JP2021513569A - 抗菌及び殺精子潤滑剤 - Google Patents
抗菌及び殺精子潤滑剤 Download PDFInfo
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- JP2021513569A JP2021513569A JP2020565535A JP2020565535A JP2021513569A JP 2021513569 A JP2021513569 A JP 2021513569A JP 2020565535 A JP2020565535 A JP 2020565535A JP 2020565535 A JP2020565535 A JP 2020565535A JP 2021513569 A JP2021513569 A JP 2021513569A
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- guanidine
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- biocide
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Images
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- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
- A01N47/40—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides
- A01N47/42—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides containing —N=CX2 groups, e.g. isothiourea
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Abstract
Description
(式中、
R1が、O、N及びSから選択される1つ以上のヘテロ原子を任意に含み、任意に1つ以上のビニル基で置換される少なくとも1つの芳香環を含む芳香環系の何れかを表し、又はエチレンを表し、又はグアニジンを排除した閉環によって得られる環状構造を有する。)
R1の例は、ベンゼン(好ましくはパラ位又はメタ位に結合)、ピリジン(好ましくはNに隣接するC原子に結合)、ジビニルベンゼン、ビフェニル(好ましくはそれぞれのパラ位に結合した両方のベンゼン)、1,3−ビス((E)−2−ビニル)ベンゼン、フラン、ピロール、チオフェン、フルオレン、エチレン(好ましくはシス配座)である。このタイプの高分子グアニジンは、WO2016/015081A1に記載される。
(式中、
Xが、−NH2、アミノグアニジン及び1,3−ジアミノグアニジンから選択され;
Yが、−H及び−R1−NH2から選択され;又はX及びYが共に、環状構造を形成するために化学結合を表し;
R1が、2〜20個の炭素原子を含む二価の有機残基から選択され、任意に1つ以上の炭素原子が、O又はNで置換されており;
a及びbは、それぞれ0又は1であり;
ここで、1,3−ジアミノグアニジンユニットが存在しない場合、a+bは、2に等しくなく;
R2が、−H及び−NH2から選択され;
ここで、R2が、a+b=0の場合、−NH2であり;
R2が、a+b=1の場合、−H又は−NH2であり;及び
R2が、a+b=2の場合、−Hであり;及びnは2より大きい)。
このタイプの高分子グアニジンは、WO2014/113835A1に記載されている。
高分子グアニジン殺生物剤:0.05重量%〜10重量%、
保湿剤:5重量%〜15重量%、
アルキルフェノキシポリエトキシエタノール殺精子剤:0.05重量%〜10重量%、
増粘剤:1重量%〜10重量%。
アシダムアスコルビカム及び/又はアシダムシトリカム:0重量%〜3重量%、
水酸化ナトリウム:0重量%〜2重量%、
クエン酸:0重量%〜4重量%、
精製水:残り〜100重量%。
基本的な製剤は、ポリグアニジン群の殺生物性物質であり(Kratzer et al., Antibiotika Monitor 1/2/2006; Buxbaum et al., Journal of Antimicrobial Chemotherapy (2006) 58, 193-197; WO 01/85676 Al; WO 2006/047800 Al; WO 2008/080184 A2; WO 2013/064161 Alに記載されるアカシド)、アカシドプラス(ポリヘキサメチレングアニジウムクロライドとポリ[2−(2−エトキシ)エトキシエチル]グアニジウムクロライド]の3:1混合物)等の様々な製剤であった。これらの殺生物性高分子グアニジン化合物は、優れた抗菌プロファイルを有し、さらに、ポリエトキシル化非イオン性化合物によって形成される群の可溶化剤なしでは混合が困難な物質を含む安定した製剤を提供することができる。
「女性用液体コンドーム」製剤は、ヒドロキシエチルセルロースを含むゲルから成る。低粘度のゲルが得られるまで、ヒドロキシエチルセルロースを精製水で5分間膨張させた。
「男性用液体コンドーム」製剤は、ヒドロキシエチルセルロース含有ゲルである。シアリング(shearing)により低粘度のゲルが得られるまで、ヒドロキシエチルセルロースを精製水で5分間膨張させた。2つの活性物質、アカシドプラス1000(例えば、0.2%の濃度)及び局所麻酔剤リドカイン塩酸(濃度0.4%)が、製造された軟膏ベースに入れ込まれた。局所麻酔は、早漏を改善するために脱感作の目的で加えられた。pHは、中性〜わずかに塩基性であった。製剤は、避妊作用がなく、主に保護されていない性行為による男性の感染を防ぐために役立つ。
計量したアカシドプラス1000をノノキシノール−9と共に溶解させたAdeps Neutralis溶液に組み込み、約40℃〜45℃に冷却した後、2gの坐剤型に流し込み、冷却し固化させた。
以下の組成物を互いに比較することにより試験し、アカシド濃度のみを(実施例1に記載されるようにアカシドプラスとして)、様々な希釈にした。
組成物2:ノノキシノール−9を有しない(代わりに水)実施例2に記載される「液体コンドーム」(「女性用液体コンドーム」)
組成物3:アカシドプラス、残り:水
・MRSA1−黄色ブドウ球菌(Staphylococcus aureus)
・EK4−エンテロコッカス・フェシウム(Enterococcus faecium)
・Strepto8−肺炎球菌(Streptococcus pneumoniae)
・E.coli13−大腸菌(Escherichia coli)
・KL37−クレブシラ肺炎桿菌(Klebsiella pneumonia)
・PS23−緑膿菌(Pseudomonas aeruginosa)
・Asp.Fum.45−アスペルギルス・フミガーツス(Aspergillus fumigatus)
・Asp.Faec.45−アスペルギルス・フミガーツス(Aspergillus fumigatus)
・C.Alb.−カンジダ・アルビカンス(Candida albicans)
・C.Krusei26−カンジダ・クルセイ(Candida Krusei)
細菌用:ミュラーヒントンブロス(Muller Hinton Broth)
真菌用:サブローブロス(Sabouraud Broth)
ウェル当たり100μLの培地が添加されたコントロールウェルを除いて、50μLの各培地を96ウェルプレートの全てのウェルに入れた。サンプルを調製し、100μLをウェルに加えた。
Claims (15)
- 少なくとも1つの高分子グアニジン殺生物剤及び少なくとも1つのアルキルフェノキシポリエトキシエタノール殺精子剤又は局所麻酔薬を含む水性溶液、及び少なくとも1つの増粘剤、を含む化学組成物。
- 前記高分子グアニジン殺生物剤が、ポリアルキレングアニジン、好ましくはポリオキシアルキレングアニジンであることを特徴とする、請求項1に記載の組成物。
- 前記高分子グアニジン殺生物剤が、ポリヘキサメチレングアニジン; ポリ[2−(2−エトキシ)エトキシエチルグアニジン; ポリトリエチレングリコールグアニジン; ポリエチレングリコールグアニジン;ポリオキシプロピレングアニジン;ポリオキシエチレングアニジン、から選択されることを特徴とする、請求項2に記載の組成物。
- 前記グアニジンが、好ましくは、ハライド、特に塩化物; リン酸、好ましくはリン酸二水素; 炭酸塩; 硝酸塩; ソルベート; 酢酸塩、好ましくはヒドロ酢酸塩;グルコン酸塩、クエン酸塩、ケイ酸塩から選択される、グアニジウム塩であることを特徴とする、請求項1〜3の何れか1項に記載の組成物。
- 前記グアニジン殺生物剤の平均分子量が、200Da〜10000Da、好ましくは500Da〜3000Daであることを特徴とする、請求項1〜4の何れか1項に記載の組成物。
- 前記アルキルフェノキシポリエトキシエタノール殺精子剤が、ノニルフェノキシポリ(エチレンオキシ)エタノール(ノノキシノール−9)であることを特徴とする、請求項1〜5の何れか1項に記載の組成物。
- 前記増粘剤が、好ましくはヒドロキシアルキルセルロース、セルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースから選択されるゲル形成剤;又は好ましくは硬脂肪、グリセロール−ゼラチン混合物又は可溶性PEG、例えばPEG400/4000から選択される坐剤ベースであることを特徴とする、請求項1〜6の何れか1項に記載の組成物。
- 前記組成物が、0.05重量%〜10重量%の高分子グアニジン殺生物剤を含むことを特徴とする、請求項1〜7の何れか1項に記載の組成物。
- 前記組成物が、0.05重量%〜8重量%のアルキルフェノキシポリエトキシエタノール殺精子剤を含むことを特徴とする、請求項1〜8の何れか1項に記載の組成物。
- 前記組成物が、1重量%〜95重量%の増粘剤を含むことを特徴とする、請求項1〜9の何れか1項に記載の組成物。
- 前記組成物が、1mL〜5mLの量で、好ましくは使い捨てピペットで、単回投与形態であることを特徴とする、請求項1〜10の何れか1項に記載の組成物。
- 前記組成物が、保湿剤、好ましくはプロピレングリコールを含むことを特徴とする、請求項1〜11の何れか1項に記載の組成物。
- 前記組成物が、以下:
高分子グアニジン殺生物剤:0.05重量%〜10重量%、
保湿剤:5重量%〜15重量%、
アルキルフェノキシポリエトキシエタノール殺精子剤:0.05重量%〜10重量%、
増粘剤:1重量%〜10重量%、
を含み、好ましくはさらに以下:
アシダムアスコルビカム:0重量%〜3重量%、
水酸化ナトリウム:0重量%〜2重量%、
クエン酸:0重量%〜4重量%、
精製水:残り〜100重量%に、
を含むことを特徴とする、請求項1〜12の何れか1項に記載の組成物。 - 性行為中の少なくとも1つの高分子グアニジン殺生物剤を含む水性溶液、及び膣内の抗菌、抗真菌及び/又は抗ウイルス消毒のための少なくとも1つの増粘剤を含む化学組成物の使用。
- 請求項1〜13の何れか1項に記載の組成物を性行為のために膣管に導入することを含む、性感染症による感染を予防するための方法又は性行為中に避妊するための方法。
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PCT/EP2019/053127 WO2019154983A1 (de) | 2018-02-08 | 2019-02-08 | Antibakterielles und spermizides gleitmittel |
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US20210038637A1 (en) | 2021-02-11 |
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EP3524055A1 (de) | 2019-08-14 |
BR112020015955A2 (pt) | 2020-12-15 |
WO2019154983A1 (de) | 2019-08-15 |
RU2020129407A (ru) | 2022-03-09 |
KR20200119829A (ko) | 2020-10-20 |
CN111787802A (zh) | 2020-10-16 |
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