TW518226B - Orally administrable formulations of quinolone- or naphthyridonecarboxylic acids - Google Patents
Orally administrable formulations of quinolone- or naphthyridonecarboxylic acids Download PDFInfo
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- TW518226B TW518226B TW086111729A TW86111729A TW518226B TW 518226 B TW518226 B TW 518226B TW 086111729 A TW086111729 A TW 086111729A TW 86111729 A TW86111729 A TW 86111729A TW 518226 B TW518226 B TW 518226B
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- acid
- water
- patent application
- quinolone
- salt
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A—HUMAN NECESSITIES
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Landscapes
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- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Description
518226 A7 經濟部中央標準局員工消費合作社印製 、發明説明(i 本發明乃有關於P奎碏酮―或p奈P定酮幾酸口服用製劑的製 備方法。 戶 口套口若嗣羧酸之指寶酸(embonic acid)鹽已被熟知,如 EP-A(歐洲公告之專利説明書)238 814,蝰畦酮與指寶酸組 成的鹽類可應用於掩蓋活性π查畦酮化合物的苦味,而製備這 些化合物時,需先製備蝰碏酮羧酸指寶酸鹽,經分離與純化 後加以製劑。 … 目如發現竣口若酮-或n奈口定酮羧酸之口服用製劑,可藉由 將蝰畦酮-或4卩定酮羧酸直接或以其水溶性鹽或衍生物(以 其鹽的水溶液較佳)形式,與指寶酸或其水溶性鹽或衍生物 (以其鹽的水溶液較佳),在賦形劑存在下混合而製得,其可 選擇地在辅助劑存在下(當採用乾燥的混合物在水存在時) 進行,並可選擇性地將產生的混合物進一步轉換成立即可用 的形式。 根據本發明的方法產生係含有蝰碏酮-或p奈畋酮羧酸之 製劑,其可經口服施用而不會產生任何問題,甚至對於一些 通常會因為蝰碏酮-或4畋酮羧酸的苦味而排斥其製劑的動 物亦然。 本項製劑的製備不需先製備及分離活性化合物之拢寶 酸鹽,再把鹽類加入賦形劑中;令人驚訝的是,只需將活性 化合物與指寶酸或其鹽及衍生物,在有水的狀況下,分別或 同時與賦形劑混合即可製成製劑,更令人驚訝的是,如此製 得之製劑能使即使是味覺敏感的動物也能毫無猶豫地經口 服用,此點是無法預期的,因為於本發明製法中產生的拢寶 請
I 意 事 項 寫 本 頁 鑣 訂 本紙張尺親财關家標準(CNS ) Μ胁( 斧18226 A7 B7 五、發明説明(2 ) 酸:疋否儿全、邵份或尚未生成並不清楚,而可確定的是 製劑在口服時具有顯著之可接受性,且係包括下列組成分: 賦形劑、邊確或定酮羧酸或它們的鹽或衍生物以及指 寶酸或其鹽或衍生物。 口奎口若嗣—或p奈畹酮羧酸或它們的水溶性鹽及衍生物,可 由EP-A(歐洲公告之專利説明書)350 950、302 372、49 355、47 005、242 789、259 804、215 650、131 839、 109 284 ; DE-A(德國公告之專利説明書)2 804 097 ; FR-P(法國公告之説明書)2 463 771 ; PCT WO 92/9596中獲知 (這些出版物中提到的化學式與特定化合物乃併入本文中供 參考用)〇 較佳的活性化合物為:temafl〇xacin 、 tosufloxacin > enrofloxacin - ciprofloxacin - ofloxacin 、 orbifloxacin 、 marbofloxacin 、 norfloxacin 、 benofloxacin 、 binfloxacin 、 danofloxacin 、 difloxacin 、 sarafloxacin 、 premafloxacin 、 ibafloxacin 〇 特佳的化合物為 enrofloxacin、danof loxacin、 sarafloxacin ° 經濟部中夬樣準局員工消費合作社印製 (請先閱讀背面之注意事項再填寫本頁) 這些活性化合物的衍生物包括它們的酯類,如Ci-C4-燒 基酯。 這些活性化合物之鹽類包括與酸形成生理可接受的鹽 類,這類的酸包括有氫_酸、磺酸、羧酸、氨基酸、(多)一 輕基羧酸、磷酸、硝酸、硫酸;特定而言為甲烷磺酸、乙磺
本紙張尺度適用中國國家標準(CNS ) A4規格(21〇><297公董) >18226 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(3 ) … 酸、輕基乙磺酸、苯磺酸、對甲苯磺酸、曱酸、乙酸、丙酸、 一甲基醇丙敗、往基乙酸、乳酸、輕基順丁烯二酸、乙二酸、 琥珀酸、反丁烯二酸、順丁埽二酸、戊二酸、丙二酸、己二 酸、抗壞血酸、蘋果酸、檸檬酸、酒石酸、氨基水揚酸、氨 茴酸、苯甲酸、輕基苯甲酸、苯乙酸、水楊酸、苯二酸、菸 酸、扁桃酸、門冬氨酸、谷氨酸、葡糖酸、葡糖醛酸、乳糖 酸奴、半乳糖酸奴、黏酸、磷酸、硝酸、氫氣酸、硫酸、5一 氧四氫畎喃-2-羧酸、2-輕基戊二酸。 特佳的化合物是氫氯酸或葡糖酸。 指寶敗及其鹽類為已知化合物,如默克索引第十版第 6867號參考資料。 ’、 ",與指寶酸形成鹽類的適當鹼包括鹼金族與鹼土族金 屬氫氧化物,如氫氧化鉀、氫氧化鈉、氫氧化鈣、氨,鹼性 氨基,如精氨酸、賴氨酸、膽鹼、.甲基葡萄糖胺、乙晞二 胺、單-,雙-二㉟基胺、被取代胺如二乙嚇、環狀胺如嗎 啉、哌4、三輕甲基氨基甲烷。 特別適合者為虱氧化i甲、精氨酸、賴氨酸、N—甲基葡萄 糖胺。 根據本發明,_帽當輯糊騎有的目體惰性物 質,可採用無機及有機物質。 無機物質之例為:一般鹽類、碳酸鹽(如碳酸鈣)、碳酸 氫鹽、鋁氧化物、矽土、黏土、沈澱或膠狀二氧化矽、磷酸 鹽。 有機物質之例為:糖類、纖維素、糖及纖維素衍生物、 5 本紙浪尺度通用〒國國豕標準(CNS ) A4規格(210x297公釐) — 1^---:---豐! (請先閲讀背面之注意事項再填寫本頁) 訂 518226 A7 B7 五、發明説明(4 ) ~~-- 殿粉(如玉米、米、馬龄薯、樹薯或小麥殿粉),糧食或飼料 如奶鈿動物食用粗粉、磨碎及搗碎穀物,上述物質之混合 物亦可作為載體。 、 其b的载體還具有結合水的功能,如羧基甲基纖維素、 曱基纖維素與其它纖維素或澱粉的衍生物、聚丙缔酸鹽、、藥 脱酸鹽、明膠、幾丁質、阿拉伯膠、聚乙缔口比哈燒嗣、聚乙 浠乙醇、乙_與_共聚物、聚乙二醇、臘、膠狀硬石或 上述物質之混合物。 根據本發明製劑時,須添加輔助劑如防腐劑、抗氧化 劑、光穩定劑、著色劑、吸附促進物質、分裂促進物質、黏 合劑或潤滑劑及安定劑。 ' 適當的防腐劑如苯基乙醇、苯酸、對輕基苯酸、丙酸及 其衍生物與鹽,以及山梨酸及其衍生物與鹽。 適當的抗氧化劑如白朊、氨基酸、抗壞血酸及其鹽與衍 生物、丁基基苯甲醚、丁絲基甲苯、衍生之氯化邊口若嗣。 適當的光穩定劑如芳香族衍生物及具適當吸收波長的 (請先閲讀背面之注意事項再填寫本頁) 、^1 化合物 〇 經濟部中央標準局員工消費合作社印製 適當的著色劑如色素’例如鐵色素、水溶性著色劑或可 溶於有機溶劑之著色劑。 < 適當的吸附促進物質如脂肪酸、脂肪酸醋及其混合物、 脂肪族醇、卵磷脂、膽酸鹽。 口 適當的穩定劑如亞硫酸鈉、乙二胺四乙酸及其鹽類。 適當的潤滑劑如硬脂酸鎂、硬脂酸、滑石、包土;適當 的分裂促進物質如澱粉或交叉鍵結的聚乙烯毗咯烷酮;適當 6 表紙張尺度適用中國國家標準(CNS ) A4規格(21 OX297公釐)
.I II» I- I 518226 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(5 ) 的黏合劑如澱粉、明膠或直鏈聚乙稀毗咯烷酮,乾的 如微晶纖維素。 — 、、根據本《之方法,係於轉在下藉齡個別成分 之方式進行,而個別成分加入的順序並不重要。 因此,將賦形劑與輔助劑放入一般的檀拌機中混合,鈇 後將活性化合物或其水溶液鹽及衍生物加入(以其鹽:水j容 液形式較佳)混合,產生的混合物再與指寶酸或其水溶液鹽 及衍生物(以其鹽的水溶液形式較佳)混合,而乾混合物則在 水存在下混合。 為了製備水溶液,添加水溶性溶劑及辅助劑可能有用。 這類的添加物包括丙二醇、乙醇:、異丙醇、丙酮、N— 甲基毗咯烷酮、2-毗咯烷酮、氯丁醇、苯甲醇、防腐劑、安 定劑如亞硫酸納、乙二胺四乙酸鋼、著色劑,增加黏度物質 如聚乙婦毗嘻燒酮、纖維素衍生物、明膠、澱粉膠。 活性化合物(鹽)溶液的濃度為0·5_50%,以10_40%較 佳0 捕寶酸(鹽)溶液的濃度為0 5-40%,以5-30%較佳。 根據本發明賴備的趟,雜化合物減寶酸的添加 比例為活性化合物1莫耳時,指寶酸為〇 5_5莫耳(以〇 7— 2莫耳較佳,1莫耳最佳)。 各f成份能在任何形式的攪拌機中混合,例如具有切碎 裝置的*強度授拌機,特別適合用於製備均質的混合物,溶 液或水以舞換、連續或批次加入乾混合物中,並可任意賴斜 翻覆注入以及噴霧或霧化。 障埋 异f*人 —^^----— (請先閲讀背面之注意事項再填寫本頁) 訂 mu m ·
本纸張尺度顏㈣目家縣 公釐) 518226 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(6 ) 澄'潤的混合物再加以磨碎、乾燥,然後過篩或粉碎。 相同的,流動床法為製備顆粒的適當方法;可將反應溶 液以一個或多個噴嘴噴霧於振動的混合物中,並在製備過程 加以乾燥〇 如果特別需要製成小顆粒時,微粒化方式可能是個選擇 (例如使用一種空氣衝擊、製粒或壓碾機)。 根據本發明之製劑方法可與其它賦形劑混合,在食品上 可應用於單一飼料或混合物,這類製劑可以擠壓或製丸形成 乾燥或溼潤的粉末狀。 根據本發明之製劑方法能應用於食品團粒之乾燥,有時 也可能需要加入黏合劑,適當的黏合劑如蔬菜油、動物油或 合成油、脂肪、脂肪酸、臘及明膠ό 根據本發明之製劑,也能使用於溼潤的團粒中,這類團 粒包含動物物質(如溼潤的團粒)。 根據本發明之製劑,尤其能用於填裝成膠囊,膠囊外層 乃由硬或軟明膠製成,而膠囊在適合時可被腸溶解。 根據本發明之製劑方法,也能用於製備其他口服用製 劑,例如口服液、稀釋後的口服用濃縮液、口服用乳劑與懸 浮液,半固體、油水或水油乳化狀態下製劑成膏或製備物, 固體製備物如粉末、前混合物或濃縮物、顆粒、擠壓物、片 劑、大丸劑或膠囊,或以上形式的混合。 根據本發明之製劑,可應用於人類或標的動物疾病的預 防或治療?尤其是細菌感染的治療。 這些製劑特別適用於老人與兒童疾病的領域,或是味覺 1 η 8 本纸張尺度適用中國國家標準(CNS ) A4規格(21〇X297公釐) C請先聞讀背面之注意事項再填寫本頁} -、·ιτ. 518226 A7
、發明説明(7) 敏感動物醫學方面,這類動物如貓、豬或备。 (請先閲讀背面之注意事項再填寫本頁) 致病備所得製劑能有效的對抗人類與動物 螺旋^屬、螺微生物包括⑴螺旋體科(如螺旋體屬、細 决二λ累體屬M2)螺旋菌科,·⑶細球菌科(如葡萄球菌 # Ί、蜂巢狀葡萄球菌);(4)鏈球菌科(如乳頭鏈球 馬鏈球K、無乳鏈球菌、缺乳鏈球菌、蓋士菲耳特 經濟部中央標準局員工消費合作社印製 緣球ft5)假單胞菌科(如鼻症桿菌、洋蔥假單胞菌、 干囷、脅麥芽假單胞菌、布魯士氏菌屬如流產布魯 杯囷、地中海熱布#士氏桿菌、豬流產布魯士氏桿菌、百曰 ^鲍,氏賴如支氣管敗血性齡氏菌、莫賊斯氏桿菌 屬L!!動力桿菌屬);⑹腸道桿菌科(如沙門氏菌B-E型、痢 ^桿菌、大腸桿菌、克雷伯士氏桿菌屬、變形桿菌屬、轉 酸桿菌、愛德華氏菌屬、嘻血桿菌屬、普洛維頓斯菌屬:耶 爾^氏桿菌);(7)狐菌科(如弧菌屬,例如霍亂弧菌、巴斯德 氏菌屬如夕此性巴斯德氏菌、產氣單胞菌屬、放線桿菌屬、 ,桿菌屬);(8)類桿菌屬(如類桿菌屬、細梭菌屬);(9)丹毒桿 菌屬、李斯特氏菌屬如單核血球增多性李斯特氏菌;(1〇)芽 胞桿菌科(如桿菌屬、梭狀芽胞桿菌屬A_D型,如產氣莢膜 梭菌;乳酸桿菌科及厭氣性球菌如東鏈球菌屬與東球菌屬,· (1—1)棒狀細菌(例如釀膿棒狀菌);⑽分枝桿菌科'(如牛結核桿 菌、鳥分枝桿菌、結核桿菌);(13)放線菌科(牛放線菌、以色 列放線菌);(14)土壤絲菌科(鼻疽土壤絲菌、星狀土壤絲菌); (15) 立克;衣氏菌科(如柯克斯立克次氏菌屬、立克次氏菌屬); (16) 巴東氏虫屬,(17)披衣菌科(如鸚鴣病披衣菌);(a)獯支漿 9 518226 經濟部中央標準局員工消費合作社印製 A7 發明説明(8 菌科(如黴狀黴漿菌、無乳黴漿菌、膽汁腐敗黴漿菌) w人類及動物的致病微生物,會引起Λ敗動t器t系統的 單獨感染或混合感染徵狀:肺部與氣管内腔,消化系統如胃與 腸,胸部與乳房,生殖系統如子宮,軟組織如皮膚肌肉,才旨 甲、爪、蹄,主動與被動活動系統如骨胳、肌肉、腱、關節,曰 泌尿生殖系統如腎臟、尿道、輸尿管,神經系統、耳朵、眼 睛、總。 如前所述,本製劑乃用於抵抗人類及動物的細菌性疾 病,這些動物包括··哺乳類動物,例如牛、馬、豬、羊、山羊、 狗、毅、魏,毛皮動物如紹、栗鼠,飼養於動物園之動物 與實驗室動物,如鼷鼠與老鼠,鳥類如鶴、難、火雞、鴨、 鴿子、飼養於大鳥舍中的鳥、實驗室鳥例如鸚鵡與虎皮鸚 鵡,魚類,特別是經濟用魚類,例如鯉魚、鱒魚、鮭声、鳗 魚、黃尾魚、海鱸魚、海鯛魚,此外如裝飾魚類及水族;;類了 攸蟲類如鱷魚、蛇、青虫圭,甲殼動物如外聰·—,例如p monodon ^ g ^ 〇 動物的細菌性疾病包括豬痢疾、雞螺旋體病、牛、豬、 馬、狗細螺旋體病:如彎曲桿菌引起的牛腸炎,羊盥 難肝炎、皮膚感染,狗膿皮症、外耳炎,牛、羊、'山羊乳腺 炎,馬、豬及其他種類動物的鏈球菌感染,牛及盆他種類動 物的肺炎雙球菌感染,鼻疽,結合膜炎,腸炎,^炎,牛、 羊、豬布魯士氏菌病,豬萎縮性鼻炎,牛、馬、羊、難及立 他種類動物的沙門氏菌病,敗血病,豬的大腸桿菌感染,^ 宮炎-乳腺炎-無乳症(MMA)徵候群,克雷士伯氏菌^染,假 ,-----------籲! (請先閲讀背面之注意事項再填寫本頁) 訂
518226
、發明説明(9 〜核涡,接觸傳染的胸膜肺炎,原 失調,牛與寵物的壞死桿菌病,纟^Ί囷病,懷孕 二李ϊί氏囷病,减,梭菌病,破傷風感染,臘 ίϊί狀祕染’牛、豬、雞及其他種類動物的 :核病,反_類結核病’土壤絲狀菌病,昆斯蘭 鳥病-鸚鵡病,腦脊髓炎,牛及其他動物的黴滎菌病,:地區 性肺炎。 魚類的細菌性疾病包括:細菌性腎臟病(由鈇魚腎菌所引 起)’鏈球菌病,假單胞菌感染如螢光假單胞菌、緩魚假單胞 菌,愛德華氏菌病感染如不活潑愛德華氏菌,產氣單胞菌感 采如鈇魚癤病產氣單胞菌、水生產氣單胞菌,派菌病如鰻魚 弧菌、鮭魚弧菌、腸炎弧菌,柱狀桿菌,立克次氏菌病如 SRS 〇 甲殼動物的細菌性感染包括:弧菌如腸炎弧菌、解藻糖弧 菌’假單胞菌感染如假單胞菌種。 根據本發明之方法生產的製劑如下: (請先聞讀背面之注意事項再填寫本頁)
經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家襟準(CNS ) A4規格(210'〆297公釐) 518226 A7 B7 五 發明説明(1G) 例1 enrofloxacin 與 指寶酸克分子比例 enrofloxacin 葡萄糖内酯 甲烷磺酸 亞硫酸納 指寶酸 N -甲基葡萄糖胺 精氨酸 一MHP-纖維素50
Ac-Di-Sol 溼潤玉米澱粉加至 (克重) 製粒a 1:1 10.00 6.00 0.10 10.82 10.88 7.00 100.0 製粒b 1:0.9 10.00 6.00 0.10 9.74 8.75 7.00 100.0 製粒c 1:1.1 2.500 1.500 0.025 2.705 2.720 1.500 100.0 製粒d 1:1.5 2.500 0.670 0.025 4.057 4.080 1.500 100.0 (請先閱讀背面之注意事項再填寫本頁) 賦形劑與辅助劑置入揽拌顆粒機並加以混合,然後加入 enrofl〇xacin-葡萄糖内酯或甲烷磺酸鹽水溶液,接著在混 合物中加入指寶酸-精氨酸或曱基葡萄糖胺鹽,將上述混合 物在適當裝置中(如流動床乾燥機)中乾燥後過篩(例如震動 篩)〇 由例1方法得到的製劑,還可將其碾磨或進—步加工產 生以下例2製劑的組成份·· 12 I適用 1¾¾標準(CNS )八4麟(210X297公ίΤ 訂 經濟部t央標準局員工消費合作社印製 518226 A7 B7 五、發明説明(11 ) 例2 每錠15毫克 % 毫克/錠 Enrof loxacin 顆粒 10% 75.00 150.0 玉米澱粉 15.00 30.0 微晶纖維素 9.55 19.1 硬酯酸鎂 0.30 0.6 膠狀矽土 0.15 0.3 200.0 例3 (請先閲讀背面之注意事項再填寫本頁) 每錠40毫克 « 〇/〇 毫克/錠 Enrofloxacin 顆粒 10% 80.00 400.0 玉米澱粉 10.00 50.0 微晶纖維素 9.55 47· 75 硬酯酸鎂 0.30 1.50 膠狀矽土 0.15 0.75 500.00 例4 經濟部中央標隼局員工消費合作社印製
Enrof loxacin 懸浮水溶液 2.5% Enrofloxacin 顆粒 10% 25.00 克 苯基醇 羧基甲基纖維素-鈉 1.40 克 0.50 克 去礦化水 加到100毫升
本紙張尺度適用中國國家樣準(CNS ) A4規格(210X297公釐) 518226
7 7 A B 經濟部中央標準局員工消費合作社印製 五、 發明説明(12) 例5 Enrof loxacin 懸浮油溶液 2.5% Enrof loxacin 顆粒 10% 25.00 克 苯基醇 1.40 克 中鏈三酸甘油酯 加到100毫升 例6 Enrof loxacin #2.5% Enrof loxacin 顆粒 10% 25.00 克 脂肪醇 5.00 克 白凡士林 10.00 克 黏石蠟 60.00 克 100·00 克 例7 Enrofloxacin 膝 2.5% Enrof loxacin 顆粒 10% 25.00 克 1,2-丙烯二醇 10.00 克 苯基醇 1.40 克 羧基甲基纖維素-鈉 2.50 克 去礦化水 61.10 克 100.00 克 例8 摻藥飼料0.05% Enrof loXacin 顆粒 10% 0·5克 飼料混合物/團粒 99.5 克 ;#ai| 100.0 克 \ ^ Vi , 1 4 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS )八4規格(210X 297公釐)
Claims (1)
- 518226A8 B8 C8 D8 、申請專利範圍專利申請案第86111729號 ROC Patent Appln. No. 86111729 修正之申請專利範圍中文本一附件一 Amended Claims in Chinese — Enel. I 「民-89年9月厂厂日送呈) (Submitted on September // , 2000) 1· 一種製備喳喏酮-(quinolone-)或峰咬酮缓酸 (naphthyridonecarboxylic acid)之口服用製劑的方法,其 特點是將喳喏酮-或喑啶酮羧酸直接或以其水溶性鹽或 衍生物形式,與据寶酸(embonic acid)或其水溶性鹽或街 生物,在賦形劑存在下混合而製得,其可選擇地在辅助 劑存在下(當採用乾燥的混合物在水存在時)進行,並 可選擇性地將產生的混合物進一步轉換成立即可用的形 2.—種顆粒狀組成物,其可藉申請專利範圍第丨項之製法 製付,其中活性化合物對摁寶酸之莫耳比為1 : 0.5 _ 5 〇 -3·根據申請專利範圍第2項的組成物,其特點係在於採用 enrofloxacin的水溶性鹽作為活性化合物。 C請先閱讀背面之注意事項再填寫本頁} 經濟部智慧財產局員工消費合作社印製
Applications Claiming Priority (1)
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DE19633480A DE19633480A1 (de) | 1996-08-20 | 1996-08-20 | Oral applizierbare Formulierungen von Chinolon- und Naphthyridoncarbonsäuren |
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TW086111729A TW518226B (en) | 1996-08-20 | 1997-08-15 | Orally administrable formulations of quinolone- or naphthyridonecarboxylic acids |
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EP (1) | EP0920317B1 (zh) |
JP (1) | JP4338222B2 (zh) |
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CN (1) | CN1113651C (zh) |
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ES (1) | ES2213829T3 (zh) |
HK (1) | HK1022435A1 (zh) |
MY (1) | MY117606A (zh) |
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WO (1) | WO1998007428A1 (zh) |
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KR100365679B1 (ko) * | 2000-04-03 | 2002-12-26 | 주식회사 엘지생명과학 | 기호성이 우수한 엔로프록사신 프리믹스 조성물 및 그제조방법 |
US6518252B2 (en) * | 2000-09-20 | 2003-02-11 | University Of Georgia Research Foundation, Inc. | Method of treating aquatic animals with an antimicrobial agent and chelating agent |
US20020122824A1 (en) * | 2001-01-24 | 2002-09-05 | Francisco Cabrera | Solid phase dispersion of quinolone-or naphthyridonecarboxylic acids |
US6589955B2 (en) | 2001-06-20 | 2003-07-08 | Bristol-Myers Squibb Company | Pediatric formulation of gatifloxacin |
WO2003031443A1 (en) * | 2001-10-04 | 2003-04-17 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Dual actions antibiotics comprising a oxazoldinone and a quinolone or naphthyridinone moiety |
BRPI0407368A (pt) * | 2003-02-10 | 2006-02-14 | Bayer Healthcare Ag | tratamento de doenças bacterianas dos órgãos respiratórios mediante aplicação local e fluor-quinolonas. |
BRPI0409955A (pt) * | 2003-04-30 | 2006-04-25 | Morphochem Ag Komb Chemie | uso de antibióticos hìbridos de oxazolidinona - quinolina para o tratamento de antrax e outras infecções |
DE10328666A1 (de) * | 2003-06-26 | 2005-01-13 | Bayer Healthcare Ag | Tabletten enthaltend Geschmacks-und/oder Aromastoffe |
DE10337191A1 (de) * | 2003-08-13 | 2005-03-17 | Bayer Healthcare Ag | Neue Verwendung von Chinolon-Antibiotika |
DE10340485B4 (de) * | 2003-09-03 | 2015-05-13 | Morphochem AG Aktiengesellschaft für kombinatorische Chemie | Verfahren zur Herstellung von Oxazolidinon-Chinolon Hybriden |
DE10351448A1 (de) * | 2003-11-04 | 2005-06-09 | Bayer Healthcare Ag | Geschmackstoffhaltige Arzneimittelformulierungen mit verbesserten pharmazeutischen Eigenschaften |
US8158797B2 (en) * | 2003-12-18 | 2012-04-17 | Morphochem Aktiengesellschaft Fur Kombinatorische Chemie | Oxazolidinone-quinolone hybrid antibiotics |
KR101176450B1 (ko) | 2003-12-18 | 2012-08-30 | 모르포켐 악티엥게셀샤프트 퓌르 콤비나토리셰 케미 | 옥사졸리디논-퀴놀론 혼성 항생제 |
FR2896416B1 (fr) * | 2006-01-24 | 2010-08-13 | Vetoquinol | Composition anti-infectieuse comprenant un compose de type pyrido (3,2,1-ij)-benzoxadiazine |
CN100360131C (zh) * | 2006-01-24 | 2008-01-09 | 新昌国邦化学工业有限公司 | 一种掩味恩诺沙星的生产方法 |
WO2008151502A1 (fr) * | 2007-06-08 | 2008-12-18 | Hainapharm Pharmaceutical Co., Ltd. Foshan | Formulation de microcapsules d'enrofloxacine et son procédé de préparation |
EP2343089A4 (en) | 2008-09-23 | 2013-05-01 | Jaer S A Lab | USE OF XYLITOL OR DERIVATIVES THEREOF FOR MASKING THE TASTE OF CHEMOTHERAPEUTIC MEDICAMENTS OF THE CHINOLO-N-NAPHTHYRIDONE-CARBOXYLIC ACID GROUP FOR PIG DICULTINATION |
EP2983713A1 (en) * | 2013-04-09 | 2016-02-17 | Cresset Biomolecular Discovery Limited | The treatment of inflammatory disorders |
CN103251552B (zh) * | 2013-05-30 | 2014-12-31 | 成都乾坤动物药业有限公司 | 一种恩诺沙星糊剂及其制备方法 |
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NL266216A (zh) * | 1960-07-12 | |||
GB1174221A (en) * | 1968-01-08 | 1969-12-17 | Ici Ltd | Acid-addition Salts of Tetramisole |
CH524372A (de) * | 1969-01-29 | 1972-06-30 | Ciba Geigy Ag | Verfahren zur Herstellung von stabilen Elixieren, welche therapeutisch verwendbare tricyclische basische Wirkstoffe in Form ihrer Mononatriumpamoate enthalten |
DE3525335A1 (de) * | 1985-07-16 | 1987-01-22 | Bayer Ag | Embonate von chinoloncarbonsaeuren und ihren derivaten |
JPS62192321A (ja) * | 1986-02-19 | 1987-08-22 | Bayer Japan Kk | 魚類用抗菌剤 |
US5281596A (en) * | 1986-02-19 | 1994-01-25 | Bayer Aktiengesellschaft | Antibacterial drugs for fish |
DE3719764A1 (de) * | 1987-06-13 | 1988-12-22 | Bayer Ag | Ionenaustauscherharze beladen mit chinoloncarbonsaeurederivaten, ihre herstellung und verwendung |
US5232919A (en) * | 1987-11-13 | 1993-08-03 | Asta Pharma Aktiengesellschaft | Azelastine embonate and compositions which contain it |
DE4032560A1 (de) * | 1990-10-13 | 1992-04-16 | Bayer Ag | 7-(2,7-diazabicyclo(3.3.0)octyl)-3-chinolon- und -naphtyridoncarbonsaeure-derivate |
-
1996
- 1996-08-20 DE DE19633480A patent/DE19633480A1/de not_active Withdrawn
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- 1997-08-07 BR BRPI9711338-7A patent/BR9711338B1/pt not_active IP Right Cessation
- 1997-08-07 DK DK97936690T patent/DK0920317T3/da active
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Also Published As
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WO1998007428A1 (de) | 1998-02-26 |
US5808076A (en) | 1998-09-15 |
CN1228023A (zh) | 1999-09-08 |
EP0920317B1 (de) | 2004-03-03 |
HK1022435A1 (en) | 2000-08-11 |
BR9711338B1 (pt) | 2009-01-13 |
CN1113651C (zh) | 2003-07-09 |
KR20000068070A (ko) | 2000-11-25 |
CA2263584A1 (en) | 1998-02-26 |
DK0920317T3 (da) | 2004-07-05 |
MY117606A (en) | 2004-07-31 |
JP4338222B2 (ja) | 2009-10-07 |
AU3942797A (en) | 1998-03-06 |
JP2000516239A (ja) | 2000-12-05 |
EP0920317A1 (de) | 1999-06-09 |
KR100493577B1 (ko) | 2005-06-10 |
AR008304A1 (es) | 1999-12-29 |
DE19633480A1 (de) | 1998-02-26 |
CA2263584C (en) | 2008-12-23 |
BR9711338A (pt) | 1999-08-17 |
DE59711379D1 (de) | 2004-04-08 |
ATE260657T1 (de) | 2004-03-15 |
ES2213829T3 (es) | 2004-09-01 |
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