JP2001039866A - Pharmaceutical composition for application to mucous membrane - Google Patents
Pharmaceutical composition for application to mucous membraneInfo
- Publication number
- JP2001039866A JP2001039866A JP11216120A JP21612099A JP2001039866A JP 2001039866 A JP2001039866 A JP 2001039866A JP 11216120 A JP11216120 A JP 11216120A JP 21612099 A JP21612099 A JP 21612099A JP 2001039866 A JP2001039866 A JP 2001039866A
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- polyphenol compound
- mucosal application
- ion
- application according
- 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.)
- Withdrawn
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 24
- 210000004400 mucous membrane Anatomy 0.000 title abstract description 7
- -1 polyphenol compound Chemical class 0.000 claims abstract description 20
- 235000013824 polyphenols Nutrition 0.000 claims abstract description 19
- 229910001425 magnesium ion Inorganic materials 0.000 claims abstract description 6
- 229910001414 potassium ion Inorganic materials 0.000 claims abstract description 6
- 229910001415 sodium ion Inorganic materials 0.000 claims abstract description 6
- JLVVSXFLKOJNIY-UHFFFAOYSA-N Magnesium ion Chemical compound [Mg+2] JLVVSXFLKOJNIY-UHFFFAOYSA-N 0.000 claims abstract description 5
- 150000007522 mineralic acids Chemical class 0.000 claims abstract description 5
- NPYPAHLBTDXSSS-UHFFFAOYSA-N Potassium ion Chemical compound [K+] NPYPAHLBTDXSSS-UHFFFAOYSA-N 0.000 claims abstract description 4
- FKNQFGJONOIPTF-UHFFFAOYSA-N Sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 claims abstract description 4
- 230000007794 irritation Effects 0.000 claims abstract description 4
- 150000007524 organic acids Chemical class 0.000 claims abstract description 4
- 159000000003 magnesium salts Chemical class 0.000 claims abstract 3
- 159000000000 sodium salts Chemical class 0.000 claims abstract 3
- LNTHITQWFMADLM-UHFFFAOYSA-N gallic acid Chemical compound OC(=O)C1=CC(O)=C(O)C(O)=C1 LNTHITQWFMADLM-UHFFFAOYSA-N 0.000 claims description 6
- 239000007923 nasal drop Substances 0.000 claims description 5
- 229920002770 condensed tannin Polymers 0.000 claims description 4
- 159000000001 potassium salts Chemical class 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 3
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000003889 eye drop Substances 0.000 claims description 3
- 229920001461 hydrolysable tannin Polymers 0.000 claims description 3
- 239000007937 lozenge Substances 0.000 claims description 3
- 239000011777 magnesium Substances 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- 210000004877 mucosa Anatomy 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- PFTAWBLQPZVEMU-DZGCQCFKSA-N (+)-catechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-DZGCQCFKSA-N 0.000 claims description 2
- ADRVNXBAWSRFAJ-UHFFFAOYSA-N catechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3ccc(O)c(O)c3 ADRVNXBAWSRFAJ-UHFFFAOYSA-N 0.000 claims description 2
- 235000005487 catechin Nutrition 0.000 claims description 2
- 229950001002 cianidanol Drugs 0.000 claims description 2
- 239000006196 drop Substances 0.000 claims description 2
- 235000004515 gallic acid Nutrition 0.000 claims description 2
- 229940074391 gallic acid Drugs 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract description 9
- 150000002500 ions Chemical class 0.000 abstract description 4
- 229920001864 tannin Polymers 0.000 abstract description 2
- 235000018553 tannin Nutrition 0.000 abstract description 2
- 239000001648 tannin Substances 0.000 abstract description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 abstract 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 12
- 239000011780 sodium chloride Substances 0.000 description 6
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 5
- 239000001095 magnesium carbonate Substances 0.000 description 5
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- XMOCLSLCDHWDHP-IUODEOHRSA-N epi-Gallocatechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@H]2O)=CC(O)=C(O)C(O)=C1 XMOCLSLCDHWDHP-IUODEOHRSA-N 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 4
- 239000003814 drug Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000001509 sodium citrate Substances 0.000 description 3
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 description 2
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 2
- XMOCLSLCDHWDHP-UHFFFAOYSA-N L-Epigallocatechin Natural products OC1CC2=C(O)C=C(O)C=C2OC1C1=CC(O)=C(O)C(O)=C1 XMOCLSLCDHWDHP-UHFFFAOYSA-N 0.000 description 2
- ZRVSAJIGCDWADZ-UHFFFAOYSA-N Leucoanthocyanin Natural products OCC1OC(CC(O)C1O)OC2C(O)c3c(O)cc(O)cc3OC2c4ccc(O)c(O)c4 ZRVSAJIGCDWADZ-UHFFFAOYSA-N 0.000 description 2
- 206010028735 Nasal congestion Diseases 0.000 description 2
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 description 2
- 241001080526 Vertica Species 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- DZYNKLUGCOSVKS-UHFFFAOYSA-N epigallocatechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3cc(O)c(O)c(O)c3 DZYNKLUGCOSVKS-UHFFFAOYSA-N 0.000 description 2
- 229940012356 eye drops Drugs 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 229940100662 nasal drops Drugs 0.000 description 2
- 229930014626 natural product Natural products 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 229910000027 potassium carbonate Inorganic materials 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 102220240796 rs553605556 Human genes 0.000 description 2
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 description 2
- 229940013618 stevioside Drugs 0.000 description 2
- 235000019202 steviosides Nutrition 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- TUSDEZXZIZRFGC-UHFFFAOYSA-N 1-O-galloyl-3,6-(R)-HHDP-beta-D-glucose Natural products OC1C(O2)COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC1C(O)C2OC(=O)C1=CC(O)=C(O)C(O)=C1 TUSDEZXZIZRFGC-UHFFFAOYSA-N 0.000 description 1
- ATJXMQHAMYVHRX-CPCISQLKSA-N Ellagic acid Natural products OC1=C(O)[C@H]2OC(=O)c3cc(O)c(O)c4OC(=O)C(=C1)[C@H]2c34 ATJXMQHAMYVHRX-CPCISQLKSA-N 0.000 description 1
- AFSDNFLWKVMVRB-UHFFFAOYSA-N Ellagic acid Chemical compound OC1=C(O)C(OC2=O)=C3C4=C2C=C(O)C(O)=C4OC(=O)C3=C1 AFSDNFLWKVMVRB-UHFFFAOYSA-N 0.000 description 1
- 229920002079 Ellagic acid Polymers 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 239000001263 FEMA 3042 Substances 0.000 description 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 1
- LRBQNJMCXXYXIU-PPKXGCFTSA-N Penta-digallate-beta-D-glucose Natural products OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-PPKXGCFTSA-N 0.000 description 1
- 235000004347 Perilla Nutrition 0.000 description 1
- 244000124853 Perilla frutescens Species 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 239000000150 Sympathomimetic Substances 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 244000299461 Theobroma cacao Species 0.000 description 1
- 235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 description 1
- 235000005767 Theobroma cacao ssp. sphaerocarpum Nutrition 0.000 description 1
- 102100031083 Uteroglobin Human genes 0.000 description 1
- 108090000203 Uteroglobin Proteins 0.000 description 1
- 239000003732 agents acting on the eye Substances 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 235000010208 anthocyanin Nutrition 0.000 description 1
- 239000004410 anthocyanin Substances 0.000 description 1
- 229930002877 anthocyanin Natural products 0.000 description 1
- 150000004636 anthocyanins Chemical class 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- 239000000043 antiallergic agent Substances 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 229940124630 bronchodilator Drugs 0.000 description 1
- 235000001046 cacaotero Nutrition 0.000 description 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000000645 desinfectant Substances 0.000 description 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 235000004132 ellagic acid Nutrition 0.000 description 1
- 229960002852 ellagic acid Drugs 0.000 description 1
- 239000003172 expectorant agent Substances 0.000 description 1
- 230000003419 expectorant effect Effects 0.000 description 1
- 239000003885 eye ointment Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000002070 germicidal effect Effects 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229960002373 loxoprofen Drugs 0.000 description 1
- WORCCYVLMMTGFR-UHFFFAOYSA-M loxoprofen sodium Chemical compound [Na+].C1=CC(C(C([O-])=O)C)=CC=C1CC1C(=O)CCC1 WORCCYVLMMTGFR-UHFFFAOYSA-M 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- FAARLWTXUUQFSN-UHFFFAOYSA-N methylellagic acid Natural products O1C(=O)C2=CC(O)=C(O)C3=C2C2=C1C(OC)=C(O)C=C2C(=O)O3 FAARLWTXUUQFSN-UHFFFAOYSA-N 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- 210000002850 nasal mucosa Anatomy 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 229940023490 ophthalmic product Drugs 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- FZHLWVUAICIIPW-UHFFFAOYSA-M sodium gallate Chemical compound [Na+].OC1=CC(C([O-])=O)=CC(O)=C1O FZHLWVUAICIIPW-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000001975 sympathomimetic effect Effects 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- LRBQNJMCXXYXIU-NRMVVENXSA-N tannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-NRMVVENXSA-N 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、使用感の優れた粘
膜適用医薬組成物に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a pharmaceutical composition for mucosal application having an excellent feeling upon use.
【０００２】[0002]
【従来の技術】ポリフェノール化合物は、茶、カカオ、
シソなど植物界に広く分布する天然化合物であり、抗菌
活性、抗ウイルス活性、抗炎症活性、収斂活性等の多く
の活性を有することから、医薬品としての適用が期待さ
れている。2. Description of the Related Art Polyphenol compounds include tea, cacao,
It is a natural compound widely distributed in the plant kingdom such as perilla, and has many activities such as antibacterial activity, antiviral activity, anti-inflammatory activity, and astringent activity, so that it is expected to be applied as a pharmaceutical.
【０００３】しかし、ポリフェノール化合物は粘膜局所
に直接適用した際、不快感を起こす独特な刺激を生じる
ことが知られており、この不快な刺激を軽減する方法に
ついてはこれまで報告がない。[0003] However, it is known that a polyphenol compound, when applied directly to a mucous membrane, produces a unique stimulus that causes discomfort, and there is no report on a method for reducing this unpleasant stimulus.
【０００４】[0004]
【発明が解決しようとする課題】本発明は、使用時にお
ける不快な刺激を軽減した粘膜適用医薬組成物を提供す
ることを目的とする。SUMMARY OF THE INVENTION An object of the present invention is to provide a pharmaceutical composition for mucosal application which reduces unpleasant irritation during use.
【０００５】[0005]
【課題を解決するための手段】本発明者らは、上記目的
のため鋭意検討を重ねた結果、意外にもある種のイオン
を配合することにより粘膜適用時に惹起されるポリフェ
ノール化合物の不快な刺激が軽減されること見いだし、
発明を完成するに至った。Means for Solving the Problems The inventors of the present invention have conducted intensive studies for the above-mentioned purpose, and as a result, unexpectedly, the unpleasant stimulation of the polyphenol compound caused by the addition of certain ions when applied to mucous membranes. Is reduced,
The invention has been completed.
【０００６】すなわち、本発明はマグネシウムイオン、
ナトリウムイオン及びカリウムイオンからなる群より選
ばれる１種または２種以上を含有することを特徴とす
る、ポリフェノール化合物含有の粘膜適用医薬組成物で
ある。That is, the present invention provides a magnesium ion,
A pharmaceutical composition for mucosal application containing a polyphenol compound, comprising one or more selected from the group consisting of sodium ions and potassium ions.
【０００７】[0007]
【課題を解決するための手段】本発明において使用する
ポリフェノール化合物とは、その分子中に多価フェノー
ルの部分構造を１個以上含有する有機化合物であって、
縮合型タンニン、加水分解型タンニン等を挙げることが
できる。縮合型タンニンの例としては、カテキン、エピ
ガロカテキン、ロイコアントシアニン等を挙げることが
できる。また、加水分解型タンニンの例としては、没食
子酸、没食子酸塩、エラグ酸等を挙げることができる。The polyphenol compound used in the present invention is an organic compound containing at least one polyhydric phenol partial structure in its molecule,
Condensed tannin, hydrolyzed tannin and the like can be mentioned. Examples of the condensed tannin include catechin, epigallocatechin, leucoanthocyanin and the like. Examples of the hydrolyzable tannin include gallic acid, gallic acid salt, ellagic acid and the like.
【０００８】また、ポリフェノール化合物の有効配合量
は、その使用目的および投与方法によって異なるが、成
人一日当たり１〜６００ｍｇであり、好ましくは１０〜
２５０ｍｇである。The effective amount of the polyphenol compound varies depending on the purpose of use and the method of administration.
250 mg.
【０００９】有機酸または無機酸とのナトリウム塩、マ
グネシウム塩及びカリウム塩とは、溶解した際にナトリ
ウムイオン、マグネシウムイオンまたはカリウムイオン
を生じる塩であり、薬理学的に許容されるものであれば
よく、具体的には、例えばクエン酸ナトリウム、塩化ナ
トリウム、炭酸カリウム、炭酸マグネシウム等を挙げる
ことができる。また、これらの塩は単独で配合しても、
２種以上混合して配合してもよい。The sodium, magnesium and potassium salts with an organic or inorganic acid are salts which, when dissolved, generate sodium, magnesium or potassium ions, provided that they are pharmacologically acceptable. More specifically, specific examples include sodium citrate, sodium chloride, potassium carbonate, magnesium carbonate and the like. Also, even if these salts are blended alone,
You may mix and mix 2 or more types.
【００１０】本発明の粘膜適用医薬組成物が含有するマ
グネシウムイオン、ナトリウムイオン、カリウムイオン
の合計量は、ポリフェノール化合物１Ｍに対し、０．０
０５〜１０００Ｍであり、好ましくは０．０２５〜４５
０Ｍ、さらに好ましくは２〜２００Ｍである。The total amount of magnesium ion, sodium ion and potassium ion contained in the pharmaceutical composition for mucosal application of the present invention is 0.0
05-1000M, preferably 0.025-45M
0M, more preferably 2 to 200M.
【００１１】粘膜適用医薬組成物とは、咽頭粘膜、鼻粘
膜、眼粘膜、口腔粘膜などの粘膜に直接使用される薬剤
であり、風邪予防薬、風邪薬、鎮咳去痰薬、鼻炎用薬、
咽喉頭局所用薬、局所鎮痛薬、眼科用薬、花粉症用薬等
として使用されるものである。[0011] The mucosa-applied pharmaceutical composition is a drug used directly on mucous membranes such as the pharyngeal mucosa, nasal mucosa, ocular mucosa, and oral mucosa.
It is used as a pharyngolaryngeal topical drug, topical analgesic, ophthalmic drug, hay fever drug and the like.
【００１２】本発明の粘膜適用医薬組成物は、非ステロ
イド性抗炎症薬、抗アレルギー薬、抗ヒスタミン薬、消
炎酵素類、気管支拡張薬、鎮咳薬、去痰薬、交感神経興
奮薬、抗コリン薬、カフェイン類、ビタミン薬、殺菌消
毒薬、生薬類、他の天然化合物、香料等の成分を適宜に
配合することができる。[0012] The pharmaceutical composition for mucosal application of the present invention comprises a nonsteroidal anti-inflammatory drug, an antiallergic drug, an antihistamine, an anti-inflammatory enzyme, a bronchodilator, an antitussive, an expectorant, a sympathomimetic, an anticholinergic. Ingredients such as caffeine, vitamins, germicidal disinfectants, herbal medicines, other natural compounds, fragrances and the like can be appropriately blended.
【００１３】本発明の粘膜適用医薬組成物は、常法によ
り調製することができる。固形剤の場合には必要に応じ
て賦形剤、滑沢剤、崩壊剤等を使用することができ、液
剤の場合には界面活性剤、溶解補助剤、緩衝剤等を使用
することができる。また、この他保存剤、色素、着色剤
等も使用することができる。The pharmaceutical composition for mucosal application of the present invention can be prepared by a conventional method. In the case of a solid preparation, an excipient, a lubricant, a disintegrant and the like can be used as necessary, and in the case of a liquid preparation, a surfactant, a solubilizing agent, a buffer and the like can be used. . In addition, preservatives, dyes, coloring agents and the like can also be used.
【００１４】本発明の粘膜適用医薬組成物は、トローチ
剤、ドロップ剤、舐剤、口腔内溶解剤、点鼻薬、点眼
薬、洗眼薬、眼軟膏、洗鼻薬の形態で供される。The pharmaceutical composition for mucosal application of the present invention is provided in the form of a troche, drop, lozenge, oral dissolving agent, nasal drop, eye drops, eyewash, eye ointment, nasal wash.
【００１５】[0015]
【発明の効果】本発明により、使用時における不快な刺
激の軽減されたポリフェノール化合物含有の粘膜適用医
薬組成物の提供が可能となった。Industrial Applicability According to the present invention, it has become possible to provide a polyphenol compound-containing pharmaceutical composition for mucosal application containing less unpleasant irritation during use.
【００１６】実施例１ 下記の各成分及び分量を秤量しＶ型混合機で１０分間均
一に混合した後、ヤリヤ粉砕器（スクリーン０．７ｍ
ｍ）で粉砕した。得られた粉砕混合物をｖｅｒｔｉｃａ
ｌ造粒機に入れ、ヌレード回転数１５０ｒｐｍ、クロス
スクリュー１０００ｒｐｍの条件下でエタノール６００
ｇを加え造粒した。造粒物を流動層乾燥器（ＰＬＯ−
１）に入れ、吸気温度７０℃で１時間乾燥させた。乾燥
後２４メッシュの篩を用いて篩過し、口腔内溶解剤とし
た。Example 1 The following components and amounts were weighed and uniformly mixed with a V-type mixer for 10 minutes.
m). The resulting milled mixture is vertica
l into a granulator, ethanol 600 rpm under the conditions of a rotation speed of 150 rpm and a cross screw of 1000 rpm.
g was added and granulated. The granulated product is fluidized bed dryer (PLO-
1) and dried for 1 hour at an intake air temperature of 70 ° C. After drying, it was sieved using a 24 mesh sieve to obtain an oral dissolving agent.
【００１７】 タンニン酸 ５００ｇ ステアリン酸マグネシウム ６００ｇ 炭酸マグネシウム １５０ｇ クエン酸ナトリウム １００ｇ 塩化ナトリウム ２０ｇ ステビオシド ３０ｇ。Tannic acid 500 g Magnesium stearate 600 g Magnesium carbonate 150 g Sodium citrate 100 g Sodium chloride 20 g Stevioside 30 g
【００１８】実施例２ 下記の各成分及び分量を秤量しＶ型混合機で１０分間均
一に混合した後、ヤリヤ粉砕器（スクリーン０．７ｍ
ｍ）で粉砕した。得られた粉砕混合物をｖｅｒｔｉｃａ
ｌ造粒機に入れ、ヌレード回転数１５０ｒｐｍ、クロス
スクリュー１０００ｒｐｍの条件下でエタノール６００
ｇを加え造粒した。造粒物を流動層乾燥器（ＰＬＯ−
１）に入れ、吸気温度７０℃で１時間乾燥させた。乾燥
後２４メッシュの篩を用いて篩過し、トローチ剤とし
た。Example 2 The following components and amounts were weighed and uniformly mixed with a V-type mixer for 10 minutes.
m). The resulting milled mixture is vertica
l into a granulator, ethanol 600 rpm under the conditions of a rotation speed of 150 rpm and a cross screw of 1000 rpm.
g was added and granulated. The granulated product is fluidized bed dryer (PLO-
The sample was placed in 1) and dried at an intake air temperature of 70 ° C. for 1 hour. After drying, the mixture was sieved using a 24-mesh sieve to give a troche.
【００１９】 エピガロカテキン ２５０ｇ ステアリン酸マグネシウム ４５０ｇ 炭酸カリウム １５０ｇ クエン酸ナトリウム １００ｇ 塩化ナトリウム ２０ｇ ステビオシド ３０ｇ。Epigallocatechin 250 g Magnesium stearate 450 g Potassium carbonate 150 g Sodium citrate 100 g Sodium chloride 20 g Stevioside 30 g
【００２０】実施例３ 下記の各成分及び分量を秤量し均一に混合した後、滅菌
精製水に溶解し洗眼薬とした。Example 3 The following components and amounts were weighed and uniformly mixed, and then dissolved in sterile purified water to prepare an eyewash.
【００２１】 没食子酸ナトリウム １００ｍＭ 炭酸マグネシウム １００ｍＭ 塩化ナトリウム ５０ｍＭ グリチルリチン酸ジカリウム １５０ｍＭ。Sodium gallate 100 mM Magnesium carbonate 100 mM Sodium chloride 50 mM Dipotassium glycyrrhizinate 150 mM
【００２２】実施例４ 下記の各成分及び分量を秤量し均一に混合した後、精製
水に溶解して全量を５０Ｌとし、点鼻薬とした。Example 4 The following components and amounts were weighed and uniformly mixed, and then dissolved in purified water to make a total volume of 50 L, which was used as nasal drops.
【００２３】 ロイコアントシアニン ５００ｇ 炭酸マグネシウム １００ｇ 塩化ナトリウム １０ｇ ｔｗｅｅｎ８０ １０ｇ。Leucoanthocyanin 500 g Magnesium carbonate 100 g Sodium chloride 10 g Tween 80 10 g.
【００２４】実施例５ 下記の各成分及び分量を秤量し均一に混合した後、滅菌
精製水に溶解して全量を５０Ｌとし、点眼薬とした。Example 5 The following components and amounts were weighed and uniformly mixed, and then dissolved in sterile purified water to make a total volume of 50 L, which was used as eye drops.
【００２５】 アントシアニン ２５０ｍＭ 炭酸マグネシウム １００ｍＭ 塩化ナトリウム ５０ｍＭ ロキソプロフェンナトリウム １８０ｍＭ グリチルリチン酸ジカリウム １００ｍＭ。Anthocyanin 250 mM Magnesium carbonate 100 mM Sodium chloride 50 mM Loxoprofen sodium 180 mM Dipotassium glycyrrhizinate 100 mM
【００２６】試験例１ 使用感の改善に関する検討 花粉症による鼻閉（鼻づまり）を訴える患者２１名（男
性１０名、女性１１名、平均年齢３２．３歳）に、ロイ
コアントシアニン及びｔｗｅｅｎ８０のみの処方（抜き
処方）のものを事前に経鼻的に投与し、その２時間後に
実施例４の点鼻薬を投与し、鼻腔内違和感の相対的強度
を評価した。Test Example 1 Investigation on improvement of feeling of use 21 patients (10 men, 11 women, average age 32.3 years) complaining of nasal congestion (nose congestion) due to hay fever were treated with leukoanthocyanin and tween 80 alone. The prescription (without prescription) was administered nasally in advance, and two hours later, the nasal drops of Example 4 were administered to evaluate the relative strength of intranasal discomfort.
【００２７】違和感の程度は、６段階評価（抜き処方投
与１分後の強い違和感を１００、比較的強い違和感を４
８、中程度の違和感を２５、比較的弱い違和感を１０、
かすかに感じる違和感を４、違和感を感じない場合を
０）として定量した。The degree of discomfort was evaluated on a six-point scale (a strong discomfort one minute after administration of the prescription without disability was 100, and a relatively strong discomfort was 4
8, medium discomfort 25, relatively weak discomfort 10,
The slight discomfort was quantified as 4, and the case where no discomfort was felt was quantified as 0).
【００２８】実施例４の点鼻薬の投与前、投与１分後、
投与１０分後の鼻腔内違和感の相対的強度の推移を数値
化した。Before administration of the nasal drop of Example 4, 1 minute after administration,
Changes in the relative intensity of intranasal discomfort 10 minutes after administration were quantified.
【００２９】その結果、２１名中１９名に咽頭部の痛み
を低下させる実感があることが明らかとなった。以下
に、測定平均値（標準偏差）の推移を示す。[0029] As a result, it became clear that 19 out of the 21 patients felt that the pain of the pharynx was reduced. The transition of the measured average value (standard deviation) is shown below.
【００３０】 投与前 ４８．７±６．９ 投与１分後 １６．５±５．５** 投与１０分後 ２８．９±７．７* ※投与前に比べ、**ｐ＜０．００１、*ｐ＜０．０１で
有意差あり。Before administration 48.7 ± 6.9 1 minute after administration 16.5 ± 5.5 ** 10 minutes after administration 28.9 ± 7.7 * * Compared to before administration, ** p <0.001 * P <0.01 with significant difference.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 ＦＩ テーマコート゛(参考） Ａ６１Ｐ 27/02 Ａ６１Ｐ 27/02 27/16 27/16 29/00 29/00 31/04 31/04 31/12 31/12 (72)発明者 角田 健司 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 Ｆターム(参考） 4C076 AA11 AA36 BB01 BB03 BB21 BB24 BB25 CC04 CC07 CC10 CC29 CC31 CC35 DD09 DD22 DD23 DD25 DD41 DD68 FF67 4C206 AA01 AA02 CA17 CA20 DA01 DA19 MA02 MA03 MA05 MA30 MA72 MA76 MA77 MA78 MA79 NA06 NA07 ZB11 ZB33 ZB35 ZC21 ──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. 7 Identification symbol FI theme coat ゛ (Reference) A61P 27/02 A61P 27/02 27/16 27/16 29/00 29/00 31/04 31/04 31 / 12 31/12 (72) Inventor Kenji Tsunoda 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd.F-term (reference) 4C076 AA11 AA36 BB01 BB03 BB21 BB24 BB25 CC04 CC07 CC10 CC29 CC31 CC35 DD09 DD22 DD23 DD25 DD41 DD68 FF67 4C206 AA01 AA02 CA17 CA20 DA01 DA19 MA02 MA03 MA05 MA30 MA72 MA76 MA77 MA78 MA79 NA06 NA07 ZB11 ZB33 ZB35 ZC21
Claims (13)
びカリウムイオンからなる群より選ばれる１種または２
種以上を含有することを特徴とする、ポリフェノール化
合物含有の粘膜適用医薬組成物。1. One or two selected from the group consisting of magnesium ion, sodium ion and potassium ion.
A mucosa-containing pharmaceutical composition containing a polyphenol compound, comprising at least one species.
トリウム塩及びカリウム塩からなる群より選ばれる１種
または２種以上を配合することを特徴とする、ポリフェ
ノール化合物含有の粘膜適用医薬組成物。2. A pharmaceutical composition for mucosal application containing a polyphenol compound, comprising one or more selected from the group consisting of magnesium salts, sodium salts and potassium salts of organic or inorganic acids.
びカリウム塩からなる群より選ばれる１種または２種以
上を配合することを特徴とする、ポリフェノール化合物
含有の粘膜適用医薬組成物。3. A pharmaceutical composition for mucosal application containing a polyphenol compound, comprising one or more selected from the group consisting of magnesium, sodium and potassium salts of inorganic acids.
ニンである請求項１〜３のいずれかに記載の粘膜適用医
薬組成物。4. The pharmaceutical composition for mucosal application according to claim 1, wherein the polyphenol compound is a hydrolyzable tannin.
である請求項１〜３のいずれかに記載の粘膜適用医薬組
成物。5. The pharmaceutical composition for mucosal application according to claim 1, wherein the polyphenol compound is a condensed tannin.
酸誘導体またはこれらの塩である請求項４記載の粘膜適
用医薬組成物。6. The pharmaceutical composition for mucosal application according to claim 4, wherein the hydrolyzable tannin is gallic acid, gallic acid derivative or a salt thereof.
類縁物質、ロイコアントシアニジンもしくはその類縁物
質、またはこれら化合物の塩である請求項５記載の粘膜
適用医薬組成物。7. The pharmaceutical composition for mucosal application according to claim 5, wherein the condensed tannin is catechin or an analog thereof, leukoanthocyanidin or an analog thereof, or a salt of these compounds.
イオン、カリウムイオンの合計量が、ポリフェノール化
合物１Ｍに対して０．００５〜１０００Ｍである請求項
１〜７のいずれかに記載の粘膜適用医薬組成物。8. The pharmaceutical composition for mucosal application according to claim 1, wherein the total amount of magnesium ion, sodium ion and potassium ion contained is 0.005 to 1000 M per 1 M of the polyphenol compound.
れかに記載の粘膜適用医薬組成物。9. The pharmaceutical composition for mucosal application according to claim 1, which is applied to the pharyngeal mucosa.
腔内溶解剤である請求項９記載の粘膜適用医薬組成物。10. The pharmaceutical composition for mucosal application according to claim 9, which is a lozenge, a drop, a lozenge or an oral dissolving agent.
記載の粘膜適用医薬組成物。11. The pharmaceutical composition for mucosal application according to claim 1, which is a nasal drop.
記載の粘膜適用医薬組成物。12. The pharmaceutical composition for mucosal application according to claim 1, which is an eye drop.
ナトリウム塩及びカリウム塩からなる群より選ばれる１
種または２種以上を配合することを特徴とする、ポリフ
ェノール化合物含有の粘膜適用医薬組成物の不快な刺激
を軽減する方法。13. A magnesium salt of an organic or inorganic acid,
1 selected from the group consisting of sodium salts and potassium salts
A method for reducing unpleasant irritation of a mucosally-applied pharmaceutical composition containing a polyphenol compound, which comprises mixing at least two or more species.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11216120A JP2001039866A (en) | 1999-07-30 | 1999-07-30 | Pharmaceutical composition for application to mucous membrane |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11216120A JP2001039866A (en) | 1999-07-30 | 1999-07-30 | Pharmaceutical composition for application to mucous membrane |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2001039866A true JP2001039866A (en) | 2001-02-13 |
Family
ID=16683574
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP11216120A Withdrawn JP2001039866A (en) | 1999-07-30 | 1999-07-30 | Pharmaceutical composition for application to mucous membrane |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2001039866A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008053942A1 (en) * | 2006-10-31 | 2008-05-08 | San-Ei Gen F.F.I., Inc. | Composition for throat |
-
1999
- 1999-07-30 JP JP11216120A patent/JP2001039866A/en not_active Withdrawn
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008053942A1 (en) * | 2006-10-31 | 2008-05-08 | San-Ei Gen F.F.I., Inc. | Composition for throat |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10195239B2 (en) | Extract of Trigonella foenum-graecum | |
| CA1207233A (en) | Nystatin pastille formulation and method | |
| EP1370247B1 (en) | Taste masked pharmaceutical compositions | |
| KR20000052950A (en) | Chewing gum containing colloidal bismuth subcitrate | |
| JP2004511561A (en) | Pharmaceutical composition | |
| JP2002537070A (en) | Bioadhesive antimicrobial wound healing composition | |
| KR101490721B1 (en) | Liquid Formulation for Deferiprone With Palatable Taste | |
| TW201244718A (en) | A pharmaceutical composition for treating a disease in the oral cavity comprising rebamipide | |
| JP2000095675A (en) | Oral solid pharmaceutical composition for treating rhinitis of intraoral soluble type or mastication type | |
| CN110314110A (en) | A kind of effervescent tablet type mouthwash and preparation method thereof | |
| JPH04159223A (en) | Emetocathartic composition | |
| AU2013346766B2 (en) | Effervescent tablet | |
| JP4366527B2 (en) | Amino acid composition suitable for treatment for the healing and / or repair of trauma and injury, especially for applications in the ophthalmic field | |
| JP2001031562A (en) | Liquid preparation for internal use | |
| NO309965B1 (en) | Oral pharmaceutical anti-cough preparation | |
| Mohire et al. | Novel approaches in development of metronidazole orodispersible tablets | |
| Sosa et al. | Topical antiinflammatory activity of an innovative aqueous formulation of actichelated® propolis vs two commercial propolis formulations | |
| JP2001151677A (en) | Composition for pharyngeal use | |
| JP2001039866A (en) | Pharmaceutical composition for application to mucous membrane | |
| KR100381622B1 (en) | Irritating-reduced oral delivery formulations of basic drugs | |
| EP3708153A1 (en) | Solution preparation for aerosol inhalation of carbocisteine, and preparation method therefor | |
| TW201542240A (en) | Liquid pharmaceutical composition for oral administration comprising FEXOFENADINE | |
| JPH0563452B2 (en) | ||
| JP2000327573A (en) | Composition for applying to mucosa | |
| US3914433A (en) | Method of relieving the discomfort of pharyngitis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20060518 |