JP2021172643A - Iodine-based liquid preparation and method for producing the same - Google Patents
Iodine-based liquid preparation and method for producing the same Download PDFInfo
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- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 title claims abstract description 122
- 229910052740 iodine Inorganic materials 0.000 title claims abstract description 122
- 239000011630 iodine Substances 0.000 title claims abstract description 122
- 238000002360 preparation method Methods 0.000 title claims abstract description 57
- 239000007788 liquid Substances 0.000 title claims abstract description 47
- 238000004519 manufacturing process Methods 0.000 title claims description 17
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 claims abstract description 24
- AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims abstract description 19
- 239000000920 calcium hydroxide Substances 0.000 claims abstract description 18
- 229910001861 calcium hydroxide Inorganic materials 0.000 claims abstract description 18
- BRPQOXSCLDDYGP-UHFFFAOYSA-N calcium oxide Chemical compound [O-2].[Ca+2] BRPQOXSCLDDYGP-UHFFFAOYSA-N 0.000 claims abstract description 18
- 239000000292 calcium oxide Substances 0.000 claims abstract description 18
- ODINCKMPIJJUCX-UHFFFAOYSA-N calcium oxide Inorganic materials [Ca]=O ODINCKMPIJJUCX-UHFFFAOYSA-N 0.000 claims abstract description 18
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 14
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 claims abstract description 12
- 208000015181 infectious disease Diseases 0.000 claims abstract description 11
- 208000030507 AIDS Diseases 0.000 claims abstract description 10
- 230000003449 preventive effect Effects 0.000 claims abstract description 10
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims description 39
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 9
- 238000002156 mixing Methods 0.000 claims description 7
- 229940124597 therapeutic agent Drugs 0.000 claims description 7
- 208000036142 Viral infection Diseases 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 238000003756 stirring Methods 0.000 claims description 6
- 230000009385 viral infection Effects 0.000 claims description 6
- CPKVUHPKYQGHMW-UHFFFAOYSA-N 1-ethenylpyrrolidin-2-one;molecular iodine Chemical compound II.C=CN1CCCC1=O CPKVUHPKYQGHMW-UHFFFAOYSA-N 0.000 claims description 5
- 229920000153 Povidone-iodine Polymers 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 229960001621 povidone-iodine Drugs 0.000 claims description 5
- 241000711573 Coronaviridae Species 0.000 abstract description 7
- 208000035473 Communicable disease Diseases 0.000 abstract description 4
- 230000001225 therapeutic effect Effects 0.000 abstract description 4
- 208000025721 COVID-19 Diseases 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 14
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 7
- 229910052791 calcium Inorganic materials 0.000 description 7
- 239000011575 calcium Substances 0.000 description 7
- 230000000694 effects Effects 0.000 description 5
- 239000000825 pharmaceutical preparation Substances 0.000 description 3
- 229940127557 pharmaceutical product Drugs 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- FVAUCKIRQBBSSJ-UHFFFAOYSA-M sodium iodide Chemical compound [Na+].[I-] FVAUCKIRQBBSSJ-UHFFFAOYSA-M 0.000 description 3
- 238000004659 sterilization and disinfection Methods 0.000 description 3
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 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 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 description 2
- 206010052428 Wound Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 150000008044 alkali metal hydroxides Chemical class 0.000 description 2
- -1 alkali metal salt Chemical class 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- 150000001342 alkaline earth metals Chemical class 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 239000000645 desinfectant Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 235000010445 lecithin Nutrition 0.000 description 2
- 239000000787 lecithin Substances 0.000 description 2
- 229940067606 lecithin Drugs 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 210000001685 thyroid gland Anatomy 0.000 description 2
- 230000003612 virological effect Effects 0.000 description 2
- 235000014653 Carica parviflora Nutrition 0.000 description 1
- 244000132059 Carica parviflora Species 0.000 description 1
- 206010073306 Exposure to radiation Diseases 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 235000006173 Larrea tridentata Nutrition 0.000 description 1
- 244000073231 Larrea tridentata Species 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 241001263478 Norovirus Species 0.000 description 1
- 206010073938 Ophthalmic herpes simplex Diseases 0.000 description 1
- 241000237502 Ostreidae Species 0.000 description 1
- 241000237509 Patinopecten sp. Species 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 206010036790 Productive cough Diseases 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 208000025865 Ulcer Diseases 0.000 description 1
- YADZBEISHVCBSJ-UHFFFAOYSA-N [I].OCC(O)CO Chemical compound [I].OCC(O)CO YADZBEISHVCBSJ-UHFFFAOYSA-N 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 229940030225 antihemorrhagics Drugs 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 239000003139 biocide Substances 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 238000001354 calcination Methods 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 239000003026 cod liver oil Substances 0.000 description 1
- 235000012716 cod liver oil Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000018823 dietary intake Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 210000003278 egg shell Anatomy 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 239000002874 hemostatic agent Substances 0.000 description 1
- 208000013403 hyperactivity Diseases 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 210000000214 mouth Anatomy 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 235000020636 oyster Nutrition 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 229940068984 polyvinyl alcohol Drugs 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229940081540 potassium iodide pill Drugs 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 235000020637 scallop Nutrition 0.000 description 1
- 235000009518 sodium iodide Nutrition 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000006379 syphilis Diseases 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 208000013076 thyroid tumor Diseases 0.000 description 1
- 206010044008 tonsillitis Diseases 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000397 ulcer Toxicity 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本発明は、ヨウ素系液体製剤、特にウイルス感染病又はエイズ感染病の治療剤として用いられるヨウ素系液体製剤及びその製造方法に関する。 The present invention relates to an iodine-based liquid preparation, particularly an iodine-based liquid preparation used as a therapeutic agent for a viral infection disease or an AIDS infection disease, and a method for producing the same.
ヨウ素あるいはヨウ化カリウム、ヨウ化ナトリウム等を含有するヨウ素製剤は、周知のように、古くから皮膚表面の一般消毒、創傷、潰瘍の殺菌・消毒等に広く用いられており、その後もその製剤の改良工夫が続けられ、多くの特許出願がなされてきている。
また、特にヨウ素の有機複合化合物であるヨードグリセリン、ポリビニルアルコールヨウ素あるいはポビドンヨードなどを含有するヨウ素製剤は、皮膚表面の一般消毒のほか、咽頭炎、扁桃炎等の口腔創傷の感染予防、口腔内消毒に或いは角膜ヘルペス、洗眼殺菌などの予防・治療剤として市販されている。
最近では、ヨウ素成分として、ポビドンヨードを含有せしめたヨウ素製剤の開発が多くなされるようになってきており、ゼラチン及び糖類等にポビドンヨードを含有せしめた外用剤も提案されている(例えば、特許文献1、2参照)。
また、殺ウイルス効果に着目して、ヨウ素分として0.6〜0.01重量%のヨウ素及び/又はヨウ素のアルカリ金属塩を含有する膣又は口腔粘膜用水性消毒液が提案されている(例えば、特許文献3参照)。
As is well known, iodine preparations containing iodine, potassium iodide, sodium iodide, etc. have been widely used for general disinfection of skin surfaces, sterilization and disinfection of wounds and ulcers, etc. Improvements and ingenuity have been continued, and many patent applications have been filed.
In particular, iodine preparations containing iodine glycerin, polyvinyl alcohol iodine, povidone iodine, etc., which are organic composite compounds of iodine, not only disinfect the skin surface in general, but also prevent infection of oral wounds such as pharyngitis and tonsillitis, and disinfect the oral cavity. It is commercially available as a preventive / therapeutic agent for iodine, corneal herpes, eye wash sterilization, etc.
Recently, many iodine preparations containing povidone iodine as an iodine component have been developed, and external preparations containing povidone iodine in gelatin, sugars and the like have also been proposed (for example, Patent Document 1). , 2).
Further, paying attention to the virus-killing effect, an aqueous disinfectant solution for vaginal or oral mucosa containing 0.6 to 0.01% by weight of iodine and / or an alkali metal salt of iodine as an iodine content has been proposed (for example). , Patent Document 3).
一方、医師による治療に用いられるヨウ素剤としてはヨウ素カリウム丸(ヨウ素分38mg/錠)、ヨウ化カリウム液(KI液ヨウ素分10mg)、ヨウ素レシチン(50〜100μg/錠)等があり、甲状腺機能亢進症を伴う甲状腺腫瘍(ヨウ化カリウム1日5〜50mg)、気管支炎及び喘息に伴う喀痰喀出困難症・第三期梅毒(ヨウ化カリウム1日0.3〜2.0g)等に使用されている。
また、アイソトープ131I放射性ヨード治療剤として甲状腺治療に活用され、更に原子力災害時における安定ヨウ素剤(放射線の内部被爆による甲状腺癌の予防:1日服用量ヨウ化カリウム100mg−ヨウ化カリウム丸2丸、ヨウ素分76mg−WHOは100mg)として推奨されている(例えば、非特許文献1参照)。
On the other hand, iodine agents used for treatment by doctors include potassium iodide pill (iodine content 38 mg / tablet), potassium iodide solution (KI solution iodine content 10 mg), iodine lecithin (50 to 100 μg / tablet), and thyroid function. Used for thyroid tumors with hyperactivity (potassium iodide 5 to 50 mg daily), bronchitis and asthma-related sputum production difficulty, stage 3 syphilis (potassium iodide 0.3 to 2.0 g daily), etc. ing.
In addition, it is used for thyroid treatment as an isotope 131I radioactive iodine therapeutic agent, and is also a stable iodine agent in the event of a nuclear disaster (prevention of thyroid cancer due to internal exposure to radiation: daily dose of potassium iodide 100 mg-potassium iodide maru 2 maru, Iodine content 76 mg-WHO is recommended as 100 mg) (see, for example, Non-Patent Document 1).
しかし、ヨウ素の摂取基準は所要量150μg/日、許容上限摂取量3mg/日(第6次日本人の栄養所要量の食事摂取基準)であり、服用ヨウ素薬剤の一日有効ヨウ素量はその利益と不利益(ヨウ素中毒症)を考慮して微量使用であり、最大で100mg(WHOや多くの諸外国における奨励服用量−安定ヨウ素剤の場合)とされている。ヨウ素は反応性が高く、人体に対して非常に強い毒性を示すことから劇薬に指定されており、従来の消毒薬或いは止血薬(ヨードチンキ等)用のヨウ素製剤においても1%以下の含有量のものとして使用され、また服用或いは注射用としても大量投与・長期運用による副作用の可能性のため慎重投与すべきとし、1日摂取量最大100mg以下で使用されている。
また、最近ではコロナウイルス科であるネコ腸コロナウイルスを用いた試験で、水酸化カルシウム水溶液が短時間(10秒)で強力な殺ウイルス効果を発揮することが報告されている。(例えば、非特許文献2参照)
However, the iodine intake standard is the required amount of 150 μg / day and the allowable upper limit intake of 3 mg / day (the dietary intake standard of the 6th Japanese nutritional requirement), and the daily effective iodine amount of the iodine drug taken is its benefit. In consideration of the disadvantage (iodine poisoning), it is used in a small amount, and the maximum dose is 100 mg (in the case of WHO and many foreign countries-recommended dose-stable iodine preparation). Iodine is designated as a powerful drug because it is highly reactive and extremely toxic to the human body, and even in conventional iodine preparations for disinfectants or hemostatic agents (iodine tincture, etc.), the content is 1% or less. It is used as an iodine, and it should be carefully administered even when taken or injected due to the possibility of side effects due to large doses and long-term operation, and it is used at a maximum daily intake of 100 mg or less.
Recently, in a test using a cat intestinal coronavirus, which belongs to the coronaviridae family, it has been reported that an aqueous solution of calcium hydroxide exerts a strong virus-killing effect in a short time (10 seconds). (See, for example, Non-Patent Document 2)
しかしながら、ウイルス感染病又はエイズ感染病に対して優れた予防効果及び治療効果を発揮するヨウ素系液体製剤は上市されていない。 However, iodine-based liquid preparations that exhibit excellent preventive and therapeutic effects against viral or AIDS-infected diseases have not been put on the market.
本発明者は鋭意研究の結果、COVID−19(新型コロナウイルス)などのウイルス感染病又はエイズ感染病に対して優れた予防効果及び治療効果を発揮するヨウ素系液体製剤を提供できる下記構成の発明を開発した。
〔1〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と、酸化カルシウム換算で0.05〜1.0重量%の水酸化カルシウムと、残部が水とからなることを特徴とするヨウ素系液体製剤。
〔2〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と、酸化カルシウム換算で0.05〜1.0重量%の水酸化カルシウムと、過酸化水素0.05〜1.0重量%、残部が水とからなることを特徴とするヨウ素系液体製剤。
〔3〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と、酸化カルシウム換算で0.05〜1.0重量%の水酸化カルシウムと、残部がエタノール濃度が70〜90vol%(容量%))のエタノール水とからなることを特徴とするヨウ素系液体製剤。
〔4〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と、酸化カルシウム換算で0.05〜1.0重量%の水酸化カルシウムと、過酸化水素0.05〜1.0重量%、残部がエタノール濃度が70〜90vol%(容量%))のエタノール水とからなることを特徴とするヨウ素系液体製剤。
〔5〕 ヨウ素が、無機ヨウ素又は有機ヨウ素であることを特徴とする〔1〕 〜〔4〕のいずれか1項に記載のヨウ素系液体製剤。
〔6〕 ヨウ素が、ヨウ素液(ヨウ素ヨウ化カリウム液)であることを特徴とする〔1〕 〜〔5〕のいずれか1項に記載のヨウ素系液体製剤。
〔7〕 ヨウ素系液体製剤がウイルス感染病又はエイズ感染病の予防剤又は治療剤であることを特徴とする〔1〕〜〔6〕のいずれか1項に記載のヨウ素系液体製剤。
〔8〕 ヨウ素換算で0.01〜1.0重量%のヨウ素を含有する水に、酸化カルシウム0.05〜1.0重量%を投入して撹拌混合することを特徴とするヨウ素系液体製剤の製造方法。
〔9〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と過酸化水素0.05〜1.0%を含有する水に、酸化カルシウム0.05〜1.0重量%を投入して撹拌混合することを特徴とするヨウ素系液体製剤の製造方法。
〔10〕 ヨウ素換算で0.01〜1.0重量%のヨウ素を含有するエタノール濃度が70〜90vol%(容量%))のエタノール水に、酸化カルシウム0.05〜1.0重量%を投入して撹拌混合することを特徴とするヨウ素系液体製剤の製造方法。
〔11〕 ヨウ素換算で0.01〜1.0重量%のヨウ素と過酸化水素0.05〜1.0%を含有するエタノール濃度が77〜88vol%(容量%))のエタノール水に、酸化カルシウム0.05〜1.0重量%を投入して撹拌混合することを特徴とするヨウ素系液体製剤の製造方法。
〔12〕 ヨウ素が、無機ヨウ素又は有機ヨウ素であることを特徴とする〔8〕 〜〔11〕のいずれか1項に記載のヨウ素系液体製剤の製造方法。
〔13〕 ヨウ素が、ヨウ素液(ヨウ素ヨウ化カリウム液)であることを特徴とする〔8〕〜〔12〕のいずれか1項に記載のヨウ素系液体製剤の製造方法。
〔14〕ヨウ素系液体製剤がウイルス感染病又はエイズ感染病の予防剤又は治療剤であることを特徴とする〔81〜〔13〕のいずれか1項に記載のヨウ素系液体製剤の製造方法。
As a result of diligent research, the present inventor can provide an iodine-based liquid preparation that exhibits excellent preventive and therapeutic effects against viral infectious diseases such as COVID-19 (new coronavirus) or AIDS infectious diseases. Was developed.
[1] Iodine characterized by containing 0.01 to 1.0% by weight of iodine in terms of iodine, 0.05 to 1.0% by weight of calcium hydroxide in terms of calcium oxide, and water as the balance. System liquid preparation.
[2] 0.01 to 1.0% by weight of iodine in terms of iodine, 0.05 to 1.0% by weight of calcium hydroxide in terms of calcium oxide, and 0.05 to 1.0% by weight of hydrogen peroxide. An iodine-based liquid preparation characterized in that the balance consists of water.
[3] 0.01 to 1.0% by weight of iodine in terms of iodine, 0.05 to 1.0% by weight of calcium hydroxide in terms of calcium oxide, and the balance of ethanol concentration is 70 to 90 vol% (volume%). )) An iodine-based liquid preparation characterized by being composed of ethanol water.
[4] 0.01 to 1.0% by weight of iodine in terms of iodine, 0.05 to 1.0% by weight of calcium hydroxide in terms of calcium oxide, and 0.05 to 1.0% by weight of hydrogen peroxide. An iodine-based liquid preparation characterized in that the balance is composed of ethanol water having an ethanol concentration of 70 to 90 vol% (volume%).
[5] The iodine-based liquid preparation according to any one of [1] to [4], wherein the iodine is inorganic iodine or organic iodine.
[6] The iodine-based liquid preparation according to any one of [1] to [5], wherein the iodine is an iodine solution (potassium iodide solution).
[7] The iodine-based liquid preparation according to any one of [1] to [6], wherein the iodine-based liquid preparation is a preventive agent or a therapeutic agent for a viral infection disease or an AIDS infection disease.
[8] An iodine-based liquid preparation characterized by adding 0.05 to 1.0% by weight of calcium oxide to water containing 0.01 to 1.0% by weight of iodine in terms of iodine and stirring and mixing. Manufacturing method.
[9] Calcium oxide 0.05 to 1.0% by weight is added to water containing 0.01 to 1.0% by weight of iodine and 0.05 to 1.0% hydrogen peroxide in terms of iodine. A method for producing an iodine-based liquid preparation, which comprises stirring and mixing.
[10] Calcium oxide 0.05 to 1.0% by weight is added to ethanol water containing 0.01 to 1.0% by weight of iodine in terms of iodine and having an ethanol concentration of 70 to 90 vol% (volume%)). A method for producing an iodine-based liquid preparation, which comprises stirring and mixing the mixture.
[11] Oxidized in ethanol water containing 0.01 to 1.0% by weight of iodine and 0.05 to 1.0% hydrogen peroxide in terms of iodine and having an ethanol concentration of 77 to 88 vol% (volume%)). A method for producing an iodine-based liquid preparation, which comprises adding 0.05 to 1.0% by weight of calcium and stirring and mixing.
[12] The method for producing an iodine-based liquid preparation according to any one of [8] to [11], wherein the iodine is inorganic iodine or organic iodine.
[13] The method for producing an iodine-based liquid preparation according to any one of [8] to [12], wherein the iodine is an iodine solution (potassium iodide solution).
[14] The method for producing an iodine-based liquid preparation according to any one of [81] to [13], wherein the iodine-based liquid preparation is a preventive agent or a therapeutic agent for a viral infection disease or an AIDS infection disease.
本発明の液体製剤は、水酸化カルシウムが溶解しているため、pHが8〜12.5のアルカリ性製剤であるが、カルシウムはアルカリ土類金属であり、ナトリウム等のアルカリ金属水酸化物のような皮膚に対する刺激性は少ない。
よって、本発明の製剤は刺激性が少なく、服用しやすいものである。
そして、本発明の液体製剤によれば、ヨウ素の殺ウイルス作用と水酸化カルシウムの殺ウイルス作用が相まってその感染を高効率で予防又は治療することができる。
さらに、過酸化水素を添加したものにあっては、液中にコロイド状の安定したヨウ素が存在するため、服用、飲用として安全に使用することができる。
また、水の代わりにエタノール水を用いた場合は、エタノールの殺ウイルス作用と相まって、その感染を高効率で予防又は治療することができる。
エイズ感染に対しても同様の予防効果及び治療効果が期待される。
The liquid preparation of the present invention is an alkaline preparation having a pH of 8 to 12.5 because calcium hydroxide is dissolved, but calcium is an alkaline earth metal and is like an alkali metal hydroxide such as sodium. Less irritating to the skin.
Therefore, the pharmaceutical product of the present invention is less irritating and easy to take.
According to the liquid preparation of the present invention, the virus-killing action of iodine and the virus-killing action of calcium hydroxide are combined to be able to prevent or treat the infection with high efficiency.
Further, in the case of adding hydrogen peroxide, since colloidal stable iodine is present in the liquid, it can be safely used for ingestion and drinking.
When ethanol water is used instead of water, the infection can be prevented or treated with high efficiency in combination with the virus-killing action of ethanol.
Similar preventive and therapeutic effects are expected for AIDS infection.
本発明の液体製剤は、水酸化カルシウムが溶解しているため、pHが8〜12.5のアルカリ性製剤であるが、カルシウムはアルカリ土類金属であり、ナトリウム等のアルカリ金属水酸化物のような皮膚に対する刺激性は少ない。
よって、本発明の製剤は刺激性が少なく、人体に優しいものである。
The liquid preparation of the present invention is an alkaline preparation having a pH of 8 to 12.5 because calcium hydroxide is dissolved, but calcium is an alkaline earth metal and is like an alkali metal hydroxide such as sodium. Less irritating to the skin.
Therefore, the pharmaceutical product of the present invention is less irritating and gentle on the human body.
本願発明で用いられるヨウ素は、ヨウ素単体を用いることもできるが、ヨウ素液のごとくヨウ化カリウムとヨウ素の混合液を使用すること、あるいはグリセリン、ポリビニルアルコール、ポビドン、レシチン、タラ肝油、竜脳、又はクレオソートからなる群の1以上から誘導された有機ヨウ素を使用することもできる。
殺ウイルス剤としては濃度0.01〜1.0重量%のヨウ素を含有するものが好ましい。
As the iodine used in the present invention, iodine alone can be used, but a mixed solution of potassium iodide and iodine like an iodine solution can be used, or glycerin, polyvinyl alcohol, povidone, lecithin, cod liver oil, dragon brain, or Organoiodine derived from one or more of the groups consisting of creosotes can also be used.
The virus-killing agent preferably contains iodine having a concentration of 0.01 to 1.0% by weight.
本願発明で用いられる酸化カルシウム又は水酸化カルシウムとしては、生物由来のカルシウム含有材料である牡蠣殻,ホタテ貝殻,ホッキ貝殻,卵殻、珊瑚などを900〜1200℃の温度で焼成して得られる焼成カルシウムが好ましいものである。
焼成したものは酸化カルシウムであるが、水和して水酸化カルシウムにしたものでも良い。
その飽和水溶液(水に対する溶解度は0.2%以下)はpHが11〜13であり、殺ウイルス作用がある。
なお、溶解度を高めて水酸化カルシウム濃度を高めようとする場合には、蔗糖やカラギーナン等の多糖類を添加することが好ましい。
As the calcium oxide or calcium hydroxide used in the present invention, calcined calcium obtained by calcining biological calcium-containing materials such as oyster shells, scallop shells, hokki shells, eggshells, and coral at a temperature of 900 to 1200 ° C. Is preferable.
The calcined product is calcium oxide, but it may be hydrated to calcium hydroxide.
The saturated aqueous solution (solubility in water is 0.2% or less) has a pH of 11 to 13, and has a virus-killing effect.
When increasing the solubility and increasing the calcium hydroxide concentration, it is preferable to add a polysaccharide such as sucrose or carrageenan.
過酸化水素は市販のオキシドールを使用することができ、本発明の水酸化カルシウム溶液に添加すると、安定なコロイド溶液を得ることができる。
微量の過酸化水素は、過剰の水酸イオンと結合し、コロイド粒子を帯電させることにより、安定なコロイド溶液を生成すると共に、ヨウ素同士が結合しないので、毒性を持つことがなくなる機能があるものと推定される。
Commercially available oxidol can be used as hydrogen peroxide, and when added to the calcium hydroxide solution of the present invention, a stable colloidal solution can be obtained.
A small amount of hydrogen peroxide binds to excess hydroxide ions and charges the colloidal particles to generate a stable colloidal solution, and since iodine does not bind to each other, it has the function of eliminating toxicity. It is estimated to be.
本願発明で用いられるエタノールは、コロナウイルス等に対する優れた殺ウイルス作用がある。
その濃度は70〜90vol%が好ましい。
なお、本願発明の液体製剤に香料、着色料や甘味料等を添加してもよい。
本願発明の液体製剤はウイルス感染病又はエイズ感染病の予防や治療に用いられるが、製剤を直接塗布あるいは噴霧するなどをして使用することができる。
Ethanol used in the present invention has an excellent virus-killing action against coronavirus and the like.
The concentration is preferably 70 to 90 vol%.
A flavoring agent, a coloring agent, a sweetening agent, or the like may be added to the liquid preparation of the present invention.
The liquid preparation of the present invention is used for the prevention and treatment of viral infections or AIDS infections, but the preparation can be directly applied or sprayed.
以下に実施例を示す。
実施例1;
500mlの水に、稀ヨウ素液(ヨウ素ヨウ化カリウム液;ヨウ素1%含有)100mlを投入・混合し、更に焼成カルシウム(水酸化カルシウム)粉末1gを添加混合した。
さらに、水を投入して全体容量を1000mlとした後、良く混合してヨウ素系液体製剤を製造した。
実施例2;
600mlのエタノール水(濃度90vol%)に、稀ヨウ素液(ヨウ素ヨウ化カリウム液;ヨウ素1%含有)100mlを投入・混合し、更に焼成カルシウム(水酸化カルシウム)粉末1gを添加混合した。
さらに、エタノール水を投入して全体容量を1000mlとした後、良く混合してヨウ素系液体製剤を製造した。
An example is shown below.
Example 1;
100 ml of a rare iodine solution (potassium iodide solution; containing 1% iodine) was added to and mixed with 500 ml of water, and 1 g of calcined calcium (calcium hydroxide) powder was further added and mixed.
Further, water was added to make the total volume 1000 ml, and then the mixture was well mixed to produce an iodine-based liquid preparation.
Example 2;
100 ml of a rare iodine solution (potassium iodide solution; containing 1% iodine) was added to and mixed with 600 ml of ethanol water (concentration 90 vol%), and 1 g of calcined calcium (calcium hydroxide) powder was further added and mixed.
Further, ethanol water was added to bring the total volume to 1000 ml, and then the mixture was well mixed to produce an iodine-based liquid preparation.
上記実施例で得られた製剤を用いて、殺ウイルス試験を行った。
その結果、ノロウイルス、コロナウイルス、新型コロナウイルス(COVID−19)に対して優れた殺ウイルス効果があることが解った。
A virus-killing test was performed using the pharmaceutical product obtained in the above example.
As a result, it was found that it has an excellent virus-killing effect on norovirus, coronavirus, and new coronavirus (COVID-19).
Claims (14)
The method for producing an iodine-based liquid preparation according to any one of claims 8 to 13, wherein the iodine-based liquid preparation is a preventive agent or a therapeutic agent for a viral infection disease or an AIDS infection disease.
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