å»ããªããã°ãªããã次ãã§éåžžã«ã©
ã ã»ã¯ãããã°ã©ãã€ãŒãçšããŠçæç©ãåé¢ã
ããã®ã§ããã åèšã®17âã¢ã·ã«åå·¥çšåŸã«ã¯ã次ãã§11âä¿
è·åºãéžæçã«è±é¢ããããšãå¿ èŠã§ãããããª
ãã«ãªãã¢ã»ããŒãä¿è·åºã¯ãè±åœç¹èš±ç¬¬
1391712å·åã³ç±³åœç¹èš±ç¬¬4024131å·æ现æžã«èšèŒ
ãããåŠãã·ãªã«ã§ã®å 溶åªå解ã«ããïŒç±³åœç¹
蚱第4024131å·æ现æžã«èšèŒãããåŠãéçé žã
ããªãŠã å æ°Žå解ã«ããïŒè±åœç¹èš±ç¬¬1097164å·
æ现æžã«èšèŒãããåŠã2.3ã7.3ã®pKaãæãã
é žã®ã¢ã«ã«ãªéå±åã¯ã¢ã«ã«ãªåé¡éå±å¡©ã§ã®å
溶åªå解ã«ããïŒåã¯è±åœç¹èš±ç¬¬2079754å·æ现
æžã«èšèŒãããåŠã觊åªéã®ãããªãŠã ã¡ããã·
ãã«ããè±é¢ãåŸããããã©ããããã©ã³â
ïŒ2â²ã€ã«ïŒãšãŒãã«åã³ããªã¡ãã«ã·ãªã«ãšãŒã
ã«ä¿è·åºã¯ãé žå æ°Žå解ã«ããè±é¢ã§ããã«å¯Ÿ
ãã11âç¡é žãšã¹ãã«ä¿è·åºã¯é ¢é žäžã§äºéãå¿
èŠãšããã ããªãã«ãªãã¢ã»ããŒãä¿è·åºã®è±é¢ã«é¢ã
ãŠãã·ãªã«åã¯2.3ã7.3ã®pKaå€ãæããé žã®ã¢
ã«ã«ãªéå±åã¯ã¢ã«ã«ãªåé¡éå±å¡©ãçšããããš
ã¯ç¹å¥æå©ãªæ¹æ³ã§ã¯ãªããããã¯åå¿ã®äžåäž
æ§ã«ãããã®ã§ãããçæç©äžã«æªåå¿ã®åæã
æ®çããåŸåãããããããŠãã©ããã®ããçµæ
ãäžããããã®åé¡ã¯éçé žãããªãŠã ãçšãã
æã§ãçãããäœæ ãªãã°ãçæç©ãšåæã¹ãã
ã€ããšãã¡ã¿ããŒã«åªè³ªäžã§å ±æ¶ããããšãå€ã
ããã§ããã觊åªéã®ãããªãŠã ã¡ããã·ããçš
ããã®ãæè¯ã®å©çšãåŸãåŸæ¥æ³ã§ãããããã
ã§ã¯åå¿ã®ãã©ã¡ãŒã¿ãŒãå³ããå¶åŸ¡ããªããã°
ãªããªãããããªããšãšã¹ãã«å®èœåºãç¹ã«21äœ
ã®ãšã¹ãã«å®èœåºãé€å»ãããŠçµãããã§ããã
ãã®äºå®ã¯è±åœç¹èš±ç¬¬1196683å·æ现æžã§èšŒæã
ããããã§ã¯ãããªãŠã ã¡ããã·ãã¯11âã¯ãã
ãžãã«ãªãã¢ã»ãã«åºã®ã¿ãªãã21âã¢ã»ããŒã
åºãåæ§ã«è±é¢ããããšé瀺ãããŠããããã®ä»
ã®ä¿è·åºã¯èªå°äœã®è£œé ã«ãããŠåé¡ãçããã
ããã€ãŠå®æœå¯èœãªæ¹æ³ã«ãããã®åºã䜿çšãã
å¯èœæ§ã¯æé€ãããã æ¬çºæã®ååç©ã®è£œé ã®ããã«äœ¿çšãããŠãã
第ïŒã®äžè¬çãªåŸæ¥æ³ã¯ç°åŒ17αïŒ21âãªã«ããž
ãšã¹ãã«ãçµç±ãããã®ã§ããããã®åŸæ¥æ³ã¯æ
åãã«ã®ãŒç¹èš±ç¬¬618831å·åã³ç¬¬619180å·æ现æž
ã«èšèŒãããåŸã«è±åœç¹èš±ç¬¬1043347å·åã³ç¬¬
1047518å·ã«èšèŒãããããã®æ¹æ³ã¯åæã17αïŒ
21âãžããããã·â20âãªã³åã®äžéšæ§é ãæã
ãå Žåã«ã®ã¿é©çšãåŸãã«éããªããã11âãã
ããã·ã«åºãä¿è·ããå¿ èŠãªãã«è¡ãªãåŸããã
ãããªãããäžéäœã®ç°åŒãªã«ããžãšã¹ãã«ã®é ž
å æ°Žå解ãååã«éžæçã§ã¯ãªããšããé£ç¹ãã
ãããããåå¿æ¡ä»¶ã«ããããŠéæã§ããã17â
ã¢ããšã¹ãã«ã«å ããŠ21âã¢ããšã¹ãã«åã³17ïŒ
21âãžããããã·ååç©ãäžããããã®åŸæ¥æ³ã
çšããéã®å¥ã®å¶çŽã¯åæã®ããªã¢ã«ãã«ãªã«ã
ãšã¹ãã«ã調補ããéã«çããæ¯éã§ãããïŒå
ããå€ãççŽ ååãå«æããé žããèªå°ãããã
ãªã¢ã«ãã«ãªã«ããšã¹ãã«ã¯ããããŠååŸå°é£ã§
ããã æ¬çºæã¯ã17âã¢ã·ã«åå·¥çšã¯åŸæ¥æ³ã«ããã
ãããäžå±€ç°¡åã§ãåå¿å€ã«é¢ããŠããçµæžçã§
ãããã€ããè¯å¥œãªåçåã³çŽåºŠã§éæã§ãããš
ããç¥èŠã«åºã¥ããã®ã§ããããããã11âããª
ãã«ãªãã¢ã»ããŒãä¿è·åºã䜿çšããå Žåããã®
è±é¢ã¯ã¢ãã³ãã¢ã³ã¢ãã¢åã¯ããã©ãžã³ã®ãã
ãããšã®åå¿ã«ããã»ãšãã©ååŠéè«çãªåçã§
æãç°¡åã«éæã§ããã æ¬çºæã®æ¹æ³ã«ããã°ãåºçºç©è³ªã¯åœæ¥è ã«æ¢
ç¥ã®æšæºçæ¹æ³ã«ãã調補ã§ãã次åŒïŒ ïŒåŒäžããR1ãR2ãR3åã³R5ã¯åèšã®æ矩ã
æããïŒã®ååç©ã§ãããR2ãããªããã¢ã»ã
ãã·åºã奜ãŸããã¯ããªãã«ãªãã¢ã»ããã·åºã§
ããå Žåããã®ä¿è·åºãããªãã«ãªãã¢ã»ãã«
åºãã¯æšæºæ³ã«ããå°å ¥ããããããšãã°11âã
ãããã·ã¹ããã€ããããªãžã³ïŒããã©ãããã
ã©ã³ã®ããšãåå¿ã«äžæŽ»æ§ãªæº¶å€ã§åžéãããŠã
ãŠãããïŒã«æº¶è§£ããããªãã«ãªãç¡æ°Žé ¢é žãæ·»
å ãã次ãã§æ £çšæ段ã«ãããäŸãã°æ°Žäžã«æ²æŸ±
ãããæ¹æ³ã«ãããæèŠã®11âããªãã«ãªãã¢ã»
ããã·ã¹ããã€ãçæç©ãåé¢ãããšããæ¹æ³ã
䜿çšãåŸãã åæã¹ããã€ãã®17äœâã¢ã·ã«åã¯ã«ã«ãã³é ž
ã®ç¡æ°Žç©ãšäžå¯Ÿã®åŒ·é žãšãçšããŠè¡ãªãããã䜿
çšãããã¹ãã«ã«ãã³é žç¡æ°Žç©ã®éã¯åæã¹ãã
ã€ãïŒã¢ã«åœã1.5ã¢ã«ä»¥äžã§ãããããšãã°ã
ãã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ããŒã 21
âã¢ã»ããŒãïŒå®æœäŸ9aïŒã«17âãã¬ã¬ãŒãåº
ãå°å ¥ããå Žåãç¡æ°Žãã¬ãªã¢ã³é žã®å¥œãŸãã䜿
çšéã¯0.76mlïŒïœã§ããããã®åå¿æ¡ä»¶ã¯ãåæ
ïŒïœåœã10mlã®ãã¬ãªã¢ã³é žã䜿çšããŠããè±åœ
ç¹èš±ç¬¬1097165å·æ现æžã®å®æœäŸïŒã«ç€ºãããæ¡
件ãšæ¯èŒããŠããããŠæå©ã§ããã䜿çšãããäž
察ã®åŒ·é žã®ãã¡ã®äžæ¹ã¯ããªããé ¢é žã§ããã¹ã
ã§ãããç¹ã«ããªãã«ãªãé ¢é žåã¯ããªã¯ããé ¢
é žã奜ãŸãããããªããé ¢é žã¯åæã¹ããã€ãã«
察ããŠ1.5ã¢ã«ä»¥äžã®ã¢ã«éã§ååšãã¹ãã§ããã ãŸããã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ããŒ
ã 21âã¢ã»ããŒãã«17âãã¬ã¬ãŒãåºãå°å ¥ã
ãå Žåã«ã¯ãããªãã«ãªãé ¢é žã®å¥œãŸãã䜿çšé
ã¯0.58mlïŒïœã§ããããããšå¯Ÿæ¯ããŠãåèšè±åœ
ç¹èš±ã®å®æœäŸïŒã§ã¯åæïŒïœåœãïŒmlã®ç¡æ°Žããª
ãã«ãªãé ¢é žãçšããŠããã äžå¯Ÿã®åŒ·é žã®ãã¡ã®ããäžæ¹ã®é žã¯è§Šåªéã§å
åšããããã¯ïœâãã«ãšã³ã¹ã«ãã³é žãã¡ã¿ã³ã¹
ã«ãã³é žããã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é žåã³å¡©
é žããéžã°ããã çš®ã ã®åå¿å€ã®æ··åé åºã¯éèŠã§ã¯ãªãããå®
éã®æ··ååŠçäžã¯åå¿åšãå·åŽããã®ã奜ãŸã
ããããªããé ¢é žãçŽïŒâã«å·åŽããããã§ã«ã«
ãã³é žç¡æ°Žç©ãå ããç¶ããŠç¬¬äºã®åŒ·é žãå ãã
æåŸã«åå¿ãããã¹ãåæã¹ããã€ããå ããã®
ãæ®éã§ããã æ¬çºæã®æãé©ãã¹ãç¹åŸŽã®äžã€ã¯çéã®åå¿
å€ã䜿çšããå Žåã«ãæ¬çºæã®æ°èŠæ¹æ³ã¯åŸæ¥æ
è¡ã®æ¹æ³ãããèããé«ãåå¿é床ãäžããç¹ã§
ããããã®ç¹ãæ¬çºæã®å©ç¹ã®äžéšãæ§æããã
ã®ã§ããã 次衚ã«ãã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ã
ãŒã 21âã¢ã»ããŒããžã®17âãã¬ã¬ãŒãåºã®å°
å ¥åå¿ã«ã€ããŠåŸèšå®æœäŸïŒã«ç€ºããæ¬çºææ¹æ³
åã³ä»£è¡šçãªåŸæ¥æè¡ã«åŸãè©ŠéšäŸã®åå¿æ¡ä»¶ã
察æ¯ããŠç€ºãã
é æ³ã«é¢ããã ã³ã«ãã³ã¹ããã€ããæçç掻æ§ãæããããš
ã«ã€ããŠã¯å€ãããç¥ãããŠãããã³ã«ãã³ã¹ã
ãã€ãã«ãšã¹ãã«å®èœåºãå°å ¥ããããšã«ããã
ç¹ã«17äœã®ã¿ã«åã¯17äœãš21äœã«ãšã¹ãã«å®èœåº
ãå°å ¥ããããšã«ãããå±æç掻æ§ãããªãå¢é²
ãããããšãåæ§ã«ç¥ãããŠããããããã®ãšã¹
ãã«åããã³ã«ãã³ã¹ããã€ãã¯ãŸãå šèº«ç³»æŽ»æ§
ãæå°ã§ãããšããå©ç¹ããæäŸããã æ¬çºæã¯åŸèšã®åŒïŒïŒã®ååç©ã補é ããæ°
èŠã§æå¹ãªã«ãŒããæäŸãããã®ã§ããã ããæ æ¬çºæã«ãããšã次åŒïŒ ïŒåŒäžïŒžãR1ãR2åã³R3ã¯åŸèšã®æ矩ãæãïŒ
R5ã¯ããããã·ã«åºåã¯R6ã§ãããR6ã¯åŸèšã®
æ矩ãæããïŒã®ååç©ã®17äœã®ã¿åã¯åèšåŒ
ïŒïŒäžã®R5ãããããã·ã«åºã§ããå Žåã«ã¯17
äœåã³21äœããšã¹ãã«åããããšãããªãããã®
éãšã¹ãã«åã¯17äœã«åã¯17äœãš21äœã«å°å ¥ãã¹
ãåºãå«ãã«ã«ãã³é žã®ç¡æ°Žç©ãããªããé ¢é žãš
ïœâãã«ãšã³ã¹ã«ãã³é žãã¡ã¿ã³ã¹ã«ãã³é žãã
ã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é žåã³å¡©é žããéžãã
äžçš®ã®é žãšãããªãäžå¯Ÿã®åŒ·é žãšãšãã«çšããŠè¡
ãªãããšãç¹åŸŽãšãã次åŒïŒ ïœåŒäžâŠã¯äºéçµåãååšãåŸãããšãè¡šããïŒ
ã¯æ°ŽçŽ ãããçŽ åã¯å¡©çŽ ã§ããïŒR1ã¯æ°ŽçŽ ã
ããçŽ ãå¡©çŽ åã¯ã¡ãã«åºã§ãããã€R1ã¯Î±äœ
åã¯Î²äœã«ååšãåŸããã®ã§ããïŒR2ã¯ããã²
ã³ããªããœåã¯ããªããã¢ã»ããã·ïŒãããããª
ããã¢ã»ãã«åºã¯ããããã·ã«ä¿è·åºã§ããïŒåº
ã§ããïŒR3ã¯æ°ŽçŽ ãαâã¡ãã«åã¯Î²âã¡ãã«
åºã§ããïŒR4ã¯åŒRCOïŒãããã¯(i)ïŒã16åã®
ççŽ ååãæããçŽéãåå²éåã¯ç°åŒã¢ã«ãã«
åºã(ii)ïŒãïŒåã®ççŽ ååãæããã¢ã©ã«ãã«åº
åã¯(iii)ããšãã«åºã§ããïŒã®ã¢ã·ã«åºã§ããïŒ
R6ã¯æ°ŽçŽ ãïŒååã¯ïŒåã®ããã²ã³çœ®æåºåã¯
OR7ããããR7ã¯åŒRâ²COïŒåŒäžRâ²ã¯ïŒ²ãšåäžã§ã
ç°ãªã€ãŠãããã(i)ïŒã16åã®ççŽ ååãæãã
çŽéãåå²éåã¯ç°åŒã¢ã«ãã«åºã(ii)ïŒãïŒåã®
ççŽ ååãæããã¢ã©ã«ãã«åºåã¯(iii)ããšãã«åº
ã§ããïŒã®ã¢ã·ã«åºã§ãããã§ããïœã®ã³ã«ãã³
ã¹ããã€ããšã¹ãã«ã®è£œé æ³ãæäŸãããã ããã«æ¬çºæã®å¥ã®äžèŠæšã¯äžèšæ¬çºæã«åŸã
æ¹æ³ã«ãããåŒïŒïŒã«ãããŠR2ãããªããã¢
ã»ããã·åºã§ããååç©ãããªãã¡æ¬¡åŒïŒ ïŒåŒäžããR1ãR3åã³R5ã¯åèšã®æ矩ãæã
ãïŒããåºçºããŠåŒïŒïŒã«ãããŠR2ãããªã
ãã¢ã»ããã·åºã§ããååç©ãããªãã¡æ¬¡åŒïŒ ïŒåŒäžãâŠããR1ãR3ãR4åã³R6ã¯åèšã®æ
矩ãæããïŒã®ååç©ã補é ããã€ãã§åŒïŒâ²ïŒ
ã®ååç©ããäœçŽã¢ã«ã³ãŒã«ã®ååšäžã«ãçªçŽ å
åãè³éŠæç°ã®äžéšãæ§æããææ©ã¢ãã³ä»¥å€ã®
ææ©ã¢ãã³ãç¡æ°Žæº¶å€äžã«æº¶è§£ãããç¡æ°Žã¢ã³ã¢
ãã¢ã¬ã¹ãæ°Žé žåã¢ã³ã¢ããŠã åã¯ããã©ãžã³ãš
åå¿ãããŠ11âããªããã¢ã»ãã«ä¿è·åºãè±é¢ã
ãããããšãããªã次åŒïŒ ïŒåŒäžãâŠããR1ãR3ãR4åã³R6ã¯åèšã®æ
矩ãæããïŒã®ã³ã«ãã³ã¹ããã€ããšã¹ãã«ã®è£œ
é æ³ã«ããã ãããã€ãŠæ¬çºæã¯ãäžã€ã®äžè¬çãªæ¹æ³ã«ã
ã€ãŠãã¿ã¡ã¿ãŸã³ããããµã¡ã¿ãŸã³ããã¯ãã¡ã¿
ãŸã³ãã¯ããã¿ãŸãŒã«ããã¬ãããœãã³ããã€ã
ãã³ã«ããŸã³ãšã¹ãã«é¡ã®è£œé æ³ãåºãå å«ãã
ãã®ã§ããã ãããååç©ã®è£œé ã«å©çšãåŸãæ¢ç¥ã®åŸæ¥æ³
ã¯ã€ãã®äžçŸ€ã«åé¡ãåŸãã 第ïŒã®åŸæ¥æ³ã¯ãäŸãã°11äœãä¿è·åºã§äœãä¿
è·ããããšãªã17âãšã¹ãã«å®èœåºãçŽæ¥åæã¹
ããã€ãã«å°å ¥ãããã®ã§ããããã®åŸæ¥æ³ã¯J.
Amer.Chem.Soc.74ã5394ã96ãïŒ1952ïŒåã³è±
åœç¹èš±ç¬¬737291å·åã³ç¬¬1070751å·æ现æžåã³ç±³
åœç¹èš±ç¬¬3721687å·æ现æžã«äŸç€ºãããŠãããã
ã®ã¢ã·ã«åã¯ïœâãã«ãšã³ã¹ã«ãã³é žã®åŠãåŒ·é ž
觊åªã®ååšäžã«äœçŽèèªæã«ã«ãã³é žã®ç¡æ°Žç©ã
çšããŠè¡ããããããããã·ã«å®èœåºã®ãšã¹ãã«
åã®é äœã¯ç¬¬ïŒçŽããããã·ã«æ¬¡ãã§ç¬¬ïŒçŽãã
ããã·ã«ãæåŸã«ç¬¬ïŒçŽããããã·ã«åºã§ããã®
ã¯åšç¥ã§ãããå³ã¡ã11ïŒ17ïŒ21âããªãããã
ã·ã¹ããã€ãã®å Žåã«ã¯ãçŽæ¥ãšã¹ãã«åãè¡ã
ãšå¹Ÿåç°ãªã€ãçŸåçã§ã®21âã¢ããšã¹ãã«ãš
11ïŒ21âãžãšã¹ãã«ãš11ïŒ17ïŒ21âããªãšã¹ãã«
ãšããæãæ··åç©ãåŸããããåŸã€ãŠãã®æ··åç©
ããæèŠã®çæç©ãåé¢ããããšã¯ãé©åœãªæ¹æ³
ãèŠåºããããšããŠãçµæžçã«ã¯å®æœãåŸãªãã
æŽã«ã¯11ïŒ17ïŒ21âããªãšã¹ãã«äžã®äžæŽ»æ§å11
âãšã¹ãã«ãéžæçã«é€å»ããæ¹æ³ã¯çŸåšç¥ãã
ãŠããªãã 第ïŒã®åŸæ¥æ³ã¯ïŒã€ä»¥äžã®ãšã¹ãã«å®èœåºã®å°
å ¥åã«åæã¹ããã€ãã®å®èœåºãä¿è·ããå·¥çšã
䌎ãªãã11âããããã·ã«å®èœåºçšã®éåžžã®ä¿è·
åºã¯ããªããã¢ã»ããŒããããªã¡ãã«ã·ãªã«ãšãŒ
ãã«ãããã©ããããã©ã³âïŒ2â²ã€ã«ïŒãšãŒãã«
åã³ç¡é žãšã¹ãã«åºã§ããããããã®ä¿è·åºã®ã
ã¡ããªããã¢ã»ããŒãã¯ç±³åœç¹èš±ç¬¬2800489å·æ
现æžã«æåã«èšèŒãããŠãããè±åœç¹èš±ç¬¬
1097165å·åã³ç±³åœç¹èš±ç¬¬4024131å·æ现æžã§çšã
ãããŠãããããªã¡ãã«ã·ãªã«ãšãŒãã«ä¿è·åºã¯
è±åœç¹èš±ç¬¬1227992å·æ现æžã§çšããŠããããã®
調補æ³ã¯æœåºæè¡ïŒåé¿ããã®ã奜ãŸããïŒã䌎
ãªã€ãŠãããããã«ãæããåŸãããåçã¯æ Œå¥
è¯å¥œã§ã¯ãªããããã©ããããã©ã³âïŒ2â²ã€ã«ïŒ
ãšãŒãã«ä¿è·åºã¯ç±³åœç¹èš±ç¬¬4024131å·æ现æžã«
èšèŒãããŠãããåæ§ã«ãã®èª¿è£œæ³ã¯æœåºæè¡ã
䌎ãªããç¡é žãšã¹ãã«ä¿è·åºã¯å ãè±åœç¹èš±ç¬¬
1082573å·æ现æžã«èšèŒãããŠãã次ãã§åã³è±
åœç¹èš±ç¬¬1158492å·æ现æžã«èšèŒãããŠãããåŸ
è ã®è±åœç¹èš±ã«ã¯ããã®ç¡é žãšã¹ãã«ä¿è·åºãçš
ããæè¡ã¯17âç¡é žãšã¹ãã«ã®çæã«ãããå šè¬
çã«ã¯å¿çšãåŸããç¹ã«21âãã¹ãªãã·ã¹ããã€
ãã«ã¯å¿çšãåŸãªããšé瀺ãããŠããã 11âããããã·ã«åºåã³ä»»æã®ä»ã®éææ§åºã
ä¿è·ãããåŸã«ã17âã¢ã·ã«åãè¡ãªãããã®17
âã¢ã·ã«åã«çšããã¹ã第ïŒã®æ¹æ³ã¯è±åœç¹èš±ç¬¬
737291å·æ现æžã«äžããããæ¹æ³ã§ãããïœâã
ã«ãšã³ã¹ã«ãã³é žã®åŠãåŒ·é žè§Šåªã®ååšäžã«äœçŽ
ã«ã«ãã³é žç¡æ°Žç©ãçšãããã®ã§ããããã®æ¹æ³
ã¯æŽã«ãšãããè±åœç¹èš±ç¬¬1158492å·åã³ç¬¬
1227992å·æ现æžã§çšããããŠãããããããªã
ãäžéã«ãããã®æ¹æ³ã¯ãé·æé100âãè¶ãã
枩床ã§17αâããããã·â20âã±ãã¹ããã€ãã
ã«ã«ãã³é žç¡æ°Žç©ãšå ±ã«å ç±ããããšã«ããã¢ã·
ã«åãè¡ãããšããå¿ èŠã§ãããšããæ¬ ç¹ãåã
ãããã®åå¿ã¯çžåœãªå解ãçèµ·ããç¹ã«å€æ°ã®
æäœæ§å®èœåºãå«æããã¹ããã€ãã§ã¯å解ãç
èµ·ããã åŸã€ãŠãã®æ¹æ³ã«åã€ãŠä»£ã€ãŠãç¬åœç¹èš±ç¬¬
1013284å·æ现æžã«èšèŒãããåŠãäžã€ãšããã
è±åœç¹èš±ç¬¬1391712å·åã³ç¬¬1158492å·æ现æžã§äœ¿
çšãããåŠãããªãã«ãªãç¡æ°Žé ¢é žãšå ±ã«èèªæ
åã¯èç°æã«ã«ãã³é žãçšããæ¹æ³ãæããã
ããããããªãããã®æ¹æ³ã§ãå ã®ç¬¬ïŒã®æ¹æ³ã«
æ¯ã¹ãŠããããªæ¹è¯ãäžããã«éããªããäœæ ãª
ãã°ããã®å Žåã«ãåå¿æ··åç©ã80ã90âã«å ç±
ããã®ããªãå¿ èŠã§ããããã§ããã 次ã«è±åœç¹èš±ç¬¬1097165å·æ现æžã¯ãïŒãïŒå
ã®ççŽ ååãå«ãèèªæåã¯èç°æã«ã«ãã³é žäžŠ
ã³ã«ããªãã«ãªãç¡æ°Žé ¢é žåã³ïœâãã«ãšã³ã¹ã«
ãã³é žã®åŠãåŒ·é žè§ŠåªãçšããŠææã®ã¢ã·ã«åã
è¡ãªãç¹ã§åºæ¬çã«ã¯åèšã®ïŒã€ã®æ¹æ³ã®çµåã
ã§ããæ¹æ³ãèšèŒããŠããããã®æ··åç©ã¯å®€æž©ã§
äœçšãããããã€ãŠãã®åœæã®åŸæ¥æè¡ãããå©
çšäŸ¡å€ãé«ããšãããŠãããããããªããäžéã«
ãããã®æ¹æ³ã§ã¯ãå¿ èŠãªåå¿å€ã®éã¯ããããŠ
å€ããäŸãã°åæã¹ããã€ãã®ïŒïœåœã10mlã®ã«
ã«ãã³é žãšïŒmlã®ããªãã«ãªãç¡æ°Žé ¢é žãšãå¿ èŠ
ã§ãããããã¯è©²æ¹æ³ãé«äŸ¡ãšããã®ã¿ãªããæ
æã®çæç©ãçŽç²ãªç¶æ ã§åé¢ããã®ãå°é£ãšã
ãªããåŸã€ãŠåå¿æ··åç©ãã¹ããŒã èžçããŠå€§é
å°ã®é žãé€å»ããªããã°ãªããã次ãã§éåžžã«ã©
ã ã»ã¯ãããã°ã©ãã€ãŒãçšããŠçæç©ãåé¢ã
ããã®ã§ããã åèšã®17âã¢ã·ã«åå·¥çšåŸã«ã¯ã次ãã§11âä¿
è·åºãéžæçã«è±é¢ããããšãå¿ èŠã§ãããããª
ãã«ãªãã¢ã»ããŒãä¿è·åºã¯ãè±åœç¹èš±ç¬¬
1391712å·åã³ç±³åœç¹èš±ç¬¬4024131å·æ现æžã«èšèŒ
ãããåŠãã·ãªã«ã§ã®å 溶åªå解ã«ããïŒç±³åœç¹
蚱第4024131å·æ现æžã«èšèŒãããåŠãéçé žã
ããªãŠã å æ°Žå解ã«ããïŒè±åœç¹èš±ç¬¬1097164å·
æ现æžã«èšèŒãããåŠã2.3ã7.3ã®pKaãæãã
é žã®ã¢ã«ã«ãªéå±åã¯ã¢ã«ã«ãªåé¡éå±å¡©ã§ã®å
溶åªå解ã«ããïŒåã¯è±åœç¹èš±ç¬¬2079754å·æ现
æžã«èšèŒãããåŠã觊åªéã®ãããªãŠã ã¡ããã·
ãã«ããè±é¢ãåŸããããã©ããããã©ã³â
ïŒ2â²ã€ã«ïŒãšãŒãã«åã³ããªã¡ãã«ã·ãªã«ãšãŒã
ã«ä¿è·åºã¯ãé žå æ°Žå解ã«ããè±é¢ã§ããã«å¯Ÿ
ãã11âç¡é žãšã¹ãã«ä¿è·åºã¯é ¢é žäžã§äºéãå¿
èŠãšããã ããªãã«ãªãã¢ã»ããŒãä¿è·åºã®è±é¢ã«é¢ã
ãŠãã·ãªã«åã¯2.3ã7.3ã®pKaå€ãæããé žã®ã¢
ã«ã«ãªéå±åã¯ã¢ã«ã«ãªåé¡éå±å¡©ãçšããããš
ã¯ç¹å¥æå©ãªæ¹æ³ã§ã¯ãªããããã¯åå¿ã®äžåäž
æ§ã«ãããã®ã§ãããçæç©äžã«æªåå¿ã®åæã
æ®çããåŸåãããããããŠãã©ããã®ããçµæ
ãäžããããã®åé¡ã¯éçé žãããªãŠã ãçšãã
æã§ãçãããäœæ ãªãã°ãçæç©ãšåæã¹ãã
ã€ããšãã¡ã¿ããŒã«åªè³ªäžã§å ±æ¶ããããšãå€ã
ããã§ããã觊åªéã®ãããªãŠã ã¡ããã·ããçš
ããã®ãæè¯ã®å©çšãåŸãåŸæ¥æ³ã§ãããããã
ã§ã¯åå¿ã®ãã©ã¡ãŒã¿ãŒãå³ããå¶åŸ¡ããªããã°
ãªããªãããããªããšãšã¹ãã«å®èœåºãç¹ã«21äœ
ã®ãšã¹ãã«å®èœåºãé€å»ãããŠçµãããã§ããã
ãã®äºå®ã¯è±åœç¹èš±ç¬¬1196683å·æ现æžã§èšŒæã
ããããã§ã¯ãããªãŠã ã¡ããã·ãã¯11âã¯ãã
ãžãã«ãªãã¢ã»ãã«åºã®ã¿ãªãã21âã¢ã»ããŒã
åºãåæ§ã«è±é¢ããããšé瀺ãããŠããããã®ä»
ã®ä¿è·åºã¯èªå°äœã®è£œé ã«ãããŠåé¡ãçããã
ããã€ãŠå®æœå¯èœãªæ¹æ³ã«ãããã®åºã䜿çšãã
å¯èœæ§ã¯æé€ãããã æ¬çºæã®ååç©ã®è£œé ã®ããã«äœ¿çšãããŠãã
第ïŒã®äžè¬çãªåŸæ¥æ³ã¯ç°åŒ17αïŒ21âãªã«ããž
ãšã¹ãã«ãçµç±ãããã®ã§ããããã®åŸæ¥æ³ã¯æ
åãã«ã®ãŒç¹èš±ç¬¬618831å·åã³ç¬¬619180å·æ现æž
ã«èšèŒãããåŸã«è±åœç¹èš±ç¬¬1043347å·åã³ç¬¬
1047518å·ã«èšèŒãããããã®æ¹æ³ã¯åæã17αïŒ
21âãžããããã·â20âãªã³åã®äžéšæ§é ãæã
ãå Žåã«ã®ã¿é©çšãåŸãã«éããªããã11âãã
ããã·ã«åºãä¿è·ããå¿ èŠãªãã«è¡ãªãåŸããã
ãããªãããäžéäœã®ç°åŒãªã«ããžãšã¹ãã«ã®é ž
å æ°Žå解ãååã«éžæçã§ã¯ãªããšããé£ç¹ãã
ãããããåå¿æ¡ä»¶ã«ããããŠéæã§ããã17â
ã¢ããšã¹ãã«ã«å ããŠ21âã¢ããšã¹ãã«åã³17ïŒ
21âãžããããã·ååç©ãäžããããã®åŸæ¥æ³ã
çšããéã®å¥ã®å¶çŽã¯åæã®ããªã¢ã«ãã«ãªã«ã
ãšã¹ãã«ã調補ããéã«çããæ¯éã§ãããïŒå
ããå€ãççŽ ååãå«æããé žããèªå°ãããã
ãªã¢ã«ãã«ãªã«ããšã¹ãã«ã¯ããããŠååŸå°é£ã§
ããã æ¬çºæã¯ã17âã¢ã·ã«åå·¥çšã¯åŸæ¥æ³ã«ããã
ãããäžå±€ç°¡åã§ãåå¿å€ã«é¢ããŠããçµæžçã§
ãããã€ããè¯å¥œãªåçåã³çŽåºŠã§éæã§ãããš
ããç¥èŠã«åºã¥ããã®ã§ããããããã11âããª
ãã«ãªãã¢ã»ããŒãä¿è·åºã䜿çšããå Žåããã®
è±é¢ã¯ã¢ãã³ãã¢ã³ã¢ãã¢åã¯ããã©ãžã³ã®ãã
ãããšã®åå¿ã«ããã»ãšãã©ååŠéè«çãªåçã§
æãç°¡åã«éæã§ããã æ¬çºæã®æ¹æ³ã«ããã°ãåºçºç©è³ªã¯åœæ¥è ã«æ¢
ç¥ã®æšæºçæ¹æ³ã«ãã調補ã§ãã次åŒïŒ ïŒåŒäžããR1ãR2ãR3åã³R5ã¯åèšã®æ矩ã
æããïŒã®ååç©ã§ãããR2ãããªããã¢ã»ã
ãã·åºã奜ãŸããã¯ããªãã«ãªãã¢ã»ããã·åºã§
ããå Žåããã®ä¿è·åºãããªãã«ãªãã¢ã»ãã«
åºãã¯æšæºæ³ã«ããå°å ¥ããããããšãã°11âã
ãããã·ã¹ããã€ããããªãžã³ïŒããã©ãããã
ã©ã³ã®ããšãåå¿ã«äžæŽ»æ§ãªæº¶å€ã§åžéãããŠã
ãŠãããïŒã«æº¶è§£ããããªãã«ãªãç¡æ°Žé ¢é žãæ·»
å ãã次ãã§æ £çšæ段ã«ãããäŸãã°æ°Žäžã«æ²æŸ±
ãããæ¹æ³ã«ãããæèŠã®11âããªãã«ãªãã¢ã»
ããã·ã¹ããã€ãçæç©ãåé¢ãããšããæ¹æ³ã
䜿çšãåŸãã åæã¹ããã€ãã®17äœâã¢ã·ã«åã¯ã«ã«ãã³é ž
ã®ç¡æ°Žç©ãšäžå¯Ÿã®åŒ·é žãšãçšããŠè¡ãªãããã䜿
çšãããã¹ãã«ã«ãã³é žç¡æ°Žç©ã®éã¯åæã¹ãã
ã€ãïŒã¢ã«åœã1.5ã¢ã«ä»¥äžã§ãããããšãã°ã
ãã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ããŒã 21
âã¢ã»ããŒãïŒå®æœäŸ9aïŒã«17âãã¬ã¬ãŒãåº
ãå°å ¥ããå Žåãç¡æ°Žãã¬ãªã¢ã³é žã®å¥œãŸãã䜿
çšéã¯0.76mlïŒïœã§ããããã®åå¿æ¡ä»¶ã¯ãåæ
ïŒïœåœã10mlã®ãã¬ãªã¢ã³é žã䜿çšããŠããè±åœ
ç¹èš±ç¬¬1097165å·æ现æžã®å®æœäŸïŒã«ç€ºãããæ¡
件ãšæ¯èŒããŠããããŠæå©ã§ããã䜿çšãããäž
察ã®åŒ·é žã®ãã¡ã®äžæ¹ã¯ããªããé ¢é žã§ããã¹ã
ã§ãããç¹ã«ããªãã«ãªãé ¢é žåã¯ããªã¯ããé ¢
é žã奜ãŸãããããªããé ¢é žã¯åæã¹ããã€ãã«
察ããŠ1.5ã¢ã«ä»¥äžã®ã¢ã«éã§ååšãã¹ãã§ããã ãŸããã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ããŒ
ã 21âã¢ã»ããŒãã«17âãã¬ã¬ãŒãåºãå°å ¥ã
ãå Žåã«ã¯ãããªãã«ãªãé ¢é žã®å¥œãŸãã䜿çšé
ã¯0.58mlïŒïœã§ããããããšå¯Ÿæ¯ããŠãåèšè±åœ
ç¹èš±ã®å®æœäŸïŒã§ã¯åæïŒïœåœãïŒmlã®ç¡æ°Žããª
ãã«ãªãé ¢é žãçšããŠããã äžå¯Ÿã®åŒ·é žã®ãã¡ã®ããäžæ¹ã®é žã¯è§Šåªéã§å
åšããããã¯ïœâãã«ãšã³ã¹ã«ãã³é žãã¡ã¿ã³ã¹
ã«ãã³é žããã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é žåã³å¡©
é žããéžã°ããã çš®ã ã®åå¿å€ã®æ··åé åºã¯éèŠã§ã¯ãªãããå®
éã®æ··ååŠçäžã¯åå¿åšãå·åŽããã®ã奜ãŸã
ããããªããé ¢é žãçŽïŒâã«å·åŽããããã§ã«ã«
ãã³é žç¡æ°Žç©ãå ããç¶ããŠç¬¬äºã®åŒ·é žãå ãã
æåŸã«åå¿ãããã¹ãåæã¹ããã€ããå ããã®
ãæ®éã§ããã æ¬çºæã®æãé©ãã¹ãç¹åŸŽã®äžã€ã¯çéã®åå¿
å€ã䜿çšããå Žåã«ãæ¬çºæã®æ°èŠæ¹æ³ã¯åŸæ¥æ
è¡ã®æ¹æ³ãããèããé«ãåå¿é床ãäžããç¹ã§
ããããã®ç¹ãæ¬çºæã®å©ç¹ã®äžéšãæ§æããã
ã®ã§ããã 次衚ã«ãã¿ã¡ã¿ãŸã³ 11âããªãã«ãªãã¢ã»ã
ãŒã 21âã¢ã»ããŒããžã®17âãã¬ã¬ãŒãåºã®å°
å ¥åå¿ã«ã€ããŠåŸèšå®æœäŸïŒã«ç€ºããæ¬çºææ¹æ³
åã³ä»£è¡šçãªåŸæ¥æè¡ã«åŸãè©ŠéšäŸã®åå¿æ¡ä»¶ã
察æ¯ããŠç€ºãã
ãè¡šã
ãã®åå¿é床ã®äžæã¯äžéšã¯åå¿æ··åç©ã®é«ã
èªé»çã«ãããã®ã§ãããšèããããããã®ããš
ã¯æ¯èŒçäœãèªé»çããã€ããã€ãã®äžæŽ»æ§åžé
å€ãçšããå Žåã«ã¯åå¿ãé²è¡ããªããšããäºå®
ã«ããç«èšŒããããããšãã°ãšã¹ãã«åã¯ã¢ã»ã
ãããªã«åã¯ãããã¡ã¿ã³ã®ååšäžã§ã¯çèµ·ãã
ããããã©ããããã©ã³ããžãªããµã³ãã¯ããã
ã«ã åã³ã¢ã»ãã³ã®ååšäžã§ã¯ãšã¹ãã«ååå¿ã¯
ããããŠç·©æ ¢ã§ãããïŒæéã®åå¿æéåŸã§ãã
åæã¹ããã€ãã®å€§éšåã¯æªå€åã®ãŸãååãã
ãããšãèªããããã奜çµæãäžããåèšïŒçš®é¡
ã®åžéå€ã¯é«ãèªé»çãæããããšãèªãããã
ã§ãããã åèšåŒïŒïŒã®åæååç©äžã®R5ã¯ãããã
ã·ã«åºã§ããåŸãã®ã§ã察称圢ã®17ïŒ21âãžãšã¹
ãã«ãåžæããå Žåã«ã¯åèšãšã¹ãã«ååå¿ã¯
17ïŒ21âãžããããã·ã¹ããã€ãã«ã€ããŠè¡ãªã
åŸãããšãèªããããã§ããããåèšåå¿ã®å®äº
åŸã«è¡ãªãããç®çç©ã®åé¢ã®ããã®æ¹æ³ã¯åæ
åã³ææã®çæç©ã«å¿ããŠæ±ºãŸããããšãã°ãå
èšåŒïŒïŒã®ååç©äžã®R2ããªããœåã¯ããã²
ã³ã§ããå Žåã«ã¯ãçæç©ã¯æ £çšã®æ段ãããšã
ã°æ°Žäžã§ã®æ²æŸ±ã«ããåŸããããåŸæ¥æè¡ã«ãã
ãŠã¯çæç©ã®åé¢ã«ã¯æ°Žèžæ°èžçãå¿ èŠã§ãããš
ãããŠããç¹ããã¿ãŠãæ¬çºæã«ãããåé¢ã«ç°¡
åãªæ £çšçåé¢æ段ãæ¡çšãåŸãç¹ãæ¬çºæã®å©
ç¹ã®äžéšãæ§æãããã®ã§ãããåŸæ¥æè¡ã«ãã
ãæ°Žèžæ°èžçã¯åœåã«äœ¿çšãã倧éå°ã®åå¿å€ã
é€å»ããããã«å¿ èŠãšããããã®ã§ãããããã
è¡ãªããªããã°æ²æŸ±ã«ããæ²¹ç¶ç©ãåŸããããã
ã¯ãã°ãã°åŠçå°é£ã§ããããã§ããããããã€
ãŠãæ¬çºæã«ãããæãŸããæå°éã®åå¿å€ã®äœ¿
çšã¯ããè¿ éãã€ã¯ãªãŒã³ãªåå¿ãéæãåŸãã®
ã¿ãªãããæèŠã®çæç©ã®çæãä¿é²ãããåæ§
ã«ãR2ãããªããã¢ã»ããã·åºã§ããåŒïŒïŒ
ã®ååç©ãçšããå Žåã«ããæ°Žäžã§ã®æ²æŸ±ã®ããš
ãæ £çšã®æ段ã«ããçæç©ã®åé¢æ³ãçšããŠ11â
ããªããã¢ã»ããŒã 17âãšã¹ãã«åçæç©ãå
é¢ããããéåžžãããªãã«ãªãã¢ã»ããŒãåä¿è·
åºã¯è¬åŠçã«èš±å®¹ãåŸãªãã®ã§ããããä¿è·åºã¯
æ®éé€å»ããå¿ èŠãããããããã€ãŠãæ¬çºæã®
å¥ã®ç¹åŸŽã¯11âããããã·ã«ååç©ãçŽæ¥åé¢ã
ãããšã«ãããããã¯ã¢ãã³åã¯ã¢ã³ã¢ãã¢ã®äœ¿
çšã«ãã€ãŠéæãåŸããã¢ãã³åã¯ã¢ã³ã¢ãã¢
ã¯ãæ°Žã®ååšåã¯äžååšã®ãããã«ãããŠãã11
âããªããã¢ã»ããŒãåºãéžæçã«é€å»ããããš
ã確èªãããããã®ç¹ã«ã€ããŠã¯ä»¥äžã«è©³è¿°ã
ããã¢ãã³ã®çœ®æååŒã¯ããããŠéèŠãªãã®ã§ã
ããšã¯æãããªãããçªçŽ ãè³éŠæç°ã®äžéšãæ§
æããã¢ãã³ãããšãã°ããªãžã³ãã¯äžæŽ»æ§ã§ã
ãæçšãªã¢ãã³ã®çŸ€ããé€å€ãããã æèŠã®çæç©ã¯äºã€ã®è¥å¹²ç°ãªãæ¹æ³ã«ãã€ãŠ
åé¢ãåŸããããªãã¡ãã¢ãã³åã¯æ°Žé žåã¢ã³ã¢
ããŠã ãã¢ã·ã«ååå¿æ··åç©ã«å ããããŠçæç©
ãæ°Žäžã§ã®æ²æŸ±ã®ãããªæ £çšã®æ段ã«ããåé¢ã
åŸããå¥æ³ãšããŠãæ°ŽïŒã¢ãã³æ··åç©ãçšããŠå
ã¯æ°Žé žåã¢ã³ã¢ããŠã 溶液ãçšããŠåå¿æ··åç©ã
çŽæ¥æ²æŸ±ãããããšãã§ãããã¢ãã³åã¯æ°Žé žå
ã¢ã³ã¢ããŠã ã®äœ¿çšéã¯ã¢ã·ã«åçšæ··åç©ã®çš®ã
ã®é žæ§æååã¯é žåé§ïŒproacidicïŒæåã®äžå
ãä¿èšŒããéå°éã§ããã¹ãã§ãããè¥å¹²ã®å Žå
ã«ã¯ã溶解æ§ã®ç¹ããããžãªããµã³ãããã©ãã
ããã©ã³åã¯ãžã¡ãã«ãã«ã ã¢ããã®ãããªäžæŽ»
æ§åžéå€ãå ããŠããªããã¢ã»ããŒãåºã®å®å šãª
è±é¢ã確ä¿ããããšãå¿ èŠã§ãããããããŠãæ¬
çºæã¯æèŠã®ïŒååã¯ïŒåã®ãšã¹ãã«åºã®å°å ¥å
ã³äžéäœååç©ãåé¢ããããšãªãã«æ¬¡åŸã®ããª
ããã¢ã»ããŒãä¿è·åºã®éžæçè±é¢ãå¯èœã«ãã
ãã®ã§ãããåŸæ¥ã¯è©²åŠçã®éæã«äºã€ã®å¥åã®
åå¿å·¥çšãå¿ èŠãšããŠããç¹ããã¿ãŠãæ¬çºæã®
åªäœæ§ã¯æããã§ããã11âããªããã¢ã»ãã«
17âãšã¹ãã«åã¹ããã€ãã®çŽæ¥æ²æŸ±ã¯åèšãã
ãšããã§ããããããŠ11âããããã·ã«çæç©ã®
ååŸã«ã¯ãããªããã¢ã»ããŒãåºãè±é¢ãããã
ãšãå¿ èŠã§ãããæ°Žã®ååšåã¯äžåšäžã®ãããã«
ãããŠããã¢ãã³ãã¢ã³ã¢ãã¢åã¯ããã©ãžã³ã®
䜿çšã«ããã»ãšãã©å®éçãªåçã§ããªããã¢ã»
ããŒãåºã®è±é¢åå¿ãéæãåŸãããšãèªããã
ãã11âããªããã¢ã»ãã« 17âãšã¹ãã«åã¹ã
ãã€ãã¯æèŠãªãã°äœçŽã¢ã«ã³ãŒã«ã奜ãŸããã¯
ã¡ã¿ããŒã«åã¯ãšã¿ããŒã«äžŠã³ã«ããã©ãããã
ã©ã³ããžãªããµã³ããžã¡ãã«ãã«ã ã¢ããã®ããš
ãäžæŽ»æ§åžéå€ã«æº¶è§£ãã次ãã§ã¢ãã³ãå°éã
奜ãŸããã¯åæã¹ããã€ãïŒã¢ã«åœã0.01ã1.0
ã¢ã«ã®å²åã§æ·»å ãããããªããã¢ã»ããŒãåºè±
é¢åå¿ã¯é垞宀枩ã§çŽ15åã§å®äºãããåŸããã
çæç©ã¯æ°Žäžã§æ²æŸ±ãããããšãæ £çšã®æ段ã«ã
ãåé¢ãåŸããå¥æ³ãšããŠãã¢ãã³ã®ä»£ãã«ç¡æ°Ž
äœçŽã¢ã«ã³ãŒã«äžã®ã¢ã³ã¢ãã¢ã¬ã¹ã®æº¶æ¶²ã䜿çš
ããããšãã§ããã ããã©ãžã³ã®äœ¿çšã¯åèšåŒïŒïŒäžã®R6ãæ°Ž
çŽ åã¯ïŒååã¯ïŒåã®ããã²ã³çœ®æåºã§ããåå
ç©ã®å Žåã«éå®ãããããã®ç¹ã¯å¥ãšããŠããã
ã©ãžã³ãçšããè±é¢åå¿ã¯ã¢ãã³ãçšããå Žåãš
åæ§ã«é²è¡ãããããã©ãžã³ã¯åèšåŒïŒïŒã®
R6ãã¢ã·ã«åºã§ããå Žåã«ã¯ãæãšããŠå¯çç©
ã®åœ¢æãããããã®ã§ã¢ãã³åã¯ã¢ã³ã¢ãã¢ãã
ãé©çšæ§ãäœãã åœæ¥è ã«åšç¥ã®ããšããã³ã«ãã³ã¹ããã€ã
17âã¢ããšã¹ãã«ã¯ç¹ã«é«æŽ»æ§ã§ãããã¢ãã³å
ã¯ã¢ã³ã¢ãã¢ãå©çšããŠ11âããªããã¢ã»ããŒã
åºã11âããªããã¢ã»ãã«â17âãšã¹ãã«â21â
ããããã·ã¹ããã€ãããè±é¢ãåŸãç¹ãæ¬çºæ
ã®ããã«å¥ã®ç¹åŸŽã§ãããé©ãã¹ãããšã«ãããª
ããã¢ã»ããŒãåºã¯ã該åºã®è±é¢å·¥çšäžã«ã21â
ãšã¹ãã«ãå šãçæããªããåã¯åã«ç¡èŠãåŸã
çšåºŠã®å°éã®ã¿çæããã«éããªãç¹ã§17âãšã¹
ãã«å®èœåºã«å¯ŸããŠå®å®åå¹æãåãŒãããã®ãš
ã¹ãã«äº€æåå¿ãé žæ§æ¡ä»¶äžåã¯å¡©åºæ§æ¡ä»¶äžã®
ãããã«ãããŠã容æã§ããã®ã¯åšç¥ã§ãããã
ããã®11ïŒ17âãžãšã¹ãã«ã¯ãè±åœç¹èš±ç¬¬
2079754å·æ现æžã«è©³è¿°ãããããšããã¢ã·ã«å
åã³ããã«ç¶ãåŒ·é žå 溶åªå解ãããªãåèšæ¹æ³
ã«ããR5ãOR7åã¯ããããã·ã«åºã§ããåŒ
ïŒïŒã®ååç©ããæãè¯å¥œã«è£œé ãåŸãã æ¬çºæã®ååç©ããæ¹è¯ããã±ã³ãžãŒ
ïŒMckenzieïŒè¡ç®¡å瞮詊éšã«ããè©ŠéšãããåŸèš
å®æœäŸ22ã«ç€ºããçµæç©ïŒ0.05ïŒ ã®æ¿åºŠåã³50mg
ã®æäžéã§ïŒãçšããŠè£œé ããã¯ãªãŒã ãå¥åº·ãª
20人ã®å¿é¡è ã®èäžã«å¡åžãããå¡åžã«çšããç¡
èã¬ãŒãŒãèŠã€ãŠããééçšããŒãã16æéåŸã«
åé€ããïŒæéãŸã§ã®æéééã§ãããã®é åã
芳å¯ãããè©Šéšã®çµæã瀺ããšããã«ããã°ãé©
ãã¹ãããšã«ããã¯ãã¡ã¿ãŸã³ 17ïŒ21âãžã¢ã»
ããŒãã¯ç€ºãããæäžæ¿åºŠã§ãã¿ã¡ã¿ãŸã³ 17â
ãã¬ã¬ãŒãåã³ãããµã¡ã¿ãŸã³ 17ïŒ21âãžãã
ããªããŒãã®äž¡è ãšå°ãªããšãåçã®å±æçå¹å
ãæãããè©Šéšããä»ã®åŸæ¥æªç¥ã®ã¹ããã€ãã
ãã®è©Šéšã§è¯å¥œãªå±æ掻æ§ã瀺ããã æ¬çºæã®ååç©ã¯åœæ¥è ã«åšç¥ã®è£œè¬äžèš±å®¹ã
åŸã賊圢å€åã³åžéå€ãšæ··åããå Žåã«å±éšçã«
æœçšãããå±æçµæç©ãšããŠæå¹ã§ãããããã
çµæç©ã®äŸãšããŠã¯ã¯ãªãŒã ãè»èãããŒã·ãš
ã³ãç¹çŒå€åã³çµå£åžå ¥åŽé§å€ããããæå¹æå
ã®å«éã¯å®éã®çµæç©ã«å¿ããŠæ±ºãŸãããäžè¬ã«
0.001ééïŒééïŒ ã0.5ééïŒééïŒ ã§ãããã
ã奜ãŸããã¯0.01ééïŒééïŒ ã0.25ééïŒéé
ïŒ ã®ç¯å²ã§ããã æ¬çºæã®ååç©ãçšããŠè£œé ããçµæç©ã¯ã³ã«
ãã³ã¹ããã€ãå¿çæ§ã®ç®èç ã®å±æåŠçœ®ã«çšã
ãããšãã§ãããããç®èç ã¯ä¹Ÿç¬ã湿ç¹ãç¥çµ
ç®èçãèæŒæ§ç®èçãæ¥è§Šç®èçãéææ§ç®è
çåã³éæŠç¹ãå å«ãåŸãã ããã«ãå®æœäŸïŒã§è£œé ãã21âããœãã·ãã¿
ã¡ã¿ãŸã³ 17âããã¿ããšãŒãã¯çèå 泚å°æ¶²ã«
ãããŠé·æéäœçšæç¶æ§ã®æŽ»æ§æåãšããŠçšãã
ã®ã«ç¹ã«é©ãããã®ã§ããã æ¬çºæã次ã®å®æœäŸã«ãã説æããããæ¬çºæ
ã¯äœããããã®å®æœäŸã«éå®ããããã®ã§ã¯ãª
ãã å®æœäŸ ïŒ ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17â
ãã¬ã¬ãŒã21âã¢ã»ããŒãã®è£œé æ¬çºæã®æ¹æ³ã«ããã¢ã·ã«åæ¡ä»¶ãåŸæ¥æè¡ã®
ã¢ã·ã«åæ¡ä»¶ãããè¿ éã§ãããšããäºå®ã説æ
ããããïŒã€ã®å®éšãè¡ãªãã第ïŒã®å®éšã§ã¯è±
åœç¹èš±ç¬¬1097165å·æ现æžã®å®æœäŸïŒã®åå¿æ¡ä»¶
ãçšããç¶ãã«ç¬¬ïŒã®å®éšã§ã¯ç¬¬ïŒã®å®éšã§ååš
ããéã®ïŒåã®åæãã¿ã¡ã¿ãŸã³11âããªãã«ãª
ãã¢ã»ããŒã21âã¢ã»ããŒããçšãããä»ã®ïŒã€
ã®è©Šéšã§ã¯æ¬çºæã«ããåå¿æ¡ä»¶ãçšãããè©Šæ
ã¯ééã眮ããŠååºããæ°Žã§åžéã次ãã§ã¯ãã
ãã«ã ã§æœåºãããããæ°ŽæŽãç¡æ°Žç¡«é žãããªãŠ
ã ã«ééããããšã«ãã也ç¥ããããåã ã®åå¿
ã®é²è¡ã¯èå±€ã¯ãããã°ã©ãã€ãŒã«ããç£èŠãã
çµæãåèšã®è¡šã«äžããããããã®çµæã¯æ¬çº
æã®æ¹æ³ãçšããæã«ã¯åå¿å€ãçžåœã«å°ãªãå
åšãããªããã¢ã·ã«ååå¿ã¯ããçæéã§å®äºã
ãããšãæããã«ç€ºããŠããã å®æœäŸ ïŒ 21âããœãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒã
ã®è£œé ç¡æ°Žããã¿ã³é žïŒ8.40mlïŒ31.78ããªã¢ã«ïŒå
ã³ããªã¯ããé ¢é žïŒ5.20ïœïŒ31.82ããªã¢ã«ïŒã
ïŒâã§æ··åãããã®åŸã«ïœâãã«ãšã³ã¹ã«ãã³é ž
ïŒ0.50ïœïŒåã³9αâãã«ãªãâ11βïŒ17αâãžãã
ããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³
âïŒïŒ20âãžãªã³ã»11âããªãã«ãªãã¢ã»ããŒã
ïŒ10.00ïœïŒ21.16ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã40ã50âã§ïŒæéæ¹æãã宀枩ã«å·åŽããã
次ãã§50ïŒ æ°Žæ§ã€ãœãããã«ã¢ãã³ã«ããããæ²
柱ããåºäœãéããæ°Žã§ååã«æŽæµãã50âã§
也ç¥ããããš9.48ïœã®21âããœãã·ãã¿ã¡ã¿ãŸã³
17âããã¿ããšãŒããåŸããã¡ã¿ããŒã«ããåçµ
æ¶ããããšåæçŽåºŠã®21âããœãã·ãã¿ã¡ã¿ãŸã³
17âããã¿ããšãŒããåŸãããã¯æ¬¡ã®ç¹æ§ãæã
ãïŒèç¹194ãïŒâããžãªããµã³äžã®æ¯æå 床ïŒ
54.28ãã å®æœäŸ ïŒ ãããµã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé ç¡æ°Žãã¬ãªã¢ã³é žïŒ3.90mlïŒ19.47ããªã¢ã«ïŒ
ããåãã€ãŠå·åŽããããªãã«ãªãé ¢é žïŒ1.50
mlïŒ19.60ããªã¢ã«ïŒã«å ããç¶ããŠãã³ãŒã³ã¹
ã«ãã³é žïŒ250mgïŒåã³æåŸã«9αâãã«ãªãâ
11βïŒ17αïŒ21âããªããããã·â16αâã¡ãã«ã
ã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âã
ãªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒãïŒ5.00ïœïŒ
9.68ããªã¢ã«ïŒãå ããããã®æ··åç©ã40ã45â
ã§ïŒæéæ¹æããŠãã25ïŒ æ°Žé žåã¢ã³ã¢ããŠã ã
å ããã30åéæ¹æããŠããã該混åç©ãæ°·ã§å·
ãããæ°Žã«ããããæ²æŸ±ããåºäœãéã«ããå
éããæ°ŽæŽã50âã§ä¹Ÿç¥ãããã秀é4.80ïœã®ç
æç©ã¯æšèšååç©ã®çæ£è©Šæãšã¯ãããã°ã©ãã€
ãŒã§ã®åæã«ããåäžã§ããããšã瀺ãããåçµ
æ¶ã«ããèç¹159âã®çæç©ãåŸãã å®æœäŸ ïŒ ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãã®è£œé ç¡æ°Žé ¢é žïŒ2.00mlïŒ21.16ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ2.00mlïŒ26.13ããªã¢ã«ïŒãšïœâã
ã«ãšã³ã¹ã«ãã³é žïŒ0.25ïœïŒãšãïŒâã§æ··åãã
9αâã¯ããâ11βïŒ17αïŒ21âããªããããã·â
16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20
âãžãªã³ 11âããªãã«ãªãã¢ã»ããŒãïŒ2.50
ïœïŒ4.95ããªã¢ã«ïŒãå ããããã®æ··åç©ã40â
ã§ïŒæé35åæ¹æãã次ãã§ïŒâã«å·åŽãããã©
ããããã©ã³ïŒ10mlïŒåã³12.5ïŒ ã¢ã³ã¢ãã¢æ°Ž
ïŒ25mlïŒãå ããã30åéæ¹æåŸã«ã該混åç©ã
æ°·ã§å·ãããæ°Žã«ããããæ²æŸ±ããçæç©ãå
ããæ°ŽæŽã50âã§ä¹Ÿç¥ããããš2.27ïœã®æšèšåå
ç©ãåŸããã¡ã¿ããŒã«ããåçµæ¶ãããŠåæçšè©Š
æãåŸãããã¯æ¬¡ã®åæå€ãæããïŒèç¹228ã
231âãã¯ãããã«ã äžã®æ¯æå 床ïŒ87.28ãã å®æœäŸ ïŒ 9αïŒ11βâãžã¯ããâ17αïŒ21âãžããããã·
â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â
ïŒïŒ20âãžãªã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé ããªãã«ãªãé ¢é žïŒ4.80mlïŒ62.72ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ4.80mlïŒ23.97ããªã¢ã«ïŒ
ãšã¡ã¿ã³ã¹ã«ãã³é žïŒ0.400mlïŒãšãïŒâã§æ··å
ãã次ãã§9αïŒ11βâãžã¯ããâ17αïŒ21âãžã
ãããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãš
ã³âïŒïŒ20âãžãªã³21âã¢ã»ããŒãïŒ7.50ïœïŒ
15.98ããªã¢ã«ïŒãå ããããã®æ··åç©ã40âã§
ïŒæéæ¹æãã次ãã§æ°·ã§å·ãããæ°Žã«ç·©æ ¢ã«
ããããéã«ããæ²æŸ±ç©ãåéããæ°ŽæŽãã50
âã§ä¹Ÿç¥ããããš8.90ïœã®æšèšååç©ãåŸããã¡
ã¿ããŒã«ããåçµæ¶ããããšãžãªããµã³äžã§ïŒ
110.53ãã®æ¯æå 床ãæããåæçŽåºŠã®è©ŠæãåŸ
ãããã該詊æã®CI質éã¹ãã¯ãã«ã¯ïœïŒe323
ã§åºéšããŒã¯ãæããªããïœïŒe553ïŒïŒïŒïŒïŒã«
äžå¿ãæãã代衚çãªååã€ãªã³æš¡æ§ã瀺ãã å®æœäŸ ïŒ 21âããœãã·ãã¯ãã¡ã¿ãŸã³ 17âããã¬ãŒã
ã®è£œé ç¡æ°Žé ªé žïŒ5.25mlïŒ32.19ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ5.25mlïŒ68.60ããªã¢ã«ïŒãšã¡ã¿ã³
ã¹ã«ãã³é žïŒ0.45mlïŒãšãïŒâã§æ··åãã次ãã§
9αâã¯ããâ11βïŒ17αâãžããããã·â16βâã¡
ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³ïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒãïŒ7.50ïœïŒ15.34ããª
ã¢ã«ïŒãå ãããåå¿æ··åç©ã40âã§ïŒæé30å
æ¹æãã次ãã§ããã©ããããã©ã³ïŒ17.4mlïŒãš
12.5ïŒ ã¢ã³ã¢ãã¢æ°ŽïŒ43.5mlïŒãšã®æ··åç©ã«ãã
ãã15åéæ¹æããåŸã«è©²æ··åç©ãæ°·ã§å·ããã
æ°Žã«ããããçæç©ãåããæ°ŽæŽãã50âã§ä¹Ÿ
ç¥ããããš6.29ïœã®æšèšååç©ãåŸããæ°·ã§å·ã
ããã¡ã¿ããŒã«ãšã¢ã»ãã³ãšã®æ··åç©ã§æŽæµãã
åŸã«ã¯ãçæç©ã¯æ¬¡ã®åæå€ãæããïŒèç¹238
ã240âãã¯ãããã«ã äžã®æ¯æå 床ïŒ102.72ãã å®æœäŸ ïŒ 9αâã¯ããâ17αâããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ11ïŒ20âããª
ãªã³17âããã¬ãŒãã®è£œé ããªãã«ãªãé ¢é žïŒ3.50mlïŒ45.73ããªã¢ã«ïŒ
ãšç¡æ°Žé ªé žïŒ3.20mlïŒ19.62ããªã¢ã«ïŒãšã¡ã¿ã³
ã¹ã«ãã³é žïŒ0.25mlïŒãš9αâã¯ããâ17αâãã
ããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³
âïŒïŒ11ïŒ20âããªãªã³ïŒ5.00ïœïŒ12.79ããªã¢
ã«ïŒãšãéåžžã®æ§åŒã§40âã§ïŒæéåå¿ãããå
å¿æ··åç©ãæ°Žäžã«æ²æŸ±ãããã¡ã¿ããŒã«ïŒãžã¯ã
ãã¡ã¿ã³ïŒãžã€ãœãããã«ãšãŒãã«ããåçµæ¶ã
ããåŸã«5.27ïœã®æšèšååç©ãåŸããèç¹154ã
ïŒâãã¯ãããã«ã äžã®æ¯æå 床ïŒ198.83ãã å®æœäŸ ïŒ 9αïŒ11βâãžã¯ããâ17αâããããã·â16βâ
ã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³17âãã¬ã¬ãŒãã®è£œé ç¡æ°Žãã¬ãªã¢ã³é žïŒ4.80mlïŒ23.97ããªã¢ã«ïŒ
ããå·åŽããããªãã«ãªãé ¢é žïŒ4.80mlïŒ62.72
ããªã¢ã«ïŒã«å ããç¶ããŠã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ0.400mlïŒåã³æåŸã«9αïŒ11βâãžã¯ããâ17α
âããããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâ
ãžãšã³âïŒïŒ20âãžãªã³ïŒ7.50ïœïŒ18.23ããªã¢
ã«ïŒãå ããã枩床ã40âã«ææž©ããããã®æ··å
ç©ãïŒæé45åæ¹æã次ãã§æ°·ã§å·åŽããæ°Žã«ç·©
æ ¢ã«ããããããããŠåŸãããåºäœãéããæ°Ž
æŽããæ°Žé žåã«ãªãŠã ã®é å€äžã§ç空也ç¥ããã
ã¡ã¿ããŒã«ããçŽã¡ã«åçµæ¶ããããš6.97ïœã®æš
èšååç©ãåŸããæ¯æ¶²ãæ¿çž®ããããšã«ããå¥é
ã®çæç©ãåŸããããçæç©ã®èç¹ã¯170ãïŒâ
ã§ãããžãªããµã³äžã®æ¯æå 床ã¯ïŒ118.54ãã§ã
ãã å®æœäŸ ïŒ ãã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»ããŒãã®
補é (a) ããªãã«ãªãé ¢é žïŒ31.32mlïŒ0.409ã¢ã«ïŒãš
ç¡æ°Žãã¬ãªã¢ã³é žïŒ41.04mlïŒ0.205ã¢ã«ïŒãšïœ
âãã«ãšã³ã¹ã«ãã³é žïŒ2.70ïœïŒãšãïŒâã§æ··
åãã9αâãã«ãªãâ11βïŒ17αïŒ21âããªã
ãããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãž
ãšã³âïŒïŒ30âãžãªã³11âããªãã«ãªãã¢ã»ã
ãŒã21âã¢ã»ããŒãïŒ54.00ïœïŒ0.102ã¢ã«ïŒã
次ãã§å ããã枩床ã40âã«ææž©ããããã®æ··
åç©ãïŒæé25åæå¹ã«æ¹æãããæ°·ã§å·åŽã
ã10ïŒ ããªãžã³ãšæ°Žãšã®æ··åç©ã§åŠçããç¶ã
ãŠæ²¹ç¶ã®åºäœãã¡ã¿ããŒã«ã«æº¶è§£ãããæ°·ã§å·
åŽããæ°Žäžã«æ²æŸ±ããããšçµæ¶è³ªã®çæç©ã
åŸããããåããæ°ŽæŽãã50âã§ä¹Ÿç¥ãã
ãããã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã
17âãã¬ã¬ãŒã21âã¢ã»ããŒãã®åéã¯60.10
ïœã§ããããã®çæç©ã¯ã¡ã¿ããŒã«äžã§242ã®
ïŒïŒ ïŒcmïŒ235ã7nïœïŒãæããã (b) 次ãã§ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ã
ãŒã17âãã¬ã¬ãŒã21âã¢ã»ããŒãã次ã®äžè¬
æ³ã«ãããã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»
ããŒãã«è»¢åããåŸãïŒ åæã¹ããã€ããã溶å€ã«å ¥ããéžå®åå¿å€ãš
æ··åããç¹å®ã®æéæäžã®æž©åºŠã§æ¹æãããæ°·ã§
å·ãããæ°Žäžã§æ²æŸ±ãããéããæ°ŽæŽã50âã§
也ç¥ãããããšã«ããçæç©ãåŸãã çš®ã ã®å®éšã®çµæã以äžã®è¡šã«äžããã
èªé»çã«ãããã®ã§ãããšèããããããã®ããš
ã¯æ¯èŒçäœãèªé»çããã€ããã€ãã®äžæŽ»æ§åžé
å€ãçšããå Žåã«ã¯åå¿ãé²è¡ããªããšããäºå®
ã«ããç«èšŒããããããšãã°ãšã¹ãã«åã¯ã¢ã»ã
ãããªã«åã¯ãããã¡ã¿ã³ã®ååšäžã§ã¯çèµ·ãã
ããããã©ããããã©ã³ããžãªããµã³ãã¯ããã
ã«ã åã³ã¢ã»ãã³ã®ååšäžã§ã¯ãšã¹ãã«ååå¿ã¯
ããããŠç·©æ ¢ã§ãããïŒæéã®åå¿æéåŸã§ãã
åæã¹ããã€ãã®å€§éšåã¯æªå€åã®ãŸãååãã
ãããšãèªããããã奜çµæãäžããåèšïŒçš®é¡
ã®åžéå€ã¯é«ãèªé»çãæããããšãèªãããã
ã§ãããã åèšåŒïŒïŒã®åæååç©äžã®R5ã¯ãããã
ã·ã«åºã§ããåŸãã®ã§ã察称圢ã®17ïŒ21âãžãšã¹
ãã«ãåžæããå Žåã«ã¯åèšãšã¹ãã«ååå¿ã¯
17ïŒ21âãžããããã·ã¹ããã€ãã«ã€ããŠè¡ãªã
åŸãããšãèªããããã§ããããåèšåå¿ã®å®äº
åŸã«è¡ãªãããç®çç©ã®åé¢ã®ããã®æ¹æ³ã¯åæ
åã³ææã®çæç©ã«å¿ããŠæ±ºãŸããããšãã°ãå
èšåŒïŒïŒã®ååç©äžã®R2ããªããœåã¯ããã²
ã³ã§ããå Žåã«ã¯ãçæç©ã¯æ £çšã®æ段ãããšã
ã°æ°Žäžã§ã®æ²æŸ±ã«ããåŸããããåŸæ¥æè¡ã«ãã
ãŠã¯çæç©ã®åé¢ã«ã¯æ°Žèžæ°èžçãå¿ èŠã§ãããš
ãããŠããç¹ããã¿ãŠãæ¬çºæã«ãããåé¢ã«ç°¡
åãªæ £çšçåé¢æ段ãæ¡çšãåŸãç¹ãæ¬çºæã®å©
ç¹ã®äžéšãæ§æãããã®ã§ãããåŸæ¥æè¡ã«ãã
ãæ°Žèžæ°èžçã¯åœåã«äœ¿çšãã倧éå°ã®åå¿å€ã
é€å»ããããã«å¿ èŠãšããããã®ã§ãããããã
è¡ãªããªããã°æ²æŸ±ã«ããæ²¹ç¶ç©ãåŸããããã
ã¯ãã°ãã°åŠçå°é£ã§ããããã§ããããããã€
ãŠãæ¬çºæã«ãããæãŸããæå°éã®åå¿å€ã®äœ¿
çšã¯ããè¿ éãã€ã¯ãªãŒã³ãªåå¿ãéæãåŸãã®
ã¿ãªãããæèŠã®çæç©ã®çæãä¿é²ãããåæ§
ã«ãR2ãããªããã¢ã»ããã·åºã§ããåŒïŒïŒ
ã®ååç©ãçšããå Žåã«ããæ°Žäžã§ã®æ²æŸ±ã®ããš
ãæ £çšã®æ段ã«ããçæç©ã®åé¢æ³ãçšããŠ11â
ããªããã¢ã»ããŒã 17âãšã¹ãã«åçæç©ãå
é¢ããããéåžžãããªãã«ãªãã¢ã»ããŒãåä¿è·
åºã¯è¬åŠçã«èš±å®¹ãåŸãªãã®ã§ããããä¿è·åºã¯
æ®éé€å»ããå¿ èŠãããããããã€ãŠãæ¬çºæã®
å¥ã®ç¹åŸŽã¯11âããããã·ã«ååç©ãçŽæ¥åé¢ã
ãããšã«ãããããã¯ã¢ãã³åã¯ã¢ã³ã¢ãã¢ã®äœ¿
çšã«ãã€ãŠéæãåŸããã¢ãã³åã¯ã¢ã³ã¢ãã¢
ã¯ãæ°Žã®ååšåã¯äžååšã®ãããã«ãããŠãã11
âããªããã¢ã»ããŒãåºãéžæçã«é€å»ããããš
ã確èªãããããã®ç¹ã«ã€ããŠã¯ä»¥äžã«è©³è¿°ã
ããã¢ãã³ã®çœ®æååŒã¯ããããŠéèŠãªãã®ã§ã
ããšã¯æãããªãããçªçŽ ãè³éŠæç°ã®äžéšãæ§
æããã¢ãã³ãããšãã°ããªãžã³ãã¯äžæŽ»æ§ã§ã
ãæçšãªã¢ãã³ã®çŸ€ããé€å€ãããã æèŠã®çæç©ã¯äºã€ã®è¥å¹²ç°ãªãæ¹æ³ã«ãã€ãŠ
åé¢ãåŸããããªãã¡ãã¢ãã³åã¯æ°Žé žåã¢ã³ã¢
ããŠã ãã¢ã·ã«ååå¿æ··åç©ã«å ããããŠçæç©
ãæ°Žäžã§ã®æ²æŸ±ã®ãããªæ £çšã®æ段ã«ããåé¢ã
åŸããå¥æ³ãšããŠãæ°ŽïŒã¢ãã³æ··åç©ãçšããŠå
ã¯æ°Žé žåã¢ã³ã¢ããŠã 溶液ãçšããŠåå¿æ··åç©ã
çŽæ¥æ²æŸ±ãããããšãã§ãããã¢ãã³åã¯æ°Žé žå
ã¢ã³ã¢ããŠã ã®äœ¿çšéã¯ã¢ã·ã«åçšæ··åç©ã®çš®ã
ã®é žæ§æååã¯é žåé§ïŒproacidicïŒæåã®äžå
ãä¿èšŒããéå°éã§ããã¹ãã§ãããè¥å¹²ã®å Žå
ã«ã¯ã溶解æ§ã®ç¹ããããžãªããµã³ãããã©ãã
ããã©ã³åã¯ãžã¡ãã«ãã«ã ã¢ããã®ãããªäžæŽ»
æ§åžéå€ãå ããŠããªããã¢ã»ããŒãåºã®å®å šãª
è±é¢ã確ä¿ããããšãå¿ èŠã§ãããããããŠãæ¬
çºæã¯æèŠã®ïŒååã¯ïŒåã®ãšã¹ãã«åºã®å°å ¥å
ã³äžéäœååç©ãåé¢ããããšãªãã«æ¬¡åŸã®ããª
ããã¢ã»ããŒãä¿è·åºã®éžæçè±é¢ãå¯èœã«ãã
ãã®ã§ãããåŸæ¥ã¯è©²åŠçã®éæã«äºã€ã®å¥åã®
åå¿å·¥çšãå¿ èŠãšããŠããç¹ããã¿ãŠãæ¬çºæã®
åªäœæ§ã¯æããã§ããã11âããªããã¢ã»ãã«
17âãšã¹ãã«åã¹ããã€ãã®çŽæ¥æ²æŸ±ã¯åèšãã
ãšããã§ããããããŠ11âããããã·ã«çæç©ã®
ååŸã«ã¯ãããªããã¢ã»ããŒãåºãè±é¢ãããã
ãšãå¿ èŠã§ãããæ°Žã®ååšåã¯äžåšäžã®ãããã«
ãããŠããã¢ãã³ãã¢ã³ã¢ãã¢åã¯ããã©ãžã³ã®
䜿çšã«ããã»ãšãã©å®éçãªåçã§ããªããã¢ã»
ããŒãåºã®è±é¢åå¿ãéæãåŸãããšãèªããã
ãã11âããªããã¢ã»ãã« 17âãšã¹ãã«åã¹ã
ãã€ãã¯æèŠãªãã°äœçŽã¢ã«ã³ãŒã«ã奜ãŸããã¯
ã¡ã¿ããŒã«åã¯ãšã¿ããŒã«äžŠã³ã«ããã©ãããã
ã©ã³ããžãªããµã³ããžã¡ãã«ãã«ã ã¢ããã®ããš
ãäžæŽ»æ§åžéå€ã«æº¶è§£ãã次ãã§ã¢ãã³ãå°éã
奜ãŸããã¯åæã¹ããã€ãïŒã¢ã«åœã0.01ã1.0
ã¢ã«ã®å²åã§æ·»å ãããããªããã¢ã»ããŒãåºè±
é¢åå¿ã¯é垞宀枩ã§çŽ15åã§å®äºãããåŸããã
çæç©ã¯æ°Žäžã§æ²æŸ±ãããããšãæ £çšã®æ段ã«ã
ãåé¢ãåŸããå¥æ³ãšããŠãã¢ãã³ã®ä»£ãã«ç¡æ°Ž
äœçŽã¢ã«ã³ãŒã«äžã®ã¢ã³ã¢ãã¢ã¬ã¹ã®æº¶æ¶²ã䜿çš
ããããšãã§ããã ããã©ãžã³ã®äœ¿çšã¯åèšåŒïŒïŒäžã®R6ãæ°Ž
çŽ åã¯ïŒååã¯ïŒåã®ããã²ã³çœ®æåºã§ããåå
ç©ã®å Žåã«éå®ãããããã®ç¹ã¯å¥ãšããŠããã
ã©ãžã³ãçšããè±é¢åå¿ã¯ã¢ãã³ãçšããå Žåãš
åæ§ã«é²è¡ãããããã©ãžã³ã¯åèšåŒïŒïŒã®
R6ãã¢ã·ã«åºã§ããå Žåã«ã¯ãæãšããŠå¯çç©
ã®åœ¢æãããããã®ã§ã¢ãã³åã¯ã¢ã³ã¢ãã¢ãã
ãé©çšæ§ãäœãã åœæ¥è ã«åšç¥ã®ããšããã³ã«ãã³ã¹ããã€ã
17âã¢ããšã¹ãã«ã¯ç¹ã«é«æŽ»æ§ã§ãããã¢ãã³å
ã¯ã¢ã³ã¢ãã¢ãå©çšããŠ11âããªããã¢ã»ããŒã
åºã11âããªããã¢ã»ãã«â17âãšã¹ãã«â21â
ããããã·ã¹ããã€ãããè±é¢ãåŸãç¹ãæ¬çºæ
ã®ããã«å¥ã®ç¹åŸŽã§ãããé©ãã¹ãããšã«ãããª
ããã¢ã»ããŒãåºã¯ã該åºã®è±é¢å·¥çšäžã«ã21â
ãšã¹ãã«ãå šãçæããªããåã¯åã«ç¡èŠãåŸã
çšåºŠã®å°éã®ã¿çæããã«éããªãç¹ã§17âãšã¹
ãã«å®èœåºã«å¯ŸããŠå®å®åå¹æãåãŒãããã®ãš
ã¹ãã«äº€æåå¿ãé žæ§æ¡ä»¶äžåã¯å¡©åºæ§æ¡ä»¶äžã®
ãããã«ãããŠã容æã§ããã®ã¯åšç¥ã§ãããã
ããã®11ïŒ17âãžãšã¹ãã«ã¯ãè±åœç¹èš±ç¬¬
2079754å·æ现æžã«è©³è¿°ãããããšããã¢ã·ã«å
åã³ããã«ç¶ãåŒ·é žå 溶åªå解ãããªãåèšæ¹æ³
ã«ããR5ãOR7åã¯ããããã·ã«åºã§ããåŒ
ïŒïŒã®ååç©ããæãè¯å¥œã«è£œé ãåŸãã æ¬çºæã®ååç©ããæ¹è¯ããã±ã³ãžãŒ
ïŒMckenzieïŒè¡ç®¡å瞮詊éšã«ããè©ŠéšãããåŸèš
å®æœäŸ22ã«ç€ºããçµæç©ïŒ0.05ïŒ ã®æ¿åºŠåã³50mg
ã®æäžéã§ïŒãçšããŠè£œé ããã¯ãªãŒã ãå¥åº·ãª
20人ã®å¿é¡è ã®èäžã«å¡åžãããå¡åžã«çšããç¡
èã¬ãŒãŒãèŠã€ãŠããééçšããŒãã16æéåŸã«
åé€ããïŒæéãŸã§ã®æéééã§ãããã®é åã
芳å¯ãããè©Šéšã®çµæã瀺ããšããã«ããã°ãé©
ãã¹ãããšã«ããã¯ãã¡ã¿ãŸã³ 17ïŒ21âãžã¢ã»
ããŒãã¯ç€ºãããæäžæ¿åºŠã§ãã¿ã¡ã¿ãŸã³ 17â
ãã¬ã¬ãŒãåã³ãããµã¡ã¿ãŸã³ 17ïŒ21âãžãã
ããªããŒãã®äž¡è ãšå°ãªããšãåçã®å±æçå¹å
ãæãããè©Šéšããä»ã®åŸæ¥æªç¥ã®ã¹ããã€ãã
ãã®è©Šéšã§è¯å¥œãªå±æ掻æ§ã瀺ããã æ¬çºæã®ååç©ã¯åœæ¥è ã«åšç¥ã®è£œè¬äžèš±å®¹ã
åŸã賊圢å€åã³åžéå€ãšæ··åããå Žåã«å±éšçã«
æœçšãããå±æçµæç©ãšããŠæå¹ã§ãããããã
çµæç©ã®äŸãšããŠã¯ã¯ãªãŒã ãè»èãããŒã·ãš
ã³ãç¹çŒå€åã³çµå£åžå ¥åŽé§å€ããããæå¹æå
ã®å«éã¯å®éã®çµæç©ã«å¿ããŠæ±ºãŸãããäžè¬ã«
0.001ééïŒééïŒ ã0.5ééïŒééïŒ ã§ãããã
ã奜ãŸããã¯0.01ééïŒééïŒ ã0.25ééïŒéé
ïŒ ã®ç¯å²ã§ããã æ¬çºæã®ååç©ãçšããŠè£œé ããçµæç©ã¯ã³ã«
ãã³ã¹ããã€ãå¿çæ§ã®ç®èç ã®å±æåŠçœ®ã«çšã
ãããšãã§ãããããç®èç ã¯ä¹Ÿç¬ã湿ç¹ãç¥çµ
ç®èçãèæŒæ§ç®èçãæ¥è§Šç®èçãéææ§ç®è
çåã³éæŠç¹ãå å«ãåŸãã ããã«ãå®æœäŸïŒã§è£œé ãã21âããœãã·ãã¿
ã¡ã¿ãŸã³ 17âããã¿ããšãŒãã¯çèå 泚å°æ¶²ã«
ãããŠé·æéäœçšæç¶æ§ã®æŽ»æ§æåãšããŠçšãã
ã®ã«ç¹ã«é©ãããã®ã§ããã æ¬çºæã次ã®å®æœäŸã«ãã説æããããæ¬çºæ
ã¯äœããããã®å®æœäŸã«éå®ããããã®ã§ã¯ãª
ãã å®æœäŸ ïŒ ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17â
ãã¬ã¬ãŒã21âã¢ã»ããŒãã®è£œé æ¬çºæã®æ¹æ³ã«ããã¢ã·ã«åæ¡ä»¶ãåŸæ¥æè¡ã®
ã¢ã·ã«åæ¡ä»¶ãããè¿ éã§ãããšããäºå®ã説æ
ããããïŒã€ã®å®éšãè¡ãªãã第ïŒã®å®éšã§ã¯è±
åœç¹èš±ç¬¬1097165å·æ现æžã®å®æœäŸïŒã®åå¿æ¡ä»¶
ãçšããç¶ãã«ç¬¬ïŒã®å®éšã§ã¯ç¬¬ïŒã®å®éšã§ååš
ããéã®ïŒåã®åæãã¿ã¡ã¿ãŸã³11âããªãã«ãª
ãã¢ã»ããŒã21âã¢ã»ããŒããçšãããä»ã®ïŒã€
ã®è©Šéšã§ã¯æ¬çºæã«ããåå¿æ¡ä»¶ãçšãããè©Šæ
ã¯ééã眮ããŠååºããæ°Žã§åžéã次ãã§ã¯ãã
ãã«ã ã§æœåºãããããæ°ŽæŽãç¡æ°Žç¡«é žãããªãŠ
ã ã«ééããããšã«ãã也ç¥ããããåã ã®åå¿
ã®é²è¡ã¯èå±€ã¯ãããã°ã©ãã€ãŒã«ããç£èŠãã
çµæãåèšã®è¡šã«äžããããããã®çµæã¯æ¬çº
æã®æ¹æ³ãçšããæã«ã¯åå¿å€ãçžåœã«å°ãªãå
åšãããªããã¢ã·ã«ååå¿ã¯ããçæéã§å®äºã
ãããšãæããã«ç€ºããŠããã å®æœäŸ ïŒ 21âããœãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒã
ã®è£œé ç¡æ°Žããã¿ã³é žïŒ8.40mlïŒ31.78ããªã¢ã«ïŒå
ã³ããªã¯ããé ¢é žïŒ5.20ïœïŒ31.82ããªã¢ã«ïŒã
ïŒâã§æ··åãããã®åŸã«ïœâãã«ãšã³ã¹ã«ãã³é ž
ïŒ0.50ïœïŒåã³9αâãã«ãªãâ11βïŒ17αâãžãã
ããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³
âïŒïŒ20âãžãªã³ã»11âããªãã«ãªãã¢ã»ããŒã
ïŒ10.00ïœïŒ21.16ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã40ã50âã§ïŒæéæ¹æãã宀枩ã«å·åŽããã
次ãã§50ïŒ æ°Žæ§ã€ãœãããã«ã¢ãã³ã«ããããæ²
柱ããåºäœãéããæ°Žã§ååã«æŽæµãã50âã§
也ç¥ããããš9.48ïœã®21âããœãã·ãã¿ã¡ã¿ãŸã³
17âããã¿ããšãŒããåŸããã¡ã¿ããŒã«ããåçµ
æ¶ããããšåæçŽåºŠã®21âããœãã·ãã¿ã¡ã¿ãŸã³
17âããã¿ããšãŒããåŸãããã¯æ¬¡ã®ç¹æ§ãæã
ãïŒèç¹194ãïŒâããžãªããµã³äžã®æ¯æå 床ïŒ
54.28ãã å®æœäŸ ïŒ ãããµã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé ç¡æ°Žãã¬ãªã¢ã³é žïŒ3.90mlïŒ19.47ããªã¢ã«ïŒ
ããåãã€ãŠå·åŽããããªãã«ãªãé ¢é žïŒ1.50
mlïŒ19.60ããªã¢ã«ïŒã«å ããç¶ããŠãã³ãŒã³ã¹
ã«ãã³é žïŒ250mgïŒåã³æåŸã«9αâãã«ãªãâ
11βïŒ17αïŒ21âããªããããã·â16αâã¡ãã«ã
ã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âã
ãªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒãïŒ5.00ïœïŒ
9.68ããªã¢ã«ïŒãå ããããã®æ··åç©ã40ã45â
ã§ïŒæéæ¹æããŠãã25ïŒ æ°Žé žåã¢ã³ã¢ããŠã ã
å ããã30åéæ¹æããŠããã該混åç©ãæ°·ã§å·
ãããæ°Žã«ããããæ²æŸ±ããåºäœãéã«ããå
éããæ°ŽæŽã50âã§ä¹Ÿç¥ãããã秀é4.80ïœã®ç
æç©ã¯æšèšååç©ã®çæ£è©Šæãšã¯ãããã°ã©ãã€
ãŒã§ã®åæã«ããåäžã§ããããšã瀺ãããåçµ
æ¶ã«ããèç¹159âã®çæç©ãåŸãã å®æœäŸ ïŒ ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãã®è£œé ç¡æ°Žé ¢é žïŒ2.00mlïŒ21.16ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ2.00mlïŒ26.13ããªã¢ã«ïŒãšïœâã
ã«ãšã³ã¹ã«ãã³é žïŒ0.25ïœïŒãšãïŒâã§æ··åãã
9αâã¯ããâ11βïŒ17αïŒ21âããªããããã·â
16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20
âãžãªã³ 11âããªãã«ãªãã¢ã»ããŒãïŒ2.50
ïœïŒ4.95ããªã¢ã«ïŒãå ããããã®æ··åç©ã40â
ã§ïŒæé35åæ¹æãã次ãã§ïŒâã«å·åŽãããã©
ããããã©ã³ïŒ10mlïŒåã³12.5ïŒ ã¢ã³ã¢ãã¢æ°Ž
ïŒ25mlïŒãå ããã30åéæ¹æåŸã«ã該混åç©ã
æ°·ã§å·ãããæ°Žã«ããããæ²æŸ±ããçæç©ãå
ããæ°ŽæŽã50âã§ä¹Ÿç¥ããããš2.27ïœã®æšèšåå
ç©ãåŸããã¡ã¿ããŒã«ããåçµæ¶ãããŠåæçšè©Š
æãåŸãããã¯æ¬¡ã®åæå€ãæããïŒèç¹228ã
231âãã¯ãããã«ã äžã®æ¯æå 床ïŒ87.28ãã å®æœäŸ ïŒ 9αïŒ11βâãžã¯ããâ17αïŒ21âãžããããã·
â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â
ïŒïŒ20âãžãªã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé ããªãã«ãªãé ¢é žïŒ4.80mlïŒ62.72ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ4.80mlïŒ23.97ããªã¢ã«ïŒ
ãšã¡ã¿ã³ã¹ã«ãã³é žïŒ0.400mlïŒãšãïŒâã§æ··å
ãã次ãã§9αïŒ11βâãžã¯ããâ17αïŒ21âãžã
ãããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãš
ã³âïŒïŒ20âãžãªã³21âã¢ã»ããŒãïŒ7.50ïœïŒ
15.98ããªã¢ã«ïŒãå ããããã®æ··åç©ã40âã§
ïŒæéæ¹æãã次ãã§æ°·ã§å·ãããæ°Žã«ç·©æ ¢ã«
ããããéã«ããæ²æŸ±ç©ãåéããæ°ŽæŽãã50
âã§ä¹Ÿç¥ããããš8.90ïœã®æšèšååç©ãåŸããã¡
ã¿ããŒã«ããåçµæ¶ããããšãžãªããµã³äžã§ïŒ
110.53ãã®æ¯æå 床ãæããåæçŽåºŠã®è©ŠæãåŸ
ãããã該詊æã®CI質éã¹ãã¯ãã«ã¯ïœïŒe323
ã§åºéšããŒã¯ãæããªããïœïŒe553ïŒïŒïŒïŒïŒã«
äžå¿ãæãã代衚çãªååã€ãªã³æš¡æ§ã瀺ãã å®æœäŸ ïŒ 21âããœãã·ãã¯ãã¡ã¿ãŸã³ 17âããã¬ãŒã
ã®è£œé ç¡æ°Žé ªé žïŒ5.25mlïŒ32.19ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ5.25mlïŒ68.60ããªã¢ã«ïŒãšã¡ã¿ã³
ã¹ã«ãã³é žïŒ0.45mlïŒãšãïŒâã§æ··åãã次ãã§
9αâã¯ããâ11βïŒ17αâãžããããã·â16βâã¡
ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³ïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒãïŒ7.50ïœïŒ15.34ããª
ã¢ã«ïŒãå ãããåå¿æ··åç©ã40âã§ïŒæé30å
æ¹æãã次ãã§ããã©ããããã©ã³ïŒ17.4mlïŒãš
12.5ïŒ ã¢ã³ã¢ãã¢æ°ŽïŒ43.5mlïŒãšã®æ··åç©ã«ãã
ãã15åéæ¹æããåŸã«è©²æ··åç©ãæ°·ã§å·ããã
æ°Žã«ããããçæç©ãåããæ°ŽæŽãã50âã§ä¹Ÿ
ç¥ããããš6.29ïœã®æšèšååç©ãåŸããæ°·ã§å·ã
ããã¡ã¿ããŒã«ãšã¢ã»ãã³ãšã®æ··åç©ã§æŽæµãã
åŸã«ã¯ãçæç©ã¯æ¬¡ã®åæå€ãæããïŒèç¹238
ã240âãã¯ãããã«ã äžã®æ¯æå 床ïŒ102.72ãã å®æœäŸ ïŒ 9αâã¯ããâ17αâããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ11ïŒ20âããª
ãªã³17âããã¬ãŒãã®è£œé ããªãã«ãªãé ¢é žïŒ3.50mlïŒ45.73ããªã¢ã«ïŒ
ãšç¡æ°Žé ªé žïŒ3.20mlïŒ19.62ããªã¢ã«ïŒãšã¡ã¿ã³
ã¹ã«ãã³é žïŒ0.25mlïŒãš9αâã¯ããâ17αâãã
ããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³
âïŒïŒ11ïŒ20âããªãªã³ïŒ5.00ïœïŒ12.79ããªã¢
ã«ïŒãšãéåžžã®æ§åŒã§40âã§ïŒæéåå¿ãããå
å¿æ··åç©ãæ°Žäžã«æ²æŸ±ãããã¡ã¿ããŒã«ïŒãžã¯ã
ãã¡ã¿ã³ïŒãžã€ãœãããã«ãšãŒãã«ããåçµæ¶ã
ããåŸã«5.27ïœã®æšèšååç©ãåŸããèç¹154ã
ïŒâãã¯ãããã«ã äžã®æ¯æå 床ïŒ198.83ãã å®æœäŸ ïŒ 9αïŒ11βâãžã¯ããâ17αâããããã·â16βâ
ã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãž
ãªã³17âãã¬ã¬ãŒãã®è£œé ç¡æ°Žãã¬ãªã¢ã³é žïŒ4.80mlïŒ23.97ããªã¢ã«ïŒ
ããå·åŽããããªãã«ãªãé ¢é žïŒ4.80mlïŒ62.72
ããªã¢ã«ïŒã«å ããç¶ããŠã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ0.400mlïŒåã³æåŸã«9αïŒ11βâãžã¯ããâ17α
âããããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâ
ãžãšã³âïŒïŒ20âãžãªã³ïŒ7.50ïœïŒ18.23ããªã¢
ã«ïŒãå ããã枩床ã40âã«ææž©ããããã®æ··å
ç©ãïŒæé45åæ¹æã次ãã§æ°·ã§å·åŽããæ°Žã«ç·©
æ ¢ã«ããããããããŠåŸãããåºäœãéããæ°Ž
æŽããæ°Žé žåã«ãªãŠã ã®é å€äžã§ç空也ç¥ããã
ã¡ã¿ããŒã«ããçŽã¡ã«åçµæ¶ããããš6.97ïœã®æš
èšååç©ãåŸããæ¯æ¶²ãæ¿çž®ããããšã«ããå¥é
ã®çæç©ãåŸããããçæç©ã®èç¹ã¯170ãïŒâ
ã§ãããžãªããµã³äžã®æ¯æå 床ã¯ïŒ118.54ãã§ã
ãã å®æœäŸ ïŒ ãã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»ããŒãã®
補é (a) ããªãã«ãªãé ¢é žïŒ31.32mlïŒ0.409ã¢ã«ïŒãš
ç¡æ°Žãã¬ãªã¢ã³é žïŒ41.04mlïŒ0.205ã¢ã«ïŒãšïœ
âãã«ãšã³ã¹ã«ãã³é žïŒ2.70ïœïŒãšãïŒâã§æ··
åãã9αâãã«ãªãâ11βïŒ17αïŒ21âããªã
ãããã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãž
ãšã³âïŒïŒ30âãžãªã³11âããªãã«ãªãã¢ã»ã
ãŒã21âã¢ã»ããŒãïŒ54.00ïœïŒ0.102ã¢ã«ïŒã
次ãã§å ããã枩床ã40âã«ææž©ããããã®æ··
åç©ãïŒæé25åæå¹ã«æ¹æãããæ°·ã§å·åŽã
ã10ïŒ ããªãžã³ãšæ°Žãšã®æ··åç©ã§åŠçããç¶ã
ãŠæ²¹ç¶ã®åºäœãã¡ã¿ããŒã«ã«æº¶è§£ãããæ°·ã§å·
åŽããæ°Žäžã«æ²æŸ±ããããšçµæ¶è³ªã®çæç©ã
åŸããããåããæ°ŽæŽãã50âã§ä¹Ÿç¥ãã
ãããã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã
17âãã¬ã¬ãŒã21âã¢ã»ããŒãã®åéã¯60.10
ïœã§ããããã®çæç©ã¯ã¡ã¿ããŒã«äžã§242ã®
ïŒïŒ ïŒcmïŒ235ã7nïœïŒãæããã (b) 次ãã§ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ã
ãŒã17âãã¬ã¬ãŒã21âã¢ã»ããŒãã次ã®äžè¬
æ³ã«ãããã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒã21âã¢ã»
ããŒãã«è»¢åããåŸãïŒ åæã¹ããã€ããã溶å€ã«å ¥ããéžå®åå¿å€ãš
æ··åããç¹å®ã®æéæäžã®æž©åºŠã§æ¹æãããæ°·ã§
å·ãããæ°Žäžã§æ²æŸ±ãããéããæ°ŽæŽã50âã§
也ç¥ãããããšã«ããçæç©ãåŸãã çš®ã ã®å®éšã®çµæã以äžã®è¡šã«äžããã
ãè¡šã
å®æœäŸ 10
ãã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒãã®è£œé
(a) è±åœç¹èš±ç¬¬2079754å·æ现æžã®å®æœäŸïŒã«ã
ããå®æœäŸ9aã®åŠã調補ãã9αâãã«ãªãâ
11βïŒ17αïŒ21âããªããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã17âãã¬ã¬ãŒã21â
ã¢ã»ããŒãïŒ45.00ïœïŒãšãã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ225mlïŒãšç¡æ°Žã¡ã¿ããŒã«ïŒ135mlïŒãšãã湿
åãæé€ããªãã18âã§45æéæ¹æããã次ã
ã§18âã25âã§23.5æéæ¹æãããããã®æ··å
ç©ãæ°·ã§å·åŽããæ°Žã«ããããæ²æŸ±ããåºäœã
éããæ°Žã§è¯ãæŽæµã50âã§ä¹Ÿç¥ããããš
38.50ïœã®ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»
ããŒã17âãã¬ã¬ãŒããåŸããç±å«æ°Žã¡ã¿ããŒ
ã«ããåçµæ¶ããããšèç¹174ã177âã®åæè©Š
æãåŸãããã (b) 次ãã§ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ã
ãŒã17âãã¬ã¬ãŒãã次ã®äžè¬çæ¹æ³ã«ããã
ã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒãã«è»¢åããåŸãïŒ åæã¹ããã€ãããç¡æ°Žã¡ã¿ããŒã«äžã®éžå®å
å¿å€ãšæ··åããæäžã®æž©åºŠã§ç¹å®ã®æéæ¹æãã
ããæ°·ã§å·ãããæ°Žäžã«æ²æŸ±ãããéããæ°ŽæŽ
ãã50âã§ä¹Ÿç¥ãããããšã«ããçæç©ãåŸãã çš®ã ã®å®éšã®çµæãè¡šã«äžããã
ããå®æœäŸ9aã®åŠã調補ãã9αâãã«ãªãâ
11βïŒ17αïŒ21âããªããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã17âãã¬ã¬ãŒã21â
ã¢ã»ããŒãïŒ45.00ïœïŒãšãã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ225mlïŒãšç¡æ°Žã¡ã¿ããŒã«ïŒ135mlïŒãšãã湿
åãæé€ããªãã18âã§45æéæ¹æããã次ã
ã§18âã25âã§23.5æéæ¹æãããããã®æ··å
ç©ãæ°·ã§å·åŽããæ°Žã«ããããæ²æŸ±ããåºäœã
éããæ°Žã§è¯ãæŽæµã50âã§ä¹Ÿç¥ããããš
38.50ïœã®ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»
ããŒã17âãã¬ã¬ãŒããåŸããç±å«æ°Žã¡ã¿ããŒ
ã«ããåçµæ¶ããããšèç¹174ã177âã®åæè©Š
æãåŸãããã (b) 次ãã§ãã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ã
ãŒã17âãã¬ã¬ãŒãã次ã®äžè¬çæ¹æ³ã«ããã
ã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒãã«è»¢åããåŸãïŒ åæã¹ããã€ãããç¡æ°Žã¡ã¿ããŒã«äžã®éžå®å
å¿å€ãšæ··åããæäžã®æž©åºŠã§ç¹å®ã®æéæ¹æãã
ããæ°·ã§å·ãããæ°Žäžã«æ²æŸ±ãããéããæ°ŽæŽ
ãã50âã§ä¹Ÿç¥ãããããšã«ããçæç©ãåŸãã çš®ã ã®å®éšã®çµæãè¡šã«äžããã
ãè¡šã
å®æœäŸ 11
9αâãã«ãªãâ11βïŒ17αâãžããããã·â21ïŒ
21âãžã€ãªãâ16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒ
âãžãšã³âïŒïŒ20âãžãªã³17âãã¬ã¬ãŒãã®è£œ
é (a) ç¡æ°Žãã¬ãªã¢ã³é žïŒ15.03mlïŒ75.05ããªã¢
ã«ïŒãšããªãã«ãªãé ¢é žïŒ13.20mlïŒ172.48ã
ãªã¢ã«ïŒãšãïŒâã§æ··åãã次ãã§ã¡ã¿ã³ã¹ã«
ãã³é žïŒ1.25mlïŒç¶ããŠ9αâãã«ãªãâ11βïŒ
17αâãžããããã·â21ïŒ21âãžã€ãªãâ16β
âã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20â
ãžãªã³11âããªãã«ãªãã¢ã»ããŒãïŒ25.00
ïœïŒ34.52ããªã¢ã«ïŒãå ãããïŒæéæ¹æåŸ
ã«ãåå¿æ··åç©ã0.025Mçé žâæ°ŽçŽ äºãããª
ãŠã 溶液ã«ç·©æ ¢ã«ããããæ°Žæ§çžãåŸã·ã€ãã
æ®çåã50ïŒ ã¢ã»ãã³ïŒã¡ã¿ããŒã«ã«æº¶è§£ãã
ããçæç©ããæ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ããã
åŸã«ããããéããæ°Žã§ååã«æŽæµãã35â
ã§ä¹Ÿç¥ããããš27.55ïœã®çæç©ãåŸãããã®
äžå®å®ãªçæç©ã®åæè©Šæã¯å°éã®ïœâãã«ãš
ã³ã¹ã«ãã³é žã®ååšäžã«å«æ°Žã¡ã¿ããŒã«ããåŸ
ããããçæç©ã®ãšãŠçŽ å«éã¯28.5ïŒ ã§ãããš
èŠåºãããã (b) åèšçæç©ïŒ3.00ïœïŒãã¡ã¿ããŒã«ïŒ18mlïŒ
ã«æº¶è§£ãããããªãšãã«ã¢ãã³ïŒïŒmlïŒ21.54
ããªã¢ã«ïŒãå ãããã®åŸã«æ··åç©ã宀枩ã§30
åéæ¹æãããæ°·ã§å·åŽããæ°Žäžã§æ²æŸ±ããã
ãšæšèšååç©ãçæãããããéããæ°ŽæŽ
ãã35âã§ä¹Ÿç¥ãããããšãŠçŽ å«éã¯23.7ïŒ ã§
ããããšã瀺ããã å®æœäŸ 12 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒãã®
補é (a) ããªã¯ããé ¢é žïŒ2.60ïœïŒ15.91ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ3.18mlïŒ15.88ããªã¢ã«ïŒ
ãšãïŒâã§æ··åãã次ãã§ïœâãã«ãšã³ã¹ã«ã
ã³é žïŒ250mgïŒãå ããç¶ããŠ9αâãã«ãªãâ
11βïŒ17αâãžããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããª
ãã«ãªãã¢ã»ããŒãïŒ5.00ïœïŒ10.58ããªã¢ã«ïŒ
ãå ããããã®æ··åç©ã40âã«å æž©ãããã®æž©
床ã§ïŒæéç¶æããã宀枩ã«å·åŽåŸã«ãããªãš
ãã«ã¢ãã³ïŒ25mlïŒãå ããæ¹æãæŽã«30åé
æç¶ããããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ããããšåº
äœãåŸããããéããæ°ŽæŽãã50âã§ä¹Ÿç¥ã
ãããã¡ã¿ããŒã«ããåçµæ¶ããããš216ãïŒ
âã®èç¹ãšãžãªããµã³äžã§ïŒ62.17ãã®æ¯æå 床
ãšãæããåæè©ŠæãåŸãããã (b) åèšåå¿ã§ããªãšãã«ã¢ãã³ã§åŠçããã«å
ã«æ°Žäžã«æ²æŸ±ãããæã«ã¯ã21âãã¹ãªãã·ã
ã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17âã
ã¬ã¬ãŒããåŸãããã (c) ç¡æ°Žã¡ã¿ããŒã«ïŒ24mlïŒã«å ¥ãã9αâãã«
ãªãâ11βïŒ17αâãžããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã17âãã¬ã¬ãŒã
ïŒ2.00ïœïŒ3.59ããªã¢ã«ïŒã100ïŒ ããã©ãžã³
ïŒ0.400mlïŒ12.52ããªã¢ã«ïŒã§15åé24âã§åŠ
çãããåå¿æ··åç©ãæ°·ã§å·åŽããæ°Žã«ãã
ããçæç©ãéããæŽæµã也ç¥ããããšèç¹
212ãïŒâã®æšèšååç©1.56ïœãåŸãã å®æœäŸ 13 ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è£œ
é ããªãã«ãªãé ¢é žïŒ2.11mlïŒ27.57ããªã¢ã«ïŒ
ãïŒâã«å·åŽããç¡æ°Žããããªã³é žïŒ2.37mlïŒ
18.39ããªã¢ã«ïŒãå ããç¶ããŠã¡ã¿ã³ã¹ã«ãã³
é žïŒ0.25mlïŒåã³9αâãã«ãªãâ11βïŒ17αïŒ21
âããªããããã·â16αâã¡ãã«ãã¬ã°ãâïŒïŒ
ïŒâãžãšã³âïŒïŒ20âãžãªã³11âããªãã«ãªãã¢
ã»ããŒã21âããããªããŒãïŒ5.00ïœïŒ9.18ããª
ã¢ã«ïŒãå ããã40ã45âã§ïŒæéæ¹æåŸã«ãã
ã®æ··åç©ããžãšãã«ã¢ãã³ã®50ïŒ æ°Žæº¶æ¶²ã«ãã
ããåŸãããçæç©ãéããæŽæµã50âã§ä¹Ÿç¥
ããããšèç¹204ãïŒâã®ãããµã¡ã¿ãŸã³17ïŒ21
âãžããããªããŒã4.10ïœãåŸãããããã®èç¹
ã¯æ°Žæ§ã¡ã¿ããŒã«ããåçµæ¶ããŠãå€åããªãã€
ãã å®æœäŸ 14 ãã¯ãã¡ã¿ãŸã³17âã¢ã»ããŒãã®è£œé åãã€ãŠã¢ã³ã¢ãã¢ã§åŠçããããšãªããå®æœ
äŸïŒã®åå¿æ··åç©ãæ°Žäžã§æ²æŸ±ãããæã«ã¯ãã
ã¯ãã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17ïŒ21
âãžã¢ã»ããŒããåŸãããããããæ现æžã«ç€ºã
ããæ¹æ³ã«ããç¡æ°Žã¡ã¿ããŒã«äžã®ç¡æ°Žã¡ã¿ã³ã¹
ã«ãã³é žãšåå¿ããããšãã¯ãã¡ã¿ãŸã³11âããª
ãã«ãªãã¢ã»ããŒã17âã¢ã»ããŒããåŸãããã
æŽã«ã¢ãã³åŠçãããšãã¯ãã¡ã¿ãŸã³17âã¢ã»ã
ãŒããåŸããã¡ã¿ããŒã«ããåçµæ¶ããããšïŒ
106.58ãã®æ¯æå 床ïŒãžãªããµã³äžïŒãæããå
æè©ŠæãåŸãããã å®æœäŸ 15 ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è£œ
é (a) ããªãã«ãªãé ¢é žïŒ1.20mlïŒ15.68ããªã¢ã«ïŒ
ãïŒâã«å·åŽãããã®æã«ç¡æ°Žããããªã³é ž
ïŒ1.512mlïŒ11.73ããªã¢ã«ïŒãå ããç¶ããŠã¡
ã¿ã³ã¹ã«ãã³é žïŒ0.20mlïŒåã³9αâã¯ããâ
11βïŒ17αïŒ21âããªããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã21âããããªããŒã
ïŒ4.00ïœïŒ7.13ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã80âã«å ç±ãããã®æž©åºŠã§æ¹æããªãã
2.5æéç¶æãããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ãã
ãåŸã«ãçæç©ãéããæ°Žã§ååã«æŽæµãã
50âã§ä¹Ÿç¥ããããš4.02ïœã®ãã¯ãã¡ã¿ãŸã³11
âããªãã«ãªãã¢ã»ããŒã17ïŒ21âãžããããª
ããŒããåŸããã¡ã¿ããŒã«ããåçµæ¶ããããš
èç¹176ãïŒâã®åæçŽåºŠã®è©ŠæãåŸãã (b) 9αâã¯ããâ11βïŒ17αïŒ21âããªãããã
ã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â
ïŒïŒ20âãžãªã³11âããªãã«ãªãã¢ã»ããŒã
17ïŒ21âãžããããªããŒãïŒ3.00ïœïŒ4.86ããª
ã¢ã«ïŒãã¡ã¿ããŒã«ïŒ18mlïŒåã³ãžãªããµã³
ïŒ12mlïŒã«æº¶è§£ããããã®åŸã«ã¢ã«ããªã³
ïŒ0.300mlïŒ3.48ããªã¢ã«ïŒãå ããã25âã§ïŒ
æéæ¹æããåŸã«ãåå¿æ··åç©ã50ïŒ æ°Žæ§é ¢é ž
ã§äžåãããæ°·ã§å·åŽããæ°Žã«æ²æŸ±ããããç
æç©ãéããæ°ŽæŽãã50âã§ä¹Ÿç¥ããããš
2.45ïœã®ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžããããªã
ãŒããåŸããã¢ã»ãã³ããåçµæ¶ãããåŸã«ã
該çæç©ã¯ããã®ç±³åœè¬å±æ¹XXh.p.l.c.æ€å®ãš
åèŽããã å®æœäŸ 16 21âãã¹ãªãã·ãã¯ãã¡ã¿ãŸã³17âãã¬ã¬ãŒã
ã®è£œé (a) ããªãã«ãªãé ¢é žïŒ27.00mlïŒ353ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ13.50mlïŒ67.4ããªã¢ã«ïŒ
ãšã®æ··åç©ãïŒâã§èª¿è£œãããã®åŸã«ïœâãã«
ãšã³ã¹ã«ãã³é žïŒ1.80ïœïŒåã³9αâã¯ããâ
11βïŒ17αâãžããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããª
ãã«ãªãã¢ã»ããŒãïŒ18.00ïœïŒ36.8ããªã¢ã«ïŒ
ãå ããã枩床40âã«ææž©ãããåå¿æ··åç©ã
ïŒæéæ¹æãããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ããã
ãšæ²¹ç¶åºäœãåŸãããã¯ã¡ã¿ããŒã«ãšå ±ã«æ··ã
ãŠæããšæ¶åºãããçæç©ãéãã50âã§ä¹Ÿ
ç¥ããããšèç¹187ã90âã®21âãã¹ãªãã·ã
ã¯ãã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17â
ãã¬ã¬ãŒã17.71ïœãåŸãã (b) 次ãã§åèšã®çæç©ã次ã®ææ³ã«ãã21âã
ã¹ãªãã·ãã¯ãã¡ã¿ãŸã³17âãã¬ã¬ãŒãã«è»¢å
ãããïŒ åèšçæç©ãã溶å€ã«å ¥ããéžå®åå¿å€ãšæ··å
ããç¹å®ã®æéæäžã®æž©åºŠã§æ¹æãããçæç©
ã¯ãæ°·ã§å·åŽããæ°Žã«æ²æŸ±ãããéããæ°ŽæŽ
ãã50âã§ä¹Ÿç¥ãããããšã«ããåŸãããã è¥å¹²ã®å®éšã®çµæã以äžã®è¡šã«äžããã
21âãžã€ãªãâ16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒ
âãžãšã³âïŒïŒ20âãžãªã³17âãã¬ã¬ãŒãã®è£œ
é (a) ç¡æ°Žãã¬ãªã¢ã³é žïŒ15.03mlïŒ75.05ããªã¢
ã«ïŒãšããªãã«ãªãé ¢é žïŒ13.20mlïŒ172.48ã
ãªã¢ã«ïŒãšãïŒâã§æ··åãã次ãã§ã¡ã¿ã³ã¹ã«
ãã³é žïŒ1.25mlïŒç¶ããŠ9αâãã«ãªãâ11βïŒ
17αâãžããããã·â21ïŒ21âãžã€ãªãâ16β
âã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20â
ãžãªã³11âããªãã«ãªãã¢ã»ããŒãïŒ25.00
ïœïŒ34.52ããªã¢ã«ïŒãå ãããïŒæéæ¹æåŸ
ã«ãåå¿æ··åç©ã0.025Mçé žâæ°ŽçŽ äºãããª
ãŠã 溶液ã«ç·©æ ¢ã«ããããæ°Žæ§çžãåŸã·ã€ãã
æ®çåã50ïŒ ã¢ã»ãã³ïŒã¡ã¿ããŒã«ã«æº¶è§£ãã
ããçæç©ããæ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ããã
åŸã«ããããéããæ°Žã§ååã«æŽæµãã35â
ã§ä¹Ÿç¥ããããš27.55ïœã®çæç©ãåŸãããã®
äžå®å®ãªçæç©ã®åæè©Šæã¯å°éã®ïœâãã«ãš
ã³ã¹ã«ãã³é žã®ååšäžã«å«æ°Žã¡ã¿ããŒã«ããåŸ
ããããçæç©ã®ãšãŠçŽ å«éã¯28.5ïŒ ã§ãããš
èŠåºãããã (b) åèšçæç©ïŒ3.00ïœïŒãã¡ã¿ããŒã«ïŒ18mlïŒ
ã«æº¶è§£ãããããªãšãã«ã¢ãã³ïŒïŒmlïŒ21.54
ããªã¢ã«ïŒãå ãããã®åŸã«æ··åç©ã宀枩ã§30
åéæ¹æãããæ°·ã§å·åŽããæ°Žäžã§æ²æŸ±ããã
ãšæšèšååç©ãçæãããããéããæ°ŽæŽ
ãã35âã§ä¹Ÿç¥ãããããšãŠçŽ å«éã¯23.7ïŒ ã§
ããããšã瀺ããã å®æœäŸ 12 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âãã¬ã¬ãŒãã®
補é (a) ããªã¯ããé ¢é žïŒ2.60ïœïŒ15.91ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ3.18mlïŒ15.88ããªã¢ã«ïŒ
ãšãïŒâã§æ··åãã次ãã§ïœâãã«ãšã³ã¹ã«ã
ã³é žïŒ250mgïŒãå ããç¶ããŠ9αâãã«ãªãâ
11βïŒ17αâãžããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããª
ãã«ãªãã¢ã»ããŒãïŒ5.00ïœïŒ10.58ããªã¢ã«ïŒ
ãå ããããã®æ··åç©ã40âã«å æž©ãããã®æž©
床ã§ïŒæéç¶æããã宀枩ã«å·åŽåŸã«ãããªãš
ãã«ã¢ãã³ïŒ25mlïŒãå ããæ¹æãæŽã«30åé
æç¶ããããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ããããšåº
äœãåŸããããéããæ°ŽæŽãã50âã§ä¹Ÿç¥ã
ãããã¡ã¿ããŒã«ããåçµæ¶ããããš216ãïŒ
âã®èç¹ãšãžãªããµã³äžã§ïŒ62.17ãã®æ¯æå 床
ãšãæããåæè©ŠæãåŸãããã (b) åèšåå¿ã§ããªãšãã«ã¢ãã³ã§åŠçããã«å
ã«æ°Žäžã«æ²æŸ±ãããæã«ã¯ã21âãã¹ãªãã·ã
ã¿ã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17âã
ã¬ã¬ãŒããåŸãããã (c) ç¡æ°Žã¡ã¿ããŒã«ïŒ24mlïŒã«å ¥ãã9αâãã«
ãªãâ11βïŒ17αâãžããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã17âãã¬ã¬ãŒã
ïŒ2.00ïœïŒ3.59ããªã¢ã«ïŒã100ïŒ ããã©ãžã³
ïŒ0.400mlïŒ12.52ããªã¢ã«ïŒã§15åé24âã§åŠ
çãããåå¿æ··åç©ãæ°·ã§å·åŽããæ°Žã«ãã
ããçæç©ãéããæŽæµã也ç¥ããããšèç¹
212ãïŒâã®æšèšååç©1.56ïœãåŸãã å®æœäŸ 13 ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è£œ
é ããªãã«ãªãé ¢é žïŒ2.11mlïŒ27.57ããªã¢ã«ïŒ
ãïŒâã«å·åŽããç¡æ°Žããããªã³é žïŒ2.37mlïŒ
18.39ããªã¢ã«ïŒãå ããç¶ããŠã¡ã¿ã³ã¹ã«ãã³
é žïŒ0.25mlïŒåã³9αâãã«ãªãâ11βïŒ17αïŒ21
âããªããããã·â16αâã¡ãã«ãã¬ã°ãâïŒïŒ
ïŒâãžãšã³âïŒïŒ20âãžãªã³11âããªãã«ãªãã¢
ã»ããŒã21âããããªããŒãïŒ5.00ïœïŒ9.18ããª
ã¢ã«ïŒãå ããã40ã45âã§ïŒæéæ¹æåŸã«ãã
ã®æ··åç©ããžãšãã«ã¢ãã³ã®50ïŒ æ°Žæº¶æ¶²ã«ãã
ããåŸãããçæç©ãéããæŽæµã50âã§ä¹Ÿç¥
ããããšèç¹204ãïŒâã®ãããµã¡ã¿ãŸã³17ïŒ21
âãžããããªããŒã4.10ïœãåŸãããããã®èç¹
ã¯æ°Žæ§ã¡ã¿ããŒã«ããåçµæ¶ããŠãå€åããªãã€
ãã å®æœäŸ 14 ãã¯ãã¡ã¿ãŸã³17âã¢ã»ããŒãã®è£œé åãã€ãŠã¢ã³ã¢ãã¢ã§åŠçããããšãªããå®æœ
äŸïŒã®åå¿æ··åç©ãæ°Žäžã§æ²æŸ±ãããæã«ã¯ãã
ã¯ãã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17ïŒ21
âãžã¢ã»ããŒããåŸãããããããæ现æžã«ç€ºã
ããæ¹æ³ã«ããç¡æ°Žã¡ã¿ããŒã«äžã®ç¡æ°Žã¡ã¿ã³ã¹
ã«ãã³é žãšåå¿ããããšãã¯ãã¡ã¿ãŸã³11âããª
ãã«ãªãã¢ã»ããŒã17âã¢ã»ããŒããåŸãããã
æŽã«ã¢ãã³åŠçãããšãã¯ãã¡ã¿ãŸã³17âã¢ã»ã
ãŒããåŸããã¡ã¿ããŒã«ããåçµæ¶ããããšïŒ
106.58ãã®æ¯æå 床ïŒãžãªããµã³äžïŒãæããå
æè©ŠæãåŸãããã å®æœäŸ 15 ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è£œ
é (a) ããªãã«ãªãé ¢é žïŒ1.20mlïŒ15.68ããªã¢ã«ïŒ
ãïŒâã«å·åŽãããã®æã«ç¡æ°Žããããªã³é ž
ïŒ1.512mlïŒ11.73ããªã¢ã«ïŒãå ããç¶ããŠã¡
ã¿ã³ã¹ã«ãã³é žïŒ0.20mlïŒåã³9αâã¯ããâ
11βïŒ17αïŒ21âããªããããã·â16βâã¡ãã«
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã21âããããªããŒã
ïŒ4.00ïœïŒ7.13ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã80âã«å ç±ãããã®æž©åºŠã§æ¹æããªãã
2.5æéç¶æãããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ãã
ãåŸã«ãçæç©ãéããæ°Žã§ååã«æŽæµãã
50âã§ä¹Ÿç¥ããããš4.02ïœã®ãã¯ãã¡ã¿ãŸã³11
âããªãã«ãªãã¢ã»ããŒã17ïŒ21âãžããããª
ããŒããåŸããã¡ã¿ããŒã«ããåçµæ¶ããããš
èç¹176ãïŒâã®åæçŽåºŠã®è©ŠæãåŸãã (b) 9αâã¯ããâ11βïŒ17αïŒ21âããªãããã
ã·â16βâã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³â
ïŒïŒ20âãžãªã³11âããªãã«ãªãã¢ã»ããŒã
17ïŒ21âãžããããªããŒãïŒ3.00ïœïŒ4.86ããª
ã¢ã«ïŒãã¡ã¿ããŒã«ïŒ18mlïŒåã³ãžãªããµã³
ïŒ12mlïŒã«æº¶è§£ããããã®åŸã«ã¢ã«ããªã³
ïŒ0.300mlïŒ3.48ããªã¢ã«ïŒãå ããã25âã§ïŒ
æéæ¹æããåŸã«ãåå¿æ··åç©ã50ïŒ æ°Žæ§é ¢é ž
ã§äžåãããæ°·ã§å·åŽããæ°Žã«æ²æŸ±ããããç
æç©ãéããæ°ŽæŽãã50âã§ä¹Ÿç¥ããããš
2.45ïœã®ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžããããªã
ãŒããåŸããã¢ã»ãã³ããåçµæ¶ãããåŸã«ã
該çæç©ã¯ããã®ç±³åœè¬å±æ¹XXh.p.l.c.æ€å®ãš
åèŽããã å®æœäŸ 16 21âãã¹ãªãã·ãã¯ãã¡ã¿ãŸã³17âãã¬ã¬ãŒã
ã®è£œé (a) ããªãã«ãªãé ¢é žïŒ27.00mlïŒ353ããªã¢ã«ïŒ
ãšç¡æ°Žãã¬ãªã¢ã³é žïŒ13.50mlïŒ67.4ããªã¢ã«ïŒ
ãšã®æ··åç©ãïŒâã§èª¿è£œãããã®åŸã«ïœâãã«
ãšã³ã¹ã«ãã³é žïŒ1.80ïœïŒåã³9αâã¯ããâ
11βïŒ17αâãžããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããª
ãã«ãªãã¢ã»ããŒãïŒ18.00ïœïŒ36.8ããªã¢ã«ïŒ
ãå ããã枩床40âã«ææž©ãããåå¿æ··åç©ã
ïŒæéæ¹æãããæ°·ã§å·åŽããæ°Žã§æ²æŸ±ããã
ãšæ²¹ç¶åºäœãåŸãããã¯ã¡ã¿ããŒã«ãšå ±ã«æ··ã
ãŠæããšæ¶åºãããçæç©ãéãã50âã§ä¹Ÿ
ç¥ããããšèç¹187ã90âã®21âãã¹ãªãã·ã
ã¯ãã¡ã¿ãŸã³11âããªãã«ãªãã¢ã»ããŒã17â
ãã¬ã¬ãŒã17.71ïœãåŸãã (b) 次ãã§åèšã®çæç©ã次ã®ææ³ã«ãã21âã
ã¹ãªãã·ãã¯ãã¡ã¿ãŸã³17âãã¬ã¬ãŒãã«è»¢å
ãããïŒ åèšçæç©ãã溶å€ã«å ¥ããéžå®åå¿å€ãšæ··å
ããç¹å®ã®æéæäžã®æž©åºŠã§æ¹æãããçæç©
ã¯ãæ°·ã§å·åŽããæ°Žã«æ²æŸ±ãããéããæ°ŽæŽ
ãã50âã§ä¹Ÿç¥ãããããšã«ããåŸãããã è¥å¹²ã®å®éšã®çµæã以äžã®è¡šã«äžããã
ãè¡šã
å®æœäŸ 17
ã¯ããã¿ãŸãŒã«17âããããªããŒãã®è£œé
(a) ããªãã«ãªãé
¢é
žïŒ2.23mlïŒ29.14ããªã¢ã«ïŒ
ãšç¡æ°Žããããªã³é žïŒ2.50mlïŒ19.40ããªã¢ã«ïŒ
ãšãïŒâã§æ··åãããã®åŸã«70ïŒ éå¡©çŽ é ž
ïŒ0.272mlïŒãš21âã¯ããâ9αâãã«ãªãâ11βïŒ
17αâãžããããã·â16βâã¡ãã«ãã¬ã°ãâ
ïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããªãã«
ãªãã¢ã»ããŒãïŒ4.90ïœïŒ9.67ããªã¢ã«ïŒãšã
å ããã40ã45âã§ïŒæéæ¹æããæ°·ã§å·åŽã
ãæ°Žäžã«æ²æŸ±ããããšåºäœãåŸããããé
ããæ°Žã§ååã«æŽæµãã50âã§ä¹Ÿç¥ããããç
æç©ã®ã¯ããã¿ãŸãŒã«11âããªãã«ãªãã¢ã»ã
ãŒã17âããããªããŒãã¯ç§€é5.15ïœã§ããã (b) åèš(a)ã§åŸãããçæç©ïŒ4.78ïœïŒãã¡ã¿ã
ãŒã«ïŒ28.7mlïŒã«æžæ¿ãããããªãšãã«ã¢ãã³
ïŒ1.195mlïŒ8.58ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã25âã§30åéæ¹æã次ãã§50ïŒ æ°Žæ§é ¢é žã®
æ·»å ã«ããäžåããããæ²æŸ±åŸã«ãçæç©ã
éããæŽæµãã50âã§ä¹Ÿç¥ããããš3.72ïœã®ç
æç©ãåŸããã¯ããã¿ãŸãŒã«17âããããªããŒ
ãã®åæè©Šæã¯ã¡ã¿ããŒã«ããåçµæ¶ãããã
ãšã«ããåŸããã200âã®èç¹ãšïŒ99.21ãã®æ¯
æå 床ïŒãžãªããµã³äžïŒãšãæããã (c) åèšæ®µé(a)ã§åŸãããçæç©ïŒ100mgïŒ0.18
ããªã¢ã«ïŒãç¡æ°Žã¡ã¿ããŒã«ã«æžæ¿ãããã
100ïŒ ããã©ãžã³ïŒ100ÎŒïŒ3.13ããªã¢ã«ïŒã
å ããåŸã«ããã®æ··åç©ã28âã§15åéæ¹æ
ãã次ãã§æ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ããããç
æç©ã¯åèšæ®µé(b)ã§åŸãããçæç©ãšã¯ããã
ã°ã©ãã€ãŒã«ããåäžã§ããããšã瀺ããã å®æœäŸ 18 ã¯ããã¿ãŸã³17âããã¬ãŒãã®è£œé ç¡æ°Žé ªé žïŒ5.28mlïŒ32.37ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ2.376mlïŒ31.05ããªã¢ã«ïŒãšãïŒâ
ã§æ··åãã次ãã§ã¡ã¿ã³ã¹ã«ãã³é žïŒ0.200mlïŒ
ãšãããã¡ã¿ã³ïŒ20.0mlïŒãš21âã¯ããâ9αâã
ã«ãªãâ17αâããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ11ïŒ20âããªãªã³
ïŒ4.00ïœïŒ9.78ããªã¢ã«ïŒãšãå ãããåå¿æ··å
ç©ã40âã§ïŒæéæ¹æã次ãã§æ°·ã§å·åŽããæ°Žäž
ã«ç·©æ ¢ã«ãããã§æ²¹ç¶ã®åºäœãåŸããããé
ããæ°ŽæŽãã也ç¥ããããš3.71ïœã®çæç©ãåŸ
ããã¡ã¿ããŒã«ããåçµæ¶ããããš184ãïŒâã®
èç¹ãšïŒ127.98ãã®æ¯æå 床ïŒãžãªããµã³äžïŒãš
ãæããåæåäœã®è©ŠæãåŸãããã å®æœäŸ 19 ãã¬ãããŸãã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé (a) ç¡æ°Žãã¬ãªã¢ã³é žïŒ3.50mlïŒ17.48ããªã¢ã«ïŒ
ãïŒâã§ããªãã«ãªãé ¢é žïŒ2.30mlïŒ30.05ã
ãªã¢ã«ïŒãšæ··åãããã®åŸã«ã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ0.25mlïŒãš11βïŒ17αïŒ21âããªããããã·â
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒã
ïŒ5.00ïœïŒ10.03ããªã¢ã«ïŒãšãå ãããåå¿æ··
åç©ã25âã«å æž©ããïŒæéæ¹æããæ°·ã§å·åŽ
ããæ°Žã«ããããšæ²¹ç¶åºäœãåŸãããããã¡ã¿
ããŒã«ã«æº¶è§£ãããæ°Žäžã«æ²æŸ±ããããšåºäœã
åŸããããéããæŽæµãã也ç¥ããããš5.30
ïœã®ãã¬ãããŸãã³11âããªãã«ãªãã¢ã»ããŒ
ã17âãã¬ã¬ãŒã21âã¢ã»ããŒããåŸãã (b) ç¡æ°Žã¡ã¿ããŒã«ïŒ18mlïŒã«å ¥ããåèšçæç©
ïŒ3.00ïœïŒ5.15ããªã¢ã«ïŒã24âã§ïŒæéããª
ãšãã«ã¢ãã³ïŒ2.40mlïŒ17.21ããªã¢ã«ïŒã§åŠ
çãããçæç©ã¯ãæ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ã
ããéããæŽæµãã也ç¥ãããããšã«ããåŸ
ããã秀é2.35ïœã§ãããã¡ã¿ããŒã«äž241ã
3nïœã§279ã®ïŒ¥ïŒïŒ ïŒcmãæããã å®æœäŸ 20 9αâã¯ããâ11βïŒ17αïŒ21âããªããããã·
â16βâã¡ãã«ãã¬ã°ãâïŒâãšã³âïŒïŒ20â
ãžãªã³17ïŒ21âãžããããªããŒãã®è£œé å®æœäŸ15ã«ãããã¯ãã¡ã¿ãŸã³17ïŒ21âãžãã
ããªããŒãã«ã€ããŠäžããããæ¹æ³ã«ããåèšç
æç©ã9αâã¯ããâ11βïŒ17αïŒ21âããªããã
ãã·â16βâã¡ãã«ãã¬ã°ãâïŒâãšã³âïŒïŒ20
âãžãªã³11âããªãã«ãªãã¢ã»ããŒã21âããã
ãªããŒããã補é ããã å®æœäŸ 21 6αâã¡ãã«ãã¬ãããŸãã³17âããã¬ãŒã21
âã¢ã»ããŒãã®è£œé ãã®çæç©ã¯ã6αâã¡ãã«ãã¬ãããŸãã³11
âããªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒããåæ
ãšããŠãå®æœäŸïŒã«ããã21âãã¹ãªãã·ãã¯ã
ã¡ã¿ãŸã³17âããã¬ãŒãã®è£œé ãšåæ§ãªèŠé ã§è£œ
é ãããã å®æœäŸ 22 æ°Žã«æ··åæ§ã®ã¯ãªãŒã çµæç© ã¯ããã¿ãŸãŒã«17âããããªããŒãã®æ°Žã«æ··å
æ§ã®ã¯ãªãŒã ã¯æ¬¡ã®åŠã補é ãåŸãïŒ éšå 次ã®æåãæ··åãã70âã§æº¶èãã ã»ãã¹ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒãã©ããã
ïŒLanetteïŒïŒ¯ãïŒåååïŒ 18.0ïŒ å€§äœ12ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³
ïŒEumulginïŒB1ãïŒåååïŒ 1.5ïŒ å€§äœ20ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³B2ãïŒåå
åïŒ 1.5ïŒ ã«ããªã«é žïŒã«ããªã³é žããªã°ãªã»ãªãïŒãããª
ããŒã«318ãïŒ 10.0ïŒ éšå 宀枩ã§æ¬¡ã®æåãæžæ¿ãããïŒ ã¯ããã¿ãŸãŒã«17âããããªããŒã
0.05ïŒ ã®ã¯ããã¿ãŸãŒã«ã«åœé ã°ãªã»ããŒã« 5.0ïŒ ãããããŒã«ãã«ç²ç ããã éšå ïŒåèžçããæ°Ž63.65ïŒ ã«ïŒâããããã·å®æ¯
éŠé žã¡ãã«0.3ïŒ ã沞ç¹ã§æº¶è§£ãããã70âã«å·
åŽãå¿ èŠãªãã°å®¹éã調ç¯ãããéšåã®1/3ã
æ¹æããªãã70âã§éšåã«å ãã次ãã§éšå
ãå ããç¶ããŠ70âã§éšåã®æ®ããå ãããã
ã®æ··åç©ãæ¹æããªããåŸã ã«å·åŽãããã®æã«
ãŒãªãŒã¯çŽ55âã§ç¡¬åãå§ãããæ¹æã宀枩ãŸã§
æç¶ãããŠè¯å¥œãªå質æ§ã確ä¿ãããPHã¯5.0ã
5.3ã§ããã å®æœäŸ 23 ããŒã·ãšã³çµæç© ïŒïŒ11âãžã¯ããâ17αâããããã·â16βâ
ã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãª
ã³17âãã¬ã¬ãŒãã®ããŒã·ãšã³çµæç©ã¯æ¬¡ã®åŠã
補é ãåŸãïŒ éšå 次ã®æåãæ··åã70âã§æº¶èããïŒ ã»ãã¹ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒãã©ããããïŒ
0.65ïŒ ãšãã¬ã³ã°ãªã³ãŒã«ã¹ãã¢ã¬ãŒãïŒãã¯ãã
ïŒCutinaïŒAGSïŒåååïŒ 0.65ïŒ å€§äœ20ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³B2ãïŒ
0.93ïŒ æµåãã©ãã€ã³ 1.95ïŒ éšå 宀枩ã§æ¬¡ã®æåãæžæ¿ãããïŒ ïŒïŒ10âãžã¯ããâ17αâããããã·â16βâã¡
ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³ïŒïŒ20âãžãªã³17
âãã¬ã¬ãŒã 芪ã¹ããã€ãã®0.1ïŒ ã«åœé ã°ãªã»ããŒã«B.P. 2.50ïŒ ãããã³âïŒâãªãŒã« 6.50ïŒ ãããããŒã«ãã«ç²ç ããã éšå ã°ãªã»ããŒã«B.P.2.50ïŒ ãšåèžçæ°Ž84.05ïŒ ãšã«
ïŒâããããã·å®æ¯éŠé žã¡ãã«0.15ïŒ ã沞ç¹ã§æº¶
解ãããã 70âã«å·åŽããå¿ èŠãªãã°å®¹éã調ç¯ããã éšåãæ¹æããªãã70âã§éšåã«å ãã次
ãã§éšåãå ããããã®æ··åç©ãæå¹ã«æ¹æã
ãªããå·åŽãŠå質æ§ã確ä¿ããã å®æœäŸ 24 è»èçµæç© ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è»
èã次ã®åŠã補é ãåŸãïŒ åºäœã¯ã»ãªã³ 91.8ïŒ æµåãã©ãã€ã³ 8.1ïŒ ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒã
ãããµã¡ã¿ãŸã³ã®0.1ïŒ ã«åœé ã¯ã»ãªã³ã溶èããæå¹ã«æ¹æããªãã50âã«
ç¶æãããã®éã«æµåãã©ãã€ã³ã«æžæ¿ãããã
ããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®ããŒã«
ãã«ç²ç æžæ¿ç©ãå ããããã®æ··åç©ãæªã ç±ã
ãŠæ¶²äœã§ããéã«ç®¡äœã«å å¡«ããã å®æœäŸ 25 çµå£åžå ¥åŽé§æ¶²çµæç© ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãã®åŽé§æ¶²
çµæç©ã¯æ¬¡ã®åŠã補é ãåŸãïŒ ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãïŒåŸ®ç²ã«ã
ãïŒ 12.06mg ãªããŒã«é ž 10.00mg ãã«ãªãããªã¯ããã¡ã¿ã³ 9990.00mg ãžã¯ãããžãã«ãªãã¡ã¿ã³ 15000.00mg ãªããŒã«é žãå·åŽãã«ãªãããªã¯ããã¡ã¿ã³ãš
æå¹ã«æ··åãã次ãã§åŸ®ç²ç¶ã¹ããã€ããå ã
ããå®å šã«åäžãªæ··åç©ãåŸããããŸã§æ··åãæ
ç¶ããããèžçºãããã«ãªãããªã¯ããã¡ã¿ã³ã¯
å¿ èŠã«å¿ããŠè£å ããªããã°ãªããªããåã ã®åž
å ¥åšã«æèŠéã®åŽé§æ¶²ãå å¡«ãããã®åŸã«åŒãå
ä»ããæèŠã®ãžã¯ãããžãã«ãªãã¡ã¿ã³ããã³ã
ã§éå ¥ããã å®æœäŸ 26 çèå 泚å°æ¶²çµæç© 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒ
ãã®çèå 泚å°æ¶²çµæç©ã次ã®åŠã補é ãåŸãïŒ 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒã
1.298ïœ è¡éº»æ²¹ 100ml æ» è埮ç²ç¶ã¹ããã€ããæ» èè¡éº»æ²¹ãšæå¹ã«æ··
åããŠåäžãªæ··åç©ã確ä¿ãããåã ã®ã¢ã³ãã«
ã«ïŒmlã®æ³šå°æ¶²ãå å¡«ããã
ãšç¡æ°Žããããªã³é žïŒ2.50mlïŒ19.40ããªã¢ã«ïŒ
ãšãïŒâã§æ··åãããã®åŸã«70ïŒ éå¡©çŽ é ž
ïŒ0.272mlïŒãš21âã¯ããâ9αâãã«ãªãâ11βïŒ
17αâãžããããã·â16βâã¡ãã«ãã¬ã°ãâ
ïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11âããªãã«
ãªãã¢ã»ããŒãïŒ4.90ïœïŒ9.67ããªã¢ã«ïŒãšã
å ããã40ã45âã§ïŒæéæ¹æããæ°·ã§å·åŽã
ãæ°Žäžã«æ²æŸ±ããããšåºäœãåŸããããé
ããæ°Žã§ååã«æŽæµãã50âã§ä¹Ÿç¥ããããç
æç©ã®ã¯ããã¿ãŸãŒã«11âããªãã«ãªãã¢ã»ã
ãŒã17âããããªããŒãã¯ç§€é5.15ïœã§ããã (b) åèš(a)ã§åŸãããçæç©ïŒ4.78ïœïŒãã¡ã¿ã
ãŒã«ïŒ28.7mlïŒã«æžæ¿ãããããªãšãã«ã¢ãã³
ïŒ1.195mlïŒ8.58ããªã¢ã«ïŒãå ããããã®æ··å
ç©ã25âã§30åéæ¹æã次ãã§50ïŒ æ°Žæ§é ¢é žã®
æ·»å ã«ããäžåããããæ²æŸ±åŸã«ãçæç©ã
éããæŽæµãã50âã§ä¹Ÿç¥ããããš3.72ïœã®ç
æç©ãåŸããã¯ããã¿ãŸãŒã«17âããããªããŒ
ãã®åæè©Šæã¯ã¡ã¿ããŒã«ããåçµæ¶ãããã
ãšã«ããåŸããã200âã®èç¹ãšïŒ99.21ãã®æ¯
æå 床ïŒãžãªããµã³äžïŒãšãæããã (c) åèšæ®µé(a)ã§åŸãããçæç©ïŒ100mgïŒ0.18
ããªã¢ã«ïŒãç¡æ°Žã¡ã¿ããŒã«ã«æžæ¿ãããã
100ïŒ ããã©ãžã³ïŒ100ÎŒïŒ3.13ããªã¢ã«ïŒã
å ããåŸã«ããã®æ··åç©ã28âã§15åéæ¹æ
ãã次ãã§æ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ããããç
æç©ã¯åèšæ®µé(b)ã§åŸãããçæç©ãšã¯ããã
ã°ã©ãã€ãŒã«ããåäžã§ããããšã瀺ããã å®æœäŸ 18 ã¯ããã¿ãŸã³17âããã¬ãŒãã®è£œé ç¡æ°Žé ªé žïŒ5.28mlïŒ32.37ããªã¢ã«ïŒãšããªã
ã«ãªãé ¢é žïŒ2.376mlïŒ31.05ããªã¢ã«ïŒãšãïŒâ
ã§æ··åãã次ãã§ã¡ã¿ã³ã¹ã«ãã³é žïŒ0.200mlïŒ
ãšãããã¡ã¿ã³ïŒ20.0mlïŒãš21âã¯ããâ9αâã
ã«ãªãâ17αâããããã·â16βâã¡ãã«ãã¬ã°
ãâïŒïŒïŒâãžãšã³âïŒïŒ11ïŒ20âããªãªã³
ïŒ4.00ïœïŒ9.78ããªã¢ã«ïŒãšãå ãããåå¿æ··å
ç©ã40âã§ïŒæéæ¹æã次ãã§æ°·ã§å·åŽããæ°Žäž
ã«ç·©æ ¢ã«ãããã§æ²¹ç¶ã®åºäœãåŸããããé
ããæ°ŽæŽãã也ç¥ããããš3.71ïœã®çæç©ãåŸ
ããã¡ã¿ããŒã«ããåçµæ¶ããããš184ãïŒâã®
èç¹ãšïŒ127.98ãã®æ¯æå 床ïŒãžãªããµã³äžïŒãš
ãæããåæåäœã®è©ŠæãåŸãããã å®æœäŸ 19 ãã¬ãããŸãã³17âãã¬ã¬ãŒã21âã¢ã»ããŒã
ã®è£œé (a) ç¡æ°Žãã¬ãªã¢ã³é žïŒ3.50mlïŒ17.48ããªã¢ã«ïŒ
ãïŒâã§ããªãã«ãªãé ¢é žïŒ2.30mlïŒ30.05ã
ãªã¢ã«ïŒãšæ··åãããã®åŸã«ã¡ã¿ã³ã¹ã«ãã³é ž
ïŒ0.25mlïŒãš11βïŒ17αïŒ21âããªããããã·â
ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãªã³11
âããªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒã
ïŒ5.00ïœïŒ10.03ããªã¢ã«ïŒãšãå ãããåå¿æ··
åç©ã25âã«å æž©ããïŒæéæ¹æããæ°·ã§å·åŽ
ããæ°Žã«ããããšæ²¹ç¶åºäœãåŸãããããã¡ã¿
ããŒã«ã«æº¶è§£ãããæ°Žäžã«æ²æŸ±ããããšåºäœã
åŸããããéããæŽæµãã也ç¥ããããš5.30
ïœã®ãã¬ãããŸãã³11âããªãã«ãªãã¢ã»ããŒ
ã17âãã¬ã¬ãŒã21âã¢ã»ããŒããåŸãã (b) ç¡æ°Žã¡ã¿ããŒã«ïŒ18mlïŒã«å ¥ããåèšçæç©
ïŒ3.00ïœïŒ5.15ããªã¢ã«ïŒã24âã§ïŒæéããª
ãšãã«ã¢ãã³ïŒ2.40mlïŒ17.21ããªã¢ã«ïŒã§åŠ
çãããçæç©ã¯ãæ°·ã§å·åŽããæ°Žäžã«æ²æŸ±ã
ããéããæŽæµãã也ç¥ãããããšã«ããåŸ
ããã秀é2.35ïœã§ãããã¡ã¿ããŒã«äž241ã
3nïœã§279ã®ïŒ¥ïŒïŒ ïŒcmãæããã å®æœäŸ 20 9αâã¯ããâ11βïŒ17αïŒ21âããªããããã·
â16βâã¡ãã«ãã¬ã°ãâïŒâãšã³âïŒïŒ20â
ãžãªã³17ïŒ21âãžããããªããŒãã®è£œé å®æœäŸ15ã«ãããã¯ãã¡ã¿ãŸã³17ïŒ21âãžãã
ããªããŒãã«ã€ããŠäžããããæ¹æ³ã«ããåèšç
æç©ã9αâã¯ããâ11βïŒ17αïŒ21âããªããã
ãã·â16βâã¡ãã«ãã¬ã°ãâïŒâãšã³âïŒïŒ20
âãžãªã³11âããªãã«ãªãã¢ã»ããŒã21âããã
ãªããŒããã補é ããã å®æœäŸ 21 6αâã¡ãã«ãã¬ãããŸãã³17âããã¬ãŒã21
âã¢ã»ããŒãã®è£œé ãã®çæç©ã¯ã6αâã¡ãã«ãã¬ãããŸãã³11
âããªãã«ãªãã¢ã»ããŒã21âã¢ã»ããŒããåæ
ãšããŠãå®æœäŸïŒã«ããã21âãã¹ãªãã·ãã¯ã
ã¡ã¿ãŸã³17âããã¬ãŒãã®è£œé ãšåæ§ãªèŠé ã§è£œ
é ãããã å®æœäŸ 22 æ°Žã«æ··åæ§ã®ã¯ãªãŒã çµæç© ã¯ããã¿ãŸãŒã«17âããããªããŒãã®æ°Žã«æ··å
æ§ã®ã¯ãªãŒã ã¯æ¬¡ã®åŠã補é ãåŸãïŒ éšå 次ã®æåãæ··åãã70âã§æº¶èãã ã»ãã¹ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒãã©ããã
ïŒLanetteïŒïŒ¯ãïŒåååïŒ 18.0ïŒ å€§äœ12ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³
ïŒEumulginïŒB1ãïŒåååïŒ 1.5ïŒ å€§äœ20ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³B2ãïŒåå
åïŒ 1.5ïŒ ã«ããªã«é žïŒã«ããªã³é žããªã°ãªã»ãªãïŒãããª
ããŒã«318ãïŒ 10.0ïŒ éšå 宀枩ã§æ¬¡ã®æåãæžæ¿ãããïŒ ã¯ããã¿ãŸãŒã«17âããããªããŒã
0.05ïŒ ã®ã¯ããã¿ãŸãŒã«ã«åœé ã°ãªã»ããŒã« 5.0ïŒ ãããããŒã«ãã«ç²ç ããã éšå ïŒåèžçããæ°Ž63.65ïŒ ã«ïŒâããããã·å®æ¯
éŠé žã¡ãã«0.3ïŒ ã沞ç¹ã§æº¶è§£ãããã70âã«å·
åŽãå¿ èŠãªãã°å®¹éã調ç¯ãããéšåã®1/3ã
æ¹æããªãã70âã§éšåã«å ãã次ãã§éšå
ãå ããç¶ããŠ70âã§éšåã®æ®ããå ãããã
ã®æ··åç©ãæ¹æããªããåŸã ã«å·åŽãããã®æã«
ãŒãªãŒã¯çŽ55âã§ç¡¬åãå§ãããæ¹æã宀枩ãŸã§
æç¶ãããŠè¯å¥œãªå質æ§ã確ä¿ãããPHã¯5.0ã
5.3ã§ããã å®æœäŸ 23 ããŒã·ãšã³çµæç© ïŒïŒ11âãžã¯ããâ17αâããããã·â16βâ
ã¡ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³âïŒïŒ20âãžãª
ã³17âãã¬ã¬ãŒãã®ããŒã·ãšã³çµæç©ã¯æ¬¡ã®åŠã
補é ãåŸãïŒ éšå 次ã®æåãæ··åã70âã§æº¶èããïŒ ã»ãã¹ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒãã©ããããïŒ
0.65ïŒ ãšãã¬ã³ã°ãªã³ãŒã«ã¹ãã¢ã¬ãŒãïŒãã¯ãã
ïŒCutinaïŒAGSïŒåååïŒ 0.65ïŒ å€§äœ20ã¢ã«ã®ãšãã¬ã³ãªãã·ããå«æããã»ãã¹
ãã¢ãªã«ã¢ã«ã³ãŒã«ïŒããšãŠã ã«ãžã³B2ãïŒ
0.93ïŒ æµåãã©ãã€ã³ 1.95ïŒ éšå 宀枩ã§æ¬¡ã®æåãæžæ¿ãããïŒ ïŒïŒ10âãžã¯ããâ17αâããããã·â16βâã¡
ãã«ãã¬ã°ãâïŒïŒïŒâãžãšã³ïŒïŒ20âãžãªã³17
âãã¬ã¬ãŒã 芪ã¹ããã€ãã®0.1ïŒ ã«åœé ã°ãªã»ããŒã«B.P. 2.50ïŒ ãããã³âïŒâãªãŒã« 6.50ïŒ ãããããŒã«ãã«ç²ç ããã éšå ã°ãªã»ããŒã«B.P.2.50ïŒ ãšåèžçæ°Ž84.05ïŒ ãšã«
ïŒâããããã·å®æ¯éŠé žã¡ãã«0.15ïŒ ã沞ç¹ã§æº¶
解ãããã 70âã«å·åŽããå¿ èŠãªãã°å®¹éã調ç¯ããã éšåãæ¹æããªãã70âã§éšåã«å ãã次
ãã§éšåãå ããããã®æ··åç©ãæå¹ã«æ¹æã
ãªããå·åŽãŠå質æ§ã確ä¿ããã å®æœäŸ 24 è»èçµæç© ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®è»
èã次ã®åŠã補é ãåŸãïŒ åºäœã¯ã»ãªã³ 91.8ïŒ æµåãã©ãã€ã³ 8.1ïŒ ãããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒã
ãããµã¡ã¿ãŸã³ã®0.1ïŒ ã«åœé ã¯ã»ãªã³ã溶èããæå¹ã«æ¹æããªãã50âã«
ç¶æãããã®éã«æµåãã©ãã€ã³ã«æžæ¿ãããã
ããµã¡ã¿ãŸã³17ïŒ21âãžããããªããŒãã®ããŒã«
ãã«ç²ç æžæ¿ç©ãå ããããã®æ··åç©ãæªã ç±ã
ãŠæ¶²äœã§ããéã«ç®¡äœã«å å¡«ããã å®æœäŸ 25 çµå£åžå ¥åŽé§æ¶²çµæç© ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãã®åŽé§æ¶²
çµæç©ã¯æ¬¡ã®åŠã補é ãåŸãïŒ ãã¯ãã¡ã¿ãŸã³17ïŒ21âãžã¢ã»ããŒãïŒåŸ®ç²ã«ã
ãïŒ 12.06mg ãªããŒã«é ž 10.00mg ãã«ãªãããªã¯ããã¡ã¿ã³ 9990.00mg ãžã¯ãããžãã«ãªãã¡ã¿ã³ 15000.00mg ãªããŒã«é žãå·åŽãã«ãªãããªã¯ããã¡ã¿ã³ãš
æå¹ã«æ··åãã次ãã§åŸ®ç²ç¶ã¹ããã€ããå ã
ããå®å šã«åäžãªæ··åç©ãåŸããããŸã§æ··åãæ
ç¶ããããèžçºãããã«ãªãããªã¯ããã¡ã¿ã³ã¯
å¿ èŠã«å¿ããŠè£å ããªããã°ãªããªããåã ã®åž
å ¥åšã«æèŠéã®åŽé§æ¶²ãå å¡«ãããã®åŸã«åŒãå
ä»ããæèŠã®ãžã¯ãããžãã«ãªãã¡ã¿ã³ããã³ã
ã§éå ¥ããã å®æœäŸ 26 çèå 泚å°æ¶²çµæç© 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒ
ãã®çèå 泚å°æ¶²çµæç©ã次ã®åŠã補é ãåŸãïŒ 21âãã¹ãªãã·ãã¿ã¡ã¿ãŸã³17âããã¿ããšãŒã
1.298ïœ è¡éº»æ²¹ 100ml æ» è埮ç²ç¶ã¹ããã€ããæ» èè¡éº»æ²¹ãšæå¹ã«æ··
åããŠåäžãªæ··åç©ã確ä¿ãããåã ã®ã¢ã³ãã«
ã«ïŒmlã®æ³šå°æ¶²ãå å¡«ããã
Claims (1)
- ãç¹èš±è«æ±ã®ç¯å²ã ïŒ æ¬¡åŒ ïŒåŒäžïŒžãR1ãR2åã³R3ã¯åŸèšã®æ矩ãæãïŒ
R5ã¯ããããã·ã«åºåã¯R6ã§ãããR6ã¯åŸèšã®
æ矩ãæããïŒã®ååç©ã®17äœã®ã¿åã¯åèšåŒ
ïŒïŒäžã®R5ãããããã·ã«åºã§ããå Žåã«ã¯17
äœåã³21äœããšã¹ãã«åããããšãããªãããã®
éãšã¹ãã«åã¯17äœã«åã¯17äœãš21äœã«å°å ¥ãã¹
ãåºãå«ãã«ã«ãã³é žã®ç¡æ°Žç©ãããªããé ¢é žãš
ïœâãã«ãšã³ã¹ã«ãã³é žãã¡ã¿ã³ã¹ã«ãã³é žãã
ã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é žåã³å¡©é žããéžãã
äžçš®ã®é žãšãããªãäžå¯Ÿã®åŒ·é žãšãšãã«çšããŠè¡
ãªãããšãç¹åŸŽãšãã次åŒïŒ ïœåŒäžâŠã¯äºéçµåãååšãåŸãããšãè¡šããïŒ
ã¯æ°ŽçŽ ãããçŽ åã¯å¡©çŽ ã§ããïŒR1ã¯æ°ŽçŽ ã
ããçŽ ãå¡©çŽ åã¯ã¡ãã«åºã§ãããã€R1ã¯Î±äœ
åã¯Î²äœã«ååšãåŸããã®ã§ããïŒR2ã¯ããã²
ã³ããªããœåã¯ããªããã¢ã»ããã·ïŒãããããª
ããã¢ã»ãã«åºã¯ããããã·ã«ä¿è·åºã§ããïŒåº
ã§ããïŒR3ã¯æ°ŽçŽ ãαâã¡ãã«åã¯Î²âã¡ãã«
åºã§ããïŒR4ã¯åŒRCOïŒãããã¯(i)ïŒã16åã®
ççŽ ååãæããçŽéãåå²éåã¯ç°åŒã¢ã«ãã«
åºã(ii)ïŒãïŒåã®ççŽ ååãæããã¢ã©ã«ãã«åº
åã¯(iii)ããšãã«åºã§ããïŒã®ã¢ã·ã«åºã§ããïŒ
R6ã¯æ°ŽçŽ ãïŒååã¯ïŒåã®ããã²ã³çœ®æåºåã¯
OR7ããããR7ã¯åŒRâ²COïŒåŒäžRâ²ã¯ïŒ²ãšåäžã§ã
ç°ãªã€ãŠãããã(i)ïŒã16åã®ççŽ ååãæãã
çŽéãåå²éåã¯ç°åŒã¢ã«ãã«åºã(ii)ïŒãïŒåã®
ççŽ ååãæããã¢ã©ã«ãã«åºåã¯(iii)ããšãã«åº
ã§ããïŒã®ã¢ã·ã«åºã§ãããã§ããïœã®ã³ã«ãã³
ã¹ããã€ããšã¹ãã«ã®è£œé æ³ã ïŒ ããªããã¢ã»ããã·åºãããªãã«ãªãã¢ã»ã
ãã·åºã§ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ ãšã¹ãã«åãããã¹ãåæã¹ããã€ãïŒã¢ã«
åœãå°ãªããšã1.5ã¢ã«ã®ã«ã«ãã³é žç¡æ°Žç©ãçš
ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ ããªããé ¢é žãããªãã«ãªã«é ¢é žåã¯ããªã¯
ãã«é ¢é žã§ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹
æ³ã ïŒ ãšã¹ãã«åãããã¹ãã¹ããã€ãïŒã¢ã«åœã
å°ãªããšã1.5ã¢ã«ã®ããªããé ¢é žãçšããã€äž
察ã®åŒ·é žã®ãã¡ã®ç¬¬äºã®é žã¯å°ãªããšã觊åªéã§
ååšãããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ ãšã¹ãã«åã¯ïŒâã80âã®ç¯å²ã®æž©åºŠã§è¡ãª
ãç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ ãšã¹ãã«åã¯20âã60âã®ç¯å²ã®æž©åºŠã§è¡ãª
ãç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ ãšã¹ãã«åã¯åå¿å®äºãŸã§ïŒã24æéè¡ãªã
ç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒ æ¬¡åŒïŒ ïŒåŒäžããR1åã³R3ã¯åŸèšã®æ矩ãæãïŒR5
ã¯ããããã·ã«åºåã¯R6ã§ãããR6ã¯åŸèšã®æ
矩ãæããïŒã®ååç©ã®17äœã®ã¿åã¯åèšåŒ
ïŒâ²ïŒäžã®R5ãããããã·ã«åºã§ããå Žåã«ã¯
17äœåã³21äœããšã¹ãã«åããŠæ¬¡åŒïŒ ïœåŒäžâŠã¯äºéçµåãååšãåŸãããšãè¡šããïŒ
ã¯æ°ŽçŽ ãããçŽ åã¯å¡©çŽ ã§ããïŒR1ã¯æ°ŽçŽ ã
ããçŽ ãå¡©çŽ åã¯ã¡ãã«åºã§ãããã€R1ã¯Î±äœ
åã¯Î²äœã«ååšãåŸããã®ã§ããïŒR3ã¯æ°ŽçŽ ã
αâã¡ãã«åã¯Î²âã¡ãã«åºã§ããïŒR4ã¯åŒ
RCOïŒãããã¯(i)ïŒã16åã®ççŽ ååãæãã
çŽéãåå²éåã¯ç°åŒã¢ã«ãã«åºã(ii)ïŒãïŒåã®
ççŽ ååãæããã¢ã©ã«ãã«åºåã¯(iii)ããšãã«åº
ã§ããïŒã®ã¢ã·ã«åºã§ããïŒR6ã¯æ°ŽçŽ ãïŒåå
ã¯ïŒåã®ããã²ã³çœ®æåºåã¯OR7ããããR7ã¯åŒ
Râ²COïŒåŒäžRâ²ã¯ïŒ²ãšåäžã§ãç°ãªã€ãŠãããã
(i)ïŒã16åã®ççŽ ååãæããçŽéãåå²éåã¯
ç°åŒã¢ã«ãã«åºã(ii)ïŒãïŒåã®ççŽ ååãæãã
ã¢ã©ã«ãã«åºåã¯(iii)ããšãã«åºã§ããïŒã®ã¢ã·ã«
åºã§ãããã§ããïœã®ã³ã«ãã³ã¹ããã€ããšã¹ã
ã«ã圢æããããã®éãšã¹ãã«åã¯17äœã«åã¯17
äœãš21äœã«å°å ¥ãã¹ãåºãå«ãã«ã«ãã³é žã®ç¡æ°Ž
ç©ãããªããé ¢é žãšïœâãã«ãšã³ã¹ã«ãã³é žãã¡
ã¿ã³ã¹ã«ãã³é žããã³ãŒã³ã¹ã«ãã³é žãéå¡©çŽ é ž
åã³å¡©é žããéžãã äžçš®ã®é žãšãããªãäžå¯Ÿã®åŒ·
é žãšãšãã«çšããŠè¡ãªããã®ãšãïŒã€ãã§ãã圢
æãããåŒïŒâ²ïŒã®ååç©ããäœçŽã¢ã«ã³ãŒã«
ã®ååšäžã«ãçªçŽ ååãè³éŠæç°ã®äžéšãæ§æã
ãææ©ã¢ãã³ä»¥å€ã®ææ©ã¢ãã³ãç¡æ°Žæº¶å€äžã«æº¶
解ãããç¡æ°Žã¢ã³ã¢ãã¢ã¬ã¹ãæ°Žé žåã¢ã³ã¢ããŠ
ã åã¯ããã©ãžã³ãšåå¿ãããŠ11âããªããã¢ã»
ãã«ä¿è·åºãè±é¢ããããããšãããªã次åŒïŒ ïŒåŒäžãâŠããR1ãR3ãR4åã³R6ã¯åèšã®æ
矩ãæããïŒã®ã³ã«ãã³ã¹ããã€ããšã¹ãã«ã®è£œ
é æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ã«äœ¿çš
ããææ©ã¢ãã³ã第ïŒçŽã¢ãã³ã§ããç¹èš±è«æ±ã®
ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒïŒ ã¢ãã³ããšãã«ã¢ãã³ãã·ã¯ãããã·ã«ã¢
ãã³ãã€ãœãããã«ã¢ãã³ãïœâããã«ã¢ãã³ã
ãã³ãžã«ã¢ãã³åã¯ãšã¿ããŒã«ã¢ãã³ã§ããç¹èš±
è«æ±ã®ç¯å²ç¬¬ïŒïŒé èšèŒã®æ¹æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ã«äœ¿çš
ããææ©ã¢ãã³ã第ïŒçŽã¢ãã³ã§ããç¹èš±è«æ±ã®
ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒïŒ ã¢ãã³ããžãšãã«ã¢ãã³ããžããšãã«ã¢ã
ã³ãã¢ã«ããªã³ããããªãžã³åã¯ãããªãžã³ã§ã
ãç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒïŒé èšèŒã®æ¹æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ã«äœ¿çš
ããææ©ã¢ãã³ã第ïŒçŽã¢ãã³ã§ããç¹èš±è«æ±ã®
ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒïŒ ã¢ãã³ãããªãšãã«ã¢ãã³åã¯ããªãšã¿ã
ãŒã«ã¢ãã³ã§ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒïŒé èšèŒã®
æ¹æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ã«äœ¿çš
ããç¡æ°Žã¢ã³ã¢ãã¢ã¬ã¹ã¯ç¡æ°ŽäœçŽã¢ã«ã³ãŒã«äž
ã«æº¶è§£ããããã®ã§ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èš
èŒã®æ¹æ³ã ïŒïŒ äœçŽã¢ã«ã³ãŒã«ãã¡ã¿ããŒã«åã¯ãšã¿ããŒ
ã«ã§ããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒïŒé èšèŒã®æ¹æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ã«äœ¿çš
ããææ©ã¢ãã³ãç¡æ°Žã¢ã³ã¢ãã¢ã¬ã¹ãæ°Žé žåã¢
ã³ã¢ããŠã 溶液åã¯ããã©ãžã³ã¯è§ŠåªéããååŠ
éè«éããããããã«éå°ã§ããéãŸã§ã®ç¯å²ã§
䜿çšããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé ãªãã第ïŒïŒé ã®
ããããã«èšèŒã®æ¹æ³ã ïŒïŒ 11âããªããã¢ã»ãã«ä¿è·åºã®è±é¢ãâ20
âãªããåå¿åªè³ªã®éæµæž©åºŠãŸã§ã®æž©åºŠã§è¡ãªã
ç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé èšèŒã®æ¹æ³ã ïŒïŒ åå¿æž©åºŠã10âã25âã§ããç¹èš±è«æ±ã®ç¯
å²ç¬¬ïŒïŒé èšèŒã®æ¹æ³ã
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PT73479 | 1981-08-04 | ||
PT7347981A PT73479B (en) | 1981-08-04 | 1981-08-04 | Process for a selective remotion of trihaloacetates of corticosteroids |
PT73864 | 1981-10-22 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS5869899A JPS5869899A (ja) | 1983-04-26 |
JPS6411039B2 true JPS6411039B2 (ja) | 1989-02-23 |
Family
ID=20082958
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP13528582A Granted JPS5869899A (ja) | 1981-08-04 | 1982-08-04 | ã³ã«ãã³ã¹ããã€ãã»ãšã¹ãã«ã®è£œé æ³ |
Country Status (3)
Country | Link |
---|---|
JP (1) | JPS5869899A (ja) |
PT (1) | PT73479B (ja) |
ZA (1) | ZA825551B (ja) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP7106773B1 (ja) * | 2022-01-25 | 2022-07-26 | åä»å»è¬åå·¥æ ªåŒäŒç€Ÿ | ã¹ããã€ãïŒïŒÎ±ïŒïŒïŒïŒãžãšã¹ãã«é¡ã®è£œé æ¹æ³ |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA751599B (en) * | 1974-03-27 | 1976-02-25 | Plurichemie Anstalt | 16-methyl-9alpha-halo steroid esters, ethers and preparation thereof |
-
1981
- 1981-08-04 PT PT7347981A patent/PT73479B/pt unknown
-
1982
- 1982-08-02 ZA ZA825551A patent/ZA825551B/xx unknown
- 1982-08-04 JP JP13528582A patent/JPS5869899A/ja active Granted
Also Published As
Publication number | Publication date |
---|---|
ZA825551B (en) | 1983-06-29 |
JPS5869899A (ja) | 1983-04-26 |
PT73479A (en) | 1981-09-01 |
PT73479B (en) | 1982-10-22 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US4267173A (en) | Use of 6β-fluoro-7α-halogenocorticoids as topical anti-inflammatories and pharmaceutical formulations useful therefor | |
US4041055A (en) | Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes | |
US4124707A (en) | 7α-Halogeno-3,20-dioxo-1,4-pregnadienes, methods for their manufacture, their use as anti-inflammatory agents, and pharmaceutical formulations useful therefor | |
US5482934A (en) | Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions | |
US4198403A (en) | 17 Beta-thiocarboxylic acid esters of 4-halo-3-oxoandrost-4-enes | |
JPS6140648B2 (ja) | ||
JPH0112758B2 (ja) | ||
JPS6058999A (ja) | ã¹ããã€ãç³»ã«ã«ãã³é žãšã¹ãã«åã³ãããå«æããå»è¬ | |
US4336200A (en) | 17α-Acyloxy-5β-corticoids | |
US4576936A (en) | 6α-Fluoro-9α-chloro-prednisolone 17,21-diesters | |
US3984544A (en) | Retinoic acid esters of steroids of the pregnane series, their use in the treatment of acne and pharmaceutical formulations useful therefor | |
US4024131A (en) | 16-Methyl-9α-halo steroid esters, ethers and preparation thereof | |
JP2004509131A (ja) | ïŒïŒâããããã·âïŒïŒïŒïŒâãªãã·ãããã²ã¹ããã³ïŒïŒïŒïœïœâïŒïœïœïŒã®è£œé æ¹æ³ | |
KR850000769B1 (ko) | ì€í ë¡ìŽë ìì€í 륎ì ì ì¡°ë°©ë² | |
KR850001208B1 (ko) | 17α-ìì€ì¥ì-5β-ìœë¥Ží°ìœìŽë ë° 17α-ìì€ì¥ì-5α-ìœë¥Ží°ìœìŽëì ì ì¡°ë°©ë² | |
US4201778A (en) | 6-Acyloxy-1,4,6-pregnatrienes, their use as anti-inflammatory agents, methods for their manufacture, and 6-oxo-1,4-pregnadiene intermediates | |
JPS6411039B2 (ja) | ||
US4021459A (en) | Process for the preparation of 21-halogeno-21-desoxy-17α-acyloxy 20-keto-pregnenes | |
US4343739A (en) | Process of selective solvolysis | |
JPH02279695A (ja) | æ°èŠã¹ããã€ããžãªãŒã«ïŒããããå«ãå»è¬çµæç©ãããã³ãããã®èª¿è£œæ¹æ³ | |
US4427591A (en) | Reduced A ring-Î9(11) -corticoids | |
US4232013A (en) | 16,17-Pyrazolino- and 16,17-isopyrazolino-1,4-pregnadiene derivatives | |
JPS636559B2 (ja) | ||
JPS5922719B2 (ja) | ïŒïŒââã¡ãã«âïŒÎ±âããã¹ããã€ãã®ãšã¹ãã«åã³ãšâãã«èªå°äœ | |
US3980680A (en) | Process for the preparation of 21-desoxy-17-acyloxy-4-pregnenes and of 21-iodo-21-desoxy-17-acyl oxy-4-pregnene intermediates useful therein |