部分中文甲苯磺酸妥舒沙星处方资料（仅供参考）

英文名：Tosufloxacin Tosilate Hydrate

商标名：OZEX ophthalmic solution

中文名：甲苯磺酸妥舒沙星滴眼液

日文名：オゼックス点眼液０．３％

原研厂家：大冢制药有限公司

药品简介
Ozex（Tosufloxacin Tosilate）是一种氟喹诺酮类抗菌剂，临床用于睑缘炎、泪袋炎、大麦粒肿、结膜炎、睑板腺炎、角膜炎（包括角膜溃疡）、眼周消毒的治疗。
オゼックス点眼液0.3%

药物分类名称

广泛的抗菌眼药水

批准日期：2006年4月

欧文商標名

OZEX ophthalmic solution 

一般名：トスフロキサシントシル酸塩水和物

(Tosufloxacin Tosilate Hydrate)

略号：TFLX (トスフロキサシン)

化学名：7-[3(RS)-3-Aminopyrrolidin-1-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid mono-4-toluenesulfonate monohydrate

構造式：

分子式：C19H15F3N4O3・C7H8O3S・H2O

分子量：594.56

性状：

白色至浅黄色结晶性粉末。 N，N - 易溶于二甲基甲酰胺，略溶于甲醇，在水或乙醇（99.5）几乎不溶。

甲醇溶液（1→100）示出了没有旋光性。

熔点：约254℃（分解）

处理注意事项

●与主滴眼剂混合将1mL该药物和1mL复合药物置于玻璃管中，用混合器混合10秒，观察外观变化。

不相容性有※4 Rinderon眼Tenmimi-滴鼻剂0.1％，Nifuran滴眼液0.1％，Jikurodo滴眼液0.1％，Buronakku滴眼液0.1％，经鼻Rinderon的溶液施加点，RIZABEN滴眼液0.5％，色甘酸钠滴眼液2％，对于谷胱甘肽滴眼液2％，Mydrin中号滴眼液0.4％，适利达眼用溶液0.005％，Timoptol滴眼液0.25％，Timoptol XE滴眼液0.5％，Trusopt滴眼液1％，2％Mikelan滴眼液，Rizumon TG滴眼液0.5％，Furabitan滴眼液0.05％，Rescula滴眼剂0.12％※5

配方无变化Tobrucine眼用溶液0.3％，Zajiten滴眼液0.05％，粘膜眼用溶液0.5％，catarin眼用溶液0.005％，Midrin P滴眼液，sankoba滴眼液0.02％

4：在混合后或在室温下1小时后立即观察到外观变化（不透明）。 推测白浊是由于托西氟沙星和铝离子的柠檬酸盐平衡的影响，这是该药物在其他眼用溶液中通过乙二胺四乙酸，柠檬酸，磷酸等的溶解机理，并且活性成分沉淀。

5：将2mL该药物和2mL复合药物置于玻璃管中并用混合器混合10秒，观察外观变化

药用药理学

1.抗菌作用

托氟沙星的抗菌谱，其是这种药物广泛Oyobi，葡萄球菌属体外，链球菌，肺炎球菌，肠球菌属微杆菌属的革兰氏阳性细菌属或类似物，莫拉氏菌的活性体，克雷伯氏菌属，肠杆菌属，沙雷氏菌属，变形杆菌属，摩根氏Morugani，普罗维登斯菌属，流感嗜血杆菌，流感嗜血杆菌Ejipuchiusu（科赫周菌），假单胞菌属，铜绿假单胞菌，洋葱伯克霍尔德氏菌，寡养单胞（黄单胞菌属）麦芽，表现出对眼部感染，如痤疮丙酸杆菌的致病细菌强的抗微生物活性是革兰氏阴性菌和不动杆菌喜欢厌氧菌。

2.作用机制

作用于DNA促旋酶和拓扑异构酶IV转换细菌DNA的构象，通过抑制DNA的复制，作用杀菌。

3.对实验性眼部感染的治疗效果

针对眼部感染模型中的角膜基质是由接种铜绿假单胞菌或表皮葡萄球菌兔的临床分离物制得，该药物表现出治疗效果。

适应症

指示或效果

<适应性真菌种类>

Tusfloxacin对葡萄球菌，链球菌，链球菌，肠球菌，微球菌，莫拉氏菌，棒状杆菌，克雷伯氏菌，肠杆菌，沙雷氏菌，变形杆菌，摩根氏菌，普罗维登西亚敏感 ，嗜血杆菌·埃及（Koch·Weeks），假单胞菌，假单胞菌，假单胞菌，伯克霍尔德氏菌·Cepacia，Stenotrophomonas（Zanthomonas）·Maltophilia，Acinetobacter，Acne bacterium

<适应症>

睑缘炎，泪囊炎，口腔炎，结膜炎，蜱上皮炎，角膜炎（包括角膜溃疡），眼科围手术期灭菌疗法

用法与用量

每天至少一次，每天三次，适用于成人和儿童。此外，应根据疾病和症状增加剂量。

临床结果

1.疾病的临床效果

表1显示了304名眼外感染患者中该药物的III期和一般临床试验中每种药物的临床效果。

2.适应细菌类型的临床效果

从上述情况分离出的适应性细菌的临床效果如表2所示。

3.在眼科手术期对灭菌疗法的影响

<临床试验>

计划进行眼科手术的患者术前消毒的抗菌效果为47例（消毒率73.4％），待评价对象数，消毒病例数为47例。 每天的滴眼量和滴眼时间为每剂量1滴，每天5次，持续2天。

<营销后>

在眼科手术期的消毒疗法中，术后判断时的抗菌效果为103例（消毒率95.1％），在103名受试者中作为消毒实例的数量进行评价。

包装

滴眼液0.3％： 5mL×5,5mL×10

制造供应商

富山化学工业株式会社

联盟：大冢制药有限公司

完整资料附件：http://www.info.pmda.go.jp/go/pack/1319751Q1020_1_10/

Otsuka Pharmaceutical releases New Quinolone Antimicrobial Eye Drop Ozec Eye Solution 0.3% on May 11

Otsuka Pharmaceutical Co., Ltd. (Head office: Chiyoda-ku, Tokyo, President: Tatsuo Higuchi, TEL: 03-3292-0021) has added a new quinolone antimicrobial ophthalmic solution "Ozox ophthalmic solution 0.3%" (generic name: tosylate tosylate) We will release it from May 11th.

Ozox Ophthalmic Solution 0.3%" is a drug developed for ophthalmic use for ophthalmic use, "Ozex tablet" for oral use New quinolone synthetic antibacterial agent which was created by Toyama Chemical Industry Co., Ltd. since 1990. "Ozox Ophthalmic Solution 0.3%" is a drug that has a broad spectrum of antimicrobial spectrum and strong antimicrobial activity in Gram positive bacteria, negative bacteria and anaerobic bacteria, and has acquired indications for various bacterial outer eye infections.

In addition to adults, clinical trials were conducted for children including newborn babies, and for the first time in Japan the dosage regimen and dose for children were recognized.

"Ozox eye drop 0.3%" is manufactured by Toyama Chemical Industry and sold by Otsuka Pharmaceutical.

Otsuka Pharmaceutical will contribute to the health of the people of the world under the corporate philosophy of "Otsuka - people creating new products for better health worldwide".

<Product features>

1) It has antimicrobial activity against infectious bacteria (Staphylococcus, Streptococcus, Streptococcus, Haemophilus influenzae, Pseudomonas aeruginosa, Acne bacterium) of eye infections.

2) A clinical trial was conducted for children (including infants and newborn babies), the effectiveness and safety were confirmed, and the use and dosage of children were clarified for the first time in Japan as an antibacterial ophthalmic solution.

3) It shows long PAE against Staphylococcus aureus, S. epidermidis, Pseudomonas aeruginosa.

4) Short-time bactericidal action against Staphylococcus aureus, S. epidermidis, Pseudomonas aeruginosa.

5) In the sterilization therapy at the ophthalmic surgery period, the preoperative sterilization rate was 73.4%, and the sterilization rate by the detection bacteria was 86.6%.

6) The side effect rate is 2.42%, the main side effects are 0.97% eye irritation and 0.65% corneal disorder such as punctate keratitis. There are reports of shock and anaphylactoid symptoms as serious side effects.

<Product outline>

Product name Ozex Eye Drop 0.3%

Indication type:

Tusfloxacin sensitive to Staphylococcus, Streptococcus, Streptococcus, Enterococci, Micrococcus, Moraxella, Corynebacterium, Klebsiella, Enterobacter, Serratia, Proteus, Morganella morganii, Providencia , Haemophilus · Egyptius (Koch · Weeks strain), Pseudomonas, Pseudomonas, Pseudomonas, Burkholderia · Cepacia, Stenotrophomonas (Zanthomonas) · Maltophilia, Acinetobacter, Acne bacterium

Indications:

Blepharitis, dacryocystitis, stomatitis, conjunctivitis, tineplateitis, keratitis (including corneal ulcer), ophthalmic perioperative sterilization therapy

Dosage/administration Usually one drop per drop for an adult and a child, three times a day. Incidentally, dosage should be increased according to disease and symptoms.

Usage notes See attached document

Active ingredient Tosufloxacin tosylate

Package 5 × 5, 5 mL × 10

Sales Otsuka Pharmaceutical Co., Ltd.

Manufacturing distributor Toyama Chemical Industry Co., Ltd.