TWI287987B - Cytokine inhibitor - Google Patents
Cytokine inhibitor Download PDFInfo
- Publication number
- TWI287987B TWI287987B TW090119214A TW90119214A TWI287987B TW I287987 B TWI287987 B TW I287987B TW 090119214 A TW090119214 A TW 090119214A TW 90119214 A TW90119214 A TW 90119214A TW I287987 B TWI287987 B TW I287987B
- Authority
- TW
- Taiwan
- Prior art keywords
- interleukin
- salt
- cargill
- production
- ministry
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract description 6
- 102000004127 Cytokines Human genes 0.000 title 1
- 108090000695 Cytokines Proteins 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- 102000015696 Interleukins Human genes 0.000 claims description 10
- 108010063738 Interleukins Proteins 0.000 claims description 10
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- 230000004054 inflammatory process Effects 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
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- 239000003814 drug Substances 0.000 claims description 3
- 230000017074 necrotic cell death Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000016396 cytokine production Effects 0.000 abstract description 5
- 150000004677 hydrates Chemical class 0.000 abstract description 2
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/495—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
1287987 A7
1287987 A7
經濟部智慧財產局員工消費合作社印製 成為禁忌。 嘉吉氟沙星屬於新型喹啉酮系抗菌劑之一種，對於革 蘭陰性菌、革蘭陽性菌、嫌氣性菌等具有強抗菌作用（參考 曰本專利之特公平8-9597號、ep 230295號）。已往之新型 唾琳酮系抗菌劑，據報告對於巨噬細胞/單核白血球或末稍 淋巴球產生炎症性組織介素有影響（參考Baiiiy等人，Int j
Immunopharmac· 12 卷，31 至 36 頁，1990 年），由於未證實 有抗炎症作用’所以目前並沒有做為抗炎症劑而實際應 用。 本發明之目的在將嘉吉氟沙星，其水合物和鹽類做為 組織介素產生抑制劑而使用。 本發明研究者發現抗菌劑之嘉吉氟沙星能抑制巨噬細 胞之組織介素之產生，更進一步發現對於細菌感染所誘致 之炎症具有專一性之抑制作用，而完成了本發明。 換言之，本發明包括下述項目： (1) 以嘉吉氟沙星，其水合物或鹽類為有效成分之組織 介素產生抑制用醫藥組成物。 (2) 如上述（1)項之醫藥組成物，其中組織介素係腫瘍壞 死因子。 (3) 如上述（1)項之醫藥組成物，其中為起因於組織介素 之炎症之預防和治療劑用途。 (4) 如上述（3)項之醫藥組成物，其中組織介素係腫瘍壞 死因子。 [圖面之簡單說明] - * -------1 訂 IT------1 c請先閱讀背面之注音？事項再填寫本頁) 本紙張尺度適用中國國家標準（CNS)A4規格（210 x 297公釐） 2 312876 1287987 A7 B7 五、發明說明（3 ) (請先閱讀背面之注意事項再填寫本頁) 第1圖示實施例1中，對於由脂多糖（Lip〇-polysaccharide，簡稱LPS)刺激，巨噬細胞生產TNF- α有 關嘉吉氟沙星之抑制效果。 第2圖示實施例2中嘉吉氟沙星等在角膜病例上之效 果。 第3圖示實施例2中嘉吉氟沙星等在結膜病例上之效 [本發明之實施形態] 做為本發明之組織介素產生抑制劑之有效成分使用之 嘉吉氟沙星，其水合物或鹽類，乃係上述日本專利中特公 平8-9597號公報，或歐洲專利中ΕΡ 230295號所記載之周 知物質’可按照該記載方法製造之。所使用之水合物例如 特開平8-176143號或WO 96/19472號公報等所記載之3/2 水合物，又，其鹽類則製藥學上容許之鹽類皆可使用，例 如鹽酸鹽等無機酸鹽、乳酸鹽等之有機酸鹽等。 經 濟 部 智 慧 財 產 局 員 工 消 費 合 作 杜 印 製 本發明之組織介素產生抑制劑，可投與在必須抑制組 織介素產生之溫血動物（例如人、猴、狗、描、諸、兔、鼠 類等之哺乳類動物’以及例如雞、火雞、轉子等之高類） 而抑制其產生組織介素。組織介素在生物體内細胞間相互 作用上扮演必須而不可缺的作用，藉由各 *網路而調節其產生。當其調節功維受到干援：：= 之生產異常時，就會呈現各種病態，例如過敏性症狀、炎 症性症狀、慢性關節風濕症、全身性紅斑症等自我免疫疾 病等。另外，病態的血管新生（例如固型腫瘤、炎症、糖尿 本i張尺度適用中國國家標準（CNS)A4規格⑵G X 297公爱） 3 312876 1287987
1287987 A7
(請先閱讀背面之注意事項再填寫本頁) 等。當做為點眼劑、眼用軟膏、點鼻劑而配方時，例如可 從溶劑（生理食鹽水、純水等）、安定化劑（乙底酸鈉、枸櫞 酸等）、乳化劑（聚乙烯吡咯烷酮等）和乳化基劑（蓖麻籽油 等）、界面活化劑（聚山梨糖醇8〇、聚氧化乙烯硬化蓖麻籽 油等）、保存劑（潔而滅、對_羥基苯甲酸酯類、氣丁醇等）、 緩衝劑（硼酸、硼砂、乙酸鈉、枸櫞酸緩衝劑、磷酸緩衝劑 等）、等滲劑（氯化鈉、甘油、甘露糖醇等）、酸鹼值調節劑 (鹽酸、氳氧化鈉等）、乾膏基劑（凡士林、羊毛脂等）、黏性 劑（羥丙基甲基纖維素、聚乙烯吡咯烷酮、聚乙烯醇等）等 周知化合物中選擇適當者使用。 經濟部智慧財產局員工消費合作社印製 使用本發明之組織介素產生抑制劑時，其用劑量視炎 症症狀或輕重，投與對象，其年齡（或周齡），體重和投與 方法等而異，例如内科領域感染症、呼吸器感染症、尿道 感染症等所伴隨炎症之成人病患以内服劑服用時，每曰1 至3次，每次投與1〇〇至3OOmg為宜。點眼劑而用在成人 病患之結膜炎等時’以嘉吉氟沙星計，含有約〇 〇 1 w/v% 至5.0 w/v%之點眼劑，視病狀每日投與1至8次，每次1 至數滴量，其中以使用約0.05 w/v%至1.0 w/v%之點眼劑 為較佳。 本發明之製劑中，不違反本發明之目的，尚可含有其 他藥效成分。 以下舉製劑例和實施例詳述本發明，但本發明不揭限 在該範圍内。 製劑例1 本紙張尺度適用中國國家標準（CNS)A4規格（210 X 297公釐） 5 312876 1287987 A7 B7 五、發明說明（6 ) 錠劑 嘉吉氟沙星 200mg 乳糖 80mg 澱粉 17mg 硬脂酸鎂 3mg 結晶纖維素 1 Omg 將上述成分做為一錠劑之份量，按照常法製成錠劑。 該錠劑可使用糖衣或薄膜（例如羥丙基甲基纖維素等）包覆 之。 製劑例2 旋劑 嘉吉氟沙星 400mg 結晶纖維素 80mg 低分子經丙基纖維素 30mg 硬脂酸鎂 12mg 羥丙基纖維素 12mg (請先閱讀背面之注意事項再填寫本頁) --------1 ^ · J.-------' 經濟部智慧財產局員工消費合作社印制农 將上述成分做為一錠劑份量之材料，按照常法製成疑 劑。該錠劑可使糖衣和薄膜（例如羥丙基甲基纖維素等）包 覆之。 製劑例3 顆粒劑 嘉吉氟沙星 75mg 甘露糖醇 75mg 澱粉 17mg 本紙張尺度適用中國國家標準（CNS)A4規格（210 X 297公釐） 6 312876 4· I I J - 1287987 A7 經濟部智慧財產局員工消費合作社印製
製劑例 五、發明說明（7 硬脂酸_ 。 3mg 將上述成刀混合均一，按照常法製成顆粒狀。本顆粒 劑在必要時可使用糖衣和薄臈(例如羥丙基甲基織維素等) 包覆之。 f劑例4 注射劑
1 OOOmg 5 OOmg 500mg 3850mg 總量為lOOmL 嘉吉氣沙星 鹽酸 氳氧化納 葡萄糖 注射用蒸餾水 少篁之注射用蒸餾水中加入嘉吉氟沙星和鹽酸並加£ 溶解^加人㈣糖溶解之後，再加人氳氧錢，調整為p] 6.0最後加入注射用蒸餾水使全量成為1〇〇mL而製成注 射劑。 注射劑
1 OOOmg 1 7 5 〇mg 1770mg 總置為1 〇〇mL (請先閱讀背面之注意事項再填寫本頁) 嘉吉氣沙星 乳酸 氫氧化鈉 注射用蒸餾水 少量之注射用蒸顧水中加入嘉吉氟沙星和乳酸，並乂 以溶解，加入氫氧化鈉調整為PH 6.0。最後加入注射用》 顧水’使總量成為1 〇〇mL，而製成注射劑。 本紙張尺度適用中國國家標準（CNS)A4規格⑵G χ 297公爱） 312876 1287987
〇.3g 0.86g 適量 適量 總量為lOOmL A7 B7 五、發明說明u ) 製劑例6 點眼劑 嘉吉氟沙星 氣化納 鹽酸 氫氧化鈉 精製水 加入嘉吉氟沙星和氣化鈉於約80mL之精製水中，並 加以溶解，再加入鹽酸和氫氧化鈉，調整為PH 6 0。最後 加入精製水使總量成為1 〇0mL，而製成點眼劑。 製劑例7 點眼劑 製劑例6中之嘉吉氟沙星和氣化鈉分別改用〇.5g和 0.83g，調節為pH 5·5，和製劑例6同樣調製成點眼劑。 製劑劑8 (請先閱讀背面之注意事項再填寫本頁) 裝--------訂---------^ 經濟部智慧財產局員工消費合作社印製 點眼劑 嘉吉氟沙星 氣化鈉 潔而滅 乙底酸鈉 鹽酸 氫氧化鈉 精製水 加入嘉吉氟沙星 氯化鈉 〇_3g 0.86g O.OOSg O.Olg 適量 適量 總量為lOOmL 潔而滅和乙底酸納於約 本紙張尺度適用中國國家標準（CNS)A4規格（210 x 297公釐） 8 312876
Claims (1)
1287987
申請專利範圍修正本 (93年2月17曰j 1. 一種起因於組織介素之炎症之預防及治療用醫藥組成 物，其特徵為以嘉言氟沙生，其3/2水合物或其鹽類為 有效成分者。 2·如申請專利範圍第1頊之窬藥組成物，其中組織介素係 腫瘍壞死因子者。 經濟部中央標準局員工福利委員會印製 312876(修正版) I紙張尺度適财(21G x 297公釐）
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| GB2400033A (en) * | 2003-03-29 | 2004-10-06 | Secr Defence | Use of fluoroquinolone antibiotics for the treatment of Q fever |
| CN1307995C (zh) * | 2005-10-12 | 2007-04-04 | 周卓和 | 加替沙星滴眼液及其制备方法 |
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| KR20030024866A (ko) | 2003-03-26 |
| WO2002013830A1 (fr) | 2002-02-21 |
| AU2001277725A1 (en) | 2002-02-25 |
| US20030176444A1 (en) | 2003-09-18 |
| CA2419178A1 (en) | 2003-02-13 |
| EP1312364A4 (en) | 2004-05-12 |
| ES2273872T3 (es) | 2007-05-16 |
| DE60124732D1 (de) | 2007-01-04 |
| EP1312364A1 (en) | 2003-05-21 |
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