JPH01500265A - Pharmaceutical preparations containing xylometazoline - Google Patents

Pharmaceutical preparations containing xylometazoline

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Publication number
JPH01500265A
JPH01500265A JP62503730A JP50373087A JPH01500265A JP H01500265 A JPH01500265 A JP H01500265A JP 62503730 A JP62503730 A JP 62503730A JP 50373087 A JP50373087 A JP 50373087A JP H01500265 A JPH01500265 A JP H01500265A
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Prior art keywords
xylometazoline
oil
pharmaceutical preparations
preparations containing
triglyceride
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JP62503730A
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Japanese (ja)
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レーベル，クラウス‐デイーター
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アシエ　アクチエンゲゼルシヤフト
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

(57)【要約】本公報は電子出願前の出願データであるため要約のデータは記録されません。 (57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

【発明の詳細な説明】 キシロメタゾリン含有薬物学的製剤 キシロメタゾリン−２−（４−（１，１−ジメチルｘチル）　＋　２　、６１” メチルフェニル）−）５−ル〕−４，５−ジヒドロ−１Ｈ−イミダゾールは、公 知のα−痙輩８及び口管収縮作用化合物であり、臀に鼻科用薬剤中で使用Ｇ　ｆ ’Ｌる（　Ａｎａｌ、　Ｐｒｏｆｉｌｅｓ　ｐｒｕｇ　５ｕｂａｔ。[Detailed description of the invention] Pharmaceutical preparations containing xylometazoline Xylometazoline-2-(4-(1,1-dimethyl x thyl) + 2, 61" Methylphenyl)-)5-l]-4,5-dihydro-1H-imidazole is a publicly known It is a compound with α-convulsant 8 and oral canal constriction effect, and is used in rhinological drugs for the buttocks. 'L (Anal, Profiles prug 5ubat.

１４．１９８５．１３５〜１５６　＠、　＠Ｒｏｔｅ　Ｌ１ｅｔｅ１９８６″； 　ｇａ１ｔ４０　Ｃａｎｔｏｒ　Ｖａｒｌａｇ　、　ｐ　−７９６０Ａｕｌｅｎ ｃＬｏｒｆ　Ｎｒ、　７１０３３、Ｎｒ、７１０３８　及びＮｒ。14.1985.135-156 @, @Rote L1ete1986″; ga1t40 Cantor Varlag, p-7960Aulen cLorf Nr, 71033, Nr, 71038 and Nr.

）１０６９癖照）０ 中性課体中のキシロメタゾリンは、比戦的世い安定性ｔ−［７るだけである（　 Ａｅｔ！Ｌ　ｐｏ：Ｌ、ｐｈａｒｍ、３　ｋ３．１９８１．９５〜９Ｂ−ｒｅｆ 、ｃ、Ａ、、９５．１９８１．２０９４７１ｘ）ので、こｎは鼻科用薬剤中では 塩酸塩として水浴液中で使用される。こｎは、この製剤か光分な貯蔵性を得る友 めに、株存剤を心安とし、粘膜の乾課によりかな９の苦訴の原因となる欠点を有 する。) 1069 quirks) 0 Xylometazoline in the neutral body has a relative stability of only t-[7 ( Aet! L po: L, pharm, 3 k3.1981.95-9B-ref , c, A, , 95.1981.209471x), so this n is not found in nasal drugs. Used in water bath liquids as the hydrochloride salt. This is because this formulation has a long shelf life in light. For this reason, we recommend using a stock-preservation agent, which has the disadvantage of causing complaints of Kana 9 due to the dryness of the mucous membranes. do.

ところで、抹存剤の助けなしに、ＡＭ外に安定で、ｆＦｒ戚町乾なキシロメタゾ リン−塩基を含有する薬物字豹製剤を装造でさることが刊−し友。この製剤は、 次の物似を有する：こｎは、キシロメタゾリン塩基０．０１〜０．５ムｍ％及び 楕油０．００〜３．００　］ｋ貢チ會、一般式： ＣＨ３（ＣＨ２）ｇ５Ｃｏｏ　−ＣＨ２〔式中１１ｙ及び２は５〜８の数である 〕の脂肋嘔トリグリセリド中に溶解含有する。By the way, xylometazoone is stable and free from AM without the aid of peripheral agents. It has been published that a pharmaceutical formulation containing phosphorus bases has been prepared. This formulation is It has the following similarities: xylometazoline base 0.01-0.5 mm% and Oval oil 0.00 to 3.00] K Gong Jikai, general formula: CH3(CH2)g5Coo　-CH2 [wherein 11y and 2 are numbers from 5 to 8 ] is dissolved in triglycerides.

この脂肋撃トリグリセリドは、式中のＸ、７及び２がそｎそれ同じものを表ｖ丁 もの、例えはエナント酸トリグリセリド、カプリル酸トリグリセリド又はカプリ ン酸トリグリセリドであってよいが、こｎは、′＠に式の同様に可能な脂肪歌ト リグリセリド（式中のｘｌｙ及び２は多くのこの境の中性油の場合のように極々 異なるものを衣わ丁）でありうる。この糧の脂Ｕ５鹸トリグリセリドは、例えば ′Ｆ５勧で入＋塾れる中性油例えば７７テノール３１Ｑ７　（８０ｆｔｅｎＯ１ ３ｉ　Ｑ７　：Ｄ７ｎａｍｉｔ　１０ｂｅ１社表）、ミグリオール　８１０／８ １２（Ｍ７ｇｒｉｏｌ　８１０／　８１２　：　Ｄｙｎａｍｌｔ　Ｎｏｂｅｘ社 製）、ミ　リ　トール３１３　（Ｍｙｒｉｔｏｌ　６１　Ｂ　：　Ｈｅｎｋｅ１ 社叔）及びｈにラブラファツク・リポ（Ｌａｂｒａｆａｃ　’Ｅ’　１ｉｐｏ　 ：Ｇａｔｔｅｆｇｓａｅ　社製）で＜＝。This triglyceride has the same formula as X, 7, and 2. such as enanthate triglyceride, caprylic triglyceride or capri may be triglyceride, but this n may be an equally possible fatty acid triglyceride of the formula '@'. liglyceride (in the formula xly and 2 are extremely They can be different things. This food fat U5 triglyceride is, for example, 'F5 recommended neutral oil that can be used for example 77 tenor 31Q7 (80ftenO1 3i Q7: D7namit 10be1 company table), Miglyol 810/8 12 (M7griol 810/812: Dynamlt Nobex ), Myritol 313 (Myritol 61 B: Henke1 Labrafac 'E' 1ipo to : Manufactured by Gattefgsae) <=.

この油状キシロメタゾリン−浴准は、本発明により、付加的になお祠油１〜３′ ｔ−含有していてよい。According to the invention, this oily xylometazoline bath may additionally be added to the abrasive oil 1 to 3'. It may contain t-.

このような油はカえは次のものでめる：濃　民 ユーカリ油　０．０１〜２９ｂ メントール　０．０１〜１　％ ハイマツ油　０．０１〜２　チ ドイットウヒ油　０．０１〜２　％ ペパーミントｌ’ａｌｌ　０．０１−３　聾チモール　０．０１〜０．５　＊ サルビア油　０．０１〜２　チ カミンレ油　０．０１〜６　％ ワイキヨウ油　０．０５〜１％ ヒマラヤスギ葉油　ｏ、０５〜１　％ アニス油　０．０１〜１　％ レモン＠ｏ、ｏ　１〜１　ラ テルペンテン油　０．０１〜１　％ ニクズク油　０．０１〜１　％ これらのｖ１１度は各々、全＆−８物に対する１檜うでめる。This kind of oil can be made with: Eucalyptus oil 0.01-29b Menthol 0.01-1% Scots pine oil 0.01-2% Deutsche spruce oil 0.01-2% Peppermint l’all 0.01-3 Deaf Thymol 0.01-0.5 * Salvia oil 0.01-2% Kaminle oil 0.01-6% Waikiyo oil 0.05-1% Himalayan cedar leaf oil o, 05-1% Anise oil 0.01-1% Lemon @ o, o 1-1 la Terpentene oil 0.01-1% Nikuzuku oil 0.01-1% Each of these v11 degrees is 1 hinoki for all &-8 objects.

本発弘によるキシロメタゾリン宮五薬物字市表銅の装造は、成分會慣用法で混合 し、滅菌は巡し、キシロメタゾリン含有医薬に慣用の用賀（０，５〜５ｏ叡）で 、適当な容器〔−一見ばひん、缶、ピペットひん、スプレー士、ポンプ配量スプ レー、配量スプレーひん、１回適用ピペット（Ｅ；１ｎｚｅｌ＋１ｏａｉｅｒｐ ｉｐｅｔｔ　）　）中に光’ＪＩＴる。Hiroshi Motoha's formulation of xylometazoline Miyagoyaku Azaichi Omotedo was made by mixing the ingredients in a customary manner. The sterilization process is then carried out using the same method used for xylometazoline-containing medicines (0.5 to 5 degrees). , a suitable container [--pump bottle, can, pipette bottle, sprayer, pump dispensing spout] spray bottle, one-time application pipette (E; 1nzel + 1oaierp) ipett )) Light 'JIT' inside.

不発明によるキシロメタゾリン言Ｍ製剤の使用量は、作用＠気を塩は垣として含 有する慣用の表銅におけると同じで７１１る。The amount of xylometazoline M preparation used according to the invention is 711, which is the same as in a conventional surface copper.

芙旅例 次の笑派例につき不発Ｆｙ３を詳述する。Fu travel example For the next funny example, I will explain in detail the unfired Fy3.

例　１ キシロメタゾリンｏ、ｓ　ｙ’を呈温で僕拌１に（約３００ｕ、ｐ、ｍ、　）、 ラブラファック［Ｆ］リボ　９９９．５．９甲に浴かしく約３０分）、滅圓撫魅 する。Example 1 Add xylometazoline o, sy' to stirring 1 at a certain temperature (approximately 300 u, p, m,), Love La Fuck [F] Ribo 999.5.9 About 30 minutes in love with Ko), Meien Natsumi do.

こうして装造した浴Ｖ、各１［１＋ｕをピペットひん甲に元横する。Place 1[1+u] of each of the thus prepared baths V into the pipette shell.

例　２ キシロメタゾリンｏ、ｂｙ及びユーカリ油１１−５＆’ｔｉｙｖ１の記載と同様 にラブラファツク■リボ９９９９甲に浴かし、戚劇ｏ）７！ｉする。Example 2 Same as described for xylometazoline o, by and eucalyptus oil 11-5&’tiyv1 ni love love ■ Ribo 9999 A bathing in the relationship drama o) 7! i do

この洛液各１０紅”ｔｅ童ススプレーん甲に光衡する。Each of these 10 drops of liquid is added to the spray bottle.

例　６ キシロメタゾリン０．５　Ｊｌ、ユーカリＭ　Ｏ，５，９及びメントール１．５ ＆に例１の記載と同様にラグラフアラ声すボ９９７．５　＆中に浴かし、滅鉋濾 過する。Example 6 Xylometazoline 0.5 Jl, Eucalyptus M O,5,9 and Menthol 1.5 & same as described in Example 1, Ragraph Ara voice 997.5 pass

この治猷各１０紅をピペットびん中に光撫する。Lightly dab 10 drops of each of these ingredients into a pipette bottle.

例　４ キシロメタゾリン１．０９及びユーカリ油０−５　＆にラブラ７アック■リボ９ ９９紅中に浴かし、力１σノ配社と１６］禄に１１ψ壇し、１０紅を配素スプレ ーびん甲に元横する。Example 4 Xylometazoline 1.09 and eucalyptus oil 0-5 &ni Labra 7ac ■ Ribo 9 Bathed in 99 red, bathed in 1σ of power and 11ψ in 16] Roku, sprayed with 10 red. - Lie down on the bottle shell.

例　５ キシロメタゾリン１．０＆及びユーカリ油０．５　ｉ　ｔ　２プラフアツタ［Ｆ ］リボ９８８．５．９中に浴かし、滅−鋤遇し、１０１をピペットびん中に元横 する６例　６ キシロメタゾリン１．０ｇ、ユーカリ油０．５　＆及びメントール１．５９をラ ブラファック■リボ９９７９中に溶かし％　’Ｉｉｊ　１のｉｔｅｍと同様に滅 菌鋒遇し、１０勘會ピペツトひん中罠光填する〇 国際調査報告 入Ｎ）ｉ’ＥＸ　Ｔｏ　ＴＨ工　ＩＮ丁三ＲＮ入τＩＣＮＡＬ　５ＥＡＲＣＨＲ ＥＰＯＲτ　ＩＪＮｒＮＴＥＲＮＡＴｌＯＮＡＬ　ＡＰＰＬＩＣＡＴＩＯＮ　Ｎ ｏ、　ＰＣＴ／ＤＥ　８７１００２８４　（ＳＡ　１７５９９１Example 5 xylometazoline 1.0 & eucalyptus oil 0.5 it 2 plastic ivy [F ] 101 was poured into a pipette bottle on 988.5.9 6 cases 6 Add 1.0 g of xylometazoline, 0.5 g of eucalyptus oil & 1.59 g of menthol. Blafac ■ Dissolve in Ribo 9979 and destroy it like item 1. Encounter the bacteria and fill the trap with 10 pipettes. international search report Enter N) i’EX To TH Work IN Ding 3RN Enter τICNAL 5EARCHR EPORτ　IJNrNTERNATlONAL　APPLICATION　N o, PCT/DE 87100284 (SA 175991

Claims (1)

【特許請求の範囲】 キシロメタゾリン含有薬物学的製剤において、これは、キシロメタゾリン塩基０ ．００１〜０．５重量％及び精油０．００〜３．００重量％を一般式：▲数式、 化学式、表等があります▼ 〔式中ｘ、ｙ及びｚはそれぞれ５〜８の数である〕の脂肪酸トリグリセリ中に溶 解含有することを特徴とする、キシロメタゾリン含有薬物学的製剤。[Claims] In xylometazoline-containing pharmaceutical formulations, this includes xylometazoline base 0 ．． 001 to 0.5% by weight and essential oil 0.00 to 3.00% by weight using the general formula: ▲ Mathematical formula, There are chemical formulas, tables, etc.▼ [wherein x, y and z are each a number from 5 to 8] dissolved in fatty acid triglyceride A pharmaceutical preparation containing xylometazoline, characterized in that it contains xylometazoline.
JP62503730A 1986-07-18 1987-06-24 Pharmaceutical preparations containing xylometazoline Pending JPH01500265A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19863624624 DE3624624A1 (en) 1986-07-18 1986-07-18 PHARMACEUTICAL PREPARATIONS CONTAINING XYLOMETAZOLINE
DE3624624.7 1986-07-18

Publications (1)

Publication Number Publication Date
JPH01500265A true JPH01500265A (en) 1989-02-02

Family

ID=6305642

Family Applications (1)

Application Number Title Priority Date Filing Date
JP62503730A Pending JPH01500265A (en) 1986-07-18 1987-06-24 Pharmaceutical preparations containing xylometazoline

Country Status (12)

Country Link
EP (1) EP0282495B1 (en)
JP (1) JPH01500265A (en)
AU (1) AU7547387A (en)
DE (2) DE3624624A1 (en)
DK (1) DK149588A (en)
ES (1) ES2004454A6 (en)
FI (1) FI881271A0 (en)
GR (1) GR871134B (en)
IL (1) IL83177A0 (en)
PT (1) PT85350B (en)
WO (1) WO1988000473A1 (en)
ZA (1) ZA875281B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL1011016C2 (en) * 1999-01-13 2000-07-14 Dagra Pharma Bv Nasal spray based on xylometazoline and chamomile extract.

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3339236A1 (en) * 1983-10-28 1985-05-09 Bayer Ag PREPARATION OF MEDICINAL PRODUCTS

Also Published As

Publication number Publication date
DK149588D0 (en) 1988-03-18
DK149588A (en) 1988-03-18
FI881271A (en) 1988-03-17
IL83177A0 (en) 1987-12-31
GR871134B (en) 1987-11-20
PT85350B (en) 1989-10-16
ES2004454A6 (en) 1989-01-01
EP0282495B1 (en) 1991-06-19
DE3770939D1 (en) 1991-07-25
FI881271A0 (en) 1988-03-17
EP0282495A1 (en) 1988-09-21
DE3624624A1 (en) 1988-01-28
AU7547387A (en) 1988-02-10
WO1988000473A1 (en) 1988-01-28
PT85350A (en) 1987-08-01
ZA875281B (en) 1988-03-30

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