JPS63159317A - Allantoin-containing aqueous preparation - Google Patents
Allantoin-containing aqueous preparationInfo
- Publication number
- JPS63159317A JPS63159317A JP30959986A JP30959986A JPS63159317A JP S63159317 A JPS63159317 A JP S63159317A JP 30959986 A JP30959986 A JP 30959986A JP 30959986 A JP30959986 A JP 30959986A JP S63159317 A JPS63159317 A JP S63159317A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- allantoin
- aqueous preparation
- containing aqueous
- aluminum
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 title claims abstract description 114
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 title claims abstract description 58
- 229960000458 allantoin Drugs 0.000 title claims abstract description 58
- 238000002360 preparation method Methods 0.000 title claims abstract description 28
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract description 24
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims abstract description 15
- 235000013922 glutamic acid Nutrition 0.000 claims abstract description 15
- 239000004220 glutamic acid Substances 0.000 claims abstract description 15
- 235000001014 amino acid Nutrition 0.000 claims abstract description 13
- 150000001413 amino acids Chemical class 0.000 claims abstract description 13
- 150000007524 organic acids Chemical class 0.000 claims abstract description 11
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims abstract description 10
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims abstract description 8
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims abstract description 8
- 235000003704 aspartic acid Nutrition 0.000 claims abstract description 8
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims abstract description 8
- 150000007522 mineralic acids Chemical class 0.000 claims abstract description 8
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims abstract description 7
- 239000003381 stabilizer Substances 0.000 claims abstract description 7
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000002585 base Substances 0.000 claims abstract description 6
- 229920000137 polyphosphoric acid Polymers 0.000 claims abstract description 6
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims abstract description 5
- 239000011975 tartaric acid Substances 0.000 claims abstract description 5
- 235000002906 tartaric acid Nutrition 0.000 claims abstract description 5
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims abstract description 4
- 239000004471 Glycine Substances 0.000 claims abstract description 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims abstract 3
- 229910052782 aluminium Inorganic materials 0.000 claims description 17
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 17
- 229940024606 amino acid Drugs 0.000 claims description 11
- UEZVMMHDMIWARA-UHFFFAOYSA-N Metaphosphoric acid Chemical compound OP(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-N 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- 229910052783 alkali metal Inorganic materials 0.000 claims description 4
- -1 alkali metal salt Chemical class 0.000 claims description 4
- 235000015165 citric acid Nutrition 0.000 claims description 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 2
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims description 2
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims description 2
- 239000004473 Threonine Substances 0.000 claims description 2
- 150000001340 alkali metals Chemical class 0.000 claims description 2
- 239000011575 calcium Substances 0.000 claims description 2
- 229910052791 calcium Inorganic materials 0.000 claims description 2
- 229910052700 potassium Inorganic materials 0.000 claims description 2
- 239000011591 potassium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 239000011668 ascorbic acid Substances 0.000 claims 1
- 229960005070 ascorbic acid Drugs 0.000 claims 1
- 235000010323 ascorbic acid Nutrition 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- SFHUSLFRIKHKPE-UHFFFAOYSA-L chloro-[(2,5-dioxoimidazolidin-4-yl)carbamoylamino]aluminum;hydrate Chemical compound O.NC(=O)NC1NC(=O)N([Al]Cl)C1=O SFHUSLFRIKHKPE-UHFFFAOYSA-L 0.000 claims 1
- XPPKVPWEQAFLFU-UHFFFAOYSA-N diphosphoric acid Chemical compound OP(O)(=O)OP(O)(O)=O XPPKVPWEQAFLFU-UHFFFAOYSA-N 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 235000006408 oxalic acid Nutrition 0.000 claims 1
- 229940005657 pyrophosphoric acid Drugs 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 239000002674 ointment Substances 0.000 abstract description 10
- 239000000843 powder Substances 0.000 abstract description 8
- 238000002156 mixing Methods 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 5
- 208000025865 Ulcer Diseases 0.000 abstract description 4
- 208000027418 Wounds and injury Diseases 0.000 abstract description 4
- 231100000397 ulcer Toxicity 0.000 abstract description 4
- 206010052428 Wound Diseases 0.000 abstract description 3
- 150000003839 salts Chemical class 0.000 abstract 2
- 206010011985 Decubitus ulcer Diseases 0.000 abstract 1
- 239000003513 alkali Substances 0.000 abstract 1
- 239000001384 succinic acid Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 31
- 239000000203 mixture Substances 0.000 description 24
- 239000008213 purified water Substances 0.000 description 22
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 14
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 13
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 12
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 9
- 238000009472 formulation Methods 0.000 description 9
- 229920002125 Sokalan® Polymers 0.000 description 8
- AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 8
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 7
- 239000002253 acid Substances 0.000 description 7
- 239000003795 chemical substances by application Substances 0.000 description 7
- 235000011187 glycerol Nutrition 0.000 description 7
- 239000011787 zinc oxide Substances 0.000 description 7
- 235000014692 zinc oxide Nutrition 0.000 description 7
- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 description 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 6
- 239000007788 liquid Substances 0.000 description 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 5
- 239000000654 additive Substances 0.000 description 5
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 5
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 239000008108 microcrystalline cellulose Substances 0.000 description 5
- 229940016286 microcrystalline cellulose Drugs 0.000 description 5
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 5
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 4
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 4
- BBEAQIROQSPTKN-UHFFFAOYSA-N pyrene Chemical compound C1=CC=C2C=CC3=CC=CC4=CC=C1C2=C43 BBEAQIROQSPTKN-UHFFFAOYSA-N 0.000 description 4
- 239000004166 Lanolin Substances 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 239000004310 lactic acid Substances 0.000 description 3
- 235000014655 lactic acid Nutrition 0.000 description 3
- 229940039717 lanolin Drugs 0.000 description 3
- 235000019388 lanolin Nutrition 0.000 description 3
- 229940040145 liniment Drugs 0.000 description 3
- 239000000865 liniment Substances 0.000 description 3
- 235000005985 organic acids Nutrition 0.000 description 3
- 241000416162 Astragalus gummifer Species 0.000 description 2
- 241000167854 Bourreria succulenta Species 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- 208000001034 Frostbite Diseases 0.000 description 2
- 208000004210 Pressure Ulcer Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 229920001615 Tragacanth Polymers 0.000 description 2
- 239000013011 aqueous formulation Substances 0.000 description 2
- GVEPBJHOBDJJJI-UHFFFAOYSA-N fluoranthrene Natural products C1=CC(C2=CC=CC=C22)=C3C2=CC=CC3=C1 GVEPBJHOBDJJJI-UHFFFAOYSA-N 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- 235000015927 pasta Nutrition 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
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- 238000003756 stirring Methods 0.000 description 2
- 239000000196 tragacanth Substances 0.000 description 2
- 235000010487 tragacanth Nutrition 0.000 description 2
- 229940116362 tragacanth Drugs 0.000 description 2
- OHVLMTFVQDZYHP-UHFFFAOYSA-N 1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)-2-[4-[2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidin-5-yl]piperazin-1-yl]ethanone Chemical compound N1N=NC=2CN(CCC=21)C(CN1CCN(CC1)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)=O OHVLMTFVQDZYHP-UHFFFAOYSA-N 0.000 description 1
- SXAMGRAIZSSWIH-UHFFFAOYSA-N 2-[3-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-1,2,4-oxadiazol-5-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1=NOC(=N1)CC(=O)N1CC2=C(CC1)NN=N2 SXAMGRAIZSSWIH-UHFFFAOYSA-N 0.000 description 1
- WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 1
- IHCCLXNEEPMSIO-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperidin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 IHCCLXNEEPMSIO-UHFFFAOYSA-N 0.000 description 1
- TWJNQYPJQDRXPH-UHFFFAOYSA-N 2-cyanobenzohydrazide Chemical compound NNC(=O)C1=CC=CC=C1C#N TWJNQYPJQDRXPH-UHFFFAOYSA-N 0.000 description 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 1
- 241000357297 Atypichthys strigatus Species 0.000 description 1
- KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 description 1
- CAHQGWAXKLQREW-UHFFFAOYSA-N Benzal chloride Chemical compound ClC(Cl)C1=CC=CC=C1 CAHQGWAXKLQREW-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 1
- 235000019687 Lamb Nutrition 0.000 description 1
- 241000219745 Lupinus Species 0.000 description 1
- 235000021360 Myristic acid Nutrition 0.000 description 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N Myristic acid Natural products CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 1
- 239000004264 Petrolatum Substances 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- 235000002595 Solanum tuberosum Nutrition 0.000 description 1
- 244000061456 Solanum tuberosum Species 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
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- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
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- XGZRAKBCYZIBKP-UHFFFAOYSA-L disodium;dihydroxide Chemical compound [OH-].[OH-].[Na+].[Na+] XGZRAKBCYZIBKP-UHFFFAOYSA-L 0.000 description 1
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- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
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- 239000011780 sodium chloride Substances 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
[産業上の利用分野]
本発明は、アラントインが安定に配合されたアラントイ
ン含有水性製剤に関し、特に、艮期間にわたりアラント
インが安定に保持された潰瘍、創傷、褥拾、凍傷、熱傷
の治療用のアラントイン含有水性製剤に関する。Detailed Description of the Invention [Industrial Application Field] The present invention relates to an allantoin-containing aqueous preparation in which allantoin is stably blended, and particularly for treating ulcers, wounds, bed sores, etc. in which allantoin is stably retained over a period of time. This invention relates to an aqueous preparation containing allantoin for the treatment of frostbite and burns.
[従来の技術]
従来より、アラントイン又はそのアルミニウム誘導体を
含有した外用製剤は、熱傷、損傷などによる皮膚、粘膜
のビラン、潰瘍等の治療剤として知られでいる。従来の
アラントイン又はそのアルミ−ラム誘導体を含有した軟
膏は、ワセリン、ラノリン、パラフィン、蝋、高級アル
;1−ルなどよりなり、患部に塗布した時、患部の滲出
液は9,11郡組織にilf吸収されて、かえって、治
療を遅延させる結果を招くことがある。また、アラント
イン又はそのアルミ;−ウl−誘導体が含有された散剤
を用いると、散剤であるために患部への付着性が悪く、
患部から崩れ落ちたりして、患者の衣服等に飛散Vると
いう欠点をもっていた。[Prior Art] External preparations containing allantoin or its aluminum derivative have been known as therapeutic agents for skin and mucous membrane lesions, ulcers, etc. caused by burns and injuries. Conventional ointments containing allantoin or its aluminum derivatives are made of petrolatum, lanolin, paraffin, wax, higher alcohol, etc., and when applied to the affected area, the exudate from the affected area spreads to 9 and 11 tissues. ilf may be absorbed, resulting in a delay in treatment. In addition, when a powder containing allantoin or its aluminum;-ul-derivative is used, it has poor adhesion to the affected area because it is a powder;
It has the disadvantage of falling off the affected area and scattering onto the patient's clothes.
−にだ、軟膏剤、散Mに共通rる欠点として、アラント
イン又はそのアルミニウム誘導体が結晶の状態で存在す
るため放出性が悪く、治療」二も好ましくなかった。こ
れらの欠点は、製剤中に水を含有させることにより解決
することができる。即ら、水を含有することにより、、
ta部に塗布した時患部、1.−に油性の膜を形成する
ことがなく、付着性に優れ、かつアラントイン又はその
誘導体を融解状態とし、放出性の良い製剤とすることが
できる。然し乍ら、アラントイン又はそのアルミニラt
−+4導体は、水存在ドで非常に不安定であり、この理
由から水を含有したこれらの製Mは、いままでなかった
。- A common drawback of the powders, ointments, and powders is that allantoin or its aluminum derivative exists in a crystalline state, resulting in poor release properties, making them unfavorable for treatment. These drawbacks can be overcome by including water in the formulation. That is, by containing water,
When applied to the ta area, the affected area, 1. - It does not form an oily film on the surface, has excellent adhesion, and can melt allantoin or its derivatives to form a preparation with good release properties. However, allantoin or its aluminum
-+4 conductors are very unstable in the presence of water, and for this reason, these materials containing water have not hitherto been available.
[発明が解決しようとφ゛る問題点]
本発明は、アラントインを含有する水性製剤において、
長期間アラントインが安定に保持される水性製剤を提供
することを目的と4−る。[Problems to be solved by the invention] The present invention provides an aqueous preparation containing allantoin,
The object of the present invention is to provide an aqueous preparation that stably retains allantoin for a long period of time.
[発明の構成]
[問題点を解決するための手段]
本発明は、アラントインを有効量含有する水性製謂にお
いて、有機酸又は無機酸又はアミノ酸或いはそれらのア
ルカリ金属塩、或いは、それらの2以上の組合せを含有
配合するニーとにより、該アうントインを安定に水性基
剤に配合せしめたニーとを特徴とする安定なアラントイ
ン含有製剤である。その時、 07r記アラントインと
して、アルミニウム・ジLドIJキシアラントイネート
又はアルミニラl、りl’lルしド【1キシアラントイ
ネートを利用できる。また、前記有機酸はクエン酸、酒
石醜、シュ・ン酸、:1ハク酸、アスー17レビン酸等
であり得。[Structure of the Invention] [Means for Solving the Problems] The present invention provides an aqueous formulation containing an effective amount of allantoin, an organic acid, an inorganic acid, an amino acid, an alkali metal salt thereof, or two or more thereof. This is a stable allantoin-containing preparation characterized by containing and blending the allantoin combination in an aqueous base. At that time, as the allantoin described in 07r, aluminum di-LD IJ xialant inate or aluminum di-LD IJ xialant inate can be used. Further, the organic acid may be citric acid, tartaric acid, citric acid, :1 citric acid, asu-17 lebic acid, and the like.
11;12無機酸はリン酸、メタリン酸、ポリリン酸。11;12 Inorganic acids are phosphoric acid, metaphosphoric acid, and polyphosphoric acid.
とIIリン酸、酢酸、塩酸等にでき、前記アルカリ金属
はナトリウム、カリウド、カルシウドであり4町! 、
前記アミノ酸としてはグルタミン酸、アスパジギン酸、
グリンン、アシ−゛−ン、バリン、0イシン、イン【1
イシン、セリン、或いはトレオニン等を使用できる。And II can be made into phosphoric acid, acetic acid, hydrochloric acid, etc., and the alkali metals are sodium, potassium, and calcium, and there are 4 towns! ,
The amino acids include glutamic acid, aspadigic acid,
Greenn, Ashin, Barin, 0ishin, In [1
Isine, serine, threonine, etc. can be used.
本発明のアラントインを有効11を含有する水性製剤に
おいて、アラントインのアルミニウム誘導体としては、
アルミニウムクロルヒト【+キシアラントイネート、ア
ルミニウムジヒド11キシアラントイネート等が挙げら
れる。アラントイン、アラントインのアルミニウム誘導
体の製剤中に1本発明により用いられる安定剤には、有
機酸類、無lIA酸類、アミノ酸類の3種がある。In the aqueous preparation containing effective allantoin 11 of the present invention, the aluminum derivative of allantoin includes:
Examples include aluminum chlorhito[+xialantoinate], aluminum dihyde 11 xialantoinate, and the like. There are three types of stabilizers used according to the invention in the formulation of allantoin, an aluminum derivative of allantoin: organic acids, IIA-free acids, and amino acids.
本発明において、有機酸類とは、クエン酸、酒石酸、乳
酸、シュウ酷、:1ハク酸、アス:Iルピン酸等の有機
酸を云う、また9本発明において、無IaI1M2類と
は、リン酸、メタリン酸、ポリリン酸。In the present invention, organic acids refer to organic acids such as citric acid, tartaric acid, lactic acid, citric acid, :1 uccinic acid, and as:I lupic acid. , metaphosphoric acid, polyphosphoric acid.
ピ■リン酷、酢酸、塩酸等の無機酸を云う、また9本発
明において、アミノ酸類とは、グルタミン酸、アスパラ
ギン酸、グリシン、アラントイン、ロイシン、イソUイ
シン、I!リン、1・しオニン等のアミノ酸を云う0件
のように本発明で用いられるアミノ酸は、酸性また中性
の両ノjを含むものである。In the present invention, amino acids include glutamic acid, aspartic acid, glycine, allantoin, leucine, iso-Uisine, I! The amino acids used in the present invention, such as amino acids such as phosphorus and 1-thionine, include both acidic and neutral amino acids.
このような安定剤が1本発明の製剤に配合されるが、そ
の配合猜は、製剤中に含有Vる基剤により異なるが、約
0.01〜20虫1^%の範囲が好適である。One such stabilizer is blended into the formulation of the present invention, and its blending amount varies depending on the base material contained in the formulation, but it is preferably in the range of about 0.01 to 20%. .
本発明による製剤は、水を含有する。即ち、水性の製剤
すべてに適用可能であり、クリーム削(W2O或いは6
7 y ) 、 u−シElン剤に限定されるものでな
く、リニメントM、パップ剤、パスタ剤、ゲル状の軟・
汗剤等の広い範囲に適用できるものである。基剤成分は
、特に限定されるものでなく、必要に応じて他の成分、
活性成分、基剤成分も添加し用いることができるもので
ある。The formulation according to the invention contains water. That is, it is applicable to all aqueous preparations, and cream shavers (W2O or 6
7y), not limited to u-silicone agents, but also liniment M, poultices, pasta agents, gel-like soft and
It can be applied to a wide range of sweat agents, etc. The base component is not particularly limited, and other components may be added as necessary.
Active ingredients and base ingredients can also be added and used.
従って1本発明の製剤には、必要に応じて1本発明の効
果を損じない範囲で、防腐剤、乳化剤。Therefore, the formulation of the present invention may contain preservatives and emulsifiers, as necessary, to the extent that they do not impair the effects of the present invention.
酸化防止剤、金属イオン封鎖剤、増粘剤等を配合するこ
とができる。Antioxidants, sequestrants, thickeners, etc. can be added.
製剤中にアラントインと、上記で述べた特定のアミノ酸
又は有機酸又は無機酸を配合すると、アラントインの経
時(El)安定性は、上記の特定のアミノ酸又は有機酸
又は無機酸を配合しない場合に比べて著しく向卜するこ
とを発見したことに基づき1本発明を成したものである
。When allantoin is combined with the above-mentioned specific amino acids or organic or inorganic acids in a formulation, the stability over time (El) of allantoin is lower than when the above-mentioned specific amino acids or organic or inorganic acids are not included. The present invention has been made based on the discovery that the present invention is significantly improved.
本発明による製剤では、水と、アラントイン又はそのア
ルミニウム誘導体が共存し、アラントイン又はそのアル
ミニウム誘導体が一部溶解状態で存在するために、従来
の油性基剤を使用した軟膏M或いは散剤に比較して、潰
瘍、創傷、褥拾、凍傷、熱傷に対して高い治療効果を発
揮するものである。In the preparation according to the present invention, since water and allantoin or its aluminum derivative coexist, and allantoin or its aluminum derivative exists in a partially dissolved state, compared to ointment M or powder using a conventional oil base, It is highly effective in treating ulcers, wounds, bedsores, frostbite, and burns.
次に1本発明のアラントインを含有する水性製剤を、共
体的な実施例により、比較例と比較しながら説明4゛る
が1本発1り目よ1次の説明に限定−〜れるものではな
い。Next, the aqueous preparation containing allantoin of the present invention will be explained using common examples and compared with comparative examples, but the explanation will be limited to the following explanation. isn't it.
[実施例1〜3及び比較例1〜3]
A、ヤタノール 6.0gソ←リ
ン 10.0gグリヒリンe/Ir
′I肪酸ニスデル 2.OgTween60
4.Ogミリスチリン酸イソブUピル 1
0.0gプ[lビルパラベン 0.1g
B、プ17ビレングリコール 10.0gアル
ミニウムク「rル
Lド■1キシアラントイネート 6.0gメチルパ
ラベン 0.1゜精製水
適i^ト記B成分及び下記の表に示す各添
加剤をとり、精製水を加え、全量で67.9gにし、7
5℃に加温して溶解し、別にA成分についても75℃に
加温溶解して、溶解したB成分と添加剤に加え、乳化混
合した後、25℃まで冷却し1表に示す°比較例1〜3
及び実施例1〜3を調製した。[Examples 1 to 3 and Comparative Examples 1 to 3] A, Yatanol 6.0g So←Rin 10.0g Glychrin e/Ir
'I fatty acid Nisdel 2. OgTween60
4. Og myristic acid isobu U pill 1
0.0g Bilparaben 0.1g
B, 17-bylene glycol 10.0g Aluminum chloride 1 Xialantoinate 6.0g Methylparaben 0.1゜Purified water
Take component B and each additive shown in the table below, add purified water to make a total of 67.9 g, and add 7
Component A was heated and dissolved at 5°C, separately heated and dissolved at 75°C, added to the dissolved B component and additives, emulsified and mixed, cooled to 25°C, and compared as shown in Table 1. Examples 1-3
and Examples 1 to 3 were prepared.
、−のように調製した各製剤を、50″Cで1ケ月保存
した後に取り出し、その残存アラントインを、IN塩酸
により抽出し、高速液体り1.Jマドグラフ法により定
駿した。その結果を次の表に示−゛。The preparations prepared as in , - were stored at 50"C for one month and then taken out. The residual allantoin was extracted with IN hydrochloric acid and determined by the high-speed liquid evaporation method using the 1.J Madograph method. The results are as follows. Shown in the table below.
第1表
添加剤 添加M晴 アラントインt゛
比較例1 − −− 60.2%回
2水酸化ナトリウム0.5% 41.0%回 3
トリエフノールアミン 0.5%
57 、1 %実施例1メタリン酸 0.5%
98.9%回 2 クエ7 Ml 3 %
99 、9 %比較例1,2.3は各々、添加
剤なし、又は本発明で使用する安定剤以外の添加剤を配
合した例である0本発明により使用する安定剤を配合し
た実施例1〜3は、比較例1〜3に比較してアルミニラ
l、にド【1キシク11ルアラントイネートの経時(1
1)安定性が1ぐれていることが明らかである。Table 1 Additive Addition M Allantoin Comparative Example 1 - -- 60.2% times
Sodium dihydroxide 0.5% 41.0% times 3
Triphenolamine 0.5%
57, 1% Example 1 Metaphosphoric acid 0.5%
98.9% times 2 Quest 7 Ml 3%
99, 9% Comparative Examples 1 and 2.3 are examples in which no additive was used or additives other than the stabilizer used in the present invention were blended.0 Example 1 in which the stabilizer used in the present invention was blended - 3 shows that compared to Comparative Examples 1 to 3, the aging of alumina l, nido [1
1) It is clear that the stability has deteriorated by 1.
[実施例4−1][++−シ5Iン/i1]アラントイ
ン 5.0g酸化亜鉛
10.0gグリヒリン
3.0g微結晶セルU−ズ 2.5g
カルボキシメチルセルU−ズ 2.5g乳酸
4.0g精製水
73.0゜[−記の割合で、微結晶セルロー
ズ、カルボキンメチルセルローズを精製水に少’+k
’1’っ加え、充分湿潤させ、溶解させたものを用、α
する0次に、別にアラントイン、酸化亜鉛、グリセリン
を、1−記の晴、混合均一としたものを、11カに作製
した微結晶セ、ルローズ、カルボキシメチルセルローズ
溶解物に加え.更に乳酸を加えて混合均一にし。[Example 4-1] [++-Syn/i1] Allantoin 5.0g Zinc oxide
10.0g Glychlin
3.0g Microcrystalline Cell U-s 2.5g
Carboxymethylcell U-zu 2.5g lactic acid
4.0g purified water
73.0゜ [Add a small amount of microcrystalline cellulose and carboquine methyl cellulose to purified water in the proportions shown below.
Add '1', thoroughly moisten and dissolve, then use α
Next, allantoin, zinc oxide, and glycerin were mixed uniformly as described in 1-1 and added to the microcrystalline cellulose, lurose, and carboxymethyl cellulose melt prepared in Step 11. Add lactic acid and mix evenly.
El−シJン剤を作製した。An El-sin agent was prepared.
[実施例4−2]
アラントイン 5.0g酸化曲鉛
10.0gゲリトリン
3.0g微結晶セル「I−ズ
2.5gカルボキシメチルセルローズ
ポリリン酸 4.0区グルタミ
ン酸 2.0g精製水
71.0g上記の割合で,微結晶セル【
1−ズ,カルボキシメチルトルローズを精製水に少量ず
つ加え,充分湿潤.溶解させたものを川,へする、次に
,別にアラントイン、酸化亜鉛,グリセリンを上記のに
混合均一としたものを,前に作製した微結晶セルローズ
、カルボキシメチルセル0−ズの混合物に加え,史にポ
リリン酸及びグルタミン酸を加えnシ合均−にし、U−
シクン剤を作製した。[Example 4-2] Allantoin 5.0g bent lead oxide
10.0g Geritrin
3.0g microcrystalline cell "I-s"
2.5g carboxymethylcellulose polyphosphoric acid 4.0 glutamic acid 2.0g purified water
71.0gWith the above ratio, microcrystalline cell [
1. Add carboxymethyl torurose little by little to purified water and moisten thoroughly. Transfer the dissolved material to a river. Next, add allantoin, zinc oxide, and glycerin to the mixture of microcrystalline cellulose and carboxymethyl cellulose prepared previously. Add polyphosphoric acid and glutamic acid to the mixture to make the total balance, and make U-
I made a Shikun medicine.
[実施例4−3]
アラントイン 5.0g酸化IIIi
鉛 10.0gグリセリン
3.0g微結晶セル日−ズ
2.5gカルボキシメチルセル[1−ズ 2,
5gクエン# 4.Ogア
スパラギンIlv[2.0g
精製水 71.0g上2の割合で
.微結晶セル【j−ズ,カルボキシメチルセル1)−ズ
を精製水に少量ずつ加え,充分i11in.溶解さけた
ものを用意する.次に,別にアシントイン,酸化亜鉛,
グリセリンを−1−記のht混合均一としたものを,前
に作成した微結晶セルU−ズ,カルボキシメチルセルU
−ズの混合物に加え.更にクエン酸及びアスパラギン酸
を加え混合均一にし,n−ジョン剤を作製した。[Example 4-3] Allantoin 5.0g Oxide IIIi
Lead 10.0g glycerin
3.0g microcrystalline cell days
2.5g carboxymethyl cell [1-s 2,
5g Quen #4. Og Asparagine Ilv [2.0g Purified water 71.0g at a ratio of 2 parts. Add microcrystalline cells [j-s, carboxymethyl cells 1)-s little by little to purified water, and stir well for 11 in. Prepare something that has not been dissolved. Next, separately asyntoin, zinc oxide,
Glycerin was uniformly mixed with ht as described in -1-, and then the microcrystalline cell U-s and carboxymethyl cell U-s prepared previously were mixed.
- Add to the mixture. Further, citric acid and aspartic acid were added and mixed uniformly to prepare an n-john agent.
[実施例4−4]
アラントイン 5.0g酸化亜鉛
10.0gグリセリン
3.0g微結晶セルローズ 2
.5gカルボキシメチJレセルローズ 2.5gビ
ロリン酸 4.Og酒石酌
2.0g精製水
71.0g上記の割合で,微結晶セルロー
ズ、カルボキシメチルセルローズを精製水に少■λずつ
加え,充分湿潤,溶解させたものを用意する.次に,別
にアラントイン、IvI化亜鉛亜鉛リセリンをF記のに
混合均一 とじたものを、前に作成した微結晶セル「1
−ズ,カルボキシメチルセル【I−ズの混合物に加λ.
,更に酒石酸及びピIJリン酸を加え混合均一にし,r
i−シ三1ン剤を作製した。[Example 4-4] Allantoin 5.0g zinc oxide
10.0g glycerin
3.0g microcrystalline cellulose 2
.. 5g carboxymethiJ recellulose 2.5g birophosphoric acid 4. Og sake stone cup
2.0g purified water
71.0g Add a small amount of microcrystalline cellulose and carboxymethyl cellulose to purified water in the above proportions, sufficiently moisten and dissolve. Next, allantoin and zinc IvI chloride lyserine were uniformly mixed and bound into the microcrystalline cell "1" prepared previously.
-s, carboxymethyl cell [λ.
, further add tartaric acid and PIIJ phosphoric acid and mix uniformly, r
An i-silicone drug was prepared.
[実施例5][パスタ剤]
アラントイン 6.0g塩化ベンザルコ
ニウム 0.1g精製ラノリン 1
2g
チンク油 75g
メクリン酸 2g
精製水 4ml
精製水にメタリン酸,アラントイン、塩化ベンザル;1
ニウムを加え分散させ.精製ラノリンを加えよく混和し
た後.チンク油を加えよく混和して均一にし,パスタ剤
を作製した。[Example 5] [Paste agent] Allantoin 6.0g Benzalkonium chloride 0.1g Purified lanolin 1
2g Chink oil 75g Meclic acid 2g Purified water 4ml Metaphosphoric acid, allantoin, benzal chloride in purified water; 1
Add Nitrium and disperse. Add purified lanolin and mix well. Chink oil was added and mixed well to make it homogeneous, and a pasta paste was prepared.
[実施例6][リニメント剤]
アルミニウムクロルヒト11キシ
アラントイネート 6.0g亜鉛華デン
プン 10.0gトラガント末
5.0gグリセリン
3.0gグルタミン酸 3.0g
精製水 73.0gミキサーに
精製水を入れ,攪拌しなからトラガント末を9址ずつ加
え溶解した後、亜鉛華デンプン、アルミニラムク[1ル
LドUキシアラントイネート、グルタミン酸、グリセリ
ンを加え均一になるまでよく混和し、リニメント製剤を
作製した。[Example 6] [Liniment agent] Aluminum chlorhito 11 xialantoinate 6.0 g Zinc white starch 10.0 g Tragacanth powder
5.0g glycerin
3.0g Glutamic acid 3.0g
Purified water 73.0g Put purified water in a mixer, add 9 pieces of tragacanth powder while stirring and dissolve, then add zinc oxide starch, aluminum lamb [1 L xialantoinate, glutamic acid, and glycerin] and mix evenly. A liniment preparation was prepared by mixing thoroughly until the mixture was mixed.
[実施例7−1][軟・H]
アルミーウムジLドUキシ
アシントイネート 3.Ogカルボ
キシビJ−ルボリマ−0,3g
トリエタノールアミン 0.05gグルグル
タミンl’i 1.5gプロピ
レングリコール 10g精製水
85.15gJ11m水にカルボキシビニ
ルポリマー、アルミニウムジヒドロキシアラントイネー
ト、グルタミン酸を加えよく混合して、溶解し、更に、
プロピレングリコールを加え混合した後、トリエタノー
ルアミン0.05gを加えゲル化させて、軟膏を作製し
た。[Example 7-1] [Soft/H] Aluminum di-L-do-U xycintoinate 3. Og Carboxybi J-Rubolimer-0.3g Triethanolamine 0.05g Gluglutamine l'i 1.5g Propylene Glycol 10g Purified Water
Add carboxyvinyl polymer, aluminum dihydroxyallantoinate, and glutamic acid to 85.15gJ11m water, mix well, and dissolve.
After adding propylene glycol and mixing, 0.05 g of triethanolamine was added and gelatinized to prepare an ointment.
[実施例7−21
アルミ、−・ン11ジhドHキシ
アシントイネート 3.Ogカルポキ
シビニルボリーン−0,3g
トリエタノールアミン・ 0.05gグルタ
ミン酸 1.5gプ11ピレング
リコール 10.0gメタリン酸
1.5g精製水
85.65g精製水にカルボキシビニルポリマー、アル
ミニウムジLド【Iキシアラントイネート、グルタミン
酸、メタリン酸を加えよく混合して、溶解し、更に、プ
ロピレングリコールを加え混合した後、トリエタノール
アミン0.05gを加えゲル化させて、軟膏を作製した
。[Example 7-21 Aluminum,--N11-dih-do-H-xyacycintoinate 3. Og Carpoxyvinylborine - 0.3g Triethanolamine 0.05g Glutamic acid 1.5g Pr-11pyrene glycol 10.0g Metaphosphoric acid
1.5g purified water
Carboxyvinyl polymer, aluminum di-L-do[I]-xialantoinate, glutamic acid, and metaphosphoric acid were added to 85.65 g of purified water, mixed well, and dissolved. Further, propylene glycol was added and mixed, and then triethanolamine was added. An ointment was prepared by adding 0.05 g of the ointment and gelling it.
[実施例7−3]
アルミニラ12ジヒド11キシ
アシントイネート 3.0gカルボキ
シビニルポリマー 0.3gトリエタノールアミ
ン 0.05gグルタミン酸
1.5gゾ【1ピレングリ:I−ル
10.Ogアス:1ルピン19 1
.5g精製水 85.65g精
製水にカルボキシビニルポリマー、アルミニウムジLド
ロキシアラントイネート、グルタミン酸、アスパラギン
酸を加えよく混合して、溶解し、史に、プロピレングリ
コールを加え混合した後、トリエタノールアミン0.0
5gを加えゲル化させて、軟膏を作製した。[Example 7-3] Aluminilla 12 dihyde 11 xyacycintoinate 3.0 g carboxyvinyl polymer 0.3 g triethanolamine 0.05 g glutamic acid
1.5g
10. Og Ass: 1 Lupine 19 1
.. 5g purified water 85.65g purified water, add carboxyvinyl polymer, aluminum di-L-droxyallantoinate, glutamic acid, and aspartic acid, mix well, dissolve, add propylene glycol, mix, and add triethanolamine 0 .0
An ointment was prepared by adding 5 g of the mixture and gelling it.
[実施例7−41
アルミ、′−ウ11ジhド【Iキシ
アシントイ羊−) 3.0gカルボ
キシビ、−ルボリ°ン−0,3gトリこ「6タノールア
ミン 0.05gグルタミン酸
1.5gゾ【Iピレングリコール
10.0gアスパラギン酸 1.
5g精製水 85.65g精製
水にカルボキシビニルポリマー、アルミニウムジヒドロ
キシアシントイネート、グルタミン酸、アスパラギン酸
を加えよく混合して、溶解し、更に、プI’!ピレング
リ:1−ルを加え混合した後、トリエタノールアミン0
.05gを加えゲル化させて、軟膏を作製した。[Example 7-41 Aluminum, '-U11 dihd [I xyacintoy] 3.0 g Carboxybin, -ruboline - 0.3 g Tricho'6-tanolamine 0.05 g Glutamic acid
1.5g [I pyrene glycol]
10.0g aspartic acid 1.
5g purified water 85.65g Add carboxyvinyl polymer, aluminum dihydroxyacintoinate, glutamic acid, and aspartic acid to purified water, mix well, dissolve, and then add P-I'! Pyrene glycol: After adding 1-l and mixing, triethanolamine 0
.. An ointment was prepared by adding 0.05 g of the ointment and gelling it.
[実施例8][パップ剤]
カルボキシビニルポリマー 2g精製水
75gポリアクリル酸ナ
トリウム 3.5gメチルパシベン
O,1gノチルバフベン
0.1gノ■ピルパシベン
0.04 g5%塩化アルミ一二つl、液
3.5gデルタグリ−lノシクトン
2゜0870%ソルビット液 1
0.0 g5%水〜化ナトリウム 2
.0gアルミニウムク【1ル
LドIJキシアジントイネート 8.Ogアス
パシギン# 4.0gl−記の配
合で、先ず、精製水にカルボキシビニルポリマーを加え
1次にアルミニウムクロルヒトUキシアラントイネート
、アスパラギン酸、ポリアクリル酸を加え溶解、練り合
した後、デルタグリコ1ノラクトン、70%ソルビトー
ル液を混合する。続いて5%塩化アルミニウム液3.5
g 、 5%水水酸化ナトリフ11液加えゲル化さけ作
製したゲル状物を保温′ノイルノ、1−に塗布して、パ
ッノ製薊を作製した。[Example 8] [Poultice] Carboxyvinyl polymer 2g purified water
75g Sodium polyacrylate 3.5g Methylpaciben
O, 1g notyl buffen
0.1g pilpaciben
0.04 g 5% aluminum chloride 12 liters, liquid
3.5g delta glycol nosictone
2゜0870% sorbitol liquid 1
0.0 g 5% sodium chloride 2
.. 0g Aluminum Oxide 8. Og Aspacigin # 4.0g - With the following formulation, firstly, carboxyvinyl polymer was added to purified water, firstly, aluminum chlorhito-U xialantoinate, aspartic acid, and polyacrylic acid were added, dissolved and kneaded, and then delta Mix glyco1nolactone and 70% sorbitol solution. Then 3.5% 5% aluminum chloride solution
g. 11 liquids of 5% sodium hydroxide were added to form a gelatinous material.The prepared gelatinous material was applied to a heat-retaining 'Noilno, 1-' to prepare a Panno-made potato.
[比較例4〜8]
実施例4〜8と同様の製法、配合組成で1本発明による
安定側を含まrに、アラントイン又はそのアルミーウ1
1誘導体の外用製削を各々製造し。[Comparative Examples 4 to 8] Using the same manufacturing method and composition as in Examples 4 to 8, 1 contained the stable side according to the present invention, and allantoin or its aluminum 1
1 derivatives for external use.
比較例4〜8とした。Comparative Examples 4 to 8 were given.
実施例4〜8と比較例4〜8の製剤について室温で保存
した時の、アラントインの安定性を試験した。その結果
を次の表に示1’、ll数経過後の残存アラントインの
htを高速液体りI!マトグシソイで分析した。この表
から本発明によるアラントイン含有水性製剤の顕著な安
定化効果が明らかである。The stability of allantoin was tested for the formulations of Examples 4-8 and Comparative Examples 4-8 when stored at room temperature. The results are shown in the table below.The residual allantoin content after 1', 1l number of hts was determined by high-speed liquid dilution. It was analyzed using Matogushi Soi. The remarkable stabilizing effect of the allantoin-containing aqueous formulation according to the invention is clear from this table.
なお、E記の実施例及び比較例でアラントインの定11
先に用いた高速液体り[1マドグラソイの運転条件は、
NH,カラl、を使用し9分析温度二室温で、紫外線吸
光光度計(測定波長:230nm)で、移動層: NH
,H,PO,ニアヒトニトリル寓1:3のものである。In addition, in the Examples and Comparative Examples in Section E, allantoin
The operating conditions of the high-speed liquid rig [1 Mado Grasoy] used earlier are:
Using NH, color, and 9 analysis temperatures at room temperature, using an ultraviolet absorption photometer (measurement wavelength: 230 nm), moving phase: NH.
, H, PO, Niahitonitrile Parable 1:3.
第2表 アラントインの安定性
[発明の効果]
本発明のアラントインを安定化した水性製剤は、第1に
、そのアラントインの顕著な安定性。Table 2 Stability of Allantoin [Effects of the Invention] The allantoin-stabilized aqueous preparation of the present invention has, firstly, remarkable stability of allantoin.
顕著なγラントイン残存率が提供されること、第2に、
長期間安定な水性製剤を容易に製造できること、第3に
9本発明による製剤においては、アラン:・インは、一
部溶解状態で水と共イfするために、他の製法のMMに
比較して、高い治癒効果が提供できることなどの技術的
効果が得られた。A remarkable gamma lantoin residual rate is provided, and secondly,
Thirdly, in the preparation according to the present invention, alan:-yne co-fuses with water in a partially dissolved state, so compared to MM of other manufacturing methods. As a result, technical effects such as the ability to provide high healing effects were obtained.
Claims (6)
、 アラントインの安定化剤として、有機酸又は無機酸又は
アミノ酸或いはそれらのアルカリ金属塩、或いは、それ
らの2以上の組合せを含有することにより、該アラント
インを安定に水性基剤に配合せしめたことを特徴とする
アラントイン含有水性製剤。(1) In an aqueous preparation containing an effective amount of allantoin, by containing an organic acid, an inorganic acid, an amino acid, an alkali metal salt thereof, or a combination of two or more thereof as a stabilizer for allantoin, the allantoin An allantoin-containing aqueous preparation, characterized in that it is stably blended with an aqueous base.
アラントイネート又はアルミニウムクロルヒドロキシア
ラントイネートである特許請求の範囲第1項記載のアラ
ントイン含有水性製剤。(2) The allantoin-containing aqueous preparation according to claim 1, wherein the allantoin is aluminum dihydroxyallantoinate or aluminum chlorohydroxyallantoinate.
ク酸又はアスコルビン酸である特許請求の範囲第1項記
載のアラントイン含有水性製剤。(3) The allantoin-containing aqueous preparation according to claim 1, wherein the organic acid is citric acid, tartaric acid, oxalic acid, succinic acid, or ascorbic acid.
ピロリン酸、酢酸又は塩酸である特許請求の範囲1第1
項記載のアラントイン含有水性製剤。(4) The inorganic acid is phosphoric acid, metaphosphoric acid, polyphosphoric acid,
Claim 1 No. 1 which is pyrophosphoric acid, acetic acid or hydrochloric acid
Allantoin-containing aqueous preparations described in Section 1.
ルシウムである特許請求の範囲第1項記載のアラントイ
ン含有水性製剤。(5) The allantoin-containing aqueous preparation according to claim 1, wherein the alkali metal is sodium, potassium, or calcium.
グリシン、アラニン、バリン、ロイシン、イソロイシン
、セリン又はトレオニンである特許請求の範囲第1項記
載のアラントイン含有水性製剤。(6) The amino acids are glutamic acid, aspartic acid,
The allantoin-containing aqueous preparation according to claim 1, which is glycine, alanine, valine, leucine, isoleucine, serine, or threonine.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP30959986A JPS63159317A (en) | 1986-12-24 | 1986-12-24 | Allantoin-containing aqueous preparation |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP30959986A JPS63159317A (en) | 1986-12-24 | 1986-12-24 | Allantoin-containing aqueous preparation |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS63159317A true JPS63159317A (en) | 1988-07-02 |
Family
ID=17994969
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP30959986A Pending JPS63159317A (en) | 1986-12-24 | 1986-12-24 | Allantoin-containing aqueous preparation |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS63159317A (en) |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000037037A3 (en) * | 1998-12-18 | 2000-10-12 | H Michael Dosch | Composition for treatment of burns |
JP2001278788A (en) * | 2000-03-30 | 2001-10-10 | Zeria Pharmaceut Co Ltd | Stable liquid preparation formulated with allantoin |
JP2002020253A (en) * | 2000-07-05 | 2002-01-23 | Kobayashi Pharmaceut Co Ltd | Composition for oral use |
EP1202700A1 (en) * | 1999-07-23 | 2002-05-08 | Alwyn Company, Inc. | Oil-in-water emulsion with improved stability |
JP2005015404A (en) * | 2003-06-27 | 2005-01-20 | Nichiban Co Ltd | Anti-inflammatory plaster |
US8877790B2 (en) | 1999-07-23 | 2014-11-04 | Scioderm, Inc. | Allantoin-containing skin cream |
US9095574B2 (en) | 2010-02-02 | 2015-08-04 | Scioderm, Inc. | Methods of treating psoriasis using allantoin |
WO2015152079A1 (en) * | 2014-03-31 | 2015-10-08 | 小林製薬株式会社 | Water-based medicinal composition |
JP2016130224A (en) * | 2015-01-13 | 2016-07-21 | 小林製薬株式会社 | External composition |
KR20160137524A (en) | 2014-03-31 | 2016-11-30 | 라이온 가부시키가이샤 | Toothpaste composition |
JP2021004184A (en) * | 2019-06-25 | 2021-01-14 | 小林製薬株式会社 | Method of stabilizing allantoin and/or derivative thereof |
JP2021004185A (en) * | 2019-06-25 | 2021-01-14 | 小林製薬株式会社 | External composition |
CN113425614A (en) * | 2021-06-28 | 2021-09-24 | 广东药科大学 | Application of amino acid or amino acid analogue or salt thereof as additive for improving dissolving property of allantoin |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5547608A (en) * | 1978-09-27 | 1980-04-04 | Key Pharma | Skin medicine |
JPS56139414A (en) * | 1980-04-01 | 1981-10-30 | Dai Ichi Seiyaku Co Ltd | Stabilizing method of aqueous solution |
JPS56156211A (en) * | 1980-05-07 | 1981-12-02 | Teika Seiyaku Kk | Preparation of stable allantoin pharmaceutical |
JPS5892621A (en) * | 1981-11-28 | 1983-06-02 | Sunstar Inc | Stable pharmaceutical preparation containing interferon |
JPS59175414A (en) * | 1983-03-23 | 1984-10-04 | Toyo Jozo Co Ltd | Stable oral preparation of macrolide antibiotic substance and method for stabilizing the same |
-
1986
- 1986-12-24 JP JP30959986A patent/JPS63159317A/en active Pending
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5547608A (en) * | 1978-09-27 | 1980-04-04 | Key Pharma | Skin medicine |
JPS56139414A (en) * | 1980-04-01 | 1981-10-30 | Dai Ichi Seiyaku Co Ltd | Stabilizing method of aqueous solution |
JPS56156211A (en) * | 1980-05-07 | 1981-12-02 | Teika Seiyaku Kk | Preparation of stable allantoin pharmaceutical |
JPS5892621A (en) * | 1981-11-28 | 1983-06-02 | Sunstar Inc | Stable pharmaceutical preparation containing interferon |
JPS59175414A (en) * | 1983-03-23 | 1984-10-04 | Toyo Jozo Co Ltd | Stable oral preparation of macrolide antibiotic substance and method for stabilizing the same |
Cited By (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000037037A3 (en) * | 1998-12-18 | 2000-10-12 | H Michael Dosch | Composition for treatment of burns |
US8877789B2 (en) | 1999-07-23 | 2014-11-04 | Scioderm, Inc. | Allantoin-containing skin cream |
EP1202700A1 (en) * | 1999-07-23 | 2002-05-08 | Alwyn Company, Inc. | Oil-in-water emulsion with improved stability |
EP1202700A4 (en) * | 1999-07-23 | 2005-01-19 | Alwyn Co Inc | Oil-in-water emulsion with improved stability |
US9084780B2 (en) | 1999-07-23 | 2015-07-21 | Scioderm, Inc. | Allantoin-containing skin cream |
US8877790B2 (en) | 1999-07-23 | 2014-11-04 | Scioderm, Inc. | Allantoin-containing skin cream |
US8877788B2 (en) | 1999-07-23 | 2014-11-04 | Scioderm, Inc. | Allantoin-containing skin cream |
JP2001278788A (en) * | 2000-03-30 | 2001-10-10 | Zeria Pharmaceut Co Ltd | Stable liquid preparation formulated with allantoin |
JP2002020253A (en) * | 2000-07-05 | 2002-01-23 | Kobayashi Pharmaceut Co Ltd | Composition for oral use |
JP2005015404A (en) * | 2003-06-27 | 2005-01-20 | Nichiban Co Ltd | Anti-inflammatory plaster |
JP4574961B2 (en) * | 2003-06-27 | 2010-11-04 | ニチバン株式会社 | Anti-inflammatory analgesic patch |
US9095574B2 (en) | 2010-02-02 | 2015-08-04 | Scioderm, Inc. | Methods of treating psoriasis using allantoin |
US9339492B1 (en) | 2010-02-02 | 2016-05-17 | Scioderm, Inc. | Methods of treating psoriasis using allantoin |
WO2015152079A1 (en) * | 2014-03-31 | 2015-10-08 | 小林製薬株式会社 | Water-based medicinal composition |
JP2015196652A (en) * | 2014-03-31 | 2015-11-09 | 小林製薬株式会社 | aqueous pharmaceutical composition |
KR20160137524A (en) | 2014-03-31 | 2016-11-30 | 라이온 가부시키가이샤 | Toothpaste composition |
KR20160138179A (en) * | 2014-03-31 | 2016-12-02 | 고바야시 세이야쿠 가부시키가이샤 | Water-based medicinal composition |
JP2016130224A (en) * | 2015-01-13 | 2016-07-21 | 小林製薬株式会社 | External composition |
JP2021004184A (en) * | 2019-06-25 | 2021-01-14 | 小林製薬株式会社 | Method of stabilizing allantoin and/or derivative thereof |
JP2021004185A (en) * | 2019-06-25 | 2021-01-14 | 小林製薬株式会社 | External composition |
CN113425614A (en) * | 2021-06-28 | 2021-09-24 | 广东药科大学 | Application of amino acid or amino acid analogue or salt thereof as additive for improving dissolving property of allantoin |
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