CN103251634A - 磷霉素钠/舒巴坦钠注射剂 - Google Patents
磷霉素钠/舒巴坦钠注射剂 Download PDFInfo
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Abstract
磷霉素钠/舒巴坦钠注射剂,卫生部病原菌耐药监测网显示近年来细菌耐药率不断增加,特别是革兰氏阴性杆菌中的非发酵菌类,耐药率已经超过了50%。细菌耐药性的增长是一个世界性的难题,新抗菌药的研发需要10年以上的时间,明显滞后于细菌耐药率的增长速度。本发明是一种复方制剂,具有广谱抗菌活性,实验室和临床研究结果显示,对现有抗菌素耐药的革兰氏阴性杆菌具有更为明显的抗菌活性,实验室敏感性达到100%,临床细菌清除率达到95%,且溶液状态的复方制剂理化性质稳定。该复方制剂生产工艺简单,容易转化为产品,任何一家合格的制药企业均可生产,预期社会效益和经济效益极高。
Description
技术领域
药品。
背景技术
1.中国细菌耐药率逐年上升。
2010年CHINANET耐药菌监测显示金葡菌和凝固酶阴性葡萄球菌甲氧西林耐药株平均为51.7%和71.6%,肺炎链球菌非脑膜炎株PRSP的检出率较2009年有所上升。部分大肠埃希菌、克雷伯菌属(肺炎克雷伯菌和产酸克雷伯菌)中产ESBLs株分别平均为56.2%和43.6 %。肠杆菌科细菌中产ESBLs株对所测试抗菌药物的耐药率均比非产ESBLs株高。。不动杆菌属(鲍曼不动杆菌占86.80o)对亚胺培南和美罗培南的耐药率分别为57. 1%和58.300。与2009年相比肺炎克雷伯菌和鲍曼不动杆菌中的泛耐药株数显著增多。
卫生部全国细菌耐药监测网 2011 年度非发酵革兰阴性杆菌耐药监测第 1 位为铜绿假单胞菌( 39373株) ,占非发酵革兰阴性菌的 41. 3%,其次为鲍曼不动杆菌,33479 株,占35. 1% 。对铜绿假单胞菌敏感率高于 70% 的药物依次为多粘菌素、阿米卡星、哌拉西林/他唑巴坦、妥布霉素、美罗培南、头孢他啶和哌拉西林。除多粘菌素( 敏感率98. 4%。注:中国没有多粘菌素) 、米诺环素( 敏感率55. 7%) 和阿米卡星( 敏感率52. 8%) 外,鲍曼不动杆菌对其它被测药物敏感率均低于 50%,对碳青霉烯类敏感率在 40% 左右,较 2010 年监测结果下降了约 5%。
结论:细菌耐药性仍呈增长趋势,非发酵革兰阴性杆菌多重耐药已成为世界关注问题,特别是鲍曼不动杆菌,耐药率仍在上升,对感染病人构成严重威胁。
2.新药敏感率逐年下降。
替加环素上市之初,对鲍曼不动杆菌敏感率几达100%,数年后则敏感率不断下降。一项研究表明,127株鲍氏不动杆菌对替加环素和米诺环素的敏感率分别为40.9%、30.7%。(中华医院感染学杂志2012年15期);另一项研究结果100株鲍曼不动杆菌对替加环素的敏感率为57%。(实验与检验医学2010年04期);中山大学附属第三医院住院患者中分离41株多耐药鲍氏不动杆菌,除亚胺培南外,其余11种抗菌药物的非敏感率均大于80%。替加环素的非敏感率为80.4%,敏感率为19.5%。(热带医学杂志2010年11期)。
3.新药研究困难重重。
一类新药研究周期大约15年左右,新药上市速度远不及耐药菌的增长速度。联合用药有一定的优势,但联合用药的方案都是经验之谈,没有实验室证据证明哪个联合更为有效,特别是针对耐药非发酵菌的联合治疗有效性的实验室研究几为空白。通过实验室方法证实联合用药的有效性,并从中找到最佳联合,制成复方制剂,比研制一类新药要简单的多。
发明内容
舒巴坦是一种β内酰胺酶抑制剂,与其他抗菌素配合,治疗产β内酰胺酶致病菌。目前已经上市的复方制剂有头孢哌酮/舒巴坦、哌拉西林/舒巴坦、阿莫西林/舒巴坦、氨苄西林/舒巴坦、头孢噻肟/舒巴坦等。尚没有磷霉素钠/舒巴坦钠的商品上市和已公布的专利申请。
本专利的申请基于严格的实验室和临床研究所得出的结论。筛选出30株泛耐药(包括含酶抑制剂的复方制剂)鲍曼不动杆菌,用磷霉素钠联合舒巴坦、头孢哌酮、哌拉西林、泰能、阿米卡星和左氧氟沙星做体外药敏试验,其中磷霉素钠/舒巴坦敏感性达到100%,其他组合均低于20%。后继的临床观察表明,磷霉素钠联合头胞哌酮舒巴坦及联合哌拉西林舒巴坦细菌清除率达95%,是目前已知抗菌素有效率最高的,而且副作用最小,价格最低。
化学稳定性:FDA和SFDA公布的磷霉素钠和舒巴坦的药品说明书均没有提及磷霉素钠与舒巴坦有配伍禁忌。国内公布的任何常用药品配伍禁忌表中,磷霉素钠与头孢哌酮舒巴坦(配伍禁忌表中没有单列舒巴坦)均没有配伍禁忌。本专利申请前做了简单的配伍稳定性试验:将2克磷霉素钠和2克舒巴坦钠溶于100毫升生理盐水中(超过实际使用浓度1倍),置于室温、室内光线30天,外观无任何变化。本专利药品保存状态的是粉针剂,理论上稳定性会更好。
该复方制剂生产工艺简单,原材料价格低廉,容易转化为产品,任何一家合格的制药企业均可生产,预期社会效益和经济效益极高。
Claims (2)
1.任何剂量比例的磷霉素钠/舒巴坦钠注射剂,包括粉针剂和液态注射剂。
2.任何剂量比例的磷霉素钠注射剂和舒巴坦钠注射剂,单独安瓶同一包装,包括粉针剂和液态注射剂。
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108883062A (zh) * | 2016-03-16 | 2018-11-23 | 阿珀斯托洛斯·吉奥格博洛斯 | 用于非胃肠道的给药的磷霉素制剂 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN101879172A (zh) * | 2010-07-13 | 2010-11-10 | 杨建彬 | 头孢噻呋钠复方制剂 |
WO2012079146A1 (en) * | 2010-10-26 | 2012-06-21 | Oral Delivery Technology Ltd. | Nitric oxide amino acid esters for improving vascular circulation, and prophylaxis or treatment of a condition associated with impaired blood circulation |
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Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN101879172A (zh) * | 2010-07-13 | 2010-11-10 | 杨建彬 | 头孢噻呋钠复方制剂 |
WO2012079146A1 (en) * | 2010-10-26 | 2012-06-21 | Oral Delivery Technology Ltd. | Nitric oxide amino acid esters for improving vascular circulation, and prophylaxis or treatment of a condition associated with impaired blood circulation |
Non-Patent Citations (1)
Title |
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WICHAI SANTIMALEEWORAGUN 等: "IN VITRO ACTIVITY OF COLISTIN OR SULBACTAM IN COMBINATION WITH FOSFOMYCIN OR IMIPENEM AGAINST CLINICAL ISOLATES OF CARBAPENEMRESISTANT ACINETOBACTER BAUMANNII PRODUCING OXA-23 CARBAPENEMASES", 《SOUTHEAST ASIAN J TROP MED PUBLIC HEALTH》 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108883062A (zh) * | 2016-03-16 | 2018-11-23 | 阿珀斯托洛斯·吉奥格博洛斯 | 用于非胃肠道的给药的磷霉素制剂 |
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